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
- 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
- Get liver function test first before
using Actos. Use with caution in patients with liver disease.
Actos Side Effects
effects of Actos include:
Edema or body swelling
respiratory tract infections.
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
- · Liver
- · Bladder
Congestive Heart Failure
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
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
not for use in patients with type 1 diabetes mellitus or patients in diabetic
ketoacidosis. It should not be used to treat diabetic emergencies.
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.
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
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
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.
Return from pioglitazone to Diabetes Medications.