Names and pronunciation
(pie-oh-glye′ta-zone) Actos
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Individual generic drug information
Extracted information for pioglitazone only.
(pie-oh-glye′ta-zone) Actos
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Func. class.: Antidiabetic, oral
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Chem. class.: Thiazolidinedione
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Do not confuse: Actos/Actonel
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ACTION: Specifically targets insulin resistance; an insulin sensitizer; regulates the transcription of a number of insulin- responsive genes
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USES: Type 2 diabetes mellitus
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Extracted information for pioglitazone only.
CONTRAINDICATIONS: Breast feeding, children, hypersensitivity to thia- zolidinedione, diabetic ketoacidosis, dia- betes mellitus, type 1, serious hepatic disease
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Black Box Warning: NYHA Class III/IV heart failure Precautions: Pregnancy, geriatric patients, geriatric patients with CV disease, renal/hepatic/thyroid dis- ease, edema, polycystic ovary syn- drome, bladder cancer, osteoporosis, pulmonary disease, secondary malignancy Black Box Warning: Heart failure: do not use in NYHA Class III/IV; excessive/ rapid weight gain >5 lb, dyspnea, edema; may need to be reduced or discontinued; monitor daily weights • Bladder cancer: avoid use in a history of bladder cancer; use of pioglitazone >1 yr has shown an increase in bladder cancer • Hypoglycemic reactions: sweating, weakness, dizziness, anxiety, tremors, hunger; hyperglycemic reactions soon after meals (rare); may occur more often with insulin or other antidiabetics • Hepatic disease: check LFTs periodi- cally: AST, LDH; do not start treatment in active heart disease or if ALT >2.5× upper limit of normal; if treatment has already begun, follow closely with continuing ALT levels; if ALT increases to >3× upper limit of normal, recheck ALT as soon as possible; if ALT remains >3× upper limit of normal, discontinue • FBS, glycosylated HbA1c, plasma lip- ids/lipoproteins, B/P, body weight during treatment • Fracture: Assess fall risk, fracture risk, diet, activity level • CBC with differential before and during therapy; more necessary in those with anemia; Hct/HB (may be decreased in first few months of treatment) • Beers: avoid use in older adults; may promote fluid retention and/or exacer- bate 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: Headache CV: MI, heart failure, death (geriatric patients) ENDO: Hypo/hyperglycemia MISC: Sinusitis, upper respiratory tract infection, pharyngitis, hepato- toxicity, edema, weight gain, anemia, macular edema; risk of bladder cancer (use >1 yr), peripheral/pulmonary edema MS: Rhabdomyolysis, fractures (females), myalgia
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INTERACTIONS Decrease: effect of atorvastatin Decrease: effect of oral contracep- tives; use alternative contraceptive method Decrease: pioglitazone effect—CYP2C8 inducers (ketoconazole, fluconazole, itraconazole, miconazole, voriconazole) Drug/Herb Increase: hypoglycemia—garlic, green tea, horse chestnut Drug/Lab Test Increase: CPK, LFTs, HDL, cholesterol Decrease: glucose, Hct/HB
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Extracted information for pioglitazone only.
DOSAGE AND ROUTES Monotherapy • Adult: PO 15 or 30 mg/day, may increase to 45 mg/day; with strong CYP2C8, max 15 mg/day; with NYHA class I/II heart failure, max 15 mg/ day Combination therapy • Adult: PO 15 or 30 mg/day with a sulfonylurea, metFORMIN, or insulin; decrease sulfonylurea dose if hypogly- cemia occurs; decrease insulin dose by 10%-25% if hypoglycemia occurs or if plasma glucose is <100 mg/dL, max 45 mg/day Hepatic dose • Do not use in active hepatic disease or if ALT >2.5 times ULN
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Available forms: Tabs 15, 30, 45 mg
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Administer: • Once a day; without regard to meals • Tabs crushed and mixed with food or fluids for patients with difficulty swal- lowing
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Extracted information for pioglitazone only.
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 self-monitor using a 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 or herbal preparations unless approved by prescriber • That diabetes is a lifelong illness; that product is not a cure, it only controls symptoms • To report symptoms of hepatic dys- function: nausea, vomiting, abdominal pain, fatigue, anorexia, dark urine, jaundice • To report weight gain, edema, chest pain, palpitations, dyspnea • That lab work, eye exams will be needed periodically • To notify prescriber if oral contracep- tives are used, effect may be decreased; not to use product if breastfeeding
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Extracted information for pioglitazone only.
PHARMACOKINETICS Maximal reduction in FBS after 12 wk; half-life 3-7 hr, terminal 16-24 hr; pro- tein binding >99%
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Filter the extracted dose blocks for this individual drug.
Monotherapy
• Adult: PO 15 or 30 mg/day, may increase to 45 mg/day; with strong CYP2C8, max 15 mg/day; with NYHA class I/II heart failure, max 15 mg/ day Combination therapy
Candidate age grouping · source page 1054
Monotherapy
• Adult: PO 15 or 30 mg/day with a sulfonylurea, metFORMIN, or insulin; decrease sulfonylurea dose if hypogly- cemia occurs; decrease insulin dose by 10%-25% if hypoglycemia occurs or if plasma glucose is <100 mg/dL, max 45 mg/day Hepatic dose
Candidate age grouping · source page 1054