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Diabetes Mellitus: Pharmacotherapy- Glinides and Biguanides!

 PHARMACOTHERAPY

2.NONSULFONYLUREA SECRETAGOGUES (GLINIDES)

  • Although producing the same effects as sulfonyl ureas, Non sulfonylurea secretogogues also referred to as Glinides or Meglitinides have rapid onset and short duration of action.

Mechanism of Action:

  • Glinides produce a pharmacological action by interacting with ATP-Sensitive potassium channels on the beta cells; however, this binding is to a receptor adjacent to those with which the sulfonyl ureas bind.

Clinical Uses:

  • The primary benefit is in reducing post-meal glucose levels.
  • These agents have resulted in a reduction of 0.8-1% A1c levels.

Indications:

  • Because they have a rapid onset of action, Glinides are supposed to be taken 15-30 minutes before the meal.

Therapy:

  • They may also be used in combination therapy with other drugs to achieve synergistic effects.
  • Combinations with Biguanides is mostly used.


3.BIGUANIDES

  • Biguanides include Metformin as the Drug of choice for T 2 DM.

Mechanism of Actions:

  • Biguanides are thought to lower the blood glucose levels by decreasing hepatic glucose production and increasing insulin sensitivity in both hepatic and peripheral muscle tissues; however, the exact mechanism of action is unknown. 

Clinical uses:

  • Metformin reduces both Fasting Blood Glucose levels and post-meal glucose levels.
  • It has shown to reduce A1c levels by 1.5-2% and FPG levels by 60-80mg/dL when used as a monotherapy.
  • Unlike sulfonylureas, metformin retains the ability to reduce fasting blood glucose levels when they are used over 300mg/dL.
  • Metformin does not affect insulin release from beta cells of the pancreas, so hypoglycemia is not a common side effect.
  • Metformin significantly reduces all-cause mortality and the risk of strokes in overweight patients with T2DM compared to the insensitivity therapy with sulfonylurea or Insulin.
  • It also reduces Diabetes-related death and Myocardial infarction as compared with a conventional Arm therapy.
  • ADA treatment algorithm considers Lifestyle modification and Metformin therapy as the first line therapy for T 2 DM 
  • Metformin has shown to produce beneficial effects on serum lipid levels and has become first-line agents for T2 DM patients with metabolic syndrome.
  • On average, Triglyceride levels and LDL levels may be reduced by as much as 18.69%-12.09% respectively and HDL levels may improve by as much as 1.17%.

Therapy:

  • Metformin is often used in combination with sulfonyl urea or Thiazolidinedione (TZD) for synergistic effects.

Pharmacokinetics:

  • Metformin does not undergo significant protein binding and is eliminated from the body via urine unchanged.

Contraindications:

  • Metformin is contraindicated in patients with:

  1. patients having creatinine clearance less than 60mL/min.
  2. Patients with serum creatinine levels > than or = to 1.4mg/dL in women and 1.5mg/dL in men.
  3. It should not be initiated in patients of 80 years of age or older unless renal function has been established.
  4. Patients undergoing radiographic procedures in which nephrotoxic dye is used.
  5. Biguanides inhibit mitochondrial oxidation of lactic acid, thereby increasing the chances of lactic acidosis occurring..
  6. Metformin should be withheld in pt. with cases of hypoxemia, sepsis or dehydration.
  7. Patients should avoid consumption of excessive alcohol with Metformin intake.

Adverse Drug Reactions:

  • Primary side effects include:

                         GIT upset, Decreased appetite, Nausea, Diarrhea

  • Interference with Vitamin B12 absorption is also reported.


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