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Active ingredients
Molsidomine
Release form
Pills
Composition
Active ingredient: Molsidomine (Molsidomine) Active ingredient concentration (mg): 2
Pharmacological effect
Peripheral vasodilator, antianginal medication from the group of sydnonimine. expands peripheral venous vessels, has antiplatelet, analgesic and antianginal effects. venodilating activity is caused by the release of nitric oxide (no), which stimulates soluble guanylate cyclase, after a series of metabolic transformations, and therefore molsidomine is considered as a donor of no. As a result, there is an accumulation of cGMP, which promotes the relaxation of smooth muscles of the vascular wall (to a greater extent - the veins). a decrease in preload, even without a direct effect on myocardial contractility, leads to the restoration of the relationship between myocardial oxygen demand and admission disturbed by ibd (the oxygen demand decreases by 26%). The drug relieves spasm of the coronary arteries, improves collateral circulation. It increases the tolerance of stress, reduces the number of strokes during exercise. inhibits the early phase of platelet aggregation, reduces the secretion and synthesis of serotonin, thromboxane and other proagregantov. patients with chronic heart failure, reducing preload, reduces the size of the heart chambers. reduces the pressure in the pulmonary artery, reduces the filling of the left ventricle and the tension of the myocardial wall, the stroke volume of the blood. The effect begins 20 minutes after ingestion, reaches a maximum after 0.5-1 h and lasts up to 6 hours. uncharacteristically (unlike nitrates).
Pharmacokinetics
Absorption and distribution After ingestion is almost completely absorbed from the gastrointestinal tract. Bioavailability - 60-70%. Cmax is 4.4 mcg / ml and is reached after 1 hour. When taken orally after a meal, absorption does slow down, but does not decrease (Cmax in the blood plasma is reached 30-60 minutes later than when taken on an empty stomach). The minimum effective plasma concentration of molsidomine is 3-5 ng / ml. Practically does not bind to plasma proteins.Not cumulative. Metabolism and excretion In the liver, it is metabolized to form the pharmacologically active compound SIN-1, (3-morpholino-sidnonimine), from which the highly unstable substance SIN-1a (N-morpholino-N-aminosynonitrile) is formed, releasing NO to form pharmacologically inactive SIN-lc connections During metabolism, other metabolites are also formed. Excreted by the kidneys by 90% (as metabolites), 9% through the intestines. T1 / 2 is 0.85-2.35 hours. Pharmacokinetics in special clinical situations. In severe liver failure (an increase in the bromsulfalein sample to 20-50%), a slowdown in excretion and an increase in the concentration of molsidomine in the blood plasma is noted. It does not cumulate (including in patients with renal failure).
Indications
Prevention of strokes.
Contraindications
- Acute myocardial infarction with arterial hypotension. - Severe arterial hypotension (systolic blood pressure below 100 mm Hg). - Collapse. - Cardiogenic shock. - Low filling pressure of the left ventricle. - Toxic pulmonary edema. - Simultaneous reception of Sildenafil. - Pregnancy. - Lactation period. - Children and adolescents under 18 years of age (efficacy and safety have not been established). - Hypersensitivity to the drug. The drug is prescribed with caution in the following cases: - Transferred hemorrhagic stroke. - Increased intracranial pressure. - Tendency to arterial hypotension. - The elderly. - Patients with glaucoma (especially closed angle). - In violation of cerebral circulation.
Precautionary measures
The drug should be stored in a dry, dark place at a temperature not higher than 25 ° C.
Use during pregnancy and lactation
The use of Sidnofarm contraindicated in pregnancy. If necessary, the appointment of the drug during lactation should abandon breastfeeding.
Dosage and administration
The dosage regimen and the duration of therapy are set individually. The drug is taken orally, regardless of the meal. The pills are swallowed whole, without chewing and squeezed with a sufficient amount of liquid. The drug is prescribed in the initial dose of 1-2 mg (0.5-1 tab.) 2 times / day. With insufficient severity of therapeutic effect, the multiplicity of appointments is increased up to 3 times / day.The maximum daily dose is 6 mg.
Side effects
Since the cardiovascular system: often - a decrease in blood pressure, collapse (with initially elevated blood pressure, the severity of its decline is greater than with initially normal or lowered blood pressure); reddening of the skin of the face, tachycardia. From the side of the central nervous system: headache (usually minor, disappears during further treatment), slowing down the speed of psychomotor reactions (mostly at the beginning of treatment), dizziness. From the side of the digestive system: nausea, loss of appetite, diarrhea. Allergic reactions: skin rash, itching, bronchospasm; rarely - anaphylactic shock.
Overdose
Symptoms: severe headache, marked reduction in blood pressure, tachycardia. Treatment: if necessary, carry out symptomatic therapy.
Interaction with other drugs
Simultaneous use of Sidnofarm with vasodilators, antihypertensive drugs and ethanol increases the severity of the hypotensive effect. With simultaneous use of Sidnopharm with acetylsalicylic acid, its antiaggregant effect is enhanced.
special instructions
The drug is not used to relieve an angina attack. With caution and under the control of blood pressure, prescribe the first dose of the drug, because intense headaches and an excessive decrease in blood pressure with loss of consciousness are possible. Older patients with impaired liver and kidney function and hypotension require dose adjustment. During treatment, alcohol should be avoided. Effects on driving ability and control mechanisms During the period of treatment (especially at the beginning therapy) it is necessary to refrain from driving vehicles and practicing potentially hazardous activities that require increased attention and speed of psychomotor reactions.