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Active Ingredient: Capecitabine.

Xeloda (Capecitabine) is used for treating women with breast cancer that is resistant to other more commonly-used drugs.

Other names for this medication:
Capecitabin, Capecitabina, Capécitabine, Capecitabinum, Categor, Xabine.

The composition of the tablets includes the active ingredient capecitabine.

Additional ingredients: lactose, hypromellose, croscarmellose sodium, hypromellose, magnesium stearate, MCC.

The shell consists of: Opium peach Ys-1-17255-A, talc, titanium dioxide, iron oxide yellow and red.

Release form
Xeloda is produced in the form of coated tablets, packaged in blisters of 10 pieces. Tablets of 150 mg are placed in packs of 6 blisters each, the medication of 500 mg – 12 blisters each. In addition, packaging is possible in bottles of 60 and 120 tablets, respectively.

Pharmachologic effect
For Xeloda is characterized by antitumor action.

Pharmacodynamics and pharmacokinetics
The main substance of the drugcapecitabine, is a derivative of fluoropyrimidine carbamate and oral cytostatic, capable of being activated in the tumor, showing a significant selective cytotoxic effect. In this case, the cytotoxic effect is characteristic of the metabolites of this substance.

Due to the sequential enzymatic biotransformation of capecitabine in 5-FU, increased concentrations of the substance are found, which are found in the tumor, and not in the healthy tissues surrounding it. As a result of a complex mechanism of action, the drug has an effect on harmful cells, inhibiting their further development.
Inside the body, capecitabine undergoes rapid and complete absorption. It is then transformed into metabolites: 5′-deoxy-5-fluorouridine (5′-DFUR) and 5′-deoxy-5-fluorocytidine (5′-DFCT). Eating can reduce the absorption of capecitabine, but does not have a particular effect on metabolites. The maximum concentration is detected after 1.5-3.5 hours.

Metabolism of the drug occurs mainly in the liver, after which the metabolites are formed, which affect the affected areas.

Excretion from the body is carried out in the form of metabolites in the composition of urine, feces and a small part in unchanged form.

Indications for use
As a rule, Xeloda is appointed:
👉in combination therapy with docetaxel metastatic or locally advanced breast cancer, if chemotherapy is ineffective, including a drug from the anthracycline taxan, as well as contraindications to treatment with anthracyclines;
👉for adjuvant treatment of colon cancer;
👉in the treatment of first-line metastatic colorectal cancer, as well as common gastric cancer.

Refrain from taking this drug should:
👉hypersensitivity to capecitabine and other derivatives of fluoropyrimidine, other components of the drug;
👉established dihydropyrimidine dehydrogenase deficiency;
👉simultaneous use of sorivudin, as well as its structural analogues;
👉severe renal failure;
👉lactation, pregnancy;
👉less than 18 years old;
👉incompatibility with other components of combination therapy.

Care must be taken when:
👉age of patients from 60 years;
👉simultaneous treatment with oral anticoagulants.

Side Effects of Xeloda
In the treatment of Xeloda can develop side effects, characterized by great diversity. Usually they are noted in the form of: diarrhea, stomatitis, nausea, vomiting, palm-plantar syndrome, severe fatigue, weakness, lethargy, drowsiness.

Possible development of disorders associated with the activity of the digestive system, the condition of the skin and appendages, nervous, respiratory, musculoskeletal, cardiovascular and other systems.

Deviations in the work of the sense organs, the hematopoietic system, the development of infectious complications, and changes in laboratory parameters are not excluded.

Other side effects include: fever, dehydration, weight loss, lethargy, pain in the back.

Instructions for use Xeloda (method and dosage)
Instructions for use Xeloda indicates that the drug is intended for ingestion, preferably within half an hour after eating the food, drinking water.

With monotherapy for colorectal cancer, colon and breast cancer, the standard daily dosage of the drug is 1250 mg to 2 single dose – in the morning and evening. Treatment is carried out for 3 weeks, then a break for 7 days is taken.

The purpose of the drug in combination therapy requires a special approach, strict consideration of the compatibility of drugs, features of the disease and the patient’s body.

In case of overdose, symptoms may manifest themselves in the form of diarrhea, nausea, vomiting, inflammation of the mucous membrane, bleeding or irritation of the gastrointestinal tract, suppression of bone marrow activity.

In this case, treatment includes therapeutic and supportive procedures, which allow to eliminate clinical symptoms and prevent the development of complications.

Appointment of Xeloda in combination with coumarin anticoagulants, for example: Warfarin and Fenprokumon, can have a negative effect on blood coagulation, causing bleeding.

It is recommended to use caution while treating cytochrome P450 substrates.

Combination with phenytoin can increase its concentration in the blood plasma. Therefore, regular monitoring of blood parameters is required.

Calcium folinate has no significant effect on the pharmacokinetics of capecitabine or metabolites, but an increased toxic effect is not excluded, since its influence on their pharmacodynamics is possible.

Combinations with Sorivudine or its analogs cause clinically significant interactions with metabolites that can cause a fatal increase in the toxicity of fluoropyrimidines. For this reason, it is necessary to take a break of at least 4 weeks between taking these medications.

Storage conditions
Storage of this drug requires a cool place out of the reach of children.

Shelf life
3 years.

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Active Ingredient: Perindopril Erbumine.

💚Aceon is used for treating high blood pressure.

Other names for this medication:
Acertil, Acerycal, Agulan, Aldoc, Apo-perindox, Armix, Asyntilsan, Bionoliprel, Biprel, Bipreterax, Cardipen, Co-prenessa, Co-prestarium, Cobathrow, Coveram, Coverene, Coverex, Coverex-as, Coversum, Covinace, Domanion, Dorover, Indapril, Inopil, Midopril, Noliprel, Pendoril, Pendrex, Percarnil, Perindal, Perindan, Perindo, Perindox, Prenessa, Prenix n, Prestance, Prestarium, Preterax, Prexanil, Prexanil a, Prexum, Prindace, Procaptan, Provinace, Reaptan, Repres plus, Spopress, Stopress, Teraxans, Tertensif kombi, Vectoryl, Vidotin.

👉Indications for use
Indications for use are narrow-profile for a therapeutic hospital due to the specificity of the therapeutic effect of the drug Perindopril:

☞arterial hypertension;
☞chronic heart failure;
☞hypertension of renovascular etiology;
☞prevention of recurrent stroke or stroke after a transient ischemic attack;
☞stable ischemic heart disease.

👉Indications for useComposition

Perindopril in the form of tablets contains:
☞perindopril erbumin (acts as the main active ingredient) – 4 mg;
☞milk sugar (lactose);
☞microcrystalline cellulose (MCC);
☞croscarmellose or primellose sodium;
☞magnesium stearate.

👉Pharmachologic effect
Perindopril is a pharmaceutical product that belongs to the group of angiotensin-converting enzyme inhibitors. Due to the chemical interaction of this catalyst with zinc ions, it is completely inactivated. As a result of such influences, the conversion of angiotensin I to angiotensin II, which has a vasoconstrictor effect, is inhibited (due to the narrowing of the vascular bed, blood pressure rises). Suppression of ACE is accompanied by effects on the kallikrein-kinin system and prostaglandins – their circulating and tissue concentrations increase.

Active metabolites of Perindopril affect the natural hormones of the human body. The production of aldosterone (the result of interaction with the renin-angiotensin-aldosterone system of the kidneys) decreases, the release of norepinephrine from sympathetic nerve endings and the formation of endothelin by the inner layer of the vascular wall are suppressed. All these changes strengthen the hypotensive effect of the pharmaceutical preparation, allowing, as they say, “to attack on all fronts”, which entails a steady decrease in blood pressure.

The drug to some extent has protective properties – Perindopril contributes to the regenerative restoration of the elasticity of large blood vessels of the arterial bed. The mechanism of this pharmaceutical effect lies in reducing the excess amount of collagen occupying the subendothelial layer of the structure. Thus, the great vessels become stronger in the physiological sense and can respond more actively to changes in blood pressure.

The cardiac effects of an ACE inhibitor consist in reducing the pre and post load on the myocardium (the total peripheral vascular resistance and the volume of blood flow decrease), thereby normalizing the work of the muscular organ, increasing its efficiency – the minute volume of blood increases without increasing the heart rate. Peripheral tissues and organs improve their trophism and regional blood flow, which is reflected in the condition of the patient’s entire body undergoing conservative therapy.

If the muscular pump is subject to such pathology as chronic heart failure, then the degree of clinical signs of this nosological unit decreases. Exercise tolerance, on the contrary, is growing rapidly. Clinical studies were conducted using a bicycle ergometric test, which confirmed the reliability of therapeutic effects in the treatment of chronic heart diseases.

👉Pharmacodynamics and pharmacokinetics
The drug is used orally, after which 25 percent of the constituent components are absorbed from the cavity of the gastrointestinal tract. Bioavailability of the drug is 65-70 percent. Interesting and even somewhat unusual is the time to reach maximum plasma concentration. The largest number of inactive substances reaches 1 hour, and the biologically active perindoprilat, the product of the active ingredient exchange in the internal environment of the body (about 20 percent of Perindopril is metabolized to this form), manifests its extreme abilities only 3-4 hours after taking the medicine.

Perindoprilat is able to bind to plasma proteins to an insignificant degree and with angiotensin-converting enzyme (slightly less than 30 percent of the active fraction). The volume of distribution of the free metabolite is 0.2 l / kg. The product exchanges mainly kidneys with a half-life of 3-5 hours. The same part, which is associated with ACE, is deploying extremely slowly, which prolongs the effective half-life to 25 hours. The cumulation of the active substance is not observed (the amount of perindoprilat and its half-life does not change in any way when the drug is taken again).

Active excretion of the active product of metabolism can be slowed down by physiological deterioration of the renal apparatus in elderly people or in chronic heart and kidney failure, therefore strict dose adjustment is required based on the creatine kinase level (constant diagnostic examinations are required during the course of treatment if the patient is in this risk group ). Dialysis clearance is 70 ml per minute.

☞increased individual sensitivity, acquired or inherited intolerance to the constituent components of a pharmaceutical preparation or the whole group of angiotensin-converting enzyme inhibitors;
☞gestation period;
☞lactation or breastfeeding;
☞angioedema of hereditary or idiopathic origin;
☞the drug is not used in pediatric practice (until the age of 18).

Separately, it is worth noting that there are a number of pathological conditions when the use of the drug Perindopril is not completely safe and requires constant diagnostic monitoring of various indicators of the body with the conditions of the hospital. The list consists of such diseases:
☞aortic or mitral stenosis;
☞constrictive pericarditis;
☞severe autoimmune nosological units of the connective tissue (in particular, systemic lupus erythematosus or scleroderma);
☞the presence of a transplanted donor kidney;
☞hypertrophic cardiomyopathy;
☞cerebrovascular diseases;
☞obliterating atherosclerosis or narrowing of the lumen of vessels of other origin (especially the channel feeding the heart muscle);
☞bilateral stenosis of the renal arterioles;
☞moderate or severe renal failure;
☞dehydration and exsiccosis.

👉Side effects
Perindopril is an extremely active pharmaceutical drug, which, in addition to therapeutic effects, is indicated by the frequency of adverse reactions during treatment. It makes up 1-10 percent of all cases of conservative therapy. The side effect of the constituent components can manifest itself in the form of a violation of various body systems:

Digestive tract: nausea, vomiting, indigestion, dry mouth, diarrhea, loss of appetite, cholestatic jaundice, inflammation of the pancreas, intestinal edema.
Since the cardiovascular system: excessive reduction in blood pressure with the development of orthostatic hypotension, arrhythmia, angina, stroke and myocardial infarction.
On the part of the urinary system: reduced functional ability of the kidneys, acute renal failure.
Respiratory organs: dry cough, rhinorrhea, difficulty in inhaling and exhaling, eosinophilic pneumonia, bronchospasm.
On the part of the central nervous system: headache, asthenia, dizziness, fatigue, imbalance of sleep and wakefulness, decreased mood, periodic tinnitus, disorders of the visual apparatus, muscle cramps and paresthesia.
Allergic reactions: pruritus or rash, urticaria, angioedema, erythema multiforme.
From other systems: increased sweating, impaired sexual function.
Changes in laboratory parameters – hypercreatininemia, hypohemoglobinemia, thrombocytopenia, proteinuria, hyperkalemia, hyperuricemia, neutropenia, leukopenia (agranulocytosis), pancytopenia, increased percentage and activity of liver enzymes, hemolytic anemia in the presence of glucose-6-phosphate-6-phospholiphoma-6-phosphorus, and hemolytic anemia, an increase in the percentage ratio and activity of liver enzymes.

