L20: Pharmacology Exam 1

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mherco
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169596
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L20: Pharmacology Exam 1
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2012-09-08 10:03:23
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Pharmacology
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Exam 1 Pharmacology Drugs - L20
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  1. What is the rate limiting step in the renin/angiotensin system?
    Renin
  2. What are the effects of the renin/angiotensin system at AT1 and AT2 recepors?
    • Renal Effects:
    •    Constrict efferent arterioles
    •    Increase sodium reabsorption in proximal tubule
    •    Increase Aldosterone
    •    Increase ADH

    • Other Effects:
    •    Increase syNS
    •    Vasoconstrict
    •    Vascular/cardiac remodeling
    •    Hypertrophy and hyperplasia
  3. Describe: Aliskiren (Tektura)
    • Renin Inhibitor
    • Function: Prevent the formation of Angiotensin I
  4. Describe: Captopril, lisinopril, enalapril, benazepril
    • ACE Inhibitors
    • Function: Increase bradykinin levels + reduce ANG II levels
  5. Describe: Losartan, candesartan, irbesartan, eprosartan
    • ANG II Receptor Antagonists
    • Competitive antagonist at AT-1 Receptor
  6. What are the effects of bradykinins at B1 and B2 receptors?
    • Vasodilation
    • Bronchoconstriction
    • Increased vascular permeability
    • Pain mediation
  7. Describe: Icatibant
    • Competitive antagonist to B2 receptors for Bradykinin
    • Function: lower pain, lower hyperplasia, lower inflammation and bronchoconstriction
  8. Describe: Aprotinin
    • Inhibits synthesis of Bradykinins
    • Can be used in conjunction with NSAIDs
  9. What are the effects of endothelium at the ETa and ETb receptors (GPCR receptors)?
    • Vasoconstriction
    • Nonvascular smM contraction
    • SmM proliferation
    • Positive inotrophy
    • Cardiovascular regulation
  10. Describe: Bosentan, Ambrisentan, Sitaxsentan
    • Antagonists of endothelin receptors
    • Function: Treat pulmonary hypertension
  11. Define the signaling cascade of ETa receptors?
    ETa - PLC - IP3 + DAG - Increase Calicum release from SR
  12. Defien the signaling cascade of ETb receptors?
    ETb - PGI2 + NO - Decrease Calcium realease - vasodilation + actions as a mitogen to stimulate cell proliferation
  13. Describe: Nesiritide, ularitide
    • Treatment of refractory heart failure
    • Ularitide: Phase III for decompensated heart failure
  14. Describe: Omapatrilat, sampatrilat, fasidotrilat
    • Neutral Endopeptidase Inhibitors
    • Function: Decrease peripheral resistance and BP; may be useful to treat CHF - not approved due to angioedema
  15. What are the 2 improtant subclasses of Tachykinins?
    • Substance P: Pain perception/response through dorsal horn
    • Neurokinin A and B: Contraction of smooth muscle
  16. Describe: Aprepitant
    • Neurokinin-1R antagonist
    • Function: Chemotherapy induced emesis
  17. Describe the function fo the 3 major vasopressin subclasses?
    • V1A: Vasocontriction
    • V1B: Increase release of ACTH in Pituitary
    • V2: Water reabsorption in kidney (ADH like)
  18. Describe the location and function of the Calcitonin Gene Related Peptides (CGRP)?
    • Location: CNS and PNS
    • Function: Migranes (release from CN V), peripheral cardiovascular regulation, potent vasodilator
  19. Describe the location and function of Neurotensin?
    • Location: CNS, GI tract, circulation
    • Effects: Neurotransmitter/neuromodulator in CNS (may play role in Schizophrenia, PD, drug abuse) and important in the GI to regulate acid/pepsin secretion and Gi motility
  20. Describe function of Adrenomedullin?
    Physiological antagonist against endogenous vasoconstrictors
  21. Describe the function of Urotensin?
    • Vasoconstriction
    • May be invovled in HTN, heart and/or renal failure, DM
  22. What is the rate limiting step in the synthesis of 5-HT?
    Tryptophan Hydroxylase
  23. What is the major catabolism enzyme of 5-HT? Final product?
    MAO to 5-hydroxyindeleacetic acid (5-HIAA)
  24. What is the function of L-Trypthophan? How is it used as a natural supplement? Associated S/E?
    • Function: Used to make melatonin in pineal gland
    • Natural Supplement: Sleep aid and antidepressent
    • S/E: Blood dyscrasias and muscle wasting
  25. Describe physiological effects of 5-HT in neurons, GI smM, platelets and vasculature?
    • Neurons: Regulate sleep, appetite, mood, temperature, pain
    • GI smM: Gi motility (5-HT-2R)
    • Platelets: Increase platelet aggregation (5-HT-2R)
    • Vasculature: Vasoconstriction (5-HT-2R) and vasodilation (endothelial cell mediated)
  26. Describe carcinoid syndrome and its effect on 5-HT production?
    • It's a tumor of the enterochrommafin cells in the GI tract
    • Produces large amounts of 5-HT
  27. Briefly describe the 5 5-HT receptors that we know of?
    • 5-HT-1A: Gi coupled, lowers cAMP
    • 5-HT-1D/B: Gi coupled, lowers cAMP
    • 5-HT-2A: Gq coupled, increases IP3/DAG
    • 5-HT-3: Works via Na/K channels
    • 5-HT-4: Gs coupled, increases cAMP
  28. Describe: Buspirone
    • Agonist at 5-HT-1A
    • Function: Anxiety
  29. Describe: Sumatriptan
    • Agonist at 5-HT-1D/B
    • Function: Migranes
  30. Describe: LSD
    • Agonist at 5-HT-2A
    • Function: Happiness
  31. Describe: Cisapride
    Agonsit at 5-HT-4
  32. Describe: Clozapine, methylsergide, cyproheptadine
    • Antagonists at 5-HT-2
    • Oppose LSD Action
  33. Describe: Ondansetron
    Antagonist of 5-HT-3
  34. What are the 4 major pharmacological drug actions pertaining to 5-HT?
    • Receptor antagonism
    • Synthesis inhibition
    • Reuptake blocking
    • MAO inhibitors
  35. What is seen in Ergotism?
    Dementia, hallucinations, vasospasms (pain, gangrene), and uterine stimulation
  36. What are the effects of ergots in CNS, vascular tissue and uterine smM?
    • CNS: Hallucination, dopamine receptors to slow prolactin release
    • Vascular: Prolonged vasoconstriction - partial agonists at both alpha and 5-HT receptors. Can produce epinephrine reversal
    • Uterine smM: Large contraction, especially in pregnant uterus
  37. Describe: Ergotamine, dihydroergotamine, metylsergide
    Used for migranes
  38. Describe: Bromocriptine, cabergoline
    Used for hyperprolactinemia
  39. Describe: Ergovine
    • Cautious use for postpartum hemorrhage
    • NEVER use before delivery

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