Vildegra
Vildegra: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Use in childhood
- 10. In case of impaired renal function
- 11. For violations of liver function
- 12. Use in the elderly
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Vildegra
ATX code: G04BE03
Active ingredient: sildenafil (Sildenafil)
Manufacturer: LLC "Ozon" (Russia)
Description and photo update: 2019-10-07
Prices in pharmacies: from 82 rubles.
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Vildegra is a drug for the treatment of erectile dysfunction, an inhibitor of PDE-5 (phosphodiesterase type 5).
Release form and composition
The drug is available in the form of tablets of prolonged action, film-coated: round, biconvex, dosage 50 mg - from pale pink to pink, dosage 100 mg - dark blue; the core of the tablets is white or almost white (1, 2, 4 or 10 pcs. in blisters, in a cardboard box 1, 2, 4 or 10 packages; 10, 20, 40, 50 or 100 pcs. in polyethylene terephthalate cans, in a cardboard box of 1 can. Each pack also contains instructions for the use of Vildegra).
1 tablet contains:
- active substance: sildenafil citrate - 70.24 or 140.48 mg, which in terms of sildenafil base is equivalent to 50 and 100 mg, respectively;
- auxiliary components: hypromellose, lactose monohydrate (milk sugar), povidone K25, magnesium stearate; additionally for a dosage of 50 mg - microcrystalline cellulose;
- composition of the film shell: dosage of 50 mg - opadry II 85F240012 pink (polyvinyl alcohol, titanium dioxide, macrogol-4000, talc, iron dye yellow oxide, iron dye red oxide); dosage 100 mg - opadry II 85F205024 blue (macrogol-4000, polyvinyl alcohol, iron oxide yellow dye, aluminum varnish with brilliant blue and indigo carmine dyes, titanium dioxide, talc).
Pharmacological properties
Pharmacodynamics
Vildegra is a drug for the treatment of erectile dysfunction. The active ingredient - sildenafil, is a potent selective inhibitor of cyclic guanosine monophosphate (cGMP) specific PDE-5.
With sexual stimulation, the physiological mechanism of erection involves the release of nitric oxide (NO) in the cavernous body, which activates guanylate cyclase. This leads to the subsequent relaxation of the smooth muscle tissues of the corpus cavernosum against the background of an increase in the level of cGMP and an increase in blood flow to them.
Sildenafil works to enhance the relaxing effect of nitric oxide (NO) by inhibiting PDE-5, which is responsible for the breakdown of cGMP. It does not have a direct relaxing effect on the isolated corpus cavernosum of a man.
The selectivity of the action of the active substance has been established under in vitro conditions. The activity of sildenafil against PDE-5 exceeds the activity against the following phosphodiesterase isoenzymes: PDE-2, PDE-4, PDE-7-PDE-11 - more than 700 times, PDE-6 - 10 times, PDE-1 - more than 80 times. In relation to PDE-3, which is one of the main enzymes in the regulation of myocardial contractility, its activity is 4000 times lower than in relation to PDE-5.
The effectiveness of sildenafil appears only against the background of sexual stimulation.
Pharmacokinetics
When using therapeutic doses, the pharmacokinetics of sildenafil is linear.
After oral administration, sildenafil is rapidly absorbed. With a single intake on an empty stomach at a dose of 100 mg, the average maximum concentration (C max) of free sildenafil in blood plasma is reached after 1.5 hours and can be about 18 ng / ml. In vitro, a concentration of 1.7 ng / ml sildenafil is sufficient to suppress human PDE-5 activity by 50%. The absolute bioavailability averages about 40%. Taking the drug in combination with fatty foods causes a decrease in the rate of absorption of sildenafil. At the same time, C max decreases on average by 29%, the period of reaching the maximum concentration (T max) increases by 1 hour, AUC (area under the pharmacokinetic curve "concentration - time") decreases by 11%.
The binding of sildenafil and its main metabolite to blood plasma proteins does not depend on the total concentration of the drug and is about 96%.
The volume of distribution of the active substance in the equilibrium state averages 105 liters. Approximately 188 ng of sildenafil (less than 0.000 2% of the dose) is found in semen 1.5 hours after ingestion.
In the liver, sildenafil is metabolized mainly under the influence of the cytochrome CYP3A4 isoenzyme and to a small extent - the cytochrome CYP2C9 isoenzyme. As a result of N-demethylation of sildenafil, the main circulating active metabolite is formed, the selectivity of which with respect to PDE is similar to that of sildenafil, and with respect to PDE-5 is about 50% of the activity of sildenafil. The concentration level of the main circulating N-demethyl metabolite in blood plasma is about 40% of the concentration of sildenafil. The main metabolite undergoes subsequent biotransformation, its half-life (T 1/2) is about 4 hours.
