Pioglitazone: Indication, Dosage, Side Effect, Precaution

Generic Medicine Info Patient Medicine Information

This information is not country-specific. Please refer to the Malaysia prescribing information.

Generic Medicine Info

Indications and Dosage

Oral
Type 2 diabetes mellitus

Adult: As an adjunct to diet and exercise to improve glycaemic control: Monotherapy or in combination with other antidiabetic agents: 15-30 mg once daily. May increase dose in 15 mg daily increments every 4-12 weeks, as needed. Max: 45 mg daily. Dosing recommendations may vary among individual products and between countries (refer to specific product guidelines).

Special Patient Group

Patient taking gemfibrozil and other strong CYP2C8 inhibitors: Max: 15 mg daily.

Hepatic Impairment

Contraindicated.

Administration

May be taken with or without food.

Contraindications

History or current heart failure (New York Heart Association [NYHA] stages I-IV); diabetic ketoacidosis, active or history of bladder cancer; uninvestigated macroscopic haematuria, hepatic impairment.

Special Precautions

Patient with oedema, risk factors for CHF (e.g. previous MI, symptomatic coronary artery disease). Elderly. Pregnancy and lactation.

Adverse Reactions

Significant: Decreased Hb or haematocrit, hypoglycaemia (if combined with other antidiabetic agents or insulin), macular oedema with decreased visual acuity, weight gain; increased risk of bladder carcinoma, bone fracture (higher risk in women), and cardiac failure; fluid retention, resumption of ovulation.
Blood and lymphatic system disorders: Anaemia.
Eye disorders: Visual disturbance.
Gastrointestinal disorders: Flatulence.
General disorders and administration site conditions: Oedema.
Musculoskeletal and connective tissue disorders: Arthralgia.
Nervous system disorders: Hypo-aesthesia, headache, dizziness.
Renal and urinary disorders: Haematuria.
Reproductive system and breast disorders: Erectile dysfunction.
Respiratory, thoracic and mediastinal disorders: Upper respiratory tract infection, dyspnoea, bronchitis.
Potentially Fatal: Very rarely, hepatic failure.

Pregnancy Category (US FDA)

PO: C

Monitoring Parameters

Monitor HbA_1c (at least twice yearly in patients with stable glycaemic control; quarterly in patients not meeting therapy goals or with changes in treatment); serum glucose; liver function (e.g. ALT, AST, alkaline phosphatase, total bilirubin) at baseline (for all patients) and periodically during therapy for patients with active or suspected liver disease; weight. Monitor for signs and symptoms of liver injury, fluid retention, heart failure, and bladder cancer.

Drug Interactions

Increased serum concentration with strong CYP2C8 inhibitors (e.g. gemfibrozil). Decreased serum concentration with CYP2C8 inducers (e.g. rifampicin), and topiramate.

Action

Description:
Mechanism of Action: Pioglitazone, a thiazolidinedione, is 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 without increasing the pancreatic secretion of insulin.
Onset: Delayed.
Pharmacokinetics:
Absorption: Rapidly absorbed. Bioavailability: >80%. Time to peak plasma concentration: Approx 2 hours; delayed with food.
Distribution: Apparent volume of distribution: 0.63 ± 0.41 L/kg. Plasma protein binding: >99%, mainly to albumin.
Metabolism: Extensively metabolised in the liver via hydroxylation and oxidation by CYP2C8 and CYP3A4 isoenzymes to active (e.g. M-III and M-IV) and inactive metabolites.
Excretion: Via urine (15-30%) and faeces, as metabolites. Elimination half-life: Pioglitazone: 3-7 hours; M-III and M-IV metabolites: 16-24 hours.

Chemical Structure

Storage

Store between 20-25°C. Protect from light, moisture, and humidity.

MIMS Class

Antidiabetic Agents

ATC Classification

A10BG03 - pioglitazone ; Belongs to the class of thiazolidinediones. Used in the treatment of diabetes.

References

Actos (Takeda Pharmaceutical Co., Ltd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 04/03/2022.

Actos 45 mg Tablets (Neon Healthcare Limited). MHRA. https://products.mhra.gov.uk. Accessed 04/03/2022.

Anon. Pioglitazone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/03/2022.

Buckingham R (ed). Pioglitazone Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/03/2022.

Joint Formulary Committee. Pioglitazone. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/03/2022.

Mylan New Zealand Ltd. Vexazone, 15 mg, 30 mg & 45 mg Tablets data sheet 16 February 2021. Medsafe. http://www.medsafe.govt.nz. Accessed 04/03/2022.

Pioglitazone Hydrochloride (Aurobindo Pharma Limited). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/03/2022.

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 © 2023 MIMS. All rights reserved. Powered by MIMS.com