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|Maprotiline HCl

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Maprotiline HCl

Pronouncation: (ma-PRO-tih-leen HIGH-droe-KLOR-ide)
Class: Tetracyclic compound

Trade Names:
Ludiomil
- Tablets 25 mg
- Tablets 50 mg
- Tablets 75 mg

Novo-Maprotiline (Canada)

Mechanism of Action

Pharmacology

Inhibits norepinephrine (but not serotonin) reuptake.

Pharmacokinetics

Absorption

Mean T _max is 12 hr.

Distribution

Maprotiline protein binding is 88% and apparent Vd is 13 to 24 L/kg.

Metabolism

Maprotiline is metabolized in the liver.

Elimination

Maprotiline is excreted in urine and feces. The mean t _½ is 51 hr.

Indications and Usage

Depression; anxiety associated with depression.

Unlabeled Uses

Relief of chronic neurogenic pain.

Contraindications

Hypersensitivity to tricyclic antidepressants; MI acute recovery period; seizure disorder; concomitant use with MAO inhibitors.

Dosage and Administration

Adults Initial dose

PO 25 to 75 mg/day as single dose or divided doses. May be increased to 150 mg/day (outpatient) or 225 mg/day (inpatient).

Storage/Stability

Store at controlled room temperature.

Drug Interactions

Alcohol, CNS depressants

Additive CNS effects possible.

MAO inhibitors

May precipitate hypertensive crisis and convulsions with possibly fatal results. Discontinue at least 14 days before starting maprotiline.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Syncope; tachycardia; palpitations; orthostatic hypotension; hypertension; MI; arrhythmias; heart block.

CNS

Drowsiness; dizziness; hallucinations; disorientation; mania; exacerbation of psychosis; nervousness; fatigue; headache; anxiety; tremor; insomnia; agitation; seizures.

EENT

Blurred vision; mydriasis.

GI

Dry mouth; constipation; nausea; diarrhea.

Genitourinary

Impotence; urinary retention.

Hematologic

Bone marrow depression, including agranulocytosis; eosinophilia; purpura; thrombocytopenia; leukopenia.

Hepatic

Increased bilirubin and alkaline phosphatase.

Metabolic

Altered blood glucose levels.

Miscellaneous

Hypersensitivity (eg, rash, itching, photosensitivity, petechiae, edema, drug fever).

Precautions

Pregnancy

Category B .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established.

Elderly

Use lower doses.

Special Risk Patients

Use with caution in patients with history of seizures, urinary retention, urethral or ureteral spasm, angle-closure glaucoma or increased IOP, CV disorders, hyperthyroid patients or those receiving thyroid medication, hepatic or renal impairment, schizophrenic or paranoid patients.

Severe depression

Do not allow patient to possess more than small quantities of drug.

Seizures

May occur in therapeutic dose or overdose.

Overdosage

Symptoms

Hypotension, tachycardia, ventricular arrhythmias, CNS depression, seizures, respiratory depression, coma.

Patient Information

Explain that full effectiveness of drug may not occur until after several doses.
Instruct patient that if dose is missed, it should be taken as soon as possible unless close to time of next dose.
Warn patient not to double up doses and to notify health care provider if more than one dose is missed.
Explain that drug may cause dry mouth and constipation. Advise patient about measures to manage these side effects.
Advise diabetic patient that drug may alter blood glucose level.
Instruct patient not to take OTC medications without consulting health care provider.
Instruct patient to avoid intake of alcoholic beverages or other CNS depressants.
Instruct patient to report these symptoms to health care provider: difficult or infrequent voiding, dizziness, chest pain, palpitations, anxiety, depression, blurred vision, excessive dry mouth, mouth sores, severe constipation.
Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness.

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