Names and pronunciation
(ros-ih-glit′ah-zone) Avandia
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Drug reference
(ros-ih-glit′ah-zone) Avandia
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Func. class.: Antidiabetic, oral
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Chem. class.: Thiazolidinedione
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Do not confuse: rosiglitazone/pioglitazone Avandia/Prandia
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ACTION: Improves insulin resistance by hepatic glucose metabolism, insulin receptor kinase activity, insulin receptor phosphorylation
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USES: Type 2 diabetes mellitus, alone or in combination with sulfonylureas, metformin, insulin
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CONTRAINDICATIONS: Breast- feeding, children, hypersensitivity to thiazolidinediones, diabetic ketoacidosis, jaundice
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Black Box Warning: NYHA III, IV acute heart failure, heart failure Precautions: Pregnancy, geriatric patients, thyroid disease, renal/hepatic disease, MI, heart failure class I, II NYHA Black Box Warning: HF/MI: dyspnea, crackles, edema, weight gain ≥5 lb, jugular venous distention; may need to change dose or discontinue product; do not use in acute coronary syndrome, NYHA Class III/IV heart failure • Hypoglycemic reactions (sweating, weakness, dizziness, anxiety, tremors, hunger), hyperglycemic reactions soon after meals • Systemic reactions: anaphylaxis, Stevens-Johnson syndrome • Hepatotoxicity: LFTs periodically, AST, ALT (if ALT >2.5 × ULN, do not use product) • Diabetes: Fasting blood sugar, A1c, plasma lipids/lipoproteins, B/P, body weight during treatment • To use product provider/patient must be enrolled in the Avandia-Rosiglitazone Medicines Access Program • Beers: avoid in older adults; may pro- mote fluid retention or exacerbate heart failure • 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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SIDE EFFECTS CNS: Fatigue, headache CV: MI, HF, death (geriatric patients), edema ENDO: Hypo/hyperglycemia GI: Weight gain, hepatotoxicity, increase total LDL, HDL cholesterol; decrease free fatty acids, diarrhea MISC: Accidental injury, URI, sinusitis, anemia, back pain, diarrhea, edema, bone fractures (female), pulmonary/ macular/peripheral edema SYST: Anaphylaxis, Stevens-Johnson syndrome
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INTERACTIONS Increase: hypoglycemia—gemfibrozil, fluvoxaMINE, ketoconazole, trimethoprim; monitor glucose • Avoid concurrent use with insulin, ni- trates • May increase or decrease level: CYP2C5 inducer/inhibitors Drug/Herb Increase: antidiabetic effect—garlic, horse chestnut Drug/Lab Test Increase: ALT, HDL, LDL, total choles- terol, blood glucose Decrease: HB/Hct
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DOSAGE AND ROUTES • Adult: PO 4 mg/day or in 2 divided doses, may increase to 8 mg/day or in 2 divided doses after 12 wk; may be added to metFORMIN, sulfonylurea for adult dose
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Available forms: Tabs 2, 4, 8 mg
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Administer: • Conversion from other oral hypoglyce- mic agents if needed; change may be made without gradual dosage change; monitor blood glucose during conversion • Store in tight container in cool envi- ronment PO route • Once or in 2 divided doses, without regard to food • Tabs crushed and mixed with food or fluids for patients with difficulty swallow- ing
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Assess:
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Evaluate: • Therapeutic response: decrease in polyuria, polydipsia, polyphagia; clear sensorium; absence of dizziness; stable gait; blood glucose, A1c improvement
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To monitor blood glucose; that peri- odic liver function tests mandatory; to report edema, weight gain • About the symptoms of hypo/hypergly- cemia, what to do about each; that these symptoms are more likely to occur in those using insulin • That product must be continued on daily basis; about the consequences of discontinuing the product abruptly • To avoid OTC medications, herbal preparations, nitrates, or insulin unless approved by prescriber • That diabetes is lifelong; that product is not a cure, only controls symptoms • That all food included in diet plan must be eaten to prevent hypoglycemia • To carry emergency ID and glucagon emergency kit • To report symptoms of hepatic dys- function (nausea, vomiting, abdominal pain, fatigue, anorexia, dark urine, jaun- dice) immediately; to report macular edema (change in vision) • That 2 wk is needed to see reduction in blood glucose level and 2-3 mo needed to see full effect of product • To notify prescriber if oral contracep- tives are used • That a medication guide should be dispensed with each prescription/refill • Not to use if breastfeeding; may be secreted in breast milk
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PHARMACOKINETICS Maximal reductions in fasting blood sugar after 6-12 wk; protein binding 99.8%; excreted in urine, feces; elimination half- life 3-4 hr; may be excreted in breast milk
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• Adult: PO 4 mg/day or in 2 divided doses, may increase to 8 mg/day or in 2 divided doses after 12 wk; may be added to metFORMIN, sulfonylurea for adult dose
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