Maprotiline

May be taken with or without food.

Seizure disorders. Concomitant use during or w/in 14 days of MAOI use.

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.

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.

PO: B

This drug may cause blurred vision, dizziness and other CNS symptoms, if affected, do not drive or operate machinery.

Monitor for symptoms of clinical worsening, unusual changes in behaviour and emergence of suicidality esp during initiation or dosage adjustment.

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.

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.

May increase CNS depressant effect of alcohol. Avoid alcohol.

Description:
Mechanism of Action: 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.

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

Store between 20-25°C. Protect from light.

Thuốc chống trầm cảm

N06AA21 - maprotiline ; Belongs to the class of non-selective monoamine reuptake inhibitors. Used in the management of depression.

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.