Adult: Each immediate-release tab contains pioglitazone 15 mg and metformin 500 mg or pioglitazone 15 mg and metformin 850 mg: Initially, 15 mg/500 mg bid or 15 mg/850 mg once daily. Patients inadequately controlled on metformin monotherapy: Initially, 15 mg/500 mg bid or 15 mg/850 mg 1-2 times daily, depending on current metformin dose. Patients inadequately controlled on pioglitazone monotherapy: Initially, 15 mg/500 mg bid or 15 mg/850 mg once daily. Max: Pioglitazone 45 mg and metformin 2,550 mg daily. Each extended-release tab contains pioglitazone 15 mg and metformin 1,000 mg or pioglitazone 30 mg and metformin 1,000 mg: Initially, 15 mg/1,000 mg or 30 mg/1,000 mg once daily. Patients inadequately controlled on metformin or pioglitazone monotherapy: 15 mg/1,000 mg bid or 30 mg/1,000 mg once daily. Max: Pioglitazone 45 mg and metformin 2,000 mg daily. Doses may be titrated gradually according to response.
Special Patient Group
Patient taking pioglitazone and metformin w/ an insulin secretagogue (e.g. sulfonylurea): Decrease insulin secretagogue dose. Patient taking pioglitazone and metformin w/ insulin: Decrease insulin dose by 10-25%. Patient taking pioglitazone and metformin w/ strong CYP2C8 inhibitors: Max: 15 mg/850 mg daily (immediate-release tab) or 15 mg/1,000 mg daily (extended-release tab).
Renal Impairment
CrCl (mL/min)
Dosage
<60
Contraindicated.
Hepatic Impairment
Contraindicated.
Administration
Should be taken with food.
Contraindications
Current or history of cardiac failure (New York Heart Association stage I to IV), active or history of bladder cancer, uninvestigated macroscopic haematuria; type 1 DM, diabetic ketoacidosis or diabetic pre-coma; acute or chronic disease which may cause tissue hypoxia (e.g. cardiac or resp failure, recent MI, shock); conditions which may alter renal function (e.g. dehydration, severe infection, shock). Acute alcohol intoxication. Hepatic or renal impairment (CrCl <60 mL/min). Lactation. Intravascular admin of iodinated contrast agents.
This drug may cause visual disturbance, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor HbA1c, serum glucose; signs and symptoms of oedema or heart failure, bladder cancer; liver enzymes, haematologic parameters, renal function; vit B12 and folate if anaemia is present. Routine ophth examination.
Alcohol may increase the risk of lactic acidosis, avoid use.
Action
Description: Mechanism of Action: Pioglitazone reduces hepatic glucose output and increases peripheral glucose disposal by increasing insulin sensitivity thru activation of specific nuclear receptors (peroxisome proliferator activated receptor-γ (PPAR-γ). Metformin decreases hepatic glucose production by inhibiting gluconeogenesis and glycogenolysis, delays intestinal glucose absorption and improves insulin sensitivity by increasing peripheral glucose uptake and utilisation. Pharmacokinetics: Absorption: Pioglitazone: Rapidly absorbed from the GI tract. Bioavailability: >80%. Time to peak plasma concentration: W/in 2 hr. Metformin: Slowly and incompletely absorbed from the GI tract. Bioavailability: Approx 50-60%. Distribution: Pioglitazone: Plasma protein binding: >99%. Metformin: Crosses the placenta and enters breast milk. Metabolism: Pioglitazone: Extensively metabolised by CYP2C8 isoenzyme to both active and inactive metabolites. Metformin: Not metabolised in the liver. Excretion: Pioglitazone: Via urine and faeces. Plasma half-life: Up to 7 hr. Metformin: Via urine. Elimination half-life: Approx 2-6 hr.
Chemical Structure
Pioglitazone Source: National Center for Biotechnology Information. PubChem Database. Pioglitazone, CID=4829, https://pubchem.ncbi.nlm.nih.gov/compound/Pioglitazone (accessed on Jan. 22, 2020)
Metformin Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 4091, Metformin. https://pubchem.ncbi.nlm.nih.gov/compound/Metformin. Accessed Feb. 27, 2023.
A10BD05 - metformin and pioglitazone ; Belongs to the class of combinations of oral blood glucose lowering drugs. Used in the treatment of diabetes.
References
Actoplus Met XR Tablet, Film Coated, Extended Release (Takeda Pharmaceuticals America, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 20/10/2015.Anon. Pioglitazone and Metformin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 20/10/2015.Buckingham R (ed). Metformin Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/10/2015.Buckingham R (ed). Pioglitazone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/10/2015.Pioglitazone and Metformin Hydrochloride Tablet, Film Coated (Teva Pharmaceuticals USA Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 20/10/2015.
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