PHRD5915 Drug Design Lecture 5 - Prodrugs I

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daynuhmay
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PHRD5915 Drug Design Lecture 5 - Prodrugs I
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2014-03-14 05:55:32
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prodrugs
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prodrugs
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  1. group on a drug that helps cross the BBB
    lipophilic group (fatty chain)
  2. optimum partition coefficient for biological activity (potency)
    log P0

    (=k/2k')
  3. axes on graph that can help determine log P0
    chain length (x) vs. potency (y)
  4. one of first prodrugs developed (used commonly today)
    aspirin (acetyl salicylic acid)
  5. prodrugs that utilize hydrolysis for drug activation
    carrier-linked
  6. prodrugs that are designed to improve site specificity
    redox drug carrier systems
  7. prodrugs that generally utilize enzymatic modification followed by spontaneous active drug formation for drug activation
    bioprecursors
  8. natural prodrugs of morphine
    • codeine
    • heroin
  9. target of omeprazole
    H+K+-ATPase (cysteine 813 residue of extracellular domain)
  10. sulphenamide intermediate of omeprazole is in the center
  11. what activates and gives Prilosec increased site selectivity?
    acid
  12. purpose of ester prodrugs
    improve topical absorption

    (acne, psoriasis)
  13. activator of ester prodrugs
    carboxylesterases
  14. purpose of phosphate prodrugs
    improve water solubility
  15. aspirin (1.drug, 2.enzyme activator, 3.disease)
    • 1. salicylic acid
    • 2. esterase
    • 3. pain/inflammation
  16. pivampicillin (1.drug, 2.enzyme activator, 3.disease)
    • 1. ampicillin
    • 2. esterase
    • 3. anti-bacterial
  17. codeine (1.drug, 2.enzyme activator, 3.disease)
    • 1) morphine
    • 2) CYP450
    • 3) pain
  18. docarpamine (1.drug, 2.enzyme activator, 3.disease)
    • 1) dopamine
    • 2) esterase/amidase
    • 3) Parkinson's
  19. progabide (1.drug, 2.enzyme activator, 3.disease)
    • 1) GABA
    • 2) esterase/amidase
    • 3) Epilepsy
  20. etopophos (1.drug, 2.enzyme activator, 3.disease)
    • 1) etoposide
    • 2) phosphatase
    • 3) anti-cancer
  21. prednisolone phosphate (1.drug, 2.enzyme activator, 3.disease)
    • 1) prednisolone
    • 2) phosphatase
    • 3) inflammation
  22. dipivalyl epinephrine (1.drug, 2.enzyme activator, 3.disease)
    • 1) epinephrine
    • 2) esterase
    • 3) glaucoma
  23. nitro-mustards (1.drug, 2.enzyme activator, 3.disease)
    • 1) mustard agents
    • 2) NADPH/P450 reductase
    • 3) cancer
  24. CPT4 (1.drug, 2.enzyme activator, 3.disease)
    • 1) camptothecin
    • 2) NQO1
    • 3) cancer
  25. irinotecan (1.drug, 2.enzyme activator, 3.disease)
    • 1) camptothecin
    • 2) esterase
    • 3) cancer
  26. BDMA (1.drug, 2.enzyme activator, 3.disease)
    • 1) valium
    • 2) P450
    • 3) sedative
  27. dopamine DHP (1.drug, 2.enzyme activator, 3.disease)
    • 1) dopamine
    • 2) NADH-trans hydrogenase
    • 3) Parkinson's
  28. Prilosec (1.drug, 2.enzyme activator, 3.disease)
    • 1) omeprazole sulfenamide
    • 2) stomach acid
    • 3) acid reflux
  29. tazarotene (1.drug, 2.enzyme activator, 3.disease)
    • 1) tazarotenic acid
    • 2) esterase
    • 3) acne
  30. fosphenytoin (1.drug, 2.enzyme activator, 3.disease)
    • 1) phenytoin
    • 2) phosphatase
    • 3) epilepsy
  31. Nexium (1.drug, 2.enzyme activator, 3.disease)
    • 1) esomeprazole sulfenamide
    • 2) stomach acid
    • 3) acid reflux
  32. tramadol (1.drug, 2.enzyme activator, 3.disease)
    • 1) O-desmethyl tramadol
    • 2) CYP2D6
    • 3) analgesic/pain
  33. dabigatran etexilate (1.drug, 2.enzyme activator, 3.disease)
    • 1) dabigatran
    • 2) carboxy esterase
    • 3) stroke/anticoagulant
  34. Tamiflu (1.drug, 2.enzyme activator, 3.disease)
    • 1) olseltamivir carboxylate
    • 2) carboxy esterase
    • 3) influenza
  35. bambuterol (1.drug, 2.enzyme activator, 3.disease)
    • 1) terbutaline
    • 2) butyrylcholinesterase 
    • 3) asthma&COPD/bronchodilator
  36. AZT (1.drug, 2.enzyme activator, 3.disease)
    • 1) AZT-triphosphate
    • 2) host thymidine-kinase
    • 3) HIV/AIDS
  37. valacyclovir (1.drug, 2.enzyme activator, 3.disease)
    • 1) acyclovir
    • 2) esterase
    • 3) herpes virus
  38. PR104 (1.drug, 2.enzyme activator, 3.disease)
    • 1) PR104M
    • 2) NADPH/P450 reductase & phosphatase
    • 3) cancer

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