Names and pronunciation
(re-pag′lih′nide) Gluconorm
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Drug reference
(re-pag′lih′nide) Gluconorm
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Func. class.: Antidiabetic
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Chem. class.: Meglitinide
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ACTION: Causes functioning β-cells in pancreas to release insulin, thereby leading to a drop in blood glucose levels; closes ATP-dependent potassium channels in the β-cell membrane; this leads to the opening of calcium channels; increased calcium influx induces insulin secretion
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USES: Type 2 diabetes mellitus
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CONTRAINDICATIONS: Hyper sensitivity to meglitinides; diabetic ketoacidosis, type 1 diabetes Precautions: Pregnancy, breastfeeding, children, geriatric patients, thyroid/car- diac disease, severe renal/hepatic dis- ease, severe hypoglycemic reactions
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SIDE EFFECTS CNS: Headache, weakness, paresthesia CV: Angina EENT: Tinnitus, sinusitis ENDO: Hypoglycemia GI: Nausea, vomiting, diarrhea, constipa- tion, dyspepsia, pancreatitis INTEG: Rash, allergic reactions MISC: Chest pain, UTI, allergy MS: Back pains, arthralgia RESP: URI, sinusitis, rhinitis, bronchitis
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INTERACTIONS • Do not use with gemfibrozil, isophane insulin (NPH) Increase: repaglinide effect—CYP3A4, OATP101, CYP2C9 inhibitors Increase: in both—levonorgestrel/ethi- nyl estradiol Increase: repaglinide metabolism— CYP3A4 inducers: rifAMPin, barbiturates, carBAMazepine Increase: repaglinide effect—NSAIDs, salicylates, sulfonamides, chloramphenicol, MAOIs, coumarins, β-blockers, probene- cid, gemfibrozil, simvastatin, fenofibrate, deferasirox Decrease: repaglinide metabolism—CYP3A4 inhibitors: antifungals (ketoconazole, micon- azole), erythromycin, macrolides Decrease: repaglinide action—calcium channel blockers, corticosteroids, oral contraceptives, thiazide diuretics, thyroid preparations, estrogens, phenothiazines, phenytoin, rifAMPin, isoniazid, PHENo- barbital, sympathomimetics Drug/Herb Increase: antidiabetic effect—garlic, chromium, horse chestnut Drug/Food Decrease: repaglinide level; give before meals Decrease: repaglinide metabolism— grapefruit juice Drug/Lab Test Increase/decrease: glucose
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TREATMENT OF OVERDOSE: Glucose 25 g IV via dextrose 50% solution, 50 mL or 1 mg glucagon
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DOSAGE AND ROUTES • Adult: PO 0.5-4 mg with each meal, max 16 mg/day; adjust at weekly inter- vals; oral hypoglycemic–naïve patients or patients with A1c <8% should start with 0.5 mg with each meal Renal/hepatic dose • Adult: PO CCr 20-39 mL/min, 0.5 mg/ day; titrate upward cautiously
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Available forms: Tabs 0.5, 1, 2 mg
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Administer: • Up to 15-30 min before meals; 2, 3, or 4×/day preprandially • Skip dose if meal skipped; add dose if meal added • Store in tight container at room tem- perature • May be added to metFORMIN for bet- ter control
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Assess: • Hypo/hyperglycemic reaction, which can occur soon after meals: dizziness, weakness, headache, tremors, anxiety, tachycardia, hunger, sweating, abdominal pain, A1c, fasting, postprandial glucose during treatment • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk, usually insu- lin is used in pregnancy; do not breast- feed, excretion unknown
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Evaluate: • Therapeutic response: decrease in polyuria, polydipsia, polyphagia; clear sensorium; absence of dizziness; stable gait; blood glucose, A1c improvement Teach family/patient: • About technique for blood glucose mon- itoring; how to use blood glucose meter • About the symptoms of hypo/hypergly- cemia, what to do about each • That product must be continued on daily basis; about the consequences of discontinuing product abruptly • To avoid OTC medications unless or- dered by prescriber; not to use alcohol • That diabetes is a lifelong illness; that product will not cure disease • That all food included in diet plan must be eaten to prevent hypoglycemia; that if a meal is omitted, dose should be omitted; to have glucagon emergency kit available; to take repaglinide 15-30 min before meals 2, 3, or 4×/day; to carry emergency ID
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CLINICAL CONSIDERATIONS
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PHARMACOKINETICS Completely absorbed by GI route; onset 30 min; peak 1 hr; duration <4 hr; half- life 1 hr; metabolized in liver by CYP3A4; excreted in urine, feces (metabolites); crosses placenta; 98% protein bound
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• Adult: PO 0.5-4 mg with each meal, max 16 mg/day; adjust at weekly inter- vals; oral hypoglycemic–naïve patients or patients with A1c <8% should start with 0.5 mg with each meal Renal/hepatic dose
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• Adult: PO CCr 20-39 mL/min, 0.5 mg/ day; titrate upward cautiously
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