Exelon

Exeton contains Rivastigmine. Rivastigmine belongs to an inhibitor of the carbamate type acetyl and butyrylcholinesterase. Its effects lie in the promotion of cholinergic transmission by slowing down the degradation of acetylcholine released from cholinergic neurons with non-damaged function. Thus, rivastigmine compensates for cognitive deficits caused by impaired cholinergic transmission in dementia caused by Alzheimer’s or Parkinson’s.

Rivastigmine interacts with target enzymes to form a covalent complex that temporarily inactivates the enzymes. In healthy young men, the application of a 3 mg oral dose reduces the activity of acetylcholinesterase (AChE) in the CSF by approximately 40% during the first 1.5 hours. The enzyme activity returns to baseline approximately 9 hours after reaching the maximum inhibitory effect. In patients with Alzheimer’s disease, the suppression of AChE activity by rivastigmine in CSF depends on the dose, up to the maximum studied dose of 6 mg 2 times a day. The decrease in the activity of butyrylcholinesterase in the CSF of 14 patients with Alzheimer’s disease who took rivastigmine was similar to the inhibition of AChE activity.

Indications

Exelon is indicated for:

• symptomatic treatment of mild to moderate dementia due to Alzheimer’s disease;
• symptomatic treatment of mild to moderate dementia in patients with idiopathic Parkinson’s disease.

Mode of application

Therapy should be started and carried out under the supervision of a physician. The doctor should be experienced in the diagnosis and treatment of dementia in Alzheimer’s disease or dementia caused by Parkinson’s disease. Exelon therapy should be started only if there are people who can regularly monitor the drug intake to patients.

Rivastigmine is taken 2 times a day, morning and evening, with food. Capsules should be swallowed whole.

Dosage

The initial dose is 1.5 mg 2 times a day.

Dose titration: initial dose – 1.5 mg 2 times a day. The dosage can be increased to 3 mg 2 times a day with good dose tolerance after at least 2 weeks of treatment. A subsequent increase to 4.5 mg and then to 6 mg 2 times a day should be based on good tolerance of the current dose. Such a dosage adjustment is allowed no earlier than after 2 weeks of treatment.

One or more doses can be skipped if there are any side effects, weight loss or worsening extrapyramidal symptoms (e.g. tremor) in patients suffering from dementia due to Parkinson’s disease. If side effects do not disappear, you should temporarily decrease the daily dosage to the previous well-tolerated dose or discontinue therapy for a while.

Overdose

In most cases, overdose was not accompanied by any clinical signs or symptoms. Almost all patients continued treatment with Exelon. Symptoms that accompanied an overdose were nausea, vomiting, diarrhea, hypertension, hallucinations. Due to the known vagotonic effect of cholinesterase inhibitors on heart rate, bradycardia and/or fainting are also possible. In one case, 46 mg of the drug was taken orally; after conservative treatment, the patient fully recovered within 24 hours.

Treatment: in case of overdose with nausea and vomiting, the use of antiemetics should be considered. In the event of other side effects, symptomatic therapy should be applied.

Contraindications

• Known hypersensitivity to rivastigmine, another carbamate derivative or any of the excipients;
• Severe violations of liver function.

Side effects

In patients with dementia due to Parkinson’s disease, the following adverse reactions were noted during treatment with rivastigmine:

• mental disorders: often – insomnia, anxiety.
• central nervous system: very often – tremor; often – dizziness, drowsiness, headache, worsening of Parkinson’s disease, bradykinesia, dyskinesia; infrequently – dystonia.
• cardiovascular system: often – bradycardia; infrequently – atrial fibrillation, AV block.
• digestive tract: very often – nausea, vomiting; often – diarrhea, loss of appetite, abdominal pain and dyspepsia, increased secretion of saliva.
• skin and subcutaneous tissue: often – increased sweating.
• musculoskeletal system and connective tissue: often – muscle stiffness.
• metabolism and nutrition disorders: very often – anorexia, dehydration.
• general disorders and reactions at the injection site: often – fatigue, asthenia; infrequently – gait disturbance.

Interactions

Being a cholinesterase inhibitor, rivastigmine can enhance the effects of muscle relaxants such as succinylcholine during anesthesia.

Due to pharmacodynamic effects, rivastigmine should not be used with other cholinomimetics; It can also interact with anticholinergics.

Pharmacokinetic interactions between rivastigmine and digoxin, warfarin, diazepam or fluoxetine were not found during studies on healthy volunteers. Exelon does not affect the increase in prothrombin time under the warfarin action. With the simultaneous use of digoxin and Exelon, an undesirable effect on cardiac conduction was not detected.

Judging by the metabolism, metabolic interactions are unlikely, although rivastigmine is able to inhibit the metabolism of other drugs mediated by butyrylcholinesterase.