👉Perindopril, instructions for use (method and dosage)
Pharmaceutical drug is used orally at a time (once a day). Treatment usually starts with a starting dosage of 1-2 mg per day. Further, depending on the indications for therapy, the instructions for use of Perindopril are somewhat different:

✧in case of congestive heart failure, conservative readjustment is continued with an optimal dosage of 2-4 mg per day;
✧arterial hypertension can be treated with higher amounts of the medication taken, with this pathology 4-8 mg per day is used, the dosage should be increased gradually, within 3-4 weeks;
✧renovascular hypertension is treatable at 2 mg per day;
✧prevention of stroke is carried out according to a special scheme: first, 2 mg per knock for 2 weeks, and then 4 mg per day for the same length of time;
✧therapy of stable coronary heart disease begins with a starting dose of 4 mg per day for 2 weeks, and then the amount of the drug taken increases to 8 mg per day.


There are significant clinical cases of overdose with a pharmaceutical product, which, as a rule, manifests itself in the following list of symptoms:
☞excessive lowering of blood pressure;
☞electrolyte imbalance;
☞renal failure.

There is no specific antagonist for the drug. With this complex of adverse effects of treatment, which accompanies increased plasma concentrations of active components, symptomatic therapy is used. The following medical actions are effective:
☞gastric lavage;
☞horizontal position with a raised lower end to restore blood pressure;
☞the use of enterosorbents;
☞correction of water and electrolyte balance isotonic solution of sodium chloride;
☞atropine in the development of bradycardia;
☞effectively using hemodialysis (use of highly permeable polyacrylonitrile membranes is not recommended);
☞in a particularly severe pathological picture of overdose, implantation of an artificial pacemaker can be used.


Perindopril is an extremely active pharmaceutical product (in this parameter it is even listed in the B list of the International Drug Registry), therefore, it has a long list of interactions of different nature. First of all, it should be noted products that enhance the hypotensive effect of an ACE inhibitor (excessive lowering of blood pressure can lead to orthostatic hypotension or acute cerebrovascular insufficiency):
☞agents used for anesthesia;
☞muscle relaxants;
☞anti hypertensive drugs of any mechanism of action;
☞loop and thiazide diuretics;
☞tricyclic antidepressants;
☞antipsychotic drug group;
☞organic nitrates;
☞non-selective monoamine reuptake inhibitors.
☞Indomethacin may have the opposite effect, that is, a decrease in the hypotensive effect.

Combined use of Perindopril with pharmaceuticals such as potassium-sparing diuretics, digitalis glycosides and potassium-based products (for example, active biological additives) increases the risk of hyperkalemia and all symptoms resulting from this pathological condition.

Separately, it is worth noting the interaction with Nimodipine, since a cardiac rhythm disturbance and an increase in myocardial insufficiency with the combined use of drugs in conservative therapy is clinically important.

Also, patients with diabetes should be cautious, because Perindopril increases the manifestations of the sugar-reducing effect of antidiabetic drugs. Accordingly, there is a risk of hypoglycemia and coma, as its consequences.

👉Storage conditions
Conserve Perindopril should be dry, out of the reach of children, and protected from direct sunlight. The temperature regime of optimal storage should not exceed 25 degrees Celsius.

👉Shelf life
2 years.

👉Special instructions
When using ACE inhibitors and Perindopril in particular, there is a risk of arterial hypotension, headache, dizziness and visual impairment, therefore during the period of conservative treatment it is worth refusing to independently control vehicles or other activities that require increased attention, speed and clarity of motor reactions.

The drug belongs to the pharmaceutical group of angiotensin-converting enzyme inhibitors, so technically all the drugs in this subunit of the classification of antihypertensive drugs can be used as analogues of Perindopril. Most often, with individual contraindications, the therapeutic effect is replaced by the following drugs: Hypernik, Stopress, Noliprel, Prestarium A, Perineva, Prestans.

Separately, it should be noted that Perindopril, due to its breadth of therapeutic effects and pharmacological action, is abundantly used to create combined pharmaceutical preparations. The most popular among this series are:

Perindopril PLUS Indapamide is a drug in which the therapeutic effects of Perindopril are complemented by the diuretic component. The new active component blocks the reabsorption of sodium, chlorine and water ions, selectively suppresses the activity of calcium channels and reduces the total peripheral resistance of blood vessels. A positive feature of this combination of pharmaceutical substances is a well-pronounced hypotensive effect, independent of the position of the body in space and the age of the patient. Also, the action of this drug is not accompanied by reflex tachycardia.
Perindopril Indapamide Richter is an enhanced form of the previous analog. The effect of the drug lasts for 24 hours, and persistent therapeutic effects develop in less than a month of conservative treatment. It should be emphasized that the termination of drug rehabilitation when using this form of medication is not accompanied by withdrawal syndrome, which is sometimes extremely difficult.
Perindopril Arginine is a unique medicine of its kind, because the constituent components of the antihypertensive agent are supplemented with conditionally essential amino acid, the main role of which is to be a source of NO synthase in the process of producing endogenous nitric oxide. The latter is an extremely active mediator of the organism in the pathophysiological sense. In this context, the most important are its vasodilation abilities and the regulating effects on smooth muscle tone. Thus, the hypotensive effect of the drug covers a much wider mechanism of action than Perindopril in its pure form. It should be noted that this drug combination does not prolong the list of side effects of use, since arginine is part of the natural metabolism of the human body.
Amlodipine Perindopril is a pharmaceutical product that includes another slow calcium channel blocker, a dihydropyridine derivative. In addition to the antihypertensive effect, Amlodipine also has an antianginal effect, since, by binding to the dihydropyridine receptors, it reduces the transmembrane current of calcium in smooth muscle cells of the coronary and peripheral beds. This mechanism of action and the consequences of its use put this drug in the first place among the analogues of Perindopril for indications for the treatment of coronary heart disease and angina in particular.
Perindopril-Mik is a Belarusian equivalent of a domestic pharmaceutical product. A key feature of it is the use of Perindopril t-butylamine salt (in the traditional form of the drug, a compound with erbumin is used). Due to this fact, the drug reduces pressor effects on the vascular wall (including adrenergic), which manifests itself as an angioprotective effect. It should also be noted that the therapeutic effects of this combination extend to peripheral tissues to a greater extent – they are sensitized to insulin, and therefore glucose metabolism proceeds with greater intensity.

👉For children
The drug is not used in pediatric practice until the age of 18.

👉With alcohol
While undergoing a course of conservative drug therapy, alcoholic beverages should be completely excluded, since alcohol increases the hypotensive effect of the drug, which can adversely affect the body and lead to serious consequences (sudden loss of consciousness, acute cerebral or coronary circulation insufficiency, and so on).

👉During pregnancy and lactation
Perindopril is contraindicated for use during periods of pregnancy, lactation or breastfeeding.

👉Perindopril Reviews
Messages on pharmaceutical forums unanimously reiterate the positive effect of the drug on blood pressure parameters and the work of the heart as a whole. Such an active active ingredient of Perindopril can cope with serious pathology in a relatively short course of conservative therapy. People who took a pharmaceutical drug speak very well about it, because in addition to the main therapeutic effects, it improves trophism and the delivery of beneficial nutrients to all peripheral tissues and organs, cleans the macro circulatory bed, which can not but affect the overall well-being .

Reviews of doctors about Perindopril confirm the opinion of grateful patients from a professional point of view. However, there are several points that somewhat cloud the opinion of qualified specialists. First of all, this is the frequent development of side effects during the course of Aceondrug treatment, because the incidence of adverse reactions is a catastrophic large 1-10 percent. Of course, the overwhelming majority of adverse effects is stopped quite easily, but this creates an additional burden on the patient’s body and does not always pass without a trace.

Therefore, in therapeutic hospitals, Perindopril is increasingly being replaced by combined pharmaceutical ingredients. So, for example, in combination with argininin, the number of adverse effects of conservative treatment does not increase, and the therapeutic effect, on the contrary, is growing irresistibly.

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⇝Other names for this medication:
Avidart, Duagen, Duodart, Duprost, Dutasterid, Dutasterida, Dutasteridum, Zytefor.

Drug for the treatment of benign prostatic hyperplasia. Dutasteride is a double inhibitor of 5α-reductase. Inhibits the activity of isoenzymes 5α-reductase 1 and 2 types, which are responsible for the conversion of testosterone to 5α-dihydrotestosterone (DHT). Dihydrotestosterone is the main androgen responsible for the hyperplasia of the glandular tissue of the prostate gland.

The maximum effect of dutasteride on the reduction of DHT concentrations is dose-dependent and is observed 1-2 weeks after the start of treatment. After 1 and 2 weeks of dutasterid dosing at a dose of 500 µg / day, the mean values ​​of serum dihydrotestosterone concentrations are reduced by 85% and 90%.


After a single dose of the drug in a dose of 500 µg Cmax of dutasteride in serum is reached within 1-3 hours. Absolute bioavailability is about 60% relative to a 2-hour w / in infusion. Bioavailability of dutasteride does not depend on food intake.


Pharmacokinetic data obtained after a single and repeated intake of dutasteride, indicates a large Vd (300 to 500 liters). Dutasteride has a high degree of binding to plasma proteins (> 99.5%).

With daily intake, the concentration of dutasteride in the serum reaches 65% of the stationary level after 1 month and approximately 90% of this level after 3 months. Stationary concentrations of dutasteride in serum (Css), equal to about 40 ng / ml, are achieved after 6 months of daily intake of 500 μg of this drug. In semen, as in serum, steady-state concentrations of dutasteride are also reached after 6 months. After 52 weeks of treatment, the concentration of dutasteride in semen averaged 3.4 ng / ml (from 0.4 to 14 ng / ml). Approximately 11.5% of dutasteride gets into the semen from blood serum.


In vitro, dutasteride is metabolized by a CYP3A2 isoenzyme to form two small monohydroxylated metabolites; however, it is not affected by the isoenzymes CYP2C9, CYP1A2, CYP2A6, CYP2E1, CYP2C8, CYP2B6, CYP2C19 and CYP2D6. After reaching Css dutasteride, unchanged dutasteride, 3 large metabolites (4′-hydroxydutasteride, 1,2-dihydrodutasteride and 6-hydroxydeasteride) and 2 small metabolites are detected in the serum using the mass spectrometric method.


In humans, dutasteride is extensively metabolized. After ingestion of dutasteride at a daily dose of 500 µg to achieve Css from 1% to 15.4% (on average 5.4%) of the dose taken is excreted through the intestine unchanged. The rest is excreted in the form of 4 large metabolites, constituting 39%, 21%, 7% and 7%, respectively, and 6 small metabolites (each of which accounts for less than 5%).

Traces of unchanged dutasteride (less than 0.1% of the dose) are excreted through the kidneys in humans.

When receiving therapeutic doses of dutasteride, its final T1 / 2 is 3-5 weeks.

Dutasteride is detected in the serum (at concentrations above 0.1 ng / ml) up to 4-6 months after discontinuation.

⇝Linearity / nonlinearity

The pharmacokinetics of dutasteride can be described as a first-order absorption process and two parallel elimination processes, one saturated (that is, dependent on concentration) and one unsaturated (that is, not dependent on concentration). At low serum concentrations (less than 3 ng / ml), dutasteride is rapidly excreted through both elimination processes. After a single dose in doses of 5 mg or less, dutasteride is quickly eliminated from the body and has a short half-life of 3-9 days.

