remimazolam

Contraindicated in:

Severe hypersensitivity to dextran 40.

Use Cautiously in:

Severe hepatic impairment (may require ↓ frequency of supplemental doses);
OB: Use during third trimester or labor can ↑ risk of respiratory depression, sedation, and neonatal withdrawal symptoms in neonate; may affect child's brain development when used during 3rd trimester;
Lactation: May ↑ risk of sedation in infant; use while breastfeeding only if potential maternal benefit justifies potential risks to infant;
Pedi: Safety and effectiveness not established in children; may affect brain development in children <3 yr.

Adv. Reactions/Side Effects ⬆ ⬇

CV: bradycardia, hypertension, hypotension, tachycardia

GI: nausea

Neuro: headache

Resp: respiratory depression, tachypnea

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS), fever, physical dependence

Interactions ⬆ ⬇

Drug-drug:

↑CNS depression with alcohol, antihistamines, opioid analgesics, and other sedative/hypnotics, including propofol.

Availability ⬆ ⬇

Lyophilized powder for injection: 20 mg/vial

Route/Dosage ⬆ ⬇

IV (Adults ): Induction of procedural sedation: 5 mg as a single dose; Maintenance of procedural sedation: 2.5 mg initially; may repeat dose after ≥2 min to maintain sedation during procedure.
IV (Adults American Society of Anesthesiologists Physical Status [ASA-PS] III or IV): Induction of procedural sedation: 2.5–5 as a mg single dose; Maintenance of procedural sedation: 1.25–2.5 mg initially; may repeat dose after ≥2 min to maintain sedation during procedure.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Binds to GABA_A receptors in brain, which decreases the firing rate of neurons and produces an inhibitory response.

Therapeutic effects:

Rapid onset/offset of sedation during/after procedure.

Classifications ⬆ ⬇

Therapeutic Classification: sedative/hypnotics

Pharmacologic Classification: benzodiazepines

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability.

Distribution: Well distributed to extravascular tissues.

Metabolism/Excretion: Metabolized by tissue esterases to inactive metabolite, which then undergoes hydroxylation and glucuronidation. Primarily excreted in urine as inactive metabolite.

Half-Life: 37–53 min.

Contr. Subst. Schedule ⬆ ⬇

Time/Action Profile ⬆ ⬇

(sedation)

ROUTE	ONSET	PEAK	DURATION
IV	rapid	3–3.5 min	11–14 min

Patient/Family Teaching ⬆ ⬇

Inform patient that this medication will decrease mental recall of the procedure.
May cause drowsiness or dizziness. Advise patient to request assistance prior to ambulation and transfer and to avoid driving or other activities requiring alertness for 24 hr following administration.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any Rx, OTC, or herbal products.
Advise patient to avoid alcohol or other CNS depressants for 24 hr following administration of remimazolam.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Advise patient to wait 5 hr after administration to breastfeed; women may pump and discard until then to reduce infant exposure. May cross the placenta and may produce respiratory depression and sedation in neonates. Monitor neonates exposed to remimazolam during pregnancy or labor for signs of sedation and monitor neonates exposed to remimazolam during pregnancy for signs of withdrawal.

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