Rivastigmine (Transdermal)

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Rivastigmine Transdermal (Exelon Patch) belongs to a class of substances called cholinesterase inhibitors.

In patients with Alzheimer’s dementia, certain nerve cells die in the brain, resulting in low levels of the neurotransmitter acetylcholine (a substance that allows nerve cells to communicate with each other).

Rivastigmine works by blocking the enzymes that break down acetylcholine: acetylcholinesterase and butyrylcholinesterase. By blocking these enzymes, Rivastigmine allows levels of acetylcholine to be increased in the brain, helping to reduce the symptoms of Alzheimer’s disease.

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[edit] STRUCTURE

Rivastigmine.jpg

[edit] MECHANISM OF ACTION

Rivastigmine exert its therapeutic effect by enhancing cholinergic function. This is accomplished by inhibiting both butyrylcholinesterase and acetylcholinesterase (unlike donepezil, which selectively inhibits acetylcholinesterase) thus increasing the concentration of acetylcholine in the brain. 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.

[edit] INDICATIONS

  • Mild, moderate, and severe dementia of the Alzheimer’s type
  • Mild to moderate dementia associated with Parkinson’s disease

[edit] DOSAGE

Apply patch on intact skin for a 24-hour period; replace with a new patch every 24 hours

  • Initiate treatment with 4.6 mg/24 hours Rivastigmine (transdermal system)
  • 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
  • For treatment interruption longer than 3 days, retitrate dosage starting at 4.6 mg/24 hours
  • Consider dose adjustments in patients with:
    • Mild to moderate hepatic impairment
    • Low (<50 kg) body weight

[edit] CONTRAINDICATIONS

Patients with known hypersensitivity to rivastigmine, other carbamate derivatives, or other components of the formulation or previous history of application site reactions with rivastigmine transdermal patch suggestive of allergic contact dermatitis

[edit] WARNINGS AND PRECAUTIONS

  • Overdose from medication errors: 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.
  • Skin reactions: Application site reactions may occur with the patch form of rivastigmine. Discontinue treatment if application site reactions spread beyond the patch size, if there is evidence of a more intense local reaction (e.g., increasing erythema, edema, papules, vesicles), and if symptoms do not significantly improve within 48 hours after patch removal.

[edit] INTERACTIONS

Cholinomimetic and anticholinergic drugs: Avoid concomitant use unless clinically necessary

[edit] PREGNANCY AND LACTATION

  • Nursing Mothers: Rivastigmine and its metabolites are excreted in rat milk following oral administration of rivastigmine; levels of rivastigmine plus metabolites in rat milk are approximately 2 times that in maternal plasma. It is not known whether rivastigmine is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from rivastigmine tartrate, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

[edit] SIDE EFFECTS

Most commonly observed adverse reactions (>5% and higher than with placebo): Nausea, vomiting, and diarrhea

[edit] RELATED LINKS

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[edit] REFERENCES

Alzheimer/Dementia
Anticholinesterases Donepezil (Aricept, Memac)   Galantamine (Reminyl)   Rivastigmine (Oral) (Exelon)   Rivastigmine (Transdermal) (Exelon Patch)
Glutamatergic NMDA receptor antagonists Memantine (Ebixa)
Psychostimulants and nootropics Aniracetam   Choline   Citicoline   Ginkgo biloba   Piracetam