Moclobemide

Moclobemide
Clinical data
Trade namesAmira, Aurorix, Clobemix, Depnil, Manerix, others
AHFS/Drugs.comMicromedex Detailed Consumer Information
Pregnancy
category
  • AU: B3
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability55–95% (increases with repeat administration)[2][3]
Protein binding50%[3][4]
MetabolismLiver[7][5]
Elimination half-life1–2 hours,[5] 4 hours (elderly)[3][6]
ExcretionKidney, Faecal (<5%)[4]
Identifiers
  • 4-chloro-N-(2-morpholin-4-ylethyl)benzamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.163.935 Edit this at Wikidata
Chemical and physical data
FormulaC13H17ClN2O2
Molar mass268.74 g·mol−1
3D model (JSmol)
  • Clc1ccc(cc1)C(=O)NCCN2CCOCC2
  • InChI=1S/C13H17ClN2O2/c14-12-3-1-11(2-4-12)13(17)15-5-6-16-7-9-18-10-8-16/h1-4H,5-10H2,(H,15,17) checkY
  • Key:YHXISWVBGDMDLQ-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Moclobemide, sold under the brand names Amira, Aurorix,[8] Clobemix, Depnil and Manerix[9] among others, is a reversible inhibitor of monoamine oxidase A (RIMA) drug primarily used to treat depression and social anxiety.[10][11][12] It is not approved for use in the United States,[13] but is approved in other Western countries such as Canada, the UK[12] and Australia.[14] It is produced by affiliates of the Hoffmann–La Roche pharmaceutical company. Initially, Aurorix was also marketed by Roche in South Africa, but was withdrawn after its patent rights expired and Cipla Medpro's Depnil and Pharma Dynamic's Clorix became available at half the cost.

No significant rise in blood pressure occurs when moclobemide is combined with amines such as tyramine-containing foods or pressor amine drugs, unlike with the older irreversible and non-selective monoamine oxidase inhibitors (MAOIs), which cause a severe rise in blood pressure with such combination.[10] Due to the lack of anticholinergic, cardiovascular, cognitive and psychomotor impairments moclobemide is advantageous in the elderly as well as those with cardiovascular disease.[10]

Moclobemide was first introduced for medical use in 1989.[15][16]

  1. ^ Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
  2. ^ Cite error: The named reference pmid1377119 was invoked but never defined (see the help page).
  3. ^ a b c Freeman H (December 1993). "Moclobemide". Lancet. 342 (8886–8887): 1528–1532. doi:10.1016/S0140-6736(05)80090-X. PMID 7902906. S2CID 208793357.
  4. ^ a b Schoerlin MP, Mayersohn M, Korn A, Eggers H (October 1987). "Disposition kinetics of moclobemide, a monoamine oxidase-A enzyme inhibitor: single and multiple dosing in normal subjects". Clinical Pharmacology and Therapeutics. 42 (4): 395–404. doi:10.1038/clpt.1987.169. PMID 3665338. S2CID 46130982.
  5. ^ a b Cite error: The named reference pmid2248087 was invoked but never defined (see the help page).
  6. ^ Gex-Fabry M, Balant-Gorgia AE, Balant LP (February 1995). "Potential of concentration monitoring data for a short half-life drug: analysis of pharmacokinetic variability for moclobemide". Therapeutic Drug Monitoring. 17 (1): 39–46. doi:10.1097/00007691-199502000-00007. PMID 7725375. S2CID 7044652.
  7. ^ Cite error: The named reference pmid2248086 was invoked but never defined (see the help page).
  8. ^ Scheen AJ (May 1994). "[Drug of the month. Moclobemide (Aurorix)]". Revue Médicale de Liège (in French). 49 (5): 291–292. PMID 8023056.
  9. ^ Cite error: The named reference pmid7905288 was invoked but never defined (see the help page).
  10. ^ a b c Cite error: The named reference pmid8875133 was invoked but never defined (see the help page).
  11. ^ Cite error: The named reference AMH was invoked but never defined (see the help page).
  12. ^ a b Cite error: The named reference BNF was invoked but never defined (see the help page).
  13. ^ Cite error: The named reference pmid10063483 was invoked but never defined (see the help page).
  14. ^ Cite error: The named reference SANDOZ was invoked but never defined (see the help page).
  15. ^ Bonnet U (2002). "Moclobemide: evolution, pharmacodynamic, and pharmacokinetic properties". CNS Drug Rev. 8 (3): 283–308. doi:10.1111/j.1527-3458.2002.tb00229.x. PMC 6741699. PMID 12353059.
  16. ^ Semple D, Smyth R (2013). Oxford Handbook of Psychiatry. Oxford Medical Handbooks. OUP Oxford. p. 29. ISBN 978-0-19-969388-7. Retrieved 10 October 2024.