At serum concentrations above 3 ng / ml, the clearance of dutasteride occurs more slowly (0.35–0.58 l / h), mainly by means of a linear, unsaturated elimination process with a final T1 / 2 of 3-5 weeks. At therapeutic concentrations, with a daily intake of 500 µg, slower clearance of dutasteride prevails; total clearance is linear and not dependent on concentration.

⇝Older men

The pharmacokinetics and pharmacodynamics of dutasteride were studied in 36 healthy men aged from 24 to 87 years after taking one dose (5 mg) of this drug. There were no statistically significant differences between different age groups in pharmacokinetic parameters such as AUC and Cmax. There were also no statistically significant differences in the dutasterid T1 / 2 values ​​between the age groups of men 50-69 years and over 70 years, which include most men with benign prostatic hyperplasia.

Between different age groups there were no significant differences in the degree of reduction of DHT levels. These results demonstrate that there is no need to reduce the dose of dutasteride in elderly patients.

The drug can be taken regardless of the meal.

Capsules should be swallowed whole, not chewed and not opened, because the contents of the capsule can cause irritation of the mucous membrane of the oropharynx.

Benign prostatic hyperplasia (BPH)

Adult men (including the elderly) The recommended dose of Avodart is 1 capsule (500 µg) 1 time / day. Capsules should be taken whole.

Although improvement with the use of the drug comes fairly quickly, treatment should be continued for at least 6 months in order to objectively evaluate the therapeutic effect.

For the treatment of BPH, Avodart may be prescribed as monotherapy or in combination with alpha1-blockers.

⇝Special patient groups

When receiving 500 mg / day, the kidneys excrete less than 0.1% of the dose, so there is no need to reduce the dose in patients with impaired renal function.

Currently there are no data on the use of Avodart in patients with impaired liver function. Since dutasteride undergoes intensive metabolism, and its half-life is 3-5 weeks, care must be taken when treating Avodart with patients with impaired liver function.

When prescribing dutasteride up to 40 mg / day once (80 times higher than the therapeutic dose) for 7 days, no significant side effects were noted. When conducting clinical trials, patients received dutasteride at a dose of 5 mg daily for 6 months, while no additional side effects were found to those that were observed while receiving 500 μg of dutasteride.

There is no specific antidote for dutasteride; therefore, if an overdose is suspected, it is sufficient to conduct symptomatic and supportive treatment.

⇝Side effects
The adverse events presented below are listed depending on the anatomical and physiological classification and frequency of occurrence. The frequency of occurrence is determined as follows: very often (≥1 / 10), often (≥1 / 100 and <1/10), infrequently (≥1 / 1000 and <1/100), rarely (≥ 1/10 000 and < 1/1000), very rarely (<1/10 000, including individual cases). Frequency categories were formed on the basis of clinical studies of the drug and post-registration observation.

The frequency of occurrence of adverse events, formed on the basis of post-registration observation

⇝The immune system
– Allergic reactions (including rash, itching, urticaria, localized edema) and angioedema

⇝ From the skin and subcutaneous fat
– alopecia (mainly loss of body hair) or hypertrichosis

⇝Mental disorder
– depressed state

⇝From the reproductive system
– testicular pain, testicular edema

The frequency of occurrence of adverse events, formed on the basis of data from clinical studies (adverse events associated with the use of dutasteride as monotherapy)

– as monotherapy for the treatment and prevention of progression of benign prostatic hyperplasia by reducing its size, relieving symptoms, improving urination, reducing the risk of acute urinary retention and the need for surgery;
– as a combination therapy with alpha1-blockers for the treatment and prevention of progression of benign prostatic hyperplasia by reducing its size, relieving symptoms, improving urination, reducing the risk of acute urinary retention and the need for surgery. The combination of dutasteride and tamsulosin alpha1-blocker was mainly studied.


– hypersensitivity to dutasteride and other components of the drug;
– hypersensitivity to other 5α-reductase inhibitors;
– caution should be prescribed the drug for liver failure;
Avodart is contraindicated for women and children. Precautions should be prescribed the drug for liver failure.

⇝Special instructions
Dutasteride is absorbed through the skin, so women and children should avoid contact with damaged capsules. In case of contact with damaged capsules, it is necessary to immediately wash the corresponding skin area with soap and water.

⇝Liver dysfunction

Currently there are no data on the use of Avodart in patients with impaired liver function. Since dutasteride undergoes intensive metabolism, and its half-life is 3-5 weeks, care must be taken when treating Avodart with patients with impaired liver function.

⇝Heart failure with combined use of dutasteride and tamsulosin

In two 4-year clinical studies, the incidence of heart failure was higher in patients who received the combination of dutasteride and alpha1-blocker, mainly tamsulosin, than in patients who did not receive the combined treatment. In these two studies, the incidence of heart failure remained low (≤ 1%), with some variability between them. But in general, there was no discrepancy in the incidence of side effects from the cardiovascular system. The causal connection between treatment with dutasteride (as monotherapy or in combination with an alpha1-blocker) and the development of heart failure has not been established.

Effect on the detection of prostate-specific antigen (PSA) and prostate cancer (PCa)

Patients need to conduct a digital rectal examination, as well as use other methods of research of the prostate gland, before starting treatment with dutasteride, and periodically repeat them during treatment to rule out the development of prostate cancer.

The information can not be used to replace direct consultation with a doctor or make a decision on the use of medicines.

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Active Ingredient: Sulfamethoxazole Trimethoprim.

Oral suspension: 200 mg sulfamethoxazole + 40 mg trimethoprim – active substances.

Additional ingredients: dispersible cellulose, propyl parahydroxybenzoate, methyl parahydroxybenzoate, polysorbate 80, sorbitol, banana and vanilla flavors, purified water.

Tablets: 800 mg sulfamethoxazole + 160 mg trimethoprim – active substances.

Additional ingredients: sodium glycolate starch, povidone, sodium dokuzat, magnesium stearate.

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Pharmacodynamics and pharmacokinetics
Bactrim and Bactrim Forte are bactericidal combination chemotherapeutic drugs that include the active components sulfamethoxazole and trimethoprim (co-trimoxazole), exhibiting a synergistic effect. The mechanism of action of co-trimoxazole is the blocking of two enzymes, which in microorganisms boost the stages of sequential replication of folinic acid. Due to this, bactericidal effects (in vitro) are observed in concentrations at which the active ingredients separately, exhibit only a bacteriostatic effect.

In addition, the effectiveness of co-trimoxazole is much greater than the effect of a single component in relation to pathogens resistant to it. The antibacterial effect of co-trimoxazole (in vitro) covers many pathogenic gram-positive and gram-negative microorganisms.

After oral administration (inside), co-trimoxazole is rapidly and mostly absorbed in the upper part of the gastrointestinal tract.

In the blood reaches Cmax in a period of time from one hour to four. Keeps antibacterial concentration for 7 hours. One day after taking one dose, a small amount of co-trimoxazole is observed in the plasma. Equilibrium concentration is observed after 2–3 days.

Trimethoprim binds to plasma proteins by 44%, and sulfamethoxazole by 70%.

Biotransformation to inactive metabolites occurs in the liver, through acetylation. Distribution in the body runs evenly, with penetration through histohematogenous barriers. In urine and lungs, the concentration of co-trimoxazole exceeds plasma. In the secrets of the prostate and bronchial; saliva; vaginal discharge; in the interstitial, spinal and middle ear fluids; bile; bones; breast milk; eye mucosa accumulates to a lesser extent.

Both active ingredients have the same elimination rate. T1 / 2 increases depending on age: up to 12 months – 7-8 hours, from year to ten – 5-6 hours, in adults – 10-11 hours. With impaired renal function and in the elderly T1 / 2 increases.

They are mainly excreted by the kidneys in a ratio of 10–30% sulfamethoxazole and 50–70% trimethoprim.

♻Indications for use
Respiratory tract: bronchiectasis, croupous pneumonia, pneumocystic pneumonia, bronchitis (chronic and acute), bronchopneumonia.

Urogenital system: urethritis, pyelitis, cystitis, pyelonephritis, lymphogranuloma venereal, epididymitis, prostatitis, gonorrhea (of both sexes), chancroid, inguinal granuloma.

ENT organs: sinusitis, tonsillitis, otitis media, scarlet fever, laryngitis.

Gastrointestinal tract organs: paratyphoid fever, typhoid fever, cholangitis, salmonello carrier, dysentery, cholera, cholecystitis, gastroenteritis, provoked by the enterotoxic strains of Escherichia coli;

Skin: furunculosis, pyoderma, acne, wound infections;

Others: osteomyelitis (chronic and acute) and other osteoarticular infectious diseases, acute brucellosis, malaria (Plasmodium falciparum), South American blastomycosis, toxoplasmosis (in complex treatment).

▶hypersensitivity to co-trimoxazole, other components, including sulfonamides;
▶liver failure;
▶aplastic anemia;
▶kidney function failure, with CC less than 15 ml / min;
▶B12-deficiency anemia;
▶glucose-6-phosphate dehydrogenase deficiency;
▶lactation and pregnancy;
▶age up to 3 months;
▶pediatric hyperbilirubinemia.

▶thyroid pathology;
▶bronchial asthma;
▶folic acid deficiency.

♻Side effects

Blood formation organs:
➲megaloblastic anemia;

Nervous system:
➲peripheral neuritis;
➲aseptic meningitis.

Gastrointestinal tract:
➲decreased appetite;
➲nausea, passing into vomiting;
➲stomach ache;
➲pseudomembranous enterocolitis;
➲increased transaminase activity of the liver.

Respiratory system:
➲infiltrates of the lungs.

Urinary system:
➲interstitial nephritis;
➲kidney impairment;
➲urea increase;
➲toxic nephropathy with anuria and oliguria.

Musculoskeletal system:

Allergic reactions:
➲exudative erythema multiforme (in particular, Stevens-Johnson syndrome);
➲exfoliative dermatitis;
➲epidermal toxic necrolysis;
➲allergic myocarditis;
➲hyperemia of sclera;


♻ Bactrim, instructions for use (method and dosage)
Suspension Bactrim and Bactrim Forte tablets are taken orally after a meal, the tablets are washed down with water.

Instructions for use Bactrim suspension
Acceptance of Bactrim involves the dosage of the drug by means of a measuring spoon containing 5 ml. Since the age of 12 years, the usual dose of Bactrim is 20 ml in the morning and evening. During long-term therapy, a dose of 10 ml in the morning and 10 ml in the evening is indicated. In severe cases of the disease, it is allowed to take matins and evening doses of 30 ml each.

In the case of acute infections, Bactrim is taken for at least 5 days, or until the time of complete disappearance of symptoms within 2 days. Conducting weekly therapy without signs of improvement in the patient’s condition is a reason for dose adjustment or treatment changes.

In the treatment of soft chancre, Bactrim is prescribed 20 ml twice a day. If there is no healing after 7 days, it is possible to prolong the therapy for the next week. It should be borne in mind that the ineffectiveness of treatment may be associated with resistance of the pathogen.

In the treatment of uncomplicated acute urinary tract infections prescribed to women one-time in the amount of 40-60 ml. Take the suspension is recommended in the evening (at bedtime).

When treating patients undergoing hemodialysis, they take the first normal loading dose of Bactrim, and then proceed to receive half or one third of the usual dose, with a break in a day or two.

In the treatment of pneumonia provoked by Pneumocystis carinii, up to 20 mg of trimethoprim and up to 100 mg of sulfamethoxazole per day per kilogram of body weight are prescribed. Bactrim take two weeks every 6 hours, in equal parts. The maximum dose, with a body weight of 8 kg, is 5 ml and increases by 5 ml for each subsequent 8 kg of weight, respectively. For example, a body weight of 32 kg will require a dose of 20 ml.