The final T1 / 2 of sildenafil is 3 to 5 hours, the total clearance is 41 l / h. It is excreted in the form of metabolites mainly through the intestines (about 80% of the dose), through the kidneys - about 13%.
In patients aged 65 years and older, the clearance of sildenafil is reduced. Compared with men 18–45 years old, in the elderly, an increase of 40% in plasma concentration of free sildenafil is allowed. Age has no clinically significant effect on the incidence of side effects.
The pharmacokinetics of sildenafil after a single oral dose of 50 mg with mild to moderate renal failure [creatinine clearance (CC) values are in the range from 30 to 80 ml / min] does not change. The clearance of sildenafil decreases in severe renal failure (CC 30 ml / min or less), which causes an approximately 2-fold increase in AUC and 88% C max compared to these indicators in patients with normal renal function of the same age group.
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 of 47% C max and 84% AUC compared with patients of the same age group with normal liver function. In severe liver dysfunction (Child-Pugh stage C), the pharmacokinetics of sildenafil have not been studied.
Indications for use
The use of Vildegra is indicated for the treatment of erectile dysfunction in men, characterized by the inability to achieve or maintain an erection of the penis sufficient for satisfactory intercourse (the drug is active only in the presence of sexual stimulation).
Contraindications
Absolute:
- cirrhosis of the liver, liver failure;
- continuous or periodic intake of nitric oxide donors, organic nitrates or nitrites in any other forms (due to the fact that sildenafil enhances the hypotensive effect of nitrates);
- arterial hypotension: systolic (upper) blood pressure (BP) - less than 90 mm Hg. Art. (mercury column), diastolic (lower) - less than 50 mm Hg. Art.;
- severe cardiovascular diseases (including severe heart failure, unstable angina pectoris) and other pathologies in which sexual activity is undesirable;
- myocardial infarction or cerebrovascular accident within the past six months;
- severe renal failure (CC less than 30 ml / min);
- retinitis pigmentosa and other inherited degenerative diseases of the retina;
- lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome;
- concomitant therapy with ritonavir (for 100 or 50 mg tablets);
- the simultaneous use of other means of treating erectile dysfunction;
- age up to 18 years;
- hypersensitivity to the components of Vildegra.
The drug is not intended for use in women.
Vildegra should be taken with caution in men with anatomical deformity of the penis (angulation, Peyronie's disease or cavernous fibrosis), arterial hypertension (blood pressure above 170/100 mm Hg), life-threatening heart rhythm disturbances, heart failure, a predisposition to the development of priapism (patients with multiple myeloma, sickle cell anemia, thrombocythemia, leukemia); with bleeding pathologies, exacerbation of gastric ulcer and duodenal ulcer, a history of episodes of development of anterior non-arteritis ischemic optic neuropathy, concomitant use of alpha-blockers.
In addition, it is recommended with caution to combine sildenafil with ritonavir or inhibitors of the cytochrome CYP3A4 isoenzyme.
Vildegra, instructions for use: method and dosage
Vildegra tablets are taken orally 1 hour before the expected sexual activity.
The recommended single dose is 50 mg. Taking into account individual tolerance and effectiveness, it can be increased to 100 mg. The maximum dose is 100 mg, the maximum frequency of use is 1 time per day.
With mild and moderate renal failure (CC 30–80 ml / min), dose reduction is not required.
When combined with alpha-blockers, Vildegra can be started only after hemodynamic stabilization is achieved in patients, this will reduce the risk of postural hypotension.
While taking ritonavir, it is necessary to use sildenafil at a dose of 25 mg and observe the dosage regimen of the drug (no more than 1 pc. 1 time in 48 hours).
If Vildegra is taken against the background of treatment with ketoconazole, itraconazole, erythromycin, saquinavir (inhibitors of the cytochrome CYP3A4 isoenzyme), then the initial dose of sildenafil should not exceed 25 mg.
Dose adjustment of Vildegra for men in old age is not required.
