Medical, Drugs, Pharmaceuticals And Diseases Information

An acetylcholinesterase inhibitor or anti-cholinesterase is a chemical that inhibits the cholinesterase enzyme from breaking down acetylcholine, so increasing both the level and duration of action of the neurotransmitter acetylcholine.

Donepezil- trade name Aricept is a centrally acting reversible acetyl cholinesterase inhibitor. It is used in the treatment of Alzheimer’s disease where it is used to increase cortical acetylcholine. Currently, there is no conclusive proof that donepezil halts/decreases the progression of Alzheimer’s disease. However many controlled studies have shown modest benefits in cognition and behavior. Many neurologists, psychiatrists, and primary care physicians use donepezil in patients with severe Alzheimer’s disease. But there is no significant improvement in functional outcome, of quality of life or of behavioral symptoms in those with mild to moderate Alzheimer’s disease. Donepezil comes as a tablet and dissolves quickly in the mouth. It is usually taken once a day, in the evening with or without food. The medicine is taken around the same time every day. It may take several weeks before the full benefits of donepezil are experienced . This drug helps control the symptoms of Alzheimer’s disease but does not cure it. It has to be taken even if the patients feels well and not stopped without talking to doctor.

 
  
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There are a range of medications approved by regulatory agencies such as the U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMEA) to treat the cognitive manifestations of Alzheimer ’s disease. The drugs are mostly acetyl cholinesterase inhibitors. There is also NMDA receptor antagonist like Memantine. However no medication currently available can delay or halt the progression of the Alzheimer’s Disease..

Reduction in the activity of the cholinergic neurons is a well-known feature of Alzheimer’s disease. Acetyl cholinesterase inhibitors are employed to reduce the rate at which acetylcholine is broken down, thereby increasing the concentration of Acetyl cholinesterase in the brain and combating the loss of Acetyl cholinesterase caused by the death of cholinergic neurons. The cholinesterase inhibitors approved for the management of AD symptoms are donepezil (Aricept), Galantamine (Razadyne), and rivastigmine ( Exelon and Exelon Patch). There is evidence for the efficacy of these medications in mild to moderate Alzheimer’s disease, and some evidence for their use in the advanced stage.

Donepezil is approved for treatment of advanced AD dementia. The use of these drugs in mild cognitive impairment has not shown any effect in a delay of the onset of Alzheimer’s disease. The most common side effects are nausea and vomiting, both of which are linked to cholinergic excess. These side effects arise in approximately ten to twenty percent of users and are mild to moderate in severity.

Glutamate is a useful excitatory neurotransmitter of the nervous system, although excessive amounts in the brain can lead to cell death through a process called excitotoxicity which consists of the over stimulation of glutamate receptors. Excitotoxicity occurs not only in Alzheimer’s disease, but also in other neurological diseases such as Parkinson’s disease and multiple sclerosis. Memantine (brand names Akatinol, Axura, Ebixa/Abixa, Memox and Namenda), is a noncompetitive NMDA receptor antagonist . It acts on the glutamatergic system by blocking NMDA receptors and inhibiting their over stimulation by glutamate. Memantine has been shown to be moderately efficacious in the treatment of moderate to severe Alzheimer’s disease.

 
  
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Many initiatives to prevent or delay the onset of AD have had contradictory results. Diet do seem to have some impact in preventing/delaying Alzheimer’s Disease. A diet rich in fruits and vegetables, bread, wheat and other cereals, olive oil, fish, and red wine, may all individually or together reduce the risk and course of Alzheimer’s disease. Many vitamins such as B12, B3, C or folic acid have appeared to be related to a reduced risk of AD. Curcumin/Turmeric in curry has shown some effectiveness in preventing brain damage in mouse models. Curry is regularly a part of diet in India. Elderly people of rural India, who eat large amounts of curry, appear to have the lowest incidence of Alzheimer’s disease in the world around 5 times lower than that of Americans.

Ginkgo is widely used in Europe for treating Alzheimer’s disease. It improves blood flow to the brain and has good antioxidant properties. There is evidence that ginkgo may improve thinking, learning, and memory in people with Alzheimer’s disease. One herb known as Ashwagandha (Botanical name Withania Somnifera) seems to have certain preventive and cognition improving effect on Alzheimer’s patients. Ashwagandha (Botanical name: Withania Somnifera) is a medicinal plant used in India to treat a wide range of age-related disorders. Its most remarkable effect may involve its ability to preserve the health of the aging brain. Research indicates that ashwagandha extract is capable of halting and even repairing damage to brain cells in an experimentally induced model of Alzheimer’s disease. In laboratory experiments in Japan 2004 and in earlier in Germany, researchers discovered that ashwagandha root extract inhibits acetyl cholinesterase in much the same way as the prescription drug donepezil, which is currently used in the treatment of Alzheimer’s disease.

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