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Riluzole
Riluzole
Riluzole
(RIL-you-zohl)
Pregnancy Category: C Rilutek (Rx)

Classification: Drug for amyotrophic lateral sclerosis

Action/Kinetics: Mechanism not known. Possible effects include (a) inhibition of glutamate release, (b) inactivation of voltage-dependent sodium channels, and (c) interference with intracellular events that follow transmitter binding at excitatory amino acid receptors. Well absorbed following PO use; high-fat meals decrease absorption. t1/2, elimination, after repeated doses: 12 hr. About 96% is bound to plasma proteins. Extensively metabolized, mainly in the liver, and excreted in the urine.

Uses: Treatment of clients with ALS; the drug extends both survival and time to tracheostomy.

Contraindications: Lactation.

Special Concerns: Use with caution in hepatic and renal impairment due to decreased excretion and higher plasma levels. Use with caution in the elderly, as age-related changes in renal and hepatic function may cause a decreased clearance. Clearance of riluzole in Japanese clients is 50% lower compared with Caucasians; clearance may also be lower in women. Safety and efficacy have not been determined in children.

Side Effects: Side effects listed occurred at a frequency of 0.1% or more. GI: N&V;, diarrhea, anorexia, abdominal pain, dyspepsia, flatulence, dry mouth, stomatitis, tooth disorder, oral moniliasis, dysphagia, constipation, increased appetite, intestinal obstruction, fecal impaction, GI hemorrhage GI ulceration, gastritis, fecal incontinence, jaundice, hepatitis, glossitis, gum hemorrhage, pancreatitis, tenesmus, esophageal stenosis. Body as a whole: Asthenia, malaise, weight loss or gain, peripheral edema, flu syndrome, hostility, abscess, sepsis photosensitivity reaction, cellulitis, facial edema, hernia, peritonitis, reaction at injection site, chills, attempted suicide enlarged abdomen, neoplasm. CNS: Dizziness (more common in women), vertigo, somnolence, circumoral paresthesia, headache, aggravation reaction, hypertonia, depression, insomnia, agitation, tremor, hallucination, personality disorders, abnormal thinking, coma, paranoid reaction, manic reaction, ataxia, extrapyramidal syndrome, hypokinesis, emotional lability, delusions, apathy, hypesthesia, incoordination, confusion, convulsion amnesia, increased libido, stupor subdural hematoma, abnormal gait, delirium, depersonalization, facial paralysis, hemiplegia, decreased libido. CV: Hypertension, tachycardia, phlebitis, palpitation, postural hypotension, heart arrest, heart failure syncope, hypotension, migraine, peripheral vascular disease, angina pectoris, MI ventricular extrasystoles, cerebral hemorrhage atrial fibrillation, bundle branch block, CHF, pericarditis, lower extremity embolus, myocardial ischemia, shock. Hematologic: Neutropenia, anemia, leukocytosis, leukopenia, ecchymosis. Respiratory: Decreased lung function, pneumonia, rhinitis, increased cough, sinusitis, apnea, bronchitis, dyspnea, respiratory disorder, increased sputum, hiccup, pleural disorder, asthma, epistaxis, hemoptysis, yawn, hyperventilation, lung edema, hypoventilation, lung carcinoma hypoxia, laryngitis, pleural effusion, pneumothorax, respiratory moniliasis, stridor. Musculoskeletal: Arthralgia, back pain, leg cramps, dysarthria, myoclonus, arthrosis, myasthenia, bone neoplasm. GU: Urinary retention, urinary urgency, urine abnormality, urinary incontinence, kidney calculus, hematuria, impotence, prostate carcinoma kidney pain, metrorrhagia, priapism. Dermatologic: Pruritus, eczema, alopecia, exfoliative dermatitis, skin ulceration, urticaria, psoriasis, seborrhea, skin disorder, fungal dermatitis. Metabolic: Gout, respiratory acidosis, edema, thirst, hypokalemia, hyponatremia. Miscellaneous: Accidental or intentional injury, death diabetes mellitus, thyroid neoplasia, amblyopia, ophthalmitis.

Laboratory Test Alterations: Gamma glutamyl transferase, alkaline phosphatase, gamma globulins. Abnormal liver function tests, + direct Coombs' test.

Drug Interactions: Amitriptyline / Elimination of riluzole higher plasma levels Caffeine / Elimination of riluzole higher plasma levels Charcoal-broiled foods / Elimination of riluzole lower plasma levels Omeprazole / Elimination of riluzole lower plasma levels Quinolones / Elimination of riluzole higher plasma levels Rifampin / Elimination of riluzole lower plasma levels Smoking (cigarettes) / Elimination of riluzole lower plasma levels Theophyllines / Elimination of riluzole higher plasma levels

How Supplied: Tablets: 50 mg.

Dosage
•Tablets Treatment of ALS.
50 mg q 12 hr. Higher daily doses will not increase the beneficial effect but will increase the incidence of side effects.