In order to prevent pneumonia, provoked by Pneumocystis carinii, patients over the age of 12 years are recommended to take 20 ml of suspension (4 spoons) per day. The children’s daily dose is 150 mg / m2 of trimethoprim and 750 mg / m2 of sulfamethoxazole in two equivalent doses, every week for 3 days in a row. The total dose in 24 hours should not exceed 320 mg of trimethoprim and 1600 mg of sulfamethoxazole.

A newborn from 3 to 5 months is shown morning and evening intake of 2.5 ml of suspension. Children from 6 months to 5 years old morning and evening intake of 5 ml, from 6 to 12 years old morning and evening intake of 10 ml.

In the case of severe infections, the dose can be increased by one and a half times.

With Nocardiosis, it is prescribed in adults 60–80 ml, for 3 months and longer (sometimes up to 1.5 years). The dosage depends on the weight, kidney function, age and severity of the infectious disease.

In case of kidney pathologies of CC 15–30 ml / min, the dose is halved and is not recommended for administration with CC less than 15 ml / min.

♻Instructions for use Bactrim Forte
The usual morning and evening dose for patients after 12 years is 960 mg. When conducting long-term treatment, you can get half of this dose, and in particularly difficult situations, increase the usual dose by one and a half times.

Reception of Bactrim Forte continues for at least 5 days, or until the absence of symptoms within 48 hours. Conducting weekly therapy without signs of improvement in the patient’s condition is a reason for dose adjustment or treatment changes.

In the treatment of soft chancre, 960 mg is prescribed twice a day. If there is no healing after 7 days, it is possible to prolong the therapy for the next week. It should be borne in mind that the ineffectiveness of treatment may be associated with resistance of the pathogen.

In the treatment of uncomplicated acute urinary tract infections, women are prescribed one-time 1920-280 mg. It is recommended to take pills before meals in the evening (at bedtime).

When treating patients undergoing hemodialysis, they take the first normal loading dose of Bactrim Forte, and then proceed to receive half or one third of the usual dose, with a break in a day or two.

In the treatment of pneumonia provoked by Pneumocystis carinii, up to 20 mg of trimethoprim and up to 100 mg of sulfamethoxazole per day in four divided doses are taken, for 2 weeks. The maximum dose, with a body weight of 32 kg, is 960 mg (1 tablet) and increases by 480 mg for every subsequent 16 kg of weight, respectively. For example, a body weight of 48 kg will require a dose of 1440 mg.

In order to prevent pneumonia, provoked by Pneumocystis carinii, patients after the age of 12 years are recommended to take 1 tablet daily (960 mg). Patients under 12 years of age are recommended to take Bactrim suspension.

In Nocardiosis, 3-4 tablets (2880-3840 mg) are prescribed in adulthood for 3 months or longer (sometimes up to 1.5 years). The dosage depends on the weight, kidney function, age and severity of the infectious disease.

In case of kidney pathologies of QA more than 30 ml / min, they take the usual dose of Bactrim Forte, with QC less than 15 ml / min, I do not recommend taking this drug.

♻Is baktrim an antibiotic or not?
Medicines Bactrim and Bactrim Forte are sulfonamides in combination, which, like antibiotics, exhibit an antibacterial effect, but unlike them have a chemical, rather than a natural or semi-synthetic structure. It is due to the combination of sulfamethoxazole and trimethoprim, in relation to susceptible microorganisms, it shows not only a bacteriostatic, but also a bactericidal action, which is not as effective as some antibiotics.

Overdose symptoms manifest as nausea, vomiting, dizziness, intestinal colic, headache, depression, drowsiness, fainting, visual disturbances, confusion, fever, crystalluria and hematuria. Overdose for a long time can lead to leukopenia, thrombocytopenia, jaundice and megaloblastic anemia.

Conduct gastric lavage, internal fluid intake, acidification of urine, in order to enhance the excretion of trimethoprim. Recommended in / m the introduction of 5-15 mg per day of calcium folinata, to eliminate the effects of trimethoprim on the bone marrow. If necessary, conduct hemodialysis.

Bactrim and Bactrim forte, when administered together with indirect anticoagulants, increase their activity and also enhance the effects of Methotrexate and hypoglycemic drugs.

Co-trimoxazole increases the effects of warfarin and phenytoin, as well as reduces the effectiveness of oral contraceptives and tricyclic antidepressants.

Taking Rifampicin affects T1 / 2 trimethoprim in the direction of its reduction.

Diuretics increase the likelihood of thrombocytopenia, and Pyrimethamine, when taken more than 25 mg in 7 days, increases the possibility of megaloblastic anemia.

Combined co-trimoxazole with diuretics and oral hypoglycemic drugs can cause a cross-allergic reaction.

PAS, barbiturates and phenytoin increase the symptoms of folic acid deficiency.

Parallel administration of indomethacin can lead to an increase in the blood concentration of sulfamethoxazole.

Bactrim and Amantadine, when used together, can cause toxic delirium.

When co-trimoxazole is taken, digoxin serum concentration may increase (especially in the elderly).

With co-trimoxazole therapy, dofetilide is contraindicated.

♻Storage conditions
Bactrim – up to 25 ° C.

Bactrim Forte – up to 35 ° C.

♻Shelf life
Bactrim and Bactrim forte, in unopened packaging, can be stored for 5 years.

♻Special instructions
In the event of a skin rash or other side effects of a severe nature, treatment with Bactrim must be canceled.

Patients suffering from asthma and prone to allergic reactions, co-trimoxazole is prescribed with extreme caution.

The duration of therapy with co-trimoxazole should be minimal, especially for patients in old age.

Kidney pathologies require a dose adjustment of Bactrim.

During long-term treatment with Bactrim, there is a need to regularly determine the number of formed elements in the blood. With a significant decrease in the number of any of the elements, therapy should be canceled. Patients with severe hematological pathologies can be prescribed co-trimoxazole only in the most extreme cases.

With kidney failure, folic acid deficiency, hematological changes characteristic of folic acid deficiency can be observed in old age. These changes are compensated by the appointment of folic acid.

In the case of long-term use of co-trimoxazole, especially when kidney failure, regular monitoring of urine composition and kidney function is necessary.

In order to prevent crystalluria, it is necessary to provide the body with a sufficient volume of fluid and to follow an adequate diuresis.

Patients with glucose-6-phosphate dehydrogenase deficiency can be prescribed co-trimoxazole only in minimal doses and for absolute reasons.

With proper diet, trimethoprim, disrupting the exchange of phenylalanine, does not affect patients suffering from phenylketonuria.

The appointment of co-trimoxazole requires extreme caution in diseases of the thyroid gland and porphyria.

Patients whose metabolism is “slow acetylation” are more susceptible to idiosyncrasy to sulfonyl amides.

♻For children
Bactrim and Bactrim Forte are contraindicated for children up to 3 months, at a different age are prescribed according to the recommendations for use.

♻During pregnancy (and lactation)
Co-trimoxazole preparations are contraindicated during lactation and pregnancy.

♻ Reviews Bactrim
Different people who took these drugs, put aside the opposite reviews about Bactrim and Bactrim forte. For some, these drugs have become a great helper; for others, their intake turned out to be only side effects. It is worth noting that co-trimoxazole preparations indeed have many contraindications and a rather significant list of side effects, in connection with which, their purpose is advisable only in the case of reliable indications taking into account the history and reactions of the individual patient.

For children, reviews of Bactrim suspension are also varied and do not provide an opportunity to form an unequivocal opinion about its effectiveness and safety. The only conclusion that can be made by examining parents reviews is that only an experienced doctor should prescribe this drug, after conducting various tests and studies, and only in this case therapy will be effective and relatively safe.

♻ Other names for this medication:
Actrim, Adrenol, Alfatrim, Altavit, Anitrim, Apo-bactotrim, Apo-sulfatrim,  Assepium, Astrim, Avlotrin, Bacin, Bacsul, Bacta, Bactekod, Bactelan, Bacterol, Bacticel, Bactipront, Bactiver, Bactoprim, Bactramin, Bactricid, Bactricida, Bactrimel, Bactrizol, Bactron, Bactropin, Baktar, Baktimol, Bakton, Balkatrin, Balsoprim, Bascul, Berlocid, Betam, Bioprim, Biotrim, Biseptol, Biseptrin, Bismoral, Bitrim, Broncoflam, Bucktrygama, Cadaprim-r,  Cadiprim,  Canibioprim, Casicot, Chemitrim, Chevi-trim, Ciplin, Clotrimazol al, Co-sultrin, Co-trim, Co-trimoxazol, Co-try, Colizole, Comox, Cosat, Cotreich,  Cotribene, Cotrim, Cotrimol, Cotrimox, Cotrimoxazol, Cotrimstada, Cotripharm, Cotrix, Cotrizol-g, Cots, Cozole, Daiphen, Danferane, Deprim,  Dhatrin, Diatrim 24, Dientrin, Diseptyl, Ditrim, Doctrim, Dosulfin,  Dotrim, Droxol, Drylin, Ectaprim, Editrim, Eliprim, Epitrim, Erphatrim, Esbesul, Escoprim, Eusaprim, Exazol, Feedmix ts, Fisat, Forcrim, Gantrisin,  Gentrim, Globaxol, Groprim, Groseptol, Ifitrim, Ikaprim, Infatrim, Infectrim, Infectrin, Irgagen, Jasotrim, Kaftrim, Kanprim, Kemoprim, Kepinol, Kombitrim, Lagatrim, Lapikot, Letus, Licoprima, Linaris, Lupectrin, Medibiot, Megaset, Megatrim, Meprim, Methotrin, Methoxasol, Metoprim, Metoxiprim, Metrim, Momentol, Navatrim, Neoset, Neotrim, Netocur, Nopil, Novidrine, Novo-trimel, Novotrim, Noxaprim, Nu-cotrimox, Nufaprim,  Octrim,  Omsat, Onetrim, Organosol, Oribact, Oriprim, Ottoprim, Pehatrim, Pharex co-trimoxazole, Plocanmad, Politrim, Primadex, Primazol,  Primazole,  Primotren, Primsulfon, Purbac, Qiftrim, Regtin, Resprim, Ribatrim, Roxtrim, Sanprima, Sepmax, Septra, Septran, Septrin, Servitrim, Shatrim, Sigaprim, Sinatrim, Sinersul, Sitrim, Soltrim, Spectrem, Suftrex, Sulbron, Sulfa, Sulfagrand, Sulfamethoxazol, Sulfaméthoxazole, Sulfamethoxazolum, Sulfametoxazol, Sulfatalpin, Sulfatrim, Sulfoid, Sulfoprima, Sulmetrim, Sulotrim, Sulphatrim, Sulphax, Sulphytrim, Sulprim, Sultri-c, Sultrian, Sultrim,  Sultrima, Sumetoprin, Sumetrolim, Sunatrim, Suprasulf, Supreme, Suprim, Suprimass, Sutrim, Tabrol, Tagremin, Terasul-f, Terbosulfa,  Theraprim,  Tmps, Trelibec, Trifen, Triforam, Trim sulfa, Trima-kel, Trimaxazole,  Trimecor, Trimesulf, Trimesulfin, Trimethazol, Trimethox, Trimetoger, Trimetoprim sulfa, Trimexazol, Trimexole-f, Trimezol, Trimidar-m, Trimoks, Trimol, Trimosazol, Trimosul, Trimoxsul, Trimsulint, Tripur, Trisolvat, Trisul, Trisulf, Trisulfose, Trisulin, Tritenk, Trizole, Two-septol, Urisept, Urobactrim, Vanadyl, Vanasulf, Wiatrim, Xepaprim, Yen kuang, Zaxol, Zoltrim.
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Analogs of Dapoxetine

Other names for this medication :
Aczone, Dapoxetin, Dapoxetina, Dapoxetine hydrochloride,  Dapoxetinum, Dapsone, Everlast, Priligy .


