PRECEDEX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PRECEDEX (PRECEDEX).
Selective alpha-2 adrenergic receptor agonist, decreasing norepinephrine release and reducing central sympathetic outflow, resulting in sedation, anxiolysis, and analgesia.
| Metabolism | Primarily metabolized via glucuronidation and N-glucuronidation by UDP-glucuronosyltransferases (UGT1A4, UGT2B10), with minor oxidative metabolism via CYP2A6. |
| Excretion | Primarily renal (95%) as unchanged drug and glucuronide conjugates, with ~85% excreted unchanged in urine. Fecal excretion accounts for <5%. |
| Half-life | Terminal elimination half-life is approximately 2 hours (1.5-3 hours) in healthy adults, prolonged in hepatic impairment (up to 7.4 hours in severe disease) and elderly patients. |
| Protein binding | 94% bound primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Steady-state volume of distribution (Vd) is approximately 2-3 L/kg, indicating extensive tissue distribution. |
| Bioavailability | IM: Bioavailability ~80%. Oral: Not available clinically due to extensive first-pass metabolism. IV: 100%. |
| Onset of Action | IV: Sedation onset within 5-10 minutes following initial loading dose. IM: Onset approximately 15-30 minutes. |
| Duration of Action | IV: Duration 1-2 hours after single dose; prolonged with continuous infusion. Clinical sedation resolves within 2-4 hours after infusion cessation. |
Loading infusion of 1 mcg/kg IV over 10 minutes, followed by maintenance infusion of 0.2 to 0.7 mcg/kg/hour IV, titrated to effect. For procedures, initial loading of 1 mcg/kg IV over 10 minutes then maintenance 0.5 mcg/kg/hour IV.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for renal impairment, including end-stage renal disease. Drug is not significantly eliminated renally. |
| Liver impairment | Reduce maintenance infusion rate in patients with hepatic impairment: Child-Pugh Class A or B: consider starting at 0.4 mcg/kg/hour; Child-Pugh Class C: consider starting at 0.2 mcg/kg/hour. Titrate to effect. |
| Pediatric use | For pediatric patients (including neonates): loading dose of 1 mcg/kg IV over 10 minutes, then continuous infusion of 0.5 to 1 mcg/kg/hour, titrated to desired sedation level. Maximum infusion rate 2 mcg/kg/hour. Use weight-based dosing. |
| Geriatric use | Elderly patients (≥65 years): consider reducing loading and maintenance doses by 20-30% due to increased sensitivity and reduced clearance. Typical starting maintenance infusion 0.2 mcg/kg/hour; titrate cautiously. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PRECEDEX (PRECEDEX).
| Breastfeeding | No data on human milk excretion. M/P ratio unknown. Dexmedetomidine is highly protein-bound (94%) limiting transfer. Consider risks vs benefits; use only if clearly needed. |
| Teratogenic Risk | Dexmedetomidine is Pregnancy Category C. Animal studies show increased embryo-fetal mortality and delayed ossification at doses ≥0.2 mg/kg/day (subcutaneous). There are no adequate human studies. Risk of fetal bradycardia and hypotension if used near term. Second and third trimester use may cause maternal hemodynamic instability affecting placental perfusion. |
■ FDA Black Box Warning
No FDA black box warnings.
| Serious Effects |
["Hypersensitivity to dexmedetomidine or any component of the formulation"]
| Precautions | ["Hypotension and bradycardia","Transient hypertension with loading dose","Withdrawal symptoms with prolonged infusion","Rebound hypertension","QT prolongation in susceptible patients","Use with caution in elderly, renal impairment, and hepatic impairment"] |
Loading safety data…
| Fetal Monitoring |
| Continuous maternal ECG, heart rate, blood pressure, oxygen saturation. Fetal heart rate monitoring if gestation >24 weeks. Assess for maternal hypotension, bradycardia, or oversedation. |
| Fertility Effects | No human data. Animal studies: no impairment of male or female fertility at subcutaneous doses up to 0.2 mg/kg/day. |