Dynamico, pills 100mg 1pc

Composition

Active ingredient:

sildenafil 100 mg

Pharmacological action

Dynamic-inhibitory PDE-5 that improves erectile function.

Pharmacodynamics

A drug for the treatment of erectile dysfunction. Restores impaired erectile function under conditions of sexual stimulation by increasing blood flow in the penis.

The physiological mechanism of erection involves the release of nitric oxide (NO) in the corpus cavernosum 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 the blood vessels and, accordingly, blood flow to the cavernous body of the penis.

Sildenafil is a selective inhibitor of cGMP-specific PDE5, which causes the breakdown of cGMP in the corpus cavernosum of the penis. It does not have a direct relaxing effect on the smooth muscles of the cavernous body, but it enhances the relaxing effect of NO and increases blood flow in the penis. When the NO–cGMP chain is activated during sexual stimulation, inhibition of PDE5 leads to an increase in cGMP levels in the cavernous body. The pharmacological effect is achieved only in the presence of sexual stimulation.

The activity of sildenafil in relation to PDE5 exceeds that of other known PDE isoenzymes: PDE6-by 10 times, PDE1-by more than 80 times; PDE2–PDE4, PDE7–PDE11-by more than 700 times. Sildenafil is 4000 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 antihypertensive effect, which in most cases does not have a clinical manifestation when taken at the recommended doses. The hypotensive 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.

Pharmacokinetics

Suction

After ingestion, it is rapidly absorbed. Cmax in blood plasma when taken on an empty stomach is reached within 0.5-2 hours, bioavailability is on average 41% (25-63%). When taken with food Cmax decreases by 20-40% and is reached in 1.5-3 hours.

Distribution

The apparent Vss is 105 liters. The association of sildenafil and its main active metabolite with plasma proteins is 96% of the administered dose and is not dose-dependent.

Metabolism

Sildenafil is mainly metabolized by the microsomal liver isoenzymes CYP3A4 (main pathway) and CYP2C9 (secondary pathway). The main circulating active metabolite is N-demethylmetabolite, whose activity against PDE is 50% of the activity of sildenafil, and its plasma concentration reaches 40% of the concentration of sildenafil. N-demethylmetabolite undergoes further metabolism with T1/2 4 h.

Deduction

The total clearance of sildenafil is 41 l/h. T 1/2 of sildenafil is 3-5 h. Inactive metabolites are excreted by the intestine (80%) and kidneys (13%).

Special patient groups

In patients over 65 years of age, the Cmax of sildenafil and its active metabolite is increased by approximately 90% compared to patients 18-45 years of age due to reduced clearance of sildenafil. The concentration of sildenafil, which is not bound to proteins in blood plasma, is 40%. In patients with moderate renal insufficiency (creatinine clearance 30-80 ml/min), the pharmacokinetics of sildenafil did not change with 50 mg, and the Cmax and AUC for N-demethylmetabolite increased by 73 and 126%, respectively. In patients with severe renal insufficiency (creatinine clearance less than 30 ml / min) The cmax and AUC of sildenafil were increased by 88 and 100%, respectively, and the cmax and AUC of N-demethylmetabolite were increased by 79 and 200%, respectively.

In patients with cirrhosis of the liver (Child-Pugh class A and B) Cmax and AUC were increased by 47 and 84%, respectively.

Indications

Treatment of erectile dysfunction, characterized by the inability to achieve or maintain a penile erection sufficient for satisfactory sexual intercourse.

It is effective only for sexual stimulation.

Use during pregnancy and lactation

Dynamiko is not intended for use in women

Contraindications

• hypersensitivity to sildenafil or any other component of the drug;
• simultaneous reception of donators of nitric oxide or organic nitrates or nitrates in any dosage forms;
• simultaneous reception of ritonavir;
• patients for whom sexual activity is undesirable, including severe cardiovascular diseases such as unstable angina, severe heart failure, life-threatening arrhythmias, hypotension (BP less than 90/50 mm Hg. article), hypertension (blood pressure more than 170/100 mm Hg. calendar);
• recent cerebrovascular accident or myocardial infarction;
• patients with loss of vision in one eye due to anterior ischemic optic neuropathy partitioning Genesis (regardless of whether it happened as a result of taking PDE 5 inhibitor or not);
• hereditary degenerative retinal disorders, including retinitis pigmentosa (a small number of such patients is genetically determined dysfunction of the PDE of the retina);
• severe hepatic insufficiency;
• female gender;
• age to 18 years.

With caution:  multiple systemic atrophy syndrome; left ventricular exit tract obstruction, including aortic stenosis; hypertrophic obstructive cardiomyopathy; anatomical deformity of the penis; priapism; multiple myeloma; leukemia; simultaneous use of alpha-blockers; lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

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 ones.

