HISTAMINE PHARMACOLOGY - RX WRITING AND DRUG COSTS (DR. TERLECKY, DR. WAKADE, DR. TODI, DR. WU AND D

  1. What is histamine?
    hydrophilic molecule formed by the decarboxylation of L-histidine
  2. Which of the following is required for histamine synthesis:





    D. pyridoxal phosphate
  3. All of the following are true of histamine degradation except:






    d. all of the above are true
    E. all of the above are true
  4. All of the following are true of the causes of histamine release except:





    D. sodium and ATP are modulators (calcium and ATP are modulators)
  5. All of the following are true of the modulation of histamine release except:





    C. compound 48/80 and penicillin act as ionophores and result in clacium influx and release of histamine (compound 48/80 and polymixin B act as ionophores and result in clacium influx and release of histamine)
  6. All of the following are true of the effects of histamine as mediated by its receptors except:






    C. increases heart rate and blood pressure via H2 receptors (histamine increases heart rate via H2 receptors and decreases blood pressure via H1 receptors)
  7. Which of the following are true of drugs that block histamine actions:







    A. epinephrine is a physiological histamine blocker
  8. Match the following.

    1. first generation antihistamines
    2. second generation antihistamines

    a. Zyrtec
    b. Clarinex
    c. Dramamine
    d. Allegra
    e. Benadryl
    f. Chlor-Trimethon
    g. Claritin
    • 1. first generation antihistamines - c. Dramamine, e. Benadryl, f. Chlor-Trimethon
    • 2. second generation antihistamines - a. Zyrtec, b. Clarinex, d. Allegra, g. Claritin
  9. All of the following are ways to treat ulcerative and inflammatory GI diseases except:





    B. administer a proton pump stimulator
  10. All of the following are true of antacids except:





    E. all of the above are true
  11. Which of the following are true of gastric secretion reduction:




    B. cholinergic receptor antagonist can be used to depress smooth muscle motility and parasympathetic mediated release of HCL
  12. All of the following are true of the enhancement of mucosal defenses except:




    B. prostaglandins increase gastric acid secretion by stimulating histamine-stimulated cAMP production (prostaglandins prevent gastric acid secretion by blocking histamine-stimulated cAMP production)
  13. Reglan exhibits _____ activity and _____ the motility of the upper GI tract without increasing gastric, biliary, or pancreatic secretions.
    muscarinic; stimulate
  14. What condition is associated with chronic use of too much Reglan (metoclopramide)?
    tardive dyskinesia
  15. What antibitoics are most commonly used to eradicate Helicobacter pylori colonization?
    • Amoxil (amoxicillin)
    • Biaxin (clarithromycin)
  16. What are the 3 basic steps involved in emesis that are controlled by the emetic center in the medulla?
    • excitation of sensors: psychic vomiting, anticipatory vomiting, motion sickness, gagging, thoracic pain and irritation of stomach (intestinal lining) and peritoneum
    • stimulation of vomiting center: received from chemoreceptor trigger zone that are composed of dopamine receptors
    • effector response: increase in pulse rate, salivation, dilation of pupils and pallor, contraction of pylorus and relaxation of gastric smooth muscle, tensing of abdominal and intercostal muscles (increase in abdominal pressure), reverse peristalsis ->> after effects: slowing of heart, drop in blood pressure, faintness and pallor
  17. All of the following are emetic agents except:




    B. Zofran (ondansteron) (antiemetic)
  18. All of the following are true of antiemetic agents except:




    D. Zofran is a neurokinin receptor antagonist (Zofran is a 5-HT3 antagonist)
  19. All of the following are true of laxatives except:




    C. castor oil, senna, and Exlax are osmotic laxatives (these are irritant/stimulant laxatives)
  20. What are the 6 most common therapeutic uses of laxatives?
    • treatment of constipation
    • poisoning
    • antihelmenthics
    • evacuation for radiological or proctological exam
    • bowel surgery
    • anorectal diseases to prevent straining
  21. All of the following are true of anti-diarrhea agents except:




    C. Lomotril is an absorbent powder that absorbs water and toxins as well as provides a protective coating to the inflammed intestine (Lomotril is a motility agent that interferes with peristaltic contractions)
  22. What is the rate-limiting step in the entire biosynthetic pathway of catecholamines?
    tyrosine hydroxylase
  23. True or false. phenylethanolamine-N-methyl-transferase (PNMT) is present mainly in the adrenal gland.
    true
  24. All of the following are true of voltage sensitive calcium channels except:




