Classifications: cholinesterase inhibitor; Therapeutic: antidementia; cholinesterase inhibitor
Prototype: Neostigmine bromide
Pregnancy Category: B
2 mg/mL oral solution; 1.5 mg, 3 mg, 4.5 mg, 6 mg capsule
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.
Inhibits acetylcholinesterase more specifically in the brain (hippocampus and cortex) than in the heart or skeletal muscle.
Treatment of mild to moderate dementia of the Alzheimer's type.
Hypersensitivity to rivastigmine or carbamate derivatives; lactation.
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
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 36 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)
- 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
, flu-like syndrome
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:
May exaggerate muscle relations with succinylcholine
and other neuromuscular blocking agents
, may attenuate effects of anticholinergic agents
Well absorbed, 40% reaches systemic circulation. Peak:
1 h. Duration:
10 h. Distribution:
Crosses bloodbrain barrier with CSF peak concentrations in 1.42.6 h, 40% protein bound. Metabolism:
By cholinesterase-mediated hydrolysis. Elimination:
In urine. Half-Life:
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.