Exelon
Exelon - General Information
Exelon is a parasympathomimetic or cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer s type. Exelon is a cholinesterase inhibitor that inhibits both butyrylcholinesterase and acetylcholinesterase.
Pharmacology of Exelon
Exelon is a parasympathomimetic and a reversible cholinesterase inhibitor. Exelon is indicated for the treatment of mild to moderate dementia of the Alzheimer's type. Pathological changes in Dementia of the Alzheimer type involve cholinergic neuronal pathways that project from the basal forebrain to the cerebral cortex and hippocampus. These pathways are thought to be intricately involved in memory, attention, learning, and other cognitive processes. While the precise mechanism of rivastigmine's action is unknown, it is postulated to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by cholinesterase. If this proposed mechanism is correct, rivastigmine's effect may lessen as the disease process advances and fewer cholinergic neurons remain functionally intact.
Exelon for patients
Caregivers should be advised of the high incidence of nausea and vomiting associated with the use of the drug along with the possibility of anorexia and weight loss. Caregivers should be encouraged to monitor for these adverse events and inform the physician if they occur. It is critical to inform caregivers that if therapy has been interrupted for more than several days, the next dose should not be administered until they have discussed this with the physician.
Exelon Interactions
Drug-Drug Interactions
Effect of Exelon (rivastigmine tartrate) on the Metabolism of Other Drugs: Rivastigmine is primarily metabolized through hydrolysis by esterases. Minimal metabolism occurs via the major cytochrome P450 isoenzymes. Based on in vitro studies, no pharmacokinetic drug interactions with drugs metabolized by the following isoenzyme systems are expected: CYP1A2, CYP2D6, CYP3A4/5, CYP2E1, CYP2C9, CYP2C8, or CYP2C19. No pharmacokinetic interaction was observed between rivastigmine and digoxin, warfarin, diazepam, or fluoxetine in studies in healthy volunteers. The elevation of prothrombin time induced by warfarin is not affected by administration of Exelon.
Effect of Other Drugs on the Metabolism of Exelon: Drugs that induce or inhibit CYP450 metabolism are not expected to alter the metabolism of rivastigmine. Single dose pharmacokinetic studies demonstrated that the metabolism of rivastigmine is not significantly affected by concurrent administration of digoxin, warfarin, diazepam, or fluoxetine. Population PK analysis with a database of 625 patients showed that the pharmacokinetics of rivastigmine were not influenced by commonly prescribed medications such as antacids (n=77), antihypertensives (n=72), β-blockers (n=42), calcium channel blockers (n=75), antidiabetics (n=21), nonsteroidal anti-inflammatory drugs (n=79), estrogens (n=70), salicylate analgesics (n=177), antianginals (n=35), and antihistamines (n=15).
Use with Anticholinergics: Because of their mechanism of action, cholinesterase inhibitors have the potential to interfere with the activity of anticholinergic medications.
Use with Cholinomimetics and Other Cholinesterase Inhibitors: A synergistic effect may be expected when cholinesterase inhibitors are given concurrently with succinylcholine, similar neuromuscular blocking agents or cholinergic agonists such as bethanechol.
Exelon Contraindications
Exelon (rivastigmine tartrate) is contraindicated in patients with known hypersensitivity to rivastigmine, other carbamate derivatives or other components of the formulation.
Additional information about Exelon
Exelon Indication: For the treatment of mild to moderate Alzheimer's disease.
Mechanism Of Action: Exelon increases the concentration of acetylcholine through reversible inhibition of its hydrolysis by cholinesterase. This acts to enhance cholinergic function.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Rivastigmine
Synonyms: Ena 713 Free Base; Rivastigmine Hydrogen Tartrate
Drug Category: Nootropic Agents; Cholinergic Agents; Parasympathomimetics
Drug Type: Small Molecule; Approved
Other Brand Names containing Rivastigmine: Exelon;
Absorption: Not Available
Toxicity (Overdose): Not Available
Protein Binding: 40%
Biotransformation: Rivastigmine is rapidly metabolized by cholinesterase-mediated hydrolysis.
Half Life: 1.5 hours
Dosage Forms of Exelon: Solution Oral
Capsule Oral
Chemical IUPAC Name: [3-[(1S)-1-dimethylaminoethyl]phenyl] N-ethyl-N-methylcarbamate
Chemical Formula: C14H22N2O2
Rivastigmine on Wikipedia: https://en.wikipedia.org/wiki/Rivastigmine
Organisms Affected: Humans and other mammals