ALZHEIMERs DRUGS

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Preg Cat Generic Available? Comments

Aricept Donepezil Alzheimer's/Dementia  Mild-Mod: 5 mg once daily at bedtime; may increase to 10 mg orally once daily at 4 to 6 weeks  Mod-Severe: tabs: 5 mg once daily at bedtime; titrate dose to 10 mg orally once daily at 4 to 6 weeks; may increase to 20 mg orally once daily at 3 months  Mod-Severe: orally disintegrating tablets: 5 mg once daily at bedtime; titrate dose to 10 mg orally once daily at 4 to 6 weeks  Tablets 5, 10mg  Orally disintegrating tablets 5, 10 mg Centrally Acting Cholinesterase Inhibitor Alzheimer's disease Dementia (Mild-Severe) Hypersensitivity decreased efficacy of donepezil: oxybutynin increased ramelteon exposure: ramelteon increased donepezil bioavailability: ketoconazole, quinidine cholinergic adverse effects: bethanecol Reversible noncompetitive acetylcholinesterase inhibitor that acts centrally on the brain (cerebral cortex). Increases Ach allowing for neuronal stimulation. A: Bioavailability: 100% D: Vd: 12 L/kg; Protein binding: approximately 96% M: Hepatic; P450 CYP2D6 and CYP3A4; extensive metabolism, glucuronidation; Active metabolite: 6-O-desmethyl donepezil T : about 70 h Common: HA, HTN, N/V/D, Syncope, Wt decreased, Loss of appetite, Contusion, Ecchymosis, Cramp, Increased creatine kinase level, Asthenia, Dizziness, Insomnia, Somnolence, Depression, Dream disorder, Urinary incontinence, Fatigue Serious: AV block, Torsades de pointes, GI hemorrhage  improvement in signs and symptoms of Alzheimer-type dementia is indicative of efficacy  symptoms of active or occult gastrointestinal bleeding; particularly with history of ulcer disease or concomitant NSAID use  take in the evening prior to retiring  may be taken w/or w/o food  ODT: allow to dissolve on tongue and follow with a glass of water  may cause diarrhea, anorexia, nausea, vomiting, muscle cramps, insomnia, or fatigue C Yes Side notes: Switching between cholinesterase inhibitors should only be considered in patients who show lack of efficacy, tolerability, or have safety issues. A minimum treatment period of 6 months (beginning when the patient has reached optimal dose) should be allowed before any decision regarding the efficacy of treatment is made.

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Exelon Rivastigmine Alzheimer's/Dementia  Mild-Mod: 4.6 mg/24 hr patch once daily; after a minimum of 4 weeks and good tolerability, increase to 9.5 mg/24 hr patch once daily  switch from oral to patch: for total daily doses of less than 6 mg of oral switch to 4.6 mg/24 hr patch; for a total daily dose between 6 to 12 mg of oral switch to 9.5 mg/24 hr patch; apply the first patch on the day following the last oral dose Dosage Adj: low body weight (< 50 kg) Transdermal Patch, Extended Release: 4.6 MG/24 HR, 9.5 MG/24 HR Centrally Acting Cholinesterase Inhibitor  Alzheimer's disease - Dementia (Mild-Moderate)  Dementia (Mild-Moderate) - Parkinson's disease hypersensitivity to rivastigmine, other carbamate derivatives increased risk of EPS: metoclopramide decreased efficacy of Rivastigmine: tolterodine, oxybutynin intermediate-acting (10 hrs) reversible carbamate acetylcholinesterase inhibitor which interacts preferentially with acetylcholinesterase G1 (found in the brain, G4 is in the heart/skeletal muscle) D: Vd: 1.8 to 2.7 L/kg; Protein binding: 40% M: Hepatic: cholinesterase-mediated hydrolysis, extensive; CYP450 minimally involved in metabolism; Metabolite: NAP226-90 (decarbamylated metabolite) T : 3 hr Common: V/D/N: more with higher common dose  improvement in cognitive performance is indicative of efficacy  ability to continue driving or operating machinery; routinely evaluate  body weight  symptoms of active or occult GI bleeding; especially in patients with an increased risk of developing ulcers  apply to dry, hairless, intact healthy skin  preferred site of application is the upper back; optional sites are upper arm or chest  rotate the site of application daily to avoid irritation, although consecutive patches can be applied to the same anatomic site; the same site should not be used within 14 days  bathing and hot weather are acceptable when using the patch B No