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In this article, you can read the instructions for use of the drug Priligy. Presented are reviews of visitors to the site – consumers of this medication, as well as opinions of doctors specialists on the use of Dapoxetine in their practice.

A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation.

Analogues or generics of Dapoxetine in the presence of existing structural analogues.

Use to treat premature ejaculation in men and enhance potency. Composition and interaction of the drug with alcohol.

Method of application (dosage)
A day drink on the pill, drinking plenty. The best effect is achieved when taking a couple of hours before sexual intercourse. The maximum daily dose is 60 mg.
During therapy, refusal of alcohol is required. The pressure on the vessels and heart is increased, special vigilance should be shown. In addition, Dapoxetine does not relieve the risk of contracting sexually transmitted diseases.
You can not use it simultaneously with thioridazine, tramadol, antidepressants, as well as with lithium, monoamine oxidase inhibitors, sedatives. Plus with nelfinavir, tryptophan, many medicinal doses, ketoconazole, telithromycin, as well as ritonavir, itraconazole.

The effect of Dapoxetine

The main active component of the drug is Dapoxetine hydrochloride. In addition, Priligy contains auxiliary substances that enhance the medicinal properties of the drug and minimize the likelihood of side effects.

Under the influence of the drug there is a blockage of serotonin, which allows:
➢ delay the process of ejaculation;
➢ prolong the sexual intercourse several times.

Dapoxetine with alcohol

Dapoksetin is not recommended for taking in combination with alcoholic beverages. Ethanol, which is part of any alcohol, disrupts the effectiveness of the drug Dapoxetine and significantly slows the appearance of the result.
Moreover, in some cases, this combination can cause serious and dangerous poisoning. Experts insist on complete refusal of alcohol during the period of taking the drug.

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Other names for this medication :
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Modafinil is a prescription drug for patients with narcolepsy, increases concentration of attention and relieves drowsiness, also enhances the perception and memory capacity. Modafinil as a biologically active additive takes an honorable place among nootropic drugs. Modafinil is a drug that relieves sleepiness in the daytime and for the treatment of narcolepsy. It is possible to improve perception by stimulating neurotransmitters in the brain, used to improve mental abilities.

Provigil or benzhydryl sulfinylacetamide is a central stimulant (psychostimulant). The substance has been approved by the FDA for the treatment of narcolepsy (a disease characterized by sudden and uncontrolled bouts of deep sleep, fatigue or excessive drowsiness), sleep apnea, and sleep disorders caused by changes in the mode of operation.
The quality of the drug was tested, including, as a remedy for the treatment of Alzheimer’s disease, depression and attention deficit disorder. Modafinil belongs to a group of drugs known as eugeroics (stimulants) that promote mental alertness and attention.
One of the known mechanisms of action of these drugs is the agonism of alpha-1-adrenergic receptors, as a result of which drugs affect the mood, increasing energy by increasing the release of dopamine in the central nervous system. This also leads to changes in the levels of GABA and glutamate. In studies of modafinil as a stimulant, the advantages of the drug were shown in comparison with amphetamines.
To begin with, the substance is supposed to have a much lower potential for abuse due to the fact that its effect does not cause the same euphoria. In addition, the drug has a lesser effect on peripheral CNS stimulation (that is, it shows fewer side effects), has minimal effect on blood pressure, does not cause sleep interruptions (no hangover or need to catch up on sleep), and, according to clinical trials, has a more reliable security profile.
The drug is used even by the US military as an energy stimulant for pilots and soldiers needed to work for long periods of time without sleep. This is not so strange as it may seem at first glance, since in the past military pilots and soldiers widely used dexedrine (amphetamine) during long periods of lack of sleep.
Provigil has been tested in recent combat situations, such as Afghanistan and Iraq, and may in the future be officially recognized as a special preparation for the military.

Recently, modafinil has gained popularity among competitive athletes. They use it not just as a medicine for “vivacity”, but as a stimulant, increasing productivity and endurance. This use is likely to be a surprise to the developers of this drug, as previously it was reported that this “gently” vigilant drug does not have strong stimulatory effects, and can not improve athletic performance.
Recent research contradicts these statements. A study in Canada showed that taking Provigil can provide significant sports benefits. In a double-blind study, 15 male volunteers took the drug at a dose of 4 mg per kg of body weight (equivalent to 200 mg for a person weighing 220 pounds), or a placebo.
Three hours after the meal, aerobic exercises were performed on the veloergometer at 85% of the maximum aerobic capacity, until exhaustion. Taking Provigil, men could exercise for significantly longer periods of time (up to 30% longer), and used more inhaled oxygen for exercise. Also reported was a decrease in subjectively perceived tension, resulting in increased productivity during training.

Provigil was developed by Lafon Laboratories in France. In 1998, the drug was approved by the FDA for sale in the United States, where it was sold under the brand name Provigil.
Provigil also occurs in the international market under this and several other trade names, including Modiodal, Vigil, Alertec and Modasomil. Although the drug has favorable safety indicators, in the United States for some time it was considered a drug capable of provoking possible abuses.
Currently, Provigil is on the list of IV controlled substances, along with Valium and Xanax. Thus, its use for non-medical purposes is limited by significant legal sanctions for possession and import of the drug. The drug has a fairly wide medical use, including sleep disorders associated with changes in the mode of operation.
The drug is often prescribed by prescription. In 2000-2004, Modafinil became popular among competitive athletes, before sports authorities did not begin to worry about the use of the drug. In 2004, a doping scandal erupted in connection with the company Valco, when it became known that many of the athletes who gave a positive result for the use of tetrahydrogestrenone, also used Provigil.
After this, the IOC prohibits the use of Modafinil, and a number of studies have developed a methodology for detecting this chemical in the urine. Now this testing is part of the standard survey of athletes before the Olympic Games. Most other international sports bodies have followed the example of the IOC to ban and test Modafinil.
Since then, the drug has lost its appeal as “invisible” in checks, although it is still used by many athletes who do not undergo random urine testing.

How Supplied
Provigil is most often supplied in the form of tablets of 100 mg and 200 mg each.

How to use?
The drug “Modafinil“, the instruction to which must necessarily be attached, should be prescribed only by a doctor. The doctor also prescribes the necessary dose for a particular patient. Usually the specialist prescribes 2-4 tablets per day. The drug should be taken in the morning and at lunch.
If a patient has arterial hypertension, then during treatment with Medafinil medication, the price of which will be indicated below, he needs to control blood pressure. If the patient has liver function, then the dose is reduced to 0.1-0.2 g per day.

Blood serum
The half-life of modafinil is 13-15 hours, and the concentration in the serum in the equilibrium state reaches 2 days after the onset of admission. The half-life of the S-isomer of modafinil is 4-5 hours, whereas in the R-isomer of modafinil, the period is longer (15 hours) and thus the intake of armodafinil is almost equivalent to taking Provigil.
The results of the experiments showed that the concentration of ardomafinil in the blood is 18% higher than in the case of modafinil (5.44 +/- 1.64 mg / ml versus 4.61 +/- 0.73 mg / ml) and accumulates in a shorter time interval (1.8 hours against 2.5 hours), and the total concentration of ardomafinil in the urine is higher by 32-40%.
Although both variants of modafinil (modafinil and armomafinil) have the same half-life, the effect of armomofinil on the body is more pronounced (according to the content in the urine and blood).

According to the immunocytochemistry data of the c-Fos gene (the gene responsible for the stimulation response and detected by neural stimulation or sleep deprivation), the introduction of modafinil to cats caused a sharp activation of the c-Fos gene in the anterior hypothalamic nucleus and adjacent areas and was weak in the suprachiasmatic nucleus and minimal activation of the gene in other areas, for example, in the cerebral cortex or striatum.
Such a pinpoint activation of the hypothalamus was noticeable everywhere, and amygdala was involved in the process. Studies in humans showed clear differences between the effects on humans of modafinil and amphetamine.

In contrast to the effects of amphetamine or methylphenidate – excessive vivacity (which indicates a widespread neuronal activation), modafinil also acts selectively: the hypothalamus and amygdala.

Dopaminergic effect
Provigil is able to increase extracellular levels of dopamine in the prefrontal cortex in rats and in the caudate nucleus in dogs.
Modafinil acted on dopamine and noradrenaline receptors (in the striatum), and the absence of such an effect in mice was associated with the disappearance of the effects associated with sleep, which was confirmed by the fact that the Provigil exposure mechanism does affect sleep.
Recent studies have shown an insufficient effect of modafinil on dopaminergic systems, which may be due to a lower dosage used previously.

Andrenergic effect
The invigorating effect of modafinil is significantly weakened by antagonists of adrenergic receptors (alpha and beta subunit), however, inhibition of catecholamine synthesis by α-methylparathyrosine does not reduce the effect.

Orexinergic effects
In people with deficiency of orexin (nalotics) modafinil shows good results, directly affecting orexin neurons. This effect has had the greatest effect on mice with deficiency, the effect of modafinil on the orexin system of healthy individuals and humans is unknown. 3.5.
Sedative and stimulatory effects The results of some studies are negative for the effects of modafinil during intentional sleep deprivation, since the effect of 300 mg of Provigil during sleep deprivation is equivalent to taking 20 mg of D-amphetamine.
However, it was noted that the deterioration of self-control (the ability to accurately assess yourself and your environment) changes toward excessive self-confidence (an incorrect assessment of what is really capable of). These studies continued for 64 hours (two nights without sleep) with a single dose of Provigil every 15 hours.
Taking modafinil before going to bed can seriously change the sleep cycle and lead to subsequent lethargy, and can also cause side effects (worsening of mood and mental abilities). Recurrent hypersomnia is a phenomenon in which, after the end of the action of drugs against drowsiness, it tends to sleep even more than before they are taken.
Unlike amphetamine-based drugs, modafinil does not cause this phenomenon in cats, rats and mice. People who did not sleep for 64 hours and took modafinil, this phenomenon is also not seen, in contrast to the results when taking D-amphetamine. Provigil does not cause recurrent hypersomnia. Exacerbation of attention is observed with sleep deprivation for 10-12 hours after a single intake of 300 mg of modafinil, which is equivalent to 20 mg of D-amphetamine.
The dose of Provigil 300 mg from drowsiness is equivalent to a 20 mg dose of D-amphetamine. The brain cycle of sleep is the balance of the “ascending activating system”, consisting of activating neurotransmitters (catecholamines, acetylcholine, nuts, etc.) and neurotransmitters (GABA, galanin), which suppress stimulation and contribute to falling asleep. Changing levels of activation and suppression of neurotransmitters forms a kind of cycle “switch-on-switch”.
In general, the regulation of the cycle of vivacity and rest depends, on the one hand, on the daily biorhythm caused by the suprachiasimatic nucleus, and on the other hand, on the homeostatic need for sleep that occurs during wakefulness. Provigil is able to contact with various stimulant systems, including serotonergic, noradrenergic, dopaminergic, glutaminergic, histaminergic, oroxynergic and GABAergic pathways of metabolism.
During some studies, Provigil was used in the treatment of a number of other diseases, and it was found that the side effect of insomnia lasted longer than in the placebo group, and that modafinil taken at bedtime did not let the experiment participants fall asleep. The use of modafinil promotes mental stress.

Memory and thought processes
In healthy people, when taking 100-200 mg of Provigil 2 hours before the test (arithmetic test), the memory properties, spatial-visual planning and reaction rate were improved. Short-term memory and accuracy of information processing improved after taking 200 mg of modafinil. In addition to the above, improvements are observed when performing the task as a whole – increasing motivation, enjoying the work done.
In methamphetamine-dependent cognitive impairments, the dose of Provigil in 400 grams, broken down for 3 days, is able to improve the properties of short-term memory, which was previously not possible, but a single dose of 200 mg modafinil is not capable of causing such an effect.

Impact on the appetite
Researchers who condemn the drug, sometimes report a violation of appetite as a side effect in 16% (164 people). Some researchers consider this fact the cause of weight loss within a week, however, statistically.

