Actos: Effective Glycemic Control for Type 2 Diabetes
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| Product dosage: 30mg | |||
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Synonyms | |||
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Actos (pioglitazone hydrochloride) is a thiazolidinedione antidiabetic agent indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It functions as an insulin sensitizer, targeting insulin resistance—a core pathophysiological defect in this metabolic disorder. By activating peroxisome proliferator-activated receptor gamma (PPAR-γ), it enhances cellular response to endogenous insulin, thereby reducing hepatic glucose output and improving peripheral glucose uptake. Clinical studies demonstrate its efficacy in lowering HbA1c, fasting plasma glucose, and postprandial glucose levels, offering a mechanism distinct from other oral antidiabetic classes. Proper patient selection and monitoring are essential to maximize therapeutic benefits while managing potential risks.
Features
- Active ingredient: Pioglitazone hydrochloride
- Available in tablet strengths: 15 mg, 30 mg, and 45 mg
- Administration: Oral, once daily with or without food
- Mechanism: Selective agonist for peroxisome proliferator-activated receptor gamma (PPAR-γ)
- Prescription-only medication requiring regular glycemic monitoring
- Compatible with other antidiabetic agents including metformin, sulfonylureas, and insulin
Benefits
- Significantly reduces HbA1c levels by improving insulin sensitivity in muscle, adipose tissue, and the liver
- Lowers fasting and postprandial blood glucose concentrations with once-daily dosing convenience
- May have beneficial effects on lipid profiles, often reducing triglycerides and increasing HDL cholesterol
- Does not cause hypoglycemia when used as monotherapy
- Provides a complementary mechanism of action for use in combination therapy regimens
- May help preserve beta-cell function over the long term
Common use
Actos is commonly prescribed for the management of type 2 diabetes mellitus in adults when glycemic control is not adequately achieved through diet and exercise alone. It is frequently used as monotherapy or in combination with other antidiabetic medications including metformin, sulfonylureas, or insulin when additional glycemic control is required. The medication is particularly valuable for patients demonstrating significant insulin resistance, as identified through clinical assessment and laboratory parameters. Healthcare providers may consider Actos when other first-line agents are contraindicated, poorly tolerated, or insufficient for achieving target glycemic goals. Regular monitoring of glycemic parameters, liver function, and cardiovascular status is recommended throughout therapy.
Dosage and direction
The recommended starting dose of Actos is 15 mg or 30 mg orally once daily, with or without food. Dosage may be increased gradually, in increments of 15 mg, after assessing glycemic response and tolerance, with a maximum recommended daily dose of 45 mg. For combination therapy with insulin, the initial Actos dose should be 15 mg or 30 mg once daily, and insulin dosage may need downward adjustment if hypoglycemia occurs. Dose adjustments should be made carefully in patients with hepatic impairment, and the medication is not recommended in patients with active liver disease or ALT levels >2.5 times the upper limit of normal. Response to therapy should be evaluated after 3-4 months of treatment, with HbA1c used as the primary efficacy parameter. If inadequate response is observed despite maximum tolerated dosage, alternative or additional therapeutic options should be considered.
Precautions
Before initiating Actos therapy, perform liver enzyme tests to establish baseline values; discontinue if ALT levels exceed 3 times the upper limit of normal during treatment. Monitor for signs and symptoms of heart failure, as thiazolidinediones can cause fluid retention that may exacerbate or lead to heart failure. Use with caution in patients with edema, particularly when used in combination with insulin. Regular ophthalmologic examinations are recommended, as thiazolidinediones may increase risk of diabetic macular edema. Monitor bone health as long-term use has been associated with increased risk of fractures, particularly in women. Observe patients for weight gain, which may occur due to fluid retention and fat accumulation. Hemoglobin and hematocrit levels may decrease during therapy, typically during the first 4-12 weeks of treatment. Use with particular caution in premenopausal anovulatory women, as the medication may restore ovulation, increasing pregnancy risk.
Contraindications
Actos is contraindicated in patients with known hypersensitivity to pioglitazone or any component of the formulation. It must not be used in patients with established New York Heart Association (NYHA) Class III or IV heart failure. The medication is contraindicated in patients with active liver disease or ALT levels exceeding 2.5 times the upper limit of normal. It is not recommended for use in patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis. Actos is contraindicated in patients with bladder cancer or a history of bladder cancer, and should be used with extreme caution in patients with risk factors for bladder cancer including smoking history or exposure to certain occupational chemicals. The medication is not indicated for use in children under 18 years of age.
