PRESAMINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PRESAMINE (PRESAMINE).
Predominantly inhibits serotonin reuptake in the presynaptic neuron, increasing serotonin availability in the synaptic cleft. Also inhibits norepinephrine reuptake to a lesser extent.
| Metabolism | Hepatic via CYP2D6, CYP2C19, CYP3A4; active metabolite N-desmethylcitalopram |
| Excretion | Primarily renal (70% as metabolites, <5% unchanged); biliary/fecal (30%). |
| Half-life | 21 hours (range 16-28 h) for imipramine; active metabolite desipramine ~24 h; clinically, steady-state reached in 5-7 days. |
| Protein binding | 90% bound primarily to alpha1-acid glycoprotein and albumin. |
| Volume of Distribution | 15 L/kg (range 10-20 L/kg), indicating extensive tissue distribution, particularly to brain and heart. |
| Bioavailability | Oral: 30-50% due to first-pass metabolism; IM: ~100%. |
| Onset of Action | Oral: 2-4 weeks for antidepressant effect; IM: 30-60 min for sedation (not for depression). |
| Duration of Action | Oral: prolonged antidepressant effect sustained with regular dosing; half-life supports once-daily dosing; clinical duration weeks. |
100-300 mg/day orally in divided doses, typically starting at 75 mg/day and titrating upward. Maximum dose 300 mg/day.
| 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 or use with extreme caution, monitor closely. |
| Liver impairment | Child-Pugh Class A: no adjustment. Child-Pugh Class B: reduce dose by 50%. Child-Pugh Class C: contraindicated. |
| Pediatric use | Not recommended for children under 12 years. For adolescents: 1-2 mg/kg/day orally, up to 100 mg/day in divided doses. |
| Geriatric use | Start at 25-50 mg/day, increase by 25 mg every 3-4 days. Maximum 150 mg/day. Monitor for orthostasis, sedation, anticholinergic effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PRESAMINE (PRESAMINE).
| Breastfeeding | Presamine is excreted into breast milk in low concentrations. M/P ratio is approximately 0.4-0.6. American Academy of Pediatrics considers it compatible with breastfeeding; however, monitor infant for drowsiness and feeding problems. |
| Teratogenic Risk | First trimester: Studies suggest a small increased risk of cardiovascular malformations, particularly septal defects. Second trimester: No specific major risks identified but fetal growth monitoring recommended. Third trimester: Risk of neonatal adaptation syndrome including respiratory distress, feeding difficulties, and irritability. |
■ 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 |
Concurrent use with MAOIs or within 14 days of MAOI therapy, known hypersensitivity to citalopram or escitalopram, and use in patients with congenital long QT syndrome or concurrent QT-prolonging drugs.
| Precautions | QT interval prolongation, serotonin syndrome, activation of mania/hypomania, seizure risk, angle-closure glaucoma, hyponatremia, and increased bleeding risk. |
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| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and ECG for arrhythmias. Assess for serotonin syndrome if combined with other serotonergic drugs. Fetal ultrasound for growth and anatomy in second trimester, and neonatal monitoring for adaptation syndrome after delivery. |
| Fertility Effects | Imipramine may cause reversible infertility in males via decreased libido, erectile dysfunction, or ejaculatory disturbances. In females, it may disrupt menstrual cycle or reduce libido. Effects are dose-dependent and reversible upon discontinuation. |