PROSOL 20% SULFITE FREE IN PLASTIC CONTAINER
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PROSOL 20% SULFITE FREE IN PLASTIC CONTAINER (PROSOL 20% SULFITE FREE IN PLASTIC CONTAINER).
Propofol is a short-acting intravenous anesthetic agent that potentiates GABA-A receptor activity, resulting in rapid loss of consciousness through inhibition of neuronal firing in the central nervous system.
| Metabolism | Primarily hepatic via conjugation to glucuronide and sulfate; also undergoes extrahepatic metabolism in lungs and kidneys; CYP450 isoenzymes not involved; clearance is high and influenced by hepatic blood flow. |
| Excretion | Renal excretion of unchanged drug is minimal (<5%). The majority is metabolized via the tricarboxylic acid cycle to CO2 and water. Biliary/fecal elimination is negligible. |
| Half-life | Terminal elimination half-life is approximately 1–2 hours in healthy individuals; may be prolonged in renal impairment due to accumulation of metabolites. |
| Protein binding | Negligible (<1%); does not bind significantly to plasma proteins. |
| Volume of Distribution | 0.2–0.3 L/kg; distributes primarily in extracellular fluid, including cerebrospinal fluid. |
| Bioavailability | Not applicable (administered intravenously); oral bioavailability is negligible due to poor absorption. |
| Onset of Action | Intravenous infusion: clinical effect (e.g., reduction of intracranial pressure) occurs within 15–30 minutes. |
| Duration of Action | Duration of osmotic effect is 4–6 hours after intravenous administration; rebound intracranial hypertension may occur after discontinuation. |
Intravenous infusion: 20 mL/kg (4 g/kg) as a 20% solution administered over 2-4 hours. May repeat up to 100 mL/kg/day if needed.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for GFR >50 mL/min. For GFR 10-50 mL/min: administer with caution, monitor for volume overload. GFR <10 mL/min: avoid use unless on dialysis. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: contraindicated due to risk of encephalopathy. |
| Pediatric use | Infants and children: 10-20 mL/kg (2-4 g/kg) as 20% solution IV over 2-4 hours, not to exceed 100 mL/kg/day. |
| Geriatric use | Elderly patients: start at lower end of dosing range; monitor for fluid overload and renal function; typical dose 10-15 mL/kg IV over 2-4 hours. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PROSOL 20% SULFITE FREE IN PLASTIC CONTAINER (PROSOL 20% SULFITE FREE IN PLASTIC CONTAINER).
| Breastfeeding | Propofol is excreted in human milk in small amounts. The milk-to-plasma ratio (M/P) is approximately 0.5. After a single bolus dose, the amount ingested by the infant is minimal and considered compatible with breastfeeding. However, caution is advised if repeated doses or continuous infusion are used, and the infant should be observed for sedation. |
| Teratogenic Risk | No adequate and well-controlled studies in pregnant women. Animal reproduction studies have not been conducted with propofol. Propofol crosses the placenta and may cause fetal depression. Use in first trimester: not recommended unless clearly necessary. Use in second and third trimesters: may cause maternal hypotension and fetal bradycardia; risk of neonatal respiratory depression and hypotonia if used near delivery. |
■ FDA Black Box Warning
For use only by trained personnel in settings equipped for monitoring and resuscitation; risk of apnea, hypotension, and hypoxia; should not be administered by the same person performing the diagnostic or surgical procedure.
| Serious Effects |
Hypersensitivity to propofol or its components (soybean oil, egg lecithin, glycerol); patients with severe lipid metabolism disorders; when general anesthesia or sedation is contraindicated.
| Precautions | Monitor for hypotension, bradycardia, and respiratory depression; caution in elderly, debilitated, or hypovolemic patients; risk of propofol infusion syndrome (PRIS) with prolonged high-dose use; lipid emulsion may cause hypertriglyceridemia; not recommended for obstetric anesthesia (crosses placenta). |
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| Fetal Monitoring | Monitor maternal blood pressure, heart rate, oxygen saturation, and level of consciousness. Fetal heart rate monitoring is recommended if propofol is used during pregnancy, especially in the second and third trimesters. Continuous maternal ECG and respiratory monitoring are required during administration. |
| Fertility Effects | No human data on fertility effects. Animal studies with propofol have not shown impaired fertility. Transient effects on sperm motility in males have been reported in vitro, but clinical significance is unknown. |