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Rivastigmine

Brands and Forms

  • Exelon
    • capsule: 1.5mg, 3mg, 4.5mg, 6mg.
    • oral solution: 2mg/ml
    • transdermal patch: 4.6mg/24hrs, 9.5mg/24hrs

Uses of Rivastigmine

Rivastigmine is used for treating Dementia. It delays the progression of the cognitive decline, and can also help to control some of the behavioral symptoms associated with Dementia.

How Rivastigmine Works

Rivastigmine is a cholinesterase inhibitor. It blocks the actions of centrally-acting acetylcholinesterase (AChE), thus making acetylcholine more available in the central nervous system. It also inhibits butyrylcholinesterase.

Cautions when Using Rivastigmine

Use with caution in people with asthma and other respiratory diseases, and seizure disorder.

Use caution when combining Rivastigmine with other medications that can increase bleeding time, including NSAIDs, as this can lead to easy bleeding.

Severe vomiting with esophageal rupture may occur if Rivastigmine is restarted at a full dose without first titrating gradually.

Dosing of Rivastigmine

The usual therapeutic range of Rivastigmine is 6-12mg/day, given twice daily. It can be started at 1.5mg twice daily and increased by 3mg/day (1.5mg twice daily) every two weeks, as tolerated, to a maximum of 6mg twice daily.

Nausea and other gastrointestinal side-effects limit the rate at which the medication can be titrated. These side-effects usually moderate with time.

The starting dose of the transdermal patch is 4.6mg per 24 hours. After 4 weeks, the dose can be increased to 9.6mg/24hrs. When switching from oral administration to the patch, it is recommended that the first patch be applied on the day following the last oral dose. If the person was already taking an oral dose of Rivastigmine of less than 6mg/day, then this can be switched to 4.6mg/24hrs of the patch. Individuals taking 6-12mg/day of the oral form should be switched directly to 9.5mg/24hrs of the patch.

When wanting to stop Rivastigmine, it can be stopped immediately without the need for a gradual taper.

Onset of action

May take up to 6 weeks before any improvement in memory of behavior becomes evident.

Kidney impairment

Dose adjustment not necessary.

Liver impairment

Dose adjustment not necessary.

Side-effects of Rivastigmine

Below is a list of most of the reported side-effects of Rivastigmine. Most of these side-effects occur in only a minority of individuals, and many also resolve with time while the medication is continued.

Cardiovascular: hypertension; fainting; angina pectoris; atrial fibrillation; bradycardia; hypotension; palpitations; postural hypotension; myocardial infarction (rare).

Central Nervous System: dizziness; headache; tremor; fatigue; insomnia; confusion; weakness; malaise; somnolence; extrapyramidal side-effects; vertigo; abnormal gait; unsteadiness; dyskinesia; paresthesia; convulsions.

Dermatologic: increased sweating; rashes of various sorts; hot flushes.

Eyes, Ears, Nose and Throat: rhinitis; pharyngitis; cataract; nose bleeds; tinnitus.

Gastrointestinal: nausea; vomiting; diarrhea; loss of appetite; abdominal pain; dyspepsia; constipation; flatulence; burping; fecal incontinence; gastritis.

Genitourinary: UTI; urinary incontinence; hematuria.

Hematologic: anemia; increased bleeing time.

Muskuloskeletal: muscle pains; joint pains; back pain; bone fracture; arthritis; leg cramps; rigors.

Psychiatric: depression; anxiety; agitation; psychosis.

Respiratory: bronchitis; coughing; upper respiratory tract infection; dyspnea.

Common side-effects of Rivastigmine

Nausea, vomiting, diarrhea, loss of appetite, abdominal pain, dizziness, headache, tremor, fatigue, insomnia.

Rare but serious side-effects of note of Rivastigmine

  • Heart attack
  • Seizures
  • Easy bleeding

Rivastigmine overdose

Bradycardia, hypotension, muscle weakness, salivation, seizures, severe nausea, sweating, vomiting, respiratory depression, cardiovascular collapse. Can be fatal.

Rivastigmine and pregnancy

Category B: animal studies have not shown any adverse effects, but no controlled human studies have been done. It is unlikely that Rivastigmine would be used for women of childbearing age.

Medical Monitoring for Rivastigmine

Monitor bleeding time and signs of occult blood loss. Also monitor weight given risk of appetite loss.

Drug Interactions with Rivastigmine

  • Use caution when combining Rivastigmine with other medications that can increase bleeding time, including NSAIDs, as this can lead to easy bleeding.