Rivastigmine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Exelon, Nimvastid, Prometax, Rivastigmin; Belgium: Exelon; Bulgaria: Exelon, Nimvastid, Prometax, Rivastigmine; Cyprus: Exelon; Czech Republic: Evertas, Exelon, Ivagalmin, Nimvastid, Prometax, Ristidic, Rivastigmin, Vastigmex; Denmark: Exelon, Prometax; Estonia: Evertas, Exelon, Nimvastid, Prometax, Rivastigmine; Finland: Exelon; France: Exelon; Germany: Exelon, Nimvastid, Prometax, Rivastigmine; Greece: Exelon, Prometax; Hungary: Exelon, Prometax; Ireland: Exelon, Nimvastid, Prometax, Rivastigmine; Italy: Exelon, Prometax; Latvia: Evertas, Exelon, Nimvastid, Prometax, Rivastigmine; Lithuania: Evertas, Exelon, Nimvastid, Prometax, Rivastigmin, Rivastigmine; Luxembourg: Exelon, Prometax; Malta: Exelon, Nimvastid, Prometax, Rivastigmine; Netherlands: Exelon, Ivagalmin, Niddastig, Prometax, Ristidic, Rivastigmine, Rivaxon, Signelon; Poland: Evertas, Exelon, Nimvastid, Prometax, Rivastigmine; Portugal: Exelon, Nimvastid, Prometax, Rivastigmina; Romania: Evertas, Exelon, Niddastig, Nimvastid, Prometax, Ristidic, Rivastigmina, Rivastigmine; Slovakia: Evertas, Exelon, Nimvastid, Prometax, Rivastigmin, Rivastigmine; Slovenia: Exelon, Nimvastid, Prometax, Rivastigmine; Spain: Exelon, Prometax; Sweden: Exelon, Niddastig, Nimvastid, Prometax, Rivastigmin, Rivastigmine; UK: Exelon.

North America

Canada: Exelon, Rivastigmine; USA: Exelon.

Latin America

Argentina: Donadox, Exelon, Luneste, Remizeral, Rivasmina; Brazil: Exelon, Prometax; Mexico: Exelon.

Drug combinations

Chemistry

Rivastigmine: C~14~H~22~N~2~O~2~. Mw: 250.34. (1)(S)-3-[1-(Dimethylamino)ethyl]phenyl ethylmethylcarbamate; (2) m-[(S)-1-(Dimethylamino)ethyl]phenyl ethylmethylcarbamate. CAS-123441-03-2 (1997).

Pharmacologic Category

Parasympathomimetic (Cholinergic) Agents. Anti-Dementia Agents; Cholinesterase Inhibitors. (ATC-Code: N06DA03).

Mechanism of action

Increases acetylcholine in CNS through reversible inhibition of its hydrolysis by cholinesterase.

Therapeutic use

Treatment of mild-to-moderate dementia associated with Alzheimer’s disease or Parkinson’s disease.

Pregnancy and lactiation implications

Should be used only if benefit outweighs potential risk to fetus. Excretion in breast milk unknown (use with caution in nursing women).

Unlabeled use

Severe dementia associated with Alzheimer’s disease. Lewy body dementia.

Contraindications

Hypersensitivity to rivastigmine, other carbamate derivatives (e.g. neostigmine, pyridostigmine, physostigmine), or any component of the formulation.

Warnings and precautions

Significant anorexia and weight loss, nausea and/or vomiting associated with use (occurs more frequently in women and during titration phase). Cholinesterase inhibitors may have vagotonic effects which may cause bradycardia and/or heart block with or without history of cardiac disease (use with caution in sick-sinus syndrome, bradycardia, or conduction abnormalities). Use with caution in risk of ulcer disease (e.g. previous history of NSAID use). May increase gastric acid secretion. Use with caution in COPD and/or asthma, in history of seizure disorder, and in bladder outlet obstruction or prostatic hyperplasia. Cholinomimetics may cause or worsen outflow obstructions, including possible exacerbation of BPH symptoms. May exaggerate neuromuscular blockade effects of depolarizing neuromuscular-blocking agents (e.g. succinylcholine). Use caution due to increased risk of adverse reactions. Nicotine increases clearance of rivastigmine by 23%.

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