MIGLITOL
Clinical safety rating
safeAnimal studies have demonstrated safety
Animal studies have demonstrated safety
Type 2 diabetes mellitus as monotherapy or in combination with sulfonylureas, metformin, or insulin when diet and exercise do not provide adequate glycemic control
Flatulence
Reversible competitive inhibitor of alpha-glucosidase in the intestinal brush border; delays glucose absorption and lowers postprandial hyperglycemia.
| Metabolism | Not metabolized; excreted unchanged in feces (via enzymatic breakdown in gut lumen) and urine (minor). |
| Excretion | Primarily excreted unchanged in urine (≈ 65%) via glomerular filtration; remainder recovered as metabolites in urine (25%) and feces (5%); total recovery in urine and feces ≈ 95% within 24 hours. |
| Half-life | Plasma elimination half-life ≈ 2 hours; clinical effect (alpha-glucosidase inhibition) persists longer due to enzyme binding; half-life increases in renal impairment (creatinine clearance < 25 mL/min). |
| Protein binding | Negligible (< 4%), primarily bound to albumin. |
| Volume of Distribution | Approximately 0.18 L/kg; distributes mainly in extracellular fluid with limited tissue penetration. |
| Bioavailability | Low and variable oral bioavailability: approximately 50% (range 35–65%) due to incomplete absorption and intestinal metabolism; dose proportional for doses up to 100 mg. |
| Onset of Action | Oral: onset of action within 1 hour (decline in postprandial glucose). |
| Duration of Action | Duration of alpha-glucosidase inhibition in intestinal brush border ≈ 2–4 hours; postprandial glucose reduction lasts for about 2–3 hours after a meal. |
| Molecular Weight | 207.2 |
25 mg orally three times daily with the first bite of each main meal; may increase to 50 mg three times daily after 4-8 weeks, maximum 100 mg three times daily.
| Dosage form | TABLET |
| Renal impairment | GFR <25 mL/min/1.73m2: contraindicated. No adjustment needed for GFR ≥25 mL/min/1.73m2. |
| Liver impairment | No dose adjustment required for hepatic impairment; not studied in Child-Pugh C. Use with caution in severe hepatic disease. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No specific dose adjustment, but monitor renal function; elderly may have age-related decline in renal function. Use lowest effective dose. |
| 1st trimester | Avoid due to limited human data; animal studies show fetal toxicity at high doses. Insulin is preferred for glycemic control. |
| 2nd trimester | Avoid; poorly controlled diabetes risks outweigh theoretical harm, but safer alternatives (e.g., insulin) are available. |
| 3rd trimester | Avoid; may cause fetal hypoglycemia. Use insulin if glycemic control required. |
Clinical note
Can reduce the bioavailability of digoxin and propranolol Can cause flatulence diarrhea and abdominal pain.
| Placental transfer | Expected to cross placenta due to low molecular weight; no human data quantified. |
| Breastfeeding | Excretion into human milk is unknown; due to low oral bioavailability, infant exposure likely minimal, but caution advised. Monitor infant for hypoglycemia. |
| Lactation Rating | L3 (Moderately Safe) or 'Use Caution' |
| Teratogenic Risk | No adequate well-controlled studies in pregnant women. Animal studies show no evidence of fetal harm at doses up to 150 mg/kg in rats and 75 mg/kg in rabbits. Risk cannot be ruled out; use only if clearly needed. |
| Fetal Monitoring | Monitor blood glucose levels; A1c may be less reliable due to interference with glucose meters. No specific fetal monitoring required beyond routine prenatal care. |
| Fertility Effects | No reported effects on fertility in animal studies. Human data not available. Theoretical concern due to carbohydrate malabsorption. |
■ FDA Black Box Warning
None.
| Common Effects | Flatulence |
| Serious Effects |
Diabetic ketoacidosisInflammatory bowel diseaseIntestinal obstruction or predisposition to obstructionChronic intestinal disease with marked disorders of digestion or absorptionHepatic cirrhosis (due to potential for lactic acidosis)
| Precautions | Hypoglycemia risk when used with insulin or sulfonylureas, Hepatotoxicity (rare, monitor liver enzymes), Gastrointestinal side effects (flatulence, diarrhea, abdominal pain) due to undigested carbohydrates in colon |
| Food/Dietary | Carbohydrates in the meal may cause increased flatulence and diarrhea. Sucrose and table sugar are not effective for treating hypoglycemia; use pure glucose. Avoid excessive simple carbohydrates if tolerated. |
| Clinical Pearls | Miglitol is an alpha-glucosidase inhibitor that delays carbohydrate absorption. It is not effective for type 1 diabetes. Monitor liver enzymes; cases of hepatitis have been reported. Do not use in patients with inflammatory bowel disease, colonic ulceration, or partial intestinal obstruction. Hypoglycemia must be treated with oral glucose (dextrose), not sucrose because sucrase is inhibited. Take with the first bite of each main meal. |
| Patient Advice | Take miglitol three times daily at the start of each main meal (with the first bite). · If you miss a dose, skip it if the meal is already finished; do not double the dose. · Common side effects include flatulence, diarrhea, and abdominal pain; these may decrease over time. · If hypoglycemia occurs, use glucose tablets or gel; table sugar (sucrose) will not work. · Inform your doctor if you have a history of kidney disease, inflammatory bowel disease, or intestinal obstruction. |
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