|Systematic (IUPAC) name|
|Routes||Oral, intramuscular injection|
3–4 hours (oral)
6 hours (IM)
|Excretion||Renal, 70% as metabolites, 5.5-10.4% as unchanged drug|
|Mol. mass||263.35 g/mol|
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 1
Adverse effects 2
- Interactions 2.1
- Pharmacology 3
- References 4
- External links 5
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:
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.
- Other common adverse effects include
- Rare adverse effects include
- Tardive dyskinesia
- Neuroleptic malignant syndrome
- Blood dyscrasias (pancytopaenia, agranulocytosis, leukopaenia, thrombocytopaenia, etc.)
- Unknown frequency adverse effects include
- Seizures (probably rare/uncommon)
- Increased intraocular pressure
- Intrahepatic cholestasis (probably rare)
- Orthostatic hypotension (probably common)
- Weight gain
- Increased appetite
** which can lead to galactorrhoea, gynecomastia, etc.
Melperone is reported to be a CYP2D6 inhibitor.
PharmacologyMelperone binds to the dopamine D2 receptor, just like all other clinically-utilised 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.
- Borgström, L; Larsson, H; Molander, L (1982). "Pharmacokinetics of parenteral and oral melperone in man". European Journal of Clinical Pharmacology 23 (2): 173–176.
- Product Information: Eunerpan(R), Melperonhydrochlorid. Knoll Deutschland GmbH, Ludwigshafen, 1995.
- Melperone Hydrochloride. Martindale: The Complete Drug Reference (The Royal Pharmaceutical Society of Great Britain). 30 January 2013. Retrieved 3 November 2013.
- Röhricht, F; Gadhia, S; Alam, R; Willis, M (2012). "Auditing Clinical Outcomes after Introducing Off-Licence Prescribing of Atypical Antipsychotic Melperone for Patients with Treatment Refractory Schizophrenia". Scientific World Journal 2012: 512047.
- Whiskey, E; Vavrova, M; Gaughran, F; Taylor, D; (February 2011). "Melperone in Treatment-Refractory Schizophrenia: A Case Series". Therapeutic Advances in Psychopharmacology 1 (1): 19–23.
- Meltzer, HY; Sumiyoshi, T; Jayathilake, K (December 2001). "Melperone in the treatment of neuroleptic-resistant schizophrenia.". Psychiatry Research 105 (3): 201–209.
- Sumiyoshi, T; Meltzer, HY; Jayathilake, K (2004). "Melperone, an atypical antipsychotic drug, in the treatment of schizophrenia: dose-response analysis on effectiveness and tolerability, and efficacy for treatment-resistant schizophrenia and cognitive function". International Clinical Psychopharmacology 19 (3): 184.
- Barbato L, Monge A, Stocchi F, Nordera G. Melperone in the treatment of iatrogenic psychosis in Parkinson’s disease. Funct Neurol. 1996 Aug;11(4):201–7.
- Friedman, JH (May 2012). "Melperone is ineffective in treating Parkinson's disease psychosis". Movement Disorders 27 (6): 803–804.
- Pöldinger, WJ (1984). "Melperone in low doses in anxious neurotic patients. A double-blind placebo-controlled clinical study". Neuropsychobiology 11 (3): 181–186.
- Bobo, WV; Jayathilake, K; Lee, MA; Meltzer HY (April 2010). "Changes in weight and body mass index during treatment with melperone, clozapine and typical neuroleptics". Psychiatry Research 176 (2-3): 114–119.
- Bobo, WV; Jayathilake, K; Lee, MA; Meltzer, HY (July 2009). "Melperone, an aytpical antipsychotic drug with clozapine-like effect on plasma prolactin: contrast with typical neuroleptics". Human Psychopharmacology: Clinical and Experimental 24 (5): 415–422.
- Molander, L; Borgström, L (1983). "Sedative effects and prolactin response to single oral doses of melperone". Psychopharmacology 79 (2-3): 142–147.
- Hui, WK; Mitchell, LB; Kavanagh, KM; Gillis, AM; Wyse, DG; Manyari, DE; Duff, HJ (January 1990). "Melperone: electrophysiologic and antiarrhythmic activity in humans". Journal of Cardiovascular Pharmacology 15 (1): 144–149.
- Bjerkenstedt, L (1989). "Melperone in the treatment of schizophrenia". Acta Psychiatrica Scandinavica Supplementum 352: 35–39.
- Molander, L; Birkhed, D (1981). "Effect of single oral doses of various neuroleptic drugs on salivary secretion rate, pH, and buffer capacity in healthy subjects". Psychopharmacology 75 (2): 114–118.
- "Product Information: Eunerpan(R), Melperonhydrochlorid". Knoll Deutschland GmbH, Ludwigshafen. 1995.
- Kirkegaard, A; Kirkegaard, G; Geismar, L (1981). "Additional studies on side effects of melperone in long-term therapy for 1 to 15 years in psychiatric patients". Arzneimittel-Forschung 31 (4): 737–740.
- Christensen, I; Geismar, L; Kirkegaard, A; Kirkegaard, G (May 1986). "Additional studies on side effects of melperone in long-term therapy for 1-20 years in psychiatric patients". Arzneimittel-Forschung 36 (5): 855–860.
- Gahr, M; Gastl, R; Kölle, MA; Schönfeldt-Lecuona, C; Freudenmann, RW (2012). "Successful treatment of schizophrenia with melperone augmentation in a patient with phenotypic CYP2D6 ultrarapid metabolization: a case report". Journal of Medical Case Reports 6 (1): 49.
- Köhnke, MD; Lutz, U; Wiatr, G; Schwärzler, F; Weller, B; Schott, K; Buchkremer, G (April 2006). "Cytochrome P450 2D6 dependent metabolization of risperidone is inhibited by melperone". European Journal of Clinical Pharmacology 62 (4): 333–334.
- Grözinger, M; Dragicevic, A; Hiemke, C; Shams, M; Müller, MJ; Härtter, S (January 2003). "Melperone is an inhibitor of the CYP2D6 catalyzed O-demethylation of venlafaxine". Pharmacopsychiatry 36 (1): 3–6.
- Seeman, P (January 2004). "Atypical Antipsychotics: Mechanism of Action" (PDF). FOCUS: The Journal of Lifelong Learning in Psychiatry 2 (1): 48–58.
- Roth, BL; Driscol, J. Database"i"PDSP K. Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Retrieved 2013-10-14.
- PubChem Substance
- ClinicalTrials.gov NCT00125138