Pharmacology Exam 6

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Pharmacology Exam 6
2011-04-16 16:01:34
Serotonin kinins

Serotonin & kinins
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  1. Serotonin
    • 5-Hydroxytryptamine
    • autocoid
    • neurotransmitter in CNS and enteric nervous system
    • local hormone that modulates GI activity
  2. Serotonin is stored in
    entero-chromaffin cells of the gut and CNS
  3. 5-HT metabolized by ___ and ____ to ____, which is extreted in the urine and is used to measure excess 5-HT production
    • monoamine oxidase and aldehyde dehydrogenase
    • product is 5-HIAA which can be measured in the urine
  4. Patients with ____ will excrete large amounts of 5-HIAA
    malignant carcinoid
  5. # of serotonin receptors
  6. 5HT1 agonists
  7. 5HT2 antagonists
    • ketanserine
    • cyproheptadine
    • ergot alkaloids
  8. 5HT3 antagonists
  9. yellow circumscribed tumor that occurs in the small intestine, appendix, stomach or colon
    • carcinoid
    • releases a lot of 5-HT
  10. 5-HT is released by platelets during
  11. 5-HT causes vasoconstricion by stimulating _____ receptors. This can be blocked by ____.
    • 5HT2
    • ketanserine
  12. 5-HT causes vasodilation by stimulating ____ receptors.
  13. 5-HT causes ____ and _____ by interacting with both 5HT1 and 5HT3 receptors
    positive inotropic and chronotropic effects
  14. Other actions of 5HT
    • increase GI motility
    • cause uterine contractions
    • cause bronchial contractions
  15. 5HT3 receptor
    • not g protein coupled
    • Na+/K+ channel
  16. Ketanserine
    • 5HT1c antagonist
    • 5HT2 antagonist
    • alpha1-adrenergic antagonist
  17. alpha 1 adrenergic receptor antagonist
    • ketanserine
    • lowers blood pressure
  18. Methysergide receptor and uses
    • 5HT1 antagonist
    • migraine prophylaxis
    • vascular headaches
    • horton's syndrome
    • ineffective for active migrane
    • toxicity limits use
  19. cyproheptadine receptors and uses
    • 5HT2 blocker
    • H1 blocker
    • muscarinic cholinergic blocker
    • treatment of post gastrectomy dumping syndrome
    • intestinal hypermotility in carcinoid tumor
  20. Buspirone receptor and use
    • 5HT1A agonist
    • non-benzodiazepine anxiolytic
  21. sumatriptan receptor and uses
    • 5HT1D partial agonists
    • accute migrane and cluster headache
    • cAMP contraction of arterial smooth muscle, esp in carotid and cranial circulation
    • PO, SC and Nasal spray
    • drug of choice for sever migraine headaches with n/v
  22. Cisapride receptor and uses
    • 5HT4 agonist
    • compassionate use in GERD and motility disorders
  23. Tegaserod receptor and uses
    • 5HT4 patial agonist
    • for IBS with constipation
  24. Antagonists of the 5HT3 receptor
    • ondansetron
    • granisetron
    • tropiseron
    • batanopride
  25. Uses of 5HT3 receptor antagonists
    control n/v resulting from intestinal vagal nerve and central CTZ stimulation from surgery or chemo/radio therapy
  26. major side effects of 5HT3 antagonists
    • headache
    • constipation
  27. Clozapine receptor and use
    • 5HT2 blocker
    • antipsychotic agent
    • little or no extrapyramidal side effects
  28. Bradykinin
    nona-peptide derived from kininogens
  29. Kallindin
    decapeptide derived from kininogens
  30. involved in synthesis of bradykinin and kallidin
    tissue and plasma kallikreins
  31. synthesis and metabolsm of kinins
    • catabolized my kininase II (ACE)
    • short 15 sec t1/2
  32. HMW kininogen + Plasma kallkrein =>
  33. LMW kininogen + tissue kallikreins =>
  34. Breaks down bradykinin and kallidin to inactive fragments
    kinases I and II
  35. changes kallidin into bradykinin
  36. Three kinins identified in mammals
    • bradykinin
    • lysylbradykinin (kallidin)
    • methionyllysylbradykinin
    • all contain bradykinin
  37. Physiological action of bradykinin and kallidin as autocoids
    • increase vascular permeability
    • produce vasodilation
    • increase synthesis of prostaglandins
    • cause pain and edema
  38. Bradykinin and kallidin contribute to pathogenesis of
    inflammatory diseases such as allergis, arthritis, asthma, sepsis, IBD, rhinitis
  39. four classis symptoms of inflammation produced by bradykinin
    • redness
    • heat
    • swelling
    • pain
  40. Rapidly generated after tissue injury and play a pivital role in the development and maintenance of these inflammatory processes
  41. Kinin B1 receptors
    located in aorta and mesenteric veins
  42. Kinin B2 receptors
    • located in the jugular vein and carotid arteries
    • g-protein coupled
    • more widespread than B1
  43. analogues of des Arg9-bradykinin or des Arg10-kallidine are selective antagonists for
    kinin B1 receptor
  44. analogues of (dephen7) bradykinin are antagonists for
    • kinin B2 receptor
    • widely used in animal studies but inactive on human B2 receptors
  45. Icatibant
    • 2nd gen B2 receptor antagonist
    • orally effective potent and selective for b2 in humans
    • treatment of hereditary angioedema and pain
    • t 1/2 60 min
  46. Fr173657 and NPC18884
    • 3rd generation kinin B2 antagonist
    • orally active
    • treatment of inflammatory pain in humans
    • t1/2 = 90 min
  47. Activation of B2 kinin receptors in all tissues leads to
    stimulation of PI-PLC resulting in formation of inositol phosphates and DAG => increase Ca2+ levels
  48. Bradykinin induced increases in Ca2+ of human airway smooth muscle are mediated both by
    • activation of PI-PLC
    • calcium influx via receptor operated calcium channels