Rosiglitazone Maleate / Glimepiride
Pronouncation: (ROE-zi-GLI-ta-zone MAL-ee-ate/glye-MEP-i-ride)Class: Antidiabetic combination
Trade Names:
Avandaryl
- Tablets rosiglitazone 4 mg/glimepiride 1 mg
- Tablets rosiglitazone 4 mg/glimepiride 2 mg
- Tablets rosiglitazone 4 mg/glimepiride 4 mg
- Tablets rosiglitazone 8 mg/glimepiride 2 mg
- Tablets rosiglitazone 8 mg/glimepiride 4 mg
Pharmacology
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Rosiglitazone, a thiazolidinedione, increases insulin sensitivity in the liver, skeletal muscle, and adipose tissues. Glimepiride, a sulfonylurea, stimulates insulin release from functioning pancreatic beta cells.
Indications and Usage
Adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes when treatment with dual rosiglitazone and glimepiride therapy is appropriate.
Contraindications
Diabetic ketoacidosis with or without coma; known hypersensitivity to any component of the product; established New York Heart Association class III or IV heart failure.
Dosage and Administration
AdultsPO Initial: rosiglitazone 4 mg/glimepiride 1 mg or rosiglitazone 4 mg/glimepiride 2 mg once daily. Titrate to clinical response (max, rosiglitazone 8 mg/glimepiride 4 mg).
Elderly, Debilitated, or Malnourished Patients or Patients With Adrenal, Hepatic, or Renal Function ImpairmentInitial dosing, dose increments, and maintenance dosage should be conservative to avoid hypoglycemia.
Switching from Separate Doses of Rosiglitazone and Glimepiride to Combined TherapyAdults
PO Usual starting dose is the dose of rosiglitazone and glimepiride already being taken.
Patients Previously Treated With Thiazolidinedione Monotherapy and Switching to Combined TherapyAdults
PO Dose titration can occur at 1- to 2-wk intervals by increasing the glimepiride component by no more than 2 mg increments.
Patients Previously Treated With Sulfonylurea Monotherapy and Switching to Combined TherapyAdults
PO Full effect of rosiglitazone component on glucose reduction may take 2 to 3 months to develop. Titration of the rosiglitazone component is recommended if patients are not adequately controlled after 8 to 12 wk. Observe patients for 1 to 2 wk for hypoglycemia when being transferred from longer half-life sulfonylureas (eg, chlorpropamide) because of potential overlapping drug effect. Dosage titration of the rosiglitazone component is recommended if patient is not adequately controlled after 2 to 3 months. Increases in rosiglitazone dose should be accompanied by careful monitoring for adverse reactions related to fluid retention.
Hepatic Function ImpairmentAdults
PO Treatment should not be initiated in patients exhibiting evidence of active liver disease or increased serum transaminase levels (ALT greater then 2.5 times ULN at the start of therapy).
General Advice
- Administer once daily with first meal of the day.
- If hypoglycemia occurs during up-titration of dose or while on maintenance therapy, reduce dose of glimepiride component.
Storage/Stability
Store tablets at 59° to 86°F. Protect from light.
Drug Interactions
AlcoholDisulfiram-like reactions (eg, breathlessness, facial flushing, headache) may occur.
Ciprofloxacin, gatifloxacinSevere and persistent hypoglycemia may occur.
CYP2C8 inducers (eg, rifampin)May reduce rosiglitazone plasma levels, decreasing the pharmacologic effects.
CYP2C8 inhibitors (eg, azole antifungal agents [ketoconazole], fluvoxamine, gemfibrozil, trimethoprim)May elevate rosiglitazone plasma levels, increasing the pharmacologic effects and adverse reactions.
Drugs that cause hyperglycemia (eg, corticosteroids, diuretics, estrogens, isoniazid, nicotinic acid, oral contraceptives, phenothiazines, phenytoin, sympathomimetics, thyroid products)May lead to loss of glycemic control.
Drugs that cause hypoglycemia (eg, beta-adrenergic blockers, chloramphenicol, fluconazole, MAOIs, miconazole, NSAIDs, probenecid, salicylates, sulfinpyrazone, sulfonamides, urine acidifiers)May lead to loss of glycemic control.
InsulinRisk of edema may be increased, even after several months of combined therapy.
NevirapineNevirapine plasma concentrations may be reduced, decreasing efficacy.
Adverse Reactions
Cardiovascular
Hypertension (2%); CHF (1%).
CNS
Headache (6%).
EENT
Nasopharyngitis (5%).
