Names and pronunciation
(flu-maz′e-nill) Anexate
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Drug reference
(flu-maz′e-nill) Anexate
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Func. class.: Antidote: benzodiazepine receptor antagonist
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Chem. class.: Imidazobenzodiazepine derivative
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Do not confuse: flumazenil/influenza virus vaccine
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ACTION: Antagonizes actions of ben- zodiazepines on CNS, competitively inhibits activity at benzodiazepine recog- nition site on GABA/benzodiazepine receptor complex
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USES: Reversal of sedative effects of benzodiazepines
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CONTRAINDICATIONS: Hyper- sensitivity to this product or benzodiaz- epines, serious cyclic antidepressant overdose, patients given benzodiazepine for control of life-threatening conditions Precautions: Pregnancy, breastfeeding, children, geriatric patients, status epilep- ticus, head injury, labor/delivery, renal/ hepatic disease, hypoventilation, panic disorder, drug and alcohol dependency, ambulatory patients, benzodiazepine dependence
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Black Box Warning: Seizures Black Box Warning: Seizures: protect from injury; most likely among those who are withdrawing from benzodiazepines; seizures are increased in head trauma • GI symptoms: nausea, vomiting; place patient in side-lying position to prevent aspiration • Allergic reactions: flushing, rash, urti- caria, pruritus Black Box Warning: Seizures/benzo- diazepine dependence: do not use in those who have used these products for status epilepticus; use in intensive care setting cautiously, there may be unrecog- nized benzodiazepine dependence • Pregnancy/breastfeeding: no well- controlled studies; use only if benefits outweigh fetal risk; discontinue breast- feeding or product
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SIDE EFFECTS CNS: Dizziness, agitation, emotional lability, confusion, seizures, somnolence, panic attacks CV: Hypertension, palpitations, cutane- ous vasodilation, dysrhythmias, brady- cardia, tachycardia, chest pain EENT: Abnormal vision, blurred vision, tinnitus GI: Nausea, vomiting, hiccups SYST: Headache, inj site pain, increased sweating, fatigue, rigors
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INTERACTIONS • Toxicity: mixed product overdosage • Antagonize action of benzodiazepines, zaleplon, zolpidem
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DOSAGE AND ROUTES Reversal of conscious sedation or general anesthesia • Adult: IV 0.2 mg over 15 sec; wait 45 sec, then 0.2 mg if consciousness does not occur; may be repeated at 60-sec in- tervals prn (max 3 mg/hr) or 1 mg/5 min • Child: IV 10 mcg (0.01 mg)/kg; cumu- lative dose of 1 mg or less Management of suspected benzodiazepine overdose • Adult: IV 0.2 mg over 30 sec; wait 30 sec, then give 0.3 mg over 30 sec if con- sciousness does not occur; further doses of 0.5 mg can be given over 30 sec at intervals of 1 min up to cumulative dose of 3 mg • Child: IV 10 mcg (0.01 mg/kg), cumu- lative dose of <1 mg
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Available forms: Inj 0.1 mg/mL
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Administer: • Check airway and IV access before ad- ministration • Use large vein Direct IV route • Give undiluted or diluted with 0.9% NaCl, D5W, LR; give over 15-30 sec into running IV, check for extravasation • Stable for 24 hr if drawn into a syringe or mixed with other solutions
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Assess: • Cardiac and respiratory status using continuous monitoring
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • Not to use with alcohol or other medi- cations for at least 24 hr • That sedation may occur after treatment • To avoid hazardous activities, driving until effects are known • That amnesia may continue
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PHARMACOKINETICS Half-life 41-79 min (adult), 20-75 min (child), metabolized in liver, onset 1-2 min 50% protein binding (albumin)
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• Adult: IV 0.2 mg over 15 sec; wait 45 sec, then 0.2 mg if consciousness does not occur; may be repeated at 60-sec in- tervals prn (max 3 mg/hr) or 1 mg/5 min
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• Adult: IV 0.2 mg over 30 sec; wait 30 sec, then give 0.3 mg over 30 sec if con- sciousness does not occur; further doses of 0.5 mg can be given over 30 sec at intervals of 1 min up to cumulative dose of 3 mg
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