Flumazenil " Anexate"
Trade names:
Anexate
Drug class: Benzodiazepine antagonist; reverses sedative effects of
benzodiazepines used in conscious sedation and general anesthesia; treatment of
benzodiazepine overdose Pregnancy: (Category C)
Therapeutic actions
Competitively
inhibits the activity at the benzodiazepine recognition site on the
GABA/benzodiazepine receptor complex. Flumazenil does not antagonize the CNS
effect of drugs affecting GABA-ergic neurons by means other than the
benzodiazepine receptor (ethanol, barbiturates, general anesthetics) and does
not reverse the effects of opioids
Dose:
§ By intravenous injection, 0.8–2 mg repeated at intervals of 2–3
minutes to a max. of 10 mg if respiratory function does not improve (then
question diagnosis); CHILD 10 micrograms/kg; subsequent dose of
100 micrograms/kg if no response
§ By subcutaneous or intramuscular injection, as intravenous
injection butonly if intravenous route not feasible (onset of action slower)
§ By continuous intravenous infusion using an infusion pump, 10 mg
diluted in 50 mL intravenous infusion solution at a rate adjusted according to
the response
Adverse Reactions
§ >10%
§ Gastrointestinal: Vomiting, nausea
§ 1% to 10%:
§ Cardiovascular: Palpitations
§ Central nervous system: Headache, anxiety, nervousness,
insomnia, abnormal crying, euphoria, depression, agitation, dizziness,
emotional lability, ataxia, depersonalization, tears increased, dysphoria,
paranoia, fatigue, vertigo
§ Endocrine & metabolic: Hot
flashes
§ Gastrointestinal: Xerostomia
§ Local: Pain at injection site
§ Neuromuscular & skeletal:
Tremor, weakness, paresthesia
§ Ocular: Abnormal vision, blurred
vision
§ Respiratory: Dyspnea,
hyperventilation
§ Miscellaneous: Diaphoresis
§ <1%:
Abnormal hearing, altered blood pressure (increases and decreases), confusion,
sensation of coldness, bradycardia, chest pain, generalized convulsions,
hiccups, hypertension, junctional tachycardia, shivering, somnolence,
tachycardia, thick tongue, ventricular tachycardia, withdrawal syndrome
§ Postmarketing and/or case reports:
Fear, panic attacks
Overdosage/Toxicology
Excessively high doses may cause anxiety, agitation, increased muscle
tone, hyperesthesia and seizures.
Nursing
Implications
§ Parenteral: For I.V. use only;
§ administer via freely running I.V.
infusion into larger vein to decrease chance of pain, phlebitis
Patient Education
§ Flumazenil does not consistently
reverse amnesia. Do not engage in activities requiring alertness for 18-24
hours after discharge.
§ Avoid alcohol or OTC medications for
24 hours after receiving this medication, unless approved by prescriber.
§ Resedation may occur in patients on
long-acting benzodiazepines (such as diazepam).
§ Pregnancy/breast-feeding
precautions: Should Inform physician if
you she is or intend to become pregnant and Consult him if she is a
breast-feeding.