Podcast Beta
Questions and Answers
What is the primary mechanism of action of sulphonylureas?
Which condition is a contraindication for using Metformin?
What distinguishes meglitinide analogues from sulphonylureas?
Which of the following is a serious adverse event associated with Metformin?
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Which of the following antidiabetic drugs is best known for causing weight gain?
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Which of the following statements about Thiazolidinediones is true?
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What is a common adverse effect of Thiazolidinediones?
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Which of the following best describes the clinical use of Meglitinide analogues?
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Which of the following pharmacokinetics characteristics applies to Thiazolidinediones?
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Study Notes
Sulphonylureas
- Mechanism involves binding to sulphonylurea receptors on pancreatic β-cells.
- Blockage of KATP channels leads to increased insulin secretion.
- Requires at least 30% functioning β-cells for effectiveness.
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Examples:
- Short-acting: Glipizide
- Long-acting: Gliclazide (Diamicron) and Glimepiride (Amaryl)
- Pharmacokinetics: Administer orally before breakfast and possibly dinner; highly protein-bound (interactions with drugs like warfarin).
- Adverse effects: Commonly cause hypoglycemia and weight gain.
Meglitinide Analogues
- Mechanism is similar to sulphonylureas but binds to a different site.
- Examples: Repaglinide and Nateglinide.
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Clinical Use:
- Rapidly acting, taken 30 minutes before meals.
- Less risk of hypoglycemia and weight gain compared to sulphonylureas.
- Suitable for individuals with an irregular lifestyle.
Biguanides (Metformin)
- Mechanism reduces hepatic glucose production (gluconeogenesis) and increases glucose uptake in skeletal muscle through AMP kinase activation.
- Also reduces insulin resistance.
- Pharmacokinetics: Taken orally 2-3 times daily; sustained release formulations available.
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Adverse effects:
- Can cause gastrointestinal upsets.
- Risk of lactic acidosis (rare), contraindicated in patients with renal, hepatic, hypoxic, respiratory, or cardiac diseases; also avoid use before iodine-containing X-ray contrast media.
- Clinical Use: First-line treatment for overweight or obese patients with type 2 diabetes; compatible with other antidiabetic medications, including insulin.
Thiazolidinediones (TZDs or Glitazones)
- Mechanism acts as insulin sensitizers by activating PPAR-γ receptors.
- Enhances transcription of insulin-sensitive genes predominantly in adipose tissue, skeletal muscle, and liver.
- Examples: Pioglitazone and Rosiglitazone.
- Pharmacokinetics: Taken orally, once daily.
- Adverse effects: Associated with weight gain, fluid retention, and decreased bone density. Contraindicated in heart failure, acute coronary syndrome, and hepatic impairment.
- Clinical Use: Glitazones have a slow glucose-lowering effect, with maximal benefit observed after 2-3 months; cardiovascular safety remains debatable.
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Description
Test your knowledge on sulphonylureas, including their mechanism of action, pharmacokinetics, and examples. This quiz will cover important details about drug interactions and potential adverse effects related to sulphonylureas. Prepare to dive deep into diabetes treatment options!
