Rivastigmine

IUPAC: (S) - {3 - [ α - (dimethylamino) ethyl] phenyl} -N-ethyl -N- methylcarbamate

  • C14H22N2O2 ( rivastigmine )
  • C14H22N2O2 · C4H6O6 [ rivastigmine hydrogen tartrate · ]

N06DA03

  • Parasympathomimetic
  • Antidementia

123-125 ° C [ · rivastigmine hydrogen (2R, 3R) -tartrate ]

Viscose liquid at room temperature [ rivastigmine · base]

Template: Infobox chemical / molecular formula search available

Rivastigmine is used as a drug for the symptomatic treatment of mild to moderate Alzheimer 's disease and is the only anti-dementia drug, the addition is approved for the treatment of Parkinson's disease dementia. The drug is marketed by Novartis as a hard capsule, solution, and as a transdermal patch.

Pharmacological therapy, the active ingredient is in a group of cholinesterase inhibitors. Rivastigmine inhibits acetylcholinesterase and butyrylcholinesterase. The purpose of this inhibition is to reduce the occurring in Alzheimer's dementia lack of acetylcholine. By inhibiting degradative enzymes ( acetyl- and butyrylcholinesterase ) an extension of the degradation of acetylcholine is reached and the messenger is still available. For this reason, rivastigmine may affect occurring in Alzheimer 's disease cholinergic-mediated cognitive deficits and achieve an improvement in symptoms.

In studies, a small but significant effect of rivastigmine on cognitive function and quality of life showed. Side effects such as nausea, vomiting, diarrhea, anorexia, headache, and syncope, however, lead to high drop-out rates (9 % higher than placebo) treatment.

The pharmaceutical formulation as a patch (TTS ) is a constant release of the active ingredient and thus constant blood level is achieved. This allows for better compatibility than with tablets or solutions. The approval of the plaster cast is based on the IDEAL study ( Investigation of Transdermal Exelon in Alzheimer 's Disease ) with 195 patients. The results of this study showed that the daily application of a patch ( 9.5 mg / day) cognitive abilities and daily living just as much improved as the highest approved dose capsule (2x6 mg / day). Otherwise commonly observed adverse reactions such as nausea and vomiting occurred in the patch application to three times less than after taking the capsules. The frequency of side effects was not higher than among placebo - preparation without drug. There are also studies that show little effect of acetylcholinesterase inhibitors.

Trade names

Exelon (D, A, CH), Nimvastid (A), Prometax (D)

CAS registry number PubChem Anatomical Therapeutic Chemical Classification System DrugBank Cognition Digital Object Identifier PubMed Central
322618
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