Product Information
Registration Status: ActiveAPO-LORAZEPAM TABLET 0.5mg is approved to be sold in Singapore with effective from 1989-06-10. It is marketed by PHARMAFORTE SINGAPORE PTE LTD, with the registration number of SIN03708P.
This product contains Lorazepam 0.5mg in the form of TABLET. It is approved for ORAL use.
This product is manufactured by APOTEX INC in CANADA.
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 benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent.
Indication
For the management of anxiety disorders, and for treatment of status epilepticus.
Mechanism of Action
Lorazepam binds to an allosteric site on GABA-A receptors, which are pentameric ionotropic receptors in the CNS. Binding potentiates the effects of the inhibitory neurotransmitter GABA, which upon binding opens the chloride channel in the receptor, allowing chloride influx and causing hyperpolerization of the neuron.
Pharmacokinetics
- Absorption
- Readily absorbed with an absolute bioavailability of 90% when given orally. When intramuscularly administered, lorazepam is completely and rapidly absorbed. It achieves max serum concentration in 3 hours. The max serum concentration of a 4 mg dose is 48 ng/mL.
- Distribution
- 1.3 L/kg. Unbound lorazepam can cross the blood-brain-barrier via passive diffusion.
- Metabolism
- Lorazepam is hepatically metabolized and is extensively conjugated to the 3-0-phenolic glucuronide. This is an inactive metabolite and is eliminated mainly by the kidneys.
- Elimination
Clearance
Total clearance, parenteral administration = 1.1±0.4 mL/min/kg.
Toxicity
The most important clinical adverse event caused by lorazepam is respiratory depression. LD50, mouse, oral = 1850 mg/kg.
Active Ingredient/Synonyms
o-Chlorooxazepam | o-Chloroxazepam | Lorazepam |
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.