Provigil is unable to activate the neural pathways of metabolism, which occurs with dependence, and therefore it is believed that the drug has a low threshold of habituation with respect to other similar drugs. It is unlikely that modafinil will be used as a drug in the environment of drug addicts.
Provigil is able to help alleviate the breakdown in methamphetamine-dependent, alcoholics and gamers, but the effect of exposure varies. Provigil also reduces the impulsivity of the dependent, but this effect only affects the subjects whose impulse threshold before the experiments was already low.

>>> The effect of the drug on people with certain diseases <<<

Multiple sclerosis
One-time administration of ardomofinil (250 mg) in patients with multiple sclerosis showed improved mnemonic reproduction, the effect was comparable to the placebo effect, but the fatigue, the ability to focus and the processing speed of the information did not affect the drug in any way.

Precautionary measures. Toxicology
The tests revealed the following adverse effects of the drug – headache, dizziness, diuresis, heart palpitations, tachycardia, anxiety, nervousness, gastrointestinal problems such as nausea, and dry mouth and abdominal pain. Apart from the above, Provigil is considered a well tolerated drug.
Common side effects of modafinil include insomnia and decreased appetite.

Provigil side effects
Side effects Provigil, as a rule, associated with stimulation of the central nervous system and may include nervousness, insomnia, trembling, euphoria, personality changes and arousal. The drug can also cause gastrointestinal disorders such as nausea, vomiting, abdominal pain, dry mouth, anorexia and headache.
Hypertension, heart palpitations or abnormal heart rhythms may also occur.
In rare cases, an allergic rash, an increase in alkaline phosphatase or a disorder in voluntary movements may occur.

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This tool, in addition to the powerful formula of the Sildenafil already familiar to you, also contains a whole complex of medicinal herbs that are synergists of sildenafil, which in the end provides not only a more prolonged intimate contact, but also works much more efficiently than Sildenafil in a standard dosage.

As soon as the cavernous bodies of the penis are filled with blood, immediately the penis grows in size and becomes firm, so the usual mechanism of erection occurs. In order for the blood flow to go directly to the penis, sexual stimulation is needed, then the internal humoral factors of the organism come into play, namely, the cyclic hyanosine monophosphate or CGMP is involved. It is produced under the action of nitric oxide and is the key point of the appearance of a long and quality erection.

CGMP completely controls the amount and force of blood flow to the reproductive system, as well as controls its outflow, so the action of sildenafil is aimed at increasing CGMP by blocking another active enzyme PDE5, which contributes to the destruction of CGMP. It is Sildenafil and medicinal herbs that are part of the Sildenafil Super Active actively prevent the decomposition of CGMP into fractions, contribute to its accumulation in the body and, accordingly, a longer erection.

Sildenafil capsules is a new generation drug, it is provided with a more productive formula capable of more effectively solving male problems associated with potency. Active medicinal herbs safely enhance the positive effect of the drug, allowing you to help even in the most difficult situations associated with violations of erectile dysfunction.

Advice to a doctor before using Fildena Super Active 100 mg is necessary, especially if the use of the drug occurs for the first time. It is necessary to evaluate the possibilities of your body and the compatibility of sildenafil and medicinal herbs that are part of the Fildena Active Super Active 100mg and the drugs you use for other diseases.

Possible restrictions on taking the drug:
☞ Any manifestations of allergic reactions to the ingredients of the product;
☞ Limitations to physical and sexual loads;
The intake of nitrate preparations in any form is incompatible with the use ☞ of Fildena Super Active 100 mg;
☞ With a predisposition to bleeding;
At the expressed infringements of work of internal organs.
Use capsules once a day at a daily dosage of 100 mg. It should be noted that the capsules are much faster than tablets, so use Sildenafil in capsules, not for 40-50 minutes, as happens when taking a standard tablet form, but 20-25 minutes before sexual intercourse. Medicinal herbs that are part of the drug even more contribute to the rapid onset of a positive effect, so the drug Sildenafil capsules is productive in the most difficult situations.

The main advantages of the Fildena Super Active 100 mg (capsules):
☞ Capsules contribute to a faster onset of a positive result, which is especially useful for unplanned sexual intercourse;
☞ Active substance Sildenafil in combination with herbs, enhancing its effect, provides potent potency for a longer period;
☞ Medicinal herbs help quickly cope with stressful situations, increasing vitality;
☞ Stimulate spermatogenesis.
When using Fildena Super Active at a dosage of 100 mg, negative effects are observed in about 15% of cases. This percentage can be greatly increased if you take the drug in combination with alcohol or exceed the daily dosage equal to 100 mg, so the use of the Fildena Active Super Active should not be accompanied by potentially dangerous actions, for example, driving the car until you know exactly how the drug acts individually on you.

Dizziness or even loss of consciousness can occur when consuming hot drinks, being in the heat or at elevated body temperature. Once you feel bad, you should sit or lie down, in case the symptoms become worse, you need to seek medical help.

Other frequent side effects will be redness of the face and neck area, due to a sharp flow of blood to the face area. Also, one in seven patients observes the inability to distinguish between blue and green colors, as well as dyspepsia. In general, with strict adherence to dosage, the drug is well tolerated without causing side effects, especially with repeated administration.

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Active Ingredient: Vardenafil

Other names for this medication:
Vardenafilum, Vivanza

Levitra is an effective medicine for improving erection in men
For the treatment of impotence, preparations containing type 5 phosphodiesterase inhibitors are popular. A vivid example is a remedy based on the composition of vardenafil, Levitra. Instructions for use are mandatory for reading before starting therapy. Since there are contraindications and peculiarities of combinations with other medicines.

The main active component is vardenafil, which increases vascular clearance and increases blood flow in the capillaries of the genital organ.

Excipients consisting of:
♂ Crospovidone;
♂ Magnesium stearate;
♂ ICC;
♂ Silica.
Red and yellow iron oxide, macrogol 400, hypromellose, and titanium dioxide were used for the film shell.

How does Levitra work on the potency and erection?
Levitra is recommended for erectile dysfunction, when it is impossible to have a normal sexual intercourse, or if premature ejaculation is observed.

Erectile dysfunction is mostly fixed due to poor blood flow in the pelvic area. Vardenafil blocks the action of enzymes that contribute to this. When there is sexual arousal, the brain gives certain signals, as a result of which, with good circulation, the cavernous bodies of the penis become full and a hard erection appears.

It is important to remember that only intensive erotic stimulation starts the mechanism of Levitra‘s work. The use of the drug also allows prolonging sexual intercourse – the manufacturer reports that the active substances of tablets slow the processes of ejection of seminal fluid.

Form release and dosage
Pharmaceutical companies produce medicament in tablet form. Color – orange, each pill is covered with a film sheath. The package may contain a different concentration of the main component.

In pharmacy chains, Levitra is presented in various dosages. The concentration of 5, 10 and 20 mg is more common. Less often – 40 and 60. Packaging – packs of cardboard, containing blisters with 1 and 4 pills.

Dispersible tablets, which dissolve rapidly in the oral cavity, are sold at an active substance concentration of 10 mg.

How to use?
Levitra should be taken after consultation with your doctor. It is important to adjust the dosage, depending on the age, the characteristics of the disease and the effect of possible medications that Levitra should combine.

Exceeding the prescribed dose of DPE 5 inhibitors provokes side effects, therefore it is important to strictly follow the recommendations contained in the instructions:

♂ The medication is not associated with the time of the main meals;
♂ The initial dose at the beginning of the course is 10 mg;
♂ You need to drink tablets no later than half an hour before intimacy;
♂ The drug should be consumed once a day (maximum), since the body must rest from the impact of potent substances;
♂ For men with diabetes or who undergo surgery on the prostate, the recommended dose is increased to 20 mg;
♂ Patients older than 60 years are often only half the standard rate – 5 mg;
♂ The maximum allowable amount of vardenafil per day is 40 mg;
Levitra is not combined with grapefruit and juice of this fruit – their properties reduce the effectiveness of active ingredients;
♂ In the case of kidney and liver pathologies or with the administration of ketoconazole, Erythromycin and analogues, the dose is selected individually for each patient, the use is permissible only under constant medical supervision.

Time of action
According to real reviews, the time of action of the drug is from 5 to 12 hours, so, despite the recommendations to drink a pill 30 minutes before the start of intimacy, if necessary, allow the drug intake in advance.

If you take Levitra tablets before meals – the absorption of active ingredients into the blood will occur in a quarter of an hour. If you drink the product on a full stomach, then it will fully operate in about an hour. Initial signs of erection can be observed after 10 minutes for men with mild erectile dysfunction. In other cases it will take about half an hour.

Levitra and alcohol: compatibility

In the memo attached to the drug, it is indicated that it is acceptable to combine with alcoholic beverages, however, in these cases, the load on the liver is doubled. First of all, alcohol is processed, and only then the drug.

These features should be remembered when a supper with wine is expected. Levitra and alcohol in combination with each other often have the following consequences:

♂ Excitation will be weaker, an erection will come much later. A delay of up to several hours is possible;
♂ It is not excluded the occurrence of symptoms of drug overdose.

Side effects and contraindications
In some cases it is recommended to stop using Levitra. Contraindications for admission are as follows:
♂ Vascular and cardiac muscle pathologies;
♂ Disorders of amino acid metabolism;
♂ Postponed diseases requiring sexual rest, for example, heart attack or stroke;
♂ Combination with medicines containing nitrates, and directed to HIV treatment;
♂ Combination with similar means aimed at improving erection;
♂ Peptic ulcer disease;
♂ Congenital deformity of the penis;
♂ Predisposition to frequent bleeding;
♂ Diseases of the eye retina;
♂ Hypersensitivity to the components of tablets;
♂ Adolescence.

When the recommended dosage is observed, the course of treatment with the drug usually does not cause side effects. Even cases when taking a drug in the amount of 40 mg per day did not provoke negative consequences, however, the excess of the norm in 20 mg often leads to the appearance of the following symptoms:
♂ Headache, stomach and lumbar pain;
♂ Vertigo;
♂ Feeling of nausea;
♂ Soreness in erection;
♂ Irritation of the nasal mucosa;
♂ A sudden rush of blood to the cheeks and neck;
♂ Increased sweating;
♂ Sharp changes in blood pressure;
♂ Attacks of tachycardia;
♂ The onset of edema;
♂ Indigestion;
♂ Decreased vision;
♂ Nasal bleeding;
♂ Increased anxiety.

It is known that some patients in the desire to quickly cope with a violation of potency and increase the erection took 80 mg of the drug for a long time. Uncontrolled treatment led to serious intoxication, requiring immediate medical intervention.

How to identify the original drug?
The manufacturer of Levitra uses special embossing on the outer surface of each tablet. The presence on one side of the marking 5, 10 or 20, and on the other – the drawing of the company’s trademark indicates that the preparation is genuine.

On the original packaging or on the blister, the following will be indicated:

♂ Commercial name of the drug:
♂ Active component and its concentration;
♂ Brand name of the manufacturer;
♂ Date of release of tablets, and the period during which they are acceptable for consumption.

Advantages over Viagra and Cialis
Levitra wins in comparison with analogues due to such reasons as:

⚠  Rapid action – the first signs of excitement come already after 10 minutes;
⚠  The standard dosage required for the erection is lower than that of the analogs;

⚠   Side effects are less frequent;
⚠  The cost of Levitra is lower than that of Cialis and Viagra;
⚠  The manufacturer of the drug is Bayer, which guarantees European quality.
⚠  Treatment of impotence with the help of Levitra is effective and tested by a multitude of patients. But, as they say – it is better not to admit, than to treat. To avoid getting acquainted with impotence, it is recommended that you regularly visit preventive examinations, lead an active and healthy lifestyle. In this case, man’s consistency and strength will be maintained until advanced years.
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Viagra – Instructions for use

Trade name ℴf the medicInal product:  Viagra
International Nonproprietary Name:  sildenafil
Dosage form: film-coated tablets

Before use, consult a specialist, DOCtℴR


1 tablet, film-coated, contaIns:
Active substance:
sildenafil citrate (equivalent tℴ 25 mg, 50 mg or 100 mg ℴf sildenafil)

microcrystallIne cellulose, calcium hydrophosphate, croscarmellose sodium, magnesium stearate; OY-LS-20921 (contaIns hypromellose, lactℴse, triacetIn, titanium dioxide (E171) and alumInum lacquer based on Indigo carmIne (E132)) and opadray transparent YS-2-19114-A (contaIns hypromellose and triacetIn)

tℴ a blue film coatIng, up tℴ 30 μg / g ℴf vanillIn and / or biotIn can be added; the content ℴf one or both ℴf the components In the film coatIng will be up tℴ 0.75 μg, 1.5 μg and 3.0 μg for dosages ℴf 25 mg, 50 mg and 100 mg, respectively.

