Indications

Demelon (Rivastigmine) is indicated for the symptomatic treatment of:

• Mild to moderately severe Alzheimer's dementia.
• Mild to moderately severe dementia in patients with Idiopathic Parkinson's disease.

Pharmacology

Rivastigmine is a carbamate derivative that acts as a reversible inhibitor of cholinesterase enzymes, specifically acetylcholinesterase and butyrylcholinesterase in the brain. By inactivating these enzymes, it prevents the breakdown of acetylcholine, leading to an increased concentration of this neurotransmitter at cholinergic synapses. This increased acetylcholine concentration is thought to improve the symptoms of dementia.

Dosage & Administration

• Capsule:
  • Initial Dose: 1.5 mg twice a day.
  • Dose Titration: If well-tolerated after a minimum of two weeks, the dose can be increased to 3 mg twice daily. Subsequent increases to 4.5 mg and then 6 mg twice daily can be made after a minimum of two weeks at each dose level, based on tolerability.
  • Maintenance Dose: The effective dose is 3 mg to 6 mg twice a day. The maximum recommended daily dose is 6 mg twice a day.
  • Administration: Must be taken with morning and evening meals.
• Transdermal Patch:
  • Initial Dose: 4.6 mg/24 hours.
  • Dose Titration: After at least 4 weeks, if tolerated, the dose can be increased to 9.5 mg/24 hours (minimum effective dose). A further increase to the maximum dose of 13.3 mg/24 hours can be considered after an additional 4 weeks.
  • Administration: Apply a new patch to intact skin every 24 hours.

Interaction

• Muscle Relaxants: May exaggerate the effects of succinylcholine-type muscle relaxants during anesthesia.
• Cholinomimetic/Anticholinergic Substances: Should not be used with other cholinomimetic drugs and may interfere with anticholinergic medications.
• Other Drugs: No significant pharmacokinetic interaction has been observed with digoxin, warfarin, diazepam, or fluoxetine.

Contraindications

Demelon is contraindicated in patients with a known hypersensitivity to the active substance or other carbamate derivatives.

Side Effects

The most common side effects are gastrointestinal, including nausea (38%) and vomiting (23%), particularly during dose titration. Female patients are more susceptible to these side effects and weight loss.

Pregnancy & Lactation

• Pregnancy: There are no clinical data on its use in pregnant women. It should only be used if clearly necessary.
• Lactation: It is not known if Rivastigmine is excreted in human milk. Women taking this medication should not breastfeed.

Precautions & Warnings

• Cardiac/Respiratory Conditions: Use with caution in patients with sick sinus syndrome, conduction defects, or respiratory diseases like asthma.
• Other Conditions: May exacerbate urinary obstruction and seizures. Use with caution in patients with renal impairment, mild to moderate hepatic impairment, or severely impaired cardiac function.
• Body Weight: Body weight should be monitored.

Use in Special Populations

• Renal and Hepatic Impairment: Dosing recommendations to titrate according to individual tolerability should be closely followed due to increased drug exposure.
• Children: Demelon is not recommended for use in children.

Overdose Effects

Overdose symptoms may include nausea, vomiting, diarrhea, hypertension, and hallucinations. Bradycardia and/or syncope may also occur. In case of asymptomatic overdose, do not administer the next dose for 24 hours. In severe overdose, atropine can be used as an antidote.

Therapeutic Class

Demelon is a drug for dementia.

Storage Conditions

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