Flumazenil

Drug #312

Flumazenil is a 1,4- benzodiazepine derivative. Flumazenil is the only benzodiazepine receptor antagonist available for clinical use at present. Flumazenil is approved for use in reversing the sedative effects of certain drugs (benzodiazipines). Flumazenil is used to counteract effects of benzodiazipines overdose. Flumazenil is administered intravenously.

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Primary Characteristics

It is of Synthetic origin and belongs to Benzodiazepine.

It belongs to Chloride Channel Potentiater antagonist pharmacological group on the basis of mechanism of action and also classified in Antidotes pharmacological group.

Molecular Weight: 303.3 · pK_a: 1.7 · Solubility in Water: 1 in 2000 · Non-proprietary name: Flumazenil.

Pharmacokinetics

Absorption: Flumazenil has an oral bioavailability is 97% (±2%), pre-systemic (first-pass) metabolism accounts for 75% (±5%).

Distribution: Flumazenil has a volume of distribution is 0.95 l/kg. plasma protein binding is 50%.

Elimination: it is metabolised via complete, Hepatic, plasma half-life is 0.7-1.3 hr, renal excretion is 90-95%.

Indications

Flumazenil is primarily indicated in conditions like Poisoning of benzodiazepine, Reversal of sedative effects of benzodiazepines in anaesthetic, Unconciousness.

Contraindications

Flumazenil is contraindicated in conditions like Epilepsy, Neuromuscular blockade.

Dosage

Flumazenil's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
200 ug	200 ug	—	IV	Load for 15 Seconds
450 ug	450 ug	—	IV	Maintenance, after 60 Sec interval
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
0 – 0	—	—		Not recommended in this age group

Drug Interactions

None recorded.

Side Effects

Flumazenil in overdosage may give rise to further complications which include Cardiac arrhythmias, Cardiac arrhythmias .

Flumazenil produces potentially life-threatening effects which include Raised intracranial pressure. Careful monitoring is needed with proper medical management.

The signs and symptoms that are produced after acute overdosage of Flumazenil are Headache, Anxiety , Facial flushing.

Flumazenil is known to cause more or less tolerable side effects which are usually transient. These include Agitation , Anxiety, Confusion, dizziness, Facial erythema, Flushing, Headache, Nausea, Resedation .

Warnings / Precautions

Flumazenil should be used with caution in patients with history of seizures, panic attacks, alcohol or drug dependency, breathing disorders, heart disease, liver disease, head injury or if have any allergy. This drug should be used only if clearly needed during pregnancy or lactation. This drug is not recommended for use in children.

Interference in Pathology

Flumazenil may interfere in the diagnosis of None well documented.

Available Brands

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Single Ingredient

Inj

100 mcg/ml

Storage Conditions

Flumazenil should be stored Inj.

Drug Classification

1.4.2.10 — Benzodiazepines poisoning

Manufacturers

Manufacturers of Flumazenil in Pakistan:

Martin