RIVASTIGMINE TARTRATE
| RIVASTIGMINE TARTRATE (ri-vas'tig-meen) Exelon Classifications: cholinesterase inhibitor; Therapeutic: antidementia; cholinesterase inhibitor Prototype: Neostigmine bromide Pregnancy Category: B |
Availability
2 mg/mL oral solution; 1.5 mg, 3 mg, 4.5 mg, 6 mg capsule
Action
Inhibits acetylcholinesterase G1 form of this enzyme in the cerebral cortex and the hippocampus. The G1 form of acetylcholinesterase is found in higher levels in the brains of patients with Alzheimer's disease.
Therapeutic Effect
Inhibits acetylcholinesterase more specifically in the brain (hippocampus and cortex) than in the heart or skeletal muscle.
Uses
Treatment of mild to moderate dementia of the Alzheimer's type.
Contraindications
Hypersensitivity to rivastigmine or carbamate derivatives; lactation.
Cautious Use
History of toxicity to cholinesterase inhibitors (e.g., tacrine); diabetes mellitus, cardiovascular/pulmonary disease; GI disorders including intestinal obstruction/peptic ulcer disease; concurrent use of other cholinergic agents, or anticholinergic agents; urogenital tract obstruction; Parkinson's disease; history of seizures; pregnancy (category B); hepatic or renal insufficiency; concurrent use of NSAIDs.
Route & Dosage
| Alzheimer's Dementia Adult/Geriatric: PO Start with 1.5 mg b.i.d with food, may increase by 1.5 mg b.i.d. q2wk if tolerated, target dose 3–6 mg b.i.d. (max: 12 mg b.i.d.) (if discontinued for a few doses, restart at ≤ last dose; if treatment is interrupted for several days, reinitiate with 1.5 mg b.i.d. and titrate q2wk as above) |
Administration
Oral- Give both capsules and liquid with food.
- Give liquid form undiluted or mixed with water, juice, or soda (do not mix with other liquids). Stir completely to dissolve. Ensure that entire mixture is swallowed.
- Discontinue drug for several days if significant anorexia, nausea, or vomiting occur. When adverse effects subside, restart at same or lower dose level (see ROUTe & DOSAGE).
- Store capsules and oral solution below 25° C (77° F). Ensure that bottle of liquid is in an UPRIGHT position.
Adverse Effects (≥1%)
Body as a Whole: Asthenia, increased sweating, syncope, fatigue, malaise, flu-like syndrome. CV: Hypertension. GI: Nausea, vomiting, anorexia, dyspepsia, diarrhea, abdominal pain, constipation, flatulence, eructation. Metabolic: Weight loss. CNS: Dizziness, headache, somnolence, tremor, insomnia, confusion, depression, anxiety, hallucination, aggressive reaction. Respiratory: Rhinitis.Interactions
Drug: May exaggerate muscle relations with succinylcholine and other neuromuscular blocking agents, may attenuate effects of anticholinergic agents.Pharmacokinetics
Absorption: Well absorbed, 40% reaches systemic circulation. Peak: 1 h. Duration: 10 h. Distribution: Crosses blood–brain barrier with CSF peak concentrations in 1.4–2.6 h, 40% protein bound. Metabolism: By cholinesterase-mediated hydrolysis. Elimination: In urine. Half-Life: 1.5 h.Nursing Implications
Assessment & Drug Effects
- Monitor cognitive function and ability to perform ADLs.
- Monitor for and report S&S of GI distress: Anorexia, weight loss, nausea and vomiting.
- Lab tests: Periodic ECG, serum electrolytes, Hgb & Hct, urinalysis, blood glucose HbA1C, especially with long-term therapy.
- Monitor ambulation as dizziness is a common adverse effect.
- Monitor diabetics for loss of glycemic control.
Patient & Family Education
- Review instruction sheet provided with liquid form of the drug.
- Monitor weight at least weekly.
- Report any of the following to the physician: Loss of appetite, weight loss, significant nausea and/or vomiting.
- Supervise activity since there is a high potential for dizziness.
Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; 
Canadian drug name; 
Prototype drug