SERPALAN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SERPALAN (SERPALAN).
Selective serotonin reuptake inhibitor (SSRI) that potentiates serotonergic activity in the CNS by blocking the reuptake of serotonin at the presynaptic terminal.
| Metabolism | Hepatic via CYP2D6 and CYP3A4; active metabolite N-desmethylserpalan. |
| Excretion | Primarily renal elimination (60-70% unchanged drug), with 20-30% biliary/fecal excretion as metabolites; less than 10% excreted unchanged in feces. |
| Half-life | Terminal elimination half-life is 12-14 hours in adults with normal renal function; prolonged to 24-36 hours in moderate renal impairment (CrCl 30-50 mL/min) and up to 60 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | Approximately 85-90% bound to serum albumin, with minor binding to alpha-1-acid glycoprotein. |
| Volume of Distribution | 1.2-1.8 L/kg, indicating extensive tissue distribution (e.g., liver, kidneys, and lungs); higher Vd in obese patients. |
| Bioavailability | Oral: 75-85% due to first-pass metabolism; IM: 90-98%; rectal: 50-70%. |
| Onset of Action | Oral: 30-60 minutes; intravenous: 2-5 minutes; intramuscular: 10-15 minutes. |
| Duration of Action | Oral: 8-12 hours; intravenous: 4-6 hours; intramuscular: 6-8 hours. Duration is dose-dependent and may be extended in hepatic impairment. |
100 mg orally twice daily
| Dosage form | TABLET |
| Renal impairment | GFR ≥ 60 mL/min: no adjustment; GFR 30-59 mL/min: 50 mg once daily; GFR < 30 mL/min: avoid use |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 50 mg once daily; Child-Pugh C: contraindicated |
| Pediatric use | Not established for patients < 18 years |
| Geriatric use | Maximum 50 mg once daily due to increased sensitivity and renal impairment risk |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SERPALAN (SERPALAN).
| Breastfeeding | Excreted into breast milk (M/P ratio 0.9). Not recommended during breastfeeding due to potential adverse effects on infant including sedation, poor feeding, and withdrawal. Consider alternative therapy. |
| Teratogenic Risk | First trimester: increased risk of structural anomalies including cardiac defects (FDA category C; animal studies show teratogenicity at clinically relevant doses). Second and third trimesters: risk of fetal growth restriction, oligohydramnios, and preterm birth. Late third trimester: neonatal withdrawal syndrome and respiratory depression. |
■ FDA Black Box Warning
Suicidal thoughts and behaviors: Increased risk in children, adolescents, and young adults during initial treatment.
| Serious Effects |
Hypersensitivity to serpalan; concurrent use of MAOIs or linezolid; concurrent use of pimozide; use of MAOIs within 14 days.
| Precautions | Serotonin syndrome with concomitant serotonergic drugs; risk of bleeding with NSAIDs/anticoagulants; activation of mania/hypomania; bone fracture risk in elderly; hyponatremia; QT prolongation at high doses. |
Loading safety data…
| Fetal Monitoring |
| Serial fetal growth ultrasounds every 4 weeks from 20 weeks; nonstress test or biophysical profile weekly from 32 weeks; maternal blood pressure and urine protein monitoring for preeclampsia; assess for signs of fetal distress during labor. |
| Fertility Effects | May reduce fertility in both sexes. In females: possible menstrual irregularities and anovulation. In males: reversible decreased sperm count and motility. Effects are dose-dependent and may persist for several months after discontinuation. |