Dynamico pills 50mg, 12pcs

Composition

Active ingredient:

sildenafil – 50 mg;

Auxiliary substances:

MCC,

hypromellose,

colloidal anhydrous silicon dioxide;

magnesium stearate;

opaday II 31F58914 white,

indigo carmine 73015

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.

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

Nervous system disorders:  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 hearing organ:  infrequently-vertigo, tinnitus; rarely-deafness.

Respiratory system disorders:  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 services:  rarely-chest pain, fatigue.

How to take, course of use and dosage

Inside, approximately 1 hour before the planned sexual activity.

Based on the effect and tolerability of the drug, the dynamic daily dose can be from 25 mg to 100 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 manage mechanisms

In the event of adverse reactions from the nervous system and sensory organs, patients are advised to refrain from driving a car and operating mechanisms, as well as to exercise caution when engaging in activities that require concentration of attention and speed of psychomotor reactions.

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