Dosing and uses of Maprotiline
Adult dosage forms and strengths
tablet
- 25mg
- 50mg
- 75mg
Depression
Outpatient (Mild to Moderate Depression)
- Initial 75 mg PO qDay for 2 weeks
- Increase by 25 mg increments to effective dosage; not to exceed 150 mg/day
- Maintenance: Decrease dose to 75-150 mg PO qDay once symptoms are controlled
- Geriatric: 50-75 mg PO qDay
Inpatient (Severe Depression)
- Initial 100-150 mg PO qDay for 2 weeks
- Increase cautiously to effective dosage; not to exceed 225 mg/day
- Geriatric: 50-75 mg PO qDay
Other Indications & Uses
Off-label: anxiety associated with depression
Pediatric dosage forms and strengths
Safety and effecay not established
Geriatric dosage forms and strengths
Initial dose: 25 mg PO at bedtime, if tolerated increase by 25 mg every 3 days for inpatients and weekly for outpatients.
Maintenance dose: 50-75 mg/day, may increase dose for nonresponders.
Maprotiline adverse (side) effects
Frequency not defined
Common
- Fatigue
- Sedation
- Lethargy
- Weakness
- Constipation
- Dry mouth
- Blurred vision
Less Common
- Agitation
- Anxiety
- Headache
- Insomnia
- Nausea
- Vomiting
- Sweating
Infrequent
- Orthostatic hypotension, ECG changes, tachycardia
- Confusion, EPS, dizziness, paresthesia, tinnitus
- Rash
- Incr LFTs
- Sexual dysfunction
Rare
- Seizure
- Agranulocytosis
- Thrombocytopenia
- Eosinophilia
- Leukopenia
- SIADH
Warnings
Black box warnings
In short-term studies, antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults (<24 yr of age) taking antidepressants for major depressive disorders and other psychiatric illnesses
This increase was not seen in patients aged >24 years; a slight decrease in suicidal thinking was seen in adults >65 years
In children and young adults, risks must be weighed against the benefits of taking antidepressants
Patients should be monitored closely for changes in behavior, clinical worsening, and suicidal tendencies; this should be done during initial 1-2 months of therapy and dosage adjustments
The patient’s family should communicate any abrupt changes in behavior to the healthcare provider
Worsening behavior and suicidal tendencies that are not part of the presenting symptoms may require discontinuation of therapy
This drug is not approved for use in pediatric patients
Contraindications
Hypersensitivity
Severe cardiovascular disorders
Narrow angle glaucoma
Within 14 days of MAO inhibitors may cause serotonin syndrome
Any drugs or conditions that prolong QT intervaL
Acute recovery post-MI
Cautions
Caution in BPH, urinary/GI retention, increased IOP, hyperthyroidism, open-angle glaucoma, seizure disorder, brain tumor, respiratory impairment
Clinical worsening & suicide ideation may occur despite medication in adolescents & young adults (18-24 years)
Risk of anticholinergic side-effects
May cause sedation (may impair physical and mental abilities), orthostatic hypotension, and anticholinergic effects
Pregnancy and lactation
Pregnancy category: B
Lactation: avoid during breastfeeding
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Maprotiline
Mechanism of action
Tetracyclic; may increase norepinephrine synaptic concentrations in the central nervous system by blocking NE reuptake by the presynaptic neuronal membrane; may also down regulate serotonin receptors and beta-adrenergic receptors and desensitize adenyl cyclase
Pharmacokinetics
Half-life elimination: 27-58 hr
Peak Plasma Time: within 12 hr (8-24 hr)
Bioavailability: Completely absorbed
Protein Bound: 88%
Metabolism: Liver
Metabolites: Desmethylmaprotiline
Excretion: Urine (70%); feces (30%)
