MIGLITOL
وهو دواء غير موجود في BNF ولكنه مقر في FDA وموجود في الولايات المتحدة
الاسم التجاري: Glyset
الإستخدام: في علاج مرض السكر
an oral for use in the management of non-insulin dependant diabetes mellitus (NIDDM)i
مجموعته:
Alfa-glucosidase inhibitor
يعني من نفس مجموعة Acarbose
Mechanism of Action
In contrast to sulfonylureas, GLYSET does not enhance insulin secretion. The antihyperglycemic action of miglitol results from a reversible inhibition of membrane-bound intestinal a-glucoside hydrolase enzymes. Membrane-bound intestinal a-glucosidases hydrolyze oligosaccharides and disaccharides to glucose and other monosaccharides in the brush border of the small intestine. In diabetic patients, this enzyme inhibition results in delayed glucose absorption and lowering of postprandial hyperglycemia. Because its mechanism of action is different, the effect of GLYSET to enhance glycemic control is additive to that of sulfonylureas when used in combination. In addition, GLYSET diminishes the insulinotropic and weight-increasing effects of sulfonylureas. Miglitol has minor inhibitory activity against lactase and consequently, at the recommended doses, would not be expected to induce lactose intoleranse
Pharmacokinetics
Absorption: Absorption of miglitol is saturable at high doses: a dose of 25 mg is completely absorbed, whereas a dose of 100 mg is only 50%-70% absorbed. For all doses, peak concentrations are reached in 2-3 hours. There is no evidence that systemic absorption of miglitol contributes to its thrapeutic effect
Distribution: The protein binding of miglitol is negligible (<4.0%). Miglitol has a volume of distribution of 0.18 L/kg, consistent with distribution primarily into the extracellular fluid
Met-abolism: Miglitol is not m etabolized in man or in any animal species studied. No m etabolites have been detected in plasma, urine or feces, indicating a lack of either systemic or presystemic m etabolism
Excretion: Miglitol is eliminated by renal excretion as unchanged drug. Thus, following a 25-mg dose, over 95% of the dose is recovered in the urine within 24 hours. At higher doses, the cumulative recovery of drug from urine is somewhat lower due to the incomplete bioavailability. The elimination half-life of miglitol from plasma is approximately 2 hours
OVERDOSE
Unlike sulfonylureas or insulin, an overdose of GLYSET Tablets will not result in hypoglycemia. An overdose may result in transient increases in flatulence, diarrhea, and abdomi-nal discomfort. Because of the lack of extra-intestinal effects seen with GLYSET, no serious systemic reactions are expected in the event of an overdose
CONTRAINDICATIONS
GLYSET Tablets are contraindicated in patients with:i
Diabetic ketoacidosis
Inflammatory bowel disease, colonic ulceration, or
partial intestinal obstruction, and in patients predisposed to intestinal obstruction
Chronic intestinal diseases associated with marked disorders of digestion or absorption, or with conditions that may deteriorate as a result of increased gas formation in the intestine
Hypersensitivity to the drug or any of its components
In contrast to acarbose (another alpha-glucosidase inhibitor), miglitol is systemically absorbed; however, it is not met-abolized and is excreted by the kidneys
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