Melperone
Antipsychotic drug
From Wikipedia, the free encyclopedia
Melperone (Bunil (PT), Buronil (AT, BE, CZ, DK, FI†, NL†, NO†, SE), Eunerpan (DE))[3] 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.[4]
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| Trade names | Buronil |
| AHFS/Drugs.com | International Drug Names |
| Routes of administration | Oral, intramuscular injection |
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| Pharmacokinetic data | |
| Bioavailability | 87% (IM), 54% (Oral via syrup), 65% (Oral, tablet)[1] |
| Protein binding | 50% |
| Metabolism | Hepatic |
| Elimination half-life | 3–4 hours (oral)[1] 6 hours (IM) |
| Excretion | Renal (70% as metabolites, 5.5–10.4% as unchanged drug)[1][2] |
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| ECHA InfoCard | 100.107.027 |
| Chemical and physical data | |
| Formula | C16H22FNO |
| Molar mass | 263.356 g·mol−1 |
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Marketing and indications
It has been tried in treatment-resistant cases of schizophrenia with some (albeit limited) success.[4][5][6][7] It has also been reported effective in the treatment of L-DOPA and other forms of psychosis in Parkinson's disease[8] (although a multicentre, double-blind, placebo-controlled study conducted in 2012 failed to support these findings[9]). It is also known to possess anxiolytic properties.[10] It is marketed in the following countries:[3][11]
Adverse effects
Melperone is reported to produce significantly less weight gain than clozapine and approximately as much weight gain as typical antipsychotics.[12] It is also purported to produce around as much prolactin secretion as clozapine (which is virtually nil).[13] It is also purported to produce sedative effects[14] and QT interval prolongation.[15] It is also known to produce less extrapyramidal side effects than the first-generation (typical) antipsychotic, thiothixene.[16] It can also produce (usually relatively mild) dry mouth.[17]
- Constipation
- Diarrhea
- Nausea
- Vomiting
- Appetite loss
- Hypersalivation (drooling)
- Extrapyramidal side effects (e.g. tremor, dystonia, hypokinesis, akathisia, dyskinesias)
- Insomnia
- Agitation
- Headache
- Dizziness
- Fatigue
- Miosis
- Mydriasis
- Blurred vision
- Elevated liver enzymes (esp. ALT and GGTP)
- Tardive dyskinesia
- Neuroleptic malignant syndrome
- Blood dyscrasias (pancytopenia, agranulocytosis, leukopenia, thrombocytopenia, etc.)
- Seizures (probably rare/uncommon)
- Increased intraocular pressure
- Intrahepatic cholestasis (probably rare)
- Orthostatic hypotension (probably common)
- Arrhythmias
- Rash
- Hyperprolactinemia (which can lead to e.g. galactorrhea, gynecomastia)
- Weight gain
- Increased appetite
Interactions
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.[23]
