Exelon Rivastigmine: Medical Guide
Exelon contains an active substance called Rivastigmine and is used to treat symptoms of mild and moderately severe forms of Alzheimer’s disease, as well as symptoms of mild to moderate forms of dementia in patients with idiopathic forms of Parkinson’s disease.
Mechanism of Action
Exelon works by inhibiting two enzymes: acetylcholinesterase and butyrylcholinesterase. Both of these enzymes are involved in the decomposition of acetylcholine – an excitatory neurotransmitter of the peripheral and central nervous system. Inhibition of these two enzymes leads to an increase in the level of acetylcholine in intact neurons, which causes an improvement in cognitive deficits in patients with Alzheimer’s and Parkinson’s disease.
The efficacy of Exelon Rivastigmine in the treatment of Alzheimer’s disease has been demonstrated on 1017 patients in two, double-blind, placebo-controlled clinical studies, and this drug has been shown to significantly improve cognitive function compared to placebo.
The efficacy of Exelon Rivastigmine in the treatment of dementia associated with Parkinson’s disease has been demonstrated in a multicenter, double-blind, placebo-controlled study that lasted for 6 months. The results were measured with Mini-Mental State Examination (MMSE) scale, andthe medicine has been shown to improve dementia in patients with Parkinson’s disease.
After oral administration, this drug is resorbed completely and rapidly, with maximum blood concentrations reached in one hour. Taking Exelon capsules with food slows down the absorptionby 90 minutes and reduces the concentration of Rivastigmine in the blood by 30%. However, this is not considered clinically significant, so Exelon can be taken with a meal.
On average, 40% of Exelon bind to plasma proteins. The medicine easily passes the blood-brain barrier, thus allowing it to work effectively on acetylcholinesterase in the brain.
The largest part (over 90%) of the Exelon capsule is excreted via the kidney.
The usual starting dose is 1.5mg twice a day (with breakfast and dinner). If a dose of 1.5mg is well tolerated, then the dosage can be increased to 3-6mg twice daily. Increasing the dose should be gradual in order to determine the minimum effective one.You should take capsules with a meal to reduce the risk of side effects.
If adverse effects occur (pain in the stomach, nausea, vomiting, loss of appetite, and weight loss) during the treatment, then one or more doses should be omitted. If side effects persist, then dose reduction should be considered.
The maximum daily dose is 12 mg.
Exelon is contraindicated in patients who have an allergic reaction to Rivastigmine or other carbamate derivatives.
Clinical studies have shown that as many as 26% of women who are on therapy with this medicine experience weight loss by 7%. Anorexia occurred in 17% of patients who used this medicament.
Exelon increases gastric acid secretion, therefore, it should be used with extra precaution in patients with gastric or duodenal ulcer.
Rivastigmine exhibits a vagotonic effect(slows down the heart rate). For this reason, it must be very carefully used in patients with second-degree or third-degreeatrioventricular block.
It is assumed that Exelon increases the risk of epileptic seizures, and must be very carefully used in patients with epilepsy.
Since it may affect bronchi and lungs, Rivastigmine must be used with caution in patients with asthma or other respiratory tract disorders.
Useful Peace of Advice
The use of Exelon is associated with significant gastrointestinal side effects, such as nausea, vomiting, weight loss, and loss of appetite. Almost 47% of patients using Rivastigmine have experienced nausea or vomiting. In order to minimize the risk of gastrointestinal side effects, you should take the drug capsules with a meal.
Interaction with Other Drugs
So far, only five major interactions have been reported with the following drugs:
- Tramadol – a drug used to treat severe pain. The simultaneous administration increases the risk of side effects of tramadol (such as seizures).
- Bupropion – a drug used to treat depression and regarded as smoking cessation aid. Bupropion can cause convulsions and simultaneous administration with Exelon increases this risk.
- Ioexol, Iopamidol, Metrizamide–drugs used before X-ray imaging tests. The simultaneous administration increases the risk of convulsions.
Since Exelon is an acetylcholinesterase inhibitor, it can potentiate the effects of certain muscle relaxants during anesthesia (such as SuccinylCholine). Therefore, discontinuation of the therapy in patients who need to undergo surgery must be considered.
Meds4sure:Buy Rivastigmine Online, Exelon Generic Tablets No Prescription must be very carefully applied with following medicines, as it may affect their efficacy:
- Tolterodine and Solifenacin– drugs used to treat symptoms of overactive bladder.
- Atropine – a drug used for the treatment of slow heart rate and for the treatment of uveitis.
- Scopolamine – a drug used for the treatment ofmotionsickness, but also for the treatment of postoperative nausea and vomiting.
- Ipratropium bromide – a drug used to treat asthma and chronic obstructive pulmonary disease.
The following drugs may reduce the efficacy of Exelon, and the simultaneous application should be avoided:
- Diphenhydramine – a drug used to treat allergic rhinitis.
- Aripiprazole (Abilify) – a drug used to treat bipolar disorders and schizophrenia.
- Tricyclic antidepressants like Amitriptyline.
The simultaneous administration with the following medicines can lead to severe bradycardia (very slow heart rate):
- Antiarrhythmic drugs, such as Amiodarone, Sotalol, Ibutylide.
- Calcium blockers, such asNifedipine, Nicardipine, Amlodipine, Verapamil, and Diltiazem.
- Beta-blockers, such as Propranolol, Carvedilol, Bisoprolol, and Metoprolol.
Pregnancy and Breastfeeding
The FDA places this drug in category B because the trials on rabbits have shown that Exelon has no adverse effect on the development of the fetus. However, for now, there is not enough data on its use in pregnant women. For this reason, Rivastigmine should be used during pregnancy only if your doctor considers that the benefit is higher than the risk.
There is no information on whether Exelon is excreted in breast milk, and you should stop breastfeeding while taking this medicine.
Exelon may cause the following side effects:
- Abdominal pain
- Loss of appetite
- Weight loss
- Aggressive behavior
- Inflammation of the mucous membrane of the nose
- Urinary tract infections
Call your doctor if you notice any side effects.