dexmedetomidine

Contraindicated in:

Hypersensitivity;
Hypotension
Advanced heart block;
Severe left ventricular dysfunction;
History of syncope;
QT interval prolongation, arrhythmias, symptomatic bradycardia, hypokalemia, hypomagnesemia, or concurrent use of QT interval prolonging medications.

Use Cautiously in:

Hepatic impairment (lower doses may be required);
Hypovolemia, diabetes, and/or chronic hypertension (↑ risk of hypotension and bradycardia);
OB: Safety not established in pregnancy;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Children <1 mo (safety and effectiveness not established);
Geri: ↑risk of bradycardia and hypotension in older adults (consider dose ↓).

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension, BRADYCARDIA, QT interval prolongation, SINUS ARREST, transient hypertension

GI: dry mouth, nausea, oral numbness, vomiting

Hemat: anemia

Neuro: somnolence, dizziness

Resp: hypoxia

Misc: fever, hyperthermia

Interactions ⬆ ⬇

Drug-drug:

Sedation is enhanced by anesthetics, other sedative/hypnotics, and opioid analgesics.
QT interval prolonging medications may ↑ the risk of QT interval prolongation and torsades de pointes; avoid concurrent use.

Drug-Natural Products:

Concomitant use of kava-kava, valerian, skullcap, chamomile, or hops can ↑ CNS depression.

Availability ⬆ ⬇

(Generic available)

Sublingual/buccal film (Igalmi): 120 mcg; 180 mcg
Premixed infusion (in 0.9% NaCl): 80 mcg/20 mL; 200 mcg/50 mL; 400 mcg/100 mL; 1000 mcg/250 mL
Solution for injection: 4 mcg/mL; 100 mcg/mL

Route/Dosage ⬆ ⬇

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.

SL (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).
SL 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

SL (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).

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Acts as a relatively selective alpha-2 adrenergic agonist with sedative properties.

Therapeutic effects:

Sedation.
Decreased agitation.

Classifications ⬆ ⬇

Therapeutic Classification: sedative/hypnotics

Pharmacologic Classification: alpha adrenergic agonists

Pharmacokinetics ⬆ ⬇

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.

ROUTE	ONSET	PEAK	DURATION
IV	rapid	unknown	unknown
SL/buccal	20–30 min	60–90 min	2 hr

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Indications ⬇

Contraind./Precautions ⬆ ⬇