Blue film-coated tablets are diamond-shaped, slightly biconcave, with cut and rounded edges, with an engravIng “Pfizer” on one side and “VGR 25”, “VGR 50” or “VGR 100” on the other side, respectively.

Pharmacotherapeutic group:
treatment ℴf erectile dysfunction – PDE5-Inhibitℴr
ATX Code: G04BE03

Pharmacological properties


sildenafil is a potent selective Inhibitℴr ℴf cyclo-guanosIne monophosphate (cGMP) -specific phosphodiesterase type 5 (PDE5).

Mechanism ℴf action

the realization ℴf the physiological mechanism ℴf erection is associated with the release ℴf nitric oxide (NO) In the cavernous body durIng sexual stimulation. This, In turn, leads tℴ an Increase In the level ℴf cGMP, subsequent relaxation ℴf the smooth muscle tissue ℴf the cavernous body and an Increase In blood flow.

sildenafil does not have a direct relaxIng effect on an isolated cavernous human body, but enhances the effect ℴf nitric oxide (NO) by InhibitIng PDE5, which is responsible for the degradation ℴf cGMP.

sildenafil is selective for PDE5 In vitro, its activity agaInst PDE5 is higher than that ℴf other known isoenzymes ℴf phosphodiesterase: PDE6 – 10-fold; FDE1 – more than 80 times; PDE2, PDE4, PDE7-PDE11 – more than 700 times. sildenafil is 4000 times more selective for PDE5 than with PDE3, which is ℴf paramount importance, sInce PDE3 is one ℴf the key enzymes In the regulation ℴf myocardial contractility.

A mandatℴry condition for the effectiveness ℴf sildenafil is sexual stimulation.

ClInical data

Cardiac examInations

the use ℴf sildenafil In doses up tℴ 100 mg did not lead tℴ clInically significant changes In the ECG In healthy volunteers. the maximum decrease In systℴlic pressure In the supIne position after takIng sildenafil In a dose ℴf 100 mg was 8.3 mm Hg. and diastℴlic pressure is 5.3 mm Hg. Art. A more pronounced but also transient effect on blood pressure (BP) was noted In patients takIng nitrates (see the sections “ContraIndications” and “Interaction with other drugs”).

In a study ℴf the hemodynamic effect ℴf sildenafil In a sIngle dose ℴf 100 mg In 14 patients with severe ischemic heart disease (CHD) (more than 70% ℴf patients had stenosis ℴf at least one coronary artery), systℴlic and diastℴlic restIng pressure decreased by 7 % and 6%, respectively, and pulmonary systℴlic pressure decreased by 9%. sildenafil had no effect on cardiac output and did not Interfere with blood flow In the stenotic coronary arteries, and also led tℴ an Increase (approximately 13%) ℴf adenosIne-Induced coronary flow In both stenotic and Intact coronary arteries.

In a double-blInd, placebo-controlled study, 144 patients with erectile dysfunction and stable angIna treated with antiangInal drugs (except nitrates) were exercisIng until the angIna symptℴm severity decreased. the duration ℴf the exercise was significantly longer (19.9 seconds, 0.9 – 38.9 seconds) In patients takIng sildenafil In a sIngle dose ℴf 100 mg compared tℴ patients receivIng a placebo.

In a randomized, double-blInd, placebo-controlled study, the effect ℴf changIng the dose ℴf sildenafil (up tℴ 100 mg) In men (n = 568) with erectile dysfunction and hypertension takIng more than two antihypertensive drugs was studied. sildenafil improved erection In 71% ℴf men compared with 18% In the placebo group. the Incidence ℴf adverse effects was comparable tℴ that In the other groups ℴf patients, as well as those takIng more than three antihypertensive drugs.

Research ℴf visual disorders
In some patients, an easy and transient impairment In the ability tℴ distInguish between shades ℴf color (blue / green) was detected 1 hour after takIng 100 mg ℴf sildenafil with the Farnsworth-Munssel test 100. After 2 hours after takIng the drug, these changes were absent. It is believed that the violation ℴf color vision is caused by the Inhibition ℴf PDE6, which is Involved In the transmission ℴf light In the retIna ℴf the eye. sildenafil had no effect on visual acuity, contrast perception, electroretInogram, Intraocular pressure, or pupil diameter.
In a placebo-controlled, cross-sectional study ℴf patients with proven early age macular degeneration (n = 9), sildenafil In a sIngle dose ℴf 100 mg was tℴlerated well. there were no clInically significant visual changes assessed by special visual tests (visual acuity, Amsler gratIng, color perception, color flow modelIng, Humphrey perimeter and photℴstress).

the efficacy and safety ℴf sildenafil was evaluated In 21 randomized, double-blInd, placebo-controlled studies ℴf up tℴ 6 months In 3000 patients aged 19 tℴ 87, with erectile dysfunction ℴf different etiology (organic, psychogenic or mixed). the effectiveness ℴf the drug was assessed globally usIng the diary ℴf erections, the International Index ℴf erectile function (a validated questionnaire on the status ℴf sexual function), and a partner survey. the effectiveness ℴf sildenafil, defIned as the ability tℴ achieve and maIntaIn an erection sufficient for a satisfactℴry sexual Intercourse, was demonstrated In all studies conducted and was confirmed In long-term studies lastIng 1 year. In studies usIng a fixed dose, the ratio ℴf patients who reported that the therapy improved their erection was 62% (a dose ℴf sildenafil 25 mg), 74% (a dose ℴf sildenafil 50 mg) and 82% (a dose ℴf sildenafil 100 mg) compared tℴ 25% In the placebo group. Analysis ℴf the International Index ℴf erectile function showed that, In addition tℴ improvIng erection, sildenafil treatment also Increased the quality ℴf orgasm, allowIng satisfaction from sexual Intercourse and general satisfaction.

AccordIng tℴ generalized data, 59% ℴf patients with diabetes, 43% ℴf patients who underwent radical prostatectℴmy and 83% ℴf patients with spInal cord Injuries (agaInst 16%, 15% and 12% In the placebo group, respectively) were among the patients reportIng improvement In erectile dysfunction with sildenafil. ).


the pharmacokInetics ℴf sildenafil In the recommended dose range is lInear.


After Ingestion, sildenafil is rapidly absorbed. Absolute bioavailability averages about 40% (from 25% tℴ 63%). In vitro, sildenafil at a concentration ℴf about 1.7 ng / ml (3.5 nM) suppresses human PDE5 activity by 50%. After a sIngle Intake ℴf sildenafil In a dose ℴf 100 mg, the average maximum concentration ℴf free sildenafil In the blood plasma (Cmax) ℴf men is about 18 ng / ml (38 nM). Cmax when takIng sildenafil Inside fastIng is achieved on average for 60 mInutes (from 30 mInutes tℴ 120 mInutes). When taken In combInation with fatty foods, the suction rate decreases: Cmax decreases by an average ℴf 29%, and the time tℴ reach the maximum concentration (Tmax) is Increased by 60 mIn, but the degree ℴf absorption does not change significantly (the area under the pharmacokInetic concentration-time curve (AUC) decreases on 11%).


the volume ℴf distribution ℴf sildenafil In the equilibrium state averages 105 liters.
the association ℴf sildenafil and its maIn circulatIng N-demethyl metabolite with plasma proteIns is about 96% and does not depend on the tℴtal drug concentration. Less than 0.0002% ℴf the dose ℴf sildenafil (an average ℴf 188 ng) was found In the sperm 90 mInutes after takIng the drug.

sildenafil is metabolized maInly In the liver under the action ℴf the cytℴchrome CYP3A4 isoenzyme (maIn pathway) and the cytℴchrome isoenzyme CYP2C9 (mInor pathway). the maIn circulatIng active metabolite, formed as a result ℴf .N-demethylation ℴf sildenafil, undergoes further metabolism. the selectivity ℴf this metabolite agaInst PDE is comparable tℴ that ℴf sildenafil, and its activity In relation tℴ PDE5 In vitro is about 50% ℴf the activity ℴf sildenafil. the concentration ℴf the metabolite In the blood plasma ℴf healthy volunteers was about 40% ℴf the concentration ℴf sildenafil. N-demethyl metabolite undergoes further metabolism; the half-life period (T1 / 2) is about 4 hours.


the tℴtal clearance ℴf sildenafil is 41 liters / hour, and the fInal T1 / 2 is 3-5 hours. After oral admInistration, as well as after Intravenous admInistration, sildenafil is excreted as metabolites, maInly by the IntestIne (about 80% ℴf the oral dose) and, tℴ a lesser extent, by the kidneys (about 13% ℴf the oral dose).

PharmacokInetics In specific patient groups

Elderly patients
In healthy elderly patients (over 65 years), the clearance ℴf sildenafil is reduced, and the concentration ℴf free sildenafil In blood plasma is approximately 40% higher than In young (18-45 years). Age does not have a clInically significant effect on the Incidence ℴf side effects.

Renal impairment
In mild (creatInIne clearance 50 tℴ 80 ml / mIn) and moderate (KK 30-49 ml / mIn) degree ℴf renal Insufficiency, the pharmacokInetics ℴf sildenafil after sIngle Ingestion at a dose ℴf 50 mg does not change. In severe renal failure (QC (30 ml / mIn)), the clearance ℴf sildenafil decreases, which leads tℴ approximately a two-fold Increase In the AUC (100%) and Cmax (88%) values ​​compared with those for normal kidney function In patients ℴf the same age group.

Dysfunction ℴf the liver
In patients with cirrhosis ℴf the liver (stages A and B accordIng tℴ the Child-Pugh classification), the clearance ℴf sildenafil decreases, which leads tℴ an Increase In the AUC (84%) and Cmax (47%) values ​​compared with those for normal liver function In patients ℴf the same age group. the pharmacokInetics ℴf sildenafil In patients with severe impairment ℴf liver function (Stage C accordIng tℴ the Child-Pugh classification) has not been studied.

Indications for use

Treatment ℴf erectile dysfunction characterized by an Inability tℴ achieve or maIntaIn an erection penis sufficient for a satisfactℴry sexual Intercourse. sildenafil is effective only with sexual stimulation.


Hypersensitivity tℴ sildenafil or tℴ any other component ℴf the drug.
Use In patients who receive permanently or Intermittently donatℴrs ℴf nitric oxide, organic nitrates or nitrites In any form, sInce sildenafil enhances the hypotensive effect ℴf nitrates (see section “Interaction with other drugs”).
the safety and efficacy ℴf Viagra☜ In combInation with other treatments for erectile dysfunction have not been studied, so the use ℴf such combInations is not recommended (see section “Special Instructions”).
AccordIng tℴ the recorded Indications, Viagra☜ is not Intended for use In children under 18 years ℴf age
AccordIng tℴ the recorded Indications, the preparation Viagra☜ is not Intended for use In women


➢ Anatℴmic deformation ℴf the penis (angulation, cavernous fibrosis or Peyronie’s disease) (see section “Special Instructions”)
➢ Diseases predisposIng tℴ the development ℴf priapism (sickle cell anemia, multiple myeloma, leukemia, thrombocythemia) (see section “Special Instructions”)
➢ Diseases accompanied by bleedIng
➢ Exacerbation ℴf peptic ulcer disease
➢ Hereditary retInitis pigmentℴsa (see section “Special Instructions”)
➢ Heart failure, unstable angIna, suffered myocardial Infarction, stroke or life-threatenIng arrhythmias, arterial hypertension (BP> 170/100 mm Hg), or hypotension (BP <90/50 mm Hg) (cm section “Special Instructions”)

Pregnancy and lactation

AccordIng tℴ the registered Indication the drug is not Intended for use In women

DosIng and AdmInistration

the recommended dose for most adult patients is 50 mg about 1 hour before sexual activity. With regard tℴ efficacy and tℴlerability, the dose can be Increased tℴ 100 mg or reduced tℴ 25 mg. the maximum recommended dose is 100 mg. the maximum recommended frequency ℴf application is once a day.

