Phenelzine
Clinical data | |
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Trade names | Nardil |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682089 |
License data |
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Pregnancy category |
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Routes of administration | By mouth |
ATC code | |
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Pharmacokinetic data | |
Metabolism | Liver |
Elimination half-life | 11.6 hours |
Excretion | Urine |
Identifiers | |
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JSmol) | |
Boiling point | 74 °C (165 °F) |
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Phenelzine, sold under the brand name Nardil, among others, is a
Synthesis of phenelzine was first described by Emil Votoček and Otakar Leminger in 1932.[5][6]
Medical uses
Phenelzine is primarily used in the
Pharmacology
Pharmacodynamics
Phenelzine is a non-selective and
Phenelzine and its metabolites also inhibit at least two other enzymes to a lesser extent, of which are
Phenelzine has also been shown to metabolize to phenethylamine (PEA).
Like many other antidepressants, phenelzine usually requires several weeks of treatment to achieve full therapeutic effects. The reason for this delay is not fully understood. Still, it is believed to be due to many factors, including achieving steady-state levels of MAO inhibition and the resulting adaptations in mean neurotransmitter levels, the possibility of necessary
Pharmacokinetics
Phenelzine is administered orally in the form of phenelzine sulfate[4] and is rapidly absorbed from the gastrointestinal tract.[25] The time to peak plasma concentration is 43 minutes, and the half-life is 11.6 hours.[26] Unlike most other drugs, phenelzine irreversibly disables MAO. As a result, it does not necessarily need to be present in the blood at all times for its effects to be sustained. Because of this, upon phenelzine treatment being ceased, its effects typically do not wear off until the body replenishes its enzyme stores, a process which can take as long as 2–3 weeks.[4]
Phenelzine is
Adverse effects
Common side effects of phenelzine may include
Interactions
The MAOIs have certain dietary restrictions and drug interactions.
Phenelzine has also been linked to vitamin B6 deficiency.[30] Transaminases such as GABA-transaminase have been shown to be dependent upon vitamin B6[31] and may be involved in a potentially related process, since the phenelzine metabolite phenylethylidenehydrazine (PEH) is a GABA transaminase inhibitor. Both phenelzine and vitamin B6 are rendered inactive upon these reactions occurring. The pyridoxine form of B6 is recommended for supplementation, since this form has been shown to reduce hydrazine toxicity from phenelzine and, in contrast, the pyridoxal form has been shown to increase the toxicity of hydrazines.[32]
Research
Phenelzine showed promise in a phase II clinical trial from March 2020 in treating prostate cancer.[33] Phenelzine has also been shown to have neuroprotective effects in animal models.[34][35][36]
References
- ^ "Phenelzine (Nardil) Use During Pregnancy". Drugs.com. 3 March 2020. Retrieved 11 July 2020.
- ^ Anvisa (31 March 2023). "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 4 April 2023). Archived from the original on 3 August 2023. Retrieved 16 August 2023.
- ^ "Phenelzine: MedlinePlus Drug Information". medlineplus.gov. Retrieved 27 October 2023.
- ^ PMID 32119395. Retrieved 23 November 2023.
- The Merck Index(12th ed.). Whitehouse Station: Merck & Co. 7181.
- .
- ^ Parke-Davis Division of Pfizer Inc. (2007). "Nardil(R) (Phenelzine sulfate tablets, USP), labeling information" (PDF). U.S. Food and Drug Administration's. Archived (PDF) from the original on 27 November 2009. Retrieved 14 December 2009.
- PMID 15552546.
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- ^ "Phenelzine". go.drugbank.com. Retrieved 23 November 2023.
- ^ "Phenelzine: Package Insert". Drugs.com. Retrieved 23 November 2023.
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- doi:10.13140/RG.2.2.11909.40165. Archived from the original on 8 January 2022. Retrieved 8 January 2022.[self-published source?]
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- Lay summary in: McDonald R (25 March 2020). "Antidepressant Appears Safe, Effective in Men with Biochemical Recurrent Prostate Cancer". Curetoday.com.
- S2CID 75140657.
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- PMID 27750484.