Rivastigmine
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| Clinical data | |
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| Trade names | Exelon |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a602009 |
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Oral, transdermal patch |
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| Pharmacokinetic data | |
| Bioavailability | 60 to 72% |
| Protein binding | 40% |
| Metabolism | Hepatic, via pseudocholinesterase |
| Biological half-life | 1.5 hours |
| Excretion | Renal, 97% |
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| ECHA InfoCard | 100.120.679 |
| Chemical and physical data | |
| Formula | C14H22N2O2 |
| Molar mass | 250.337 g/mol |
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Rivastigmine (sold under the trade name Exelon) is a parasympathomimetic or cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease. The drug can be administered orally or via a transdermal patch; the latter form reduces the prevalence of side effects, which typically include nausea and vomiting.
The drug is eliminated through the urine, and appears to have relatively few drug-drug interactions.
Rivastigmine capsules, liquid solution and patches are used for the treatment of mild to moderate dementia of the Alzheimer's type and for mild to moderate dementia related to Parkinson's disease.
Rivastigmine has demonstrated treatment effects on the cognitive (thinking and memory), functional (activities of daily living) and behavioural problems commonly associated with Alzheimer's and Parkinson's disease dementias.
In people with either type of dementia, rivastigmine has been shown to provide meaningful symptomatic effects that may allow patients to remain independent and ‘be themselves’ for longer. In particular, it appears to show marked treatment effects in patients showing a more aggressive course of disease, such as those with younger onset ages, poor nutritional status, or those experiencing symptoms such as delusions or hallucinations. For example, the presence of hallucinations appears to be a predictor of especially strong responses to rivastigmine, both in Alzheimer's and Parkinson's patients. These effects might reflect the additional inhibition of butyrylcholinesterase, which is implicated in symptom progression and might provide added benefits over acetylcholinesterase-selective drugs in some patients. Multiple-infarct dementia patients may show slight improvement in executive functions and behaviour. No firm evidence supports usage in schizophrenia patients.
Its efficacy is similar to donepezil and tacrine. Doses below 6 mg/d may be ineffective. The effects of this kind of drug in different kinds of dementia (including Alzheimer's dementia) are modest, and it is still unclear which AcCh(ButCh) esterase inhibitor is better in Parkinson's dementia, though rivastigmine is well-studied.
Side effects may include nausea and vomiting, decreased appetite and weight loss.
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