Pioglitazone + Metformin


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Type 2 diabetes mellitus
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.
Nhóm bệnh nhân đặc biệt
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).
Suy thận
CrCl (mL/min) Dosage
<60 Contraindicated.
Suy gan
Contraindicated.
Cách dùng
Should be taken with food.
Chống chỉ định
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.
Thận trọng
Patient w/ oedema, anaemia. Premenopausal, anovulatory women. Pregnancy.
Tác dụng không mong muốn
Oedema, wt gain, hypoglycaemia, macular oedema, bone fractures, anaemia, upper resp infection, headache, diarrhoea, nausea, UTI, sinusitis.
Potentially Fatal: Lactic acidosis, CHF, bladder cancer, hepatic failure.
Thông tin tư vấn bệnh nhân
This drug may cause visual disturbance, if affected, do not drive or operate machinery.
Chỉ số theo dõi
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.
Tương tác
May impair vit B12 absorption. Increased plasma levels w/ strong CYP2C8 inhibitors (e.g. gemfibrozil). Decreased plasma levels w/ CYP2C8 inducers (e.g. rifampicin). Reduced metabolism w/ cationic drugs eliminated by renal tubular secretion.
Tương tác với thức ăn
Alcohol may increase the risk of lactic acidosis, avoid use.
Tác dụng
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.
Đặc tính

Chemical Structure Image
Pioglitazone

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 4829, Pioglitazone. https://pubchem.ncbi.nlm.nih.gov/compound/Pioglitazone. Accessed Nov. 23, 2023.


Chemical Structure Image
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.

Bảo quản
Store at 25°C. Protect from light and humidity.
Phân loại MIMS
Thuốc trị đái tháo đường
Phân loại ATC
A10BD05 - metformin and pioglitazone ; Belongs to the class of combinations of oral blood glucose lowering drugs. Used in the treatment of diabetes.
Tài liệu tham khảo
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 Hydrochloride. 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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