Bioavailability file: Rivastigmine tartrate


Mutlu N. B. , Deǧim Z.

Fabad Journal of Pharmaceutical Sciences, vol.30, no.3, pp.150-157, 2005 (Scopus) identifier

  • Publication Type: Article / Review
  • Volume: 30 Issue: 3
  • Publication Date: 2005
  • Journal Name: Fabad Journal of Pharmaceutical Sciences
  • Journal Indexes: Scopus
  • Page Numbers: pp.150-157
  • Gazi University Affiliated: Yes

Abstract

Rivastigmine tartrate is a carbamate derivative drug used for treatment of mild to moderate Alzheimer's disease. It is used for increasing cognitive performance aiming to continue the patient's daily life. The mean plasma elimination half-life of rivastigmine is 1.5-2 hours, which is shorter than that of other carbamate derivative drugs. Rivastigmine especially prevents decreases in the amount of acetylcholine and butyrylcholine by inhibiting acetylcholine esterase and butyrylcholine esterase. It binds the esteratic site of the enzymes and dissociation occurs after an extended time period. Thus, rivastigmine is effective for a long period although it has a short plasma elimination half-life. Rivastigmine's extended inhibition of both acetylcholine esterase and butyrylcholine esterase is one of its advantages. Rivastigmine is distributed throughout the body, penetrates the blood-brain barrier and also reaches the cerebrospinal fluid. It is metabolized by hydrolyzing with esterases enzymes. It is eliminated in the urine as its conjugates and metabolites. Rivastigmine can be applied orally and intravenously. Commercial products of rivastigmine are solution and capsule dosage forms. In this review, the physicochemical, pharmacological, and pharmacokinetic properties and bioavailability of rivastigmine are discussed.