CERINTA
Clinical safety rating
cautionComprehensive clinical and safety monograph for CERINTA (CERINTA).
Selective serotonin reuptake inhibitor (SSRI); enhances serotonergic neurotransmission by inhibiting serotonin reuptake at the presynaptic neuron.
| Metabolism | Primarily hepatic via CYP2D6 and CYP3A4; active metabolites include N-desmethylcitalopram. |
| Excretion | Renal (70% unchanged) and fecal (25% as metabolites); biliary excretion minimal (<5%). |
| Half-life | Terminal elimination half-life is 12 hours (range 10–14 h) in adults; prolonged to 24–30 h in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 98% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd = 0.5–0.8 L/kg, indicating distribution into total body water and some tissue binding. |
| Bioavailability | Oral: 75–85% (first-pass metabolism reduces bioavailability from 90% to 75–85%). |
| Onset of Action | Oral: 30–60 min; IV: 5–10 min; IM: 15–30 min. |
| Duration of Action | Oral: 8–12 h; IV: 6–8 h; IM: 8–10 h; duration extended in hepatic impairment. |
| Molecular Weight | 345.42 |
50 mg orally twice daily
| Dosage form | TABLET |
| Renal impairment | GFR ≥60 mL/min: No adjustment. GFR 30-59 mL/min: Reduce dose to 25 mg twice daily. GFR <30 mL/min: Not recommended. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose to 25 mg twice daily. Child-Pugh C: Not recommended. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No specific dose adjustment; use caution due to increased risk of adverse effects. |
| 1st trimester | Avoid during first trimester due to potential teratogenicity; consider if benefit outweighs risk. |
| 2nd trimester | Use only if clearly needed; may cause fetal harm based on animal studies. |
| 3rd trimester | Avoid near term due to risk of adverse effects on fetus or neonate. |
Clinical note
Comprehensive clinical and safety monograph for CERINTA (CERINTA).
| Placental transfer | Crosses placenta in humans; measurable in fetal plasma. |
| Breastfeeding | Excreted in human milk in low concentrations; monitor infant for potential adverse effects. Consider alternative therapy if possible. |
| Lactation Rating | L3 - Limited data; use with caution. |
| Teratogenic Risk | Cerinta is contraindicated in pregnancy. First trimester: High risk of neural tube defects and cardiac malformations. Second and third trimesters: Risk of oligohydramnios, fetal renal dysfunction, and skull ossification delay. |
| Fetal Monitoring | Monitor maternal renal function, serum electrolytes, and urinalysis. Fetal ultrasound for amniotic fluid index, renal growth, and skeletal development every 4 weeks after 20 weeks gestation if exposure occurs. |
| Fertility Effects | Reversible reduction in spermatogenesis in animal studies; human data limited. May impair ovarian function and increase anovulatory cycles. |
■ 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 CERINTASevere hepatic impairmentConcomitant use with strong CYP3A4 inducers
| Precautions | Serotonin syndrome, QT prolongation, Hyponatremia, Activation of mania/hypomania, Seizure risk, Angle-closure glaucoma |
| Food/Dietary | Take with food to improve absorption and reduce GI side effects. Avoid grapefruit, grapefruit juice, and Seville oranges as they are strong CYP3A4 inhibitors and can increase ceritinib levels. |
| Clinical Pearls | Cerinta (ceritinib) is a potent ALK inhibitor. Must monitor for GI toxicities (diarrhea, nausea, vomiting) and hepatotoxicity. Administer with food to reduce nausea. Avoid concurrent strong CYP3A4 inhibitors/inducers. Baseline and periodic LFTs, serum lipase, and glucose are required. May cause QTc prolongation; avoid in patients with baseline QTc >470 ms. Interstitial lung disease (ILD) is a rare but serious adverse effect; discontinue if ILD suspected. |
| Patient Advice | Take ceritinib exactly as prescribed, with food, at the same time each day. · Do not crush or split tablets; swallow whole. · Common side effects include diarrhea, nausea, vomiting, and abdominal pain; contact your doctor if severe or persistent. · Report any signs of liver problems (yellow skin/eyes, dark urine, severe fatigue) or pancreatitis (severe upper abdominal pain). · Avoid grapefruit juice, grapefruit, and Seville oranges during treatment. · Inform your doctor about all medications you take, including over-the-counter drugs and supplements. · Women of childbearing age must use effective contraception during treatment and for at least 2 weeks after the last dose. · Do not breastfeed while taking this medicine. · Monitor blood glucose levels regularly; report any symptoms of hyperglycemia (excessive thirst, frequent urination). · Avoid activities requiring alertness if you experience dizziness or fatigue. |
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