Rivastigmine

Products

Rivastigmine is commercially available as capsules, oral solution, and transdermal patch (Exelon, generics). It has been approved in many countries since 1997.

Structure and properties

Rivastigmine (C14H22N2O2, Mr = 250.3 g/mol) is a phenyl carbamate. It exists in the oral forms as rivastigmine hydrogenotartrate, a white crystalline powder that is very soluble in water.

Effects

Rivastigmine (ATC N06DA03) has indirect cholinergic properties. The effects are due to selective and pseudo-irreversible inhibition of acetyl- and butyrylcholinesterase, resulting in inhibition of acetylcholine degradation.

Indications

Symptomatic treatment of mild to moderate dementia in Alzheimer’s or Parkinson’s disease.

Dosage

According to the SmPC. The oral forms are to be taken with meals. The transdermal patch is applied to healthy skin once daily. The site should be changed daily to prevent skin irritation. For tips on administration: see Administering TTS.

Contraindications

  • Hypersensitivity to the active substance and carbamates.
  • Severe hepatic insufficiency

Full precautions can be found in the drug label.

Interactions

Rivastigmine interacts poorly with cytochromes and is mainly degraded by esterases. Therefore, no corresponding drug-drug interactions are expected. Rivastigmine should not be given with parasympathomimetics and parasympatholytics (anticholinergics) because of its pharmacologic properties. Rivastigmine may potentiate the effects of succinylcholine-type muscle relaxants.

Adverse effects

The most common possible adverse effects include dizziness, nausea, vomiting, diarrhea, and loss of appetite. Other common side effects include abdominal pain, dyspepsia, agitation, confusion, anxiety, weight loss, sweating, headache, drowsiness, tremor, fatigue, asthenia, and malaise. The patch may cause local reactions at the administration site such as itching and redness.