Dynamico, 100 mg 12 pcs

Dinamico is an FDE-5 inhibitor that improves erectile function.

Pharmacodynamics

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

The physiological mechanism of erection involves 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 cGMP concentration. In turn, cGMP causes smooth muscles of blood vessels to relax and, accordingly, the flow of blood into the cavernous body of the penis.

Sildenafil is a selective inhibitor of cGMP-specific FDE5, 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 it enhances the relaxing effect of NO and increases blood flow in the penis. During activation of NO-cGMF chain, observed during sexual stimulation, inhibition of FDE5 leads to an increase of cGMF level in the cavernous body. The pharmacological effect is achieved only in the presence of sexual stimulation.

The activity of sildenafil in relation to FDE5 is superior to other known FDE isoenzymes: FDE6 – 10 times, FDE1 – more than 80 times; FDE2-FDE4, FDE7-FDE11 – more than 700 times. Sildenafil is 4,000 times more selective against FDE5 compared with FDE3, which is important because FDE3 is one of the key enzymes regulating myocardial contractility.

Sildenafil has a mild and short-lived hypotensive effect, in most cases with no clinical manifestation when taken at recommended doses. The hypotensive effect is due to the vasodilatory effect of sildenafil due to an increase in cGMP in the vascular smooth muscle membrane.

Pharmacokinetics

Intake

After oral administration is rapidly absorbed. Cmax in 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 is decreased by 20-40% and is reached after 1.5-3 hours.

Distribution

The apparent Vss is 105L. The binding of sildenafil and its main active metabolite to plasma proteins is 96% of the administered dose and is not dose dependent.

Metabolism

Sildenafil is metabolized mainly by the microsomal liver isoenzymes CYP3A4 (main route) and CYP2C9 (additional route). The main circulating active metabolite is N-demethylmetabolite, which has activity against FDE of 50% of sildenafil activity and its plasma concentration reaches 40% of sildenafil concentration. N-demethylmetabolite is further metabolized with a T1/2 of 4 hours.

The total clearance of sildenafil is 41 l/h. The T1/2 of sildenafil is 3-5 hours. Inactive metabolites are excreted by the intestine (80%) and the kidneys (13%).

Particular groups of patients

In patients older than 65 years the Cmax of sildenafil and its active metabolite is increased by approximately 90% compared to patients 18-45 years due to decreased clearance of sildenafil. The concentration of sildenafil not bound to plasma proteins is 40%. In patients with moderate renal impairment (creatinine Cl 30-80 ml/min), the pharmacokinetics of sildenafil is unchanged when taking 50 mg, and the Cmax and AUC for N-demethylmetabolite are increased by 73 and 126%, respectively. In patients with severe renal impairment (creatinine Cl less than 30 ml/min), the Cmax and AUC of sildenafil are increased by 88 and 100%, respectively, and the Cmax and AUC of N-demethylmetabolite are increased by 79 and 200%, respectively.

In patients with cirrhosis (Child-Pugh grades A and B), Cmax and AUC are increased by 47% and 84%, respectively.

Indications

The treatment of erectile dysfunction characterized by the inability to achieve or maintain an erection of the penis sufficient for satisfactory intercourse.

Effective only with sexual stimulation.

Active ingredient

Composition

The active ingredient:

sildenafil – 100 mg;

Excipients:

MCC,

Hypromellose,

Silicon dioxide colloidal anhydrous;

magnesium stearate;

opadia II 31F58914 white,

indigo carmine 73015

How to take, the dosage

Ingestion, about 1 hour before planned sexual activity.

Dynamico’s daily dose can be between 25 mg and 100 mg, depending on its effect and tolerability.

It is recommended that the drug be taken no more than once a day.

Special Instructions

Before using Dynamico, the patient should be thoroughly examined to diagnose erectile dysfunction and to determine the cause of the dysfunction. The risk of serious adverse reactions due to sexual activity should be assessed in patients with cardiovascular disease and concomitant medication. Sildenafil causes a mild decrease in BP.

Particularly susceptible to the hypotensive effects of sildenafil are patients with left ventricular obstruction or rare multiple atrophy syndrome. Before using sildenafil in such patients, the risk of adverse effects of low BP during sexual activity should be excluded. Most adverse cardiovascular reactions develop immediately after sexual intercourse or a short time thereafter; in single cases, adverse reactions may develop before sexual intercourse.

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

In case of visual defects, you should immediately consult a physician.
Doses greater than 200 mg do not increase efficacy, but increase, the frequency and severity of dose-dependent side effects.
Effect on driving and operating machinery

In case of adverse reactions from the nervous system and sensory organs, patients are advised to refrain from driving and operating machinery, and to exercise caution when engaging in activities requiring concentration and quick psychomotor reactions.

Contraindications

Side effects

Nervous system: very common – headache; common – dizziness; infrequent – somnolence, hypoesthesia; rare – stroke, fainting; frequency unknown – transient ischemic attack, seizures, including recurrent.

Cardiovascular system: frequent – “flushes”; infrequent – palpitations, tachycardia; rare – increase or decrease in blood pressure, myocardial infarction, atrial fibrillation; frequency unknown – ventricular arrhythmia, unstable angina, sudden death.

An organ of vision: often – visual impairment, impaired color perception; infrequent – conjunctival damage, impaired lacrimation, increased perception of light, impaired visual clarity, transient chromatopsia; rarely – redness of sclerae, pain in the eyeballs; frequency unknown – ischemic anterior optical neuropathy, retinal vascular occlusion, narrowed visual fields.

Hearing organ: infrequent – vertigo, tinnitus; rarely – deafness.

Respiratory system: often – nasal congestion; rarely – nasal bleeding.

Gastro-intestinal tract: often – dyspepsia; infrequent – vomiting, nausea, dry mouth.

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

Genital organs: frequency unknown – priapism, prolonged erection.

Others: rare – chest pain, fatigue.

Similarities