brands

Class

• Benzodiazepine receptor antagonist

Flumazenil commonly prescribed for

(Bold for FDA approved)

How Flumazenil works

• Blocks benzodiazepine receptors at GABA-A ligand-gated chloride channel complex, preventing benzodiazepines from binding there

How long until Flumazenil works

• Onset of action 1–2 minutes; peak effect 6–10 minutes

Notable Side Effects

• May precipitate benzodiazepine withdrawal in patients dependent upon or tolerant to benzodiazepines

• Dizziness, injection site pain, sweating, headache, blurred vision

Life Threatening Side Effects

• Seizures

• Death (majority occurred in patients with severe underlying disease or who overdosed with non-benzodiazepines)

• Cardiac dysrhythmia

weight gain

unusual

sedation

unusual

What to do about Flumazenil side effects

• Monitor patient

• Restrict ambulation because of dizziness, blurred vision, and possibility of resedation

usual dosage range

• 0.4–1 mg generally causes complete antagonism of therapeutic doses of benzodiazepines

• 1–3 mg generally reverses benzodiazepine overdose

Dosage Forms

• Intravenous 0.1 mg/mL–5 mL multiple-use vial, 10 mL multiple-use vial

long term use

• Not a long-term treatment

habit forming

• No

Renal Impairment

• Dosage adjustment may not be necessary

Hepatic Impairment

• Prolongation of half-life

• Moderate: clearance reduced by half

• Severe: clearance reduced by threequarters

Cardiac Impairment

• Dosage adjustment may not be necessary

Elderly

• Dosage adjustment may not be necessary

Children and Adolescents

• More variability of pharmacokinetics than in adults

• Safety and efficacy established for reversal of conscious sedation for children over age 1

• Initial 0.01 mg/kg (up to 0.2 mg) over 15 seconds; same dosing pattern as adults; maximum 0.05 mg/kg or 1 mg

• Safety and efficacy for reversal of benzodiazepine overdose, general anesthesia induction or resuscitation of a newborn have not been established, but anecdotal data suggest similar safety and efficacy as for conscious sedation

Pregnancy

• Effective June 30, 2015, the FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001

• Controlled studies have not been conducted in pregnant women

• Not recommended to treat the effects of benzodiazepines during labor and delivery because the effects on the infant have not been studied

Breast Feeding

• Unknown if flumazenil is secreted in human breast milk, but all psychotropics are assumed to be secreted in breast milk

• If treatment with flumazenil is necessary, it should be administered with caution