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Review for the Test

Review for the Test. The Test. 57 Questions/Need to Answer 55 27 My Section 9.30-11.30p ? 1-2 minutes/question. COX-2 Physiological Role. Renin-angiotensin system blood pressure and fluid balance Ovulation and labor Wound healing Vascular endothelium Vascular remodeling.

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Review for the Test

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  1. Review for the Test

  2. The Test • 57 Questions/Need to Answer 55 • 27 My Section • 9.30-11.30p? • 1-2 minutes/question

  3. COX-2 Physiological Role • Renin-angiotensin system • blood pressure and fluid balance • Ovulation and labor • Wound healing • Vascular endothelium • Vascular remodeling

  4. Modified PGs (mostly) • Block w-oxidation • Methyls at 15 and/or 16 • Phenyl in 17-20 range • Increase Lipophilicity • Add methyls, phenyls and esters

  5. ADME: Metabolism E b E b 15 14 15 E Prevents Beta-oxidaton R 13 b O D w G 14 E R 13 O b R 14 13 Talfuprost E=Esterase, O=Oxidation, R=Reduction, b=b-Oxidation, w=w-Oxidation, D=dealkylation, G=glucuronidation

  6. Overview • Prostaglandins (PGs) and Thromboxanes (TXs) • NSAIDs • Gout

  7. PGs and TXs • Structures • Functions • Signaling • Transport • Synthesis and Degradation • PG as drugs

  8. What Prostaglandin is this? • PGE1 • PGE2 • PGF2alpha • PGG2 • PGH2 • PGI2 • TXA2 :10

  9. What Prostaglandin is this? • PGE1 • PGE2 • PGF2alpha • PGG2 • PGH2 • PGI2 • TXA2 :10

  10. What Prostaglandin is this? • PGE1 • PGE2 • PGF2alpha • PGG2 • PGH2 • PGI2 • TXA2 :10

  11. PG and TXs • Structures • Functions • Signaling • Transport • Synthesis and Degradation • PG as drugs

  12. Select the one that is not true • PGE2 relaxes vascular smooth muscle • TXA2 increases renal blood flow • PGI2 protects the gastric mucosa • PGF2alpha contracts uterine smooth muscles • PGF2alpha causes bronchoconstriction :10

  13. PG and TXs • Structures • Functions • Signaling • Transport • Synthesis and Degradation • PG as drugs

  14. Prostaglandin signaling within the cell is? • Endocrine • Autocrine • Paracrine • Intracrine :10

  15. What are not involved in Prostaglandin and Thromboxane signaling • Plasma membrane bound GPCRs • Nuclear membrane bound GPCRs • Nuclear Receptors • OATP transporter :10

  16. Prostaglandin E2 (PGE2) binds to what type of receptor • DP1 • EP1 • FP • IP • TP :10

  17. PG and TXs • Structures • Functions • Signaling • Transport • Synthesis and Degradation • PG as drugs

  18. What ways are PG and TX transported • Active Efflux • Active Influx • Passive Diffusion • All the above :10

  19. PG and TXs • Structures • Functions • Signaling • Transport • Synthesis and Degradation • PG as drugs

  20. The substrate of COX 2 is? • Arachidonic Acid • PGE1 • PGE2 • PGF2alpha • PGG2 • PGH2 • PGI2 • TXA2 :10

  21. The product of COX 2 is? • Arachidonic Acid • PGE1 • PGE2 • PGF2alpha • PGG2 • PGH2 • PGI2 • TXA2 :10

  22. What is not a mechanism of metabolism for PG? • alpha-oxidation • beta-oxidation • omega-oxidation • reduction • alcohol dehydrogenation :10

  23. How is TXB2 produced • reduction • oxidation • hydrolysis • conjugation :10

  24. Which Cytochrome P450 (CYP) is involved in w-oxidation? • CYP1A1 • CYP2C9 • CYP3A4 • CYP4A :10

  25. PG and TXs • Structures • Functions • Signaling • Transport • Synthesis and Degradation • PG as drugs

  26. NSAIDs will interfere with PG drugs because they can • Inhibit PG synthetases • Induce COX 2 expression • Reduce COX 2 expression • Inhibit COX 1 • Inhibit COX 2 • D and E :10 diclofenac

