Rivastigmine Tartrate capsule is indicated for the symptomatic treatment of mild to moderately severe Alzheimer’s dementia. It is also indicated for the symptomatic treatment of mild to moderately severe dementia in patients with idiopathic Parkinson’s disease.

Rivastigmine is a carbamate derivative structurally related to physostigmine, but not to donepezil or tacrine. Its exact mechanism is not fully established, but it is known to reversibly inhibit cholinesterase enzymes (acetylcholinesterase and butyrylcholinesterase), thereby preventing the breakdown of acetylcholine. This results in increased acetylcholine levels at cholinergic synapses. Rivastigmine shows relatively selective activity for brain cholinesterase compared to peripheral tissues.

Rivastigmine capsule: Rivastigmine capsule should be administered twice a day, with morning and evening meals.

• Initial dose: Rivastigmine 1.5 mg twice a day.
• Dose titration: The starting dose is Rivastigmine 1.5 mg twice a day. If this dose is well tolerated after a minimum of two weeks of treatment, the dose may be increased to Rivastigmine 3 mg twice a day. Subsequent increases to 4.5 mg and then 6 mg twice a day should also be based on good tolerability of the current dose and may be considered after a minimum of two weeks of treatment at that dose level.
• Maintenance dose: The effective dose is 3 mg to 6 mg twice a day; to achieve maximum therapeutic benefit patients should be maintained on their highest well tolerated dose. The recommended maximum daily dose is 6 mg twice a day. Maintenance treatment can be continued for as long as a therapeutic benefit for the patient exists.
• Re-initiation of therapy: If treatment is interrupted for more than several days, it should be re-initiated at 1.5 mg twice daily. Dose titration should then be carried out as described above.

Rivastigmine transdermal patch: Apply patch on intact skin for a 24-hour period; replace with a new patch every 24 hours.

• Initial Dose: Initiate treatment with 4.6 mg/24 hours Rivastigmine transdermal patch.
• Dose Titration: After a minimum of 4 weeks, if tolerated, increase dose to 9.5 mg/24 hours, which is the minimum effective dose. Following a minimum additional 4 weeks, may increase dosage to maximum dosage of 13.3 mg/24 hours.
• Mild to Moderate Alzheimer's Disease and Parkinson’s Disease Dementia: Rivastigmine transdermal patch 9.5 mg/24 hours or 13.3 mg/24 hours once daily.
• Severe Alzheimer’s Disease: Rivastigmine transdermal patch 13.3 mg/24 hours once daily.
• For treatment interruption longer than 3 days, retitrate dosage starting at 4.6 mg per 24 hours.

Your doctor will tell you which Rivastigmine transdermal patch is most suitable for you.

• Treatment usually starts with Rivastigmine 4.6 mg/24 hr.
• The recommended usual daily dose is Rivastigmine 9.5 mg/24 hr. If well tolerated, the treating physician may consider increasing the dose to 13.3 mg/24 hr.
• Only wear one Rivastigmine patch at a time and replace the patch with a new one after 24 hours. During the course of the treatment your doctor may adjust the dose to suit your individual needs.

As a cholinesterase inhibitor, Rivastigmine may enhance the effects of succinylcholine-type muscle relaxants during anesthesia. Care is required when selecting anesthetic agents, and temporary discontinuation or dose adjustment may be considered if necessary. Due to its pharmacodynamic effects, Rivastigmine should not be used with other cholinomimetic drugs and may interfere with anticholinergic medicines. No pharmacokinetic interaction has been observed with digoxin, warfarin, diazepam, or fluoxetine in healthy volunteers. The effect of warfarin on prothrombin time is not altered by Rivastigmine. No adverse effects on cardiac conduction were seen with concurrent use of digoxin.

Contraindicated in patients with hypersensitivity to Rivastigmine or other carbamate derivatives.

The most common adverse effects are gastrointestinal, mainly nausea (38%) and vomiting (23%), especially during dose titration. Female patients are more prone to gastrointestinal side effects and weight loss.

There are no adequate clinical data. Rivastigmine should be used during pregnancy only if clearly necessary. It is excreted in animal milk, but it is unknown whether it passes into human milk. Breastfeeding is not recommended during treatment.

Use with caution in patients with sick sinus syndrome, conduction disorders, respiratory diseases, asthma, urinary obstruction, or seizure disorders. May increase gastric acid secretion and worsen extrapyramidal symptoms. Monitor body weight regularly. Caution in pregnancy, renal or hepatic impairment (mild to moderate), and lactation.

Renal and hepatic impairment: Due to increased drug exposure in patients with moderate renal impairment and mild to moderate hepatic impairment, dosing should be carefully adjusted according to individual tolerability and closely monitored.

Use in children: Rivastigmine is not recommended for use in pediatric patients.

Most cases of accidental overdose are not associated with clinical symptoms, and many patients continued treatment without complications. When symptoms occur, they may include nausea, vomiting, diarrhea, hypertension, or hallucinations. Due to the vagotonic effect of cholinesterase inhibitors, bradycardia and/or syncope may also occur. In one reported case of 46 mg ingestion, the patient recovered fully within 24 hours with conservative management. Since rivastigmine has a plasma half-life of about 1 hour and acetylcholinesterase inhibition lasts about 9 hours, no further dose should be given for 24 hours in asymptomatic overdose cases. In cases with severe nausea and vomiting, antiemetics may be used. Supportive symptomatic treatment should be provided as needed. In severe overdose, atropine may be used (initial dose 0.03 mg/kg IV atropine sulfate, with further doses based on response). Scopolamine is not recommended as an antidote.

Drugs for Dementia

Store in a cool, dry place, protected from light.