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. 2022 Apr 4;69(1):49–58. doi: 10.2344/anpr-69-01-09

Table 1. .

Summary of Reversal Agents*

Pharmacology
Flumazenil
Naloxone
Neostigmine
Sugammadex
Phentolamine
Indication for use Complete or partial reversal of BZD-induced overdose Complete or partial reversal of opioid-induced overdose Reversal of nondepolarizing NMBDs Reversal of rocuronium and vecuronium Rocuronium-induced allergy or anaphylaxis?† Reversal of local anesthetic At risk for self-injurious behaviors or needed return of normal functions
Contraindications Hypersensitivity Chronic/continued BZD use Head injury Alcoholism or drug dependency Signs of tricyclic antidepressants overdose Hypersensitivity Hypersensitivity Peritonitis Mechanical obstruction of the intestinal or urinary tract Hypersensitivity Severe renal impairment Hypersensitivity Severe cardiovascular disease
Pharmacologic effect BZD receptor competitive antagonist Opioid receptor competitive antagonist Acetylcholinesterase inhibitor Cyclodextrin encapsulates rocuronium or vecuronium Nonselective α-adrenergic receptor antagonist
Onset, min 1-2 1-2 1 2 (2 mg/kg) 3 (4 mg/kg) 1.5 (16 mg/kg) 50 (maxilla) 70 (mandible)
Duration, min 19-50 5-45 20-30
Peak effect, min 6-10 5-15 9
Available formulation(s) 0.1 mg/mL IV 0.02 mg/mL IV 0.4 mg/mL IV 1 mg /mL IV 2 mg/0.1 mL IN2 4 mg/0.1 mL IN 1 mg/mL IV 0.5 mg/mL IV 200 mg/2 mL IV 500 mg/5 mL IV 0.4 mg/mL × 1.7 mL cartridge
Recommended adult dosing 0.2 mg over first 15 s, then 0.2 mg every 1 min as necessary; max dose 1 mg 0.1-0.2 mg increments 0.05 mg/kg lean body weight 2-16 mg/kg actual body weight 0.8 mg (12+ y)
Recommended pediatric dosing 0.01 mg/kg over first 15 s up to max 0.2 mg, then 0.01 mg/kg up to 0.2 mg every 1 min; max 4 additional doses or max 1 mg or 0.05 mg/kg, whichever is lower 0.01 mg/kg IV/IM/ETT 0.03-0.07 mg/kg IV; max 5 mg Add atropine 0.02 mg/kg or glycopyrrolate 0.015 mg/kg IV Not established for ≤17 y 0.4 mg (6-11 y, ≥ 30 kg) 0.2 mg (6-11 y, 15-30 kg) 0.1 mg (≥10 kg)
Adverse events Seizures Withdrawal Dysrhythmias Anxiety Dysrhythmia Hypertension Tachycardia Pulmonary edema N/V Sweating Seizures Pain Dysphoria N/V Bradycardia Dysrhythmia QT prolongation Bronchospasm Salivation Miosis GI peristalsis Pain N/V Fever Headache Sore throat Back pain Cough Constipation Pain Hypertension Bradycardia Headache
Precautions Prolonged monitoring (2 h) Prolonged monitoring (2 h) Anticholinergic crisis Hypersensitivity Bradycardia Prolonged blockade QT prolongation AV block Cardiac arrest Tachycardia Dysrhythmia
* 

BZD, benzodiazepine; ETT, endotracheal tube; GI, gastrointestinal; IN, intranasal; IV, intravenous; IM, intramuscular; NMBDs, neuromuscular blocking drugs; N/V, nausea and vomiting.

† 

Case report finding, not indicated by product monograph.3