Description
Release form
Coated tablets.
Packing
In the package 4 pcs.
Pharmacological action
Dynamically – a drug for the treatment of erectile dysfunction. Under the conditions of sexual stimulation, it restores impaired erectile function by increasing blood flow in the penis.
The physiological mechanism of erection involves the release of nitric oxide (NO) in the cavernous body due to sexual arousal. NO activates the enzyme guanylate cyclase, which leads to an increase in the concentration of cGMP. In turn, cGMP causes relaxation of the smooth muscles of blood vessels and, accordingly, the flow of blood into the cavernous body of the penis.
Sildenafil is a selective inhibitor of cGMP-specific type 5 phosphodiesterase (PDE5), which causes the breakdown of cGMP in the cavernous body of the penis. It does not have a direct relaxing effect on the smooth muscles of the cavernous body, but enhances the relaxing effect of NO and increases blood flow in the penis. Upon activation of the NO cGMP chain observed during sexual stimulation, inhibition of PDE5 leads to an increase in the level of cGMP in the cavernous body. The pharmacological effect is achieved only in the presence of sexual stimulation.
The activity of sildenafil in relation to PDE5 is superior to activity against other known phosphodiesterase isoenzymes: PDE6 – 10 times, PDE1 – more than 80 times PDE2 PDE4, PDE7 PDE11 – more than 700 times. Sildenafil is 4,000 times more selective for PDE5 compared to PDE3, which is of great importance, since PDE3 is one of the key enzymes in the regulation of myocardial contractility.
Sildenafil has a mild and short-term hypotensive effect, in most cases without clinical manifestations when taken in recommended doses. The antihypertensive effect is associated with the vasodilating effect of sildenafil due to an increase in the content of cGMP in the smooth muscle membrane of blood vessels.
Contraindications
– Hypersensitivity to the components of the drug.
– Patients who are continuously or intermittently receiving nitric oxide donors, organic nitrates.
Special instructions
Before using the drug Dynamically, a thorough examination of the patient should be carried out in order to diagnose erectile dysfunction and determine the causes of its occurrence. It is necessary to assess the risk of developing serious adverse reactions due to sexual activity, in patients with cardiovascular disease, as well as concomitant medication. Sildenafil causes a mild decrease in blood pressure. Patients with left ventricular obstruction or with rare multiple atrophy syndrome are especially susceptible to the hypotensive effect of sildenafil. Before using sildenafil in such patients, it is necessary to exclude the risk of the adverse effects of low blood pressure during sexual activity. Most adverse reactions from the cardiovascular system develop immediately after sexual intercourse or shortly after it, in rare cases, adverse reactions can develop before sexual intercourse.
The simultaneous use of several different drugs for the treatment of erectile dysfunction is not recommended.
Dynamically 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 predisposing 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 effectiveness, but increase the frequency and severity of dose-dependent side effects.
Influence on the ability to drive vehicles and control mechanisms
In case of adverse reactions from the nervous system and sensory organs, patients are advised to refrain from driving and controlling mechanisms, as well as be careful when engaging in activities, requiring concentration and speed of psychomotor reactions.
Composition
1 tablet contains sildenafil 50 mg.
Dosage and administration of
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 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.
Side effects
From the nervous system: very often – headache often – dizziness infrequently – drowsiness, hypesthesia rarely – stroke, fainting frequency unknown – transient ischemic attack, convulsions, including recurrent.
From the cardiovascular system: often – hot flashes infrequently – palpitations, tachycardia rarely increase or decrease in blood pressure, myocardial infarction, atrial fibrillation, frequency unknown – ventricular arrhythmia, unstable angina, sudden death.
From the side of the organ of vision: often – impaired vision, impaired color perception infrequently – conjunctival damage, lacrimation, increased light perception, impaired vision, transient chromatopsia rarely – redness of the sclera, pain in the eyeballs frequency unknown – anterior ischemic optic neuropathy, vascular occlusion retina, narrowing of visual fields.
On the part of the hearing organ: infrequently – vertigo, tinnitus is rarely deafness.
On the part of the respiratory system: often – nasal congestion rarely – nosebleeds.
From the gastrointestinal tract: often – dyspepsia infrequently – vomiting, nausea, dry oral mucosa.
Allergic reactions: infrequently – skin rash frequency is unknown – Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome).
From the genital organs: frequency is unknown – priapism, prolonged erection.
Other: rarely – chest pain, fatigue.
Drug Interactions
– Effect of other drugs on Dynamically Sildenafil is metabolized by cytochrome P450 isoenzymes (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 a 59% increase in plasma sildenafil concentration when taken together by healthy volunteers. The simultaneous administration of a single dose of 50 or 100 mg of erythromycin, a specific inhibitor of SUR, increases sildenafil by 182%. With the combined use of sildenafil (a single dose of 50 or 100 mg) with the HIV protease inhibitor saquinavir (daily dose of 1200 mg / 3 times a day), against the background of achieving a constant level, there is an increase in C max of sildenafil by 140% and AUC of sildenafil by 210%. Sildenafil has no effect on the pharmacokinetics of saquinavir. More potent SUR inhibitors, ketoconazole and itraconazole can even more inhibit sildenafil clearance. Single doses of antacids (magnesium or aluminum hydroxide) do not affect the bioavailability of sildenafil. SUR2C9 inhibitors (tolbutamide or warfarin) and SUR2D6 (tetracyclic antidepressants), thiazides, ACE inhibitors, calcium antagonists do not affect the pharmacokinetics of sildenafil. The AUC of sildenafil dysmethyl metabolite increases by 62% when using loop and potassium-sparing diuretics and by 102% when using non-specific beta-blockers.
– Effect of Dynamic on other drugs Sildenafil is a weak inhibitor of isoenzymes 1A2, 2C9, 2C19, 2B6, 2E1, 3A4 (IC50> 150mM) cytochrome P450. With the simultaneous use of sildenafil 50 mg or 100 mg with amlodipine 5 mg or 10 mg in patients with hypertension, an additional decrease in blood pressure of 8/7 mm Hg was observed. No significant interaction of sildenafil with tolbutamide and warfarin metabolized by SUR2C9 was noted. Sildenafil (50 and 100 mg) does not increase bleeding time when given simultaneously with aspirin. It also does not potentiate the hypotensive effect of alcohol in healthy volunteers at a maximum alcohol level of 0.08%. Sildenafil also has no effect on the HIV protease inhibitors saquinavir and ritonavir, which are substrates of ¡ £ 3F4. Sildenafil potentiates the antiplatelet effect of sodium nitroprusside (NO donor). The combination with heparin has an additive effect on bleeding time in anesthetized rabbits, but no such effects were found in humans.
Storage conditions
Keep out of the reach of children, at a temperature not exceeding 25 ° C.
The Expiration of
is 3 years.
Deystvuyuschee substances
sildenafil
pharmacy terms and conditions for prescription
Form of Treatment
tablets
