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The active ingredient Donepezil is indicated for the symptomatic treatment of mild to moderate forms of Alzheimer’s dementia (forgetfulness). It improves the memory and watch assets, but does not prevent the progression of the disease. Here you can read everything of interest to Donepezil: action, use and possible side effects
How Donepezil acts
Donepezil is an antidementia, ie a remedy for dementia. The most common form of dementia is Alzheimer’s disease. This gradually dying neurons (neurons) in the brain. Usually a non-negligible part of the nerve cell is already dead before the first symptoms appear and the disease is discovered. One of the most important chemical messengers (neurotransmitters) between nerve cells, which are involved in memory, retentiveness and memory, is acetylcholine.
In order to communicate with other neurons may distribute a nerve cell messenger substances such as acetylcholine. This docks to specific docking sites in the membrane of the second nerve cell and thus transmits a particular signal. Thereafter, the neurotransmitter by an enzyme (acetylcholinesterase) is cleaved in acetate and choline, which no longer act on the receptors, whereby the signal is terminated. The two fission products are resumed in the first nerve cell, linked and then when you need it to be distributed.
Since nerve cells not only have one-to-one connections, but a nerve cell usually is in contact with many thousands of other nerve cells, one notices a cell death only when a threshold is exceeded. The remaining cell contacts then are no longer sufficient to route signals.
To the symptoms of Alzheimer’s disease to alleviate and improve memory performance, Donepezil is used as a selective inhibitor of the enzyme acetylcholinesterase. When this enzyme is inhibited in the brain, acetylcholine remains longer on the receptors of the postsynaptic nerve cell, whereby the signal is so to speak more. For our remaining nerve cells can still communicate with normal intensity.
Up, degradation and excretion of Donepezil
The active ingredient Donepezil passes after taking a tablet through the intestines into the bloodstream and from there through the blood-brain barrier into the central nervous system. He exerts its effect. In the liver Donepezil is metabolized in part to active and inactive breakdown products. These are mostly excreted in the urine, to a lesser extent in the faeces. Approximately 70 hours after taking the drug has left the body back to the half.
When will Donepezil used?
Donepezil is approved for the symptomatic treatment of mild to moderate Alzheimer’s disease.
Outside the scope of accreditation (“off-label” application), it is also used for the severe Alzheimer’s disease as a palliative drug.
It has to be taken permanently to maintain the effect.
How Donepezil is used
The active ingredient is a salt (Donepezil hydrochloride) in the form of tablets or orodispersible tablets that dissolve in the mouth in seconds ingested. Treatment is started with five milligrams of Donepezil once daily. After a month, it is judged by the doctor whether the dose is adequate or needs to be increased to ten milligrams of Donepezil daily. Higher doses are not recommended. Therapy should only be done when the patient is placed in a nursing home or a caregiver has, which monitors the administration of Donepezil.
What are the side effects of Donepezil?
More than ten percent of those treated complain of nausea and headaches.
It often happens while you are taking Donepezil addition to, and fatigue.
In a hundred to a thousand patients also Donepezil side effects such as seizures, slow heartbeat and gastrointestinal bleeding may occur.
What should be considered when taking Donepezil?
Since the active ingredient Donepezil in the liver mainly by two different enzymes (cytochrome P450 2D6 and 3A4) is degraded, which break down other substances, may cause interactions when these drugs are combined.
Examples of this are many antibiotics (Erythromycin, Metronidazole, Chloramphenicol), HIV drugs (ritonavir, indinavir), the blood pressure agent Verapamil, antifungal (Fluconazole, ketoconazole, itraconazole) and also many herbal remedies (valerian, goldenseal, ginseng ) and grapefruit juice.
Some agents ensure that more enzymes are produced in the liver, which degrade faster Donepezil. This affects its effectiveness. This cause, for example remedy for convulsions and epilepsy (Phenytoin, Carbamazepine, Oxcarbazepine), the anesthetic phenobarbital and some foods (garlic, licorice).
Patients with respiratory diseases such as asthma or COPD should take Donepezil with caution because of the risk of an asthma attack increases under certain circumstances.
If in addition to Donepezil non-steroidal anti-inflammatory drugs (NSAIDs such as aspirin, Ibuprofen, Diclofenac) to be taken regularly, possibly increasing the risk of gastrointestinal bleeding.
Children and adolescents as well as pregnant and nursing mothers should not take Donepezil, as no studies on the safety and efficacy of revenue.
Also, patients should not with severe hepatic dysfunction due to lack of experience are taking Donepezil.
How to obtain drugs with Donepezil
The antidementia Donepezil can be bought with a doctor’s prescription in the pharmacy.
Since when Donepezil is known?
The development of Donepezil began in 1983 with the Japanese pharmaceutical company Eisai. His first registration received the drug in the US in 1996. Since 2010 are generic with the active ingredient Donepezil on the market.