Molsidomine

Benjamin Clanner-Engelshofen is a freelance writer in the medical department. He studied biochemistry and pharmacy in Munich and Cambridge / Boston (USA) and noticed early on that he particularly enjoyed the interface between medicine and science. That is why he went on to study human medicine.

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The active ingredient molsidomine is a nitric oxide-releasing agent used to treat angina pectoris. Angina pectoris ("chest tightness") is a symptom that is commonly associated with coronary artery disease. The arteries of the heart constrict, which can trigger severe attacks of the heart. Read here how molsidomine can help and what side effects are possible.

This is how molsidomine works

In coronary artery disease (CHD), the arteries of the heart are narrowed, mostly due to arteriosclerosis ("hardening of the arteries"). The coronary vessels supply the muscles of the heart with oxygen and nutrients. The more the vessels are narrowed, the worse the blood supply to the heart. At the onset of the disease, when the vessels are only slightly narrowed, the patient only notices the undersupply when the heart has to perform at its maximum, for example during exercise. Later, when the coronary arteries are already more narrow, painful attacks of angina pectoris can occur even in quiet situations.The undersupply of the heart can also lead to cardiac arrhythmias and cardiac insufficiency (heart failure). If a coronary vessel is completely blocked, a heart attack or sudden cardiac death occurs.

The symptoms of cardiac deficiency can be alleviated with nitric oxide (NO) -releasing agents such as molsidomine. Nitric oxide dilates the blood vessels and thus improves blood circulation. It is produced by the body, but can also be supplied in the form of molsidomine. Molsidomine is a so-called "prodrug", so it is only converted into the effective NO in the body in two steps:

Molsidomine is first transported in the blood from the intestine to the liver, where it is converted into linsidomine. This is released back into the bloodstream, where it slowly breaks down into NO without the involvement of the body's own enzymes. Some of this NO reaches the heart vessels and allows them to expand. This can alleviate the usually dull, pressing and burning pain of angina pectoris. However, since the conversion takes some time (usually half an hour to a full hour), molsidomine is not suitable for acute treatment. So it is only used as a precaution against angina pectoris complaints.

In contrast to other NO-releasing active ingredients such as nitroglycerin, in which NO is released enzymatically, molsidomine does not have a nitrate tolerance. This “tolerance” (in the sense of a reduced effect of the drug) arises from the fact that the enzyme that enables the release of NO is increasingly inhibited by this released NO. This can be prevented with a regular nitrate-free interval, for example by removing the nitrate patch (patch with an NO-releasing agent) at night. Such a nitrate-free interval is not necessary with molsidomine, since NO is released non-enzymatically.

Uptake, breakdown and excretion of molsidomine

After taking molsidomine, it enters the bloodstream via the intestines and reaches the liver. There it is converted into linsidomine, which slowly breaks down to NO after being released into the blood. The highest blood levels of linsidomine are reached after about one to two hours. It then takes another one to two hours for the blood level to halve. Most of it is excreted via the kidneys with the urine.

When is molsidomine used?

Molsidomine is approved for the prevention and long-term treatment of angina pectoris if other drugs are not tolerated or must not be used, or in elderly patients. It is not suitable for the acute therapy of an angina pectoris attack.

This is how molsidomine is used

The active ingredient molsidomine is usually given as a tablet or an extended-release tablet (a slow-release tablet). Doctors can also give the drug directly into a vein (intravenous use).

As a rule, the dosage of molsidomine tablets is two milligrams of the active ingredient twice a day. If the dosage is not sufficient, it can be increased to two milligrams of molsidomine up to four times a day (corresponding to 16 milligrams per day).

The prolonged-release tablets, each containing eight milligrams of molsidomine, are taken once or twice a day. If the dose is too high, however, the prolonged-release tablets cannot simply be divided. Instead, you should take lower-dose, non-release tablets.

Molsidomine is taken independently of meals with a glass of water at approximately the same time intervals.

The active ingredient is only slowly released from the prolonged-release tablets in the intestine. Sometimes the prolonged-release tablet can be found in the stool, but this does not mean that the active ingredient has not been absorbed.

What are the side effects of molsidomine?

Because molsidomine dilates the blood vessels, one to ten percent of patients experience side effects such as low blood pressure and headaches, especially at the beginning of treatment.

Occasionally, molsidomine can also lead to "orthostatic dysregulation", i.e. dizziness when getting up from a lying or sitting position.

What should be considered when taking molsidomine?

The combination of molsidomine with other drugs that lower blood pressure may reduce the patient's blood pressure excessively. Such drugs are, for example, organic nitrates (nitroglycerin), beta blockers (metoprolol, bisoprolol), calcium channel blockers (nifedipine, verapamil, diltiazem), ACE inhibitors (captopril, ramipril), sartans (candesartan, valsartan), dehydrating agents (hydrochlorothiazide) , Antidepressants and antipsychotics (neuroleptics).

Above all, molsidomine must not be taken together with sexual enhancers from the class of PDE-5 inhibitors (sildenafil, vardenafil, tadalafil, avanafil), as this can lead to a drop in blood pressure that is sometimes life-threatening.

Pregnant and breastfeeding women are not allowed to take molsidomine, because here the safety and the benefit of an application are not guaranteed. In addition, molsidomine is excreted in breast milk.

The active substance can be used in patients with severe liver and kidney problems, but may be given a lower starting dose than usual.

How to get drugs with molsidomine

Preparations with the active ingredient molsidomine are subject to prescription and pharmacy requirements in every dosage and pack size.

Since when is molsidomine known?

As early as the 19th century it was noticed that handling nitroglycerin (used as an explosive) leads to headaches and low blood pressure. From 1878 the doctor William Murrell in London treated patients with nitroglycerin for angina pectoris and high blood pressure. However, it was still about a century before the organic nitrates were further developed and the side effects diminished in the process. In 1986, the pharmaceutical company Sanofi-Aventis received approval in Germany to market molsidomine. Since the patent protection has now expired, there are now also generics with the active ingredient molsidomine.

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