Stahl's Essential Psychopharmacology Online
In Collaboration With
Riluzole
Therapeutics
Brands
• Rilutek
Generic?
No
Class
• Neuromuscular drug, centrally acting
Commonly Prescribed for
(FDA approved in bold)
• Amyotrophic lateral sclerosis (ALS)
How the Drug Works
• The
mode of action is unknown, but the effect in ALS is felt to be from
glutamate antagonism. Putative mechanisms include
inhibition of glutamate release,
interference with transmitter binding at excitatory amino acid
receptors, and inactivation
of voltage-gated sodium channels. In
animal models, appears to be neuroprotective in mice with human
superoxide dismutase
mutations and has sedative and
myorelaxant properties at large doses
How Long Until It Works
• Steady state is reached in 5 days, but it can take months to assess any clinical effect from the drug
If It Works
• ALS is a degenerative disease and deterioration is the general rule. Riluzole can increase survival or time to tracheostomy
but is not a cure
If It Doesn't Work
• It
is difficult to determine if the treatment is effective, especially
because ALS progression varies greatly from patient
to patient. Supportive care is the
mainstay of current ALS treatment. This may include monitoring and
treatment of gait, swallowing
and respiratory difficulties
Best Augmenting Combos for Partial Response or Treatment-Resistance
• No other medication is indicated for the treatment of ALS progression
Tests
• Measure
serum transaminases, including ALT levels, at baseline and monthly for 3
months. Then evaluate every 3 months for
the first year and periodically
after that. Once ALT exceeds 5 times normal, begin checking weekly, and
discontinue if ALT
exceeds 10 times normal or clinical
symptoms, such as jaundice, occur