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 h.
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 h.
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 MAOIs.
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.
MAOIs
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 function 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 adverse reactions.
- 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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