"Amyotrophic lateral sclerosis (ALS), often referred to as Lou Gehrig's
disease, is a progressive neurodegenerative disease that affects nerve
cells in the brain and the spinal cord. Motor neurons reach from the
brain to the spinal cord and from the spinal cord to the muscles
throughout the body. The progressive degeneration of the motor neurons
in ALS eventually lead to their death. When the motor neurons die, the
ability of the brain to initiate and control muscle movement is
This is a direct quote from the ALS Association.
For more info, please
Mechanism of Action The etiology and pathogenesis of amyotrophic lateral sclerosis
(ALS) are not known, although a number of hypotheses have been advanced.
One hypothesis is that motor neurons, made vulnerable through either
genetic predisposition or environmental factors, are injured by
glutamate. In some cases of familial ALS the enzyme superoxide dismutase
has been found to be defective.
The mode of action of RILUTEK is unknown. Its pharmacological properties
include the following, some of which may be related to its effect: 1) an
inhibitory effect on glutamate release, 2) inactivation of
voltage-dependent sodium channels, and 3) ability to interfere with
intracellular events that follow transmitter binding at excitatory amino
Riluzole has also been shown, in a single study, to delay median time to
death in a transgenic mouse model of ALS. These mice express human
superoxide dismutase bearing one of the mutations found in one of the
familial forms of human ALS.
It is also neuroprotective in various in vivo experimental models of
neuronal injury involving excitotoxic mechanisms. In in vitro tests,
riluzole protected cultured rat motor neurons from the excitotoxic
effects of glutamic acid and prevented the death of cortical neurons
induced by anoxia.
Due to its blockade of glutamatergic neurotransmission, riluzole also
exhibits myorelaxant and sedative properties in animal models at doses
of 30 mg/kg (about 20 times the recommended human daily dose) and
anticonvulsant properties at a dose of 2.5 mg/kg (about 2 times the
recommended human daily dose).
Recommended dose: 50 mg
q12h. No increased benefit can be expected from higher daily doses, but
adverse events are increased. Rilutek tablets should be taken at least
an hour before, or two hours after, a meal to avoid a food-related
decrease in bioavailability.
[Supplied: 50 mg
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