Active Ingredients

Reserpine – Effect, Application & Risks

Reserpine

Reserpine is a drug used as an antihypertensive and neuroleptic . Originally, the active ingredient comes from some plants from the snake root group .

What is reserpine?

Reserpine is a chemical compound that occurs naturally in plants. The substance belongs to the indole alkaloids. Indole alkaloids are the largest group within the alkaloids . They are characterized by their indole or indoline base.

The medicinal substance reserpine became known in western medicine in particular through the plant Rauvolfia serpentina from India. Reserpine was one of the drugs that ushered in the era of modern psychomedication. The substance was initially used in psychiatric institutions for schizophrenia as a neuroleptic. Neuroleptics are now also referred to as antipsychotics. These are drugs that have an antipsychotic and/or sedative effect.

Later, reserpine was mainly used as a remedy for high blood pressure (hypertension). Today, due to various side effects, reserpine is neither a neuroleptic nor an antihypertensive drug of first choice.

Pharmacological action

The effect of reserpine in the human body can be divided into a central and a peripheral effect. Reserpine inhibits the neurotransmitter noradrenaline in the sympathetic nervous system . The postganglionic system is particularly affected. Although more nerve cells are discharged due to the depletion of the neurotransmitter than before the drug was taken, the stimulus is not transmitted to the periphery of the body. By inhibiting the sympathetic nervous system, the heart rate is lowered and thus the blood pressure is lowered accordingly.

At the same time, reserpine lowers the concentration of dopamine and serotonin in the central nervous system . At the cellular level, reserpine also depletes the stores of biogenic amines. These include neurotransmitters like serotonin, dopamine , and norepinephrine. In addition, the neurotransmitters can no longer be absorbed into the cell via the vesicles . Due to these mechanisms of action, reserpine has an antipsychotic and sedative effect.

Medical Application & Use

Reserpine was first isolated from the Rauvolfia serpentina plant in 1952. While the drug was commonly used as an antihypertensive and neuroleptic in the 1950s, 1960s and 1970s, reserpine is rarely found in drugs today. The substance was replaced by more effective drugs with fewer side effects . In pharmacologically relevant amounts, reserpine is now only on the market as a component of diuretics . Reserpine is combined with thiazide diuretics, dihydralazine and hydrochlorothiazide . However, the frequency of prescribing these remaining preparations with reserpine is also decreasing. Currently there is also a homeopathic preparationon the market that contains reserpine as a pure substance in the potency D3 32 milligrams.

Reserpine can also be used diagnostically. The drug is sometimes used when there is a suspicion of a carcinoid . Carcinoids are neuroendocrine tumors that produce tissue hormones such as kallikrein and serotonin . The reserpine test is a provocation test. Carcinoids usually produce large amounts of serotonin. Reserpine ensures the release of serotonin from the tumor cells, so that the typical symptoms of the carcinoid are intensified after reserpine administration. In addition, there is a greatly increased concentration of 5-HIES in the urine . 5-HIES is a breakdown product of serotonin.

Risks & side effects

Reserpine has fallen into disrepute mainly because of its serious side effects. Reserpine decreases the availability of catecholamines and thus lowers the sympathetic tone . However, acetylcholine , another neurotransmitter, remains unaffected by this effect, so that the parasympathetic nervous system predominates in its activity as a result of drug intake. Constriction of the pupils , droopy eyelids and swelling of the nasal mucous membranes can occur. This phenomenon is also known as reserpine rhinitis.

Other side effects caused by the increased activity of the parasympathetic nervous system are loss of potency and libido and diarrhea . Stomach and intestinal ulcers can develop. In addition to the desired bradycardia, a position -related drop in blood pressure can also occur. This orthostatic hypotension can be so severe that those affected lose consciousness when standing up quickly.

Reserpine can damage the unborn or newborn child via breast milk and the placenta . If mothers took reserpine in the last trimester of their pregnancy , the children suffer significantly more often from breathing and drinking disorders after birth . Newborns often show marked lethargy . The fetus may have a slow heartbeat. In women, reserpine can also cause menstrual cramps .

In the central nervous system, the side effects are mainly caused by the lack of serotonin and dopamine. It comes to so-called extrapyramidal motor disorders and Parkinsonism with symptoms such as muscle rigidity , immobility, muscle tremors and postural instability.

When reserpine is overdosed, blood pressure, heart rate, and body temperature drop rapidly. Those affected suffer from severe drowsiness . There may also be cramps .

It should be noted that a so-called reserpine reversal occurs with prior administration of tricyclic or tetracyclic antidepressants . The motor excitement is not inhibited as intended, but increased. Indirect sympathomimetics are not effective after pretreatment with reserpine. On the other hand, the lowering effect of antidiabetics on the blood sugar level is increased by reserpine. The effect of antiparkinson drugs such as levodopa or bromocriptine is disrupted. Patients who take cardioactive glycosides and reserpine at the same time can develop cardiac arrhythmias .

Reserpine is contraindicated in the case of a history of depressive episodes , existing gastric and duodenal ulcers and bronchial asthma .

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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.