Pharmacology

• What is pharmacokinetics about?

  What the body does to the API
• What are the symptoms discussed in the study material related to the GI tract?

  Acid indigestion, heartburn, and ulcers
• What inorganic treatment options are discussed for acid indigestion and ulcers?

  Antacids and alginate raft formulations
• What is the role of H2 receptor antagonists in treating ulcers?

  They reduce gastric acid release
• How does knowledge of structure activity relationships influence drug development?

  It helps in designing effective drugs
• What are prodrugs and their significance in treating ulcers?

  Inactive until converted to active drugs
• What is the mechanism of action of PPIs?

  They irreversibly inhibit the proton pump
• What condition results from excess acid production?

  Acid indigestion
• What causes heartburn?

  Excess acid in the oesophagus
• What are the main anti-ulcer therapies mentioned?

  Antacids, H2 antagonists, and PPIs
• What is the global spending on antacids according to the WHO?

  More than $10 billion annually
• Why is the demand for antacids expected to grow?

  Due to an ageing population and stress
• What are common examples of antacids?

  CaCO3, NaHCO3, Mg(OH)2
• What is the reaction of Al(OH)3 with HCl?

  Al(OH)3 + 3 HCl → AlCl3 + 3 H2O
• What side effect can magnesium compounds cause?

  Diarrhea
• What can excessive use of NaHCO3 lead to?

  Gas production and alkaline urine
• How do alginates help prevent acid reflux?

  They form a neutralizing layer in the stomach
• What happens when alginates react with stomach acid?

  They form a gel-like substance
• What is the role of anti-foaming agents in antacid formulations?

  They prevent gas formation and reduce flatulence
• What is the significance of the pharmacophore in drug design?

  It is responsible for the drug's activity
• What is the purpose of Structure Activity Relationships (SAR)?

  To modify and test drug structures for activity
• What is the natural agonist for the H2-receptor?

  Histamine
• What is the main action of H2-receptor antagonists?

  They block histamine from stimulating acid release
• What is a significant feature of the H2-receptor antagonist design?

  Modification of the natural agonist histamine
• What condition can result from administering H2-receptor antagonists?

  Kidney damage and granulocytopenia
• What is the role of protonation in the mechanism of PPIs?

  It activates the prodrug to the active form
• What is the significance of the pH in the activation of PPIs?

  They are activated in acidic conditions
• What is the target enzyme for PPIs?

  H+/K+-ATPase
• What is chiral switching in drug development?

  Switching to a pure enantiomer for patenting
• What is the advantage of PPIs over H2 antagonists?

  They act on the final stage of HCl release
• What are the key features of PPIs and their mechanism of action?

  • PPIs are prodrugs activated in acidic conditions.
  • They irreversibly inhibit the proton pump (H+/K+-ATPase).
  • They have few side effects due to selectivity.
  • They concentrate at the target site in parietal cells.
• What are the main therapeutic approaches for treating ulcers?

  1. Antacids
  2. H2 receptor antagonists
  3. Proton pump inhibitors (PPIs)
  4. Alginate raft formulations
• What are the side effects of antacids?

  • Magnesium compounds may cause diarrhea.
  • Aluminium compounds may cause constipation.
  • Carbonates may lead to gas production.
• What are the structural features important for H2-receptor antagonists?

  • Heterocyclic ring is crucial for activity.
  • Amine group can be modified.
  • Extending the carbon chain is beneficial.
• What are the advantages of using prodrugs?

  • They are inactive until converted in the body.
  • They can improve drug targeting and reduce side effects.