pharmacology midterm

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pharmacology midterm
2011-10-24 14:02:24

pharmacology midterm
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  1. -afil
    • erectile dysfunction
    • e.g. sildenafil
  2. Acetylcholine:
    nAchR agonist, mAchR agonist

    choline ester: major hydrolysis by AchE

    initiates local depolarization at synaptic region via ligand-gated ion channels
  3. botulinum toxin
    taken up into synaptic terminal

    blocks release of Ach via proteases
  4. dantrolene
    blocks Ca release from SR

    used to counteract malignant hyperthermia caused by succinylcholine excess
  5. decamethonium
    partial agonist of nAchR

    i.e. depolarizing blocker

    first activates, then desensitizes
  6. donepezil
  7. echothiophate
  8. edrophonium
    AchE inhibitor

    non-covalent, rapidly reversible

    half-life: ~few minutes (i.e. short acting)

    used as diagnostic for myasthenia gravis
  9. hemicholinium-3
    blocks choline uptake

    depletes Ach
  10. isoflurophate (di-isoflurophate, DFP)
    organic phosphate --> AchE inhibitor

    covalent, irreversible binding
  11. mivacurium
    competitive antagonist of AchR

    metabolized by pChE

    ~15 min duration
  12. neostigmine
    AchE inhibitor

    carbamate ester

    covalent, reversible

    half-life ~0.5 -- couple hours

    used to counteract d-turbocararine and other nAchR antagonists
  13. physostigmine
    AchE inhibitor

    carbamate ester

    covalent, reversible binding

    half-life ~0.5 -- couple hours

    used to counteract nAchR antagonists
  14. pralidoxime (2-PAM)
    normally reactivates AchE that has been phosphorylated

    cannot reactivate "aged" phosphorylated AchE
  15. succinylcholine
    partial agonist of AchR

    i.e. depolarizing blocker

    first activates, then desensitizes

    hydrolyzed by pChE

    can lead to malignant hyperthermia in predisposed: treat with dantrolene
  16. d-turbocurarine
    competitive antagonist of AchR

    ~40 min duration
  17. hexamethonium (C6)
    nAchR inhibitor
  18. trimethaphan
    nAchR inhibitor
  19. nicotine
    nAchR agonist
  20. DMPP (1,1-dimethyl-4-phenylpiperazinium)
    nAchR agonist
  21. bethanechol
    major mAchR agonist in GI, urinary; NO nAchR activity

    choline ester: NOT hydrolyzed by ChE

    used as GI stimulant
  22. carbamylcholine (carbachol)
    major nAchR agonist, major mAchR agonist in GI, urinary (not CV)

    choline ester: NOT hydrolyzed by ChE

  23. methacholine
    mostly mAchR agonist, slight nAchR agonist

    choline ester: slight hydrolysis by AchE

    used as diagnostic for airway hyperreactivity
  24. muscarine
    mAchR agonist (alkaloid)

  25. pilocarpine
    mAchR agonist (alkaloid)


    • used to treat:
    • glaucoma
    • dry mouth
  26. atropine
    mAchR inhibitor (tertiary)

    • biphasic dose response:
    • low dose: increases PNS flow from CNS
    • low dose: acts preferentially on presynaptic mAchR, causes more release of Ach onto heart mAchR, which causes decresed heart rate

    high dose: blocks mAchR on terminal and heart, causes increased heart rate

    • uses:
    • block vasodilation, but little effect on BP alone
  27. cevimeline
    selective M3 mAchR agonist

    • uses:
    • xerostomia
    • Sjorgren's syndrome

    fewer side effects than pilocarpine
  28. ipratropium
    mAchR inhibitor (quaternary)

    not lipid soluble (vs. atropine), poorly absorbed into general circulation

    • uses:
    • inhaled for bronchodilation without inhibiting ciliary clearance of mucous
    • asthma, COPD
    • sometimes combined with beta2-agonists
  29. McN-A-343
    selectively activates mAchR (M1) in SNS ganglia

    • uses:
    • increases BP by stimulating SNS modulatory pathway
  30. methylatropine (N-methylatropine)
    mAchR inhibitor (quaternary)
  31. pirenzepine
    selectively blocks mAchR (M1) in SNS ganglia
  32. scopalamine
    mAchR inhibitor (tertiary)
  33. tiotropium
    selective M3 mAchR inhibitor (quaternary)

