PRECOSE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PRECOSE (PRECOSE).
Alpha-glucosidase inhibitor; competitively inhibits brush-border alpha-glucosidases in the small intestine, delaying carbohydrate digestion and reducing postprandial hyperglycemia.
| Metabolism | Not extensively metabolized; primarily excreted unchanged in the urine as active drug. Small fraction undergoes intestinal metabolism by digestive enzymes. |
| Excretion | Primarily excreted in feces (about 85%) as unchanged drug and metabolites, with less than 2% excreted renally as active metabolites. |
| Half-life | Terminal elimination half-life is approximately 2 hours for the parent drug, but clinical effect persists due to prolonged binding to intestinal alpha-glucosidases. |
| Protein binding | Low protein binding, approximately 5%, primarily to albumin. |
| Volume of Distribution | Volume of distribution is approximately 0.3 L/kg, indicating minimal distribution into tissues and predominantly confined to extracellular fluid. |
| Bioavailability | Oral bioavailability is low, approximately 2%, due to local action in the gastrointestinal tract and minimal systemic absorption. |
| Onset of Action | Onset of action occurs within 15-30 minutes after oral administration, corresponding to gastric emptying and arrival at small intestine. |
| Duration of Action | Duration of action is approximately 4-6 hours, covering postprandial glucose peaks after each meal. |
Initial: 25 mg orally three times daily with the first bite of each main meal; maintenance: 50-100 mg three times daily; maximum 100 mg three times daily.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment recommended for mild to moderate renal impairment. Contraindicated in severe renal impairment (eGFR <25 mL/min/1.73 m²). |
| Liver impairment | No dose adjustment recommended for mild hepatic impairment. Not studied in moderate to severe hepatic impairment (Child-Pugh B or C); avoid use. |
| Pediatric use | Not recommended for pediatric patients (safety and efficacy not established). |
| Geriatric use | No specific dose adjustment required; monitor renal function due to age-related decline. Start at low end of dosing range (25 mg three times daily). |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PRECOSE (PRECOSE).
| Breastfeeding | Unknown if excreted in human milk. Caution advised. M/P ratio not established. |
| Teratogenic Risk | Pregnancy Category B. No evidence of teratogenicity in animal studies at doses up to 200 mg/kg/day (6-15 times human exposure). No adequate human studies; risk cannot be ruled out. |
| Fetal Monitoring | Monitor maternal blood glucose and hemoglobin A1c; fetal monitoring not specifically required; standard obstetric care. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to acarbose or any component","Diabetic ketoacidosis","Cirrhosis","Inflammatory bowel disease","Colonic ulceration","Partial intestinal obstruction or predisposition to intestinal obstruction","Chronic intestinal diseases associated with marked disorders of digestion or absorption","Conditions that may deteriorate as a result of increased intestinal gas formation (e.g., Roemheld syndrome)","Severe renal impairment (CrCl <25 mL/min)"]
| Precautions | ["Hypoglycemia: Acarbose does not cause hypoglycemia when used alone, but may increase risk when combined with sulfonylureas or insulin. Hypoglycemic episodes should be treated with glucose (dextrose), not sucrose.","Hepatic injury: Rare cases of acute hepatitis, jaundice, and fulminant hepatic failure; monitor liver function tests.","Renal impairment: Contraindicated in patients with CrCl <25 mL/min.","Gastrointestinal effects: Frequently causes flatulence, diarrhea, and abdominal discomfort due to undigested carbohydrates; these effects may diminish with continued use."] |
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| Fertility Effects | No evidence of impaired fertility in animal studies. No human data. |