Melperone (Bunil ( PT), Buronil ( AT, BE, CZ, DK, FL^†, NL^†, NO^†, SE), Eunerpan ( DE)) 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.

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: * Austria * Belgium * Czech Republic * Denmark * Estonia * Finland * Germany * Iceland *

Lithuania Lithuania (; lt, Lietuva ), officially the Republic of Lithuania ( lt, Lietuvos Respublika, links=no ), is a country in the Baltic region of Europe. It is one of three Baltic states and lies on the eastern shore of the Baltic Sea. Lithuania ...

Latvia Latvia ( or ; lv, Latvija ; ltg, Latveja; liv, Leţmō), officially the Republic of Latvia ( lv, Latvijas Republika, links=no, ltg, Latvejas Republika, links=no, liv, Leţmō Vabāmō, links=no), is a country in the Baltic region of ...

* Portugal *

Sweden Sweden, formally the Kingdom of Sweden,The United Nations Group of Experts on Geographical Names states that the country's formal name is the Kingdom of SwedenUNGEGN World Geographical Names, Sweden./ref> is a Nordic country located on ...

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 nil). It is also purported to produce sedative effects and QT interval prolongation. It is also known to produce less

extrapyramidal side effects Extrapyramidal symptoms (EPS) are symptoms that are archetypically associated with the extrapyramidal system of the brain's cerebral cortex. When such symptoms are caused by medications or other drugs, they are also known as extrapyramidal side ...

than the first-generation (typical) antipsychotic, thiothixene. It can also produce (usually relatively mild) dry mouth. ;Other common adverse effects include * Constipation * Diarrhea * Nausea * Vomiting * Appetite loss * Hypersalivation (drooling) *

Extrapyramidal side effects Extrapyramidal symptoms (EPS) are symptoms that are archetypically associated with the extrapyramidal system of the brain's cerebral cortex. When such symptoms are caused by medications or other drugs, they are also known as extrapyramidal side ...

(e.g. tremor,

dystonia Dystonia is a neurological hyperkinetic movement disorder in which sustained or repetitive muscle contractions result in twisting and repetitive movements or abnormal fixed postures. The movements may resemble a tremor. Dystonia is often inten ...

, hypokinesis, akathisia, dyskinesias) * Insomnia * Agitation * Headache * Dizziness * Fatigue * Miosis * Mydriasis * Blurred vision * Elevated liver enzymes (esp. ALT and GGTP) ;Rare adverse effects include * Tardive dyskinesia * Neuroleptic malignant syndrome * Blood dyscrasias (pancytopenia, agranulocytosis, leukopenia, thrombocytopenia, etc.) ;Unknown frequency adverse effects include * 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

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.

Synthesis

For the last step of the synthesis the sidechain 4-Chloro-4'-Fluorobutyrophenone 874-54-2(1) is attached to 4-Methylpiperidine (4-Pipecoline) 26-58-4(2).

References

External links

PubChem Substance
* {{Navboxes , title = Pharmacodynamics , titlestyle = background:#ccccff , list1 = {{Acetylcholine receptor modulators {{Adrenergic receptor modulators {{Dopamine receptor modulators {{Histamine receptor modulators {{Serotonin receptor modulators Atypical antipsychotics Fluoroarenes Piperidines Butyrophenone antipsychotics Dopamine antagonists Serotonin receptor antagonists Alpha-1 blockers Alpha-2 blockers