Rivastigmine (Oral)

From Drugs Prescribing Information
Jump to: navigation, search

Rivastigmine belongs to a class of substances called cholinesterase inhibitors.

Rivastigmine is used for the treatment of memory disorders in patients with Alzheimer’s disease. It is also used for the treatment of dementia in patients with Parkinson’s disease.

Contents

[edit] BRAND NAMES

[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 to moderate dementia of the Alzheimer’s type
  • Mild to moderate dementia associated with Parkinson’s disease

[edit] DOSAGE

Alzheimer’s Disease

  • Initiate treatment with 1.5 mg twice a day
  • After a minimum of 2 weeks, if tolerated, increase dose to 3 mg twice a day and further to 4.5 mg twice a day and 6 mg twice a day if tolerated with a minimum of 2 weeks at each dose

Parkinson’s Disease Dementia

  • Initiate treatment with 1.5 mg twice a day
  • After a minimum of 4 weeks, if tolerated, increase dose to 3 mg twice a day and further to 4.5 mg twice a day and 6 mg twice a day if tolerated with a minimum of 4 weeks at each dose

Rivastigmine tartrate should be taken with meals in divided doses in the morning and evening.

[edit] CONTRAINDICATIONS

  • Known hypersensitivity to rivastigmine, other carbamate derivatives or other components of the formulation.
  • History of application site reaction with rivastigmine transdermal patch suggestive of allergic contact dermatitis, in the absence of negative allergy testing

[edit] WARNINGS AND PRECAUTIONS

  • 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.
  • Hypersensitivity reactions of the skin: Discontinue rivastigmine in case of disseminated hypersensitivity reaction of the skin, which may occur after oral or transdermal administration. In patients with suspected allergic contact dermatitis after transdermal rivastigmine use, switch to oral rivastigmine only after negative allergy testing.

[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 2 times greater than placebo): nausea, vomiting, anorexia, dyspepsia, and asthenia.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[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