Molsidomine

Absorption

Peak plasma drug concentration (tmax) occurs from 1 to 2 hours after administration.

Chemical properties

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Originator

Corvasal,Hoechst

The Uses of Molsidomine

Molsidomine is an antianginal agent. Molsidomine is an effective therapeutic agents in the treatment of angina pectoris. Molsidomine is a sydnonimine derivative that acts as a heterocyclic direct nitr ic oxide donor.

The Uses of Molsidomine

Molsidomine is an antianginal agent. Molsidomine is an effective therapeutic agents in the treatment of angina pectoris. Molsidomine is a sydnonimine derivative that acts as a heterocyclic direct nitric oxide donor.

Background

Molsidomine is an orally active, long-acting vasodilator, which belongs to the class of medications known as syndnones. Interestingly, it is being studied as being a preventive measure in cerebral infarction .

Indications

The indications for use of molsidomine include ischemic heart disease, angina, chronic heart failure, and pulmonary hypertension .

What are the applications of Application

Molsidomine is a long-lasting, NO releasing vasodilator that activates soluble guanylate cyclase

Definition

ChEBI: 1-ethoxy-N-[3-(4-morpholinyl)-5-oxadiazol-3-iumyl]methanimidate is a member of morpholines.

Manufacturing Process

1.6 parts by volume of ethyl chloroformate is stirred dropwise into a suspension of 1.0 part by weight of 3-morpholinosydnonimine hydrochloride in 5 parts by volume of pyridine, and the mixture is agitated for a while to allow reaction to take place. Pyridine is removed from the reaction mixture by evaporation, and the residue is dissolved in a small amount of water and extracted with chloroform several times. The extract is dehydrated by adding anhydrous magnesium sulfate and subjected to filtration. Chloroform is removed from the filtrate by distillation, crude crystals being obtained. Recrystallization of the crude crystals from toluene gives 0.6 part by weight of 3-morpholino-N-carboethoxysydnonimine having a melting point of 140°- 141°C. Yield 51%.

brand name

Corvaton (Hoechst-Roussel).

Therapeutic Function

Coronary vasodilator

Pharmacokinetics

Molsidomine leads to smooth muscle relaxation in the coronary blood vessels, relieving symptoms of angina and increasing blood flow to the coronary arteries.

Metabolism

Molsidomine hepatically metabolized to linsidomine. Linsidomine releases nitric oxide (NO) from endothelial cells when it decays, and acts as the active vasodilating metabolite responsible for molsidomine's pharmacological effects.
Oral absorption of Molsidomine is found to be 95.5% ±4.5. Presystemic metabolism is noted to be 56% and metabolism is reported extensive by Liver. Renal Excretion accounts for 95 % and plasma half-life is 5 hr. Back to top