DIPRIVAN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DIPRIVAN (DIPRIVAN).
Propofol potentiates GABA-A receptor activity, leading to rapid sedation and hypnosis by enhancing chloride conductance and neuronal hyperpolarization.
| Metabolism | Primarily hepatic conjugation to inactive metabolites (propofol glucuronide), with minor metabolism via CYP2B6 and CYP2C9 to 4-hydroxypropofol. |
| Excretion | Renal (approximately 88% as metabolites, <1% unchanged); fecal (approximately 2%); other (10% as metabolites via other routes). |
| Half-life | Terminal elimination half-life: 4-7 hours (with context of context-sensitive half-life increasing after prolonged infusion). |
| Protein binding | 95-99% bound, primarily to albumin. |
| Volume of Distribution | 2-10 L/kg (large Vd indicating extensive tissue distribution). |
| Bioavailability | Intravenous: 100%; not available orally due to extensive first-pass metabolism. |
| Onset of Action | Intravenous: 30-60 seconds (loss of consciousness). |
| Duration of Action | Intravenous bolus: 5-10 minutes (anesthetic effect); after prolonged infusion: recovery in 10-20 minutes due to redistribution. |
Induction: 2-2.5 mg/kg IV bolus; maintenance: 25-75 mcg/kg/min IV infusion.
| Dosage form | INJECTABLE |
| Renal impairment | No adjustment required; propofol is not significantly renally eliminated. |
| Liver impairment | No specific Child-Pugh based guidelines; use lower doses due to impaired clearance, especially in cirrhosis. |
| Pediatric use | Induction: 2.5-3.5 mg/kg IV bolus; maintenance: 125-300 mcg/kg/min IV infusion. Not approved for ICU sedation in <16 years. |
| Geriatric use | Reduce induction dose to 1-1.5 mg/kg IV bolus and maintenance infusion to 20-50 mcg/kg/min IV due to increased sensitivity and decreased clearance. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DIPRIVAN (DIPRIVAN).
| Breastfeeding | Propofol is excreted into breast milk in low concentrations. M/P ratio not established. Due to low oral bioavailability, risk to infant is minimal. However, caution is advised due to potential CNS depression in neonates. The manufacturer recommends discontinuing breastfeeding for 24 hours after administration. |
| Teratogenic Risk | Propofol (DIPRIVAN) is Pregnancy Category B. Animal studies at clinical doses did not show teratogenicity. Use in first trimester only if clearly needed. During second and third trimesters, propofol crosses the placenta and may cause neonatal respiratory depression and neurobehavioral depression. Risk of fetal acidosis and bradycardia. No major teratogenic effects reported in human studies, but limited data. |
■ FDA Black Box Warning
Propofol should be administered only by persons trained in the administration of general anesthesia and not involved in the conduct of the surgical/diagnostic procedure. Patients should be continuously monitored for early signs of hypotension, bradycardia, apnea, airway obstruction, and oxygen desaturation. For sedation of intubated, mechanically ventilated patients in the ICU, propofol should be used with caution in patients with increased intracranial pressure or impaired cerebral circulation.
| Serious Effects |
["Hypersensitivity to propofol or any component of the formulation","Hypersensitivity to eggs, egg products, soybeans, or soy products (due to lipid vehicle)","Patients with severe lipid metabolism disorders (e.g., hyperlipidemia)","Not recommended for general anesthesia in patients with increased intracranial pressure or impaired cerebral circulation unless benefits outweigh risks"]
| Precautions | ["Risk of hypotension and bradycardia, especially in elderly or hypovolemic patients","Respiratory depression and apnea requiring airway management","Propofol infusion syndrome (PRIS): metabolic acidosis, rhabdomyolysis, renal failure, cardiac failure, especially with prolonged high-dose infusions","Hypertriglyceridemia; monitor lipids with prolonged use","Risk of pancreatitis","Use with caution in patients with epilepsy; may increase seizure risk during withdrawal","May cause green discoloration of urine, hair, or nails"] |
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| Fetal Monitoring | Monitor maternal cardiovascular status, respiratory rate, oxygen saturation, and level of consciousness. Fetal heart rate monitoring is recommended during prolonged use. Neonatal monitoring for respiratory depression and neurobehavioral status post-delivery. |
| Fertility Effects | Propofol has no known direct effects on fertility in humans. Animal studies showed no impairment of fertility at clinically relevant doses. |