Molsidomine

Molsidomine is an active substance from the family of nitrovasodilators, a group of drugs that are broken down in the smooth muscle of the vessels of the large and small circulation and the draining urinary and biliary tracts, thereby releasing NO (NO donors). Nitrovasodilators are basic therapeutics for coronary heart disease. Due to its vasodilating effect, molsidomine is suitable for the long-term treatment and prevention of angina pectoris.

All therapeutically applied nitrovasodilators develop their antiischemic efficacy uniformly via the same mechanism. They release radical NO, albeit via different bioactivation pathways. NO has the greatest relaxation effect where there is the greatest lack of physiological NO. Coronary angiographic studies in humans have also confirmed that coronary vessel segments that are arteriosclerotically altered react particularly strongly to organic nitro compounds. There appears to be an inverse correlation between the amount of NO formed, which is normally necessary for dilation, and the reaction to organic nitro compounds. Improvement of myocardial function and increase of oxygen supply for poorly perfused parts of the myocardium.

Molsidomine is an active ingredient for the long-term treatment and prevention of angina pectoris. Molsidomine itself does not have a vasodilating effect, it is a prodrug which is metabolized in the liver into linsidomine and ultimately converted into the unstable substance sydnonimine. During this metabolisation, nitric oxide is released, which has a vasodilating effect against angina pectoris. As a result of the metabolism, molsidomine is not suitable for the treatment of acute attacks of angina pectoris because the vasodilating effect only sets in after 30 to 60. The average half-life of the substance is about 1.5 h.

Prevention and long-term treatment of angina pectoris.

Molsidomine should be used with caution in combination with other antihypertensive drugs (e.g. vasodilators such as nitrates, beta-receptor blockers, calcium antagonists, other drugs for high blood pressure or tricyclic antidepressants and neuroleptics) as their antihypertensive effect can be enhanced.

Due to a possible contrary effect of nitric oxide donors, such as ergot alkaloids, simultaneous application should be avoided.

Shock, collapse, hypotension (RR systolic below 100 mmHg)

PDE-5 inhibitors (e.g. sildenafil, vardenafil or tadalafil), must not be used at the same time, as there is a risk of a severe drop in blood pressure.

Pregnancy, lactation: only under strict indication, teratogenicity not completely excluded

Corvaton® 2mg i.v. (injection and infusion solution); Corvaton®2mg tablets

1. Graefe KH et al Pharma with effects on the vascular system In: Graefe KH et al (Eds) Pharmacology and Toxicology. Georg Thieme Publisher Stuttgart S.177-181
2. Speeches J (1990) Molsidomine. Blood Vessels 27:282-294