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Pioglitazone

 
Drug Info: Pioglitazone
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Brand names: Actos®

Chemical formula:



Pioglitazone tablets

What are pioglitazone tablets?

PIOGLITAZONE (Actos™) helps to treat type 2 diabetes mellitus. Pioglitazone helps your body to use insulin more efficiently and helps to lower high blood sugar. Generic pioglitazone tablets are not yet available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• heart problems
• kidney or liver problems
• swelling of the arms, legs, or feet
• an unusual or allergic reaction to pioglitazone, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I take this medicine?

Take pioglitazone tablets by mouth. Follow the directions on the prescription label. Swallow the tablets with a drink of water with meals. Take your doses at the same time each day; do not take more often than directed.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What drug(s) may interact with pioglitazone?

• atorvastatin
• birth control pills or other hormonal methods of birth control
• bosentan
• itraconazole
• ketoconazole
• midazolam
• nifedipine
• other medicines for diabetes, including insulin
• topiramate

Many medications may cause changes (increase or decrease) in blood sugar, these include:
• alcohol containing beverages
• angiotensin converting enzyme inhibitors (ACE inhibitors), often used for high blood pressure or heart problems (examples: captopril, enalapril, lisinopril)
• antiretroviral protease inhibitors (examples: indinavir, ritonavir, saquinavir)
• aspirin and aspirin-like drugs
• baclofen
• beta-blockers, often used for high blood pressure or heart problems (examples include atenolol, metoprolol, propranolol)
• certain medicines used for mental depression, emotional, or psychotic disturbances
• chromium
• cisapride
• clonidine
• cyclosporine
• diazoxide
• disopyramide
• epinephrine
• female hormones, such as estrogens or progestins, birth control pills
• fibric acid derivatives, used to treat high cholesterol (examples: fenofibrate and gemfibrozil)
• glucagon
• growth hormone (somatropin)
• guanethidine
• isoniazid
• lithium
• metoclopramide
• male hormones or anabolic steroids
• medications to suppress appetite or for weight loss
• medicines for allergies, asthma, cold, or cough
• niacin
• nicotine (including nicotine found in patches and gum)
• octreotide
• pentamidine
• phenytoin
• quinolone antibiotics (examples: ciprofloxacin, levofloxacin, ofloxacin)
• some herbal dietary supplements
• steroid medicines such as prednisone or cortisone
• sulfonamides, medicines for infection (examples: Azulfidine®, Bactrim®, Gantrisin® Septra®)
• tacrolimus
• tegaserod
• thyroid hormones
• water pills (diuretics)

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking pioglitazone?

Visit your prescriber or health care professional for regular checks on your progress. Learn how to monitor blood or urine sugar and urine ketones regularly. Check with your prescriber or health care professional if your blood sugar is high, you may need a change of dose of pioglitazone. Do not skip meals. If you are exercising much more than usual you may need extra snacks to avoid side effects caused by low blood sugar. If you have mild symptoms of low blood sugar, eat or drink something containing sugar at once and contact your prescriber or health care professional. It is wise to check your blood sugar to confirm that it is low. It is important to recognize your own symptoms of low blood sugar so that you can treat them quickly. Make sure family members know that you can choke if you eat or drink when you have serious symptoms of low blood sugar, such as seizures or unconsciousness. They must get medical help at once.

Your health care professional will have to check blood tests regularly to assess the effect of this medication on your liver. Pioglitazone may rarely cause changes in some of these measurements.

If you are going to have surgery, tell your prescriber or health care professional that you are taking pioglitazone.

Wear a medical identification bracelet or chain to say you have diabetes, and carry a card that lists all your medications.

What side effects may I notice from taking pioglitazone?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• anxiety or nervousness, confusion, difficulty concentrating
• blurred vision
• breathing problems such as rapid, deep breathing or difficulty breathing with activity
• cold sweats, increased sweating
• cool, pale skin
• dark yellow or brown urine, or yellowing of the eyes or skin
• diarrhea
• drowsiness
• muscle pain
• nausea, vomiting
• skin rash or hives
• slow heartbeat
• tremors or shakiness
• unusual tiredness or weakness
• swelling of the hands, legs, and/or feet

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• headache
• weight gain

Where can I keep my medicine?

