Indications
Sedation of initially intubated and mechanically ventilated
patients during treatment in an intensive care setting;
should not be used for 24 hr. Sedation of non-intubated
patients before and/or during surgical and
other procedures.
Action
Acts as a relatively selective alpha-adrenergic agonist
with sedative properties. Therapeutic Effects: Sedation.
Pharmacokinetics
Absorption: IV administration results in complete
bioavailability.
Distribution: Unknown.
Protein Binding: 94%.
Metabolism and Excretion: Mostly metabolized
by the liver, some metabolism by P450 enzyme system.
Metabolites are mostly excreted in urine.
Half-life: 2 hr.
TIME/ACTION PROFILE (sedation)
ROUTE ONSET PEAK DURATION
IV rapid unknown unknown
Contraindications/Precautions
Contraindicated in: Hypersensitivity.
Use Cautiously in: Hepatic impairment (lower
doses may be required); Advanced heart block; Severe
left ventricular dysfunction; Geri:qrisk of bradycardia and hypotension (consider dosep); OB, Lactation,
Pedi: Safety not established.
Adverse Reactions/Side Effects
Resp: hypoxia. CV: BRADYCARDIA, SINUS ARREST, hypotension,
transient hypertension. GI: dry mouth, nausea,
vomiting. Hemat: anemia. Misc: fever.
Interactions
Drug-Drug: Sedation is enhanced by anesthetics,
other sedative/hypnotics, and opioid analgesics.
Drug-Natural Products: Concomitant use of
kava-kava, valerian, skullcap, chamomile, or
hops canqCNS depression.
Route/Dosage
ICU Sedation
IV (Adults): Loading infusion—1 mcg/kg over 10
min followed by maintenance infusion of 0.2–0.7
mcg/kg/hr for maximum of 24 hr; rate is adjusted to
achieve desired level of sedation.
IV (Children): Loading infusion—0.5–1 mcg/kg
followed by maintenance infusion of 0.2–1 mcg/kg/
hr. Children 1 yr may require higher end of infusion
rate.
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).
Availability (generic available)
Solution for injection (requires further dilution):
100 mcg/mL. Premixed infusion (in 0.9%
NaCl): 4 mcg/mL.
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