Side effects
- on the part of the cardiovascular system: often (from ≥ 1% to <10%) - vasodilation (hot flashes); infrequently (from ≥ 0.1% to <1%) - tachycardia, palpitations; rarely (≥ 0.01% to <0.1%) - decrease or increase in blood pressure, atrial fibrillation, myocardial infarction; the frequency has not been established (based on the available data, it is not possible to establish the frequency of occurrence of adverse reactions) - unstable angina pectoris, ventricular arrhythmia, cardiac arrest;
- from the nervous system: very often (≥ 10%) - headache; often - dizziness; infrequently - hypesthesia, drowsiness; rarely - fainting, stroke; frequency not established - seizures (including recurrent seizures), transient ischemic attack;
- from the organ of hearing: infrequently - tinnitus, vertigo; rarely - sudden hearing loss, hearing loss;
- on the part of the organ of vision: often - violation of color perception, visual impairment; infrequently - violation of lacrimation, damage to the conjunctiva; frequency not established - visual field defect, retinal vascular occlusion, anterior ischemic optic neuropathy;
- from the respiratory system, chest and mediastinal organs: often - nasal congestion; rarely - nosebleeds;
- from the gastrointestinal tract: often - dyspepsia; infrequently - dryness of the oral mucosa, nausea, vomiting;
- from the genital organs: infrequently - bleeding from the penis, hematospermia; frequency not established - prolonged erection, priapism;
- on the part of the musculoskeletal system: infrequently - myalgia;
- allergic reactions: infrequently - skin rash; frequency not established - Stevens-Johnson syndrome, Lyell's syndrome (toxic epidermal necrolysis);
- others: rarely - fatigue, chest pain.
Overdose
Symptoms: an overdose of the drug increases the risk of adverse events with a greater degree of severity.
Treatment: the appointment of symptomatic therapy. The use of hemodialysis is ineffective.
special instructions
Taking Vildegra should be started as directed by a doctor, after a thorough physical examination, collection and study of a complete medical history, allowing to diagnose erectile dysfunction and determine the possible causes of their occurrence in a man. In addition, before prescribing any therapy for erectile dysfunction, it is necessary to perform an examination of the patient's cardiovascular system, since sexual activity involves an increase in certain risks for heart disease.
Vildegra should not be prescribed to men for whom sexual activity is undesirable.
If after taking the drug, an erection persists for more than 4 hours, you must seek medical help. In case of late treatment of priapism, damage to the tissues of the penis or the onset of irreversible loss of potency may occur.
The results of clinical studies showed no effect of Vildegra on the incidence of myocardial infarction in patients or on the incidence of fatal outcomes from cardiovascular diseases.
Adverse events, including serious cardiovascular complications in the form of hypertension or hypotension, myocardial infarction, unstable angina pectoris, ventricular arrhythmia, hemorrhagic stroke, transient ischemic attack, sudden cardiac death, which were recorded during the post-marketing use of sildenafil, were not directly related to it … In most cases, they occurred in patients with risk factors for cardiovascular complications.
Before prescribing Vildegra, it is necessary to carefully assess the likelihood of developing side effects associated with the systemic vasodilating effect of sildenafil. A decrease in blood pressure, sometimes occurring after taking sildenafil, is of a transient clinically insignificant character and in most patients does not lead to undesirable consequences. It is recommended to take into account the increased susceptibility to vasodilators in patients with obstruction of the left ventricular outflow tract (hypertrophic obstructive cardiomyopathy, aortic stenosis), as well as in patients with multiple systemic atrophy syndrome, manifested by severe impairment of blood pressure regulation by the autonomic nervous system.
Risk factors for the development of anterior non-arteritic ischemic neuropathy of the optic nerve include: deepening of the optic nerve head, diabetes mellitus, coronary heart disease, arterial hypertension, hyperlipidemia, smoking, age over 50 years.
In case of sudden deterioration or loss of hearing while taking Vildegra, a doctor's consultation is required.
The results of laboratory studies of sildenafil indicate that it enhances the antiplatelet effect of sodium nitroprusside on human platelets. It should be borne in mind that in patients with pulmonary hypertension caused by diffuse connective tissue diseases, nosebleeds occur more often than in patients with primary pulmonary hypertension. In addition, the risk of nosebleeds is increased when sildenafil is combined with a vitamin K antagonist.
Influence on the ability to drive vehicles and complex mechanisms
While taking Vildegra, there is a risk of developing adverse events (including lowering blood pressure, blurred vision, chromatopsia), therefore, during the period of treatment, patients should independently assess the individual effect of the drug and their ability to drive vehicles or perform other potentially hazardous activities that require the speed of psychomotor reactions and increased concentration of attention.
Pediatric use
The use of Vildegra is contraindicated under the age of 18 years.
With impaired renal function
It is contraindicated to use Vildegra tablets in patients with severe renal failure (CC less than 30 ml / min).
With mild to moderate renal failure (CC 30–80 ml / min), dose adjustment is not required.
For violations of liver function
It is contraindicated to take Vildegra tablets for liver cirrhosis and liver failure.
Use in the elderly
No dose adjustment is required for older men.
