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Tuesday, July 28, 2015

減重應用: 糖尿病長效注射GLP-1藥物(Exenatide (Byetta, Bydureon/ microsphere) and liraglutide (Victoza))

Byetta, Victoza and Bydureon for diabetes lose weight  M. Regina Castro, M.D.

Exenatide (Byetta, Bydureon) and liraglutide (Victoza) are taken by injection, similar to insulin, but they're not insulin. These medications are in a class of drugs called incretin mimetics, which improve blood sugar control by mimicking the action of a hormone called glucagon-like peptide 1 (GLP-1). Among other things, these drugs stimulate insulin secretion in response to rising blood sugar levels after a meal, which results in lowering of the blood sugar. Byetta, Bydureon and Victoza not only improve blood sugar control, but may also lead to weigacause weight loss. They appear to help suppress appetite. But the most prominent effect of these drugs is that they delay the movement of food from the stomach into the small intestine. As a result, you may feel "full" faster and longer, so you eat less. Byetta is injected twice daily, and Victoza is injected once a day. Bydureon, a newer formulation, is injected once a week. These drugs do have different effects and side effects to consider. Exenatide (Byetta, Bydureon). The most common side effect of exenatide is mild to moderate nausea, which improves with time in most people. Several cases of kidney problems, including kidney failure, have been reported in people who have taken exenatide. Rarely, exenatide may cause harmful inflammation of the pancreas (pancreatitis).

Liraglutide (Victoza). Some studies have found that liraglutide reduces systolic blood pressure and triglycerides, in addition to improving blood sugar control. The most common side effects are headache, nausea and diarrhea. Clinical studies have also shown that liraglutide may cause pancreatitis.

BYDUREON (exenatide extended-release for injectable suspension) is supplied as a sterile powder to be suspended in diluent and administered by subcutaneous injection. Exenatide is a 39-amino acid synthetic peptide amide with an empirical formula of C 184H282N50O60S and a molecular weight of 4186.6 Daltons. The amino acid sequence for exenatide is shown below. H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val­Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2 BYDUREON is a white to off-white powder that is available in a dosage strength of 2 mg exenatide per vial or per pen. Exenatide is incorporated in an extended-release microsphere formulation containing the 50:50 poly(D,L-lactide-co-glycolide) polymer (37.2 mg per dose) along with sucrose (0.8 mg per dose). The powder must be suspended in the diluent prior to injection. The diluent for the BYDUREON vial is supplied in a prefilled syringe within each single -dose tray. The diluent for the BYDUREON Pen is contained within each single -dose pen. Each configuration contains sufficient diluent to deliver 0.65 mL. The diluent is a clear, colorless to pale-yellow solution composed of carboxymethylcellulose sodium (19 mg), polysorbate 20 (0.63 mg), sodium phosphate monobasic monohydrate (0.61 mg), sodium phosphate dibasic heptahydrate (0.51 mg), sodium chloride (4.1 mg), and water for injection. Sodium hydroxide may be added during manufacture of BYDUREON Pen for pH adjustment.

 

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