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riluzole (Rilutek)

Indications: - amyotrophic lateral sclerosis (ALS) - Huntington's disease Dosage: 1) 50 mg PO every 12 hours 2) no increased benefits fromm larger amounts 3) take at same time each day, 1 hour before or 2 hours after meals Tabs: 50 mg. Dosage adjustment with hepatic impairment. Avoid excessive alcohol. Pharmacokinetics: - metabolized in the liver by cyt P450 1A2 Monitor: 1) liver function tests (serum AST, serum ALT, serum bilirubin, serum GGT) baseline [5] 2) serum transaminases (serum AST, serum ALT) a) monthly for 1st 3 months b) every 3 months for remainder of 1st year c) periodically thereafter 2) complete blood count (CBC) Adverse effects: - common (> 10%) - nausea, abdominal pain, constipation, elevation of serum alanine aminotransferase (ALT) Drug interactions: 1) drugs that induce cyt P450 1A2 reduce effect of riluzole a) cigarette smoke b) charbroiled foods c) rifampin d) omeprazole 2) inhibitors of cyt P450 1A2 increase toxicity of riluzole a) caffeine b) theophylline c) amitriptyline d) quinolones Mechanism of action: 1) antiglutamate activity; inhibits release of glutamate [1] 2) may slow the progression of amyotrophic lateral sclerosis a) benefit primarily in patients with bulbar-onset disease b) effectiveness in patients with limb-girdle disease is uncertain

Related

amyotrophic lateral sclerosis (ALS); Lou Gerig's disease cytochrome p450 1A2 (cytochrome P3-450, phenacetin deethylase, cytochrome p450-4, CYP1A2)

General

miscellaneous pharmacologic agent

Properties

MISC-INFO: elimination route LIVER KIDNEY pregnancy-category C safety in lactation -

Database Correlations

PUBCHEM cid=5070

References

  1. Medical Knowledge Self Assessment Program (MKSAP) 11, 17. American College of Physicians, Philadelphia 1998, 2015
  2. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: 220233 (subscription needed) http://www.prescribersletter.com
  5. Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: 260704 (subscription needed) http://www.prescribersletter.com