Maprotiline


Concise Prescribing Info
Indications/Uses
Depression.
Dosage/Direction for Use
Adult : PO Mild to moderate: Initial: 75 mg/day in single or divided doses for 2 wk, then increase as needed. Max: 150 mg/day. Severely depressed, hospitalised patient: Initial: 100-150 mg/day. Max: 225 mg/day.
Dosage Details
Oral
Depression
Adult: Mild to moderate: Initially, 75 mg daily as single or in divided doses for 2 wk, then gradually increase in 25 mg increments as required and tolerated. Max: 150 mg daily. Severely depressed, hospitalised patient: Initially, 100-150 mg daily, gradually increased as required and tolerated. Max: 225 mg daily.
Elderly: Initially, 25 mg daily. May increase gradually to 50-75 mg daily, according to response.
Administration
May be taken with or without food.
Contraindications
Seizure disorders. Concomitant use during or w/in 14 days of MAOI use.
Special Precautions
Patient w/ history of increased intraocular pressure, phaeochromocytoma, chronic severe constipation and urinary retention (e.g. prostatic disease), risk of QT prolongation, bipolar disorder (or risk of), CV disease (e.g MI), hyperthyroidism, nocturnal enuresis. Renal and hepatic impairment. Elderly. Pregnancy and lactation. Concomitant electroconvulsive therapy. Avoid abrupt withdrawal.
Adverse Reactions
Significant: Suicidality, clinical worsening, unusual behavioural changes, anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia, seizures, mild pupillary dilation. Rarely, hypomanic or manic episodes, neutrophil depression.
Nervous: Drowsiness, dizziness, nervousness, headache, tremor.
CV: Sinus tachycardia, palpitations, flushing, orthostatic hypotension.
GI: Dry mouth, constipation, nausea, vomiting, abdominal disorders, increased appetite.
Genitourinary: Erectile dysfunction, micturition disorder.
Endocrine: Hot flush, abnormal wt gain.
Musculoskeletal: Muscular weakness.
Ophthalmologic: Blurred vision, accommodation disorder.
Dermatologic: Rash, urticaria, photosensitivity, hyperhidrosis.
Others: Fatigue, pyrexia.
Potentially Fatal: Rarely, ventricular tachycardia, ventricular fibrillation, torsade de pointes.
Patient Counseling Information
This drug may cause blurred vision, dizziness and other CNS symptoms, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor for symptoms of clinical worsening, unusual changes in behaviour and emergence of suicidality esp during initiation or dosage adjustment.
Overdosage
Symptoms: Somnolence, stupor, coma, ataxia, restlessness, agitation, enhanced reflexes, muscular rigidity and choreo-athetotic movements, convulsions, hypotension, tachycardia, QT prolongation, arrhythmias, conduction disorders, shock, heart failure, ventricular tachycardia, ventricular fibrillation, torsade de pointes, cardiac arrest, resp depression, cyanosis, vomiting, fever, mydriasis, sweating and oliguria or anuria. Management: Symptomatic and supportive treatment. Protect patient’s airway. Establish an IV line and initiate GI decontamination including large volume gastric lavage followed by admin of activated charcoal.
Drug Interactions
May cause increased atropine-like effects w/ anticholinergic and sympathomimetic drugs. Phenothiazines and benzodiazepines (w/ rapidly tapered dose) may increase risk of seizures. Thyroid drugs may increase CV adverse effects. Increased plasma concentration w/ hepatic enzyme inhibitors (e.g. cimetidine, fluoxetine). Decreased plasma concentration w/ hepatic enzyme inducers (e.g. barbiturates, phenytoin). May increase effects of barbiturates and other CNS depressants. May decrease pharmacologic effects of antihypertensive drugs (e.g. guanethidine).
Potentially Fatal: Risk of severe interactions including hyperpyrexia, tremor, delirium, and generalised clonic convulsions w/ MAOIs.
Food Interaction
May increase CNS depressant effect of alcohol. Avoid alcohol.
Action
Description: Maprotiline, a tetracyclic antidepressant and non-selective monoamine reuptake inhibitor, also inhibits norepinephrine reuptake in the presynaptic neuronal membrane. It alleviates the mood, anxiety, agitation and psychomotor retardation.
Pharmacokinetics:
Absorption: Slowly but completely absorbed from the GI tract. Absolute bioavailability: 66-70%. Time to peak plasma concentration: 8-24 hr.
Distribution: Widely distributed. Enters breast milk. Volume of distribution: 23-27 L/kg. Plasma protein binding: 88-90%.
Metabolism: Metabolised in the liver via demethylation mainly by CYP2D6 to desmethylmaprotiline; further metabolised via hydroxylation and conjugation.
Excretion: Via urine (70%) and faeces (30%). Elimination half-life: 51 hr.
Chemical Structure

Chemical Structure Image
Maprotiline

Source: National Center for Biotechnology Information. PubChem Database. Maprotiline, CID=4011, https://pubchem.ncbi.nlm.nih.gov/compound/Maprotiline (accessed on Jan. 21, 2020)

Storage
Store between 20-25°C. Protect from light.
MIMS Class
ATC Classification
N06AA21 - maprotiline ; Belongs to the class of non-selective monoamine reuptake inhibitors. Used in the management of depression.
References
AFT Pharmaceuticals Ltd. Ludiomil 25 mg and 75 mg Film Coated Tablets data sheet 17 May 2016. Medsafe. http://www.medsafe.govt.nz/. Accessed 13/07/2017.

Anon. Maprotiline. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 13/07/2017.

Buckingham R (ed). Maprotiline. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/07/2017.

Maprotiline Hydrochloride Tablet, Film Coated (Mylan Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 13/07/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Maprotiline Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 13/07/2017.

Disclaimer: This information is independently developed by MIMS based on Maprotiline from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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