Pioglitazone

What is Pioglitazone?

• Pioglitazone (Actos) is a thiazolidinedione and an agonist for peroxisome proliferator-activated receptor (PPAR) gamma is an anti-diabetic medication used to treat type 2 diabetes.

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Pioglitazone

What are the uses of this medicine?

• Pioglitazone (Actos) is used with diet and exercise to improve blood sugar (glucose) control in adults with type 2 diabetes. Pioglitazone tablets are a diabetes medicine called pioglitazone that may be taken alone or with other diabetes medicines.

Limitations of Use:

• Pioglitazone tablets are not for people with type 1 diabetes.
• Pioglitazone tablets are not for people with diabetic ketoacidosis (increased ketones in your blood or urine).

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Pioglitazone ball-and-stick model

How does this medicine work?

• Pioglitazone (pye" oh gli' ta zone) is a thiazolidinedione thought to act by engagement of PPARγ receptors which induce multiple genes involved in glucose and fatty acid metabolism.
• In clinical trials, pioglitazone was found to lower blood glucose and HbA1c levels and had additive effects with the sulfonylureas and metformin.
• Pioglitazone is a thiazolidinedione that depends on the presence of insulin for its mechanism of action.
• Pioglitazone decreases insulin resistance in the periphery and in the liver resulting in increased insulin-dependent glucose disposal and decreased hepatic glucose output.
• Pioglitazone is not an insulin secretagogue.
• Pioglitazone is an agonist for peroxisome proliferator-activated receptor-gamma (PPARγ).
• PPAR receptors are found in tissues important for insulin action such as adipose tissue, skeletal muscle and liver.
• Activation of PPARγ nuclear receptors modulates the transcription of a number of insulin responsive genes involved in the control of glucose and lipid metabolism.
• Because pioglitazone enhances the effects of circulating insulin (by decreasing insulin resistance), it does not lower blood glucose in animal models that lack endogenous insulin.

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Pioglitazone 2D

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• have severe heart failure
• are allergic to any of the ingredients in pioglitazone tablets.

What drug interactions can this medicine cause?

Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following:

• atorvastatin (Lipitor, in Caduet), gemfibrozil (Lopid), hormonal contraceptives (birth control pills, patches, rings, implants, and injections), insulin or other medications to treat diabetes
• ketoconazole (Nizoral), midazolam, nifedipine (Adalat, Afeditab, Procardia), ranitidine (Zantac), rifampin (Rifadin, Rifater, in Rifamate)
• theophylline (Elixophyllin, Theo-24, Theochron)

Is this medicine FDA approved?

• Pioglitazone was approved for use in the United States in 1999 and remains in wide use.
• Current indications for pioglitazone are as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes.

How should this medicine be used?

• Obtain liver tests before starting pioglitazone tablets. If abnormal, use caution when treating with pioglitazone tablets, investigate the probable cause, treat (if possible) and follow appropriately. Monitoring liver tests while on pioglitazone tablets is not recommended in patients without liver disease.

Recommended dosage:

• The recommended starting dose for patients without congestive heart failure is 15 mg or 30 mg once daily.
• The recommended starting dose for patients with congestive heart failure (NYHA Class I or II) is 15 mg once daily.
• If there is inadequate glycemic control, the dose can be increased in 15 mg increments up to a maximum of 45 mg once daily.
• If hypoglycemia occurs in a patient co-administered pioglitazone tablets and an insulin secretagogue (e.g., sulfonylurea), the dose of the insulin secretagogue should be reduced.
• If hypoglycemia occurs in a patient co-administered pioglitazone tablets and insulin, the dose of insulin should be decreased by 10% to 25%.

Concomitant Use with Strong CYP2C8 Inhibitors:

• The maximum recommended dose of pioglitazone tablets is 15 mg daily when used in combination with gemfibrozil or other strong CYP2C8 inhibitors.

Administration:

• Take pioglitazone tablets one time each day, with or without food.
• If you miss a dose of pioglitazone tablets, take your next dose as prescribed unless your doctor tells you differently. Do not take two doses at one time the next day.
• Stay on your diet and exercise programs and test your blood sugar regularly while taking pioglitazone tablets.
• Your doctor should do certain blood tests before you start and while you take pioglitazone tablets.
• Your doctor should also do hemoglobin A1C testing to check how well your blood sugar is controlled with pioglitazone tablets.
• Your doctor should check your eyes regularly while you take pioglitazone tablets.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 15 mg, 30 mg and 45 mg

This medicine is available in fallowing brand namesː

• Actos

What side effects can this medication cause?

