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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Pioglitazone Hydrochloride
Brand Name
Pioglitazone Hydrochloride
Generic Name
Pioglitazone Hydrochloride
Active Ingredient
PioglitazoneCategory
Peroxisome Proliferator Receptor alpha Agonist [EPC]
Salt Form
Hydrochloride
Variants
15
References used for this content
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Pioglitazone Hydrochloride, you must consult a qualified healthcare professional.
| 30 mg/1 | TABLET | ORAL | 71335-9664 |
| 45 mg/1 | TABLET | ORAL | 50090-6384 |
| 30 mg/1 | TABLET | ORAL | 82009-104 |
| 15 mg/1 | TABLET | ORAL | 50090-6386 |
| 15 mg/1 | TABLET | ORAL | 82009-103 |
| 45 mg/1 | TABLET | ORAL | 82009-105 |
| 30 mg/1 | TABLET | ORAL | 65862-513 |
| 45 mg/1 | TABLET | ORAL | 70518-4519 |
| 30 mg/1 | TABLET | ORAL | 50090-7846 |
+ 3 more variants
Detailed information about Pioglitazone Hydrochloride
Pioglitazone is an oral antidiabetic medication belonging to the thiazolidinedione class, used primarily to improve glycemic control in adults with type 2 diabetes mellitus by enhancing insulin sensitivity.
The dosing of pioglitazone must be individualized based on the patient's glycemic response and tolerability.
Pioglitazone is not approved for use in pediatric patients. The safety and effectiveness of pioglitazone in children under the age of 18 have not been established. Clinical trials in pediatric populations have not demonstrated sufficient efficacy to warrant approval, and concerns regarding long-term effects on bone health and weight gain are particularly relevant in this age group.
No dosage adjustment is generally required for patients with renal impairment (kidney disease). Because the drug is primarily eliminated through the liver and feces, kidney function does not significantly alter the clearance of pioglitazone. However, because these patients may be at higher risk for fluid retention, they should be monitored closely for signs of heart failure.
Pioglitazone should not be initiated in patients with active liver disease or those with significantly elevated liver enzymes (ALT > 2.5 times the upper limit of normal). For patients with mild hepatic impairment, use with caution. If a patient develops jaundice or other signs of liver injury while on the drug, therapy should be discontinued immediately.
In general, no specific dose adjustment is needed for elderly patients based solely on age. However, healthcare providers should be mindful that older adults are at a higher risk for bone fractures and congestive heart failure, both of which are known risks associated with pioglitazone therapy. A lower starting dose may be considered to assess tolerability.
If you miss a dose of pioglitazone, take it as soon as you remember on the same day. If you do not remember until the next day, skip the missed dose and take your next dose at the regular time. Do not take two doses at once to make up for a missed one, as this increases the risk of side effects.
In the event of an overdose, contact your local poison control center or seek emergency medical attention immediately. Symptoms of overdose are generally consistent with an exaggeration of the drug's side effects, such as severe swelling or significantly low blood sugar (hypoglycemia), especially if taken with other diabetes medications. While pioglitazone alone rarely causes hypoglycemia, an overdose in combination with insulin or sulfonylureas can be life-threatening.
> Important: Follow your healthcare provider's dosing instructions. Do not adjust your dose without medical guidance. Regular follow-up appointments are necessary to monitor your progress and check for potential side effects.
Pioglitazone is generally well-tolerated, but some side effects occur frequently. The most common include:
Pioglitazone is a powerful metabolic regulator that requires careful medical supervision. It is not suitable for patients with type 1 diabetes or for the treatment of diabetic ketoacidosis. Patients should be aware that the medication takes several weeks to reach its full effect and should not be discontinued without consulting a physician.
Congestive Heart Failure Risk: The FDA mandates a boxed warning for pioglitazone because it can cause the body to retain extra fluid, which puts a significant strain on the heart. This can lead to new heart failure or make existing heart failure worse. Patients with a history of heart disease must be exceptionally cautious. If you have been diagnosed with New York Heart Association (NYHA) Class III or IV heart failure, you should not take this medication.
There are few absolute contraindications for drug combinations with pioglitazone, but certain drugs significantly alter its metabolism.
There are specific medical conditions where pioglitazone must NEVER be used due to the high risk of life-threatening complications:
FDA Pregnancy Category C (under the older system). There are no adequate and well-controlled studies of pioglitazone in pregnant women. In animal studies, pioglitazone was associated with delayed parturition and embryotoxicity at high doses.
It is not known whether pioglitazone is excreted in human milk, though it has been detected in the milk of lactating rats. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants (such as hypoglycemia), a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Pioglitazone is a potent and selective agonist for the Peroxisome Proliferator-Activated Receptor-gamma (PPAR-γ). These receptors are nuclear receptors (receptors found inside the cell nucleus) that regulate the expression of numerous genes involved in lipid and glucose metabolism.
