Molsidomine

(BAN, USAN, rINN)
Molsidomine Chemical formula
Synonyms: CAS-276; Molsidomiini; Molsidomin; Molsidomina; Molsidominum; Morsydomine; SIN-10. N-Ethoxycarbonyl-3-morpholinosydnonimine.
Cyrillic synonym: Молсидомин.

💊 Chemical information

Chemical formula: C9H14N4O4 = 242.2.
CAS — 25717-80-0.
ATC — C01DX12.
ATC Vet — QC01D X12.

Pharmacopoeias.

In Eur..

Ph. Eur. 6.2

(Molsidomine). A white or almost white, crystalline powder. Sparingly soluble in water; soluble in anhydrous alcohol and in dichloromethane. A 1% solution in water has a pH of 5.5 to 7.5. Protect from light.

💊 Profile

Molsidomine is a nitrovasodilator used in angina pectoris. It may also be used in heart failure and after myocardial infarction (below). Molsidomine is given in usual oral doses of 1 to 4 mg two to four times daily. Modified-release preparations are also available. It is also given intravenously in single doses of 2 to 4 mg and doses of 2 mg may be repeated at intervals of at least 2 hours if necessary; total doses of up to 40 mg daily have been given. Infusions may be given at a rate of up to 3 mg/hour. Molsidomine is metabolised to linsidomine, an active metabolite.

Carcinogenicity.

Molsidomine tends to degrade into morpholine (even when protected from the light), a compound considered potentially carcinogenic. This finding led to the suspension of marketing of one molsidomine formulation;1 an earlier temporary suspension was related to evidence of carcinogenicity in some animals, although this has not been confirmed in humans.
1. Anonymous. Corvaton Tropfen. Dtsch Apotheker Ztg 1989; 129 (49): VI.

Myocardial infarction.

Although intravenous nitrates (glyceryl trinitrate or sodium nitroprusside) may be used in the management of acute myocardial infarction, molsidomine and its active metabolite linsidomine (a nitric oxide donor) had no effect on mortality.1
1. European Study of Prevention of Infarct with Molsidomine (ESPRIM) Group. The ESPRIM trial: short-term treatment of acute myocardial infarction with molsidomine. Lancet 1994; 344: 91–7.

Pharmacokinetics.

The pharmacokinetics of molsidomine have been reviewed.1 Molsidomine is metabolised in the liver to linsidomine and other morpholine derivatives. Prolonged elimination half-lives of molsidomine and linsidomine due to reduced plasma clearance have been reported in patients with liver cirrhosis.2
1. Rosenkranz B, et al. Clinical pharmacokinetics of molsidomine. Clin Pharmacokinet 1996; 30: 372–84
2. Spreux-Varoquaux O, et al. Pharmacokinetics of molsidomine and its active metabolite, linsidomine, in patients with liver cirrhosis. Br J Clin Pharmacol 1991; 32: 399–401.

💊 Preparations

Proprietary Preparations

Arg.: Molsicor; Molsidaine; Austria: Molsidolat; Molsihexal; Belg.: Coruno; Corvatard†; Corvaton; Cz.: Corvaton; Molsihexal; Molsiket; Fr.: Corvasal; Ger.: Corvaton; duracoron†; Molsi-Azu†; Molsi-Puren; Molsi†; Molsibeta; Molsihexal; molsiket; Hung.: Corvaton; Port.: Corvaton†; Rus.: Dilasidom (Диласидом); Sydnopharm (Сиднофарм); Spain: Corpea; Molsidain; Switz.: Corsifar†; Corvaton.
Published May 08, 2019.