The most common side effects of this medicine include:

• cold-like symptoms (upper respiratory tract infection)
• headache
• sinus infection
• muscle pain
• sore throat

Pioglitazone tablets may cause serious side effects including:

• new or worse heart failure
• fluid retention
• hypoglycemia
• liver problems
• bladder cancer
• fractures
• macular edema
• release of an egg from an ovary in a woman (ovulation) leading to pregnancy

What special precautions should I follow?

• Pioglitazone, like other thiazolidinediones, can cause dose-related fluid retention when used alone or in combination with other antidiabetic medications and is most common when pioglitazone is used in combination with insulin. Fluid retention may occur and can exacerbate or lead to congestive heart failure. Combination use with insulin and use in congestive heart failure NYHA Class I and II may increase risk. Monitor patients for signs and symptoms.
• Patients receiving pioglitazone in combination with insulin or other antidiabetic medications (particularly insulin secretagogues such as sulfonylureas) may be at risk for hypoglycemia. When used with insulin or an insulin secretagogue, a lower dose of the insulin or insulin secretagogue may be needed to reduce the risk of hypoglycemia.
• Post-marketing reports of hepatic failure, sometimes fatal. Causality cannot be excluded. If liver injury is detected, promptly interrupt pioglitazone and assess patient for probable cause, then treat cause if possible, to resolution or stabilization. Do not restart pioglitazone if liver injury is confirmed and no alternate etiology can be found.
• Pioglitazone may increase the risk of bladder cancer. Do not use in patients with active bladder cancer. Use caution when using in patients with a prior history of bladder cancer.
• Edema was reported more frequently in patients treated with pioglitazone. Patients treated with pioglitazone should be monitored for signs and symptoms of congestive heart failure.
• Increased incidence of bone fracture in female patients. Apply current standards of care for assessing and maintaining bone health.
• Macular edema has been reported in post-marketing experience in diabetic patients who were taking pioglitazone or another thiazolidinedione. Recommend regular eye exams in all patients with diabetes according to current standards of care with prompt evaluation for acute visual changes.
• There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with pioglitazone.
• Pioglitazone has been linked to rare instances of acute liver injury. While the initial thiazolidinedione approved for use – troglitazone – was associated with high rates of serum aminotransferase elevations and multiple reports of severe liver injury and death from acute liver failure, pioglitazone has been associated with only rare instances of clinically apparent liver injury.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• It is not known if pioglitazone tablets can harm your unborn baby.
• There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy.

Can this medicine be used in children?

• It is not known if pioglitazone tablets are safe and effective in children under the age of 18.
• Pioglitazone tablets are not recommended for use in children.

What are the active and inactive ingredients in this medicine?

• Active Ingredient: pioglitazone hydrochloride
• Inactive Ingredients: carboxymethyl cellulose calcium, hydroxypropyl cellulose, lactose monohydrate, and magnesium stearate.

Who manufactures and distributes this medicine?

Manufactured by:

• Lek Pharmaceuticals d.d.
• Ljubljana, Slovenia for
• Sandoz Inc., Princeton, NJ

What should I know about storage and disposal of this medication?

• Store pioglitazone tablets at 20° to 25°C (68° to 77°F).
• Keep pioglitazone tablets in the original container and protect from light.
• Keep the pioglitazone tablets bottle tightly closed and keep tablets dry.

Antidiabetics

•  Alpha-Glucosidase Inhibitors
  • Acarbose
  • Miglitol
• Incretin-Based Drugs
  • Dipeptidyl Peptidase-4 (DPP-4) Inhibitors
    • Alogliptin
    • Linagliptin
    • Saxagliptin
    • Sitagliptin
  • Glucagon-Like Peptide-1 (GLP-1) Analogues
    • Albiglutide
    • Dulaglutide
    • Exenatide
    • Liraglutide
    • Lixisenatide
•  Insulin
• Metformin
• Metiglinide Analogues
  • Nateglinide
  • Repaglinide
• Pramlintide
• Sodium Glucose Cotransporter-2 (SGLT-2) Inhibitors
  • Canagliflozin
  • Dapagliflozin
  • Empagliflozin
• Sulfonylureas
  • First Generation Sulfonylureas
    • Acetohexamide
    • Chlorpropamide
    • Tolazamide
    • Tolbutamide
  • Second Generation Sulfonylureas
    • Gliclazide
    • Glimepiride
    • Glipizide
    • Glyburide (Glibenclamide)
• Thiazolidinediones
  • Pioglitazone
  • Rosiglitazone
  • Troglitazone

• Dailymed label info on Pioglitazone
• FDA Pioglitazone

Pioglitazone Resources
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