Therapeutic Classification: sedative/hypnotics
Pharmacologic Classification: alpha adrenergic agonists
Absorption: IV administration results in complete bioavailability. 72% absorbed following SL administration; 82% absorbed following buccal administration.
Distribution: Widely distributed to extravascular tissues.
Protein Binding: 94%.
Metabolism/Excretion: Mostly metabolized by the liver, some metabolism by P450 enzyme system. Metabolites are mostly excreted in urine.
Half-Life: IV: 2 hr; SL/buccal: 2.8 hr.
ICU Sedation
- IV (Adults ): Loading infusion: 1 mcg/kg over 10 min followed by Maintenance infusion: 0.2–0.7 mcg/kg/hr for maximum of 24 hr; rate is adjusted to achieve desired level of sedation.
Procedural Sedation
- IV (Adults ): Loading infusion: 1 mcg/kg (0.5 mcg/kg for ophthalmic surgery or patients >65 yr) over 10 min followed by maintenance infusion of 0.6 mcg/kg/hr; rate is adjusted to achieve desired level of sedation (usual range 0.2–1 mcg/kg/hr) (maintenance infusion of 0.7 mcg/kg/hr recommended for fiberoptic intubation until endotracheal tube secured).
- IV (Children ≥2 yr): Loading infusion: 2 mcg/kg over 10 min followed by maintenance infusion of 1.5 mcg/kg/hr; rate is adjusted to achieve desired level of sedation (usual range 0.5–1.5 mcg/kg/hr).
- IV (Children 1 mo–<2 yr): Loading infusion: 1.5 mcg/kg over 10 min followed by maintenance infusion of 1.5 mcg/kg/hr; rate is adjusted to achieve desired level of sedation (usual range 0.5–1.5 mcg/kg/hr).
Acute Treatment of Agitation Associated with Schizophrenia or Bipolar I or II Disorder.
(Adults <65 yr): Mild or moderate agitation: 120 mcg initially; if agitation continues, up to two additional doses of 60 mcg may be administered ≥2 hours apart (max total dose = 240 mcg/day). Severe agitation: 180 mcg initially; if agitation continues, up to two additional doses of 90 mcg may be administered ≥2 hours apart (max total dose = 360 mcg/day).
Geriatric Patients ≥65 yr): Mild, moderate, or severe agitation: 120 mcg initially; if agitation continues, up to two additional doses of 60 mcg may be administered ≥2 hours apart (max total dose = 240 mcg/day).
Hepatic Impairment
(Adults ): Mild or moderate hepatic impairment: Mild or moderate agitation: 90 mcg initially; if agitation continues, up to two additional doses of 60 mcg may be administered ≥2 hours apart (max total dose = 210 mcg/day). Severe agitation: 120 mcg initially; if agitation continues, up to two additional doses of 60 mcg may be administered ≥2 hours apart (max total dose = 240 mcg/day). Severe hepatic impairment: Mild or moderate agitation: 60 mcg initially; if agitation continues, up to two additional doses of 60 mcg may be administered ≥2 hours apart (max total dose = 180 mcg/day). Severe agitation: 120 mcg initially; if agitation continues, up to two additional doses of 60 mcg may be administered ≥2 hours apart (max total dose = 240 mcg/day).
