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Haloperidol was synthesized on February 11, 1958, by Bert Hermans at Janssen Laboratories in Belgium. Initially identified as R1625, it was found to be much more potent than chlorpromazine, requiring smaller doses to achieve similar effects. Early clinical studies, starting in 1958, showed its effectiveness in treating agitation, delusions, and hallucinations. Haloperidol belongs to the neuroleptic drug family and is widely used in treating acute and chronic schizophrenia. It is metabolized primarily by CYP3A4, with interactions that can affect its pharmacokinetics when coadministered with other drugs.
Haloperidol works by blocking dopamine type 2 receptors in the brain. This action reduces the effects of dopamine, which is often overactive in conditions like schizophrenia. By blocking these receptors, haloperidol helps to control symptoms such as delusions and hallucinations. Additionally, it has low activity against alpha-1 adrenergic receptors, meaning it doesn't significantly affect blood pressure or cause other common side effects associated with alpha-1 receptor blockage
Parameter | Details |
---|---|
Class of Drug | Butyrophenone Antipsychotic (5mg/1mL) |
Mechanism of Action | Central dopamine type 2 receptor antagonist with low alpha-1 antiadrenergic activity. |
Pharmacodynamic Effects | Suppresses delusions and hallucinations by blocking dopaminergic signaling. Causes psychomotor sedation, impacting mania and agitation. |
Indications | Nausea & vomiting, Psychotic... |
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