Product Information
Registration Status: ActivePMS-BACLOFEN TABLET 10mg is approved to be sold in Singapore with effective from 1998-09-22. It is marketed by MEDICELL PHARMACEUTICAL (S) PTE LTD, with the registration number of SIN10026P.
This product contains Baclofen 10mg in the form of TABLET. It is approved for ORAL use.
This product is manufactured by Pharmascience 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
Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant. Baclofen stimulates GABA-B receptors leading to decreased frequency and amplitude of muscle spasms. It is especially useful in treating muscle spasticity associated with spinal cord injury. It appears to act primarily at the spinal cord level by inhibiting spinal polysynaptic afferent pathways and, to a lesser extent, monosynaptic afferent pathways.
Indication
For the alleviation of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity.
Mechanism of Action
Baclofen is a direct agonist at GABAB receptors. The precise mechanism of action of Baclofen is not fully known. It is capable of inhibiting both monosynaptic and polysynaptic reflexes at the spinal level, possibly by hyperpolarization of afferent terminals, although actions at supraspinal sites may also occur and contribute to its clinical effect.
Pharmacokinetics
- Absorption
- Rapidly and almost completely absorbed from the GI tract.
- Distribution
- * 59 L
- Metabolism
- ~ 15% of the dose is metabolized in the liver, primarily by deamination. 70-80% of the dose is excreted unchanged or as metabolites in urine and the remainder is excreted in feces.
- Elimination
Clearance
* 180 mL/min
Toxicity
LD50=45 mg/kg (male mice, IV); LD50=78 mg/kg (male rat, IV)
Active Ingredient/Synonyms
(+-)-Baclofen | 4-Amino-3-(4-chlorophenyl)butyric acid | Baclofene | Baclofeno | Baclofenum | beta-(4-Chlorophenyl)gaba | beta-(Aminomethyl)-4-chlorobenzenepropanoic acid | beta-(Aminomethyl)-P-chlorohydrocinnamic acid | beta-(P-Chlorophenyl)-gamma-aminobutyric acid | DL-4-Amino-3-P-chlorophenylbutanoic acid | DL-Baclofen | gamma-Amino-beta-(P-chlorophenyl)butyric acid | Baclofen |
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.