rosiglitazone

Absorption: Well absorbed (99%) following oral administration.

Distribution: Unknown.

Protein Binding: 99.8% bound to plasma proteins.

Metabolism/Excretion: Entirely metabolized by the liver.

Half-life: 3.2–3.6 hr (↑ in liver disease).

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity
Diabetic ketoacidosis
NYHA class II or III HF
Clinical evidence of active liver disease or increased ALT (>2.5 times upper limit of normal)
Renal dysfunction (SCr >1.5 mg/dL in males or 1.4 mg/dL in females
Pedi: Safety and effectiveness not established.

Use Cautiously in:

Edema
Concurrent use with insulin (may ↑ risk of adverse cardiovascular reactions)
Hepatic impairment
OB: Use only if potential maternal benefit justifies potential fetal risk
Lactation: Use only if potential maternal benefit justifies potential risk to infant
Rep: May restore ovulation and risk of pregnancy in premenopausal women
Geri: Dose ↓ and careful titration recommended due to age-related ↓ in renal function. Avoid maximum dose. Should not be given to patients >80 yr.

Adv. Reactions/Side Effects ⬆ ⬇

CV: HF, edema.

Derm: urticaria.

EENT: new onset and worsening diabetic macular edema.

GI: hepatitis, ↑ liver enzymes.

Hemat: anemia.

Metab: ↑total cholesterol, LDL and HDL, weight gain.

Neuro: STROKE.

Misc: ANGIOEDEMA, fractures (arm, hand, foot) in female patients.

Interactions ⬆ ⬇

Drug-Drug:

Concurrent use with rifampin↓ levels and may ↓ effectiveness.
Gemfibrozil↑ levels and may ↑ risk of hypoglycemia (↓ dose of rosiglitazone).
Concurrent use with insulin may ↑ risk of fluid retention and worsening HF

Drug-Natural Products:

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

Route/Dosage ⬆ ⬇

PO (Adults): 4 mg once daily or 2 mg twice daily; after 8 wk, may be ↑ if necessary to 8 mg once daily or 4 mg twice daily.

Implementation ⬆ ⬇

Do not confuse Avandia (rosiglitazone) with Prandin (repaglinide) or Coumadin (warfarin).
Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.
PO: May be administered with or without meals.

US Brand Names ⬆ ⬇

Classifications ⬆ ⬇

Therapeutic Classification: antidiabetics

Pharmacologic Classification: thiazolidinediones

Availability ⬆ ⬇

Tablets: 2 mg; 4 mg; 8 mg;

Time/Action Profile ⬆ ⬇

(effects on blood glucose)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	unknown	12–24 hr

Assessment ⬆ ⬇

Observe patient taking concurrent insulin for signs and symptoms of hypoglycemia (sweating, hunger, weakness, dizziness, tremor, tachycardia, anxiety).
Assess patient for edema and signs of HF (dyspnea, rales/crackles, peripheral edema, weight gain, jugular venous distention). May require discontinuation of rosiglitazone.

Lab Test Considerations:

Monitor serum glucose and glycosylated hemoglobin periodically during therapy to evaluate effectiveness.
- Monitor CBC with differential periodically during therapy. May cause ↓ in hemoglobin, hematocrit, and WBC, usually during the first 4–8 wk of therapy; then levels stabilize.
- Monitor AST and ALT prior to initiating therapy and periodically thereafter or if jaundice or symptoms of hepatic dysfunction occur. May cause irreversible ↑ in AST and ALT or hepatic failure (rare). If ALT increases to >3 times the upper limit of normal, recheck ALT promptly. Discontinue rosiglitazone if ALT remains >3 times normal.
- May cause ↑ in total cholesterol, LDL, and HDL and ↓ in free fatty acids.
- Monitor renal function tests prior to initiating therapy and periodically thereafter (BUN, creatinine, creatinine clearance), especially in older adults.

Pot. Nursing Diagnoses ⬆ ⬇

Imbalanced nutrition: more than body requirements (Indications).

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication as directed. If dose for 1 day is missed, do not double dose the next day.
Explain to patient that this medication controls hyperglycemia but does not cure diabetes. Therapy is long term.
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.
Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hypoglycemic or hyperglycemic episodes.
Instruct patient in proper testing of serum glucose and ketones. These tests should be closely monitored during periods of stress or illness and health care professional notified if significant changes occur.
Advise patient to notify health care professional immediately if signs of hepatic dysfunction (unexplained nausea, vomiting, abdominal pain, fatigue, anorexia, dark urine) or HF 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.
Advise patient to inform health care professional of medication regimen prior to treatment, studies using IV contrast, or surgery.
Advise patient to carry a form of sugar (sugar packets, candy) and identification describing disease process and medication regimen at all times.
Rep: Insulin is the preferred method of controlling blood glucose during pregnancy. Counsel females of reproductive potential that higher doses of oral contraceptives or a form of contraception other than oral contraceptives may be required and to notify health care professional promptly if pregnancy is planned or suspected or if breastfeeding. May result in unintended pregnancy in some premenopausal anovulatory women due to its effect on ovulation.
Emphasize the importance of routine follow-up exams.

section name header

Pronunciation ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