Chemistry:Isocarboxazid
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| Clinical data | |
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| Trade names | Marplan |
| AHFS/Drugs.com | Consumer Drug Information |
| MedlinePlus | a605036 |
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| Routes of administration | Oral |
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| Pharmacokinetic data | |
| Bioavailability | Low, peak at 1-2 h[1] |
| Metabolism | Liver (Carboxylesterase[3]) |
| Metabolites | Hippuric acid[2] |
| Elimination half-life | 1.5-4h[1] |
| Excretion | Urine |
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| Chemical and physical data | |
| Formula | C12H13N3O2 |
| Molar mass | 231.255 g·mol−1 |
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Isocarboxazid (Marplan, Marplon, Enerzer) is a non-selective, irreversible monoamine oxidase inhibitor (MAOI) of the hydrazine class used as an antidepressant.[4] Along with phenelzine and tranylcypromine, it is one of only three classical MAOIs still available for clinical use in the treatment of psychiatric disorders in the United States ,[5][6] though it is not as commonly employed in comparison to the others.[5][6]
Isocarboxazid is primarily used to treat mood and anxiety disorders. It has also been investigated in the treatment of schizophrenia,[7] Parkinson's disease and other dementia-related disorders.[8]
Isocarboxazid, as well as other MAOIs, increase the levels of the monoamine neurotransmitters serotonin, dopamine, norepinephrine, epinephrine, melatonin, phenethylamine in the brain.[9]
Classical MAOIs, including isocarboxazid, are used only rarely due to prominent food and drug interactions and have been largely superseded by newer antidepressants such as the selective serotonin reuptake inhibitors (SSRIs). The cause of the interactions is because MAOIs inhibit the metabolism of dietary amines (e.g., tyramine) and the monoamine neurotransmitters. In combination with other drugs that increase the levels of the monoamine neurotransmitters such as the SSRIs, or with certain foods high in dietary amines such as aged cheeses, MAOIs can produce dangerous elevations of monoamine neurotransmitters resulting in potentially life-threatening syndromes such as hypertensive crisis and serotonin syndrome.
See also
References
- ↑ 1.0 1.1 "Clinical psychopharmacology.". Companion to psychiatric studies.. January 2010. pp. 227–294. doi:10.1016/B978-0-7020-3137-3.00011-5. ISBN 9780702031373.
- ↑ "Reaction: Isocarboxazid to 1 product". https://go.drugbank.com/reactions/2399.
- ↑ "Inhibitory effect of leptophos on carboxylesterase (isocarboxazid amidase) in rat liver". Toxicology Letters 11 (1–2): 81–85. April 1982. doi:10.1016/0378-4274(82)90110-2. PMID 6178187.
- ↑ "Inhibition of monoamine oxidase in monoaminergic neurones in the rat brain by irreversible inhibitors". Biochemical Pharmacology 35 (8): 1381–1387. April 1986. doi:10.1016/0006-2952(86)90285-6. PMID 2870717.
- ↑ 5.0 5.1 Pocket Guide For The Textbook Of Pharmacotherapy For Child And Adolescent Psychiatric Disorders. Routledge. 21 August 2013. pp. 176–. ISBN 978-1-134-86002-9. https://books.google.com/books?id=fep_AAAAQBAJ&pg=PA176.
- ↑ 6.0 6.1 Handbook of Psychiatric Drug Therapy. Lippincott Williams & Wilkins. 28 March 2012. pp. 99–. ISBN 978-1-4511-5307-1. https://books.google.com/books?id=xrZfcE8MydIC&pg=PA99.
- ↑ "Isocarboxazid (marplan) in ambulatory psychiatric patients". The American Journal of Psychiatry 116 (4): 355–356. October 1959. doi:10.1176/ajp.116.4.355. PMID 13814129.
- ↑ "MAO-inhibitors in Parkinson's Disease". Experimental Neurobiology (Experimental Neurology) 20 (1): 1–17. March 2011. doi:10.5607/en.2011.20.1.1. PMID 22110357.
- ↑ "Monoamine oxidase inhibitors. A perspective on their use in the elderly". Drugs & Aging 13 (5): 341–55. November 1998. doi:10.2165/00002512-199813050-00002. PMID 9829163.
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