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Donepezil improves the function of nerve cells in the brain. It works by preventing the breakdown of a chemical called acetylcholine (ah SEET il KOE leen). People with dementia usually have lower levels of this chemical, which is important for the processes of memory, thinking, and reasoning. Donepezil is used to treat mild to moderate dementia caused by Alzheimer's disease.crl-40 940 powder buy
Donepezil Hydrochloride is a noncompetitive acetylcholinesterase inhibitor (IC50 = 11.6 nM. It is known that Donepezil Hydrochloride is a useful tool in the study of Alzheimer's disease. Studies indicate that Donepezil Hydrochloride protects the brain against diisopropylfluorophosphate-induced effects. Studies indicate that Donepezil Hydrochloride selectively inhibits acetylcholinesterase, whereas it has little effect on butyrylcholinesterase. Alternate studies suggest that Donepezil Hydrochloride increases the concentration of extracellular acetylcholine.

Donepezil HCl Application (indications)
Donepezil is approved for the symptomatic treatment of mild to moderate dementia of the Alzheimer's type. It can relieve the symptoms of dementia and slow the progression of symptoms for some time. Although the effect was statistically significantly demonstrated in scientific clinical trials using different measuring methods, it is very low. In severe Alzheimer's dementia, it is outside the drug approval in the form of a so-called off-label use as a second-line choice. Also without drug approval Donepezil is occasionally used in vascular dementia and is therefore the first choice. Its effectiveness in treating mild cognitive impairment, often heralding or showing signs of dementia, is considered minimal and poorly documented.
Contraindications (Contraindications)
Donepezil is contraindicated in a known hypersensitivity to this drug or other piperidine derivatives such as domperidone. In patients with gastric ulcers, arrhythmia (sick sinus syndrome, supraventricular conduction disorders), syncope, seizures, obstructive pulmonary disease (eg, bronchial asthma, chronic obstructive pulmonary disease), bladder obstruction or regular use of non-steroidal anti-inflammatory drugs, such as acetylsalicylic acid or naproxen, special Precautions and the use of donepezil are subject to a benefit-risk assessment.

Since donepezil may be ineffective for the individual and in this case should be discontinued after 15 to 20 weeks, the possible improvement in cognitive performance must be monitored. Patients should also be monitored for possible gastrointestinal complaints (which may indicate gastric ulcers or gastrointestinal bleeding) and for their ECG (which may indicate new cardiac arrhythmias). Therefore, a comparison ECG should be derived before starting therapy.
Due to its effect on acetylcholine metabolism, donepezil may show pharmacodynamic interactions with other drugs with effects on the acetylcholine system. These include in particular muscle relaxants, such as succinylcholine, anticholinergics and acetylcholine agonists. Pharmacodynamic interactions with beta-blockers are also possible.

Since donepezil is metabolised via the cytochrome P450 enzyme system, there is, at least in theory, the possibility of an interaction with substances that inhibit or induce this enzyme system. For example, CYP3A4 inhibitors, such as ketoconazole and erythromycin, and CYP2D6 inhibitors, such as fluoxetine, may inhibit the degradation of donepezil, leading to an increase in the blood plasma level of the drug. On the other hand, enzyme inducers such as rifampicin, phenytoin, carbamazepine and alcohol can accelerate the degradation of donepezil and thus lower its plasma levels. However, the extent of these interactions and their clinical relevance has not been sufficiently investigated.

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