Classifications: benzodiazepine anxiolytic; sedative-hypnotic; Therapeutic: antianxiety; sedative-hypnotic
Pregnancy Category: D
Controlled Substance: Schedule IV
2 mg/mL syrup; 1 mg/mL, 5 mg/mL injection
Short-acting parenteral benzodiazepine that intensifies activity of gamma-aminobenzoic acid (GABA), a major inhibitory neurotransmitter
of the brain, by interfering with its reuptake and promoting its accumulation at neuronal synapses. This calms the patient,
relaxes skeletal muscles, and in high doses produces sleep.
Has CNS depressant with muscle relaxant, sedative-hypnotic, anticonvulsant, and amnestic properties.
Sedation before general anesthesia, induction of general anesthesia; to impair memory of perioperative events (anterograde
amnesia); for conscious sedation prior to short diagnostic and endoscopic procedures; and as the hypnotic supplement to
nitrous oxide and oxygen (balanced anesthesia) for short surgical procedures.
Intolerance to benzodiazepines; acute narrow-angle glaucoma; shock, coma; acute alcohol intoxication; intraarterial injection;
status asthmaticus; pregnancy (category D), obstetric delivery, lactation.
Patient with COPD; chronic kidney failure; cardiac disease; pulmonary insufficiency; dementia; electrolyte imbalance; neuromuscular
disease; Parkinson's disease; psychosis; CHF; older adults; bipolar disorder.
Route & Dosage
Adult: IM 0.070.08 mg/kg 3060 min before procedure IV 12.5 mg, may repeat in 2 min prn; Intubated Patients, 0.050.2 mg/kg/h by continuous infusion
Child: IM 0.08 mg/kg x 1 dose PR 0.3 mg/kg x 1 dose; Intubated Patients, 2 mcg/kg/min by continuous infusion, may increase by 1 mcg/kg/min q30 min until light sleep is induced
Neonate: IV 0.51 mcg/kg/min
IV Induction for General Anesthesia
Adult: IV Premedicated, 0.150.25 mg/kg over 2030 sec, allow 2 min for effect IV Non premedicated, 0.30.35 mg/kg over 2030 sec, allow 2 min for effect
Child: IV 0.15 mg/kg followed by 0.05 mg/kg q2min times 13 doses
Child: IV Loading Dose >2 mo, 0.15 mg/kg IV Maintenance Dose 1 mcg/kg/min infusion, may titrate upward as needed q5min
Child: PO <5 y, 0.5 mg/kg; >5 y, 0.40.5 mg/kg
- Inject IM drug deep into a large muscle mass.
PREPARE: Direct: Dilute in D5W or NS to a concentration of 0.25 mg/mL (e.g., 1 mg in 4 mL or 5 mg in 20 mL). IV Infusion: Add 5 mL of the 5 mg/mL concentration to 45 mL of D5W or NS to yield 0.5 mg/mL.
ADMINISTER: Direct for Conscious Sedation: Give over ≥2 min. Direct for Induction of Anesthesia: Give over 2030 sec. Direct for Neonate: DO NOT give bolus dose; give over at least 2 min. IV Infusion: Give at a rate based on weight.
INCOMPATIBILITIES Solution/additive: Lactated Ringer's, pentobarbital, perphenazine, prochlorperazine. Y-site: Albumin, amoxicillin, amoxicillin/clavulanate, amphotericin B cholesteryl complex, ampicillin, bumetanide, butorphanol,
ceftazidime, cefuroxime, clonidine, dexamethasone, foscarnet, fosphenytoin, furosemide, hydrocortisone, imipenem/cilastatin,
methotrexate, nafcillin, omeprazole, sodium bicarbonate, thiopental, TPN, trimethoprim/sulfamethoxazole.
- Store at 15°30° C (59°86° F), therapeutic activity is retained for 2 y from date of manufacture.
Adverse Effects (≥1%)CNS: Retrograde amnesia,
headache, euphoria, drowsiness, excessive sedation, confusion. CV:
Hypotension. Special Senses:
Blurred vision, diplopia
, nystagmus, pinpoint pupils. GI:
Nausea, vomiting. Respiratory:
(rare), respiratory arrest. Skin:
Hives, swelling, burning, pain, induration at injection site, tachypnea. Body as a Whole:
Hiccups, chills, weakness.
InteractionsDrug: Alcohol, cns depressants
increases midazolam plasma
levels, increasing its toxicity
; may decrease antiparkinsonism effects of levodopa;
may increase phenytoin
decreases sedative and antianxiety effects. Food: Grapefruit juice
(>1 qt/d) may increase risk of myopathy and rhabdomyolysis. Herbal: Kava, valerian
may potentiate sedation. Echinacea, St. John's wort
may reduce efficacy
15 min IV
; 515 min IM, 2030 min PO. Peak:
2060 min. Duration:
<2 h IV
; 16 h IM. Distribution:
Crosses bloodbrain barrier and placenta. Metabolism:
In liver (CYP3A4). Elimination:
In urine. Half-Life:
Assessment & Drug Effects
- Inspect insertion site for redness, pain, swelling, and other signs of extravasation during IV infusion.
- Monitor closely for indications of impending respiratory arrest. Resuscitative drugs and equipment should be immediately
- Monitor for hypotension, especially if the patient is premedicated with a narcotic agonist analgesic.
- Monitor vital signs for entire recovery period. In obese patient, half-life is prolonged during IV infusion; therefore, duration
of effects is prolonged (i.e., amnesia, postoperative recovery).
- Be aware that overdose symptoms include somnolence, confusion, sedation, diminished reflexes, coma, and untoward effects
on vital signs.
Patient & Family Education
- Do not drive or engage in potentially hazardous activities until response to drug is known. You may feel drowsy, weak, or
tired for 12 d after drug has been given.
- Be prepared for amnesia to prevent an upsetting postoperative period.
- Review written instructions to assure future understanding and compliance. Patient teaching during amnestic period may not
be remembered. Even if dose is small and depth of amnesia is unclear, relearn information.