Sildenafil

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Available since: 2019-09-19

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Clinical Pharmacology

Selective inhibitor cycloguanosine monophosphate (cGMP) -specific PDE5. PDE5, which is responsible for the decay of cGMP, is contained not only in the cavernous body of the penis, but also in the vessels of the lungs. Restores impaired erectile function and provides a natural response to sexual arousal. Sildenafil does not have a direct relaxing effect on the cavernous body, but actively enhances the relaxing effect of nitric oxide on this tissue. During sexual arousal, the local release of NO under the influence of sildenafil leads to the inhibition of PDE5 and an increase in the level of cGMP in the cavernous body, resulting in the relaxation of smooth muscles and increased blood flow in the cavernous body. Being an inhibitor of PDE5, sildenafil increases the cGMP content in the smooth muscle cells of the pulmonary vessels and causes them to relax. In patients with pulmonary hypertension, taking sildenafil leads to dilation of the pulmonary vessels and, to a lesser extent, other vessels. Sildenafil is selective for in vitro PDE5. Its activity against PDE5 exceeds the activity against other known PDE isoenzymes: PDE6, which participates in the transmission of a light signal in the retina, 10 times; PDE1 - 80 times; PDE2, PDE4, PDE7-PDE11 - more than 700 times. The activity of sildenafil in relation to PDE5 is more than 4000 times greater than its activity in relation to PDE3, cAMP-specific PDE, which participates in the contraction of the heart. Sildenafil can cause a mild and transient disorder in color (blue / green). A supposed mechanism of color vision impairment is the inhibition of PDE6, which is involved in the process of transmitting light in the retina. In vitro studies have shown that the effect of sildenafil on PDE6 is 10 times lower than its activity against PDE5.

Suggested use

Treatment of erectile dysfunction: take orally about 1 hour before planned sexual activity. A single dose is 50 mg. Given the efficacy and tolerability, the dose may be increased to 100 mg or reduced to 25 mg. The maximum single dose is 100 mg. The maximum frequency of use is 1 time / day. For elderly patients over the age of 65 years and with concomitant violations of renal or liver function, the dose is 25 mg. Pulmonary hypertension: by mouth 20 mg 3 times / day with an interval of about 6-8 hours, regardless of the meal. The maximum daily dose is 60 mg. Patients with impaired renal function dose adjustment is not required, but in case of poor tolerance the dose is reduced to 20 mg 2 times / day.

Indications

The drug is used for the treatment of disorders of potency, expressed inability to achieve or maintain an erection of the penis, to ensure full sexual intercourse. The active substance of the drug (sildenofril) is effective only when exposed to sexual arousal.

Sildenafil is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Vildegra			pills
Viatyle	Sun Pharmaceutical Industries Ltd	India	pills
Viagra	Pfizer	USA	pills
Sildenafil	Vertex	Russia	pills
Effex Sildenafil	Evalar	Russia	pills
Vizarsin Q-Tab	Krka dd Novo mesto AO	Slovenia	pills
Dynamico®	STSBio Inc	Korea	sachet
Sildenafil-SZ	North Star	Russia	pills
Maxigra®	Polpharma	Poland	pills
Viasan-LF	Lecpharm	Russia	pills
Vizarsin	Krka dd Novo mesto AO	Slovenia	pills
Tornetis	Sandoz	Switzerland	pills
Revatio®	Pfizer	USA	pills
Dynamico®	Pliva Hrvatska doo	Croatia	pills

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Dosage and Administration

For most patients, a single dose of 60 mg is recommended 1 hour before sexual activity. But in some cases, it is possible to use the Dynamics from 4 hours to 0.5 hours before sexual activity.

Based on the effect and tolerability of the drug, the daily dose may be increased to 100 mg, or reduced to 25 mg,

It is recommended to take the drug no more than 1 time per day.

Adverse reactions

From the nervous system: very often - headache; often - dizziness; infrequently - drowsiness, hypesthesia; rarely - stroke, fainting; frequency is unknown - transient ischemic attack, convulsions, including recurrent.
Since the cardiovascular system: often - "tides"; infrequently - palpitations, tachycardia; rarely, an increase or decrease in blood pressure, myocardial infarction, atrial fibrillation; frequency is unknown - ventricular arrhythmia, unstable stenocardia, sudden death.
On the part of the organ of vision: often - impaired vision, violation of color perception; infrequently - damage to the conjunctiva, violation of tearing, enhanced perception of light, impaired visual clarity, transient chromatopsia; rarely - redness of the sclera, pain in the eyeballs; unknown frequency - anterior ischemic optic neuropathy, retinal vascular occlusion, narrowing of the visual fields.
On the part of the organ of hearing: infrequently - vertigo, tinnitus; rarely - deafness.
On the part of the respiratory system: often - nasal congestion; rarely - nosebleeds.
From the gastrointestinal tract: often - dyspepsia; infrequently - vomiting, nausea, dryness of the oral mucosa.
Allergic reactions: rarely - skin rash; frequency is unknown - Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).
On the part of the genitals: the frequency is unknown - priapism, prolonged erection.
Other: rarely - chest pain, fatigue.

