General

Pronunciation:
rem-ih-maz-oh-lam

Trade Name(s)

• Byfavo

Ther. Class.

sedative/hypnotics

Pharm. Class.

benzodiazepines

Controlled Substance Schedule: IV

Indications

Induction and maintenance of procedural sedation in patients undergoing procedures lasting ≤30 min.

Action

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

Therapeutic Effect(s):

Rapid onset/offset of sedation during/after procedure.

Pharmacokinetics

Absorption: IV administration results in complete bioavailability.

Distribution: Well distributed to extravascular tissues.

Metabolism and 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.

TIME/ACTION PROFILE (sedation)

Contraindication/Precautions

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.

Adverse Reactions/Side Effects

CV: bradycardia, hypertension, hypotension, tachycardia

GI: nausea

Neuro: headache

Resp: RESPIRATORY DEPRESSION, tachypnea

Misc: HYPERSENSITIVITY REACTIONS (including anaphylaxis), fever, physical dependence

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

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

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.

Availability

Lyophilized powder for injection: 20 mg/vial

Assessment

• Assess level of sedation and level of consciousness during and for 2 hr following administration.
• Monitor BP, pulse, and respiration for early signs of hypoventilation, airway obstruction, and apnea using capnography, pulse oximetry, and clinical assessment continuously during administration, especially if coadministering opioid analgesics. Oxygen and resuscitative equipment should be immediately available during IV administration.
• Monitor for signs and symptoms of hypersensitivity reactions (rash, urticaria, pruritus, anaphylaxis) during therapy. Provide symptomatic support if symptoms occur.

If signs and symptoms of overdose (drowsiness, confusion, lethargy, with possible progression to ataxia, respiratory depression, hypotension) occurs, monitor pulse, respiration, and BP continuously. Maintain patent airway and assist ventilation as needed. If hypotension occurs, treatment includes IV fluids, repositioning, and vasopressors.

• The effects of remimazolam can be reversed with flumazenil.

Implementation

• Only personnel trained in the administration of procedural sedation and not involved in the conduct of the diagnostic or therapeutic procedure should administer remimazolam.
• IV Push:   Reconstitution: Reconstitute with 8.2 mL 0.9% NaCl, directing stream of solution toward wall of vial. Swirl gently until contents are fully dissolved; do not shake.  Concentration: 2.5 mg/mL. Solution is clear and colorless to pale yellow; do not use solutions that are cloudy, discolored, or contain particulate matter. Reconstituted solution is stable up to 8 hr at room temperature.
• Y-Site Compatibility:
  • dexmedetomidine
  • fentanyl
  • midazolam
  • MORE...
    • remifentanil
    • rocuronium
    • vecuronium

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.

Evaluation/Desired Outcomes

Rapid onset/offset of sedation during/after procedure.