  27. What prostaglandin is Aprostadil? • PGE1 • PGE2 • TXA2 • Prostacyclin only • PGI2 only • Prostacyclin and PGI2 :10 Aprostadil

  28. What is not a use of Aprostadil • Erectile dysfunction • Congenital hear defect • Hypertension • Induce labor • A and B • C and D :10

  29. Aprostadilbinding to a GPCR causes all but the following • Increase intracellular Ca2+ • Decrease intracellular Ca2+ • Activate adenylatecyclase • Increase cAMP :10

  30. What are not formulations of Alprostadil? • IV injection • Penile injection • Oral • Urethral Suppository :10

  31. What are ADR of Alprostadil? • Pain/Rash • Light Headed • Bleeding and Bruising • Flu Symptoms • All the above :10

  32. Talfluprost

  33. The compounds on the previous pagearemodified versions of what prostaglandin? • PGE1 • PGE2 • TXA2 • PGF2a • PGI2 • 15-methyl PGF2a :10

  34. Overview • Prostaglandins (PGs) and Thromboxanes (TXs) • NSAIDs • Gout

  35. NSAIDs • COX 1, COX 2 and COX3 • COX 1/COX 2 IC50 ratios • COX 1 and COX 2 inhibitor side effects • Cancer • Structural Classes of NSAIDs

  36. NSAIDs will inhibit [blank] in a patient • COX 1 • COX 2 • COX 3 • COX 1 and COX 2 • COX 1, COX 2 and COX 3 :10

  37. COX 3 should be considered with NSAID therapeutic regiments. • True • False :10

  38. COX 1 has a larger active site than COX 2. • True • False :10

  39. NSAIDs • COX 1, COX 2 and COX3 • COX 1/COX 2 IC50 ratios • COX 1 and COX 2 inhibitor side effects • Cancer • Structural Classes of NSAIDs

  40. A new COX inhibitor has a COX-1/COX-2 IC50 ratio of 0.1. What COX enzyme is it selective for? • COX-1 • COX-2 • Non-specific • COX-3 :10

  41. NSAIDs • COX 1, COX 2 and COX3 • COX 1/COX 2 IC50 ratios • COX 1 and COX 2 inhibitor side effects • Cancer • Structural Classes of NSAIDs

  42. Inhibition of PG leads to all but the following in the GI tract • Increase HCO3 • Increase in H+ • Increase in mucus • Decrease in mucus • A and B • B and C • A and C :10

  43. What are not COX 1 side effects • GI bleeding • Hypotension • Clotting disorders • Bronchodilation • A and B • B and C • B and D :10

  44. PG inhibition leads to bronchoconstriction through • PGE2 • PGE1 • PGG2 • Leukotrienes (LT) • TXA2 :10

  45. What type of adverse side effects do you anticipate by interfering with renin-angiotensin system through COX-2 inhibition? • Hypertension • Hypertension and Renal Failure • Renal Failure • Brain Damage • None of the above :10

  46. NSAIDs • COX 1, COX 2 and COX3 • COX 1/COX 2 IC50 ratios • COX 1 and COX 2 inhibitor side effects • Cancer • Structural Classes of NSAIDs

  47. What are non COX 2 functions for NSAIDs in Cancer cells? • Block NF-kappaB signaling • Activate Peroxisome proliferator receptor • Increase Apoptosis • Activate NF-kappaB signaling • A, B and C • All the above :10

  48. Which drug is non-selective for COX 1 and COX 2 • Low dose Aspirin • High dose Aspirin • Ibuprofen • Celecoxib • All the above • B and C :10

  49. What is not a structural class of NSAIDs? • Salicylates • Profens • Fenacs • Oxicams • Statins :10

  50. Salicylates inhibit by the following mechanisms • Competitive • Irreversible • Non-competitive • Uncompetitive • A and B • B and C • All the above :10

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