Rivastigmine

What it is and how it works

Mechanism of Action Although the precise mechanism of action of rivastigmine is unknown, it is thought to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by cholinesterase. The effect of rivastigmine may lessen as the disease process advances and fewer cholinergic neurons remain functionally intact. There is no evidence that rivastigmine alters the course of the underlying dementing process.

Mechanism class: Cholinesterase Inhibitors

Indications

Rivastigmine Transdermal System is an acetylcholinesterase inhibitor indicated for treatment of: Mild, moderate, and severe dementia of the Alzheimer's type (AD) Mild-to-moderate dementia associated with Parkinson's disease (PD) Alzheimer's Disease Rivastigmine Transdermal System is indicated for the treatment of dementia of the Alzheimer's type (AD). Efficacy has been demonstrated in patients with mild, moderate, and severe Alzheimer's disease. Parkinson's Disease Dementia Rivastigmine Transdermal System is indicated for the treatment of mild-to-moderate dementia associated with Parkinson's disease (PDD).

Dosage and administration (summary)

Apply patch on intact skin for a 24-hour period; replace with a new patch every 24 hours. ( 2.1 , 2.4 ) Initial Dose : Initiate treatment with 4.6 mg/24 hours Rivastigmine Transdermal System. Dose Titration : After a minimum of 4 weeks, if tolerated, increase dose to 9.5 mg/24 hours, which is the minimum effective dose. Following a minimum additional 4 weeks, may increase dosage to maximum dosage of 13.3 mg/24 hours. Mild-to-Moderate Alzheimer's Disease and Parkinson's Disease Dementia : Rivastigmine Transdermal System 9.5 mg/24 hours or 13.3 mg/24 hours once daily. Severe Alzheimer's Disease : Rivastigmine Transdermal System 13.3 mg/24 hours once daily.

Contraindications

Rivastigmine Transdermal System is contraindicated in patients with: known hypersensitivity to rivastigmine, other carbamate derivatives, or other components of the formulation . previous history of application site reactions with rivastigmine transdermal patch suggestive of allergic contact dermatitis . Isolated cases of generalized skin reactions have been described in postmarketing experience .

Warnings and precautions

Hospitalization and, rarely, death have been reported due to application of multiple patches at same time. Ensure patients or caregivers receive instruction on proper dosing and administration. Gastrointestinal Adverse Reactions : May include significant nausea, vomiting, diarrhea, anorexia/decreased appetite, and weight loss, and may necessitate treatment interruption. Dehydration may result from prolonged vomiting or diarrhea and can be associated with serious outcomes. Application site reactions may occur with the patch form of rivastigmine.

Pregnancy

Pregnancy Risk Summary There are no adequate data on the developmental risks associated with the use of Rivastigmine Transdermal System in pregnant women. In animals, no adverse effects on embryo-fetal development were observed at oral doses 2-4 times the maximum recommended human dose (MRHD) (see Data ) .

Storage and supply

Rivastigmine Transdermal System: 9.5 mg/24 hours Each patch of 10 cm2 contains 18 mg rivastigmine base with in vivo release rate of 9.5 mg/24 hours. NDC 72162-1609-3: Carton of 30 Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) . Keep Rivastigmine Transdermal System in the individual sealed pouch until use.

Source: Rivastigmine (Rivastigmine Transdermal System) — US FDA prescribing information, 2024-12-24, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.