General Anesthetic
Propofol is an intravenous general anesthetic and sedative indicated for general anesthesia induction and maintenance, monitored anesthesia care (MAC) sedation, combined sedation and regional anesthesia, and intensive care unit (ICU) sedation of mechanically ventilated patients.
藥理
Propofol is a short-acting, lipophilic intravenous general anesthetic.It causes global CNS depression, presumably through agonism of GABAA receptors and perhaps reduced glutamatergic activity through NMDA receptor blockade.
藥動學
1.Distribution: Large volume of distribution; highly lipophilic ; Vd: approaches 60 L/kg(adults); decreased in the elderly.
2.Protein binding: 97% to 99%
3.Metabolism: Hepatic to water-soluble sulfate and glucuronide conjugates (~50%)
4.Excretion: Urine (~88% as metabolites, 40% as glucuronide metabolite)
禁忌症
1.Hypersensitivity to propofol or any component of the formulation.
2.Hypersensitivity to eggs, egg products, soybeans, or soy products.
懷孕分類
Fetal risk cannot be ruled out.Propofol crosses the placenta and may be associated with neonatal CNS and respiratory depression.
哺乳分類
Infant risk cannot be ruled out.Propofol may present in breast milk.
副作用
Serious:
1.Cardiovascular: Bradyarrhythmia (4.8% ), Heart failure (up to 10% ), Hypertension, Peds (8%)
2.Propofol-related infusion syndrome (PRIS)
3.Respiratory: Apnea, Respiratory acidosi
Other: Bacterial sepsis, Infusion syndrome Common:
1.Dermatologic: Injection site pain (Up to 66.8% )
2.Gastrointestinal: Nausea and vomiting (2% to 2.5% )
3.Musculoskeletal: Involuntary movement, Muscle (17%)
劑量和給藥方法
General anesthesia:
1.Induction(Healthy adults): Usual total dose: 1 to 2.5 mg/kg.
2.Maintenance(Healthy adults): Continuous IV infusion: Usual dosing range: 50 to 200 mcg/kg/minute. Rapid sequence intubation outside the operating room (induction): IV: 1.5 to 2 mg/kg once; usual dose range: 1 to 3 mg/kg. Sedation:
1.Mechanically ventilated patients in the ICU, sedation: Continuous IV infusion: Initial: 5 mcg/kg/minute; increase by 5 to 10 mcg/kg/minute every 5 to 10 minutes until goal sedation level is achieved.
2.Monitored anesthesia care(Healthy adults):Continuous IV infusion: Initial: 25 to 75 mcg/kg/minute; titrate to adequate sedation.
小兒調整劑量
Anesthesia, general:
1.Induction: Children 3 years and Adolescents <17 years: IV: 2.5 to 3.5 mg/kg over 20 to 30 seconds.
2.Maintenance: 125 to 300 mcg/kg/min IV (7.5 to 18 mg/kg/hr) Procedural sedation:1 mg/kg IV followed by 0.5 mg/kg every 3 to 5 minutes as needed for sedation