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glimepiride

(glye meh' per ide)


Amaryl

Pregnancy Category C

Drug classes
Antidiabetic
Sulfonylurea (second generation)

Therapeutic actions
Stimulates insulin release from functioning beta cells in the pancreas; may improve
binding between insulin and insulin receptors or increase the number of insulin receptors;
thought to be more potent in effect than first-generation sulfonylureas

Indications
• As an adjunct to diet to lower blood glucose in patients with type 2 (non–insulin-
dependent) diabetes mellitus whose hypoglycemia cannot be controlled by diet
and exercise alone.
• In combination with metformin or insulin to better control glucose as an adjunct
to diet and exercise in patients with type 2 diabetes mellitus.

Contraindications and cautions


• Contraindicated with allergy to sulfonylureas; diabetes complicated by fever,
severe infections, severe trauma, major surgery, ketosis, acidosis, coma (insulin is
indicated in these conditions); type 1 (insulin-dependent), serious hepatic or renal
impairment, uremia, thyroid or endocrine impairment, glycosuria, hyperglycemia
associated with primary renal disease; labor and delivery—if glimepiride is used
during pregnancy, discontinue drug at least 1 mo before delivery; lactation, safety
not established.
• Use cautiously with pregnancy.

Available forms
Tablets—1, 2, 4 mg

Dosages
ADULTS
Usual starting dose is 1–2 mg PO once daily with breakfast or first meal of the day; usual
maintenance dose is 1–4 mg PO once daily, depending on patient response and glucose
levels. Do not exceed 8 mg/day.
• Combination with insulin therapy: 8 mg PO daily with first meal of the day with
low-dose insulin.
• Transfer from other hypoglycemic agents: No transition period is necessary.
PEDIATRIC PATIENTS
Safety and efficacy not established.
PATIENTS WITH RENAL IMPAIRMENT
Usual starting dose is 1 mg PO once daily; titrate dose carefully, lower maintenance
doses may be sufficient to control blood sugar.

Pharmacokinetics
Route Onset Peak
Oral 2–3 hr 2–3 hr

Metabolism: Hepatic; T1/2: 5.5–7 hr


Distribution: Crosses placenta; enters breast milk
Excretion: Bile and urine

Adverse effects
• CNS: Drowsiness, asthenia, nervousness, tremor, insomnia
• CV: Increased risk of cardiovascular mortality (possible)
• Endocrine: Hypoglycemia, SIADH
• GI: Anorexia, nausea, vomiting, epigastric discomfort, heartburn, diarrhea
• Hematologic: Leukopenia, thrombocytopenia, anemia
• Hypersensitivity: Allergic skin reactions, eczema, pruritus, erythema, urticaria,
photosensitivity, fever, eosinophilia, jaundice
• Other: Diuresis, tinnitus, fatigue

Interactions
Drug-drug
• Increased risk of hypoglycemia with androgens, anticoagulants, azole antifungals,
chloramphenicol, clofibrate, fenfluramine, fluconazole, gemfibrozil, H2 blockers,
magnesium salts, MAOIs, methyldopa, oxyphenbutazone, phenylbutazone,
probenecid, salicylates, sulfinpyrazone, sulfonamides, TCAs, urinary acidifiers
• Decreased effectiveness of both glimepiride and diazoxide if taken concurrently
• Increased risk of hyperglycemia with rifampin, thiazides
• Risk of hypoglycemia and hyperglycemia with ethanol; "disulfiram reaction" has
also been reported
• Possible decreased hypoglycemic effect with beta blockers, calcium channel
blockers, cholestyramine, corticosteroids, diazoxide, estrogens, hydantoins,
hormonal contraceptives, isoniazid, nicotinic acid, phenothiazines, rifampin,
sympathomimetics, thiazide diuretics, thyroid agents, urinary alkalinizers
Drug-alternative therapy
• Increased risk of hypoglycemia if taken with juniper berries, ginseng, garlic,
fenugreek, coriander, dandelion root, celery

Nursing considerations
Assessment
• History: Allergy to sulfonylureas; diabetes complicated by fever, severe
infections, severe trauma, major surgery, ketosis, acidosis, coma (insulin is
indicated in these conditions); type 1 diabetes, serious hepatic or renal
impairment, uremia, thyroid or endocrine impairment, glycosuria, hyperglycemia
associated with primary renal disease; pregnancy
• Physical: Skin color, lesions; T; orientation, reflexes, peripheral sensation; R,
adventitious sounds; liver evaluation, bowel sounds; urinalysis, BUN, serum
creatinine, liver function tests, blood glucose, CBC

Interventions
• Monitor urine or serum glucose levels frequently to determine effectiveness of
drug and dosage being used.
• Transfer to insulin therapy during periods of high stress (eg infections, surgery,
trauma).
• Use IV glucose if severe hypoglycemia occurs as a result of overdose.
• Arrange for consultation with dietitian to establish weight-loss program and
dietary control.
• Arrange for thorough diabetic teaching program, including disease, dietary
control, exercise, signs and symptoms of hypoglycemia and hyperglycemia,
avoidance of infection, hygiene.

Teaching points
• Take this drug once a day with breakfast or the first main meal of the day.
• Do not discontinue this drug without consulting your health care provider;
continue with diet and exercise program for diabetes control.
• Monitor urine or blood for glucose and ketones as prescribed.
• Do not use this drug if you are pregnant.
• Avoid alcohol while using this drug.
• Report fever, sore throat, unusual bleeding or bruising, rash, dark urine, light-
colored stools, hypoglycemic or hyperglycemic reactions.

Adverse effects in Italic are most common; those in Bold are life-threatening.

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