Keep out of the reach of children in a container that small children cannot open.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Keep container tightly closed and protect from moisture and humidity. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

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Wikipedia: Pioglitazone
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Home > Library > Miscellaneous > Wikipedia
Pioglitazone
Systematic (IUPAC) name
(RS)-5-(4-[2-(5-ethylpyridin-2-yl)ethoxy]benzyl)thiazolidine-2,4-dione
Identifiers
CAS number 111025-46-8
ATC code A10BG03
PubChem 4829
DrugBank APRD00653
Chemical data
Formula C19H20N2O3S 
Mol. mass 356.44 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Protein binding >99%
Metabolism liver (CYP2C8)
Half life 3–7 hours
Excretion in bile
Therapeutic considerations
Licence data

EU EMEA:link, US FDA:link
Pregnancy cat.

C
Legal status

POM(UK) ℞-only(US)
Routes oral
 Yes check.svgY(what is this?)  (verify)

Pioglitazone is a prescription drug of the class thiazolidinedione (TZD) with hypoglycemic (antihyperglycemic, antidiabetic) action. Pioglitazone is marketed as trademarks Actos in the USA and UK, Glustin in Europe, Zactos in Mexico by Takeda Pharmaceuticals & Piozer in Pakistan by Hilton Pharmaceuticals.

Contents

Pharmacology

Pioglitazone selectively stimulates the nuclear receptor peroxisome proliferator-activated receptor gamma (PPAR-γ) and to a lesser extent PPAR-α.[1][2] It modulates the transcription of the insulin-sensitive genes involved in the control of glucose and lipid metabolism in the lipidic, muscular tissues and in the liver. As a result, pioglitazone reduces insulin resistance in the liver and peripheral tissues; increases the expense of insulin-dependent glucose; decreases withdrawal of glucose from the liver; reduces quantity of glucose, insulin and glycated haemoglobin in the bloodstream. Although not clinically significant, pioglitazone decreases the level of triglycerides and increases that of high-density lipoproteins (HDL) without changing low-density lipoproteins (LDL) and total cholesterol in patients with disorders of the lipid metabolism, although statins are the drug of choice for this.

More recently, pioglitazone and other active TZDs have been shown to bind to the outer mitochondrial membrane protein mitoNEET with affinity comparable to that of pioglitazone for PPARγ.[3][4]

Indications and usage

Pioglitazone is used for the treatment of diabetes mellitus type 2 (previously known as non-insulin-dependent diabetes mellitus, NIDDM) in monotherapy and in combination with sulfonylurea, metformin, or insulin. Pioglitazone has also been used to treat non-alcoholic steatohepatitis (fatty liver), but this use is presently considered experimental.[5]

Contraindications

Pioglitazone cannot be used in patients with a known hypersensitivity to pioglitazone, other thiazolidinediones or any of components of its pharmaceutical forms. It is ineffective and possibly harmful in diabetes mellitus type 1 and diabetic ketoacidosis. Its safety in pregnancy, lactation (breastfeeding) and people under 18 is not established.

Given previous experiences with the related drug troglitazone, acute diseases of the liver are regarded as a contraindication for pioglitazone.

Side effects

A press release by GlaxoSmithKline in February 2007 noted that there is a greater incidence of fractures of the upper arms, hands and feet in female diabetics given rosiglitazone compared with those given metformin or glyburide. The information was based on data from the ADOPT trial. Following release of this statement, Takeda also admitted that pioglitazone has similar implications for female patients.[citation needed]

The risk of hypoglycemia is low in the absence of other drugs that lower blood glucose.

Like other thiazolidinediones, pioglitazone can cause fluid retention and peripheral edema. As a result, it may precipitate congestive heart failure (which worsens with fluid overload in those at risk). It may cause anemia. Mild weight gain is common due to increase in subcutaneous adipose tissue. In studies, patients on pioglitazone had a slightly increased proportion of upper respiratory tract infection, sinusitis, headache, myalgia and tooth problems.