    C. N-type calcium channels are located in neurons and their pharmacological antagonists are omega-conatoxin GVIA and dilthiazam (pharmacological antagonists are omega-conatoxin GVIA and Cadmium)
  25. All of the following are true of the locations of alpha-1-adrenergic receptors except:





    B. blood platelets (location of alpha-2-receptors)
  26. All of the following are true of the locations of alpha-2-adrenergic receptors except:




    C. blood vessels (location of alpha-1-receptors)
  27. All of the following are true of alpha agonists except:




    A. methoxamine is more potent than phenylephrine
  28. Which of the following is true of beta-adrenergic receptors:





    E. more than one of the above (b and d)
  29. All of the following is true of adrenergic response on the heart except:





    E. the rate of decrease of the "potassium leak" from the SA node pacemaker cells during diastolic interval is slowed down leading to shortened time for depolarization to threshold (...diastolic interval is accelerated...)
  30. Which of the following is true of adrenergic response on the heart:





    E. velocity of impulse transfer from SA node and AV nodes is increased and refractory period of AV node is decreased
  31. All of the following are true of adrenergic receptors and their affect on vascular beds except:





    D. kidney is predominately mediated by alpha-2 receptors and activation leads to vasoconstriction in response to epinephrine and norepinephrine and slight vasodilation with ISO (predominately alpha-1-receptors, remember we're talking about the vascular beds in the kidney!)
  32. Which of the following is true of adrenergic receptors and their affect on vascular beds:





    B. alpha cells of the pancreas contain beta-receptors that when stimulated, secrete glucagon
  33. All of the following are true of the cardiovascular system and adrenergic stimulation except:




    B. NE and low[EPI] produces an increase in both systolic and diastolic pressure, an increase in BP, an increase in CO and an increase in TPR (...a decrease in CO...)
  34. All of the following are true of smooth muscles and adrenergic stimulation except:





    • A. bronchial smooth muscle contain beta-2-receptors that when stimulated cause bronchoconstriction (...bronchodilation)
  35. Which of the following is true of smooth muscles and adrenergic stimulation:





    A. spleen smooth muscle contain alpha-1-receptors that result in contraction and blood expulsion when stimulated
  36. True or false. When EPI is given systemically, it may cause some respiratory stimulatin, restlessness and anxiety.
    true
  37. Indirect-acting adrenergic drugs include _____, _____ and _____, all of which are _____.
    ; tyramine; amphetamine; ephedrine; phenylethylamines
  38. Why are tyramine, amphetamine and ephedrine called indirect-acting adrenergic drugs?
    they do not directly stimulate adrenergic receptors but cause release of NE from sympathetic neurons that then act on alpha or beta-receptors
  39. What are the responses of tyramine injection and what are its possible drug-drug interaction?
    • increase in BP and heart rate
    • MAO inhibitors (effects of tyramine are potentiated because MAO oxidizes tyramine into its inactive form)
  40. All of the following are true of amphetamine and ephedrine except:





    E. all of the above are true
  41. True or false. Ephedrine is used in the US therapeutically for the management of bronchial asthma.
    False, ephedrine is not used in the US, but pseudoephedrine is used therapeutically for the management of bronchial asthma.
  42. All of the following are true of the antihypertensive agent, Serpasil (reserpine), except:





    E. all of the above are true
  43. All of the following are true of the antihypertensive agent, Ismalin (guanethidine), except:




    A. mechanism of action is blockage of exocytosis via interference with calcium entry (does not interfere with with calcium entry, but somehow exocytosis is blocked!)
  44. How does Catapress (clonidine) lower BP and what are some possible side effects?
    activation of alpha-2-receptors of CNS and reducing sympathetic outflow to blood vessels; dizzness, nausea, impotence and dry mouth
  45. True or false. Sudden withdrawal from clonidine after long-term  use can result in hypertensive crisis caused by over activity of sympathetic nervous system.
    true
  46. What are the symptoms of hypertensive crisis?
    • nervousness
    • headache
    • tachycardia
    • hypertension
    • sweating
  47. The effect of alpha-Me-NE is to _____ sympathetic nerve impulse activity originating in the _____ of the medulla by activation of _____ receptors.
    reduce; nucleus tractus solitarus; alpha-2
  48. All of the following are true of tricyclic antidepressants except:




    A. amitryptyline is the most potent inhibitor of NET (desipramine is the most potent inhibitor of NET)
  49. All of the following are true of cocaine abuse and its affect on adrenergic response except:




    B. irreversibly binds to NET and blocks uptake of NE and EPI in CNS (reversibly binds to NET and blocks uptake of NE and EPI in CNS)
  50. All of the following are true of amphetamine and its affect on adrenergic response except:






    F. all of the above are true
  51. What 3 drugs should be given in the event of an anaphylactic shock (cardiovascular emergency)?
    • EPI
    • NE
    • PE
  52. What drug should be given in the event of a circulatory shock (cardiovascular emergency)?
    NE
  53. Match the following.

