Sydnopharm, tablets 2 mg 30 pcs

Pharmacodynamics

Sydnopharm has venodilator, antiaggregant, analgesic and antianginal action. Venodilator activity is due to the release of nitric oxide (N0), stimulating soluble guanylate cyclase, after a series of metabolic transformations, in this regard, molcidamine is considered as a “donator” of N0. Accumulation of cGMP causes relaxation of smooth muscle cells of the vascular wall (mostly veins).

The reduction of preload, even without direct effect on myocardial contractility, leads to restoration of the disturbed in patients with coronary insufficiency correlation between oxygen demand and oxygen supply (oxygen demand decreases by 26%).

May widen the sections of the coronary arteries capable of vasodilation, improves collateral circulation.Increases exercise tolerance, reduces the number of angina attacks that occur during exercise. Suppresses the early phase of platelet aggregation, reduces the release and synthesis of serotonin, thromboxane and other proaggregants.

In patients with chronic heart failure, by reducing the preload, it helps to reduce the size of the heart chambers. It reduces the pressure in the pulmonary artery, decreases left ventricular filling and myocardial wall tension, blood stroke volume. The action begins 20 minutes after oral administration, reaches a maximum in 0.5-1 hour and lasts up to 6 hours. Unlike nitrates, the development of tolerance with a decrease in efficacy during long-term therapy is uncharacteristic.

Pharmacokinetics

After oral administration, Sydnopharm is almost completely absorbed from the gastrointestinal tract. Bioavailability is 60-70%. Maximum concentration is reached (4.4 mcg/ml) -1 hour. When taken orally after a meal, absorption, although slower, is not reduced (maximum plasma concentration is reached 30-60 minutes later than when taken on an empty stomach).

The minimum effective concentration of molcidomine in blood plasma is 3-5 ng/ml. It is practically not bound to plasma proteins. It is metabolized in liver with formation of pharmacologically active compound SIN-1, (3-morpholino-sidnonimine), from which very unstable substance SIN-la (N-morpholino-N-aminosinonitrile) is formed, which releases NO with formation of pharmacologically inactive compound SIN-lc. Other metabolites are also formed during metabolism.

It is excreted by the kidneys by 90% (as metabolites), 9% – through the intestine. The elimination half-life is 0.85-2.35 hours. It does not cumulate (including in patients with renal insufficiency). In severe hepatic insufficiency (increase of bromsulfalein test up to 20-50%) retardation of excretion and increase of its concentration in blood plasma were noted.

Indications

Prevention of angina attacks.

Pharmacological effect

Pharmacodynamics

Sidnopharm has venodilating, antiplatelet, analgesic and antianginal effects. Venodilating activity is due to the release of nitric oxide (NO) after a series of metabolic transformations, stimulating soluble guanylate cyclase; therefore, molsidamine is considered as a “donor” of NO. The accumulation of cGMP causes relaxation of the smooth muscle cells of the vascular wall (mostly veins).

A decrease in preload, even without a direct effect on myocardial contractility, leads to the restoration of the relationship between the need for oxygen and its supply that is disturbed in patients with coronary insufficiency (the need for oxygen decreases by 26%).

It can expand the narrowed sections of the coronary arteries that are capable of vasodilation, improves collateral circulation. Increases exercise tolerance, reduces the number of angina attacks that occur during physical activity. Suppresses the early phase of platelet aggregation, reduces the release and synthesis of serotonin, thromboxane and other proaggregants.

In patients with chronic heart failure, by reducing preload, it helps to reduce the size of the heart chambers. Reduces pressure in the pulmonary artery, reduces filling of the left ventricle and tension of the myocardial wall, stroke volume of blood. The action begins 20 minutes after ingestion, reaches a maximum after 0.5-1 hour and lasts up to 6 hours. Unlike nitrates, the development of tolerance with decreased effectiveness during long-term therapy is uncommon.

Pharmacokinetics

After oral administration, Sidnopharm is almost completely absorbed from the gastrointestinal tract. Bioavailability – 60-70%. The maximum concentration is reached (4.4 μg/ml) within 1 hour. When taken orally after a meal, although absorption slows down, it does not decrease (the maximum concentration in the blood plasma is reached 30-60 minutes later than when taken on an empty stomach).

The minimum effective concentration of molsidomine in blood plasma is 3-5 ng/ml. Practically does not bind to blood plasma proteins. It is metabolized in the liver to form the pharmacologically active compound SIN-1, (3-morpholino-sydnonimine), from which a very unstable substance SIN-la (N-morpholino-N-aminosyntonitrile) is formed, which releases NO with the formation of the pharmacologically inactive compound SIN-lc. During metabolism, other metabolites are also formed.

90% is excreted by the kidneys (in the form of metabolites), 9% through the intestines. The half-life is 0.85 – 2.35 hours. It does not accumulate (including in patients with renal failure). In severe liver failure (increase in bromsulfalein test to 20-50%), a slowdown in excretion and an increase in its concentration in the blood plasma are noted.

Special instructions

Do not use Sidnopharm to relieve angina attacks!

The first dose of the drug is prescribed with caution (and under blood pressure monitoring), intense headaches and an excessive decrease in blood pressure with loss of consciousness are possible.

Elderly patients with impaired liver and kidney function and arterial hypotension require dose adjustment.

During treatment, ethanol intake should be avoided.

If it is necessary to prescribe the drug during lactation, breastfeeding should be avoided.

During the treatment period (especially at the beginning), it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Molsidomin

Composition

1 tablet contains:

active ingredient:

Molsidomine 2.00 mg.

excipients:

lactose,

wheat starch,

mannitol,

colloidal silicon dioxide,

magnesium stearate,

hydroxypropyl methylcellulose,

mint oil,

dye “Sunset yellow”,

microcrystalline cellulose.

Pregnancy

The use of Sidnofarm is contraindicated during pregnancy.

If it is necessary to prescribe the drug during lactation, breastfeeding should be avoided.

Contraindications

Hypersensitivity to the drug Sidnopharm,
severe arterial hypotension (systolic blood pressure below 100 mmHg),
collapse,
cardiogenic shock,
low left ventricular filling pressure,
acute myocardial infarction occurring with arterial hypotension,
toxic pulmonary edema,
simultaneous use of sildenafil,
pregnancy,
lactation period,
age under 18 years (efficacy and safety have not been established).

With caution
Patients who have suffered a hemorrhagic stroke, with increased intracranial pressure, patients prone to arterial hypotension; old age, glaucoma (especially angle-closure), cerebrovascular accident.

Side Effects

Headache (usually minor, disappears with further treatment); decrease in blood pressure, collapse (with initially high blood pressure (BP), the severity of its decrease is greater than with initially normal or low blood pressure);
redness of the facial skin;
slowing down the speed of mental and motor reactions (to a greater extent at the beginning of treatment);
dizziness;
nausea, loss of appetite, diarrhea;
tachycardia;
allergic reactions (skin rash, itching, bronchospasm, rarely – anaphylactic shock).

Interaction

When Sidnopharm is prescribed simultaneously with other vasodilators, antihypertensive drugs and ethanol, the severity of the hypotensive effect increases.

Acetylsalicylic acid enhances antiplatelet activity.

Overdose

Symptoms: severe headaches, marked decrease in blood pressure, tachycardia.

Treatment: symptomatic.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 ° C.

Shelf life

3 years.

Manufacturer

Sopharma JSC, Bulgaria