Anexate Injection, Iv Injection, Solution

Anexate, an imidazobenzodiazepine derivative, competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex.

Uses

Reversal of benzodiazepine-induced sedation, Benzodiazepine overdose

Anexate is also used to associated treatment for these conditions: Sedation caused by benzodiazepine, Anesthesia reversal, Reversal of sedation therapy

Trade Name Anexate
Generic Flumazenil
Other Names Flumazenil, Flumazenilo, Flumazenilum, Flumazepil
Weight 100mcg/ml, 0.5mg/5ml, 0.1mg/ml,
Type Injection, Iv Injection, Solution
Formula C15H14FN3O3
Weight Average: 303.2884
Monoisotopic: 303.101919534
Protein binding

Protein binding is approximately 50%, mostly (66%) to albumin. Protein binding is reduced in patients with hepatic cirrhosis.

Therapeutic Class Antidote preparations, Benzodiazepine antagonist
Manufacturer Martin Dow Pharmaceuticals (pak) Ltd,, Roche Bangladesh Limited
Available Country Pakistan, Bangladesh, Saudi Arabia, Portugal,
Last Updated: June 23, 2021 at 9:29 am

Dosage

Anexate dosage

Intravenous- Reversal of benzodiazepine-induced sedation

  • Adult: Anaesth: Initially, 200 mcg over 15 sec. A 2nd dose of 100 mcg can be given if desired degree of consciousness is not obtained w/in 60 sec. May be repeated at 60-sec intervals if necessary. Usual: 300-600 mcg. Max: 1,000 mcg. Intensive care: Initially, 300 mcg over 15 sec. A repeat dose of 100 mcg may be administered if desired degree of consciousness is not obtained w/in 60 sec. May be repeated at 60-sec intervals if necessary. Max: 2,000 mcg. If drowsiness recurs, admin a 2nd bolus inj. Infusion of 100-400 mcg/hr is also useful, adjust according to desired level of sedation.
  • Child: >1 yr Initially, 10 mcg/kg (up to 200 mcg) over 15 sec. Repeat at 60-sec intervals if desired level of consciousness is not obtained after 45 sec. Max: 50 mcg/kg or 1,000 mcg, whichever is lower.

Intravenous-

Benzodiazepine overdose

  • Adult: Initially, 200 mcg over 30 sec. Additional dose of 300 mcg may be given after 30 sec, followed by 500 mcg at 60-sec intervals if required. Max: 3,000 mcg or 5,000 mcg. Alternatively, infusion may be given at 100-500 mcg/hr, adjusted according to response. Further doses may not be useful if a cumulative dose of up to 5,000 mcg does not produce any response. If symptoms of intoxication recur, may repeat doses at 20-min intervals; repeat doses should not exceed 1,000 mcg/dose (given as 500 mcg/min) and 3,000 mcg/hr.

Side Effects

Dizziness, pain at inj site, increased sweating, headache, abnormal or blurred vision, nausea, vomiting, palpitations, anxiety, fear, transient HTN, flushing, agitation, chills, sensory disturbances.

Precaution

Patient with head injury, alcoholism and other drug dependencies, history of panic disorder. Not intended to treat benzodiazepine dependence or withdrawal syndrome. Should only be used until effects of neuromuscular blockade have been fully reversed. Hepatic impairment. Pregnancy and lactation.

Interaction

Antagonises central effects of benzodiazepines and non-benzodiazepine agonists (e.g. zopiclone, triazolopyridazine) by competitive interaction at the receptor.

Food Interaction

  • Take separate from meals. Eating during an intravenous infusion of flumazenil increases the elimination of flumazenil, potentially through elevated hepatic blood flow.

Volume of Distribution

  • 0.9 to 1.1 L/kg

Half Life

Initial distribution half-life is 4 to 11 minutes and the terminal half-life is 40 to 80 minutes. Prolongation of the half-life to 1.3 hours in patients with moderate hepatic impairment and 2.4 hours in severely impaired patients. Compared to adults, the elimination half-life in pediatric patients was more variable, averaging 40 minutes (range: 20 to 75 minutes).

Clearance

  • 1 L/hr/kg [healthy volunteers receiving a 5-minute infusion of a total of 1 mg]

Pregnancy & Breastfeeding use

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Contraindication

Patient receiving benzodiazepines to control potentially life-threatening conditions (e.g. status epilepticus, raised intracranial pressure). Severe intoxication w/ tricyclic and related antidepressants.

Storage Condition

Store between 20-25°C.