|| See TERMINOLOGY & ABBREVIATIONS ||
|Indication(s) & Dosage||Type 2 diabetes mellitus
Adult: For patients who are inadequately controlled on rosiglitazone monotherapy: Usual starting dose: 1000 mg of metformin per day plus the dose of rosiglitazone patient is already taking. For patients who are inadequately controlled on metformin monotherapy: Usual starting dose: 4 mg of rosiglitazone per day plus the dose of metformin patient is already taking. Titrate dose in steps of 4 mg of rosiglitazone and/or 500 mg of metformin if adequate control is not seen in 1-2 wk after an increase in metformin dosage, or 8-12 wk after an increase in rosiglitazone dosage. Daily max dose: 8 mg rosiglitazone/2000 mg metformin; given in 2 divided doses.
Child: Not recommended in children aged below 18 yr.
Elderly: Generally do not titrate to maximum dosage.
Hepatic impairment: Do not initiate if patient exhibits evidence of active liver disease or baseline ALT>2.5x upper limit of normal (ULN).
|Overdose||Supportive treatment is recommended. Metformin: Lactic acidosis may occur. Accumulated drug may be removed by haemodialysis.|
|Contraindications||New York Heart Association (NYHA) class I to IV heart failure, acute coronary syndrome, ischaemic heart disease, significant renal disease or renal dysfunction, acute or chronic metabolic acidosis including diabetic ketoacidosis, Type 1 DM, patients undergoing radiologic studies involving admin of IV iodinated contrast material.|
|Special Precautions||Restrict for use in Type 2 DM patients who are unable to achieve adequate glycaemic control with other medications. Caution in patients with oedema as rosiglitazone can cause fluid retention which may cause or exacerbate CHF. Not recommended for use in patients with peripheral arterial disease. Caution in elderly. Avoid use in patients with hepatic disease or renal impairment. Check renal function and liver enzymes at baseline and periodically thereafter. Renal function should be monitored at least annually and more frequently if renal dysfunction is expected. Monitor patients for signs and symptoms of heart failure and lactic acidosis. Risk of lactic acidosis increases with renal impairment, hepatic insufficiency, excess alcohol intake, dehydration, sepsis and acute CHF. May cause resumption of ovulation in some premenopausal anovulatory female, hence contraception is recommended. In patients undergoing radiologic studies with intravascular iodinated contrast materials, discontinue drug temporarily at the time or before the procedure, and for 48hr after the procedure; reinstate drug only after renal function has been evaluated to be normal. Co-admin with insulin or nitrates is not recommended. Do not use during pregnancy and lactation.|
|Adverse Drug Reaction(s)||Rosiglitazone:
Upper respiratory tract infections, nasopharyngitis, sinusitis, constipation, hypertension, back pain, increased risk of bone fractures (especially in
females), fatigue, hypoglycaemia; dose-related wt gain, oedema and anaemia; macular ordema, hepatitis, elevated liver enzymes, hyperlipedaemia. Metformin:
Anorexia, nausea, vomiting, diarrhoea, wt loss, flatulence, occasional metallic taste; weakness; hypoglycaemia; rash, malabsorption of vit B12.
Potentially Fatal: CHF, possible increased risk of myocardial ischaemia; lactic acidosis in presence of renal failure and alcoholism.
|Drug Interactions||Rosiglitazone: Increased effect with NSAIDs, pioglitazone, gemfibrozil, fluconazole, sulfonamides. Decreased effect with carbamazepine,
phenytoin, secobarbital, phenobarbital and rifampin. Metformin: Additive effect with sulphonylureas. Antagonistic effects with diuretics, corticosteroids,
phenothiazines, thyroid products, oestrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, Ca channel blockers and isoniazid.
