Glimepiride + Rosiglitazone
Indications
Glimepiride + Rosiglitazone is used for:
Type 2 DM
Adult Dose
Type 2 Diabetes
Starting Dose: 1 tab (4mg/1mg) qDay with first meal of day
Titrate: glimepiride component increased not to exceed 2 mg q1-2 week
Not to exceed 8 mg rosiglitazone/4 mg glimepiride
Elderly: Starting Dose: 1 tab (4mg/1mg) qDay with first meal of day
Titrate dose carefully
Hepatic impairment
Starting dose: 1 tab (4mg/1mg) qDay with first meal of day; titrate carefully
ALT <2.5 xULN: Use caution
ALT >2.5 xULN: Do not administer
ALT >3 xULN or jaundice after initiating therapy: Discontinue
Child Dose
Safety and efficacy not established
Renal Dose
Renal impairment, starting dose: 1 tab (4mg/1mg) qDay with first meal of day; titrate carefully
Administration
Contra Indications
Patients with established Class III or IV heart failure is contraindicated.
Precautions
Hypoglycemia: All sulfonylurea drugs are capable of producing severe hypoglycemia. Proper patient selection, dosage, and instructions are important to avoid hypoglycemic episodes. Debilitated or malnourished patients and those with adrenal, pituitary, renal, or hepatic insufficiency are particularly susceptible to the hypoglycemic action of glucose lowering drugs.
Loss of Control of Blood Glucose:
When a patient stabilized on any antidiabetic regimen is exposed to stress such as fever, trauma, infection, or surgery, a temporary loss of glycemic control may occur.
Edema:
Combination of Glimepiride and Rosiglitazone should be used with caution in patients with edema.
Since thiazolidinediones, including Rosiglitazone can cause fluid retention, which can exacerbate or lead to congestive heart failure, Combination of Glimepiride and Rosiglitazone should be used with caution in patients at risk for heart failure.
Weight Gain:
Dose-related weight gain was seen with Rosiglitazone alone and in combination with other hypoglycemic agents.
Hepatic Effects:
Liver enzymes should be checked prior to the initiation of therapy with combination of Glimepiride and Rosiglitazone in all patients and periodically thereafter per the clinical
judgment of the healthcare professional.
Lactation: not known if crosses into breast milk, avoid
Pregnancy-Lactation
Pregnancy Category: C
Lactation: not known if crosses into breast milk, avoid
Interactions
Glimepiride: Salicylates, sulfonamides, chloramphenicol, clarithromycin, coumarin anticoagulants, probenecid, CYP2C9 inhibitors, fibric acid derivatives, disopyramide, fluoxetine, quinolones, ACE inhibitors, MAOIs and ?-blockers may potentiate the hypoglycaemic action of glimepiride. Thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, oestrogens, phenytoin, nicotinic acid, sympathomimetics and CYP2C9 inducers may reduce hypoglycaemic effect of glimepiride. Reduced plasma concentration w/ colesevelam.
Rosiglitazone: Increased plasma conc w/ gemfibrozil. Decreased plasma conc w/ rifampicin.
Side Effects
Side effects of Glimepiride + Rosiglitazone :
1-10%
Edema (3%), Myocardial infarction (<3%), Cerebrovascular accident (<2%), Cardiac failure (<3%), Headache (3-6%), Hypoglycemia (4-6%), Bone fracture (<8%), Nasopharyngitis (4-5%)
<1%
Weight gain, Cardiac failure, Increased serum ALT
Mode of Action
Glimepiride: Initial effect to increase insulin secretion from beta cells; may also decrease rate of hepatic glucose production and increase insulin receptor sensitivity.
Rosiglitazone: Lowers glucose by improving target cell response to insulin without increasing pancreatic cell secretion; activates nuclear peroxisome proliferator-activated receptor gamma, which influences the production of gene products involved in glucose and lipid metabolism.