| Quick reference: | |
| Therapeutic class: Antidiabetic | |
| Pharmacologic class: Second-Generation Sulfonylurea | |
| Pregnancy risk category C | |
| Generic name: glimepiride | |
| Brand name: Amaryl |
Glimepiride is a second-generation sulfonylurea with a long half-life. It has a half-life of 9 hours and an action duration of 24 hours, allowing for once-daily dosing. Glimepiride administration with food reduces the AUC slightly while increasing the time to peak concentration slightly. It has a peak effect on plasma glucose concentrations 2 to 3 hours after each dose. Glimepiride is completely metabolized by the liver, and its main metabolite has 30% of the parent drug's activity. Metabolite excretion occurs in the urine and feces. Interestingly, research suggests that sulfonylureas, similar to their action at the β-cell, may close ATP-sensitive potassium channels in cardiac tissue. This effect in the heart could prevent vasodilation during an ischemic episode (i.e., ischemic preconditioning).
Mechanism of action:
Lowers glucose levels, possibly by stimulating insulin release from functioning pancreatic beta cells, and may improve insulin binding to insulin receptors or increase the number of insulin receptors with prolonged administration; may also reduce basal hepatic glucose secretion; ineffective if the patient does not have functioning B-cells. It is believed that second-generation sulfonylureas are more effective than first-generation sulfonylureas.
Therapeutic outcome:
-Decrease in polyuria
-Polydipsia
-Polyphagia
-Clear sensorium
-Absence of dizziness
-Stable gait
Pharmacokinetics:
-Completely absorbed from GI tract
-Protein binding: greater than 99%
-Metabolized in liver
-Excreted in urine (60%), feces (40%)
-Half-life: 5–9.2 hrs
-In patients with type 2 diabetes mellitus whose hypoglycemia cannot be controlled by diet and exercise alone, as an adjunct to diet to lower blood glucose.
-In patients with type 2 diabetes mellitus, in combination with metformin or insulin, to improve glucose control as an adjunct to diet and exercise.
Available forms:
Tablets: 1 mg, 2 mg, 4 mg
P.O.
Give with breakfast or the first main course.
| Type 2 diabetes mellitus | |
| BY MOUTH | |
| Adult: | |
| Initially 1 mg daily, adjusted according to response, then increased in 1 mg steps every 1–2 weeks to 4 mg daily, the daily dose may be increased further in exceptional circumstances; dose to be taken shortly before or with the first main meal, maximum 6 mg per day. | |
| Maximum: 8 mg/day |
| ELDERLY: | |
| Initially, 1 mg per day. To avoid hypoglycemia, adjust the dose. |
| Dosage in Renal Impairment: | |
| 1 mg/day at first, then titrate based on fasting serum glucose levels. |
| Dosage in Hepatic Impairment: | |
| There is no need to change the dose (not studied). |
| (CNS) central nervous system |
|
| Drowsiness | |
| Asthenia | |
| Nervousness | |
| Tremor | |
| Insomnia | |
| Blurred vision | |
| Headache |
| (CV) cardiovascular system |
|
| Increased risk of CV mortality (possible) |
| Endocrine system |
|
| Hypoglycemia | |
| Syndrome of Inappropriate Antidiuretic Hormone Secretion (SIADH) |
| (GIT) gastrointestinal tract |
|
| Anorexia | |
| Nausea | |
| Vomiting | |
| Epigastric | |
| Discomfort | |
| Heartburn | |
| Diarrhea | |
| Hepatotoxicity | |
| Cholestatic jaundice |
| Hematologic | |
| Leukopenia | |
| Thrombocytopenia | |
| Anemia |
| Hypersensitivity | |
| Allergic skin reactions | |
| Eczema | |
| Pruritus | |
| Erythema | |
| Urticaria | |
| Photosensitivity | |
| Fever | |
| Eosinophilia | |
| Jaundice |
| Other | |
| Diuresis | |
| Tinnitus | |
| Fatigue | |
| weight gain | |
| Hyponatremia |
-Contraindicated in patients who are hypersensitive to the drug or who have diabetic ketoacidosis, which should be treated with insulin.
-Contraindicated in pregnant women and the elderly, as well as the sole treatment for type 1 diabetes.
-It is not recommended for breastfeeding mothers because it may cause hypoglycemia in breast-fed infants.
-Use with caution in patients who are debilitated or malnourished, as well as those who have adrenal, pituitary, hepatic, or renal insufficiency; these patients are more vulnerable to the hypoglycemic action of glucose-lowering drugs.
-Use with caution when taking medications that can cause hypoglycemia.
-Use with caution in patients who are allergic to sulfonamides.
-Use with caution in patients who have G6PD deficiency.
- No evidence of safety or efficacy in children has been found.
(Drug-drug)
Beta-blockers:
These medications may mask hypoglycemic symptoms.Keep an eye on your blood glucose levels.
Drugs that cause hyperglycemia (e.g., corticosteroids, estrogens, fosphenytoin, hormonal contraceptives, isoniazid, nicotinic acid, other diuretics, phenothiazines, phenytoin, thyroid products):
May result in glucose control loss.Dosage should be adjusted.
Insulin:
Increases the risk of hypoglycemia. Use together with caution.
NSAIDs and other highly protein-bound drugs (for example, beta-blockers, chloramphenicol, coumarin, MAO inhibitors, probenecid, sulfonamides):
Sulfonylureas, such as glimepiride, may have an increased hypoglycemic effect. Keep an eye on your blood glucose levels.
Thiazide diuretics and rifamycins:
Hyperglycemia risk may be increased. Keep an eye on your blood glucose levels.
Salicylates:
Sulfonylurea's hypoglycemic effects may be exacerbated by salicylates.Keep an eye on your blood glucose levels.
Burdock, dandelion, eucalyptus, and other(drug-herbs).
Marshmallow:
May amplify drug effects. Use together is discouraged.
Drug-lifestyle:
Alcohol consumption can alter glycemic control, most commonly resulting in hypoglycemia. It is also possible that a disulfiram-like reaction will occur. Use together is discouraged.
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2.Kizior, R.J. and Hodgson, B.B. (2018). Saunders nursing drug handbook 2019. Philadelphia: Saunders.
3.Williams and Wolters Kluwer Health (2012). Nursing 2012 drug handbook. Philadelphia, Pa.: Wolters Kluwer Health/Lippincott Williams & Wilkins.
4.Kolesar, J.M. (2013). Top 300 pharmacy drug cards 2016-2017. Mcgraw-Hill.
5.Al, E. (2013). Applied therapeutics: the clinical use of drugs. Philadelphia: Wolters Kluwer Health - Lippincott Williams & Wilkins, Cop.
6.Skidmore-Roth, L. (2019). Mosby’s Drug Guide for Nursing Students. 13th ed. S.L.: Mosby.
7.Amy Morrison Karch (2013). 2014 Lippincott’s nursing drug guide. Philadelphia, Pennsylvania: Lippincott Williams & Wilkins.
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