Certificate of conformity (COC) Dynamico pills 20mg, 1pc

Dynamico pills 20mg, 1pc

$64.00

Active ingredient:	Tadalafil
Dosage form:	Pills
Indications for use:	Erectile dysfunction

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Categories: Genitourinary system, Impotence, Medication

Description
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Composition

1 film-coated tablet contains the Active ingredient: sildenafil citrate-35.12 mg,70.24 mg or 140.48 mg (in terms of sildenafil-25.00 mg,50.00 mg or 100.00 mg, respectively); excipients: microcrystalline cellulose 102.88 mg,205.76 mg or 411.52 mg, croscarmellose sodium 5.25 mg,10.50 mg or 21.00 mg, hypromellose 4.50 mg,9.00 mg or 18.00 mg, colloidal anhydrous silicon dioxide 0.75 mg,1.50 mg or 3.00 mg; magnesium stearate 1.50 mg,3.00 mg or 6.00 mg; film coating: Opadray II 31F58914 white (hypromellose, lactose monohydrate, titanium dioxide, macrogol-4000, sodium citrate) 5.955 mg,11.91 mg or 23.82 mg, indigocarmin E 132 0.045 mg,0.09 mg or 0.18 mg

Pharmacological action

Pharmacotherapy group: The treatment for erectile dysfunction is a PDE5 inhibitor. ATX Code: G04BE03 Pharmacological Properties Pharmacodynamics . The drug for the treatment of erectile dysfunction, restores the disturbed 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 cyclic guanosine monophosphate (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 phosphodiesterase type 5 (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 nitric oxide on this tissue and increases blood flow to the penis. When the NO – cGMP chain is activated during sexual stimulation, inhibition of PDE5 leads to an increase in 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 exceeds that of other known phosphodiesterase 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 PDE5, which is of great importance, since PDE5 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. Absorption: Rapidly absorbed after oral use. The maximum concentration in blood plasma (Cmax) 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. Distributionthe apparent volume of distribution at equilibrium 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 isoenzymes CYP3A4 (main pathway) and CYP2C9 (secondary pathway) of microsomal liver isoenzymes. The main circulating active metabolite is N-demethylmetabolite, whose phosphodiesterase activity is 50% of that of sildenafil, and its plasma concentration reaches 40% of that of sildenafil. N-demethylmetabolite undergoes further metabolism with a half-life of 4 hours. Elimination The total clearance of sildenafil is 41 l/h. The half-life (Ti/2) of sildenafil is 3-5 hours. Inactive metabolites are eliminated by the intestines (80%) and kidneys (13%). Pharmacokinetics in special groups of patients. 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 in the blood plasma that is not bound to proteins 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 area under the concentration-time curve (AUC) for N-demethylmetabolite increased by 73% and 126%, respectively. In patients with severe renal insufficiency (creatinine clearance less than 30 ml/min), Cmax and AUC were increased by 88% and 100%, respectively, and 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; concomitant use of nitric oxide donors or organic nitrates or nitrates in any dosage forms; concomitant use of ritonavir; patients for whom sexual activity is undesirable, including those with severe cardiovascular diseases, such as unstable angina, severe heart failure, life-threatening arrhythmias, hypotension (blood pressure (BP) less than 90/50 mm Hg), arterial hypertension (BP more than 170/100 mm Hg), recently suffered a cerebral circulation disorder or myocardial infarction; patients with loss of vision in one eye due to anterior ischemic optical neuropathy of non-arterial origin (regardless of whether this occurred due to taking a PDE5 inhibitor or not); hereditary retinal degenerative diseases, including retinitis pigmentosa (a smaller proportion of such patients have a genetic disease of retinal PDE); severe liver failure; female gender; age under 18 years. With caution, multiple systemic atrophy syndrome; left ventricular exit tract obstruction, including aortic stenosis, hypertrophic obstructive cardiomyopathy; penile anatomical deformity; priapism; multiple myeloma; leukemia; concomitant use of alpha-blockers; lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Side effects

the incidence of side effects is classified according to the recommendations of the world health organization: very often – at least 10%; often – not less than 1% but < 10%; infrequently – no more than 0.1% but < 1%; rarely – not less than 0.01%, but less than 0.1%; very rarely – less than 0.01%, including isolated cases. 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 I erection. Other: rarely-chest pain, fatigue.

Interaction

Inhibitors of the isoenzymes CYP3A4 and CYP2C9 (ketoconazole, erythromycin, cimitidine) reduce metabolism and increase the concentration of sildenafil in the blood. In this case, treatment with sildenafil begins with a dose of 25 mg.

Concomitant use with ritonavir increases the Cmax of sildenafil by 300%, AUC by 1000% and remains at a high level even one day after taking sildenafil.

Concomitant use with saquinavir increases the Cmax of sildenafil by 140%, and the AUC by 210%.

The pharmacokinetics of ritonavir and saquinavir do not change with sildenafil.

Sildenafil enhances the antiplatelet effect of sodium nitroprusside.

Nicorandil may cause severe hypotension due to its nitrate component when interacting with sildenafil.

Simultaneous use of sildenafil and organic nitrates and other nitric oxide donors can lead to a fatal outcome due to the mutual strengthening of the effects.

Sildenafil enhances the antihypertensive effects of slow calcium channel blockers, beta-blockers, and angiotensin-converting enzyme inhibitors.

When used simultaneously, it increases the effectiveness of hypoglycemic agents.

Azithromycin has no effect on the pharmacokinetics of sildenafil.

With the simultaneous use of sildenafil and alpha-blockers, including doxazosin, especially in the first 4 hours after taking sildenafil, a pronounced decrease in blood pressure and orthostatic hypotension may occur.

Grapefruit juice may moderately increase the concentration of sildenafil in the blood.

How to take it, course of use and dosage

Inside, approximately 1 hour before the planned sexual activity. 50 mg once a day. Depending on the efficacy and tolerability, the dose can be increased to 100 mg or reduced to 25 mg. No dose adjustment is required in patients with mild or moderate renal insufficiency (creatinine clearance 30-80 ml / min). For patients with severe renal insufficiency (creatinine clearance less than 30 ml / min), the first dose is 25 mg. With good tolerance, the dose can be increased to 50 or 100 mg. For elderly patients, the first dose is 25 mg. With good tolerance, the dose can be increased to 50 or 100 mg. For patients with mild or compensated hepatic insufficiency, the first dose is 25 mg. With good tolerance, the dose can be increased to 50 or 100 mg. For patients taking alpha-blockers, the first dose is 25 mg. With good tolerance, the dose can be increased to 50 or 100 mg.

Overdose

Symptoms: with a single dose of the drug up to 800 mg, adverse reactions (headache, hot flashes, dizziness, dyspepsia, nasal congestion, visual impairment) were more pronounced and occurred more often than with conventional doses; doses up to 200 mg increase the frequency, but not the severity of adverse reactiontreatment: symptomatic therapy. Hemodialysis is ineffective.

Special instructions

Before using sildenafil, 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. Sildenafil 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.