Possible side effect
Common side effects (occurring in >5% of patients) include upper respiratory tract infection, headache, sinusitis, myalgia, tooth disorder, and diabetes mellitus aggravated. Hypoglycemia may occur when used in combination with insulin or insulin secretagogues. Weight gain of 2-4 kg occurs in some patients, typically during the first year of treatment. Edema and fluid retention have been reported in 4-6% of patients receiving monotherapy and up to 15% when combined with insulin. Less common but serious adverse reactions include congestive heart failure (particularly when used with insulin), fractures (mainly in female patients), macular edema, and hepatic enzyme elevations. Rare cases of hepatitis and hepatic failure have been reported, though causal relationship remains uncertain. Urinary bladder cancer has been observed in epidemiological studies with prolonged use.
Drug interaction
Actos may interact with strong CYP2C8 inhibitors (such as gemfibrozil) which can significantly increase pioglitazone exposure—consider dose reduction if coadministration is necessary. Inducers of CYP2C8 (such as rifampin) may decrease pioglitazone concentrations, potentially reducing efficacy. Concurrent use with other hypoglycemic agents including insulin, sulfonylureas, or meglitinides may increase the risk of hypoglycemia, requiring dose adjustment of these medications. Medications that cause fluid retention (such as NSAIDs) may exacerbate the fluid-retaining effects of pioglitazone. Oral contraceptives containing ethinyl estradiol and norethindrone may have decreased efficacy when coadministered with Actos. Atorvastatin appears to have no clinically significant effect on pioglitazone pharmacokinetics. Regular monitoring is recommended when initiating or discontinuing concomitant medications.
Missed dose
If a dose of Actos is missed, it should be taken as soon as remembered on the same day. However, if it is almost time for the next scheduled dose, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not take a double dose to make up for a missed one. Consistency in daily administration is important for maintaining stable glycemic control, so patients should be counseled on establishing a routine for medication intake. If multiple doses are missed, patients should contact their healthcare provider for guidance, as glycemic control may be compromised. Use of pill organizers or reminder systems may help improve adherence for patients with frequent missed doses.
Overdose
Cases of overdose with Actos have been reported with doses up to 120 mg daily. The primary expected manifestation would be hypoglycemia, particularly when combined with other hypoglycemic agents. Additional symptoms may include excessive fluid retention leading to peripheral edema or potentially heart failure exacerbation. There is no specific antidote for pioglitazone overdose. Management should include supportive measures with close monitoring of blood glucose, electrolyte balance, and cardiac status. Hypoglycemia should be treated appropriately with oral carbohydrate or intravenous dextrose based on severity and patient consciousness. Hemodialysis is unlikely to be effective due to high protein binding of pioglitazone. Gastric lavage may be considered if ingestion was recent. Patients should be observed for at least 24-48 hours due to the medication’s prolonged half-life.
Storage
Store Actos tablets at controlled room temperature, 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C and 30°C (59°F and 86°F). Keep the medication in its original container with the lid tightly closed to protect from moisture and light. Do not store in bathrooms or other areas with high humidity. Keep out of reach of children and pets. Do not use tablets that are discolored, damaged, or beyond the expiration date printed on the packaging. Proper disposal of unused medication is important; consult a pharmacist or use medication take-back programs rather than flushing down toilets or throwing in household trash.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Actos is a prescription medication that should be used only under the supervision of a qualified healthcare professional. Individual patient responses may vary, and treatment decisions should be based on the healthcare provider’s assessment of the specific clinical situation. Patients should not initiate, adjust, or discontinue medication without consulting their healthcare provider. The complete prescribing information should be consulted for comprehensive details regarding use, warnings, and precautions. This summary does not include all possible information about this medication and cannot replace professional medical judgment.
Reviews
Clinical trials demonstrate that Actos produces significant reductions in HbA1c, typically ranging from 0.5% to 1.5% depending on baseline levels and concomitant therapies. Many endocrinologists note its particular effectiveness in insulin-resistant patients who have responded inadequately to metformin alone. Patient reviews often mention improved energy levels and reduced thirst and urination symptoms associated with hyperglycemia. Some patients report dissatisfaction with weight gain side effects, while others consider the glycemic benefits to outweigh this concern. Healthcare providers frequently emphasize the importance of appropriate patient selection and monitoring, particularly regarding cardiac and hepatic parameters. Long-term observational studies continue to provide data on real-world effectiveness and safety profiles in diverse patient populations.