Common Brand Name: Exelon
Capsules: 1.5 mg, 3 mg, 4.5 mg, 6 mg (as rivastigmine tartrate)
Solution: 2 mg/mL (as rivastigmine tartrate)
Transdermal Patch: 4.6 mg/24 hours, 9.5 mg/24 hours, 13.3 mg/24 hours (as rivastigmine base)
For the treatment of mild to moderate dementia of the Alzheimer’s type: Oral: Initiate treatment with 1.5 mg given twice a day. After 2 weeks, and if well tolerated, the dose may be increased to 3 mg twice a day. Subsequent increases to 4.5 mg or 6 mg twice a day may be made every 2 weeks, if tolerated. Oral solution and capsules may be interchanged in equal doses. Transdermal: Initiate treatment with 4.6 mg/hour patch applied to the skin once daily. After 4 weeks, and if well tolerated, the dose may be increased to the maximum daily dose of 13.3 mg/24 hours.
For the treatment of dementia associated with Parkinson’s Disease: Initiate treatment with 1.5 mg twice a day. After 4 weeks, and if well tolerated, the dose may be increased to 4.5 mg and 6 mg twice a day may be made every 4 weeks, if tolerated.
Monitor: LFT, RFT, Weight
Pharmacology/Pharmacokinetics:
Rivastigmine is a cholinergic agonist which increases acetylcholine through reversible inhibition to its hydrolysis by cholinesterase. After application of transdermal patches, peak plasma levels are reached in 8 hours with 1 hour lag times of absorption. Elimination half-life is 3 hours following patch removal. Metabolism occurs via hydrolysis by cholinesterase and excretion via the kidneys. Rivastigmine is loosely bound to plasma proteins (40%).
Drug Interactions:
Smoking increases rivastigmine clearance. May increase the effects of other cholinergic agonists and inhibit the actions of anticholinergics.
Contraindications/Precautions:
Contraindicated in patients allergic to any component of any formulation. Use a lower dose and caution in patients with renal or hepatic impairment. Use with caution in patients at risk for seizures and in patients with COPD. Use caution in patients with history of stomach ulcers. Use with caution in nursing mothers. Pregnancy Category B.
Adverse Effects:
The most common adverse effect (>10%) with the oral and transdermal dosage forms is nausea. Vomiting, diarrhea, anorexia, and weight loss are also common (5-10%). Less common effects are dizziness, anxiety, headache, depression, UTI, and fatigue (2-4%). The transdermal dosage form generally has fewer adverse effects than the oral form. Application site pruritus can occur with transdermal use (4%).
If therapy is interrupted for more than 3 days, restart treatment with the lowest dose. If interrupted for less than 3 days, continue the current treatment or decrease to the next lowest dose.
If a dose is missed, skip it and return to the normal dosing schedule. Do not double doses.
It is important to remove the old patch before applying the new patch. Serious adverse effects have occurred in patients who administered multiple patches.
Apply the patch to the upper back, chest, or upper arm.
Contact your prescriber if any of the above side effects are severe or persistent.