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pioglitazone (Rx)Brand and Other Names:Actos

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 15mg
  • 30mg
  • 45mg
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Type 2 Diabetes Mellitus

Indicated as monotherapy or with insulin or insulin secretagogues

15-30 mg PO with meal qDay initial; may increase dose by 15 mg with careful monitoring to 45 mg qDay maximum

Monitor ALT at start of treatment, qMonth for 12 months, q3Months thereafter

Dosing Considerations

Coadministration with insulin secretagogue (eg, sulfonylurea): Decrease insulin secretagogue dose

Coadministration with insulin: Decrease insulin dose by 10-25%

Coadministration with strong CYP2C8 inhibitors (eg, gemfibrozil): Limit maximum pioglitazone dose to 15 mg qDay

Not recommended

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Interactions

Interaction Checker

pioglitazone and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Edema when used in combination with sulfonylurea or insulin (<27%)

            Hypoglycemia (<27%)

            Upper respiratory infection (13%)

            1-10%

            Headache (9%)

            Heart failure (up to 8%)

            Sinusitis (6%)

            Fracture of bone (5%)

            Pharyngitis (5%)

            Myalgia (5%)

            Frequency Not Defined

            Aggravated diabetes

            Diabetic macular edema

            Hepatic failure (rare)

            Increased cholesterol

            Decreased serum triglycerides

            Hematocrit/hemoglobin

            Bladder cancer

            Decreased visual acuity

            Dyspnea

            Increased transaminases

            Pharyngitis

            Sinusitis

            Weight gain

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            Warnings

            Black Box Warnings

            Thiazolidinediones, including pioglitazone and rosiglitazone, cause or exacerbate congestive heart failure in some patients

            After initiation of these drugs, as well as after dose increases, observe patients carefully for signs and symptoms of heart failure (including excessive, rapid weight gain; dyspnea; and/or edema); if these signs or symptoms develop, the heart failure should be managed according to the current standards of care; furthermore, discontinuation or dose reduction of these drugs must be considered.

            These drugs are not recommended for patients with symptomatic heart failure; initiation of these drugs in patients with established NYHA class III or IV heart failure is contraindicated

            Contraindications

            Hypersensitivity to pioglitazone

            Diabetic ketoacidosis

            Moderate-severe hepatic impairment (ALT >2.5x ULN)

            CHF (NYHA class III, IV)

            Cautions

            Do initiate treatment in patients with active liver disease who have ALT levels >2.5 times the upper limit of normal (ULN); if ALT >3 times the ULN, stop treatment; if ALT is 1.5-3 times the ULN, retest qWeek until normal or until it reaches 3 times the ULN and treatment must be discontinued

            New onset or exacerbation of existing edema, rapid weight gain, macular edema dyspnea reported

            Thiazolidinediones, which are peroxisome proliferator-activated receptor (PPAR) gamma agonists, can cause dose-related fluid retention, particularly when used in combination with insulin

            Risk of hypoglycemia, in combination with insulin or other oral agents

            May result in ovulation in some premenopausal, anovulatory women; ensure adequate contraception

            May decrease hemoglobin/hematocrit

            Increased fracture risk in females

            Use with caution in premenopausal/anovulatory females (patient may resume ovulation and increase the risk of pregnancy)

            Increased risk of CHF; not recommended in symptomatic heart failure

            Cancer risk

            • Bladder cancer
              • 5-year interim results of a 10-year cohort study suggest that pioglitazone use >12 months increases the relative risk of developing bladder cancer in any given year by 40%, an increase from ~7 cases in 10,000 to ~10 cases in 10,000
              • Greatest risk was shown in patients with long-term use and the highest cumulative doses
              • FDA recommendations include not prescribing pioglitazone for patients with active bladder cancer and cautious use in patients with a history of bladder cancer
              • 7/22/2015: A prospective study found that during ~7 years' follow-up, the rate of incident bladder cancer was higher in patients who had ever used pioglitazone than nonusers (89.8 vs. 75.9 per 100,000 person-years), but the difference was not significant after adjustment for potential confounders [JAMA 2015 July 21;314(3):265-277]
            • Prostate cancer
              • 7/22/2015: Compared with nonuse, pioglitazone use was associated with increased risk for prostate cancer (453.3 vs. 449.3 per 100,000 person-years) [JAMA 2015 July 21;314(3):265-277]
            • Pancreatic cancer
              • 7/22/2015: Compared with nonuse, pioglitazone use was associated with increased risk for pancreatic cancer (81.1 vs. 48.4 per 100,000 person-years)
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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Not known if excreted in breast milk; discontinue drug or do not nurse

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Improves target-cell response to insulin; decreases hepatic gluconeogenesis; depends on the presence of insulin for activity

            Absorption

            Onset: Initial effect (delayed), max effect (several weeks)

            Duration: 24 hr

            Peak plasma time: 2-4 hr (delayed by food)

            Distribution

            Protein bound: >99%

            Vd: 0.63 L/kg

            Metabolism

            Metabolized by hepatic CYP2C8 and CYP3A4 into active metabolites

            Active metabolites: Metabolite II (hydroxy derivative), metabolite III (keto derivative), metabolite IV (active hydroxy derivative)

            Elimination

            Half-life: 3-7 hr

            Excretion: Urine (15-30%)

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            Images

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            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

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            • View the formulary and any restrictions for each plan.
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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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