Pioglitazone
Pioglitazone
Actos
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Summary
Pharmacy
Starting dose
15-30 mg PO once daily; titrate to 45 mg
Preparations
15, 30, 45 mg tablets
US FDA Max
45 mg/d
Pharmacology
Routes
Oral
Onset
HbA1c effect at 12-16 weeks (slower than other classes)
Duration
24 hours
Half-life
~3-7 hours (parent); 16-24 hours including active metabolites[1]
Bioavailability
High (oral; absorption not affected by food)[1]
Pregnancy
Limited data; switch to insulin where feasible.[citation needed]
Legal status
Purported mechanism
Pioglitazone is a selective agonist of peroxisome proliferator-activated receptor γ (PPAR-γ); the activated receptor remodels transcription of adipocyte differentiation, lipid storage, and insulin-sensitivity genes, lowering insulin resistance with effects on free fatty acid handling, adiponectin secretion, and inflammatory tone.0 Mechanism is insulin-sensitizing rather than insulin-secretagogue, so monotherapy hypoglycemia risk is low. Characteristic adverse effects: fluid retention (HF precipitation), weight gain, distal bone fracture risk (especially in women), and a small bladder cancer signal historically debated; benefit in NASH/MASH and the IRIS trial's stroke recurrence benefit in insulin-resistant non-diabetics keep pioglitazone clinically interesting[1].
References
- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Actos (pioglitazone HCl), Takeda, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021073s055lbl.pdf