EXENATIDE
Working
This medicine lowers glucose levels by four different means:
• It acts on the beta cells to cause insulin
release.
• It decreases the glucagon release from alpha cells after
meals.
• It slows stomach emptying.
• It reduces appetite and promotes weight loss.
Exenatide works in exactly the same way as glucagon-like polypeptide 1 (GLP-1), a hormone
released by the small intestine in response to food. GLP-1 is rapidly broken down in the body, and so would
have to be given continuously to be effective. On the other hand, exenatide needs to be injected only twice a
day, within one hour of breakfast and one hour of the evening meal. The recommended dose is 5 g (micrograms)
twice a day for the first month, and if well tolerated, it is increased to 10 g twice a
day.
Exenatide is particularly effective at releasing insulin when glucose is elevated, but not as
effective when glucose is normal. This glucose-dependent insulin release means that there is less risk for
hypoglycemia when this drug is used on its own. Backup supplies of exenatide should be stored in the
refrigerator (not the freezer), but the pen you are currently using can be kept at room
temperature.
In experimental animals and in islets in culture, exenatide has a protective effect preventing
their death (apoptosis). This raises the possibility that if this is the case in humans (not yet shown), then
this medicine may prevent loss of beta cells with time and may even reverse
diabetes.
Side Effects
Nausea occurs in approximately 40 percent of individuals using
exenatide. In approximately 5 percent of these people, the nausea is so severe that the drug has to be stopped. For
most people, the nausea is manageable and tends to improve with time. Sometimes people tolerate the 5-g dose but
not the 10-g dose. People who have gastroparesis should not use exenatide because it slows gastric emptying,
making the symptoms of gastroparesis worse. Exenatide cannot be used if you have severe kidney
failure.
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