Exelon (rivastigmine)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Rivastigmine is a centrally active, reversible cholinesterase inhibitor.
Rivastigmine tartrate, a carbamate derivative, is an intermediate-acting, reversible cholinesterase inhibitor that is structurally related to physostigmine but unrelated to donepezil or tacrine. The precise mechanism(s) of action of rivastigmine in patients with dementia of the Alzheimer's type (Alzheimer's disease) and dementia associated with Parkinson's disease has not been fully elucidated. The drug is an anticholinesterase agent that binds reversibly with and inactivates cholinesterases (e.g., acetylcholinesterase, butyrylcholinesterase), thus inhibiting hydrolysis of acetylcholine and increasing the concentration of acetylcholine at cholinergic synapses.
The anticholinesterase activity of rivastigmine is relatively specific for brain acetylcholinesterase and butyrylcholinesterase compared with that in peripheral tissues. After a 6-mg oral dose administered twice daily, cholinesterase activity in CSF is inhibited for approximately 10 hours, with a maximum inhibition of about 60% at 5 hours after dosing.
A deficiency of acetylcholine caused by selective loss of cholinergic neurons in the cerebral cortex, nucleus basalis, and hippocampus is a pathologic feature of Alzheimer's disease associated with cognitive deficits. The deficiency of cholinergic transmission has been associated with the accumulation of beta-amyloid peptide and neurofibrillary tangles that is characteristic of Alzheimer's disease. Because synaptic loss has been shown to correlate with cognitive decline in Alzheimer's disease, enhancement of cholinergic function with an anticholinesterase agent such as rivastigmine is one of the pharmacologic approaches to treatment.
However, the potential benefits of anticholinesterase agents may theoretically diminish as the disease process advances and fewer cholinergic neurons remain functioning.
Metabolism of rivastigmine is rapid and extensive and occurs principally via cholinesterase-mediated hydrolysis to the decarbamylated metabolite, which is tenfold less active than rivastigmine. The drug is only minimally metabolized by cytochrome P-450 (CYP) isoenzymes.
USES: Rivastigmine is used to treat confusion (dementia) related to Alzheimer's disease and to Parkinson's disease. Rivastigmine does not cure either of these diseases, but it may improve memory, awareness, and the ability to perform daily functions. This medication works by restoring the balance of natural substances (neurotransmitters) in the brain.
Generic name: rivastigmine
Pronunciation: (riv-uh-STIG-meen)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Exelon
Indications
The following indications are listed for Exelon:
- Dementia Associated With Parkinson's Disease
- Mild To Moderate Alzheimer's Type Dementia
- Moderate To Severe Alzheimer's Type Dementia
Dosing
Dosage of rivastigmine tartrate is expressed in terms of rivastigmine.
Rivastigmine is administered orally (as capsules or oral solution) twice daily. The drug also is available as a transdermal system for topical application.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Known hypersensitivity to rivastigmine or any ingredient in the formulation. Although there are no reports of cross-sensitivity to date, the manufacturer states that the drug also is contraindicated in patients with known hypersensitivity to other carbamates.
History of previous application site reactions with rivastigmine transdermal system suggestive of allergic contact dermatitis, in the absence of negative allergy testing.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
In clinical trials of oral rivastigmine in patients with dementia of the Alzheimer's type, adverse effects occurring in 5% or more of patients receiving rivastigmine and more than twice as frequently as among those receiving placebo included nausea, vomiting, anorexia, dyspepsia, and asthenia. Dizziness, diarrhea, headache, abdominal pain, accidental trauma, fatigue, insomnia, confusion, urinary tract infection, depression, malaise, somnolence, constipation, and anxiety occurred in at least 5% of patients receiving rivastigmine and more frequently than in patients receiving placebo in clinical studies in patients with dementia of the Alzheimer's type.
In clinical trials of oral rivastigmine in patients with dementia associated with Parkinson's disease, adverse effects occurring in 5% or more of patients receiving rivastigmine and more than twice as frequently as among those receiving placebo included nausea, vomiting, tremor, anorexia, and dizziness.
In a clinical trial that evaluated rivastigmine transdermal therapy in patients with dementia of the Alzheimer's type, nausea, vomiting, and diarrhea occurred in at least 5% of patients receiving rivastigmine (one system delivering 9.5 mg/24 hours) and more frequently than in patients receiving placebo. Most patients experienced no, slight, or mild skin irritation.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of rivastigmine in pediatric patients have not been established. The drug is not recommended for pediatric use.
There are no adequate data on the developmental risks associated with the use of rivastigmine in pregnant women. In animal reproduction studies, no adverse embryofetal effects were observed with oral dose exposures of 2-4 times the maximum recommended human dose.
It is not known whether rivastigmine is distributed into milk or if the drug has any effects on nursing infants or on milk production. The known benefits of breast-feeding should be considered along with the mother's clinical need for rivastigmine and any potential adverse effects on the breast-fed infant from the drug or the underlying maternal condition.
No overall differences in safety and efficacy have been observed between geriatric patients and younger adults in clinical studies of rivastigmine and in other reported clinical experiences; however, the possibility of increased sensitivity to rivastigmine in some geriatric patients cannot be ruled out.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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