Names and pronunciation
(toll′cah′pone) Tasmar
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Drug reference
(toll′cah′pone) Tasmar
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Func. class.: Antiparkinson agent
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Chem. class.: COMT inhibitor
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ACTION: Inhibits COMT; used as adjunct to levodopa/carbidopa therapy
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USES: Parkinson’s disease
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CONTRAINDICATIONS: Hyper- sensitivity, rhabdomyolysis Precautions: Pregnancy, breastfeeding, cardiac/renal disease, hypertension, asthma, history of rhabdomyolysis
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Black Box Warning: Hepatic disease Black Box Warning: Hepatic disease: AST, ALT, alk phos, LDH, bilirubin, CBC; monitor ALT, AST q2wk × 1 yr, then q4wk × 6 mo, then q8wk thereafter; if LFTs el- evated, product should not be used, if no improvement in 3 wk, discontinue; do not use in hepatic disease • Involuntary movements of parkinson- ism: akinesia, tremors, staggering gait, muscle rigidity, drooling • B/P, respiration during initial treat- ment; hypo/hypertension should be re- ported • Mental status: affect, mood, behavioral changes, avoid use in those with dystonia Black Box Warning: To report signs of hepatic injury: clay-colored stools, jaun- dice, fatigue, appetite loss, lethargy, fa- tigue, itching, right upper abdominal pain • To report diarrhea, nausea, vomiting, anorexia; that nausea may occur at be- ginning of treatment See Appendix B
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SIDE EFFECTS CNS: Dystonia, dyskinesia, dreaming, fatigue, headache, confusion, psycho- sis, hallucination, dizziness, sleep disorders CV: Orthostatic hypotension, chest pain, hypotension EENT: Cataract, eye inflammation GI: Nausea, vomiting, anorexia, abdom- inal distress, diarrhea, constipation, fatal hepatic failure, increased LFTs GU: UTI, urine discoloration, uterine tumor, micturition disorder, hematuria HEMA: Hemolytic anemia, leukopenia, agranulocytosis INTEG: Sweating, alopecia MS: Rhabdomyolysis
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INTERACTIONS Increase: CNS depression—CNS depressant • May influence pharmacokinetics of α- methyldopa, DOBUTamine, apomorphine, isoproterenol • Inhibition of normal catecholamine metabolism: MAOIs; MAO-B inhibitor may be used
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DOSAGE AND ROUTES • Adult: PO 100-200 mg tid with le- vodopa/carbidopa therapy; max 600 mg/day, discontinue if no benefit after 3 wk
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Available forms: Tabs 100, 200 mg
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Administer: • Only to be used if levodopa/carbidopa does not provide satisfactory results • Give without regard to food
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Assess:
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Evaluate: • Therapeutic response: decrease in akathisia, increased mood
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To change positions slowly to prevent orthostatic hypotension • That urine, sweat may change color • That food taken within 1 hr before meals or 2 hr after meals decreases ac- tion of product by 20%; may be taken without regard to food • To notify prescriber if pregnancy is planned or suspected • That CNS changes may occur, halluci- nations, involuntary movement • To avoid hazardous activities until re- action is known; dizziness may occur • To notify prescriber of poor impulse control, urges to gamble, spend money (rare)
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PHARMACOKINETICS Rapidly absorbed, peak 2 hr, protein binding 99%, extensively metabolized, half-life 2-3 hr, excreted in urine (60%)/ feces (40%)
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• Adult: PO 100-200 mg tid with le- vodopa/carbidopa therapy; max 600 mg/day, discontinue if no benefit after 3 wk
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