glimepiride/rosiglitazone

Action and Spectrum

Actions and Spectrum 

glimepiride is a sulfonylurea which stimulates the pancreas production of insulin, which is how it works to treat diabetes. The greater amount of insulin is released as a result of it binding to the sulfonylurea receptor on pancreatic beta cells.  

By enhancing insulin sensitivity and secretion, glimepiride largely lowers blood glucose levels. rosiglitazone belongs to the thiazolidinedione class of medications.

Peroxisome proliferator-activated receptor-gamma (PPAR-γ) is activated in target tissues to function as an insulin sensitizer. It effectively lowers blood glucose levels both before and after meals.

Drug Interaction

Adverse Reaction

Frequency defined  

<1% 

Cardiac failure 

Increased serum ALT 

Weight gain 

1-10% 

Edema (3%) 

Headache (3-6%) 

Nasopharyngitis (4-5%) 

Cardiac failure (≤3%) 

Hypoglycemia (4-6%) 

Bone fracture (≤8%) 

Myocardial infarction (≤3%) 

Cerebrovascular accident (≤2%) 

Post marketing Reports  

Thrombocytopenic purpura 

Thrombocytopenia 

Black Box Warning

Black Box Warning 

glimepiride, carries a black box warning regarding the risk of hypoglycemia. Elderly people, people who are undernourished, and people who have liver or renal problems may be more at risk of developing hypoglycemia.  

Following starting the medication and following dose increases, closely monitor the patient for any signs or symptoms of heart failure, such as excessive weight gain or dyspnoea. 

rosiglitazone carries a black box warning related to an increased risk of cardiovascular events, including myocardial infarction and heart related deaths. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Previous history of hypersensitivity to rosiglitazone/glimepiride or any of its ingredients. 
• Previous history of sulfonamide derivative allergy. 
• Diabetes-related ketoacidosis, with or without coma  

Caution: 

• glimepiride should be used with caution in patients who are at an increased risk of hypoglycemia.  
• rosiglitazone should be used with caution, and the potential cardiovascular risks should be carefully considered in patients with a history of heart disease. 

Pregnancy / Lactation

Pregnancy consideration: 

Pregnancy category: C 

Lactation: Excretion into human milk is unknown  

Pregnancy Categories:         

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.  

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women. 

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 

Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology  

glimepiride binds sulfonylurea receptors on the pancreatic beta cells, leading to closure of ATP-sensitive potassium channels and subsequent depolarization of the cell membrane. 

The activation of PPAR-γ in rosiglitazone leads to increased insulin sensitivity and increased glucose uptake in peripheral tissues, and improved glycemic control. 

Pharmacodynamics 

In peripheral tissues including muscle and adipose tissue, glimepiride increases insulin sensitivity. Insulin resistance is decreased as a result of improved glucose absorption and utilization by these tissues. 

rosiglitazone helps reduce blood glucose levels by increasing insulin sensitivity. It enhances glycemic management by lowering insulin resistance, which affects both fasting and postprandial blood glucose levels. 

Pharmacokinetics 

Absorption   

glimepiride/rosiglitazone both rapidly absorbed from the gastrointestinal tract after oral administration. 

Distribution 

glimepiride has a relatively small volume of distribution whereas rosiglitazone has a large volume of distribution.  

Metabolism 

glimepiride/rosiglitazone both undergoes extensive metabolism in the liver by cytochrome P450 enzymes, primarily through CYP2C9. 

Elimination and excretion 

The metabolites of glimepiride are excreted in the urine. The elimination half-life of glimepiride is approximately 5 to 9 hours. 

The metabolites of rosiglitazone are excreted in both urine and feces. The elimination half-life of rosiglitazone is approximately 3 to 4 hours. 

Adminstartion

Administration 

glimepiride/rosiglitazone are typically administered orally in form of tablets.

Patient Information Leaflet

Patient information leaflet 

Generic Name: glimepiride/rosiglitazone 

Why do we use glimepiride/rosiglitazone? 

glimepiride/rosiglitazone primarily used to lower blood glucose levels in individuals with type 2 diabetes.  

glimepiride is used to control both fasting and postprandial blood glucose levels. 

rosiglitazone acts as an insulin sensitizer, enhancing the sensitivity of target tissues such as adipose tissue, liver and muscle to insulin.