Products
Pipamperone is commercially available in tablet form (dipiperone). It has been approved in many countries since 1964.
Structure and properties
Pipamperone (C21H30FN3O2, Mr = 375.5 g/mol) is present in drugs as pipamperondihydrochloride. It is structurally closely related to haloperidol, which also belongs to the butyrphenones. Butyrphenones, like numerous other active ingredients, originated in the laboratory of Dr. Paul Janssen, founder of Janssen Pharmaceutica.
Effects
Pipamperone (ATC N05AD05) has antidopaminergic, antipsychotic, sedative, antiexcitant, and sleep-promoting properties and is barely anticholinergic. It should be noted that the studies conducted are older and lack modern pivotal studies.
Indications
In many countries, pipamperone is approved for the treatment of chronic psychosis. In other countries, it is approved for the treatment of sleep disorders in the elderly and for psychomotor agitation.
Dosage
According to the drug label. Dosage is gradual and is adjusted on an individual basis. The intake is independent of meals.
Contraindications
- Hypersensitivity
- CNS depression
- Conditions involving central nervous system depression, e.g., coma or intoxication
- Use in patients with Parkinson’s disease is not indicated due to antidopaminergic properties.
Full and comprehensive precautions can be found in the drug label.
Interactions
Metabolism data are incomplete. Pipamperone is known to be metabolized by oxidative N-dealkylation, piperidine oxidation, and ketone reduction, suggesting metabolism via CYPs. Very rarely, QT interval prolongation has been reported during treatment. Therefore, combination with other agents that prolong the QT interval should be avoided. Drugs that induce hypokalemia, for example diuretics, may promote the development of QT prolongation. Centrally depressant drugs, for example, sedatives, sleeping pills, antidepressants, neuroleptics, opioids, or alcohol may increase sedation. Antihypertensive drugs may increase lowering of blood pressure. Pipamperone may reverse the effects of dopamine agonists such as levodopa, bromocriptine, and lisuride. Enzyme inducers may decrease effects, and pipamperone should not be combined with agents that lower the brain‘s seizure threshold.
Adverse Effects
A common adverse effect is nausea, which may also lead to vomiting and loss of appetite. Occasionally, central disturbances occur, such as fatigue, drowsiness (sometimes desirable), dizziness, depression, and headache. Depending on the dose, extrapyramidal symptoms such as drug-induced parkinsonism and an urge to make motor movements occur. Low blood pressure with a rapid pulse and urinary retention are other occasional side effects. Potential serious side effects, which are rare to very rare, include malignant neuroleptic syndrome, arrhythmias (torsade de pointes), severe skin and hypersensitivity reactions, and liver dysfunction. The complete list of adverse effects can be found in the Drug Information Leaflet.