Has venodilatiruyuschee, antiplatelet, analgesic and anti-anginal action. Venodilatiruyuschaya activity after release due to a number of metabolic conversions of nitrogen oxide , stimulating soluble guanylate cyclase, thereby molsidamin considered “donator” . The accumulation of cGMP causes the relaxation of smooth muscle cells of the vascular wall (to a greater extent – the veins). Reduced preload, even without a direct effect on myocardial contractility, leading to the restoration of impaired in patients with coronary insufficiency ratio between the demand for oxygen and its intake (26% reduced oxygen demand). Can expand capable of vasodilation narrowed sections of coronary arteries, improves tolerability krovoobraschenie.Uvelichivaet collateral loads, reduces the number of angina attacks that occur during exercise. Suppresses the early phase of platelet aggregation, reduces isolation and synthesis of serotonin, thromboxane and other proagregantov. In patients with chronic heart failure, reducing preload, it helps to reduce halotestin results the size of the heart chambers. It reduces pressure in the pulmonary artery, reduces the filling of the left ventricle and myocardial wall stress, stroke volume. The action starts after 20 min after oral administration, reaching a peak after halotestin cycle hours and lasts up to six hours. In contrast to nitrate, development of tolerance with a decrease in effectiveness during prolonged therapy is unusual.
After oral administration almost completely absorbed from the gastrointestinal tract. Bioavailability – 60-70%. The maximum concentration is achieved (4.4 ug / ml) -1ch. When administered after food intake although slowing, but not reduced (maximum plasma concentration is reached 30-60 minutes later than in the fasting state). The minimum effective concentration of molsidomine in plasma of 3-5 ng / ml. Almost does not bind to plasma proteins. The liver is metabolized to pharmacologically active compound SIN-1 (3-morpholino-sydnonimine), which is formed from a very unstable substance SIN-la (N-morpholino-N-aminosintonitril) releasing to form pharmacologically inactive compounds SIN-lc. And other metabolites halo cycle are produced during the metabolism. Excreted by the kidneys by 90% (in the form of metabolites), 9% – via the intestine. Thehalotestin cycle accumulates (including in patients with renal insufficiency). In severe hepatic impairment (increased bromsulfaleinovoy samples up to 20-50%) observed slowing clearance and an increase in its concentration in blood plasma.
Contraindications: Hypersensitivity to the drug, severe hypotension (systolic blood pressure below 100 mm Hg), collapse, cardiogenic shock, low pressure filling of the left ventricle, acute myocardial infarction, flowing with arterial hypotension, toxic pulmonary edema, concomitant use of sildenafil, bsrsmsnnost, lactation, age 18 years (effectiveness and safety have been established).
Be wary of patients after suffering a hemorrhagic stroke, with increased intracranial pressure, patients prone to hypotension; older age, glaucoma (especially the closure), cerebrovascular accident.
Dosing and Administration Inside, regardless of meals. Tablets are swallowed whole, without chewing and drinking plenty of fluids. With the lack of expression of the therapeutic effect of the multiplicity of purposes increased to 3 times a day. The maximum daily dose of 6 mg. The dosage and duration halotestin cycle of treatment is determined individually.
Side effects Headache (usually slight, disappears in the course of further treatment); decrease in blood pressure, collapse (when the initially high blood pressure (BP), the severity of its decline is greater than the initially normal or reduced blood pressure); redness of the skin; slowing of mental and motor reactions (mainly at the beginning of the treatment); dizziness; nausea, loss of appetite, diarrhea; tachycardia; allergic reactions (skin rash, pruritus, bronchospasm, rarely – anaphylactic shock).
Overdose Symptoms: severe headaches, marked reduction of blood pressure, tachycardia. Treatment: symptomatic.
Interaction with other drugs severity of the hypotensive effect enhanced by the simultaneous administration with other vasodilators, antihypertensive drugs and ethanol. Aspirin increases the antiplatelet activity.
Cautions Do not use for halotestin cycle the relief of angina attacks! Be wary (and under the control of blood pressure) appoint the first dose, there may be intense headaches and excessive reduction of blood pressure with loss of consciousness. Elderly patients with impaired liver and kidney function and arterial hypotension require dose adjustment. At the time of treatment should be deleted reception of ethanol. If necessary, the appointment during lactation should abandon breastfeeding. During treatment (especially in the beginning) should refrain from vehicles and Occupation of driving potentially hazardous activities that require high concentration and psychomotor speed reactions.
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