Rivastigmine is a carbamate derivative similar to physostigmine but not donepezil or tacrine in structure. The exact mechanism of rivastigmine is unknown, however it is thought that rivastigmine binds reversibly to and inactivates chlolinesterase (e.g., acetylcholinesterase, butyrylcholinesterase), limiting acetycholine hydrolysis and thereby increasing acetylcholine content at cholinergic synapses. When compared to acetylcholinesterase and butyrylcholinesterase in peripheral tissues, rivastigmine's anticholinesterase activity is relatively selective for brain acetylcholinesterase and butyrylcholinesterase.
Dosage & Administration
Rivastigmine transdermal patch: Apply patch on intact skin for a 24-hour period; replace with a new patch every 24 hours.
Rivastigmine should be administered twice a day, with morning and evening meals.
As a cholinesterase inhibitor, rivastigmine may exaggerate the effects of succinylcholine-type muscle relaxants during anesthesia. Be careful when choosing anesthetics. If necessary, consider possible dose adjustments or temporarily discontinue treatment. In view of its pharmacodynamic effects, rivastigmine should not be taken at the same time as other cholinergic drugs, as it may interfere with the activity of anticholinergics. No pharmacokinetic interaction between rivastigmine and digoxin, warfarin, diazepam, or fluoxetine was observed in the healthy volunteer study. The increase in prothrombin time caused by warfarin was not affected by the administration of rivastigmine. After using digoxin and rivastigmine in combination, no adverse effects on cardiac conduction were observed.
The use of this medicinal product is contraindicated in patients with hypersensitivity to the active substance or other carbamate derivatives.
The most common adverse events are gastrointestinal, with nausea (38%) and vomiting (23%) being the most common, especially during titration. In clinical investigations, female patients were found to be more vulnerable to gastrointestinal side effects and weight loss than male ones.
Pregnancy & Lactation
There are no clinical data on Rivastigmine. Rivastigmine should only be administered if absolutely essential during pregnancy. Rivastigmine is secreted in milk by animals. There is no information on whether rivastigmine is excreted in human milk. As a result, women who are on rivastigmine should not breastfeed.
Precautions & Warnings
Patients with sick sinus syndrome or conduction problems, as well as patients with respiratory illnesses. Gastric acid production may be increased by cholinergic activation. Urinary obstruction and convulsions may be worsened. Pregnancy. Renal failure, as well as mild to moderate hepatic failure. Keep an eye on your weight if you have asthma or obstructive pulmonary disease. Extrapyramidal symptoms may become worse. Lactation.
Drugs for Dementia
Store in a cool and dry place, protected from light.