Products
Baclofen is commercially available as in tablet form and as a solution for injection (Lioresal, generics). It has been approved in many countries since 1970.
Structure and properties
Baclofen (C
10
H
12
ClNO
2
, M
r
= 213.7 g/mol) exists as a white and odorless powder that is sparingly soluble in water. It is a derivative of GABA and a racemate.
Effects
Baclofen (ATC M03BX01) has antispasmodic, central depressant, and antinociceptive properties. The effects are due to inhibition of excitatory transmission in the spinal cord by stimulation of GABA
B
-receptors. This inhibits the release of the excitatory amino acids glutamate and aspartate. The half-life is between 3 to 4 hours.
Indications
- For the treatment of muscular spasticity in multiple sclerosis.
- For spinal spasticity with an infectious, degenerative, traumatic or neoplastic cause.
Dosage
According to the professional information. Treatment is started gradually. Tablets are usually taken three times daily with meals. Baclofen may also be administered intrathecally.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Adverse effects
The most common possible adverse effects include drowsiness, somnolence, and nausea.
