Flumazenil
Indications
Flumazenil is used for:
Benzodiazepine-induced sedation, Benzodiazepine overdose
Adult Dose
Reversal of Conscious Sedation and General Anesthesia
0.2 mg IV over 15 sec
IF after 45 sec no response, administer 0.2 mg again over 1 min; may repeat at 1 min intervals; not to exceed 4 doses (1 mg)
IF resedation occurs, may repeat doses at 20-min intervals; not to exceed 1 mg/dose or 3 mg/hr
Benzodiazepine Overdose
0.2 mg IV over 15-30 sec
IF no response after 30 sec, administer 0.3 mg over 30 sec 1 min later; IF no response, repeat dose of 0.5 mg IV over 30 sec at 1-min intervals to max cumulative dose of 3 mg/hr
In the event of resedation, may repeat dose at 20-min intervals if needed; not to exceed 1 mg (administered as 0.5 mg/min) administered at any one time and no more than 3 mg/hr
Rarely patient may require titration up to total dose 5 mg; IF no response after 5 min, sedation unlikely to be secondary to benzodiazepines
Hepatic impairment: Initial dose adjustment not necessary; reduce dose or frequency of subsequent doses
Child Dose
Reversal of Benzodiazepine Sedation
Initial dose: 0.01 mg/kg IV x1 dose over 15 sec
May repeat after 45 sec and then every minute; not to exceed 4 doses for a maximum 0.05 mg/kg or 1 mg, whichever is lower
Renal Dose
Renal impairment: Not studied
Administration
Contra Indications
Hypersensitivity. Patients receiving benzodiazepines for control of a potentially life-threatening condition such as status epilepticus and control of intracranial pressure. Severe intoxication with tricyclic and related antidepressants.
Precautions
Should only be used until the effects of neuromuscular blockade have been fully reversed. Risk of raising intracranial pressure, precipitating convulsions or altering cerebral blood flow in patients with head injuries. Increased risk of seizures in high-risk patients. May provoke panic attacks in patient with a history of panic disorder. Hepatic impairment. Pregnancy and lactation.
Lactation: Excretion in milk unknown; use with caution
Pregnancy-Lactation
Pregnancy category: C
Lactation: Excretion in milk unknown; use with caution
Interactions
Toxic effects with cyclic antidepressants. Reverses effects of benzodiazepines.
Side Effects
Side effects of Flumazenil :
>10%
Nausea and vomiting (11%)
1-10%
Dizziness (10%), Abnormal/blurred vision (3-9%), Agitation (3-9%), Dyspnea (3-9%), Hyperventilation (3-9%), Pain at injection site (3-9%), Xerostomia (3-9%), Diaphoresis (1-3%), Emotional lability (1-3%), Fatigue (1-3%), Headache (1-3%), Paresthesia (1-3%), Tremor (1-3%), Weakness (1-3%)
<1%
Delirium, Abnormal hearing, Junctional tachycardia, Thick tongue, Tinnitus, Coldness sensation, Generalized seizure
Mode of Action
Flumazenil competitively inhibits the activity at the benzodiazipine recognition site on the GABA/benzodiazepine receptor complex.