Dilasid

Dilasidom is an antianginal drug that belongs to the subgroup of sydnone imines.

Its active ingredient is molsidomin, and its active metabolic element is linsidomin (SIN1A). The latter has antiplatelet activity and reduces the tone of the smooth muscles of the vascular walls. The antiplatelet effect of molsidomine has clinical significance in the treatment of coronary artery disease. Molsidomin does not lead to the development of tachycardia, which distinguishes it from nitrates. [1]

Indications Dilasid

It is used to treat CHF (in combination with diuretics and SG), as well as to prevent the development of angina attacks.

Release form

The release of the medication is sold in the form of tablets - 30 pieces each inside a cell package; inside the box - 1 package.

Pharmacodynamics

When smooth muscles relax, the venous volume increases, due to which the capacity of the vascular bed increases and venous return decreases - as a result, the filling pressure of both cardiac ventricles decreases. At the same time, the cardiac load is weakened and the properties of hemodynamics in the coronary bloodstream are improved.

With dilatation of large coronary arteries, weakening of the systemic vascular resistance occurs, the tension of the myocardial wall and cardiac load decrease, which reduces the oxygen demand of the myocardium. At the same time, molsidomin dilates the large branches of the coronary arteries and weakens their spasm. [2]

The effect of molsidomine develops after approximately 20 minutes from the moment of oral administration; the maximum effect reaches after 0.5-1 hour. The duration of the therapeutic effect is within 4-6 hours. [3]

Pharmacokinetics

Absorption and distribution processes.

When administered orally, molsidomin is absorbed from the gastrointestinal tract by approximately 90%. The bioavailability index is approximately 65%. Protein synthesis is 11%.

There is no information as to whether molsidomin or its metabolic components can be excreted in mother's milk. Molsidomin does not accumulate inside the body.

Exchange processes.

Intrahepatic biotransformation of molsidomine occurs by an enzymatic method, with the formation of the active metabolic element sydnoneimine-1 (SIN-1); from it SIN-1A - linsidomin is formed non-enzymatically.

Excretion.

Molsidomin is mainly excreted through the kidneys (90-95%; 2% is excreted unchanged) and the intestine (3-4%). The level of systemic clearance of molsidomine is 40-80 l / h, and that of the SIN-1 element is 170 l / h. The half-life of molsidomine is 1.6 hours, and linsidomine is within 1-2 hours.

With liver failure in a severe degree, the term half-life of molsidomine increases - with hepatic cirrhosis, for example, it is approximately 13.1 hours. The half-life of linsidomine also rises to about 7.5 hours.

Dosing and administration

To prevent the development of angina pectoris, you need to use 2-4 mg of the drug, 1-2 times a day. If necessary, the dosage can be increased to 12-16 mg per day (1 tablet of 4 mg, 3-4 times per day).

Elderly people, those with insufficient liver / kidney function or low blood pressure, the dose of the medication should be reduced.

The tablets are taken at regular intervals with plain water (about 0.5 cups). The medication is used regardless of food intake.

• Application for children

It is forbidden to prescribe to children under the age of 18, since there is no data on the safety and therapeutic effect of drugs for this group.

Use Dilasid during pregnancy

You can not use Dilasid during pregnancy (especially in the 1st trimester), as well as breastfeeding.

If it is required to use the medicine for HB, breastfeeding should be abandoned.

Contraindications

The main contraindications:

• collapse or shock;
• a strong decrease in blood pressure (systolic blood pressure indicators less than 100 mm Hg);
• decrease in the values of venous central pressure;
• weak left ventricular filling pressure;
• active form of myocardial infarction;
• use together with substances that slow down PDE-5, including tadalafil and sildenafil with vardenafil (since this increases the likelihood of lowering blood pressure);
• severe intolerance to molsidomine.

Caution is required when using drugs in case of glaucoma (especially angle-closure), cerebral blood flow disorder, increased ICP values, and in addition to people with a tendency to lower blood pressure levels, the elderly, with liver / kidney failure and after an active form of myocardial infarction.

Side effects Dilasid

Among the side effects:

• dysfunction of the CVS: a strong drop in blood pressure, sometimes reaching collapse, as well as orthostatic hypotension;
• problems with the work of the central nervous system: at the beginning of therapy, cephalalgia sometimes develops, occasionally dizziness is observed. Motor and mental reactions may slow down (mainly at the beginning of therapy);
• digestive disorders: nausea;
• allergy symptoms: itching, facial hyperemia, bronchospasm. Epidermal eruptions and anaphylactic shock are sporadic.

Overdose

Manifestations of intoxication: tachycardia, severe cephalalgia and a marked decrease in blood pressure values.

If less than 60 minutes have elapsed since the use of an increased dosage of drugs, the option with gastric lavage should be considered. In addition, symptomatic procedures are performed.

Interactions with other drugs

With a combination of molsidomine and drugs that block slow Ca channels, peripheral vasodilators, ethyl alcohol and antihypertensive substances, the hypotensive effect is potentiated.

The combination of Dilasidom and aspirin potentiates the antiplatelet effect.

There is a high probability of a decrease in blood pressure values when the drug is combined with PDE-5 inhibitors (for example, tadalafil, sildenafil or vardenafil), so they cannot be used together.

Storage conditions

Dilasidom should be stored in a dark and dry place, out of the reach of small children. Temperature indicators are in the range of 15-25 ° C.

Shelf life

Dilasidom can be used for a 36-month term from the date of manufacture of the medicinal substance.

Analogs

Analogs of the medication are Sidocard, Advocaard, Sidnopharm with Molsikor, Solmidon and Sidnokard.