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Pioglitazone

Antidiabeticprescriptionoral · inferred

Thiazolidinedione (TZD) PPAR-gamma agonist improving insulin sensitivity in type 2 diabetes. Active metabolites contribute substantially to effect and extend apparent half-life to 16-24 hours. Typical 15-45 mg once daily. PROactive and IRIS trials suggest cardiovascular and stroke benefit; concerns include weight gain, edema, heart failure, and fracture risk.

Projected serum levels — 30 mg, once daily

Pioglitazone
Pioglitazone modeled serum levels, 30 mg once daily over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 1 days. 0 6.3 12.5 18.8 25 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 1

Maintenance schedule: 30 mg once daily (oral).

Modeled steady state after ~1 days: peak ≈ 20.2 mg, trough ≈ 1.1 mg body load. Population-based estimate over 15 days for a 30 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category
Antidiabetic
Route modeled
Oral
Model confidence
inferred
Half-life
5 h
Common dose
30 mg
Suggested maximum
45 mg/day
Reference dose range
15–45 mg (single dose)
Suggested cadence
once daily
Validated against
30 mg oral — Cmax 1 mg/L at 2 h

Documented interactions

  • danger
    Clopidogrel (Plavix) + Pioglitazone CYP inhibition

    Clopidogrel (Plavix) reversible_inhibitor of CYP2C8 predicted to change Pioglitazone AUC by ~2.07x

  • danger
    Efavirenz (Sustiva) + Pioglitazone CYP induction

    Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Pioglitazone AUC by ~0.40x

  • danger
    Levothyroxine (Synthroid) + Pioglitazone Protein binding

    Pioglitazone may displace Levothyroxine (Synthroid) from plasma protein binding sites, transiently raising free drug concentration. This drug has a narrow therapeutic index; free concentration…

  • danger
    Montelukast (Singulair) + Pioglitazone CYP inhibition

    Montelukast (Singulair) reversible_inhibitor of CYP2C8 predicted to change Pioglitazone AUC by ~2.07x

  • danger
    Quercetin + Pioglitazone CYP inhibition

    Quercetin reversible_inhibitor of CYP2C8 predicted to change Pioglitazone AUC by ~2.07x

  • danger
    Rifampin + Pioglitazone CYP induction

    Rifampin inducer of CYP3A4 predicted to change Pioglitazone AUC by ~0.40x

Serum checks 340 modeled interaction pairings for pioglitazone across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. Secondary prevention of macrovascular events in patients with type 2 diabetes in the PROactive Study (PROspective pioglitAzone Clinical Trial In macroVascular Events) Dormandy JA et al. · Lancet, 2005 DOI

    PROactive RCT of 5238 T2D patients with macrovascular disease showed pioglitazone reduced the main secondary composite of death/MI/stroke by 16% over 2.85 years.

  2. Pioglitazone after Ischemic Stroke or Transient Ischemic Attack (IRIS) Kernan WN et al. · New England Journal of Medicine, 2016 DOI

    IRIS RCT of 3876 insulin-resistant non-diabetic patients with recent stroke/TIA showed pioglitazone reduced stroke or MI by 24% over 4.8 years vs placebo.

  3. Clinical pharmacokinetics of pioglitazone Eckland DA, Danhof M · Experimental and Clinical Endocrinology & Diabetes, 2000 DOI

    PK review characterizing pioglitazone's ~85% oral bioavailability, parent half-life 3-7 hours, and active metabolite half-lives of 16-24 hours that dominate steady-state exposure.

3 published studies referenced in the app, each with a plain-language summary.