Actos

This will be the first time I’m using the brand name for a medication in my post.  If you remember from a few weeks ago, I told you that Actos is now available as a generic called pioglitazone.  Since the generic is so new and most of you will still know this drug by the name Actos, I’m going to make things easier and call it by its brand name.  Actos is one of two drugs in the category known as the TZDs.  I won’t bother spelling out the name of the class for you here, because quite frankly it is just a mouthful, but if you are curious you can read my previous post about it here.

How does it lower blood sugar: Actos lowers the amount of glucose in your blood by making your cells more sensitive to insulin.  As a reminder, insulin is the hormone that opens the door to your cell, allowing glucose in.  Think of insulin as a butler and the glucose in your blood as guests wanting to get into the house (cell).  In type 2 diabetes, your cells do not recognize insulin very well (the butler is left out in the cold, and so are the guests!).  But Actos helps the cell recognize the insulin so that it can do its job, kind of like the maid opening the door for the butler (forgive my pathetic analogy, but I bet you’ll remember how Actos works now!).

Another interesting thing about Actos is how it affects your fat cells.  We have two types of fat in our bodies – subcutaneous and visceral.  Subcutaneous fat exists right underneath your skin.  Visceral fat is deeper in your body and surrounds your organs (liver, stomach, and even streaking in your muscles).  This visceral fat is the “bad” kind of fat – big amounts of it are related to type 2 diabetes and heart disease.  Visceral fat cells are less sensitive to insulin, and subcutaneous fat cells are more sensitive.  Actos actually cause your body to produce less visceral fat cells and more subcutaneous fat cells!  This means that more glucose can be pulled out of your blood!

The effect on your numbers: Actos can lower your A1c by 1-2% (an A1c of 9.5 could go down to 8.5 or 7.5 with Actos).  However, it does take at least 4-8 weeks to see an effect on your A1c, and it might even take up to 16 weeks to see the full effectiveness of the medicine.  What’s the other number that Actos can affect?  Weight.  Actos can cause weight gain of about 12 pounds, or more depending upon what other diabetic medications you are taking.

Dosing: Actos is usually started at a dose of 15 mg once daily.  You can take Actos with or without food (Actos does not cause hypoglycemia like some of the meds I’ve already talked about!).  If your A1c does not come down far enough after 6-8 weeks, then we will increase the dose or try another medication.  Doses can be increased up to a maximum of 45 mg taken once daily.  However, doses over 30 mg are not usually effective and may cause more side effects.

Side effects: So what are the side effects of Actos?  I’ve already mentioned one – weight gain.  This is due mainly to a buildup of fluid in your body (usually legs and feet) called edema.  Fortunately this stabilizes after you’ve been on Actos for about six months, but your doctor might put you on a “water pill” to help get that extra fluid out of your body.  Other side effects that you might notice when on Actos are headache, upper respiratory infection, and bone fracture.

A unique side effect of Actos is that it can cause ovulation and menstruation in women that previously were not ovulating or menstruating.  This includes women who are premenopausal and those with polycystic ovary syndrome (PCOS).  It is important that women taking Actos are aware of this because Actos should not be taken when pregnant, so doctors will advise them to take adequate precautions.

Who should not take Actos: The most major precaution with Actos has to do with the heart.  If you have congestive heart failure, talk to your doctor about whether or not Actos is right for you.  Actos can cause fluid to build up in the lungs, or even lead to heart failure, in patients with a bad heart.  This has found to be even more of a concern with the other drug in this class (Avandia) that I will talk about next week, but it is important to know about Actos.  Generally we can control this fluid buildup by adding a “water pill” and decreasing your Actos dose, but sometimes we will have to try other medications instead of Actos.

Actos can cause liver toxicity, so patients with liver problems should not take Actos.  Actos is not effective for patients with type 1 diabetes or those type 2 diabetics that are no longer producing their own insulin.  Due to a risk of potential bladder cancer caused by long periods on Actos and high doses, patients with active or prior bladder cancer should not take this medicine.

Drug interactions:  It is possible that Actos may decrease the effectiveness of oral birth control.  Other medications that can interact with Actos include the cholesterol medications Lipitor and gemfibrozil, the antibiotic ketoconazole, and thyroid medications.  As always, this is not the full list and every patient is different, so consult with your local doctor and pharmacist regarding other medications that you are taking.

Monitoring: As always, you should be checking your blood sugars on a daily basis when on Actos.  Your doctor will also be checking your A1c to see how your diabetes is being controlled.  Also, you can expect liver tests when taking Actos, to make sure that it is not causing problems.  We will also watch for fluid buildup in your legs and feet and will monitor bone health, especially in elderly women, to try to prevent fractures.

Place in therapy for diabetes: Currently Actos is considered the second step for a patient after diet, exercise, and metformin have failed.  We will usually give metformin a trial run for three months and then switch to either insulin, one of the sulfonylureas that I’ve already talked about, or a TZD like Actos.  Actos is considered for patients that have trouble with low blood sugars, because the sulfonylureas and insulin cause more hypoglycemia.  And now that Actos is generic, it will soon become a cost-effective choice.  However, be aware that up to 25% of patients not see any effect on their A1c from Actos, so we might have to try another medication.

If you’d like to read more about Actos (and see a really cool video showing how it works!), visit the manufacturer’s website here.

Next week I will talk about the other TZD.  This is the medication that you might be seeing on television commercials, and not for a good reason!  So come back next week and I will break down the rumors and truths about Avandia.

——————————————————————————————-

As a disclaimer, I am your “virtual” pharmacist, here to provide you with information and answers to questions.  However, I am not your local pharmacist and could, in no way, be aware of your specific medical needs.  Remember to always check with your medical provider and pharmacist before stopping or starting any new medications.  My posts are based on general pharmacy principles and should not be regarded as your “first opinion” when it comes to your health.  Please consult with your doctor and pharmacist about anything regarding your health.

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