Melperone

Jump to: navigation, search
Melperone
Melperone Wiki Str.png
Melperone3Dan.gif
Clinical data
Trade namesBuronil
AHFS/Drugs.comInternational Drug Names
Routes of
administration
Oral, intramuscular injection
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability87% (IM), 54% (Oral via syrup), 65% (Oral, tablet)[1]
Protein binding50%
MetabolismHepatic
Elimination half-life3–4 hours (oral)[1]
6 hours (IM)
ExcretionRenal, 70% as metabolites, 5.5-10.4% as unchanged drug[1][2]
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC16H22FNO
Molar mass263.35 g/mol
3D model (JSmol)
  (verify)

WikiDoc Resources for Melperone

Articles

Most recent articles on Melperone

Most cited articles on Melperone

Review articles on Melperone

Articles on Melperone in N Eng J Med, Lancet, BMJ

Media

Powerpoint slides on Melperone

Images of Melperone

Photos of Melperone

Podcasts & MP3s on Melperone

Videos on Melperone

Evidence Based Medicine

Cochrane Collaboration on Melperone

Bandolier on Melperone

TRIP on Melperone

Clinical Trials

Ongoing Trials on Melperone at Clinical Trials.gov

Trial results on Melperone

Clinical Trials on Melperone at Google

Guidelines / Policies / Govt

US National Guidelines Clearinghouse on Melperone

NICE Guidance on Melperone

NHS PRODIGY Guidance

FDA on Melperone

CDC on Melperone

Books

Books on Melperone

News

Melperone in the news

Be alerted to news on Melperone

News trends on Melperone

Commentary

Blogs on Melperone

Definitions

Definitions of Melperone

Patient Resources / Community

Patient resources on Melperone

Discussion groups on Melperone

Patient Handouts on Melperone

Directions to Hospitals Treating Melperone

Risk calculators and risk factors for Melperone

Healthcare Provider Resources

Symptoms of Melperone

Causes & Risk Factors for Melperone

Diagnostic studies for Melperone

Treatment of Melperone

Continuing Medical Education (CME)

CME Programs on Melperone

International

Melperone en Espanol

Melperone en Francais

Business

Melperone in the Marketplace

Patents on Melperone

Experimental / Informatics

List of terms related to Melperone

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Melperone (Bunil (PT), Buronil (AT, BE, CZ, DK, FL†, 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]

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]

Adverse effects

Melperone is reported to produce significantly less weight gain than clozapine and approximately as much weight gain as typical antipsychotics.[11] It is also purported to produce around as much prolactin secretion as clozapine (which is virtually nill).[12] It is also purported to produce sedative effects[13] and QT interval prolongation.[14] It is also known to produce less extrapyramidal side effects than the first-generation (typical) antipsychotic, thiothixene.[15] It can also produce (usually relatively mild) dry mouth.[16]

Other common adverse effects include[17][18][19]

* tremor, dystonia, hypokinesis, akathisia, dyskinesias

Rare adverse effects include[17][18][19]
Unknown frequency adverse effects include[17][18][19]
  • Seizures (probably rare/uncommon)
  • Increased intraocular pressure
  • Intrahepatic cholestasis (probably rare)
  • Orthostatic hypotension (probably common)
  • Arrhythmias
  • Rash
  • Hyperprolactinaemia**
  • Weight gain
  • Increased appetite

** which can lead to galactorrhoea, gynecomastia, etc.

Interactions

Melperone is reported to be a CYP2D6 inhibitor.[20][21][22]

Pharmacology

Melperone 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.[23]

Receptor Ki [nM][24]
5-HT1A 2,200
5-HT1D 3,400
5-HT2A 230
5-HT2C 2,100
5-HT6 1,254
5-HT7 578
α1 180
α2 150
M1 >10,000
M2 2,400
M3 >10,000
M4 4,400
M5 >10,000
D2 194
D3 8.95
D4 555
H1 580

References

  1. 1.0 1.1 1.2 Borgström, L; Larsson, H; Molander, L (1982). "Pharmacokinetics of parenteral and oral melperone in man". European Journal of Clinical Pharmacology. 23 (2): 173–176. doi:10.1007/BF00545974. PMID 7140807.
  2. Product Information: Eunerpan(R), Melperonhydrochlorid. Knoll Deutschland GmbH, Ludwigshafen, 1995.
  3. 3.0 3.1 Melperone Hydrochloride. Martindale: The Complete Drug Reference. The Royal Pharmaceutical Society of Great Britain. 30 January 2013. Retrieved 3 November 2013.
  4. 4.0 4.1 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. doi:10.1100/2012/512047. PMC 3330679. PMID 22566771.
  5. Whiskey, E (February 2011). "Melperone in Treatment-Refractory Schizophrenia: A Case Series". Therapeutic Advances in Psychopharmacology. 1 (1): 19–23. doi:10.1177/2045125311399800. PMC 3736899. PMID 23983923. Unknown parameter |coauthors= ignored (help)
  6. Meltzer, HY; Sumiyoshi, T; Jayathilake, K (December 2001). "Melperone in the treatment of neuroleptic-resistant schizophrenia". Psychiatry Research. 105 (3): 201–209. doi:10.1016/s0165-1781(01)00346-8. PMID 11814539.
  7. 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. doi:10.1097/00004850-200405000-00039.
  8. 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.
  9. Friedman, JH (May 2012). "Melperone is ineffective in treating Parkinson's disease psychosis". Movement Disorders. 27 (6): 803–804. doi:10.1002/mds.24942. PMID 22362330.
  10. Pöldinger, WJ (1984). "Melperone in low doses in anxious neurotic patients. A double-blind placebo-controlled clinical study". Neuropsychobiology. 11 (3): 181–186. doi:10.1159/000118074. PMID 6147789.
  11. 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. doi:10.1016/j.psychres.2009.03.026. PMID 20199813.
  12. 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. doi:10.1002/hup.1036. PMID 19551763.
  13. Molander, L; Borgström, L (1983). "Sedative effects and prolactin response to single oral doses of melperone". Psychopharmacology. 79 (2–3): 142–147. doi:10.1007/bf00427801. PMID 6133301.
  14. 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. doi:10.1097/00005344-199001000-00023. PMID 1688972.
  15. Bjerkenstedt, L (1989). "Melperone in the treatment of schizophrenia". Acta Psychiatrica Scandinavica Supplementum. 352: 35–39. PMID 2479227.
  16. 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. doi:10.1007/bf00432171. PMID 6119724.
  17. 17.0 17.1 17.2 "Product Information: Eunerpan(R), Melperonhydrochlorid". Knoll Deutschland GmbH, Ludwigshafen. 1995. Missing or empty |url= (help)
  18. 18.0 18.1 18.2 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. PMID 6113835.
  19. 19.0 19.1 19.2 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. PMID 2873821.
  20. 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. doi:10.1186/1752-1947-6-49. PMC 3298719. PMID 22309430.
  21. 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. doi:10.1007/s00228-006-0098-y. PMID 16534635.
  22. 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. doi:10.1055/s-2003-38084. PMID 12649767.
  23. Seeman, P (January 2004). "Atypical Antipsychotics: Mechanism of Action" (PDF). FOCUS: The Journal of Lifelong Learning in Psychiatry. 2 (1): 48–58.
  24. Roth, BL; Driscol, J. "PDSP Ki Database". 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.

External links


Linked-in.jpg