KETALAR
Clinical safety rating
cautionComprehensive clinical and safety monograph for KETALAR (KETALAR).
Noncompetitive NMDA receptor antagonist; inhibits glutamate activity, modulates opioid receptors, and interacts with other neurotransmitter systems.
| Metabolism | Primarily hepatic via N-demethylation by CYP3A4 and CYP2B6 to norketamine, then further metabolized via hydroxylation and conjugation. |
| Excretion | Renal: 90% as metabolites (norketamine, dehydronorketamine); unchanged: 2-4%. Fecal: <3%. |
| Half-life | Terminal elimination half-life: 2.5-3 hours (ketamine); norketamine: 12 hours. Clinical context: Short half-life facilitates rapid recovery, but context-sensitive half-life increases with infusion duration. |
| Protein binding | 12-50% primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 1-2 L/kg (large, indicating extensive tissue distribution). Highly lipophilic, crosses blood-brain barrier rapidly. |
| Bioavailability | Oral: 16-24% (extensive first-pass metabolism); Intranasal: 45-50%; IM: 93%; Subcutaneous: 100%. |
| Onset of Action | IV: 30-60 seconds; IM: 1-5 minutes; Oral: 15-30 minutes; Intranasal: 5-15 minutes. |
| Duration of Action | IV/IM: 5-15 minutes (anesthetic), 30-60 minutes (analgesic); Oral: 1-2 hours; Intranasal: 15-30 minutes. Context: Subanesthetic doses produce prolonged analgesia. |
| Molecular Weight | 274.39 |
| Action Class | General anaesthetic agents |
| Brand Substitutes | Ketam 10mg Injection, Ketamax 10mg Injection, Aneket 10mg Injection, Ketmin 10mg Injection |
1-4.5 mg/kg IV or 6.5-13 mg/kg IM for induction of anesthesia; 0.1-0.5 mg/kg/min IV infusion for maintenance.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for GFR >10 mL/min; for GFR <10 mL/min, consider dose reduction by 50% due to accumulation of active metabolite norketamine. |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B: reduce dose by 50%; Child-Pugh Class C: avoid use or use with extreme caution, reduce dose by 75%. |
| Pediatric use | Induction: 1-2 mg/kg IV or 4-6 mg/kg IM; maintenance: 0.5-1 mg/kg IV boluses or 10-50 mcg/kg/min IV infusion. Titrate to effect. |
| Geriatric use | Reduce initial dose by 50% (e.g., 0.5-2 mg/kg IV) and titrate slowly due to increased sensitivity and risk of delirium; consider lower infusion rates (0.1-0.3 mg/kg/min). |
| 1st trimester | Use only if clearly needed; risk of teratogenicity not established in humans, but animal studies show adverse effects at high doses. |
| 2nd trimester | May be used for procedures when benefits outweigh risks; consider effects on maternal and fetal hemodynamics. |
| 3rd trimester | Avoid near term; may cause neonatal respiratory depression and neurotoxicity. |
Clinical note
Comprehensive clinical and safety monograph for KETALAR (KETALAR).
| Placental transfer | Ketamine crosses the placenta rapidly, with fetal concentrations approximately 50-80% of maternal levels. |
| Breastfeeding | Ketamine enters breast milk in low amounts. Monitor infant for sedation, respiratory depression, or feeding difficulties. Consider pumping and discarding milk for 24 hours after use. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | First trimester: Limited human data; animal studies show no teratogenicity. Second/third trimester: Use only if clearly needed; may cause neonatal respiratory depression, hypotonia, and altered neurobehavior if used near delivery. |
| Fetal Monitoring | Monitor maternal vital signs (BP, HR, respiratory rate), oxygen saturation, and depth of anesthesia. Fetal heart rate monitoring during prolonged use. Assess neonatal respiratory status and Apgar scores if used near delivery. |
| Fertility Effects | No significant adverse effects on fertility reported in animal studies; human data lacking. |
■ FDA Black Box Warning
Hemodynamic instability (hypertension, tachycardia) and increased intracranial pressure; risk of emergent reactions (hallucinations, delirium); potential for abuse and dependence.
| Serious Effects |
Hypersensitivity to ketamineSevere hypertensionEclampsia or preeclampsiaHistory of stroke or intracranial hemorrhageSevere cardiac decompensation
| Precautions | Monitor blood pressure and cardiac function; use with caution in patients with hypertension, heart failure, or increased intracranial pressure; emergence reactions may occur; laryngospasm risk; respiratory depression. |
| Food/Dietary | No specific food interactions; avoid alcohol for 24 hours due to additive CNS depression. |
| Clinical Pearls | Ketamine (Ketalar) produces dissociative anesthesia with potent analgesia. Onset of action is rapid (30 seconds IV, 5 minutes IM). Emergence reactions (hallucinations, delirium) can be mitigated with benzodiazepines. Contraindicated in patients with hypertension, aneurysms, or increased intracranial pressure due to sympathomimetic effects. Use with caution in patients with psychosis or thyroid disorders. |
| Patient Advice | You may experience vivid dreams or hallucinations as the medication wears off; this is common and can be reduced with other medications. · Do not drive, operate machinery, or make important decisions for at least 24 hours after receiving ketamine. · Avoid alcohol and other sedatives for 24 hours after administration. · Inform your healthcare provider if you have high blood pressure, heart disease, or a history of psychosis. |
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