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NOOTROPICS DONEPEZIL HCL CAS 120011-70-3

    • 575 posts
    August 8, 2019 11:01 AM EDT
    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.



    Monitoring
    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.