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Pronunciation

pi-o-GLIT-a-zone

Classifications

Therapeutic Classification: antidiabetics

Pharmacologic Classification: thiazolidinediones

Indications

REMS


Action

  • Improves sensitivity to insulin by acting as an agonist at receptor sites involved in insulin responsiveness and subsequent glucose production and utilization.
  • Requires insulin for activity.
Therapeutic effects:
  • Decreased insulin resistance, resulting in glycemic control without hypoglycemia.

Pharmacokinetics

Absorption: Well absorbed following oral administration.

Distribution: Well distributed to tissues.

Protein Binding: >99%. Active metabolites are also highly (>99%) bound.

Metabolism/Excretion: Extensively metabolized by the liver via the CYP2C8 isoenzyme); at least two metabolites have pharmacologic activity. Primarily excreted in feces and urine as metabolites.

Half-Life: Pioglitazone: 3–7 hr; total pioglitazone (pioglitazone plus metabolites): 16–24 hr.

Time/Action Profile

(effects on blood glucose)

ROUTEONSETPEAKDURATION
PO30 min2–4 hr24 hr



Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: edema, HF

EENT: macular edema

GI: liver enzymes, LIVER FAILURE

GU: BLADDER CANCER

Hemat: anemia

MS: fractures (arm, hand, foot) (females), RHABDOMYOLYSIS

Interactions

Drug-drug:

Drug-Natural Products:

Route/Dosage

Availability

(Generic available)

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Actos

Pill Image

pioglitazone_195-8891.jpg
pioglitazone_195-8892.jpg

Code

NDC Code