Molsidomine

N-( ethoxycarbonyl ) -3 - (4- morpholinyl) - sydnonimine

C01DX12

Vasodilator

Vasodilation by elimination of nitric oxide

140-141 ° C

Attention

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Molsidomine belongs to the group of non-enzymatic nitric oxide donors. This medication is nitric oxide ( NO) release and leads to a vasodilation of the coronary arteries ( coronary arteries ), therefore it is used to treat angina pectoris used.

Pharmacokinetics

In molsidomine is an inactive precursor ( prodrug ). Molsidomine itself is not responsible for the vasodilatory effect but is metabolized in the liver to linsidomine (SIN -1). This goes without the action of enzymes on in the open-ring form and the actual active substance, nitric oxide is cleaved. Since the formation of free nitric oxide no enzymes are necessary, it is also used for long- term administration not to weaken the effect ( nitrate tolerance). Molsidomine inhibited in low grade bond the platelets. However, this effect is of no clinical relevance because of the small effect.

→ → → NO

Molsidomine → linsidomine (SIN- 1) → SIN -1A → nitric oxide

Pharmacodynamics

The release of nitric oxide leading to a vasodilatation of the coronary arteries, the vena cava and large vessels of the lung, so that the preload of the heart is decreased. According to the Frank -Starling mechanism, this results in that the blood filling of the heart decreases, the heart wall is not stretched so much, and thus the oxygen consumption is reduced. Because the more the heart wall is stretched, the more work it performs. The dilatation of the coronary vessels and the decrease in filling lead to better blood flow to the heart wall, and thus to improve the oxygen supply to the heart muscle.

The active substance directly, linsidomine, is also available for direct intravenous therapy.

Application

Therapeutic molsidomine is prescribed for prophylaxis of angina pectoris attacks. Acute therapy, however, is not possible with molsidomine, since the maximum effect is reached after 30 to 60 minutes.

Side effects

The most important side effects may occur due to the strong vasodilatation headache, dizziness, and hypotension.

In animal studies with rats, at high doses of molsidomine more on malignant nasal tumors.

Trade names

Corvaton (D, CH), Molsibeta (D), Molsidolat (A), Molsiket (D), Molsi - meshing (D ), various generics (D)