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Phenelzine

Phenelzine
Phenelzine2DACS.svg
Phenelzine3Dan2.gif
Clinical data
Trade names Nardil
AHFS/Drugs.com Monograph
MedlinePlus a682089
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
Routes of
administration
Oral
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Metabolism Liver
Biological half-life 11.6 hours
Excretion Urine
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard 100.000.108
Chemical and physical data
Formula C8H12N2
Molar mass 136.19 g/mol
3D model (Jmol)
Boiling point 74 °C (165 °F)
  

Phenelzine (Nardil, Nardelzine) is a non-selective and irreversible monoamine oxidase inhibitor (MAOI) of the hydrazine class which is used as an antidepressant and anxiolytic. Along with tranylcypromine and isocarboxazid, phenelzine is one of the few non-selective MAOIs still in widespread clinical use. It is typically available in 15 mg tablets and doses usually range from 30–90 mg per day, with 15 mg every day or every other day suggested as a maintenance dose following a successful course of treatment.

Phenelzine is used primarily in the treatment of major depressive disorder (MDD). Patients with depressive symptomology characterized as "atypical", "nonendogenous", and/or "neurotic" respond particularly well to phenelzine. The medication is also useful in patients who do not respond favorably to first and second-line treatments for depression, or are "treatment-resistant". In addition to being a recognized treatment for major depressive disorder, phenelzine is effective in treating dysthymia,bipolar depression (BD),panic disorder (PD),social anxiety disorder,bulimia, and post-traumatic stress disorder (PTSD).

Phenelzine is a non-selective and irreversible inhibitor of the enzyme monoamine oxidase (MAO). It inhibits both of the respective isoforms of MAO, MAO-A and MAO-B, and does so almost equally, with slight preference for the former. By inhibiting MAO, phenelzine prevents the breakdown of the monoamine neurotransmitters serotonin, melatonin, norepinephrine, epinephrine, and dopamine, as well as the trace amine neuromodulators such as phenethylamine, tyramine, octopamine, and tryptamine. This leads to an increase in the extracellular concentrations of these neurochemicals and therefore an alteration in neurochemistry and neurotransmission. This action is thought to be the primary mediator in phenelzine's therapeutic benefits.


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