Pipamperone is an antipsychotic from the butyrophenone group. It has a sedative effect and belongs to the group of low-potency neuroleptics (antipsychotics).
What is pipamperone?
Pipamperone is used to treat inner restlessness, sleep disorders, and mood swings. Pipamperone is also known as dipiperone or floropipamide. It is a drug from the class of antipsychotics. Just like haloperidol or benperidol, pipamperone belongs to the butyrophenones. Butyrophenones are drugs derived from 1-phenylbutan-1-one. They are preferentially used in psychiatric institutions for the treatment of schizophrenia. Pipamperone belongs to the class of renal depotent neuroleptics. Compared to the highly potent drugs from the group of antipsychotics, the effect of pipamperone is rather mild. Its tolerability is relative, so the drug is also used in child and adolescent psychiatry.
Pharmacological action
Various neurotransmitters serve to transmit signals in the body. The messengers of the brain and nervous system are called neurotransmitters. When neurotransmitters are imbalanced, mental illness can result. The neurotransmitters dopamine and serotonin are particularly commonly involved. Pipamperone mainly blocks the action of dopamine. It binds to D2 and D4 receptors, preventing dopamine from docking at these receptors. Pipamperone thus has an antidopaminergic effect. At the psychotropic level, dopamine has a drive-increasing and motivating effect. However, excessively high dopamine levels are suspected of triggering schizophrenia. Pipamperone, however, blocks not only dopamine receptors but also serotonin receptors. As a result, it has antipsychotic, sedative, and agitation-dampening effects. A sleep-promoting effect can also be observed. Unlike other neuroleptics, pipamperone is barely anticholinergic, meaning that it does not inhibit the neurotransmitter acetylcholine. It also does not affect histamine1 receptors. The half-life of pipamperone in the blood is 16 to 22 hours. The drug is degraded via N-dealkylation and oxidation.
Medicinal use and application
Pipamperone is used to treat inner restlessness, sleep disorders, and mood swings. It is said to have a regulating effect on neurotransmitter balance and promote sleep. Pipamperone is also thought to reduce agitation and aggression. Primarily, the drug is prescribed as a light sleep aid. However, in the elderly and in people with mental illness, pipamperone also serves as a sedative. To reduce aggression, pipamperone is mainly administered to children. In Switzerland, the drug is also approved for the treatment of chronic psychosis. The dosage is always adjusted individually by the specialist. The drug is sneaked in for better tolerability. It can be taken independently of meals.
Risks and side effects
Compared with other neuroleptics, pipamperone is relatively well tolerated. Anticholinergic side effects are absent, but extrapyramidal motor disturbances may occur at higher doses. In this case, the movement disorders manifest themselves primarily in the face. Typical are spasms of the pharynx and the so-called “rabbit syndrome”. The involuntary mewling of the patients is reminiscent of the mewling of a rabbit. Sit restlessness, twitching, grimacing, and involuntary movements of the extremities may also occur. In very rare cases, malignant neuroleptic syndrome may occur. It is manifested by akinesia, extreme muscle rigidity, hyperthermia with profuse sweating, lockjaw, mutism, confusion, and impaired consciousness and even coma. Malignant neuroleptic syndrome can be fatal and is therefore a feared complication of neuroleptic therapy. More often, patients suffer from loss of appetite, nausea, or vomiting while taking the drug. Hyperprolactinemia may develop due to the effect on the endocrine system. As a result, breast enlargement and menstrual disorders occur. At the cardiovascular level, the pulse may be accelerated and blood pressure too low. Very rarely, cardiac arrhythmias occur. Since pipamperone can prolong the QT interval, it should not be combined with other agents that also cause prolongation of the QT interval. These include, for example, diuretics.Centrally depressant drugs such as sleeping pills, antidepressants, opioids or even alcohol can increase the sedative effect of pipamperone. If pipamperone is administered in combination with antihypertensive drugs, blood pressure may drop sharply. The combination of pipamperone with dopamine antagonists such as lisuride, bromocriptine or levodopa is also not recommended. In addition, pipamperone should not be administered with drugs that lower the brain‘s seizure threshold. Epileptic seizures could otherwise occur.
