Davis's Drug Guide

pioglitazone

General

Pronunciation:
pi-o-glit-a-zone


Trade Name(s)

  • Actos

Pregnancy Category
Category C

Ther. Class.
antidiabetics (oral)

Pharm. Class.
thiazolidinediones

Indications

Type 2 diabetes mellitus (with diet and exercise); may be used with metformin, sulfonylureas, or insulin.

Action

  • Improves sensitivity to insulin by acting as an agonist at receptor sites involved in insulin responsiveness and subsequent glucose production and utilization.
  • Requires insulin for activity.

Therapeutic Effect(s):

Decreased insulin resistance, resulting in glycemic control without hypoglycemia.

Pharmacokinetics

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Protein Binding: >99% bound to plasma proteins. Active metabolites are also highly (>99%) bound.

Metabolism and Excretion: Extensively metabolized by the liver (primarily by CYP2C8); at least two metabolites have pharmacologic activity. Minimal renal excretion of unchanged drug.

Half-life: Pioglitazone– 3–7 hr; total pioglitazone (pioglitazone plus metabolites)– 16–24 hr.

TIME/ACTION PROFILE (effects on blood glucose)

ROUTEONSETPEAKDURATION
PO30 min2–4 hr24 hr

Contraindication/Precautions

Contraindicated in:

  • Hypersensitivity;
  • Type 1 diabetes;
  • Diabetic ketoacidosis;
  • Clinical evidence of active liver disease or ↑ ALT (>2.5 times upper limit of normal);
  • Active bladder cancer;
  • OB: Lactation: Insulin should be used to control blood glucose levels;
  • Pedi: Children.

Use Cautiously in:

  • Edema;
  • HF (avoid use in moderate to severe HF);
  • Hepatic impairment;
  • History of bladder cancer;
  • Women (may ↑ distal upper and lower limb fractures);
  • Women with childbearing potential (may restore ovulation and ↑ risk of pregnancy).

Adverse Reactions/Side Effects

CV: CHF, edema

EENT: macular edema

GI: LIVER FAILURE, ↑ liver enzymes

GU: BLADDER CANCER (ESPECIALLY AFTER >1 YR)

Hemat: anemia

MS: RHABDOMYLOLYSIS

Misc: fractures (arm, hand, foot) in female patients

* CAPITALS indicate life-threatening.
Italics indicate most frequent.

Interactions

Drug-Drug

  • May ↓ efficacy of hormonal contraceptives .
  • Strong CYP2C8 inhibitors, including gemfibrozil may ↑ levels.
  • Ketoconazole may ↑ effects of pioglitazone.
  • Concurrent use with insulin may ↑ risk of fluid retention and worsening HF.

Drug-Natural Products:

  • Glucosamine may worsen blood glucose control.
  • Chromium, and coenzyme Q-10 may produce ↑ hypoglycemic effects.

Route/Dosage

PO: (Adults) No heart failure– 15–30 mg once daily, may be ↑ in increments of 15 mg/day to 45 mg/day if needed; NYHA class I-II heart failure– 15 mg once daily; may be ↑ in increments of 15 mg/day to 45 mg/day if needed; Concurrent use of gemfibrozil– do not exceed 15 mg once daily.

Availability (generic available)

Tablets: 15 mg, 30 mg, 45 mg

Cost:

Generic: 15 mg $25.49/90, 30 mg $22.75/90, 45 mg $38.12/90

In Combination with: metformin (Actoplus Met, Actoplus Met XR), glimepride (Duetact), alogliptin (Oseni); see combination drugs.

Assessment

  • Observe patient taking concurrent insulin for signs and symptoms of hypoglycemic reactions (sweating, hunger, weakness, dizziness, tremor, tachycardia, anxiety).
  • Assess for signs and symptoms of heart failure (edema, dyspnea, rapid weight gain, unusual tiredness) after initiation and with dose increases.

Lab Test Considerations:

Monitor serum glucose and Hb A1c periodically during therapy to evaluate effectiveness.

  • Monitor CBC with differential periodically during therapy. May cause ↓ in hemoglobin and hematocrit, usually during the first 4–12 wk of therapy; then levels stabilize.
  • Monitor serum AST, ALT, alkaline phosphatase, and total bilirubin levels before starting therapy and periodically thereafter or if jaundice or symptoms of hepatic dysfunction occur. Pioglitazone should not be started in patients with active liver disease or ALT levels >2.5 times the upper limit of normal. Patients with mild ALT ↑ should have more frequent monitoring. If ALT ↑ to >3 times the upper limit of normal, recheck ALT promptly. Discontinue pioglitazone if ALT remains >3 times normal.
  • May cause transient ↑ in CPK levels.

Potential Diagnoses

Implementation

  • Do not confuse Actos (pioglitazone) with Actonel (risedronate).
  • Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.
  • PO: May be administered with or without meals.

Patient/Family Teaching

  • Instruct patient to take medication as directed. If dose for 1 day is missed, do not double dose the next day.
  • Explain to patient that this medication controls hyperglycemia but does not cure diabetes. Therapy is long-term.
  • Review signs of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to take a glass of orange juice or 2–3 tsp of sugar, honey, or corn syrup dissolved in water and notify health care professional.
  • Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hypoglycemic or hyperglycemic episodes.
  • Instruct patient in proper testing of serum glucose and ketones. These tests should be closely monitored during periods of stress or illness, and health care professional should be notified if significant changes occur.
  • Advise patient to notify health care professional immediately if signs of hepatic dysfunction (nausea, vomiting, upper right abdominal pain, fatigue, anorexia, dark urine, jaundice), bladder cancer (hematuria, dysuria, urinary urgency), or HF (edema, shortness of breath, rapid weight gain, tiredness) occur.
  • Advise patient to inform health care professional of medication regimen before treatment or surgery.
  • Insulin is the preferred method of controlling blood glucose during pregnancy. Counsel female patients that higher doses of oral contraceptives or a form of contraception other than oral contraceptives may be required and to notify health care professional promptly if pregnancy is planned or suspected.
  • Advise patient to carry a form of sugar (sugar packets, candy) and identification describing disease process and medication regimen at all times.
  • Emphasize the importance of routine follow-up exams.

Evaluation/Desired Outcomes

Control of blood glucose levels.

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