On July 30, 2007 an Advisory Committee of the Food and Drug Administration concluded that the use of rosiglitazone for the treatment of type 2 diabetes was associated with a greater risk of "myocardial ischemic events" when compared to placebo, but when compared to other active comparators, there was no increased risk. Pioglitazone is currently being reviewed. A meta-analysis released subsequently showed that pioglitazone reduced the number of ischemic cardiac events rather than increase the risk, but increases CHF, a common class effect of the TZD's..[6] The PERISCOPE study compared pioglitazone with glimepiride in diabetics; atherosclerotic plaque volume was measured and followed over time. Glimepiride therapy had highly significant progression of plaque volume over time of 0.73 percent. In comparison, pioglitazone had a -0.16 percent regression in plaque volume. This is the first study to show that diabetic therapy slowed progression of atherosclerosis. Therapy with pioglitazone raised HDL, and lowered triglyceride and hsCRP; these are all beneficial effects on risk factors for coronary artery disease, however to date, no oral anti-diabetic drug has been shown to reduce the risk of cardiovascular complications.[7]

Drug interactions

Sulfonamides, metformin, and insulin reciprocally exponentiate hypoglycemia. Therapy with pioglitazone increased risk for pregnancy in those taking oral contraception.

How supplied

Pioglitazone as Actos is supplied in oral tablets containing 15, 30 or 45 mg of pioglitazone base. It is also available in combination with metformin as ActoplusMet (tablets containing 15 mg pioglitazone and either 500 or 850 mg of metformin) or in combination with Amaryl as Duetact (tablets containing 30 mg pioglitazone and either 2 or 4 mg of Amaryl).

References

  1. ^ Gillies PS, Dunn CJ (August 2000). "Pioglitazone". Drugs 60 (2): 333–43; discussion 344–5. doi:10.2165/00003495-200060020-00009. PMID 10983737. 
  2. ^ Smith U (September 2001). "Pioglitazone: mechanism of action". Int J Clin Pract Suppl (121): 13–8. PMID 11594239. 
  3. ^ Colca JR, McDonald WG, Waldon DJ, Leone JW, Lull JM, Bannow CA, Lund ET, Mathews WR (2004). "Identification of a novel mitochondrial protein ("mitoNEET") cross-linked specifically by a thiazolidinedione photoprobe". Am. J. Physiol. Endocrinol. Metab. 286 (2): E252–60. doi:10.1152/ajpendo.00424.2003. PMID 14570702. 
  4. ^ Paddock ML, Wiley SE, Axelrod HL, Cohen AE, Roy M, Abresch EC, Capraro D, Murphy AN et al. (2007). "MitoNEET is a uniquely folded 2Fe 2S outer mitochondrial membrane protein stabilized by pioglitazone". Proc. Natl. Acad. Sci. U.S.A. 104 (36): 14342–7. doi:10.1073/pnas.0707189104. PMID 17766440. 
  5. ^ Belfort R, Harrison SA, Brown K, Darland C, Finch J, Hardies J, Balas B, Gastaldelli A et al. (2006). "A placebo-controlled trial of pioglitazone in subjects with nonalcoholic steatohepatitis". N. Engl. J. Med. 355 (22): 2297–307. doi:10.1056/NEJMoa060326. PMID 17135584. 
  6. ^ Lincoff AM, Wolski K, Nicholls SJ, Nissen SE (2007). "Pioglitazone and risk of cardiovascular events in patients with type 2 diabetes mellitus: a meta-analysis of randomized trials". JAMA 298 (10): 1180–8. doi:10.1001/jama.298.10.1180. PMID 17848652. 
  7. ^ Nissen SE, Nicholls SJ, Wolski K (2008). "Comparison of pioglitazone vs glimepiride on progression of coronary atherosclerosis in patients with type 2 diabetes". JAMA 299 (13): 1561. doi:10.1001/jama.299.13.1561. PMID 18378631. http://jama.ama-assn.org/cgi/content/full/299.13.1561v1. 

External links

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This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)

 
 

 

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