MIGLITOL
Clinical safety rating: safe
Animal studies have demonstrated safety
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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Can reduce the bioavailability of digoxin and propranolol Can cause flatulence diarrhea and abdominal pain.
| Breastfeeding | No data on presence in human milk. M/P ratio unknown. Consider benefit of breastfeeding versus potential risk to infant. |
| 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 |
■ FDA Black Box Warning
None.
| Common Effects | Flatulence |
| Serious Effects |
["Diabetic ketoacidosis","Inflammatory bowel disease","Colonic ulceration","Intestinal obstruction or predisposition to obstruction","Chronic intestinal diseases associated with malabsorption","Hypersensitivity to miglitol"]
| 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"] |
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| 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. |