From the cardiovascular system: often-hot flashes; infrequently-palpitation, tachycardia; rarely-increased or decreased blood pressure, myocardial infarction, atrial fibrillation; frequency unknown-ventricular arrhythmia, unstable angina, sudden death.

From the side of the visual organ: often-visual impairment, color perception disorder; infrequently-conjunctival damage, lacrimation disorder, increased light perception, visual clarity disorder, transient chromatopsia; rarely-reddening of the sclera, pain in the eyeballs; frequency unknown-anterior ischemic optical neuropathy, retinal vascular occlusion, narrowing of the visual fields.

From the side of the organ of hearing: infrequently-vertigo, tinnitus; rarely-deafness.

From the respiratory system: often-nasal congestion; rarely-nosebleeds.

From the gastrointestinal tract: often-dyspepsia; infrequently-vomiting, nausea, dryness of the oral mucosa.

Allergic reactions: infrequently-skin rash; frequency unknown-Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome).

From the genitals: frequency unknown-priapism, prolonged erection.

Other: rarely-chest pain, fatigue.

Interaction

– The effect of other drugs on the dynamics of Sildenafil is metabolized by cytochrome P450 (SUR) isoenzymes,3A4 (mainly) and 2C9 (minimally), so inhibitors of these enzymes can reduce the clearance of sildenafil. Cimetidine (800 mg), a specific anionic inhibitor of SUR, causes a 59% increase in the concentration of sildenafil in plasma when taken together in healthy volunteers.

Concomitant use of a single dose of 50 or 100 mg of erythromycin, a specific inhibitor of SUR, increases the AUC of sildenafil by 182%. When sildenafil is co-administered (a single dose of 50 or 100 mg) with the HIV protease inhibitor saquinavir (a daily dose of 1200 mg / 3 times a day) against the background of achieving a constant level, an increase in the cmax of sildenafil by 140% and the AUC of sildenafil by 210% is observed.

Sildenafil does not affect the pharmacokinetics of saquinavir. Stronger SUR inhibitors ketoconazole and itraconazole may further inhibit sildenafil clearance. Single doses of antacids ( magnesium or aluminum hydroxide) do not affect the bioavailability of sildenafil. CYP2C9 inhibitors (tolbutamide or warfarin) and CYP2D6 (tetracyclic antidepressants), thiazides, ACE inhibitors, and calcium antagonists do not affect the pharmacokinetics of sildenafil. The AUC of sildenafil dismethylmetabolite increases by 62% when using loop and potassium-sparing diuretics and by 102% when using non-specific beta-blockers.

– Dynamic effect on other drugs Sildenafil is a weak inhibitor of cytochrome P 450 isoenzymes 1 A 2,2 C 9,2 C 19,2 B 6,2 E 1,3 A 4 (IC50>150 mM). When sildenafil 50 mg or 100 mg was co-administered with amlodipine 5 mg or 10 mg in hypertensive patients, an additional decrease in blood pressure of 8/7 mm Hg was observed. There was no significant interaction of sildenafil with tolbutamide and warfarin, metabolized by SUR 2 with 9.

Sildenafil (50 and 100 mg) does not increase bleeding time when co-administered 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 the HIV protease inhibitors saquinavir and ritonavir, which are substrates of SUR 3F4. Sildenafil potentiates the antiplatelet effect of sodium nitroprusside (a NO donor). The combination with heparin has an additive effect on bleeding time in anaesthetized rabbits, but no such effects have been found in humans.

How to take, course of use and dosage

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

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

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

Special instructions

Before using the drug Dynamico, 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 serious adverse reactions due to sexual activity in patients with cardiovascular diseases, as well as concomitant use of medications. Sildenafil causes a mild decrease in blood pressure. Patients with left ventricular obstruction or rare multiple atrophy syndrome are particularly susceptible to the hypotensive effect of sildenafil. Before using sildenafil in such patients, it is necessary to exclude the risk of adverse effects of low blood pressure during sexual activity. Most adverse reactions from the cardiovascular system develop immediately after sexual intercourse or a short time after it, in some cases, adverse reactions may develop before sexual intercourse. The simultaneous use of several different medications for the treatment of erectile dysfunction is not recommended. Dynamico 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 defect occurs, you should immediately consult a doctor. Doses of more than 200 mg do not increase the effectiveness, but increase the frequency and severity of dose-dependent side effects. Influence on the ability to drive motor vehicles and control mechanisms In case of adverse reactions from the nervous system and sensory organs, patients are advised to refrain from driving a car and controlling mechanisms, as well as to exercise caution when engaging in activities that require concentration of attention and speed of psychomotor reactions.

Form of production

Tablets

Storage conditions

Keep out of reach of children, at a temperature not exceeding 25°C.

Shelf

life is 3 years.

Active ingredient

Sildenafil

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For men, For adults as prescribed by a doctor

Indications

Erectile Dysfunction