AMARYL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AMARYL (AMARYL).
Sulfonylurea that stimulates insulin secretion from pancreatic beta cells by binding to the sulfonylurea receptor (SUR1) on ATP-sensitive potassium channels, causing channel closure and calcium influx.
| Metabolism | Primarily hepatic metabolism via CYP2C9 to inactive metabolites. |
| Excretion | Approximately 60% excreted renally as metabolites (mainly M1 and M2) and 40% in feces; <1% excreted unchanged. |
| Half-life | Terminal elimination half-life is 5-7 hours; clinically, dosing is once daily due to sustained glucose-lowering effect beyond half-life. |
| Protein binding | >99.5% bound, primarily to albumin. |
| Volume of Distribution | 0.12-0.17 L/kg; suggests limited extravascular distribution. |
| Bioavailability | Oral: 100% (absolute bioavailability). |
| Onset of Action | Oral: 30-60 minutes; peak effect at 2-4 hours. |
| Duration of Action | Glucose-lowering effect persists 24 hours with once-daily dosing; maximum duration up to 24 hours. |
Initial dose 1-2 mg orally once daily, titrated to target glucose. Maximum dose 8 mg daily.
| Dosage form | TABLET |
| Renal impairment | eGFR 30-60: Start 1 mg daily, titrate cautiously. eGFR <30: Contraindicated. |
| Liver impairment | Mild-moderate impairment (Child-Pugh A/B): Start 1 mg daily, titrate cautiously. Severe impairment: Not recommended. |
| Pediatric use | Not approved in pediatric patients. |
| Geriatric use | Start 1 mg daily due to increased hypoglycemia risk; titrate slowly. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for AMARYL (AMARYL).
| Breastfeeding | Excreted in human milk; M/P ratio unknown. Avoid breastfeeding due to risk of neonatal hypoglycemia. If used, discontinue breastfeeding or drug. |
| Teratogenic Risk | Pregnancy Category C. First trimester: Limited human data; animal studies show fetal harm (increased skeletal variations and fetal death). Second and third trimesters: Use only if benefit outweighs risk; may cause neonatal hypoglycemia, macrosomia. Crosses placenta. |
| Fetal Monitoring |
■ FDA Black Box Warning
Increased risk of cardiovascular mortality: The drug may increase cardiovascular mortality risk based on studies with similar sulfonylureas.
| Common Effects | Hypoglycemia low blood glucose level Headache Nausea Dizziness Weakness |
| Serious Effects |
["Type 1 diabetes mellitus","Diabetic ketoacidosis","Known hypersensitivity to glimepiride or sulfonamides","Severe hepatic impairment"]
| Precautions | ["Hypoglycemia: Risk increased with skipped meals, excessive exercise, or renal impairment.","Cardiovascular risk: Possible increased risk of cardiovascular mortality.","Hepatic impairment: Use caution; prolonged hypoglycemia may occur.","Renal impairment: Increased risk of hypoglycemia; consider dose adjustment.","Hemolytic anemia: Rarely reported in patients with G6PD deficiency."] |
| Food/Dietary |
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| Monitor maternal blood glucose, HbA1c, renal function, hepatic function. Fetal: ultrasound for growth, amniotic fluid assessment, fetal heart rate monitoring. |
| Fertility Effects | No significant effects on fertility reported in animal studies. In humans, uncontrolled diabetes may impair fertility; improved glycemic control may benefit. |
| Take glimepiride with food to reduce gastrointestinal upset and align with meal-induced insulin release. Avoid excessive alcohol intake as it can potentiate hypoglycemia. Consistent carbohydrate intake is important to minimize blood glucose fluctuations. |
| Clinical Pearls | Amaryl (glimepiride) is a sulfonylurea that stimulates insulin secretion from pancreatic beta-cells. It should be taken with the first main meal of the day to reduce hypoglycemia risk. Dose adjustments are needed in renal impairment; contraindicated in eGFR <30 mL/min. Can cause weight gain. Avoid use with meglitinides due to overlapping mechanism. |
| Patient Advice | Take glimepiride with your first meal of the day to prevent low blood sugar. · Monitor blood sugar regularly as directed and recognize symptoms of hypoglycemia (shakiness, sweating, confusion). · Do not skip meals while on this medication. · Avoid alcohol; it can cause severe hypoglycemia. · Report any signs of hypoglycemia or unusual bruising/bleeding (possible blood dyscrasias). |