Names and pronunciation
(riv-as-tig′mine) Exelon, Exelon Patch
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Drug reference
(riv-as-tig′mine) Exelon, Exelon Patch
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Func. class.: Anti-Alzheimer agent
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Chem. class.: Cholinesterase inhibitor
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ACTION: Potent, selective inhibitor of brain acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)
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USES: Mild to severe Alzheimer’s dementia, mild to moderate Parkinson’s disease dementia (PDD)
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Unlabeled uses: Vascular dementia, dementia with Lewy bodies, Pick’s disease
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CONTRAINDICATIONS: Hyper- sensitivity to this product, other carba- mates Precautions: Pregnancy, breastfeeding, children, respiratory/cardiac/renal/hepatic disease, seizure disorder, peptic ulcer, uri- nary obstruction, asthma, increased intra- cranial pressure, surgery, GI bleeding, jaundice
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SIDE EFFECTS CV: QT prolongation, AV block, cardiac arrest, angina, MI, palpitations, brady- cardia CNS: Tremors, confusion, insomnia, psychosis, hallucination, depression, diz- ziness, headache, anxiety, somnolence, fatigue, syncope, EPS, exacerbation of Parkinson’s disease GI: Nausea, vomiting, anorexia, abdominal distress, flatulence, diar- rhea, constipation, dyspepsia, colitis, eructation, fecal incontinence, GI bleed- ing/obstruction, GERD, gastritis, pancre- atitis MISC: Urinary tract infection, asthenia, increased sweating, hypertension, flulike symptoms, weight change
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INTERACTIONS Increase: synergistic effect—cholinergic agonists, other cholinesterase inhibitors Increase: metabolism—nicotine Increase: GI effects—NSAIDs Decrease: rivastigmine effect—anticho- linergics, sedating H1 blockers, tricyclics, phenothiazines
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DOSAGE AND ROUTES Dementia of Alzheimer's type • Adult: PO 1.5 mg bid with food; after ≥4 wk, may increase to 3 mg bid; may increase to 4.5 mg bid and thereafter 6 mg bid, max 12 mg/day; TRANSDER- MAL apply 4.6 mg/24 hr/day, after ≥4 wk may increase to 9.5 mg/24 hr/day; max 13.3 mg/24 hr Parkinson's disease dementia • Adult: PO 1.5 mg bid, after 4 wk may increase to 3 mg bid; TD 4.6 mg/24-hr patch daily, after 4 wk, may increase to 9.5 mg/ 24 hr
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Available forms: Caps 1.5, 3, 4.5, 6 mg; transdermal patch 4.6, 9.5, 13.3 mg/24 hr
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Administer: • With meals; take with morning and evening meal even though absorption may be decreased • If adverse reactions cause intoler- ance, discontinue treatment for several doses; restart at same or next lower dosage level • If treatment is interrupted for more than several days, treatment should be initiated with lowest daily dose and ti- trated as indicated previously Transdermal route • Once a day to hairless, clean, dry skin, not in an area that clothing will rub; ro- tate sites daily; do not apply to same site more than once q14days; remove liner; apply firmly; may be used during bathing, swimming; avoid excess sunlight or ex- ternal heat such as saunas; each 5-cm2 patch contains 9 mg base, rate of 4.6 mg/24 hr, each 10-cm2 patch 18 mg base, rate of 9.5 mg/24 hr
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Assess: • Hepatic studies: AST, ALT, alk phos, LDH, bilirubin, CBC • Severe GI effects: nausea, vomiting, anorexia, weight loss, diarrhea, GI bleeding • CV status: B/P, heart rate, respiration during initial treatment; hypo/hyperten- sion should be reported • Cognitive/mental status: affect, mood, behavioral changes, depression, insom- nia; complete suicide assessment • Gout/mobility: Assistance with ambu- lation during beginning therapy; dizzi- ness may occur • Skin: assess for hypersensitivity-re- lated dermatitis • TD: overdoses have occurred and may be fatal • Beers: avoid use in older adults; in- creased risk of orthostatic hypotension or bradycardia • Pregnancy/breastfeeding: use only if clearly needed; do not breastfeed, excre- tion unknown
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Evaluate: • Therapeutic response: improved mood/cognition
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • How to apply transdermal product, to fold in half and throw away, not to get in eyes, to wash hands after application; not to use heating pad, sauna, tanning bed • To notify prescriber of severe GI effects • That product may cause dizziness, an- orexia, weight loss • That effect may take weeks or months; not to discontinue abruptly • To notify prescriber if pregnancy is planned or suspected • To give with food in AM, PM if using oral tablet • To notify prescriber of history of low heart rate, sick sinus syndrome, risk of bradycardia • How to take B/P, pulse at home • To report nausea, vomiting, diarrhea • To inform prescriber of all products taken
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PHARMACOKINETICS Rapidly and completely absorbed; peak 1 hr, metabolized to decarbamylated metab- olite; half-life 1.5 hr; excreted via kidneys (metabolites); clearance lowered in geriat- ric patients, hepatic disease and increased with nicotine use; 40% protein binding
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• Adult: PO 1.5 mg bid with food; after ≥4 wk, may increase to 3 mg bid; may increase to 4.5 mg bid and thereafter 6 mg bid, max 12 mg/day; TRANSDER- MAL apply 4.6 mg/24 hr/day, after ≥4 wk may increase to 9.5 mg/24 hr/day; max 13.3 mg/24 hr Parkinson's disease dementia
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• Adult: PO 1.5 mg bid, after 4 wk may increase to 3 mg bid; TD 4.6 mg/24-hr patch daily, after 4 wk, may increase to 9.5 mg/ 24 hr
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