SUFENTA PRESERVATIVE FREE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SUFENTA PRESERVATIVE FREE (SUFENTA PRESERVATIVE FREE).
Sufentanil is a synthetic opioid analgesic that acts as a selective agonist at mu-opioid receptors in the central nervous system, leading to activation of descending pain pathways and inhibition of nociceptive transmission.
| Metabolism | Primarily metabolized by CYP3A4 and CYP2C9 enzymes in the liver to N-desmethylsufentanil and other minor metabolites. Undergoes phase II conjugation before renal excretion. |
| Excretion | Renal (metabolites, <1% unchanged) and biliary; sufentanil is extensively metabolized in liver via N-dealkylation and O-demethylation, with metabolites primarily excreted in urine (approximately 80%) and feces (approximately 20%). |
| Half-life | Terminal elimination half-life is approximately 2.5-3.5 hours in adults, 3-4 hours in neonates; clinical context: context-sensitive half-life increases with infusion duration (e.g., ~30 minutes after 2-hour infusion, ~45 min after 8-hour infusion). |
| Protein binding | Approximately 92-93% bound to plasma proteins, primarily α1-acid glycoprotein and albumin. |
| Volume of Distribution | Vdss (steady-state volume of distribution) is approximately 1.5-2.5 L/kg in adults; higher in neonates (2-3 L/kg); indicates extensive tissue distribution. |
| Bioavailability | Intravenous: 100%; epidural: ~90-95% (due to vascular absorption); intrathecal: ~100% (but with minimal systemic absorption due to high lipid solubility); nasal: ~70-80%; transmucosal: ~50-60% (buccal). |
| Onset of Action | Intravenous: 1-3 minutes; epidural: 5-10 minutes; intrathecal: 5-15 minutes. |
| Duration of Action | Intravenous: 20-45 minutes (analgesic), 30-60 minutes (anesthetic); epidural: 2-4 hours (with lipid solubility providing rapid redistribution, but shorter duration than morphine); intrathecal: 2-4 hours. |
1-2 mcg/kg IV initially, then 0.15-0.3 mcg/kg/min IV infusion; doses up to 8 mcg/kg for anesthesia induction.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment required; active metabolite normeperidine accumulates in renal failure, use with caution and monitor for CNS toxicity. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 25-50%; Child-Pugh C: avoid use or reduce to 25% of usual dose; monitor for prolonged effects. |
| Pediatric use | Neonates and infants: 0.3-0.5 mcg/kg IV bolus; children: 0.2-0.5 mcg/kg IV bolus, then 0.1-0.3 mcg/kg/min IV infusion; dose based on ideal body weight. |
| Geriatric use | Reduce initial dose by 50% and titrate slowly; increased sensitivity to respiratory depression and hypotension; monitor renal function as clearance may be reduced. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SUFENTA PRESERVATIVE FREE (SUFENTA PRESERVATIVE FREE).
| Breastfeeding | Sufentanil is excreted in human milk. The milk-to-plasma ratio is approximately 2:1. Breastfeeding infants may be exposed to low levels, but the clinical significance is unknown. The American Academy of Pediatrics considers opioids compatible with breastfeeding, but caution is advised due to potential for CNS depression in the infant. Monitor for drowsiness and feeding difficulties. |
| Teratogenic Risk | Sufentanil is Pregnancy Category C. There is no evidence of teratogenicity in animal studies at doses up to 2.5 times the human dose. However, sufentanil crosses the placenta and can cause neonatal respiratory depression and withdrawal if used chronically or at high doses near term. Use during labor and delivery may cause respiratory depression in the neonate. There are no adequate and well-controlled studies in pregnant women; use only if potential benefit justifies the potential risk to the fetus. |
■ FDA Black Box Warning
Risk of respiratory depression, especially in non-opioid-tolerant patients and when used for acute pain management. Accidental ingestion or exposure can cause fatal respiratory depression in children. Concomitant use with benzodiazepines or other CNS depressants may result in profound sedation, respiratory depression, coma, and death.
| Serious Effects |
["Hypersensitivity to sufentanil or any component of the formulation","Significant respiratory depression (in unmonitored settings or absence of resuscitative equipment)","Acute or severe bronchial asthma","Known or suspected paralytic ileus","Concurrent use of monoamine oxidase inhibitors (MAOIs) or within 14 days of discontinuation"]
| Precautions | ["Respiratory depression: Monitor oxygenation and ventilation closely; have resuscitation equipment available.","CNS depression: Additive effects with alcohol, sedatives, and other CNS depressants.","Neonatal opioid withdrawal syndrome: Prolonged use during pregnancy may cause withdrawal in neonates.","Serotonin syndrome: Risk when used with serotonergic drugs.","Hypotension and bradycardia: May occur, especially during induction of anesthesia.","Biliary spasm: May cause spasm of the sphincter of Oddi.","Tolerance and dependence: Prolonged use can lead to physical and psychological dependence."] |
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| Fetal Monitoring | Monitor maternal respiratory rate, oxygen saturation, blood pressure, heart rate, and level of consciousness. Fetal heart rate should be monitored during labor. Assess for signs of neonatal respiratory depression if used close to delivery. Beta-hCG levels and ultrasonography may be used to assess fetal status in chronic use. |
| Fertility Effects | No specific studies on human fertility effects. Animal studies have not shown impaired fertility at clinically relevant doses. However, opioids may alter hormone levels (e.g., prolactin, GnRH) and could potentially affect fertility. Clinical significance is unknown. |