Dantrolene (Dantrium)

Post a comment

Name: Dantrolene (Dantrium)

Class: Muscle Relaxant (Peripherally Acting)

Mechanism: Decreases excitation-contraction coupling in muscle fibers by interfering w/release of Ca2+ from sarcoplasmic reticulum.

Absorption:

Dist.:

Metabolism.:

Excretion, :

Toxicity/S.E.s: Muscle weakness, sedation. Chronic treatment occasionally ® hepatitis.

Utility: Treat spasticity due to spinal cord injury, cerebral palsy, multiple sclerosis, stroke, amyotrophic lateral sclerosis. Treat malignant hyperthermia. Treat neuroleptic malignant syndrome (efficacy prob. not due to block of Ca2+ release).

Special Features: A hydantoin derivative.

 

Baclofen (Lioresal)

Post a comment

Name: Baclofen (Lioresal)

Class: Muscle Relaxant (Centrally Acting)

Mechanism: GABAB agonist ® inhib. of neurotrans. release ® ¯ release of glutamate from Ia afferents & upper motor neurons.

Absorption:

Dist.:

Metabolism.:

Excretion, :

Toxicity/S.E.s: Sedation (much less than diazepam), ­ seizure activity in epileptics, dizziness, blurred vision, muscle weakness, ataxia.

Utility: Preferred drug for treatment of spasticity assoc. w/ALS, spinal cord trauma, multiple sclerosis, & cerebral palsy.

Special Features:

 

Entacapone

Post a comment

Name: Entacapone

Class: Antiparkinsonian (COMT Inhibitor)

Mechanism: Inhib. COMT ® ­ plasma conc. of L-Dopa ® ­ free L-Dopa in brain ® ­ DA in brain.

Absorption:

Dist.:

Metabolism.:

Excretion, :

Toxicity/S.E.s: Nausea (from ­ peripheral DA), ­ dyskinesia.

Utility: Treat symptoms of Parkinson’s Disease. Increases duration of response to L-Dopa, decreases required daily dose of L-Dopa.

Special Features:

 

Tolcapone

Post a comment

Name: Tolcapone

Class: Antiparkinsonian (COMT Inhibitor)

Mechanism: Inhib. COMT ® ­ plasma conc. of L-Dopa ® ­ free L-Dopa in brain ® ­ DA in brain.

Absorption:

Dist.:

Metabolism.:

Excretion, :

Toxicity/S.E.s: Nausea (from ­ peripheral DA), ­ dyskinesia.

Utility: Treat symptoms of Parkinson’s Disease. Increases duration of response to L-Dopa, decreases required daily dose of L-Dopa.

Special Features:

 

Amantadine (Symmetrel)

Post a comment

Name: Amantadine (Symmetrel)

Class: Antiviral/Antiparkinsonian Agent

Mechanism: Blocks a late stage in assembly of influenza A virus

Absorption: Well absorbed orally.

Distribution:

Metabolism.:

Excretion, t½: Excreted unchanged in urine.

Toxicity/S.E.s: CNS toxicity (nervousness, confusion, hallucinations, insomnia, depression, confusion). Overdose ® toxic psychosis. Freq. livedo reticularis (skin mottling). Peripheral edema, freq. nausea. C/I w/hist. of seizures or congestive heart failure. Amantadine>rimantadine

Utility: Treat influenza A. Treat Parkinson’s Disease symptoms ® improvement
of akinesia, rigidity, tremor, gait disturbances, & total disability in ~ 50% of patients (Mechanism unknown). Use alone or w/L-Dopa for PD.

Features: Can be used prophylactically for influenza A. For PD, sustained improvement may last up to 30 months, but may also be short lived (1-3 months). For PD, as good as or better than anticholinergics.