Skip to main content

Diabetes Mellitus: Pharmacotherapy-Sulfonyl Ureas!

 


PHARMACOTHERAPY

Oral and injectable agents are available to treat patients with T2DM who are unable to achieve glycemic control through meal planning and physical activity.

Medications classifications include:

  1.  Sulfonyl Urea's
  2. Nonsylfonylurea Secretagogues (a-Glinides)
  3. Biguanides
  4. Thiazolidinediones
  5. a-Glucosidase Inhibitors
  6. Dipeptidyl Peptidase-4 Inhibitors(Gliptins)
  7. Sodium-glucose co-transporter (SGLT) Inhibitors 
  8. Central-Acting Dopamine Agonists
  9. Bile Acid Sequestrants
  10. Insulin therapy

SULFONYL UREAS

  • Sulfonylureas represent the first class of Oral blood glucose lowering agents approved by the United States.
  • These drugs are classified as either First- or Second-Generation drugs.
  • Both classes of sulfonyl ureas are effective when given at equipotent doses.

Mechanism of Action

  • Sulfonyl ureas enhance insulin secretion by blocking ATP-sensitive potassium channels in the cell membranes of pancreatic beta cells. This action results in membrane depolarization, allowing the influx of calcium to cause the translocation of secretory granules of Insulin to the cell surface and enhances insulin secretion in a non-glucose dependent manner.

Metabolism

  • All sulfonyl ureas undergo hepatic biotransformation with most agents being metabolized by Cytochrome-P450 2C9 Pathway. 
  • The first-generation sulfonyl ureas are most likely to cause drug interaction than the second-generation ones.
  • All sulfonyl ureas except Tolbutamide require dose adjustment or are not recommended for renal impairment.

Clinical Use

  • Sulfonyl ureas blood-glucose lowering agents can be observed in both Fasting and post-prandial levels.

Therapy

  • Monotherapy with these agents generally produce a 1.5-2% decline in A1c levels. and a 60-70mg/dL reduction in Fasting blood glucose levels (FBG).

Adverse Drug Reactions

  • Hypoglycemia
  • Weight Gain
  • Sulfa allergy


**ONLY SULFONYL UREAS THAT DOESNOT REQUIRE DOSE ADJUSTMENTS IS TOLBUTAMIDE**

Labels:

Comments

Post a Comment

Popular posts from this blog

Diabetes Mellitus: Non-Pharmacological Therapy--MNT!

 NON PHARMACOLOGICAL THERAPY  MNT Glycemic Index Dietary supplements Weight measurements Physical Activity Psychological assessment Immunizations 1. MEDICAL NUTRITION THERAPY (MNT)  " Medical Nutrition Therapy (MNT) is a term used by the ADA to describe the optimal condition of caloric intake with other aspects of diabetes therapy (Insulin, Exercise, Weight loss)". The ADA has issued recommendations for three types of MNT: Primary prevention measures of MNT are directed at preventing or delaying the onset of type 2 Diabetes in high-risk individuals (obese or with pre-diabetes) by promoting weight reduction. Secondary prevention measures of MNT are directed at preventing or delaying-related complications in diabetic individuals by improving glycemic control. Tertiary prevention measures of MNT are directed at managing diabetes-related complications (cardiovascular disease, neuropathy) in diabetic individuals. Despite the popular notion, there is not any " Diabetic diet...
Post a Comment
Read more

PNEUMONIA- Its Etiology, Pathophysiology, Classification and Severity Assessment Method!

 PNEUMONIA Definition: "Pneumonia is an infection of pulmonary parenchyma". (Harrison)                                                    OR "Pneumonia is defined as an acute respiratory illness associated with recently developed radiological pulmonary shadowing which may be segmental, lobar or multilobar". (Davidson) Etiology: Microorganisms gain excess to the lower respiratory tract in several ways: Aspiration from the oropharynx (most common). Inhalation of contaminated droplets. Hematogenous spread. Contiguous extension. Pathophysiology of Pneumonia: Pneumonia results from proliferation of microbial pathogens at the alveolar level and the hosts response to these microorganisms.  Defensive Mechanisms against Pneumonia: The defensive mechanism against pneumonia involve: Branching architecture of tracheobronchial tree. Muco-ciliary clearance. Local...
Post a Comment
Read more

Anatomy and the Complications Associated with Liver Diseases!

  LIVER AND THE COMPLICATIONS ASSOCIATED WITH THE PROGRESSION OF DISEASE! Liver: The liver weighs up to 1.5kg in adults and is the 2nd largest organ in the body. Hepatocytes are the functioning unit of liver. Impairment of liver may lead to: Acute liver diseases Chronic liver diseases Liver cirrhosis Acute Liver Disease (ALD): ALD is a self-limiting episode of hepatocyte damage which in most cases spontaneously without clinical sequelae, but acute liver failure (ALF) may develop. This is a rare condition in which there is a rapid deterioration in liver function with associated encephalopathy and coagulopathy. ALF carries significant morbidity and mortality and may require emergency liver transplant. Chronic Liver Disease (CLD): CLD occurs when the longstanding cell damage causes permanent structural changes within the liver, with the loss of normal liver structure and functions. In many cases, this may lead to cirrhosis where fibrosis sears divide the liver cells into areas of rege...
Post a Comment
Read more