Description

Simple

A medication used to treat depression, bipolar disorder, and anxiety associated with depression.

Clinical

A tetracyclic antidepressant used to treat depressive illness, major depressive disorder, bipolar disorder, and anxiety associated with depression.

Overview

Maprotiline is a tetracyclic antidepressant with similar pharmacological properties to tricyclic antidepressants (TCAs). Similar to TCAs, maprotiline inhibits neuronal norepinephrine reuptake, possesses some anticholinergic activity, and does not affect monoamine oxidase activity. It differs from TCAs in that it does not appear to block serotonin reuptake. Maprotiline may be used to treat depressive affective disorders, including dysthymic disorder (depressive neurosis) and major depressive disorder. Maprotiline is effective at reducing symptoms of anxiety associated with depression.

Pharmacology

Indication

For treatment of depression, including the depressed phase of bipolar depression, psychotic depression, and involutional melancholia, and may also be helpful in treating certain patients suffering severe depressive neurosis.

Pharmacodynamic

Maprotiline is a tetracyclic antidepressant. Although its main therapeutic use is in the treatment of depression, it has also been shown to exert a sedative effect on the anxiety component that often accompanies depression. In one sleep study, it was shown that maprotiline increases the duration of... Read more

Mechanism of action

Maprotiline exerts its antidepressant action by inhibition of presynaptic uptake of catecholamines, thereby increasing their concentration at the synaptic clefts of the brain. In single doses, the effect of maprotiline on the EEG revealed a rise in the alpha-wave density, a reduction of the alpha-wa... Read more

Absorption

Slowly, but completely absorbed from the GI tract following oral administration.

Protein binding

88%

Volume of distribution

Maprotiline and its metabolites may be detected in the lungs, liver, brain, and kidneys; lower concentrations may be found in the adrenal glands, heart and muscle. Maprotiline is readily distributed into breast milk to similar concentrations as those in maternal blood.

Clearance

Information currently not available.

Half life

Average ~ 51 hours (range: 27-58 hours)

Route of elimination

Approximately 60% of a single orally administered dose is excreted in urine as conjugated metabolites within 21 days; 30% is eliminated in feces.

Toxicity

LD50=~900 mg/kg (Orally in rats); LD50=90 mg/kg (Orally in women); Signs of overdose include motor unrest, muscular twitching and rigidity, tremor, ataxia, convulsions, hyperpyrexia, vertigo, mydriasis, vomiting, cyanosis, hypotension, shock, tachycardia, cardiac arrhythmias, i... Read more

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

  • Limit caffeine intake.
  • Take with or without food.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Maprotiline.
(S)-Warfarin
The risk or severity of adverse effects can be increased when Maprotiline is combined with (S)-Warfarin.
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine
The metabolism of Maprotiline can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
1,10-Phenanthroline
The therapeutic efficacy of Maprotiline can be decreased when used in combination with 1,10-Phenanthroline.
2,5-Dimethoxy-4-ethylamphetamine
2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative and stimulatory activities of Maprotiline.
2,5-Dimethoxy-4-ethylthioamphetamine
2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative and stimulatory activities of Maprotiline.
4-Bromo-2,5-dimethoxyamphetamine
4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative and stimulatory activities of Maprotiline.
4-hydroxycoumarin
The risk or severity of adverse effects can be increased when Maprotiline is combined with 4-hydroxycoumarin.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when Maprotiline is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Maprotiline is combined with 5-methoxy-N,N-dimethyltryptamine.
6-O-benzylguanine
The metabolism of 6-O-benzylguanine can be decreased when combined with Maprotiline.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Maprotiline is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Maprotiline.
8-azaguanine
The metabolism of 8-azaguanine can be decreased when combined with Maprotiline.
8-chlorotheophylline
The metabolism of 8-chlorotheophylline can be decreased when combined with Maprotiline.
9-Deazaguanine
The metabolism of 9-Deazaguanine can be decreased when combined with Maprotiline.
9-Methylguanine
The metabolism of 9-Methylguanine can be decreased when combined with Maprotiline.
Abacavir
Maprotiline may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abatacept
The metabolism of Maprotiline can be increased when combined with Abatacept.
Abediterol
The risk or severity of Tachycardia can be increased when Maprotiline is combined with Abediterol.