glimepiride

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Protein Binding: 99.5%.

Metabolism/Excretion: Mostly metabolized by the liver; one metabolite has hypoglycemic activity.

Half-Life: 5–9.2 hr.

Time/Action Profile ⬆ ⬇

(hypoglycemic activity)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2–3 hr	24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Hypersensitivity to sulfonamides (cross-sensitivity may occur);
Type 1 diabetes;
Diabetic coma or ketoacidosis;
Uncontrolled infection, serious burns, or trauma.

Use Cautiously in:

Severe cardiovascular or hepatic disease;
Glucose 6-phosphate dehydrogenase deficiency (↑ risk of hemolytic anemia);
Severe renal impairment (↑ risk of hypoglycemia);
Infection, stress, or changes in diet may alter requirements for control of blood sugar;
Impaired thyroid, pituitary, or adrenal function;
Malnutrition, high fever, prolonged nausea, or vomiting;
OB: Crosses the placenta and risk of neonatal hypoglycemia; should be discontinued 2 wk before delivery; insulin recommended during pregnancy;
Lactation: May risk of hypoglycemia in infant; use while breastfeeding only if maternal benefit justifies potential risk to infant;
Pedi: Not recommended for use in children because weight and risk of hypoglycemia;
Geri: Appears on Beers list. risk of prolonged hypoglycemia in older adults. Avoid use as first- or second-line monotherapy or as add-on treatment in older adults unless there are significant barriers to the use of safer and more effective agents. If a sulfonylurea must be used, glipizide is preferred.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: photosensitivity, rash

Endo: hypoglycemia

F and E: hyponatremia

GI: constipation, cramps , diarrhea, dyspepsia, hepatitis, nausea, vomiting

Hemat: hemolytic anemia, thrombocytopenia

Metab: ↑appetite

Neuro: dizziness, drowsiness, headache, weakness

Interactions ⬆ ⬇

Drug-drug:

Ingestion of alcohol may result in disulfiram-like reaction.
Effectiveness may be ↓ by concurrent use of diuretics, corticosteroids, phenothiazines, oral contraceptives, estrogens , thyroid preparations , phenytoin, sympathomimetics, and isoniazid.
Alcohol, androgens (testosterone), chloramphenicol,clarithromycin, disopyramide, fluoroquinolones, fluoxetineMAO inhibitors, NSAIDs (except diclofenac), salicylates, and warfarin may ↑ risk of hypoglycemia.
Concurrent use with warfarin may alter the response to both agents (↑ effects of both initially, then ↓ activity); close monitoring recommended during any changes in dose.
Beta-blockers may mask the signs and symptoms of hypoglycemia.
May ↑ cyclosporine levels.
Colesevelam may ↓ effects; administer glimepiride ≥4 hr before colesevelam.

Route/Dosage ⬆ ⬇

PO (Adults ): 1–2 mg once daily initially; may ↑ every 1–2 wk up to 8 mg/day (usual range 1–4 mg/day).

Availability ⬆ ⬇

(Generic available)

Tablets: 1 mg; 2 mg; 4 mg
In combination with: pioglitazone (Duetact). See Appendix [not included in this PDA edition].

Assessment ⬆ ⬇

Observe patient for signs and symptoms of hypoglycemic reactions (sweating, hunger, weakness, dizziness, tremor, tachycardia, anxiety). Patients on concurrent beta-blocker therapy may have very subtle signs of hypoglycemia.
Assess patient for allergy to sulfonamides.

Lab Test Considerations:

Monitor serum glucose and glycosylated hemoglobin (HbA_1C) periodically during therapy to evaluate effectiveness.
- Monitor CBC periodically during therapy. Report ↓ blood counts promptly.
- May cause an ↑ in AST, ALT, LDH, BUN, and serum creatinine.

Toxicity and Overdose:

Overdose is manifested by symptoms of hypoglycemia. Mild hypoglycemia may be treated with administration of oral glucose. Severe hypoglycemia should be treated with IV D50W followed by continuous IV infusion of 10% glucose solution at a rate sufficient to keep serum glucose at approximately 100 mg/dL.

Implementation ⬆ ⬇

Accidental administration of oral hypoglycemic agents to nondiabetic adults and children has resulted in serious harm or death. Before administering, confirm that patient has type 2 diabetes.
Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.
- To convert from other oral hypoglycemic agents, gradual conversion is not required.
PO: May be administered once in the morning with breakfast or the main meal.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication at same time each day. Take missed doses as soon as remembered unless almost time for next dose. Do not take if unable to eat.
Explain to patient that this medication controls hyperglycemia but does not cure diabetes. Therapy is long term.
Review signs of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to drink a glass of orange juice or ingest 2–3 tsp of sugar, honey, or corn syrup dissolved in water or an appropriate number of glucose tablets and notify health care professional.
Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hypoglycemic or hyperglycemic episodes.
Instruct patient in proper testing of serum glucose and ketones. These tests should be closely monitored during periods of stress or illness and health care professional notified if significant changes occur.
Concurrent use of alcohol may cause a disulfiram-like reaction (abdominal cramps, nausea, flushing, headaches, and hypoglycemia).
May occasionally cause dizziness or drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Caution patient to avoid other medications, especially aspirin and alcohol, while on this therapy without consulting health care professional.
Caution patient to use sunscreen and protective clothing to prevent photosensitivity reactions.
Advise patient to inform health care professional of medication regimen prior to treatment or surgery.
Advise patient to notify health care professional promptly if unusual weight gain, swelling of ankles, drowsiness, shortness of breath, muscle cramps, weakness, sore throat, rash, or unusual bleeding or bruising occurs.
Advise patient to carry a form of sugar (sugar packets, candy) and identification describing disease process and medication regimen at all times.
Rep: Insulin is the recommended method of controlling blood sugar during pregnancy. Counsel female patients to use a form of contraception other than oral contraceptives and to notify health care professional promptly if pregnancy is planned or suspected or if breastfeeding. Neonates of women with gestational diabetes who are treated with sulfonylureas during pregnancy may be at increased risk for hypoglycemia and respiratory distress.
Emphasize the importance of routine follow-up exams.

section name header

Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