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