Donepezil

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Donepezil.jpg

[edit] MECHANISM OF ACTION

The pathogenesis of the cognitive signs and symptoms of Alzheimer’s disease may due to a deficiency of cholingeric neurotransmission in the cerebral cortex and other areas of the brain.

Donepezil is a centrally acting reversible acetylcholinesterase inhibitor, it can enhance cholinergic function by increasing the concentration of acetylcholine.

[edit] INDICATIONS

Treatment of dementia of the Alzheimer’s type

[edit] DOSAGE

  • Mild to Moderate Alzheimer’s Disease: 5 mg or 10 mg administered once daily
  • Moderate to Severe Alzheimer’s Disease: 10 mg or 23 mg administered once daily

A dose of 10 mg once daily can be administered once patients have been on a daily dose of 5 mg for 4 to 6 weeks. A dose of 23 mg once daily can be administered once patients have been on a dose of 10 mg once daily for at least 3 months.

[edit] DOSAGE FORMS AND STRENGTHS

  • Tablets: 5 mg, 10 mg and 23 mg
  • Orally Disintegrating Tablets: 5 mg and 10 mg

[edit] CONTRAINDICATIONS

Patients with known hypersensitivity to Donepezil

[edit] WARNINGS AND PRECAUTIONS

  • Cholinesterase inhibitors are likely to exaggerate succinylcholine type muscle relaxation during anesthesia.
  • Cholinesterase inhibitors may have vagotonic effects on the sinoatrial and atrioventricular nodes manifesting as bradycardia or heart block
  • Donepezil can cause vomiting. Patients should be observed closely at initiation of treatment and after dose increases.
  • Cholinesterase inhibitors may be expected to increase gastric acid secretion due to increased cholinergic activity. Patients should be monitored closely for symptoms of active or occult gastrointestinal (GI) bleeding, especially those at increased risk for developing ulcers.
  • The use of Donepezil in a dose of 23 mg once daily is associated with weight loss.
  • Cholinomimetics may cause bladder outflow obstructions.
  • Cholinomimetics are believed to have some potential to cause generalized convulsions.
  • Cholinesterase inhibitors should be prescribed with care to patients with a history of asthma or obstructive pulmonary disease
  • Aggressive Behaviour: In patients with severe Alzheimer’s disease, Donepezil should be used with caution in patients at risk of aggression

[edit] INTERACTIONS

  • Cholinesterase inhibitors have the potential to interfere with the activity of anticholinergic medications (for example: Oxybutynin (Oral), Oxybutynin (Transdermal), Trospium chloride, Solifenacin, used to treat overactive bladder with symptoms of urge urinary incontinence)
  • A synergistic effect may be expected with concomitant administration of succinylcholine, similar neuromuscular blocking agents, or cholinergic agonists

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Based on animal data, Donepezil may cause fetal harm. There are no adequate or well-controlled studies in pregnant women. Donepezil should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Lactation: It is not known whether donepezil is excreted in human breast milk and there are no studies in lactating women. Excretion of donepezil and/or its metabolites into milk occurred after oral treatment of nursing rats, with milk concentrations similar to those in plasma. Therefore, women on donepezil should not breast feed.

[edit] SIDE EFFECTS

The most common adverse reactions in clinical studies of Donepezil are nausea, diarrhea, insomnia, vomiting, muscle cramps, fatigue, and anorexia

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Alzheimer/Dementia
Anticholinesterases Donepezil (Aricept, Memac)   Galantamine (Reminyl)   Rivastigmine (Oral) (Exelon)   Rivastigmine (Transdermal) (Exelon Patch)
Glutamatergic NMDA receptor antagonists Memantine (Ebixa)
Psychostimulants and nootropics Aniracetam   Choline   Citicoline   Ginkgo biloba   Piracetam