Adult: In patients clinically characterised as atypical, nonendogenous, neurotic or who have not responded to other antidepressants: Initially, 15 mg tid; may increase dose to 15 mg 4 times daily after 2 weeks, if necessary. For severe cases, may give up to 30 mg tid. Gradually reduce the dose once target response is achieved. Usual maintenance dose: 15 mg every other day. Treatment and dosing recommendations may vary among individual products and between countries (refer to specific product guidelines). Elderly: Initiate at the lower end of the dosing range.
Renal Impairment
Severe: Contraindicated.
Hepatic Impairment
Contraindicated.
Contraindications
Cerebrovascular disease, phaeochromocytoma, CHF, abnormal LFTs or history of hepatic disease. Hepatic and severe renal impairment. Concomitant use with or within 14 days of discontinuing other MAOIs, bupropion, buspirone, dibenzazepine derivative agents (including TCAs, perphenazine, carbamazepine), SSRIs, SNRIs, sympathomimetics or related compounds. Concurrent use with guanethidine, dextromethorphan, CNS depressants (e.g. alcohol, narcotic analgesics), local anaesthesia containing sympathomimetic vasoconstrictors, spinal anaesthesia, ophthalmic agents (e.g. apraclonidine). Concurrent use or within 5 weeks of discontinuing fluoxetine. Contraindications may vary between individual products (refer to specific product labelling for detailed information).
Special Precautions
Patient with diabetes mellitus, hyperthyroidism, angle-closure glaucoma, bipolar disorder, blood dyscrasias, porphyria, CV disease; risk for seizures (e.g. history of seizures, head trauma, brain damage, alcoholism, concurrent use with medications that may lower seizure threshold). Withhold therapy for at least 10 days before elective surgery. Patients undergoing electroconvulsive therapy. Avoid abrupt withdrawal. Not indicated for use in manic phase. Elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Increased risk of suicidal thinking and behaviour; CNS depression; shift to mania or hypomania (particularly in patients with bipolar disorder); postural hypotension, sensitisation to insulin, pyridoxine deficiency. Eye disorders: Blurred vision. Gastrointestinal disorders: Nausea, vomiting, dry mouth, constipation. General disorders and administration site conditions: Oedema, weakness, fatigue. Investigations: Elevated serum transaminases. Musculoskeletal and connective tissue disorders: Myoclonic movements, hyperreflexia. Nervous system disorders: Headache, dizziness, drowsiness. Psychiatric disorders: Insomnia, anorgasmia. Potentially Fatal: Hypertensive crisis associated with intracranial bleeding.
Patient Counseling Information
This drug may cause CNS depression, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor blood pressure, heart rate, blood glucose, renal function, liver function and mental status. Assess for signs of worsening depression, suicidality or unusual changes in behaviour (particularly at the start of treatment or during dose adjustments).
Overdosage
Symptoms: Drowsiness, dizziness, faintness, severe headache, irritability, agitation, hyperactivity, hallucinations, trismus, opisthotonus, rigidity, convulsions, rapid and irregular pulse, precordial pain, respiratory depression and failure, hyperpyrexia, diaphoresis, cool and clammy skin; hypomania, euphoria followed by coma with hypotension, acute hypertension with subarachnoid haemorrhage, extrapyramidal symptoms. Management: Intensive symptomatic and supportive treatment. Induce emesis or perform gastric lavage. Support respiration by airway management, supplemental oxygen and mechanical ventilation, if necessary. Correct hypertension with IV phentolamine. Monitor body temperature and manage fever by cooling. Maintain fluid and electrolyte balance with IV therapy. May administer slow IV inj of diazepam for any CNS stimulation. In case of severe hypotension and deep coma, hydrocortisone inj may be given.
Drug Interactions
May potentiate the effects of antihypertensives, hypoglycaemic agents, anti-Parkinson agents, local anaesthetics and antimuscarinics. Potentially Fatal: May enhance serotonergic effect with buspirone, dextromethorphan, pethidine, TCAs, SSRIs (e.g. fluoxetine, sertraline, paroxetine, citalopram), SNRIs or other serotonergic agents. May result in hypertensive crises when given concomitantly with sympathomimetic agents (e.g. amphetamines, cocaine, methylphenidate, dopamine, epinephrine, norepinephrine, ephedrine) and related compounds (e.g. methyldopa, levodopa, tryptophan). Increased risk of hypertension with guanethidine and bupropion. May increase the adverse or toxic effects of perphenazine, apraclonidine and morphine. Increased risk of toxicity with carbamazepine.
Food Interaction
May potentiate the effects of alcohol. Increased risk of hypertensive crisis with foods and beverages rich in tyramine.
Action
Description: Mechanism of Action: Phenelzine is a monoamine oxidase (MAO) inhibitor antidepressant. It is believed to act by increasing the endogenous levels of norepinephrine, dopamine and serotonin through inhibition of MAO, which is the enzyme responsible for breaking down these neurotransmitters. Onset: Initial effects: Within 1-2 weeks with continued improvements through 4-6 weeks. Pharmacokinetics: Absorption: Readily absorbed from the gastrointestinal tract. Time to peak plasma concentration: 43 minutes. Metabolism: Extensively metabolised mainly via oxidation by MAO and via acetylation (minor pathway) into N2-acetylphenelzine. Excretion: Via urine (73% as metabolites). Elimination half-life: 11.6 hours.
Chemical Structure
Phenelzine Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3675, Phenelzine. https://pubchem.ncbi.nlm.nih.gov/compound/Phenelzine. Accessed Oct. 29, 2024.
Storage
Store between 2-8°C. Do not freeze. Storage recommendations may vary among individual products and between countries (refer to specific product guidelines).
N06AF03 - phenelzine ; Belongs to the class of non-selective monoamine oxidase inhibitors. Used in the management of depression.
References
Anon. Phenelzine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 01/10/2024.Brayfield A, Cadart C (eds). Phenelzine Sulfate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/10/2024.Joint Formulary Committee. Phenelzine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/10/2024.Nardil 15 mg Film-coated Tablets (Neon Healthcare Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 01/10/2024.Neon Healthcare Ltd. Nardil 15 mg Film Coated Tablet data sheet 19 April 2024. Medsafe. http://www.medsafe.govt.nz. Accessed 01/10/2024.Phenelzine Sulfate Tablet, Film Coated (Greenstone LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 01/10/2024.Phenelzine. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 01/10/2024.
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