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Rivastigmine (Exelon)

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.

Administered orally or via a transdermal patch.

Associated with nausea and vomiting.

Eliminated via the kidney.

As a cholinesterase inhibitor, it requires doses to be increased gradually over several weeks.

The titration phase doses of rivastigmine are titrated with a 3 mg per day increment every 2 to 4 weeks.

Atropine is used to reverse bradycardia.

Rivastigmine is a cholinesterase inhibitor that inhibits both butyrylcholinesterase and acetylcholinesterase, enzymes, which would otherwise break down the brain chemical acetylcholine.

Significant treatment effects on the cognitive, functional and behavioural problems that are commonly associated with Alzheimer’s and Parkinson’s disease dementias.

Shown to provide meaningful symptomatic effects that may allow patients to remain independent for longer.

Shows marked treatment effects in patients showing a more aggressive course of disease, such as those with a younger age of onset, a poor nutritional status, or those experiencing symptoms such as delusions or hallucinations.

Presence of hallucinations appears to be a predictor of efficacious responses to rivastigmine, both in Alzheimer’s and Parkinson’s disease patients.

Use may provide some improvement in executive functions and behaviour.

Side effects include nausea and vomiting.

Rates of nausea and vomiting are markedly reduced with the once-daily rivastigmine patch.

Rivastigmine patch has target dose of 9.5 mg/24 hour provides similar clinical effects as the highest doses of rivastigmine capsules, but with three times fewer reports of nausea and vomiting.

Orally is well absorbed with a bioavailability of about 40% in the 3 mg dose.

Pharmacokinetics are linear up to 3 mg BID but non-linear at higher doses.

Elimination is through the urine, and plasma binding is 40%.

Oral administratio associated with peak plasma concentrations in about one hour, with peak CSF concentrations at 1.4–3.8 hours.

Transdermal patch pharmacokinetics associated with lower peak plasma concentrations and reduced fluctuations, with the 9.5 mg/24 h rivastigmine patch providing comparable exposure to 12 mg/day capsules.

The drug does cross the blood-brain barrier.

Major route of metabolism is by its target enzymes via cholinesterase-mediated hydrolysis.

Low potential for drug-drug interactions.

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