SERPALAN
Clinical safety rating
cautionComprehensive 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. |
| Molecular Weight | 425.38 |
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 | Severe teratogenicity; contraindicated. Risk of severe fetal malformations (e.g., neural tube defects, facial clefts). |
| 2nd trimester | Risk of fetal toxicity and growth retardation; avoid use unless benefit clearly outweighs risk. |
| 3rd trimester | Risk of neonatal complications (e.g., hypotension, renal failure); avoid use near term. |
Clinical note
Comprehensive clinical and safety monograph for SERPALAN (SERPALAN).
| Placental transfer | Extensive placental transfer; fetal plasma concentrations reach 50-100% of maternal levels, with rapid equilibration. |
| Breastfeeding | Excreted into breast milk in high concentrations; may cause severe adverse effects in the infant (e.g., sedation, respiratory depression). Discontinue nursing or the drug. |
| Lactation Rating | L5 (Contraindicated) |
| 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. |
| 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. |
■ FDA Black Box Warning
Suicidal thoughts and behaviors: Increased risk in children, adolescents, and young adults during initial treatment.
| Serious Effects |
PregnancyBreastfeedingSevere hepatic impairmentHypersensitivity to SERPALAN or any excipient
| 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. |
| Food/Dietary | Avoid concurrent use of alcohol; may worsen central nervous system effects. No specific food restrictions; take with or without food. Grapefruit juice has no significant interaction. |
| Clinical Pearls | SERPALAN is a selective serotonin reuptake inhibitor (SSRI) used for major depressive disorder. Monitor for serotonin syndrome, especially when co-prescribed with other serotonergic drugs. Initiate at 20 mg daily; titrate to 40 mg after 4 weeks if needed. Do not abruptly discontinue; taper gradually to avoid withdrawal symptoms. Use with caution in patients with hepatic impairment (dose reduction recommended). Avoid MAOIs within 14 days. |
| Patient Advice | Take this medication at the same time each day, with or without food. · Do not stop taking this medication suddenly; consult your doctor for a tapering schedule. · It may take 2–4 weeks to feel the full benefit; continue taking even if you do not notice immediate improvement. · Notify your doctor if you experience new or worsening anxiety, agitation, or suicidal thoughts. · Avoid alcohol while taking this medication. · Do not take other medications, including over-the-counter drugs, without consulting your doctor. |
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