    • uses:
    • inhaled bronchodilator
    • COPD
  34. imipromide
    selective H2 receptor agonist

    • uses:
    • diagnostic for Zollinger-Elson syndrome
  35. ethanolamines
    1st generation H1 receptor inhibitors


    • common:
    • dimenhydrinate (dramamine)
    • diphenhydramine (benedryl)

    major sedation
  36. piperazines
    1st generation H1 receptor inhibitor

    common: hyroxyzine (highly sedative)

    non-OTC: potential for abuse

    • uses:
    • motion sickness
    • anxiety
  37. ethylenediamines
    highly selective H1 antagonism

    common GI side effects, moderate sedation

    moderate sedation
  38. alkylamines
    H1 antagonists

    pheniramine derivatives

    • common:
    • brompheniramine (dimetapp)

    OTC: allergy, common cold, rhinitis

    slight sedation
  39. phenothiazines
    H1 antagonist

    common: promethazine (phenergan)

    strong sedation

    • non-OTC:
    • pre-operative anesthetic
    • alpha-adrenergic blockade
    • used for severe motion sickness
  40. cyproheptadine (periactin)
    1st generation piperidine

    • uses:
    • anti-serotonin effect
    • used for adolescent migraine
    • used for Cushing's syndrome

    lead compound for 2nd generation H1 antagonists
  41. 2nd generation H1 antagonists
    • common:
    • loratadine (claritin)
    • fexofenadine (allegra)
    • zyrtec

    • drugs of choice for allergy
    • highly selective for H1 receptor
    • non-sedating

    • complications:
    • lethal ventricular arrhythmias
  42. H2 receptor antagonists
    used to reduce gastric acid secretions

    • common:
    • ranitidine (zantac)
    • famotidine (pepcid)
  43. H3 receptor antagonists
    stimulant, nootropic effects

    treat neurodegeneration, obesity, sleep disorders, etc.
  44. H4 receptor antagonists
    none currently used clinically
  45. PPI
    current drugs of choice for GA disorder

    • common:
    • omeprazole (prilosec)
    • pantoprazole (protium)
  46. Mucosal protective agents
    • common:
    • sucralfate
    • prostaglandin analogs
    • bismuth compunds
  47. albuterol
    B2-adrenergic agonist
  48. ampthetamine
    indirect sympathomimetic
  49. dobutamine
    B1-adrenergic agonist

    • increases contractile force of heart
    • little effect on HR and TPR
  50. dopamine
  51. ephedrine
    mixed-acting sympathomimetic
  52. epinephrine
    more potent at B2 than a1

    uses: treat anaphylatic shock, cardiac stimulation, relaxation of GI/bronchi
  53. fenoldopam
    dopaine D1 receptor agonist

    emergency managment of HTN
  54. isoproterenol
    stimulates B1 and B2 adrengergic receptors
  55. norepinephrine
    strongly stimulate B-adr and a1-adr
  56. phenylphrine
    stimulates a1-adr
  57. ritodrine
    B2-adrenergic agonist
  58. salmeterol
    B2-adrenergic agonist
  59. terbutaline
    B2-adrenergic agonist
  60. tyramine
    indirect sympathomimetic
  61. atenolol
    selective B1 beta-blocker
  62. butoxamine
    selective B2 beta-blocker
  63. carvedilol
    non-selective beta-blocker AND a1-blocker
  64. esmolol
    selective B1 beta-blocker
  65. labetolol
    non-selective beta-blocker AND a1-blocker
  66. metoprolol
    selective B1 beta-blocker
  67. nadolol
    non-selective B-adrenergic inhibitor
  68. phenoxybenzamine
    covalent, nonselective alpha-adrenergic inhibitor
  69. phentolamine
    noncovalent, non-selective alpha-adrenergic inhibitor
  70. prazosin
    selective a1 alpha-adrenergic inhibitor
  71. propranolol
    non-selective B-adrenergic inhibitor
  72. timolol
    non-selective B-adrenergic inhibitor
  73. yohimbine
    selective a2 alpha-adrenergic inhibitor
  74. 6-hydroxydopamine
  75. bretylium
  76. cocaine
  77. clonidine
  78. guanadrel
  79. guanethidine
  80. imipramine
  81. methyldopa
  82. methyltyrosine
  83. pargyline
  84. reserpine