MIORELCopy

• DRUGBANK - Baclofen
• 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.

• pharmacology:

• mechanism:

  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.

• toxicity:

  LD<sub>50</sub>=45 mg/kg (male mice, IV); LD<sub>50</sub>=78 mg/kg (male rat, IV)

• absorprion:

  Rapidly and almost completely absorbed from the GI tract.

• halflife:

  2.5-4 hours

• roouteelimination:

  In a study using radiolabeled baclofen, approximately 85% of the dose was excreted unchanged in the urine and feces. Baclofen is excreted primarily by the kidney as unchanged drug; 70 - 80% of a dose appears in the urine as unchanged drug. The remainder is excreted as unchanged drug in the feces or as metabolites in the urine and feces.

• volumedistribution:

  * 59 L

• clearance:

  * 180 mL/min