    Local anesthetics for:

    1. urticaria
    2. nasal decongestant
    3. mydriatic agent
    4. CNS stimulant

    a. amphetamine (oral)
    b. PE
    c. naphazoline
    d. methamphetamine
    e. EPI (parenteral)
    f. ephedrine (topical)
    • 1. urticaria - e. EPI (parenteral)
    • 2. nasal decongestant - b. PE, c. naphazoline
    • 3. mydriatic agent - b. PE, f. ephedrine (topical)
    • 4. CNS stimulant - a. amphetamine (oral), d. methamphetamine
  54. Dobutamine is an _____ _____ and comes as a racemic mixture of (L) and (D) isomers. The _____ isomer acts on both receptors as an alpha-agonist and weak beta-1-agonist. The _____ isomer acts as an alpha-1-antagonist and a potent beta-1-agonist. Dobutamine is commonly used in the acute management of _____ _____ to improve _____ _____.
    adrenergic agonist; L; D; heart failure; cardiac output
  55. All of the following are true of alpha adrenergic blocking agents except:




    C. prazosin is a selective antagonist of alpha-1 and alpha-2 receptors and is used to treat hypertension, lowers preload and increases afterload, and treats congestive heart failure (prazosin is a selective antagonist for alpha-1-receptors only!)
  56. All of the following are true of propanolol except:





    E. more than one of the above (a and d; propanolol is a selective competitive beta-receptor antagonist and causes an increase in peripheral resistance)
  57. All of the following are true of beta-blockers except:





    E. more than one of the above (b and c;  decrease peripheral manifestations of hyperthyroidism and intraocular pressure)
  58. What are some important situations to consider before prescribing a beta-blocker?
    • should not be used in asthmatic patients
    • can worsen congestive heart failure, Raynaud's syndrome and diabetes
    • should never be used concomitantlywith calcium channel blockers ->> can result in AV block
    • withdraw gradually to avoid withdrawal symptoms and myocardial infarction
  59. True or false. Selectivity of beta-blockers decreases with higher concentrations.
    true
  60. What is Bystolic and what are its effects?
    more specific blocker for beta-1 receptors than beta-2 receptors; reduces force of contraction and heart rate, vasodilation and reduction in peripheral resistance.
  61. What drug is most commonly known for blocking both alpha AND beta receptors?
    labetalol
  62. All of the following are true of glucocorticoids except:





    E. all of the above are true
  63. All of the following are true of glucocorticoid actions except:







    G. more than one of the above (a and e; inhibit production of IL-1, IL-2, IL-4, and TNF-alpha and inhibit phospholipase A2 and COX-2)
  64. All of the following are true of immunophilins except:





    D. primarily act on cytotoxic T-cells and inhibit cytokine release (act on helper T-cells)
  65. All of the following are true of calcineurin inhibitors except:





    B. NSAIDS and acyclovir decrease cyclosporin and tacrolimus levels (NSAID and acyclovir potentiate the nephrotoxic effects of cyclosporin and tacrolimus, while agents like phenytoin, phenobarbital and rifampin decrease cyclosporin and tacrolimus levels)
  66. All of the following are possible side effects of calcineurin-inhibiting agents except:






    B. hypotension (hypertension)
  67. Which of the following is true of sirolimus:






    F. more than one of the above (b, c and d)
  68. All of the following are true of azathioprine except:





    D. it is an alkylating agent that decreases B and T lymphocyte numbers, and decreases immunoglobulin and IL-2 production (azathioprine is an anti-metabolite agent)
  69. All of the following are true of methotrexate except:






    B. it is a structural analog of folic acid that can competitively and reversibly bind to DHFR that reduces dihydrofolic acidto its active form (...irreversibly binds to DHFR...)
  70. True or false. Methotrexate toxicity can be severe and even fatal.
    true
  71. All of the following are true of mycophenolate mofetil except:





    D. decreased production of IL-1 and IL-2 (no effect on IL-1 and IL-2)
  72. True or false. Leflunomide is a prodrug inhibitor of purine synthesis.
    False, leflunomide is a prodrug inhibitor of pyrimidine synthesis.
  73. Which of the following is true of cyclophosphamide:






