How molsidomine works
Molsidomine is a drug from the group of vasodilators. The active ingredient has vasodilatory and blood pressure-lowering properties.
In coronary artery disease (CAD), the coronary vessels are narrowed, usually due to arteriosclerosis (“hardening of the arteries”). The coronary vessels supply the heart muscle cells with oxygen and nutrients.
Later, when the coronary vessels are already more constricted, painful angina pectoris attacks can occur even in resting situations. The undersupply of the heart can also lead to cardiac arrhythmias and cardiac insufficiency. If a coronary vessel is completely blocked, a heart attack or sudden cardiac death occurs.
Molsidomine dilates the vessels
Molsidomine is a so-called “prodrug” – it is first converted into the active NO in the body in two steps: First, molsidomine is transported with the blood from the intestine to the liver, where it is converted into linsidomine. This is released back into the bloodstream, where it slowly decomposes into NO and another metabolic product without the involvement of the body’s own enzymes.
Advantage over other NO-releasing agents
In contrast to other NO-releasing agents such as nitroglycerin, in which NO is released enzymatically, molsidomine does not cause so-called nitrate tolerance. This “tolerance” (in the sense of a reduced effect of the drug) occurs because the enzyme that enables the release of NO is increasingly inhibited by this very NO that is released.
With molsidomine, such a nitrate-free interval is not necessary, since – as mentioned – NO is released non-enzymatically here. It can therefore be taken in the morning and in the evening.
Absorption, degradation and excretion
After ingestion of molsidomine, it enters the bloodstream via the intestine and reaches the liver. There it is converted into Linsidomine, which after release into the blood slowly decomposes releasing NO.
When is molsidomine used?
Molsidomine is approved in Germany and Austria for the prevention and long-term treatment of angina pectoris when other drugs are not tolerated or may not be used, or in elderly patients. It is not suitable for the acute therapy of an angina pectoris attack!
How molsidomine is used
Molsidomine is usually used as a tablet or sustained-release tablet (slow-release tablet). However, doctors can also administer the active substance directly into a vein (intravenous use) if necessary.
The sustained-release tablets are taken once or twice daily. If the dose is too high, do not simply divide the sustained-release tablets. Instead, one should take lower-dose unretarded tablets or reduce the dosage to once daily.
Molsidomine is taken independently of meals with a glass of water at approximately equal intervals.
What are the side effects of molsidomine?
Because molsidomine dilates the blood vessels, one to ten percent of patients experience low blood pressure and headaches, especially at the beginning of treatment.
Occasionally, molsidomine can also cause “orthostatic dysregulation,” which is dizziness when standing up from a lying or sitting position.
What should I be aware of when taking molsidomine?
Contraindications
Molsidomine must not be used in:
- acute circulatory failure
- severely reduced blood pressure (severe hypotension)
- simultaneous use of agonists of soluble guanylate cyclase (e.g. riociguat – used in special forms of pulmonary hypertension)
Interactions
Above all, molsidomine must not be taken together with potency medications from the class of PDE-5 inhibitors (sildenafil, vardenafil, tadalafil, avanafil), because this can lead to sometimes life-threatening drops in blood pressure.
Trafficability and operation of machines
Age restriction
Use in children and adolescents under 18 years of age has not been studied and therefore cannot be recommended.
Pregnancy and lactation
The safety of molsidomine in pregnant women has not been studied. Therefore, the active substance should not be used during pregnancy – unless the treating physician considers it absolutely necessary.
How to obtain medicines containing molsidomine
Preparations containing the active ingredient molsidomine are subject to prescription and pharmacy requirements in Germany, Austria, and Switzerland in every dosage and package size.
Since when is Molsidomine known?
However, it took about another century before organic nitrates were further developed and the side effects mitigated in the process. In 1986, molsidomine was approved for marketing in Germany. Since patent protection has since expired, there are now also generics containing this active ingredient.
