pioglitazone (Rx)

Brand and Other Names:Actos
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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

Dosage Modification

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

X-Linked Adrenoleukodystrophy (Orphan)

Hydroxypioglitazone: Orphan designation for treatment of X-linked adrenoleukodystrophy

Sponsor

  • Minoryx Therapeutics S.L.; TecnoCampus Mataro-Maresme. TCM3 602, Av. Ernest Lluch, 32; Mataró, Spain

Not recommended

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Interactions

Interaction Checker

and pioglitazone

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

            Not recommended for patients with symptomatic heart failure; may cause or exacerbate congestive heart failure in some patients; monitor patients carefully after initiating therapy; observe for signs and symptoms of heart failure; if signs and symptoms develop, manage heart failure according to current standards of care; consider discontinuing therapy or reducing the dose

            New onset or exacerbation of existing edema and dyspnea reported

            Macular edema reported; patients should be seen by an ophthalmologist if any visual symptoms arise during therapy; all diabetic patients should have regular eye exams

            Delayed related weight gain reported with use; likely associated with fluid retention and fat accumulation

            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)

            Discuss potential for unintended pregnancy with premenopausal women as therapy with pioglitazone, like other thiazolidinediones, may result in ovulation in some anovulatory women

            Increased risk of CHF; not recommended in symptomatic heart failure

            Cancer risk

            • Bladder cancer
              • Pioglitazone may be linked to an increased risk of bladder cancer
              • Do not prescribe for patients with active bladder cancer
              • Consider benefit:risk ratio before prescribing in patients with a history of bladder cancer
              • Instruct patients to contact their physician if signs of bladder cancer observed after initiating therapy (eg, blood or red colored urine, new or worsening urinary urgency, pain on urination)
            • 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: Limited data with pioglitazone in pregnant women are not sufficient to determine a drug- associated risk for major birth defects or miscarriage; there are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy; poorly controlled diabetes in pregnancy increases maternal risk for diabetic ketoacidosis, pre-eclampsia, spontaneous abortions, preterm delivery, still birth and delivery complications; poorly controlled diabetes increases fetal risk for major birth defects, still birth, and macrosomia related morbidity

            Lactation: There is no information regarding the presence of pioglitazone in human milk, the effects on the breastfed infant, or the effects on milk production; the developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for pioglitazone and any potential adverse effects on the breastfed infant from pioglitazone or from the underlying maternal condition

            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

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            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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            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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