When pioglitazone binds to PPAR-γ, it forms a complex with the Retinoid X Receptor (RXR). This complex then binds to specific DNA sequences called Peroxisome Proliferator Response Elements (PPREs). This binding 'turns on' the transcription of genes that increase the production of glucose transporters (GLUT1 and GLUT4) and enzymes involved in glucose oxidation. The result is a significant increase in insulin sensitivity in the liver, skeletal muscle, and adipose tissue.
Additionally, pioglitazone has some affinity for PPAR-alpha, which helps modulate lipid metabolism, leading to a decrease in triglycerides and an increase in HDL ('good') cholesterol. This dual activity is thought to provide a more favorable cardiovascular metabolic profile than other drugs in the same class.
Common questions about Pioglitazone Hydrochloride
Pioglitazone is an oral medication used to improve blood sugar control in adults with type 2 diabetes mellitus. It works as an insulin sensitizer, making the body's cells more responsive to the insulin already being produced. It is typically prescribed alongside a healthy diet and regular exercise program. It can be used alone or in combination with other diabetes medications like metformin or insulin. It is not intended for the treatment of type 1 diabetes or diabetic ketoacidosis.
The most frequently reported side effects of pioglitazone include swelling (edema) in the legs or ankles, weight gain, and upper respiratory tract infections like the common cold. Some patients also experience headaches or muscle aches shortly after starting the medication. Weight gain is common and is often caused by a combination of fluid retention and changes in how the body stores fat. While these are common, they should still be discussed with a healthcare provider to ensure they do not become severe.
It is generally advised to limit alcohol consumption while taking pioglitazone. Alcohol can interfere with blood sugar management and may increase the risk of experiencing low blood sugar (hypoglycemia), especially if you are also taking other diabetes medications. Additionally, both pioglitazone and excessive alcohol can place stress on the liver. If you choose to drink, it should be done in moderation and only after discussing it with your doctor to ensure it is safe for your specific health profile.
Pioglitazone is generally not recommended for use during pregnancy. There is limited data on its safety in humans, and animal studies have suggested potential risks to the developing fetus. Most healthcare providers recommend switching to insulin therapy during pregnancy, as insulin is the gold standard for maintaining safe blood sugar levels for both the mother and the baby. If you are taking pioglitazone and planning to become pregnant, you should consult your doctor to discuss a safer alternative.
Pioglitazone does not lower blood sugar immediately. Because it works by affecting gene expression and the production of new proteins in the cells, the process takes time. You may begin to see a slight decrease in blood sugar within 1 to 2 weeks, but the full therapeutic effect is typically not achieved for 8 to 12 weeks. It is important to continue taking the medication exactly as prescribed, even if you do not see an immediate change in your glucose readings.
You should not stop taking pioglitazone without first consulting your healthcare provider. Stopping the medication abruptly can cause your blood sugar levels to rise significantly, which may increase the risk of diabetes-related complications. If you need to discontinue the drug due to side effects or a change in treatment plan, your doctor will provide instructions on how to safely transition to another medication. Always maintain a consistent supply of your medication to avoid missing doses.
If you miss a dose of pioglitazone, take it as soon as you remember on the same day. However, if you do not remember until the following day, skip the missed dose entirely and take your next scheduled dose at the normal time. Never take two doses at once to 'catch up,' as this can increase the risk of side effects like severe swelling or low blood sugar. Setting a daily alarm can be a helpful way to ensure you take your medication consistently.
Yes, weight gain is a well-documented side effect of pioglitazone. This weight gain occurs through two primary mechanisms: fluid retention (edema) and the redistribution of body fat into subcutaneous areas. While the increase in weight can be frustrating, some studies suggest that the redistribution of fat away from internal organs (visceral fat) may actually have some metabolic benefits. However, if you experience a very rapid weight gain of more than 3-5 pounds in a few days, you should contact your doctor immediately, as this could be a sign of heart failure.
Pioglitazone is frequently taken with other medications, but some combinations require caution. It is often paired with metformin or sulfonylureas to improve blood sugar control. However, taking it with insulin significantly increases the risk of fluid retention and heart failure. Some medications, like the cholesterol drug gemfibrozil, can dangerously increase the levels of pioglitazone in your blood. Always provide your doctor and pharmacist with a complete list of all prescriptions, over-the-counter drugs, and herbal supplements you are taking.
Yes, pioglitazone is available as a generic medication, which is typically much more affordable than the brand-name version, Actos. Generic pioglitazone is required by the FDA to have the same active ingredient, strength, dosage form, and route of administration as the brand-name drug. It must also prove bioequivalence, meaning it works in the body the same way. Most insurance plans cover the generic version of pioglitazone, making it a cost-effective option for long-term diabetes management.
Other drugs with the same active ingredient (Pioglitazone)
> Warning: Stop taking Pioglitazone and call your doctor immediately if you experience any of these serious symptoms.
