Dilasidom

Dilasid is an antianginal drug that belongs to the sydnone imine subgroup.

Its active component is molsidomine, and its active metabolic element is linsidomine (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 heart disease. Molsidomine does not lead to the development of tachycardia, which distinguishes it from nitrates. [ 1 ]

Indications Dilasidom

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 drug is released in the form of tablets - 30 pieces in a cell package; 1 package in a box.

Pharmacodynamics

When smooth muscles relax, venous volume increases, which increases the capacity of the vascular bed and reduces venous return - as a result, the filling pressure of both ventricles decreases. At the same time, cardiac load is reduced and hemodynamic properties in the coronary blood flow are improved.

When large coronary arteries are dilated, the OPSS is weakened, the tension of the myocardial wall and cardiac load are reduced, which reduces the oxygen demand of the myocardium. At the same time, molsidomine dilates large branches of the coronary arteries and weakens their spasm. [ 2 ]

The effect of molsidomine develops approximately 20 minutes after oral administration; maximum effect is achieved 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, molsidomine is absorbed from the gastrointestinal tract by approximately 90%. The bioavailability index is approximately 65%. Protein synthesis is 11%.

There is no information on whether molsidomine or its metabolic components can be excreted in human milk. Molsidomine does not accumulate in the body.

Exchange processes.

Intrahepatic biotransformation of molsidomine occurs enzymatically, with the formation of the active metabolic element sydnonimine-1 (SIN-1); from it, SIN-1A – linsidomine – is formed non-enzymatically.

Excretion.

Molsidomine is excreted mainly via the kidneys (90-95%; 2% is excreted unchanged) and intestines (3-4%). The systemic clearance rate of molsidomine is 40-80 l/hour, and that of SIN-1 is 170 l/hour. The half-life of molsidomine is 1.6 hours, and that of linsidomine is within 1-2 hours.

In severe liver failure, the half-life of molsidomine increases – in liver cirrhosis, for example, it is approximately 13.1 hours. The half-life of linsidomine also increases to approximately 7.5 hours.

Dosing and administration

To prevent the development of an angina attack, it is necessary 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 a day).

For elderly people, people with liver/kidney failure or low blood pressure, the dosage of the medicine should be reduced.

The tablets are taken at equal time intervals, washed down with plain water (approximately 0.5 glass). The medication is used regardless of food intake.

• Application for children

It is prohibited to prescribe to children under 18 years of age, since there is no data regarding the safety and therapeutic effect of the drug for this group.

Use Dilasidom during pregnancy

Dilasid should not be used during pregnancy (especially in the first trimester) or breastfeeding.

If it is necessary to use the medicine during breastfeeding, breastfeeding should be discontinued.

Contraindications

Main contraindications:

• collapse or shock;
• a strong decrease in blood pressure (systolic blood pressure readings less than 100 mm Hg);
• decrease in central venous pressure values;
• 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 the drug in cases of glaucoma (especially closed-angle), cerebral blood flow disorders, increased intracranial pressure, and in addition to this, in individuals with a tendency to decrease blood pressure, in the elderly, with liver/kidney failure, and after an active form of myocardial infarction.

Side effects Dilasidom

Side effects include:

• dysfunction of the cardiovascular system: a sharp drop in blood pressure, sometimes leading to collapse, as well as orthostatic hypotension;
• problems with the central nervous system: at the beginning of therapy, cephalgia sometimes develops, dizziness is observed occasionally. Motor and mental reactions may slow down (mainly at the beginning of therapy);
• digestive disorders: nausea;
• Allergy symptoms: itching, facial hyperemia, bronchial spasm. Epidermal rashes and anaphylactic shock are observed sporadically.

Overdose

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

If less than 60 minutes have passed since the intake of an increased dose of the drug, the option of gastric lavage should be considered. In addition, symptomatic procedures are performed.

Interactions with other drugs

When molsidomine is combined with agents that block slow Ca channels, peripheral vasodilators, ethyl alcohol and antihypertensive agents, the hypotensive effect is potentiated.

The combination of Dilasidom and aspirin potentiates the antiplatelet effect.

There is a high risk of lowering blood pressure values when combining the drug with PDE-5 inhibitors (eg, tadalafil, sildenafil or vardenafil), so they should not be used together.

Storage conditions

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

Shelf life

Dilasid can be used for a period of 36 months from the date of manufacture of the medicinal substance.

Analogues

Analogues of the drug are Sidocard, Advocard, Sidnofarm with Molsicor, Solmidon and Sidnocard.