Difference between revisions of "Ketamine"
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| drug_class_color = sedative_hypnotic | | drug_class_color = sedative_hypnotic | ||
| uses = Induction and maintenance of anesthesia, sedation, analgesia | | uses = Induction and maintenance of anesthesia, sedation, analgesia | ||
| contraindications = | | contraindications = * <3 months old | ||
* <3 months old | |||
* Situations where elevated blood pressure or myocardial oxygen demand would be dangerous | * Situations where elevated blood pressure or myocardial oxygen demand would be dangerous | ||
* Schizophrenia | * Schizophrenia | ||
* Use controversial with elevated ICP or IOP | * Use controversial with elevated ICP or IOP | ||
| routes = IV, IM, IN, PO, PR | | routes = IV, IM, IN, PO, PR | ||
| dosage = Induction of anesthesia: | | dosage = Induction of general anesthesia: 0.5-2 mg/kg IV | ||
| dosage_calculation = ketamine | |||
| mechanism = NMDA-receptor antagonism | |||
| mechanism = NMDA antagonism | |||
| adverse_effects = Laryngospasm | | adverse_effects = Laryngospasm | ||
Hypersalivation | Hypersalivation | ||
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* IM: 12-30 minutes (residual 0.5-2 hours) | * IM: 12-30 minutes (residual 0.5-2 hours) | ||
* PO: 1-6+ hours | * PO: 1-6+ hours | ||
*Context-sensitive half-time: 40-55 minutes after 8 hours of continuous infusion | |||
| metabolism = Liver (CYP3A4, CYP2B6) | | metabolism = Liver (CYP3A4, CYP2B6) | ||
| halflife_elimination = 2.5-3 hours | | halflife_elimination = 2.5-3 hours | ||
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=== Pharmacokinetics<!-- Describe the pharmacokinetics of the drug. --> === | === Pharmacokinetics<!-- Describe the pharmacokinetics of the drug. --> === | ||
Metabolized by hepatic microsomal enzymes to norketamine via ''N''-demethylation. Norketamine is then metabolized to hydroxynorketamine. Ultimately, hydroxynorketamine undergoes glucuronide conjugation and is excreted in the urine. | |||
Norketamine has 33% of the potency of ketamine | |||
The plasma disappearance of ketamine is traditionally described by a two-compartment model. | |||
Elimination half-life: 2.5-2.8 hr | |||
Clearance: 12-17 mL/kg/min | |||
Vd at steady state: 3.1 L/kg | |||
== Chemistry and formulation<!-- Describe the chemistry and formulation of the drug. --> == | == Chemistry and formulation<!-- Describe the chemistry and formulation of the drug. --> == | ||
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== References == | == References == | ||
Kamp J, Olofsen E, Henthorn TK, van Velzen M, Niesters M, Dahan A; Ketamine Pharmacokinetic Study Group. Ketamine Pharmacokinetics. Anesthesiology. 2020 Dec 1;133(6):1192-1213. doi: 10.1097/ALN.0000000000003577. PMID: 32997732. | |||
Miller, Ronald D. Miller's Anesthesia. 7th ed. Philadelphia, PA: Churchill Livingstone/Elsevier, 2010. | |||
[[Category:Drug reference]] | [[Category:Drug reference]] | ||
[[Category:General anesthetics]] | |||
[[Category:Intravenous anesthetics]] | |||
[[Category:Sedative hypnotics]] | |||
[[Category:NMDA antagonists]] |
Latest revision as of 17:50, 14 July 2022
Trade names |
Ketalar |
---|---|
Clinical data | |
Drug class |
Sedative hypnotic |
Uses |
Induction and maintenance of anesthesia, sedation, analgesia |
Contraindications |
|
Routes of administration |
IV, IM, IN, PO, PR |
Dosage |
Induction of general anesthesia: 0.5-2 mg/kg IV |
Dosage | |
Pharmacodynamics | |
Mechanism of action |
NMDA-receptor antagonism |
Adverse effects |
Laryngospasm Hypersalivation Emesis Emergence reaction |
Pharmacokinetics | |
Onset of action |
|
Duration of action |
|
Metabolism |
Liver (CYP3A4, CYP2B6) |
Elimination half-life |
2.5-3 hours |
Protein binding |
23-47% |
Physical and chemical data | |
Formula |
C13H16ClNO |
Molar mass |
237.73 g/mol |
Article quality | |
Editor rating | |
User likes | 0 |
Ketamine is a dissociative anesthetic used for the induction of anesthesia, procedural sedation, and as an analgesic adjunct.
Uses
Contraindications
Absolute contraindications
Precautions
Pharmacology
Pharmacodynamics
Mechanism of action
Adverse effects
Pharmacokinetics
Metabolized by hepatic microsomal enzymes to norketamine via N-demethylation. Norketamine is then metabolized to hydroxynorketamine. Ultimately, hydroxynorketamine undergoes glucuronide conjugation and is excreted in the urine.
Norketamine has 33% of the potency of ketamine
The plasma disappearance of ketamine is traditionally described by a two-compartment model.
Elimination half-life: 2.5-2.8 hr
Clearance: 12-17 mL/kg/min
Vd at steady state: 3.1 L/kg
Chemistry and formulation
History
References
Kamp J, Olofsen E, Henthorn TK, van Velzen M, Niesters M, Dahan A; Ketamine Pharmacokinetic Study Group. Ketamine Pharmacokinetics. Anesthesiology. 2020 Dec 1;133(6):1192-1213. doi: 10.1097/ALN.0000000000003577. PMID: 32997732.
Miller, Ronald D. Miller's Anesthesia. 7th ed. Philadelphia, PA: Churchill Livingstone/Elsevier, 2010.