Trade names Buronil Molar mass 263.35 g/mol | ATC code N05AD03 (WHO) | |
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AHFS/Drugs.com International Drug Names Routes of
administration Oral, intramuscular injection Legal status In general: ℞ (Prescription only) Bioavailability 87% (IM), 54% (Oral via syrup), 65% (Oral, tablet) | ||
Melperone (Bunil , Buronil , Eunerpan ) is an atypical antipsychotic of the butyrophenone chemical class, making it structurally related to the typical antipsychotic haloperidol. It first entered clinical use in 1960s.
Contents
Marketing and indications
It has been tried in treatment-resistant cases of schizophrenia with some (albeit limited) success. It has also been reported effective in the treatment of L-DOPA and other forms of psychosis in Parkinson's disease (although a multicentre, double-blind, placebo-controlled study conducted in 2012 failed to support these findings). It is also known to possess anxiolytic properties. It is marketed in the following countries:
Adverse effects
Melperone is reported to produce significantly less weight gain than clozapine and approximately as much weight gain as typical antipsychotics. It is also purported to produce around as much prolactin secretion as clozapine (which is virtually nill). It is also purported to produce sedative effects and QT interval prolongation. It is also known to produce less extrapyramidal side effects than the first-generation (typical) antipsychotic, thiothixene. It can also produce (usually relatively mild) dry mouth.
* tremor, dystonia, hypokinesis, akathisia, dyskinesias
** which can lead to galactorrhea, gynecomastia, etc.
Interactions
Melperone is reported to be a CYP2D6 inhibitor.
Pharmacology
Melperone binds to the dopamine D2 receptor, just like all other clinically-utilized antipsychotics, but it does so with a very low affinity and hence may be liable to rapidly dissociate from the D2 receptor hence potentially giving it the profile of an atypical antipsychotic.