Pioglitazone

Pioglitazone is Actos generic name. It was first approved by the FDA to treat adults with type 2 diabetes mellitus. It is to be used in combination with diet and exercise. Actos is in the class of diabetes medication known as thiazolidinedione which is peroxisome proliferator-activated receptor (PPAR) agonist. Actos is supplied in tablets of three different strengths: 15mg, 30mg and 45mg.


How Actos works

  • . This diabetic medication works only when there is insulin in the body. It cannot be used for the treatment of type 1 diabetes. Like other PPAR agonists, it works by:
  • ·         Decreasing the resistance of the body to insulin.
  • ·         Causing the liver to move more glucose from the blood to storage.
  • ·         Decreasing the amount of glucose the liver puts into the blood.
  • It does these by getting the PPARs into action. The PPARs then cause the genes that control the use of insulin to use glucose and fats in the normal way. Actos makes the body to respond to insulin in a better way.  In this way, it reduces blood sugar and triglycerides. It also increases the good cholesterol which is the HDL but has not been proved to reduce the bad cholesterol, which is the LDL.
  • Actos is mostly metabolized by the liver and excreted in bile through the feces. A small portion of the metabolites are excreted in urine.
  • The half-life of pioglitazone can be up to 7 hours while that of its metabolites can be up to 24 hours.
  • This diabetic medicine can be used in people with kidney problems. Use with caution in patients with liver damage.
  • Store this medication away from light and at room temperature..

How to Use Actos

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  •  Only a doctor or other prescribing clinician can prescribe Actos.
  •    Start with 15mg or 30mg a day.
  •    Start with 15mg a day if the patient is in NYHA Class I or Class II heart failure and do not increase this dose.
  •  For patients who are not in heart failure, the dose can be increased by 15mg at a time, up to a maximum of 45mg a day, if needed to achieve blood sugar control.
  •  Limit the daily dose of Actos to 15mg if the patient is in NYHA Class I or Class II heart failure or if the patient is taking strong CYP2C8 inhibitors like gemfibrozil and trimethoprim.
  •  Actos can be taken with or without meals.
  • Get liver function test first before using Actos. Use with caution in patients with liver disease.

Actos Side Effects

The side effects of Actos include:

  • ·         Edema or body swelling
  • ·         Upper respiratory tract infections.
  • ·         Hypoglycemia
  • ·         Headache
  • ·         Sinusitis
  • ·         Muscle pain
  • ·         Pharyngitis
  • ·         Flatulence
  • ·         Weight gain
  • ·         Urinary tract infections.
  • ·         Back pain
  • ·         Dizziness
  • ·         Anemia

Drug Interactions with Actos

CYP2C8 inhibitors like gemfibrozil and trimethoprim increase the concentration of pioglitazone in the blood. It is recommended that patients taking gemfibrozil decrease their Actos dose to 15mg daily. Gemfibrozil increases the level of this diabetes medication in the blood three times the level it would be if the patient was not taking gemfibrozil. Other medications that can increase the amount of pioglitazone in the body include ritonavir with brand name Norvir; Atazanavir with brand name Reyataz; and ketoconazole with band name Nizoral.

CYP2C8 inducers like rifampin or Rifadin; phenytoin or Dilantin; carbamazepine or Tegretol; primidone or Mysoline;  fosphenytoin or Cerebyx; and phenobarbital or Luminal will decrease the concentration of Actos in the blood. Those patients need higher doses of pioglitazone  for it to be effective. Even in those circumstances, Actos dose should not exceed 45mg daily. When these medications are stopped, the dose may need to be reduced.

Other medications that can decrease the amount of Actos in the body include midazolam, atorvastatin, Nifedipine and ranitidine or Zantac This decrease is mutual as Actos, in turn decreases the amount of those medications in the body too. Actos also can cause a small decrease in the concentration of some oral contraceptives in the body.



The combination medicine of metformin and pioglitazone is Actoplus MET.