Potentially Fatal: Rosiglitazone: Increased effect with NSAIDs, pioglitazone, gemfibrozil, fluconazole, sulfonamides. Decreased effect with carbamazepine, phenytoin, secobarbital, phenobarbital and rifampin. Metformin: Additive effect with sulphonylureas. Antagonistic effects with diuretics, corticosteroids, phenothiazines, thyroid products, oestrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, Ca channel blockers and isoniazid. Please consult detailed drug interactions before prescribing.
|Food Interaction||May decrease rosiglitazone levels when used with St John's wort. Avoid alcohol.|
|Pregnancy Category (FDA)||Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.|
|Storage||Oral: Store at 25Â°C.|
|Pharmacology||Rosiglitazone is a thiazolidinedione antidiabetic agent which targets insulin resistance by lowering blood-glucose level without
increasing pancreatic insulin secretion. Its action is dependent on the presence of insulin. Metformin improves glucose tolerance in patients with type 2
diabetes, lowering both basal and post-prandial blood glucose. It decreases hepatic gluconeogenesis, decreases intestinal absorption of glucose, and improves
insulin sensitivity by increasing peripheral glucose uptake and utilisation.
Absorption: Rosiglitazone: Absolute bioavailbility: About 99%; Tmax: about 1 hr. Metformin: Absolute bioavailability: About 50-60% (fasting condition).
Distribution: Rosiglitazone: About 99.8% is protein bound (primarily to albumin). Metformin: Negligible protein-binding; steady-state concentration reached within 24-48 hr. Partitions into erythrocytes.
Metabolism: Rosiglitazone: Extensively metabolised by N-demethylation and hydroxylation, followed by sulphate and glucuronic acid conjugation to less potent metabolites. Metformin: Not metabolised by liver.
Excretion: Rosiglitazone: Urine (64%); faeces (23%); 3-4 hr (elimination half-life). Metformin: Urine (as unchanged drug); about 90% of absorbed dose is excreted via renal route. Plasma and blood half-life prolonged in renal impairment.
|ATC Classification||A10BA02 - metformin; Belongs to the class of
biguanides. Used in the treatment of diabetes.
A10BG02 - rosiglitazone; Belongs to the class of thiazolidinediones. Used in the treatment of diabetes.
Total Products : 10
|Brand Name||Manufacturer/Marketer||Composition||Dosage Form||Pack Size & Price|
|AROMET-1||Aristopharma Ltd.||Rosiglitazone 1mg+ Metformin hydrochloride 500mg||Film Coated Tablet||30's: 120.00 MRP|
|AROMET-2||Aristopharma Ltd.||Rosiglitazone 2mg+ Metformin hydrochloride 500mg||Film Coated Tablet||30's: 180.00 MRP|
|METARIN Plus||Popular Pharmaceuticals Ltd.||Rosiglitazone 1mg+ Metformin hydrochloride 500mg||Film Coated Tablet||30's: 120.62 MRP|
|METIGLIT 1||General Pharmaceuticals Ltd||Rosiglitazone 1mg+ Metformin hydrochloride 500mg||Film Coated Tablet||30's: 120.60 MRP|
|METIGLIT 2||General Pharmaceuticals Ltd||Rosiglitazone 2mg+ Metformin hydrochloride 500mg||Film Coated Tablet||30's: 180.60 MRP|
|ORAMET-PLUS||Drug International Ltd||Rosiglitazone 2mg+ Metformin hydrochloride 500mg||Film Coated Tablet||50's: 350.00 MRP|
|ROGMET 2||Pacific Pharmaceuticals Ltd.||Rosiglitazone 2mg+ Metformin hydrochloride 500mg||Film Coated Tablet||30's: 180.00 MRP|
|ROSIMET-1||Delta Pharma Limited||Rosiglitazone 1mg+ Metformin hydrochloride 500mg||Film Coated Tablet||30's: 120.00 MRP|
|ROSIMET-2||Delta Pharma Limited||Rosiglitazone 2mg+ Metformin hydrochloride 500mg||Film Coated Tablet||30's: 180.00 MRP|
|ROSIMIN 1||The White Horse Pharma||Rosiglitazone 1mg+ Metformin hydrochloride 500mg||Film Coated Tablet||30's: 120.00 MRP|