Contraindications

- Hypersensitivity to the drug.
- Patients who continuously or intermittently receive donators of nitric oxide, organic nitrates.

Drug interactions

- The effect of other drugs on Dynamic Sildenafil is metabolized by isoenzymes of cytochrome P450 (SUR), 3A4 (mainly) and 2C9 (minimally), therefore inhibitors of these enzymes can reduce the clearance of sildenafil. Cimetidine (800 mg), a specific anionic inhibitor of SUR, causes an increase in plasma concentration of sildenafil by 59% when taken together by healthy volunteers. Simultaneous administration of a single dose of 50 or 100 mg of erythromycin, a specific inhibitor of SUR, increases by 182% AUC of sildenafil. With the joint use of sildenafil (single dose of 50 or 100 mg) with HIV protease inhibitor saquinavir (daily dose of 1200 mg / 3 times a day) while achieving a constant level, a C max increase of sildenafil by 140% and AUC of sildenafil by 210% is observed. Sildenafil has no effect on the pharmacokinetics of saquinavir. Stronger inhibitors of SUR, ketoconazole and itraconazole, may further inhibit the clearance of sildenafil. Single doses of antacids (magnesium or aluminum hydroxide) do not affect the bioavailability of sildenafil. The inhibitors SUR2S9 (tolbutamide or warfarin) and SUR2D6 (tetracyclic antidepressants), thiazides, ACE inhibitors, calcium antagonists do not affect the pharmacokinetics of sildenafil. AUC dismethylmetabolite sildenafil increases by 62% with the use of loop and potassium-saving diuretics and 102% with non-specific beta-blockers.

- The effect of Dynamic on other drugs Sildenafil is a weak inhibitor of 1A2, 2C9, 2C19, 2B6, 2E1, 3A4 isoenzymes (IC50> 150 mM) of cytochrome P450. With simultaneous use of sildenafil 50 mg or 100 mg with amlodipine 5 mg or 10 mg, an additional decrease in blood pressure of 8/7 mm Hg was observed in patients with hypertension. No significant interaction of sildenafil with tolbutamide and warfarin metabolized by SUR2C9 was noted.Sildenafil (50 and 100 mg) does not increase the bleeding time while being prescribed with aspirin. It also does not potentiate the hypotensive effect of alcohol in healthy volunteers at the maximum alcohol level of 0.08%. Sildenafil also has no effect on HIV protease inhibitors saquinavir and ritonavir, which are substrates of СUR3F4. Sildenafil potentiates the antiplatelet effect of sodium nitroprusside (NO donator). The combination with heparin has an additive effect on bleeding time in anesthetized rabbits, but such effects have not been found in humans.

Special instructions

Before using the drug Dynamic should conduct a thorough examination of the patient in order to diagnose erectile dysfunction and determine its causes. It is necessary to assess the risk of serious adverse reactions due to sexual activity in patients with cardiovascular diseases, as well as concomitant medication. Sildenafil causes a mild decrease in blood pressure. Particularly susceptible to the hypotensive effect of sildenafil patients with left ventricular obstruction or with a rare syndrome of multiple atrophy. Before using sildenafil in these patients, it is necessary to eliminate the risk of adverse effects of low blood pressure during sexual activity. Most adverse reactions of the cardiovascular system develop immediately after intercourse or shortly thereafter, in rare cases, adverse reactions can develop before sexual intercourse.

The simultaneous use of several different medicines for the treatment of erectile dysfunction is not recommended.
Dynamic should be used with caution in patients with anatomical deformities of the penis (angulation, cavernous fibrosis or Peyronie's disease), as well as in patients with diseases that predispose to priapism (sickle cell anemia, myeloma, leukemia).

If a visual impairment occurs, consult a doctor immediately.
Doses of more than 200 mg do not increase efficacy, but they increase the frequency and severity of dose-dependent side effects.
Influence on ability to drive motor transport and control mechanisms

In the event of the development of adverse reactions from the nervous system and sensory organs, patients are advised to refrain from driving and controlling machinery, and also to be careful when engaging in activities that require attention concentration and psychomotor speed.