Metabolic-Nutritional
Hypoglycemia (5%).
Miscellaneous
Edema (3%).
Precautions
WarningsCHFMay occur or be exacerbated. Observe patients for signs and symptoms of heart failure after starting therapy or increasing the dose. Manage heart failure according to current standards of care. Consider discontinuation or dose reduction if signs or symptoms occur. Use of drug is not recommended in patients with symptomatic heart failure. |
MonitorObtain periodic fasting blood glucose and hemoglobin A 1c (HbA 1c ) concentrations to monitor therapeutic response. Assess liver enzymes prior to initiation of therapy and periodically thereafter. Monitor all patients for signs and symptoms associated with fluid retention (eg, edema, heart failure). |
Pregnancy
Category C . Not recommended during pregnancy.
Lactation
Undetermined.
Children
Safety and efficacy not established.
Elderly
Particularly susceptible to hypoglycemic action.
Hepatic Function
Do not initiate therapy in patients with clinical evidence of active liver disease or baseline ALT more than 2.5 × ULN. Initiation or continuation of therapy in patients with mildly elevated liver enzymes (ALT less than 2.5 × ULN) should proceed with caution; discontinue therapy in these patients if ALT increases to more than 3 × ULN and persists.
Bone fractures
Increased incidence of bone fractures noted in women but not in men.
CV mortality
Has occurred in patients treated with oral hypoglycemic drugs.
Concomitant treatment with insulin
Safety and efficacy of rosiglitazone/glimepiride in combination with insulin not established; therefore, concomitant use is not recommended.
Edema
Rosiglitazone may cause fluid retention. Use with caution in patients with edema or at risk of heart failure.
Hematologic
Decreases in Hgb (1 g/dL or less), Hct (3.3% or less), and WBC have been reported in patients receiving rosiglitazone.
Hypoglycemia
May produce severe hypoglycemia. Debilitated or malnourished patients, and those with adrenal, pituitary, renal, or hepatic insufficiency, are particularly susceptible.
Macular edema
New-onset or worsening macular edema with decreased visual acuity has been reported rarely in patients receiving rosiglitazone.
Ovulation
Rosiglitazone therapy may result in resumption of ovulation in premenopausal anovulatory women with insulin resistance. Consider contraceptive measures in such patients.
Type 1 diabetes
Do not use in these patients.
Weight gain
Dose-related weight gain has been reported. Assess patients who experience unusually rapid increases in weight for fluid accumulation and volume-related events (eg, edema, heart failure).
Overdosage
Symptoms
Hypoglycemic reactions with coma, seizures, or other neurological impairment.
Patient Information
- Advise patient to review the patient information leaflet carefully before starting therapy and to reread and check for new information each time the medication is refilled.
- Advise patient to take prescribed dose with the first meal of the day.
- Advise patient that a reduction in blood glucose may be noted within days of starting therapy but that it may take 2 to 3 mo before the full effect is seen.
- Instruct patient that this drug is not a substitute for diet and exercise, and to follow prescribed regimens.
- Educate patient regarding type 2 diabetes and its management.
- Emphasize the importance of regular daily blood glucose monitoring and periodic HbA 1c tests. Ensure that patient knows their target values for both.
- Educate patient regarding potential long-term complications of diabetes and need for regular general physical and eye examinations.
- Advise patient to carry medical identification (eg, card, bracelet) of diabetes.
- Advise patient to report any of the following to health care provider immediately: abdominal pain, anorexia, dark urine, edema or swelling, fatigue, unexplained nausea and/or vomiting, unexplained shortness of breath, unusually rapid increase in weight, vision changes, or yellowing of the skin or eyes.
- Review symptoms of hypoglycemia and hyperglycemia and action plans to undertake if either occurs.
- Advise patient to discuss with health care provider a plan for managing each of the following situations: accidental administration of too little or too much medication, change in physical activity, dosing during intercurrent conditions (eg, infection, sick days, stress, trauma, vomiting), inadequate food intake or a skipped meal, missed doses, travel across time zones.
- Instruct patient to notify health care provider if experiencing hypoglycemic or hyperglycemic episodes.
- Advise patient that blood will be drawn to check liver function prior to starting therapy and then periodically thereafter.
- Advise patient to avoid unnecessary exposure to sunlight or tanning lamps and to use sunscreen and wear protective clothing to avoid photosensitivity reactions.
- Caution women that drug can cause resumption of ovulation in premenopausal anovulatory women with insulin resistance. Advise such women to discuss adequate contraceptive measures with health care provider.
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