repaglinide

Absorption: Well absorbed (56%) following oral administration.

Distribution: Unknown.

Protein Binding: >98%.

Metabolism/Excretion: Mostly metabolized by the liver; metabolites are excreted primarily in feces.

Half-Life: 1 hr.

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
PO	within 30 min	60–90 min	<4 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Diabetic ketoacidosis;
Type 1 diabetes;
Concurrent use of gemfibrozil;
Lactation: Lactation.

Use Cautiously in:

Hepatic impairment (longer dosing intervals may be necessary);
Severe renal impairment (dose ↓ recommended);
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Pedi: Safety and effectiveness not established in children;
Geri: Consider age-related ↓ in renal/hepatic/cardiovascular function.

Adv. Reactions/Side Effects ⬆ ⬇

CV: angina, chest pain

Endo: hypoglycemia

Interactions ⬆ ⬇

Drug-drug:

Ketoconazole, miconazole, gemfibrozil, itraconazole, clarithromycin, and erythromycin may ↓ metabolism and ↑ risk of hypoglycemia; concurrent use with gemfibrozil contraindicated.
Levels and effects may also be ↑ by NSAIDs, clopidogrel, cyclosporine, hormonal contraceptives, simvastatin, sulfonamides, chloramphenicol, warfarin, probenecid, deferasirox, MAO inhibitors, and beta blockers; avoid concurrent use with clopidogrel, if possible (if not possible, ↓ dose of repaglinide).
Effects may be ↓ by corticosteroids, phenothiazines, thyroid preparations, estrogens, hormonal contraceptives, phenytoin, nicotinic acid, sympathomimetics, isoniazid, and calcium channel blockers.

Drug-Natural Products:

Glucosamine may worsen blood glucose control.
Chromium and coenzyme Q-10 may produce ↑ hypoglycemic effects.

Route/Dosage ⬆ ⬇

PO (Adults ): 0.5–4 mg taken before meals (not to exceed 16 mg/day); Concurrent use with cyclosporine: Not to exceed 6 mg/day;Concurrent use with clopidogrel: Initiate at 0.5 mg taken before meals (not to exceed 4 mg/day).

Renal Impairment

PO (Adults ): Severe renal impairment: Start with 0.5 mg/day and titrate carefully.

Availability ⬆ ⬇

(Generic available)

Tablets: 0.5 mg; 1 mg; 2 mg

Assessment ⬆ ⬇

Observe patient for signs and symptoms of hypoglycemic reactions (abdominal pain, sweating, hunger, weakness, dizziness, headache, tremor, tachycardia, anxiety). Hypoglycemia may be difficult to recognize in geriatric patients and in patients taking beta blockers. Hypoglycemia is more likely to occur with insufficient caloric intake, following intense prolonged exercise, or when alcohol or more than 1 hypoglycemic agent is used.

Lab Test Considerations:

Monitor fasting serum glucose and glycosylated hemoglobin periodically during therapy to evaluate effectiveness.

Implementation ⬆ ⬇

Do not confuse repaglinide with rasagiline.
Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin. Withhold repaglinide and reinstitute after resolution of acute episode.
- Repaglinide therapy should be temporarily discontinued for patients requiring surgery involving restricted intake of food and fluids.
- There is no fixed dose of repaglinide. Dose is based on periodic monitoring of blood glucose and long-term response is based on glycolysated hemoglobin levels. If adequate response is not achieved, metformin may be added to regimen. If combination therapy is unsuccessful, oral hypoglycemic therapy may need to be discontinued and replaced with insulin.
- When replacing other oral hypoglycemic agents, repaglinide may be started on the day following discontinuation of the other agent. Monitor blood glucose closely. Discontinuation of long-acting oral hypoglycemics may require monitoring for a wk or more.
- Short-term repaglinide therapy may be used for patients well controlled with diet experiencing transient loss of control.
PO: Administer up to 30 min before meals. Patients who skip a meal or add an extra meal should skip or add a dose, respectively, for that meal.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take repaglinide before each meal, exactly as directed.
Explain to patient that repaglinide helps control hyperglycemia but does not cure diabetes. Therapy is usually long term.
Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hyperglycemic or hypoglycemic episodes.
Review signs of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to take a glass of orange juice or 2–3 tsp of sugar, honey, or corn syrup dissolved in water, and notify health care professional.
Instruct patient in proper testing of blood glucose. These tests should be monitored closely during periods of stress or illness and a health care professional notified if significant changes occur.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications and alcohol.
Advise patient to inform health care professional of medication regimen prior to treatment or surgery.
Rep: Insulin is the recommended method of controlling blood glucose 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 and to avoid breastfeeding; may cause infant hypoglycemia.
Advise patient to carry a form of sugar (sugar packets, candy) and identification describing disease process and medication regimen at all times.
Emphasize the importance of routine follow-up exams and regular testing of blood glucose and glycosylated hemoglobin.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