Posted by djmmm on April 4, 2002, at 20:57:55
In reply to advise; Baclofen GHB connection?, posted by 3 Beer Effect on April 3, 2002, at 3:17:07
from cponline
http://cp.gsm.com/apps/images/photo_us_h/001//bacl001g.jpg
Description: Baclofen is an oral skeletal muscle relaxant. It is a structural analog of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). Clinically, baclofen is used to treat spasticity and improve mobility in patients with multiple sclerosis and other spinal cord lesions by decreasing the number and severity of spasms and relieving associated pain, clonus, and muscle rigidity. Baclofen also improves bowel and bladder function in some of these patients. Baclofen was approved by the FDA in November 1977. In February 1995, the FDA granted approval under a treatment IND to use intrathecal baclofen for the treatment of spasticity of cerebral origin; full FDA approval was granted in 1997.
Mechanism of Action: Baclofen's mechanism of action is not fully understood, but it is believed that the drug works mainly at the level of the spinal cord to block polysynaptic afferent pathways and, to a lesser extent, monosynaptic afferent pathways. Baclofen may inhibit the transmission of impulses through these pathways by acting as an inhibitory neurotransmitter itself or by hyperpolarizing the primary afferent nerve terminals, which inhibits the release of excitatory neurotransmitters such as glutamate and aspartic acids. Because large doses of baclofen cause CNS depression, it is postulated that the drug works at supraspinal sites as well. Baclofen has been described as a gamma-aminobutyric acid (GABA) agonist; the drug stimulates the GABA-B receptor. This leads to a decreased release of the neurotransmitters aspartate and glutamate and decreased excitatory input into alpha-motor neurons.
poster:djmmm
thread:101545
URL: http://www.dr-bob.org/babble/20020402/msgs/101866.html