Composition, form of production and packaging
Tablets are white or almost white, oblong, biconcave, on both sides engraved "MFG" and stylized letter "h", separated by a risk.
1 tab.
molsidomine 4 mg
Excipients: lactose monohydrate, crospovidone, macrogol 6000, magnesium stearate.
10 pieces. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
Corvaton is an antianginal drug from the sydnonimine group. Molsidomine, as a result of a number of metabolic transformations, releases nitric oxide (NO), which stimulates soluble guanylate cyclase; The accumulation of cGMP causes relaxation of the smooth muscle cells of the vascular wall (mostly veins).
The main mechanism of antianginal action of molsidomine is the reduction of preload in the heart. Molsidomin reduces venous pressure, the end diastolic pressure in the ventricles and pressure in the pulmonary artery. Reduces the need for myocardium in oxygen. Expands large coronary arteries, improves collateral circulation in coronary atherosclerosis. In chronic heart failure under the influence of Corvathon, ventricular dilatation decreases. In addition, the drug inhibits the early phase of platelet aggregation, reduces the release (or synthesis) of serotonin, thromboxane and other factors that promote platelet aggregation.
The action of Corvathon begins about the first 20 minutes after ingestion, the maximum effect is achieved after 30-60 minutes, the duration of action is from 4 to 6 hours.
PHARMACOKINETICS
After oral administration, it is absorbed almost completely from the digestive tract. Bioavailability is 60-70%.
The remaining 30-40% are metabolized in the liver. Molsidomin is metabolized in the liver to form a pharmacologically active compound SIN-1 (3-morpholino-sydnonimine), from which the unstable substance SIN-1A (N-, morpholino-M-aminosinonitrile) forms NO to form a pharmacologically inactive SIN-1C. In the course of metabolism, other metabolites are formed.
The minimum effective concentration of molsidomine in blood plasma is 3-5 ng / ml. Virtually does not bind to plasma proteins.
It is excreted by the kidneys by 90% (in the form of metabolites) and through the intestine (9%); the rest is displayed unchanged. T 1/2 is 0.85-2.35 hours.
Do not cumulate (including in patients with renal insufficiency). With severe hepatic insufficiency (an increase in the bromosulfalein test to 20% -50%), a delay in excretion and an increase in its concentration in the blood plasma was noted.
INDICATIONS
- prevention of angina attacks;
- chronic heart failure (as part of a combination therapy with cardiac glycosides, diuretics).
DOSING MODE
Corvatone tablets should be taken at regular intervals with a sufficient amount of liquid (about 1/2 glass). Tablets can be taken as before, or during or after a meal.
Corvathon is assigned to 1 tab. 1-2 times / day.
If necessary, the dose may be increased to 12-16 mg / day (1 tablet 3-4 times / day).
SIDE EFFECT
From the side of the central nervous system: at the beginning of treatment, sometimes - headache, in rare cases - dizziness.
From the digestive tract: nausea.
From the side of the cardiovascular system: a marked decrease in blood pressure, sometimes up to a collapse.
Other: in rare cases, the development of allergic reactions (skin rash, itching, bronchospasm), slowing the speed of psychomotor reactions is possible. Very rarely - the development of anaphylactic shock.
CONTRAINDICATIONS
- shock;
- Vascular collapse or severe arterial hypotension (systolic blood pressure less than 100 mm Hg);
- lower central venous pressure;
- Pregnancy;
- the period of breastfeeding;
- simultaneous use of phosphodiesterase type 5 inhibitors (PDE 5) - sildenafil, tadalafil, vardenafil - in connection with a high risk of arterial hypotension;
- age up to 18 years;
- Hypersensitivity to molsidomine.
With caution: patients with impaired cerebral circulation, with increased intracranial pressure, with a tendency to arterial hypotension, elderly patients, after myocardial infarction, patients with glaucoma (especially closed-angle).
PREGNANCY AND LACTATION
If it is necessary to prescribe the drug during lactation, breastfeeding should be abandoned.
APPLICATION FOR CHILDREN
Contraindication: age to 18 years.
APPLICATION IN ELDERLY PATIENTS
With caution: elderly patients.
SPECIAL INSTRUCTIONS
Corvathon is not applicable for stopping angina attacks!
Patients with a high risk of developing an antihypertensive reaction should individually approach the dosage of the drug.
In the acute phase of myocardial infarction, Corvaton can be used only after stabilizing the circulation.
With renal failure, the concentration of molsidomine in the blood plasma does not change.
The drug can be combined with other antianginal agents (for example, add to two- or three-component treatment - nitrates, slow calcium channel blockers and beta-adrenoreceptor blockers).
If the liver function is abnormal, only with a marked decrease in it (an increase in the bromsulfalein test to 20-50%) increases the concentration of molsidomine in the blood plasma and the half-life, which may require adjustment of the dose of the drug.
At the time of treatment should be excluded from taking ethanol.
Impact on the ability to drive vehicles and manage mechanisms
During the period of treatment (especially at the beginning) it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
OVERDOSE
Symptoms: severe headache, marked decrease in blood pressure, tachycardia.
Treatment: symptomatic.
DRUG INTERACTION
With the simultaneous appointment of Corvatone with peripheral vasodilators, slow calcium channel blockers, antihypertensive agents and ethanol, the hypotensive effect is enhanced.
With the simultaneous use of Corvatone with acetylsalicylic acid, antiplatelet activity increases.
There is a high risk of developing hypotension with simultaneous use of phosphodiesterase 5 (PDE 5) inhibitors, such as sildenafil, tadalafil, vardenafil. The combined use of PDE5 with molsidomine is contraindicated.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
Store in a dark place at a temperature of no higher than 25 В° C. Keep out of the reach of children. Shelf life - 2 years. Do not use after the expiry date printed on the package.