Drug interactions
- erythromycin, ketoconazole, itraconazole, cimetidine, saquinavir and other inhibitors of the cytochrome CYP3A4 isoenzyme: cause a decrease in the clearance of sildenafil, which leads to an increase in its concentration in plasma. So, with a single dose of sildenafil at a dose of 100 mg against the background of ritonavir reaching [an inhibitor of HIV (human immunodeficiency virus) - protease and a strong inhibitor of cytochrome P 450] constant concentration in the blood during treatment at a dose of 500 mg 2 times a day, there is an increase in 4 times C maxsildenafil and 11 times the AUC. After a day, the concentration of sildenafil in the blood plasma continues to be about 200 ng / ml. With a stable level of concentration in the blood of HIV protease inhibitors (saquinavir, ritonavir), sildenafil (100 mg) has no effect on their pharmacokinetic parameters. In patients receiving strong inhibitors of the cytochrome CYP3A4 isoenzyme, taking Vildegra at the recommended dose is well tolerated;
- magnesium hydroxide, aluminum hydroxide: a single dose of antacid does not affect the bioavailability of sildenafil;
- tolbutamide, warfarin (inhibitors of the cytochrome CYP2C9 isoenzyme), tricyclic antidepressants, selective serotonin reuptake inhibitors, thiazide and thiazide-like diuretics, angiotensin-converting enzyme inhibitors, calcium antagonists, azithromycin 3-day dose Pharmaquil (in suethochromycin) 500 mg
- bosentan (inducer of isoenzymes CYP3A4 and CYP2C9): being an antagonist of endothelin receptors, bosentan causes a decrease in C max of sildenafil by 52.4% and AUC - by 62.6%. At the same time, there is an increase in C max and AUC of bosentan by 42 and 49.8%, respectively;
- nitrates, nitric oxide donors: the hypotensive effect of nitrates, taken for a long time or in acute indications, is enhanced (joint administration is contraindicated);
- alpha-blockers (doxazosin): increase the risk of symptomatic hypotension or symptomatic postural hypotension;
- acetylsalicylic acid (in a daily dose of 150 mg): does not cause an additional increase in bleeding time;
- antihypertensive drugs (amlodipine): no clinically significant signs of interaction have been established, co-administration does not cause additional side effects;
- ethanol: the hypotensive effect of alcohol is not enhanced.
The effect of sildenafil on the clearance of drugs that are substrates of such cytochrome P 450 isoenzymes as CYP1A2, CYP3A4, CYP2C9, CYP2C19, CYP2D6, CYP2E1 is unlikely.
Analogs
Vildegra's analogs are: Sildenafil, Sildenafil VERTEX, Sildenafil Cardio, Viagra, Viasan-LF, Vizarsin, Viatail, VIVAIRA, Dynamo, Dynamiko Forward, Invida ODP, Olmax Strong, Revazio, Maxigdenra, Sidjerafilamp, Silhamp, Siladez and etc.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C in a dark place.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Vildegre
Reviews about Vildegre are positive. Men, characterizing the effectiveness of the drug, report that it gives vivid sensations from sex, allows you to feel confident and increase self-esteem. Taking the drug causes a very persistent and more powerful erection, a surge of strength, allows you to prolong sexual intercourse, and, if desired, repeat it.
They note the good tolerance of Vildegra, in rare cases - the appearance of a rapid heart rate, nasal congestion.
Price for Vildegra in pharmacies
The approximate price for Vildegra, tablets with a dosage of 100 mg, can be for a package containing 1 pc. - from 145 rubles, 4 pcs. - from 331 to 436 rubles., 10 pcs. - from 549 to 687 rubles, 30 pcs. - from 1097 rubles. The price for tablets with a dosage of 50 mg can be for a package containing 1 pc. - from 105 to 124 rubles, 4 pcs. - from 275 to 329 rubles, 10 pcs. - from 513 to 581 rubles., 30 pcs. - from 879 rubles.
Vildegra: prices in online pharmacies
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Drug name Price Pharmacy |
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Vildegra 100 mg film-coated tablets of prolonged action 1 pc. 82 RUB Buy |
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Vildegra 50 mg film-coated tablets of prolonged action 4 pcs. 141 r Buy |
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Vildegra 100 mg film-coated tablets of prolonged action 4 pcs. 347 r Buy |
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Vildegra 100 mg film-coated tablets, 10 pcs. 430 RUB Buy |
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Vildegra 50 mg film-coated tablets, 10 pcs. 462 r Buy |
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Vildegra prolonged release tablets. p.p. 50mg 10 pcs. 502 RUB Buy |
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Vildegra 50 mg film-coated tablets, 30 pcs. RUB 699 Buy |
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Vildegra 100 mg film-coated tablets of prolonged action 30 pcs. 800 RUB Buy |
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Vildegra prolonged release tablets. p.p. 50mg 30 Pcs. 828 RUB Buy |
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Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