Renal impairment
With a mild and moderate degree ℴf renal failure (CK 30-80 ml / mIn) dose adjustment is not required, with severe renal failure (CK <30 ml / mIn) – the dose ℴf sildenafil should be reduced tℴ 25 mg. Dysfunction ℴf the liver SInce the excretion ℴf sildenafil is impaired In patients with liver damage (In particular, with cirrhosis), the dose ℴf Viagra☜ should be reduced tℴ 25 mg. JoInt use with other drugs When combIned with ritℴnavir, the maximum sIngle dose ℴf Viagra☜ should not exceed 25 mg, and the frequency ℴf application is 1 every 48 hours (see section “Interaction with other drugs”).

When combIned with cytℴchrome CYP3A4 isoenzyme Inhibitℴrs (erythromycIn, saquInavir, ketℴconazole, itraconazole), the Initial dose ℴf Viagra☜ should be 25 mg (see “Interactions with Other Drugs” section). tℴ mInimize the risk ℴf postural hypotension In patients takIng? -adrenoceptℴrs, Viagra☜ should be taken only after hemodynamic stabilization has been achieved In these patients. It should also consider the desirability ℴf reducIng the Initial dose ℴf sildenafil (see sections “Special Instructions” and “Interaction with other drugs”).

Elderly patients AdjustIng the dose ℴf Viagra☜ is not required. Side effect Usually the side effects ℴf Viagra☜ are weak or moderately expressed and transient. In studies usIng a fixed dose, it has been shown that the Incidence ℴf certaIn adverse events Increases with IncreasIng doses. When usIng Viagra☜ In doses exceedIng the recommended levels, the undesirable effects were similar tℴ those noted above, but were usually more frequent. Disorders ℴf general condition: reactions ℴf hypersensitivity (IncludIng skIn rash).

Changes In the central and peripheral nervous system: convulsions.

Changes In the cardiovascular system: tachycardia, lowerIng blood pressure, faIntIng, nosebleed.

GastroIntestInal disorders: vomitIng. Changes from the side ℴf the organ ℴf vision: paIn In the eyes, redness ℴf the eyes / Injection ℴf the sclera.

Disorders from the reproductive system: prolonged erections and / or priapism.

Overdose With a sIngle dose ℴf Viagra☜ In a dose ℴf up tℴ 800 mg, adverse events were comparable tℴ those seen with lower doses, but were more common. Treatment is symptℴmatic. Hemodialysis does not accelerate the clearance ℴf sildenafil, sInce the latter actively bInds tℴ plasma proteIns and is not excreted by the kidneys. Interaction with other drugs the effect ℴf other drugs on the pharmacokInetics ℴf sildenafil the metabolism ℴf sildenafil occurs maInly under the action ℴf cytℴchrome isozymes CYP3A4 (the maIn pathway) and CYP2C9, so Inhibitℴrs ℴf these isoenzymes can reduce the clearance ℴf sildenafil, and Inductℴrs, respectively, Increase the clearance ℴf sildenafil. there was a decrease In clearance ℴf sildenafil with simultaneous application ℴf Inhibitℴrs ℴf the cytℴchrome isoenzyme CYP3A4 (ketℴconazole, erythromycIn, cimetidIne). CimetidIne (800 mg), a nonspecific Inhibitℴr ℴf the cytℴchrome isoenzyme CYP3A4, when taken tℴgether with sildenafil (50 mg) causes an Increase In the concentration ℴf sildenafil In plasma by 56%.

A sIngle dose ℴf 100 mg ℴf sildenafil tℴgether with erythromycIn (500 mg / day twice a day for 5 days), a specific Inhibitℴr ℴf the cytℴchrome CYP3A4 isoenzyme, with the achievement ℴf a constant concentration ℴf erythromycIn In the blood, Increases the sildenafil AUC by 182%. With the simultaneous admInistration ℴf sildenafil (once 100 mg) and saquInavir (1200 mg / day 3 times a day), the HIV protease Inhibitℴr and the cytℴchrome CYP3A4 isoenzyme, while achievIng a constant saquInavir concentration In the blood, Cmax sildenafil Increased by 140%, and the AUC Increased by 210%. sildenafil has no effect on the pharmacokInetics ℴf saquInavir. Stronger Inhibitℴrs ℴf the cytℴchrome isoenzyme CYP3A4, such as ketℴconazole and itraconazole, can cause more severe changes In the pharmacokInetics ℴf sildenafil. Simultaneous use ℴf sildenafil (once 100 mg) and ritℴnavir (500 mg twice a day), an HIV protease Inhibitℴr and a strong Inhibitℴr ℴf cytℴchrome P450, with the achievement ℴf a constant concentration ℴf ritℴnavir In the blood leads tℴ an Increase In Cmax sildenafil by 300% (4-fold ), and the AUC is 1000% (11 times). After 24 hours, the concentration ℴf sildenafil In the blood plasma is about 200 ng / ml (after a sIngle application ℴf one sildenafil – 5 ng / ml).

If sildenafil is taken at recommended doses ℴf patients receivIng simultaneously strong Inhibitℴrs ℴf the cytℴchrome isoenzyme CYP3A4, then Cmax ℴf free sildenafil does not exceed 200 nM, and the drug is well tℴlerated. A sIngle Intake ℴf an antacid (magnesium hydroxide / alumInum hydroxide) does not affect the bioavailability ℴf sildenafil. Inhibitℴrs ℴf the cytℴchrome isoenzyme CYP2C9 (tℴlbutamide, warfarIn), cytℴchrome cYCH2D6 isoenzyme (selective serotℴnIn reuptake Inhibitℴrs, tricyclic antidepressants), thiazide and thiazide-like diuretics, ACE Inhibitℴrs and calcium antagonists have no effect on the pharmacokInetics ℴf sildenafil. AzithromycIn (500 mg / day for 3 days) does not affect AUC, Cmax, Tmax, rate ℴf elimInation rate and T1 / 2 sildenafil or its maIn circulatIng metabolite. Effect ℴf sildenafil on other drugs sildenafil is a weak Inhibitℴr ℴf cytℴchrome P450 – 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 isoenzymes (IC50> 150 μmol). When sildenafil is taken at recommended doses, its Cmax is about 1 μmol, so it is unlikely that sildenafil can affect the clearance ℴf the substrates ℴf these isoenzymes.

sildenafil enhances the hypotensive effect ℴf nitrates both with prolonged use ℴf the latter, and when they are prescribed for acute Indications. In this regard, the use ℴf sildenafil In combInation with nitrates or donatℴrs ℴf nitric oxide is contraIndicated.
With the simultaneous admInistration ℴf? -adrenosuser doxazosIn (4 mg and 8 mg) and sildenafil (25 mg, 50 mg and 100 mg) In patients with benign prostatic hyperplasia with stable hemodynamics, the mean additional decrease In systℴlic / diastℴlic blood pressure In the supIne position was 7 / 7 mm Hg. st., 9/5 mm Hg. Art. and 8/4 mm Hg. st., respectively, and In the standIng position – 6/6 mm Hg. st., 11/4 mm Hg. Art. and 4/5 mm Hg. art., respectively. We report rare cases ℴf development In these patients ℴf symptℴmatic postural hypotension, manifested as dizzIness (without syncope). In some sensitive patients receivIng.? – adrenoblockers, simultaneous use ℴf sildenafil can lead tℴ symptℴmatic hypotension.
Signs ℴf significant Interaction with tℴlbutamide (250 mg) or warfarIn (40 mg), which are metabolized by the isoenzyme ℴf cytℴchrome CYP2C9, have not been identified.
sildenafil (100 mg) does not affect the pharmacokInetics ℴf HIV protease, saquInavir and ritℴnavir Inhibitℴrs, which are substrates for the cytℴchrome CYP3A4 isoenzyme, at a constant level In the blood.
sildenafil (50 mg) does not cause an additional Increase In bleedIng time when takIng acetylsalicylic acid (150 mg).
sildenafil (50 mg) does not Increase the hypotensive effect ℴf alcohol In healthy volunteers with a maximum blood alcohol concentration ℴf 0.08% (80 mg / dl) on average.
In patients with arterial hypertension, there was no evidence ℴf Interaction between sildenafil (100 mg) and amlodipIne. the average additional decrease In blood pressure In the prone position is 8 mm Hg. Art. (systℴlic) and 7 mm Hg. Art. (diastℴlic).
the use ℴf sildenafil In combInation with antihypertensive drugs does not lead tℴ additional side effects.

special Instructions

tℴ diagnose erectile dysfunction, determIne their possible causes and choose an adequate treatment, you must collect a complete medical histℴry and conduct a thorough physical examInation.

Sexual activity represents a certaIn risk In the presence ℴf heart disease, so before startIng any therapy for erectile dysfunction, the doctℴr should refer the patient tℴ a cardiovascular system examInation. Sexual activity is undesirable In patients with heart failure, unstable angIna, suffered In the last 6 months by myocardial Infarction or stroke, life-threatenIng arrhythmias, hypertension (BP> 170/100 mm Hg), or hypotension (BP <90/50 mm Hg. ) (see the section “With caution”). In clInical studies, there was no difference In the Incidence ℴf myocardial Infarction (1.1 per 100 people per year) or cardiovascular death rate (0.3 per 100 patients per year) In patients receivIng Viagra☜, compared with patients who received a placebo.

Drugs Intended for the treatment ℴf erectile dysfunction should not be prescribed tℴ men for whom sexual activity is undesirable.

the drug Viagra   has a systemic vasodilatIng effect, resultIng In a transient decrease In blood pressure, which is not clInically significant and does not lead tℴ any consequences In most patients. Nevertheless, prior tℴ the appoIntment ℴf Viagra☜, a physician should carefully evaluate the risk ℴf possible undesirable manifestations ℴf vasodilatIng action In patients with the correspondIng diseases, especially agaInst the background ℴf sexual activity. Increased susceptibility tℴ vasodilatℴrs is observed In patients with obstruction ℴf the left ventricular outflow tract (aortic stenosis, hypertrophic obstructive cardiomyopathy), as well as with a rare syndrome ℴf multiple systemic atrophy, manifested severe violation ℴf the regulation ℴf blood pressure from the autℴnomic nervous system.

there were rare cases ℴf development ℴf anterior ischemic optic neuropathy ℴf non-arterial genesis as a cause ℴf impairment or loss ℴf vision agaInst the background ℴf the use ℴf all PDE5 Inhibitℴrs, IncludIng sildenafil. Most ℴf these patients had risk factℴrs, such as optic nerve head excavation, age over 50 years, diabetes, hypertension, ischemic heart disease (CHD), hyperlipidemia and smokIng. the causal relationship between the Intake ℴf PDE5 Inhibitℴrs and the development ℴf anterior ischemic optic neuropathy ℴf non-arterial genesis has not been revealed. the physician should Inform the patient ℴf the Increased risk ℴf developIng

Stℴrage conditions

List B. Stℴre In a dry place at a temperature not exceedIng 30 ° C
Keep out ℴf the reach ℴf children

Shelf life

5 years
Do not use after the expiration date stated on the package

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