Pioglitazone
ACTOS
What it isPPAR-gamma agonist improving insulin sensitivity; type 2 diabetes.
Why this oneDurable A1c reduction with no hypoglycemia, and benefit in NAFLD and after stroke in insulin-resistant patients.
What limits itFluid retention and weight gain, and it precipitates heart failure. Bone fracture risk in women; onset takes weeks.
FDA-approved for
- type 2 diabetes (1999)
Off-label
- NASH
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Type 2 diabetes mellitus | Adult | 15 or 30 mg QD (15 mg QD if NYHA Class I/II HF) | Titrate by HbA1c | 45 mg QD (15 mg QD with strong CYP2C8 inhibitors, e.g., gemfibrozil) |
Renal Undefined
Hepatic Obtain liver tests before starting; initiate with caution if abnormal; do not start with active liver disease
Instructions
- Take once daily without regard to meals
- Obtain liver tests before initiation; monitor for signs of heart failure after initiation and dose increases
Contraindications
- Initiation in patients with established NYHA Class III or IV heart failure
Cautions
- Congestive heart failure/fluid retention (highest risk with insulin)
- Hypoglycemia with insulin or insulin secretagogues
- Postmarketing hepatic failure reports
- Bladder cancer — do not use in active bladder cancer
- Dose-related edema
- Increased fracture incidence in females
- Macular edema
Adverse reactions
- Upper respiratory tract infection
- Headache
- Sinusitis
- Myalgia
- Pharyngitis
- Edema
- Weight gain
- Hypoglycemia (combination use)
Pregnancy Limited data; poorly controlled diabetes carries risk; may induce ovulation in anovulatory women.
Lactation No information on presence in human milk.
⚠ BOXED WARNING
- Congestive heart failure
Cost, est. cash$5–$150/month
Generic entry2012
Classes and tags
Clinical profile
Legacy pregnancy categoryMultiple / indication-, trimester- or formulation-dependent
Defining liabilityAgent-specific hypoglycemia, ketoacidosis, volume, renal or gastrointestinal toxicity.
Mechanism of action: Pioglitazone ballicule
Open Pioglitazone in the interactive console ↗
Memory aids: mascots and interaction avatars