Prolonged use of pioglitazone (usually more than one year) is associated with a gradual decrease in bone mineral density. This increases the risk of osteoporosis-related fractures. Additionally, long-term use requires ongoing monitoring for bladder health. Patients should also be aware that the weight gain associated with the drug may persist as long as the medication is taken.
The FDA has issued a Black Box Warning for pioglitazone regarding the risk of Congestive Heart Failure (CHF). Thiazolidinediones, including pioglitazone, cause or exacerbate congestive heart failure in some patients. After initiation of pioglitazone, and after dose increases, patients should be observed carefully for signs and symptoms of heart failure (including excessive, rapid weight gain, dyspnea, and/or edema). If these signs and symptoms develop, the heart failure should be managed according to current standards of care, and discontinuation or dose reduction of pioglitazone must be considered. Pioglitazone is not recommended in patients with symptomatic heart failure and is contraindicated in patients with established NYHA Class III or IV heart failure.
Report any unusual symptoms to your healthcare provider. Early detection of side effects is key to managing your health while on this medication.
To ensure the safe use of pioglitazone, your doctor will require regular monitoring:
Pioglitazone itself does not usually cause drowsiness or impair coordination. However, if taken with other diabetes medications (like insulin or sulfonylureas), it can contribute to low blood sugar (hypoglycemia). Symptoms of low blood sugar include dizziness, shakiness, and confusion, which can make driving or operating machinery dangerous. Always ensure your blood sugar is stable before engaging in these activities.
Alcohol can affect blood sugar levels and may increase the risk of hypoglycemia when taking pioglitazone. Furthermore, excessive alcohol consumption can strain the liver, which is already a concern for patients on this medication. It is generally advised to limit alcohol intake and discuss your habits with your doctor.
Do not stop taking pioglitazone suddenly unless instructed by your doctor (for example, if you experience a serious side effect). Stopping the medication will likely lead to a rise in blood sugar levels. If the drug must be stopped, your doctor will provide a plan to transition you to a different therapy.
> Important: Discuss all your medical conditions with your healthcare provider before starting Pioglitazone. Transparency about your heart, liver, and bladder history is vital for your safety.
Pioglitazone can cause small decreases in hemoglobin and hematocrit levels (usually 2-4%). This is generally due to an increase in plasma volume (dilutional effect) rather than actual anemia. It may also cause a slight decrease in ALT levels, which is actually a sign of improved liver fat content in many diabetic patients.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking. Even over-the-counter products can influence how pioglitazone works in your body.
These are conditions where the drug may be used, but only with extreme caution and frequent monitoring:
There is a potential for cross-sensitivity among members of the thiazolidinedione class. If a patient experienced severe edema or liver issues with Rosiglitazone (Avandia), they may be more likely to experience similar issues with Pioglitazone. However, there is no known cross-reactivity with sulfonylureas or metformin.
> Important: Your healthcare provider will evaluate your complete medical history before prescribing Pioglitazone. Ensure you disclose any history of heart, liver, or bladder issues.
Pioglitazone is not approved for use in children under 18. In a 26-week trial of pediatric patients with type 2 diabetes, pioglitazone did not show a statistically significant improvement in HbA1c compared to placebo. Given the risks of weight gain and potential long-term effects on bone development, its use is not recommended in this population.
Clinical studies did not identify significant differences in safety or effectiveness between patients over 65 and younger patients. However, the geriatric population is naturally at higher risk for:
No dosage adjustment is required in patients with renal impairment. Pioglitazone and its metabolites are primarily eliminated via the feces. However, patients with kidney disease are often more sensitive to fluid balance changes, so monitoring for edema is critical.
Pioglitazone should not be started if the patient exhibits clinical evidence of active liver disease or increased serum transaminase levels (ALT > 2.5 times the upper limit of normal) at the start of therapy. For patients with mild hepatic impairment, the drug should be used with caution, and liver enzymes should be monitored more frequently.
> Important: Special populations require individualized medical assessment. Always inform your doctor if you are planning to become pregnant or are over the age of 65.
| Parameter | Value |
|---|---|
| Bioavailability | > 80% |
| Protein Binding | > 99% (mainly Albumin) |
| Half-life (Parent Drug) | 3 - 7 hours |
| Half-life (Metabolites) | 16 - 24 hours |
| Tmax (Time to Peak) | ~2 hours |
| Metabolism | Hepatic (CYP2C8, CYP3A4) |
| Excretion | Fecal (85%), Renal (15%) |
Pioglitazone is the primary representative of the Thiazolidinedione (TZD) class. It is also classified as a PPAR-gamma agonist. It is distinct from other antidiabetics like Biguanides (Metformin), Sulfonylureas (Glipizide), and SGLT2 inhibitors (Empagliflozin) because of its unique focus on improving insulin sensitivity at the nuclear level.