DIPRIVAN
Clinical safety rating
cautionComprehensive 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. |
| Molecular Weight | 278.21 |
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 | Propofol is associated with neural tube defects in animal studies; human data limited. Use only if clearly needed. |
| 2nd trimester | May cause maternal hypotension and decreased uterine blood flow; use with caution. |
| 3rd trimester | Risk of neonatal respiratory depression and hypotonia; avoid near delivery unless necessary. |
Clinical note
Comprehensive clinical and safety monograph for DIPRIVAN (DIPRIVAN).
| Placental transfer | Rapidly crosses the placenta with fetal/maternal ratio ~0.7-1.3; significant transfer. |
| Breastfeeding | Propofol is excreted into breast milk in low concentrations. After a single dose, amounts are negligible, but repeated or high doses may cause infant sedation. Avoid breastfeeding for 24 hours after propofol administration. |
| Lactation Rating | L3 (Moderately Safe) - single doses acceptable; caution with prolonged use. |
| 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. |
| 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. |
■ 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 componentEgg allergy (soy lecithin content)Soy allergyPropofol infusion syndrome risk (e.g., mitochondrial disease)
| 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 |
| Food/Dietary | No specific food interactions; however, propofol emulsion contains soybean oil and egg lecithin, so avoid in patients with egg or soy allergies. The emulsion can be contaminated if bottle is reused; discard after single use. No dietary restrictions required for administration. |
| Clinical Pearls | DIPRIVAN (propofol) causes pain on injection, especially in small veins; pretreatment with lidocaine or use of a larger vein can mitigate. It is formulated as a lipid emulsion containing soybean oil and egg lecithin, thus contraindicated in patients with egg or soybean allergies. Propofol can cause profound hypotension and respiratory depression; ensure airway equipment and vasopressors are immediately available. The infusion syndrome (PRIS) is rare but lethal, characterized by metabolic acidosis, rhabdomyolysis, and cardiac failure; avoid prolonged high-dose infusions (>5 mg/kg/hr for >48 hours). |
| Patient Advice | You will be monitored continuously during and after administration due to risk of low blood pressure and slowed breathing. · You may feel a burning or stinging sensation at the injection site; inform your healthcare provider if it persists. · Do not drive or operate machinery for at least 24 hours after receiving propofol due to residual sedation. · Inform your medical team if you have allergies to eggs, soy, or sesame seeds. · Propofol is not intended for home use; it is only administered in a supervised medical setting. |
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