Ketanserin: Effects, Uses & Risks

Ketanserin refers to a substance that has wound-healing and blood pressure-lowering properties. The active ingredient is a serotonin antagonist and acts on different receptors in the human brain. However, ketanserin does not have approval as a drug for these purposes in the Federal Republic and is only used clinically in exceptional cases.

What is ketanserin?

The active ingredient is a serotonin antagonist and acts on different receptors in the human brain. Ketanserin is a special derivative that has undergone many studies and tests to obtain a detailed pharmacological analysis. Ketanserin is a very effective serotonin antagonist, which is a component of numerous preparations. The drug ketanserin has many different modes of action that directly affect the autonomic and central nervous systems. The effect of ketanserin on cardiac function, for example, is very complex, ranging from the effect on cardiac muscle activity such as contraction and relaxation to the effect on the muscles of the blood vessels. The vasoconstrictor property of ketanserin continues to take place in the lungs and kidneys. In the muscles of the bone structure, the vasodilatory property prevails. Serotonin thus causes a phasic change in blood pressure in the human circulation. Initially, there is a drop in blood pressure, but after a few seconds it rises again, and sustained high blood pressure is formed. Ketanserin can counteract this very well as an antagonist and lowers blood pressure to a normal level in the longer term.

Pharmacologic action

Ketanserin refers to a selective and competitive serotonin antagonist. The active ingredient inhibits local symptoms caused by serotonin, such as vasoconstriction, permeability, platelet aggregation, and the blocking and release of all factors regarding growth in the human body. Also, this ensures the supply of oxygen to the blood, and the circulation of wounds is favored. The so-called endothelial cells and fibroblasts multiply considerably under the stimulating influence of ketanserin. This results in improved wound healing, which in turn prevents infections. Furthermore, the administration of this drug leads to a blockade of histamine receptors and the vessels are dilated. The serotonin antogonist ketanserin refers to a substance that acts directly on the receptors in the human brain. It is capable of activating and influencing tissue hormones and neurotransmitters such as serotonin. Ketanserin also acts selectively and discriminates about 20 different receptors in the brain. It is also used in the treatment of migraine, depression or anxiety, as well as in the so-called irritable bowel syndrome or as an appetite suppressant. Here there were different preparations with different trade names, which are now no longer available throughout Europe.

Medical application and use

Ketanserin lowers blood pressure, so it acts mainly as a so-called antihypertensive. However, there is no appropriate marketing authorization for this drug in Germany. In other countries, too, there are considerable restrictions on the use of ketanserin. In practice, the substance is usually only used as a reserve for particularly critical blood pressure values. It is therefore frequently used during surgery or for poisoning during pregnancy. In Europe, ketanserin is only available in the Netherlands under the name Ketesin. All other preparations, which were initially marketed in various European countries, are no longer on the market. However, ketanserin is used in pharmacology research. Here it is used to analyze the different mechanisms of action of drugs. In Switzerland, the drug is used in wound treatment of animals and is available as a gel.

Risks and side effects

Ketanserin has some risks and side effects. Sensitivity reactions and allergic symptoms may occur and should not be used in the presence of hypokalemia. There is also the possibility of side effects such as drowsiness, headache, and fatigue. Weight gain and dry mouth are also common.Particularly sensitive patients often experience dizziness due to significant blood pressure fluctuations during treatment with ketanserin. In medical studies, some cases of cardiac arrhythmia and tachycardia (heart palpitations) occurred. Thus, ketanserin may be contraindicated in medical conditions such as AV block, arrhythmia, bradycardia and tachycardia, various cardiovascular syndromes, and ventricular fibrillation.