LUDIOMIL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LUDIOMIL (LUDIOMIL).
Tricyclic antidepressant; inhibits reuptake of norepinephrine and serotonin at presynaptic terminals, increasing synaptic concentrations of these neurotransmitters.
| Metabolism | Hepatic, primarily via CYP2D6 and CYP1A2; active metabolite desmethylmaprotiline. |
| Excretion | Primarily renal (≥60% as metabolites, ~2% unchanged); biliary/fecal excretion accounts for ~30%. |
| Half-life | 51 hours (range 36–68 h) in adults; requires dose adjustment in hepatic impairment. |
| Protein binding | 88–93% bound to alpha1-acid glycoprotein and albumin. |
| Volume of Distribution | 17–22 L/kg; extensive tissue binding with deep peripheral compartment. |
| Bioavailability | Oral: 30–60% due to first-pass metabolism; IM: 100% (relative to oral). |
| Onset of Action | Oral: 2–3 weeks for antidepressant effect; IM: 7–14 days. |
| Duration of Action | After single dose: ~48 h; after chronic dosing: steady state achieved in 2–3 weeks. |
Oral, 75-150 mg daily in divided doses (or as a single dose at bedtime); may increase to 225 mg daily. Maximum: 300 mg daily.
| Dosage form | TABLET |
| Renal impairment | GFR >30 mL/min: no adjustment; GFR 10-30 mL/min: reduce dose by 50%; GFR <10 mL/min: avoid use or use extreme caution with 50% dose reduction and monitor closely. |
| Liver impairment | Child-Pugh A: 50% of normal dose; Child-Pugh B: 25% of normal dose; Child-Pugh C: contraindicated. |
| Pediatric use | Not recommended for children under 16 years. Age 16-18: initial 25 mg daily, increase gradually to 75-150 mg daily based on response. |
| Geriatric use | Elderly (≥65 years): initial dose 25-50 mg daily, titrate slowly to 50-75 mg daily; maximum typically 100 mg daily due to increased sensitivity and risk of side effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LUDIOMIL (LUDIOMIL).
| Breastfeeding | Maprotiline is excreted into breast milk with an M/P ratio of approximately 1.3. Infant exposure is estimated at 2-5% of maternal weight-adjusted dose. Monitor for sedation, poor feeding, and weight gain in infants. Generally considered compatible with breastfeeding if clinically necessary. |
| Teratogenic Risk | First trimester: Limited data; animal studies show no teratogenicity at clinically relevant doses. Second and third trimesters: Risk of neonatal adaptation syndrome, including respiratory depression, feeding difficulties, and irritability, particularly with late exposure. No major malformations reported. |
■ FDA Black Box Warning
Increased risk of suicidal thinking and behavior in children, adolescents, and young adults with major depressive disorder and other psychiatric disorders.
| Serious Effects |
["Hypersensitivity to maprotiline or any component","Concurrent use of MAOIs or within 14 days","Recent myocardial infarction","History of seizures","Angle-closure glaucoma","Urinary retention"]
| Precautions | ["Suicidality risk in pediatric patients","Seizure risk, especially at high doses","Cardiotoxicity (QT prolongation, arrhythmias)","Anticholinergic effects (dry mouth, constipation, urinary retention)","Orthostatic hypotension","Serotonin syndrome when combined with other serotonergic drugs"] |
Loading safety data…
| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and ECG at baseline and periodically due to cardiovascular effects. In neonates, observe for signs of withdrawal or toxicity such as jitteriness, respiratory depression, and feeding difficulties for 48-72 hours after delivery. |
| Fertility Effects | No specific studies in humans; animal data suggest no adverse effects on fertility. In males, potential for ejaculatory dysfunction or impotence. In females, may cause menstrual irregularities. Reversible upon discontinuation. |