Pioglitazone


Concise Prescribing Info
Indications/Uses
Type 2 DM.
Dosage/Direction for Use
Adult : PO 15 or 30 mg once daily. Max: 45 mg/day.
Dosage Details
Oral
Type 2 diabetes mellitus
Adult: 15 or 30 mg once daily, increased in increments if necessary. Max: 45 mg/day.
Elderly: No dosage adjustment needed.
Renal Impairment
No dosage adjustment needed.
Hepatic Impairment
Moderate to severe: Avoid.
Administration
May be taken with or without food.
Contraindications
Type 1 DM or diabetic ketoacidosis. Severe heart failure (NYHA class III or IV). Active or history of bladder cancer. Moderate to severe hepatic impairment. Patients w/ uninvestigated macroscopic haematuria.
Special Precautions
Symptomatic and congestive heart failure (NYHA class I or II). Mild hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Oedema, wt gain, sinusitis, upper resp tract infections, hepatic dysfunction (e.g. vomiting, unexplained nausea, anorexia, dark urine, abdominal pain, fatigue), bone loss and fracture, myalgia, visual disturbances; decreased haemoglobin and haematocrit counts (dose related); decreased serum triglycerides, increased HDL-cholesterol; abnormal LFT.
Potentially Fatal: Rare: Mixed hepatocellular-cholestatic liver injury and liver failure; hepatitis.
Patient Counseling Information
Adequate contraception is recommended in premenopausal anovulatory women as pioglitazone may cause resumption of ovulation.
MonitoringParameters
Monitor for signs and symptoms of heart failure (e.g. dyspnoea, rapid wt gain, unexplained fatigue or cough), bladder cancer (e.g. blood in urine, urinary urgency, pain on urination, or back or abdominal pain), and fluid retention. Periodically monitor fasting plasma glucose levels. LFT should be performed prior to treatment and monitor periodically.
Drug Interactions
Increased risk of oedema w/ insulin, metformin and sulfonylureas. Increased plasma levels w/ gemfibrozil and ketoconazole. Decreased plasma levels w/ rifampicin.
Action
Description: Pioglitazone is as a potent and highly selective agonist for the peroxisome proliferator activated receptor-γ (PPAR-γ). Activation of these receptors promotes the production of gene products involved in lipid and glucose metabolism. It also improves insulin response to target cells w/o increasing the pancreatic secretion of insulin.
Onset: Delayed.
Pharmacokinetics:
Absorption: Rapidly absorbed. Bioavailability: >80%. Time to peak plasma concentration: Approx 2 hr.
Distribution: Volume of distribution: 0.63 L/kg. Plasma protein binding: >99% (mainly to albumin).
Metabolism: Extensive hepatic metabolism via CYP2C8 and CYP3A4 isoenzymes to its active and inactive metabolites.
Excretion: Via urine (15-30%); faeces (as metabolites). Elimination half-life: 3-7 hr (parent drug).
Storage
Store at 25°C.
MIMS Class
References
Actos Tablet (Takeda Pharmaceutical America, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 07/11/2013.

Anon. Pioglitazone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/11/2013.

Buckingham R (ed). Pioglitazone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/11/2013.

Joint Formulary Committee. Pioglitazone. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/11/2013.

McEvoy GK, Snow EK, Miller J et al (eds). Pioglitazone. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 06/11/2013.

Disclaimer: This information is independently developed by MIMS based on Pioglitazone from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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