Actos Adverse Reactions

  • ·     Congestive heart failure
  • ·    Edema or body swelling
  • ·    Fractures, especially in women.
  • ·     Hypoglycemia
  • ·     Vision problems
  • ·      Liver failure
  • ·      Bladder cancer

Congestive Heart Failure

Actos is black boxed for congestive heart failure (CHF). CHF may the single most frequent serious adverse effects of actos. Monitor patients for fluid retention, which is the cause of heart failure. Monitor for signs and symptoms of fluid retention especially when it is started initially and any time the dose is increased. The signs and symptoms of fluid retention include sudden weight gain and body swelling or edema. Patients should also be monitored for other signs and symptoms of heart failure, including shortness of breath, cough, weakness, rapid heartbeat, irregular heartbeat, activity intolerance and others.

Contraindications for Actos

Do not give Actos to diabetics is in NYHA Class III or Class IV heart failure.

Do not use if a diabetic patient is allergic to pioglitazone hydrochloride or any of the other ingredients that are used to make the drug. Other ingredients in Actos are lactose monohydrate, hydroxypropylcellulose, carboxymethylcellulose calcium and magnesium stearate.

Limitations of Use

Actos is not for use in patients with type 1 diabetes mellitus or patients in diabetic ketoacidosis. It should not be used to treat diabetic emergencies.

Actos should not be used by pregnant women because it is possible that this drug may cause damage to the fetus. It is in Pregnancy Category C.

This diabetic medicine should not be taken by nursing mothers because it may get into the baby through the milk.

Do not use in pediatric patients.

Precautions and Warnings

  • ·         Actos may cause fluid retention which could lead to heart failure. The higher the dose, the more likely that it will cause fluid retention and heart failure. Diabetics who are using pioglitazone in combination with insulin should be monitored for fluid retention and heart failure. Patients who are already in NYHA class I and class II heart failure who are taking Actos should be closely monitored.
  • ·         Because of water retention, there could be visible swelling or edema on hands, feet or elsewhere in the body.
  • ·         Watch patients for any signs and symptoms of liver damage. These include dark urine, jaundice, fatigue, right upper abdominal pain or anorexia. If that occurs, stop taking Actos, unless it can be proved that something else, other than Actos, caused the liver problem.
  • ·         Watch patients for any signs of weak bones. Women on Actos have been noted to have more incidents of fractures than women who are not on this drug. Women should take steps to protect the health of their bones while on Actos.
  • ·         Actos may cause bladder cancer, especially with long term use. There is a possibility that it may increase the risk of bladder cancer by up to 40% a year if taken for longer than one year. Do not start this diabetes medication if you have bladder cancer or a family history of bladder cancer. If you are taking Actos, tell your doctor if you have blood in the urine, experience urgency or pain with urination or experience pain in the back or lower abdomen. Bladder cancer risk has caused countries like France and Germany to stop and limit the use of Actos respectively. Bladder cancer is the reason for most Actos lawsuit which runs in thousands of filings. At this time, there is no Actos recall.
  • ·         Watch diabetic patients for hypoglycemia if the patient is also taking insulin or any insulin secretagogue, which are diabetic medicines that work by making the body to release more insulin. If the patients develop hypoglycemia, they may need to reduce the insulin dose or the dose of the inulin releasing medication.
  • ·         Watch patients for changes in vision which may be caused by swelling of the eye brought about by pioglitazone. If  patient experiences blurred vision or any decreases in sharpness of images seen, the patient should report it promptly to their clinicians.
  • ·         Menopausal women taking Actos should be aware that it could cause them to ovulate and at risk for getting pregnant. This medication is, nevertheless, not a fertility drug for menopausal women and should not be used as such.
  • ·         Elderly diabetic patients may need to use lower doses.
  • ·         In case of accidental overdose, any symptoms of overdose should be treated.
  • ·        If you experience any serious adverse effects with the use of Actos, you can report to or call Takeda Pharmaceuticals America, Inc at 877-825-3327

Lab Tests for Patients on Actos

Periodic liver function tests are recommended for patients who have liver disease at the time of initiation or who develops liver disease while on pioglitazone.

HBA1C every three months to see how well it is keeping the blood glucose within limits.

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