Description
General Information
- Metabolism: Ketazolam breaks down in the blood to diazepam which breaks down to demoxepam which breaks down to desmethyldiazepam. Route of Elimination: Diazepam and its metabolites are excreted mainly in the urine, predominantly as their glucuronide conjugates. Half Life: 26-200 hours
- Uses/Sources: Ketazolam could be used for the treatment of anxiety. In approved countries, it is indicated for the treatment of anxiety, tension, irritability and similar stress related symptoms.
- Symptoms: Symptoms of overdose include somnolence, confusion, coma, and diminished reflexes. Respiration, pulse and blood pressure should be monitored.
- Treatment: General supportive measures should be employed, along with intravenous fluids, and an adequate airway maintained. Hypotension may be combated by the use of norepinephrine or metaraminol. Dialysis is of limited value. Flumazenil (Anexate) is a competitive benzodiazepine receptor antagonist that can be used as an antidote for benzodiazepine overdose. In particular, flumazenil is very effective at reversing the CNS depression associated with benzodiazepines but is less effective at reversing respiratory depression. Its use, however, is controversial as it has numerous contraindications. It is contraindicated in patients who are on long-term benzodiazepines, those who have ingested a substance that lowers the seizure threshold, or in patients who have tachycardia or a history of seizures. As a general rule, medical observation and supportive care are the mainstay of treatment of benzodiazepine overdose. Although benzodiazepines are absorbed by activated charcoal, gastric decontamination with activated charcoal is not beneficial in pure benzodiazepine overdose as the risk of adverse effects often outweigh any potential benefit from the procedure. It is recommended only if benzodiazepines have been taken in combination with other drugs that may benefit from decontamination. Gastric lavage (stomach pumping) or whole bowel irrigation are also not recommended.
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
Gamma-aminobutyric acid receptor subunit alpha-1 Gamma-aminobutyric acid receptor subunit alpha-2 Gamma-aminobutyric acid receptor subunit alpha-3 Gamma-aminobutyric acid receptor subunit alpha-5 Gamma-aminobutyric acid receptor subunit beta-1 Gamma-aminobutyric acid receptor subunit beta-2 Gamma-aminobutyric acid receptor subunit beta-3 Gamma-aminobutyric acid receptor subunit delta Gamma-aminobutyric acid receptor subunit gamma-2 Gamma-aminobutyric acid receptor subunit gamma-3 Gamma-aminobutyric acid receptor subunit pi Gamma-aminobutyric acid receptor subunit rho-1 Gamma-aminobutyric acid receptor subunit rho-2 Gamma-aminobutyric acid receptor subunit gamma-1 Gamma-aminobutyric acid receptor subunit rho-3 Gamma-aminobutyric acid receptor subunit epsilon Translocator protein GABA-A receptor (anion channel) |
2874815 17139284 11752352 18384456 17016423 6738302 11443263 17631921 11752090 2867566 15009644 |