Donepezil Hydrochloride: Difference between revisions
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|Donepezil hydrochloride is readily absorbed from the gastrointestinal tract with a relative oral bioavailability of 100%. It is about 95% bound to plasma proteins, mainly albumin. | |Donepezil hydrochloride is readily absorbed from the gastrointestinal tract with a relative oral bioavailability of 100%. It is about 95% bound to plasma proteins, mainly albumin. | ||
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!style="text-align: left"| | !style="text-align: left"| Onset of action | ||
| | |Peak plasma levels in 3-4 hours | ||
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!style="text-align: left"| | !style="text-align: left"| Elimination half-life | ||
| | |70 hours, but around 100 hours in elderly | ||
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!Duration of action | |||
|With daily dosing, steady-state concentration is reached within 3 weeks after initiation of therapy. Once at steady-state, plasma donepezil hydrochloride concentrations show little variability over the course of the day. | |||
|} | |} | ||
Revision as of 23:06, 29 September 2020
Pronunciation
Donepezil hydrochloride 10mg (ARICEPT 10mg)
Donepezil hydrochloride 5mg (ARICEPT 5mg)
Introduction
Donepezil hydrochloride, is a reversible inhibitor of acetylcholinesterase. It is used for the treatment of mild to moderate dementia in Alzheimer’s disease.
| Generic Name 藥名 | HA Code 藥物代碼 | Classification藥物分類 |
|---|---|---|
| Donepezil HCL Tablet 5mg | DONE01 | P1S1S3 |
| Donepezil HCL Tablet 10mg | DONE02 | P1S1S3 |
| Donepezil HCL Orodispersible Tablet 5mg | DONE03 | P1S1S3 |
Mechanism of Action
Acetylcholinesterase inhibiting drug
Dosage
By Oral: initially 5 mg once daily at bedtime, increased if necessary, after one month to max. 10 mg daily.
Clinical benefit should be assessed on a regular basis. Up to half the patients will show a slower rate of cognitive decline. Donepezil should be discontinued in those not responding.
Side Effects
Common side effects include
- Nausea and vomiting
- difficulty sleeping
- aggression
- Loss of appetite
- Diarrhoea
- Feeling tired
- Muscle cramps
These effects usually last 1 – 3 weeks and then lessen
Serious side effects may include:
- Abnormal heart rhythms
- Difficulty emptying urine from the bladder
- seizures
Donepezil, like other acetylcholinesterase inhibitors, can cause nightmares due to enhanced activation of the visual association cortex during REM sleep. Taking donepezil in the morning can reduce the frequency of nightmares.
Pharmacokinetics
| Oral bioavailability | Donepezil hydrochloride is readily absorbed from the gastrointestinal tract with a relative oral bioavailability of 100%. It is about 95% bound to plasma proteins, mainly albumin. |
|---|---|
| Onset of action | Peak plasma levels in 3-4 hours |
| Elimination half-life | 70 hours, but around 100 hours in elderly |
| Duration of action | With daily dosing, steady-state concentration is reached within 3 weeks after initiation of therapy. Once at steady-state, plasma donepezil hydrochloride concentrations show little variability over the course of the day. |