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Razadyne galantamine Alzheimer's/Dementia  Mild-Mod: IR tablets and oral solution: 4 mg twice daily for a minimum of 4 weeks; 8 mg twice daily if previous dose tolerated; further increases to 12 mg twice daily can be attempted only after a minimum of 4 weeks at the previous dose  Mild-Mod: ER capsules: 8 mg/day once daily for a minimum of 4 weeks; 16 mg/day once daily for a minimum of 4 weeks, further increases to 24 mg/day may be attempted after a minimum of 4 weeks at the previous dose, max 24 mg/d Dosage Adj: renal impairment, hepatic impairment  Oral Capsule, ER: 8, 16, 24 MG  Oral Solution: 4 MG/ML  Oral Tablet: 4, 8, 12 MG Centrally/Peripherally Acting Cholinesterase Inhibitor Alzheimer's disease - Dementia (Mild-Mod) hypersensitivity decreased efficacy of galantamine: tolterodine, oxybutynin increased galantamine plasma [ ]: ketoconazole, quinidine, paroxetine, fluoxetine, amitriptyline, fluvoxamine A competitive and reversible inhibitor of acetylcholinesterase accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by cholinesterase A: IR about 1 hr; ER 4.5 to 5 hr D: Vd: 175 L; Protein binding: 18% M: Hepatic; P450 CYP2D6 and CYP3A4; Metabolites: norgalantamine, epigalanthamine, galanthaminone T : 7 hr Common: HA, Weight loss, Loss of appetite, Dizziness, N/V/D Serious: HF, Bradyarrhythmia, Esophageal perforation, GI hemorrhage Thrombocytopenia, Death  improvement in cognitive performance  hepatic and renal function  S/S of bradycardia or AV block  S/S of GI bleeding; especially with history of ulcer disease or concomitant NSAID use  ensure adequate fluid intake  ER: swallow whole, do not crush, break, or chew; take in morning preferably with food  tablets, oral solution: give preferably with morning and evening meals  may cause dizziness, weight loss, diarrhea, loss of appetite, nausea, vomiting, or headache  report S/S of bradycardia, especially if concurrently taking a drug that slows heart rate or if patient has a history of conduction disorders  report S/S of GI bleeding or ulcers, especially if concomitantly using NSAIDs or if patient has a history of ulcers B Yes

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Namenda Memantine Alzheimer's disease  Mod-Severe: IR 5 mg once daily; increase dose at minimum 1 wk intervals in 5 mg increments to 10 mg/day (5 mg twice daily), 15 mg/day (5 mg and 10 mg in separate doses), and 20 mg/day (10 mg twice daily); target dose is 20 mg/day; maintenance, 10 mg twice daily  Mod-Severe: ER 7 mg once daily; increase dose in 7-mg increments at least 1 wk between dose increase to a target dose of 28 mg once daily as tolerated; max 28 mg/day Dosage Adj: renal impairment  Oral Solution: 2 MG/ML  Oral Tablet: 5, 10 mg N-Methyl-D-Aspartate Receptor Antagonist Alzheimer's disease (Mod-Severe) hypersensitivity None Low to moderate affinity noncompetitive NMDA receptor antagonist which binds to NMDA receptor-operated cation channels. Also blocks the 5HT3 receptor and nicotinic acetylcholine receptors. However, has low to negligible affinity for GABA, benzodiazepine, dopamine, adrenergic, histamine, and glycine receptors and for voltage-dependent Ca, Na, or K channels. A: IR 3 to 7 hr; ER 9 to 12 hr D: Vd: 9 to 11 L/kg; Protein binding: 45% M: Liver: partial; no CYP450 involvement; N-glucuronide conjugate, 6-hydroxy memantine and 1-nitroso-deaminated memantine: minimally active T : 60 to 80 hr; Renal impairment, severe: increased by 95%; dosage should be reduced Common: HTN, HA, D/V, Hypotension, Syncope, Backache ,Confusion, Dizziness, Cough, Pain Serious: Stevens-Johnson syndrome, DVT, Hepatitis, Liver failure, Cerebral infarction, TIA, CVA, Grand mal seizure, acute renal failure, Intracranial hemorrhage, Seizure, Neuroleptic malignant syndrome  improvement in cognitive function and activities of daily living is indicative of clinical response  take with or without food  ER: do not chew, crush, or divide dose; may open capsule and sprinkle entire content on applesauce to be consumed  may cause dizziness, headache, confusion, diarrhea, constipation, or hypertension B No