Look Up > Drugs > Maprotiline
Maprotiline
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Adverse Reactions
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(ma PROE ti leen)

U.S. Brand Names
Ludiomil®

Generic Available

Yes


Synonyms
Maprotiline Hydrochloride

Pharmacological Index

Antidepressant, Tetracyclic


Use

Treatment of depression and anxiety associated with depression


Pregnancy Risk Factor

B


Contraindications

Hypersensitivity to maprotiline; use of monoamine oxidase inhibitors within 14 days; use in a patient during the acute recovery phase of MI


Adverse Reactions

>10%:

Central nervous system: Drowsiness

Gastrointestinal: Xerostomia

1% to 10%:

Central nervous system: Insomnia, nervousness, anxiety, agitation, dizziness, fatigue, headache

Gastrointestinal: Constipation, nausea

Neuromuscular & skeletal: Tremor, weakness

Ocular: Blurred vision

<1%: Hypotension, hypertension, tachycardia, palpitations, arrhythmias, heart block, syncope, confusion, hallucinations, disorientation, delusions, restlessness, nightmares, hypomania, mania, exacerbation of psychosis, hyperglycemia, breast enlargement, rash, petechiae, photosensitivity, diaphoresis (excessive), vomiting, diarrhea, bitter taste, epigastric distress, abdominal cramps, dysphagia, weight gain or loss, edema of testicles, urinary retention, decreased libido, impotence, numbness, tingling, motor hyperactivity, akathisia, seizures, EPS, ataxia, dysarthria, accommodation disturbances, mydriasis, tinnitus


Drug Interactions

CYP1A2 and 2D6 enzyme substrate

Maprotiline inhibits the antihypertensive response to bethanidine, clonidine, debrisoquin, guanadrel, guanethidine, guanabenz, guanfacine; monitor BP; consider alternate antihypertensive agent

Abrupt discontinuation of clonidine may cause hypertensive crisis, maprotiline may enhance the response

Use with altretamine may cause orthostatic hypertension

Maprotiline may be additive with or may potentiate the action of other CNS depressants (sedatives, hypnotics, or ethanol); with MAO inhibitors, hyperpyrexia, hypertension, tachycardia, confusion, seizures, and deaths have been reported (serotonin syndrome), this combination should be avoided

Maprotiline may increase the prothrombin time in patients stabilized on warfarin

Cimetidine and methylphenidate may decrease the metabolism of maprotiline

Additive anticholinergic effects seen with other anticholinergic agents

The SSRIs, to varying degrees, inhibit the metabolism of TCAs and clinical toxicity may result

Use of lithium with a TCA may increase the risk for neurotoxicity

Phenothiazines may increase concentration of some TCAs and TCAs may increase concentration of phenothiazines; monitor for altered clinical response

TCAs may enhance the hypoglycemic effects of tolazamide, chlorpropamide, or insulin; monitor for changes in blood glucose levels

Cholestyramine and colestipol may bind TCAs and reduce their absorption; monitor for altered response

TCAs may enhance the effect of amphetamines; monitor for adverse CV effects

Verapamil and diltiazem appear to decrease the metabolism of imipramine and potentially other TCAs; monitor for increased TCA concentrations. The pressor response to I.V. epinephrine, norepinephrine, and phenylephrine may be enhanced in patients receiving TCAs; this combination is best avoided.

Grapefruit juice, indinavir, ritonavir may inhibit the metabolism of clomipramine and potentially other TCAs; monitor for altered effects; a decrease in TCA dosage may be required

Quinidine may inhibit the metabolism of TCAs; monitor for altered effect

Combined use of anticholinergics with TCAs may produce additive anticholinergic effects; combined use of beta-agonists with TCAs may predispose patients to cardiac arrhythmias


Mechanism of Action

Traditionally believed to increase the synaptic concentration of norepinephrine in the central nervous system by inhibition of their reuptake by the presynaptic neuronal membrane. However, additional receptor effects have been found including desensitization of adenyl cyclase, down regulation of beta-adrenergic receptors, and down regulation of serotonin receptors.


Pharmacodynamics/Kinetics

Absorption: Slow

Serum half-life: 27-58 hours (mean, 43 hours)

Time to peak serum concentration: Within 12 hours


Usual Dosage

Oral:

Adults: 75 mg/day to start, increase by 25 mg every 2 weeks up to 150-225 mg/day; given in 3 divided doses or in a single daily dose

Elderly: Initial: 25 mg at bedtime, increase by 25 mg every 3 days for inpatients and weekly for outpatients if tolerated; usual maintenance dose: 50-75 mg/day, higher doses may be necessary in nonresponders


Dietary Considerations

May be administered with food to decrease GI distress


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

Use with caution; epinephrine, norepinephrine and levonordefrin have been shown to have an increased pressor response in combination with TCAs


Dental Health: Effects on Dental Treatment

>10% of patients experience dry mouth; long-term treatment with TCAs such as amoxapine increases the risk of caries by reducing salivation and salivary buffer capacity


Patient Information

Avoid alcohol ingestion; do not discontinue medication abruptly; may cause drowsiness; full effect may not occur for 3-6 weeks; dry mouth may be helped by sips of water, sugarless gum, or hard candy; rise slowly to avoid dizziness


Nursing Implications

Offer patient sugarless hard candy for dry mouth

Monitor blood pressure and pulse rate prior to and during initial therapy; evaluate mental status; monitor weight and appetite


Dosage Forms

Tablet, as hydrochloride: 25 mg, 50 mg, 75 mg


References

Bergman RN and Watson WA, "Cardiac Toxicity Associated With Acute Maprotiline Self Poisoning," Am J Emerg Med, 1983, 2(2):144-6.

Boakes AJ, Laurence DR, Teoh PC, et al, "Interactions Between Sympathomimetic Amines and Antidepressant Agents in Man," Br Med J, 1973, 1(849):311-5.

Hrdina PD, Rovei V, Henry JF, et al, "Comparison of Single-Dose Pharmacokinetics of Imipramine and Maprotiline in the Elderly," Psychopharmacology, 1980, 70(1):29-34.

Jastak JT and Yagiela JA, "Vasoconstrictors and Local Anesthesia: A Review and Rationale for Use," J Am Dent Assoc, 1983, 107(4):623-30.

Larochelle P, Hamet P, and Enjalbert M, "Responses to Tyramine and Norepinephrine After Imipramine and Trazodone," Clin Pharmacol Ther, 1979, 26(1):24-30.

Mitchell JR, "Guanethidine and Related Agents. III Antagonism by Drugs Which Inhibit the Norepinephrine Pump in Man," J Clin Invest, 1970, 49(8):1596-604.

Rundegren J, van Dijken J, Mörnstad H, et al, "Oral Conditions in Patients Receiving Long-Term Treatment With Cyclic Antidepressant Drugs," Swed Dent J, 1985, 9(2):55-64.

Svedmyr N, "The Influence of a Tricyclic Antidepressive Agent (Protriptyline) on Some of the Circulatory Effects of Noradrenaline and Adrenalin in Man," Life Sci, 1968, 7(1):77-84.

Wynn RL, "New Antidepressant Medications," Gen Dent, 1997, 45(1):24-8.


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