Product Information
Registration Status: ActiveZACETIN TABLET 0.25mg is approved to be sold in Singapore with effective from 1998-11-20. It is marketed by ZYFAS MEDICAL CO, with the registration number of SIN10458P.
This product contains Alprazolam 0.25mg in the form of TABLET. It is approved for ORAL use.
This product is manufactured by MEDICA KOREA CO LTD in KOREA, and in REPUBLIC OF.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of panic disorders, with or without agoraphobia, and in generalized anxiety disorders. (From AMA Drug Evaluations Annual, 1994, p238)
Indication
For the management of anxiety disorder or the short-term relief of symptoms of anxiety and for the treatment of panic disorder, with or without agoraphobia.
Mechanism of Action
Benzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
Pharmacokinetics
- Absorption
- Readily absorbed from the gastrointestinal tract. Bioavailability is 80-90%.
- Distribution
- Metabolism
- Hepatic. Hydroxylated in the liver to α-hydroxyalprazolam, which is also active. This and other metabolites are later excreted in urine as glucuronides.
- Elimination
Clearance
* 2.13 +/- 0.54 mL/min/kg [CYP3A inducers] * 0.90 +/- 0.21 mL/min/kg [without CYP3A inducers]
Toxicity
Oral, mouse: LD50=1020 mg/kg. Symptoms of overdose include confusion, coma, impaired coordination, sleepiness, and slowed reaction time.
Active Ingredient/Synonyms
8-Chloro-1-methyl-6-phenyl-4H-S-triazolo(4,3-a)(1,4)benzodiazepine | Alprazolam | Alprazolam |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.