    A. it is an alkylating agent used in the treatment of severe, life threatening autoimmune and inflammatory diseases
  74. Antithymocyte globulin is used largely to _____ immunosuppression and its side effects are _____, _____, _____, and _____.
    induce; infection; fever; headache; lymphoma
  75. Muromonab-CD3 _____, _____, and _____ T-cells. Its side effects are _____, _____, and _____.
    inactivates; depletes; destroys; fever; headache; hypertension
  76. Humira (adalimumab), Remicade (infliximab) and Enbrel (entanercept) are all examples of what types of agents?
    anti-TNF-alpha agents
  77. What are the 2 anti-cytokine monoclonal antibodies that we discussed in class?
    • Zenapax(daclizumab)
    • Simulect (basiliximab)
  78. All of the following are true of the COX enzymes except:





    B. COX-1 is inducible and is found mostly in the stomach and platelets (COX-1 is constitutive)
  79. All of the following are true of COX products and their affect on the kidney except:






    C. PGE2 and PGI2 are vasoconstrictors and decrease GFR (PGE2 and PGI2 are vasodilators and increase GFR)
  80. All of the following are true of COX products and their affect on blood vessels except:





    D. IV injection of PGI2 can cause hypertension and reflex tachycardia (IV injection of PGI2 can cause hypotension and reflex tachycardia)
  81. All of the following are true of COX products and their affect on the GI tract except:





    A. PGF2 and PGD2  are synthesized by COX1 in the stomach where they are cytoprotective by maintaining the (PGE2 and PGI2  are synthesized by COX1 in the stomach where they are cytoprotective by maintaining the secretion of mucins and limiting pepsin and acid secretion)
  82. All of the following are true of COX products and their affect on platelets except:





    B. TXA2 is a vasodilator and potent platelet aggregator (TXA2 is a vasoconstrictor and potent platelet aggregator)
  83. Which of the following is true of COX products and their affect on the lung:




    C. none of the above (TXA2 constricts bronchiolar and tracheal muscleb; PGI2 and PGE2 relax bronchiolar and tracheal muscle)
  84. Which of the following is true of COX products and their affect on the nervous system:





    E. more than one of the above (b and c are true)
  85. True or false. TXA2, PGF2-alpha, and low doses of PGE2 cause uterine contraction.
    true
  86. Which of the following is true of COX products and their affect on inflammation:





    A. PGE2 inhibit differentiation of B-lymphocytes into plasma cells
  87. What is the most likely explanation for the anti-inflammatory effect of COX-inhibitors?
    diminished eicosanoid effects on vasodilation and sensitization of nociceptive nerves
  88. All of the following are descriptive of prostaglandins that are used as pharmacological agents except:




    D.  alprostadil is a PGF2 that is used for its vasodilating effect of impotence and maintenance of the patent ductus arteriosus prior to cardiac surgery (it is a PGE1)
  89. All of the following are true of LOX enzymes except:




    D. PMNs, basophils, mast cells,eosinophils and macrophages contain the 12-LOX isoform (PMNs, basophils, mast cells,eosinophils and macrophages contain the 5-LOX isoform)
  90. Which of the following is true of LOX enzymes:






    F. all of the above
  91. Which of the following is true of LOX products and their affect on airways:

    a. LTC4 and LTD4 are secreted in anaphylaxis asthma and are powerful broncoconstrictors
    b. LTC4 and LTD4 increase permeability of microvessels leading to mucus secretion and plasma exudation
    c. none of the above
    e. all of the above
    e. all of the above
  92. True or false. LTC4 is secreted by colonic epithelial cells and levels of this leukotriene are high in inflammatory bowel disease.
    False, LTB4 is secreted by colonic epithelial cells and levels of this leukotriene are high in inflammatory bowel disease.
  93. _____ and _____ are leukotrienes that depress myocardium and coronary blood flow.
    LTC4; LTD4
  94. Inhibitors of _____ and _____ antagonists are effective in asthma but are not useful in generalized inflammation like rheumatoid arthritis.
    5-LOX; LT-receptor
  95. True or false. Aspirin inhibits COX1 and COX2, but has a higher affinity for COX2.
    False, aspirin inhibits COX1 and COX2, but has a higher affinity for COX1.
  96. All of the following are true of aspirin and its pharmacological effects except:





    E. more than one of the above (b and d; blocks pyrogen induced prostaglandin synthesis in the hypothalamus and only lowers febrile body temperature not basal body temperature, aspirin irreversibly inhibits platelet COX1 without affecting endothelial COX2)
  97. All of the following are true of aspirin and its possible side effects except:





    B. gastric irritation, bleeding and peptic ulcers are due to inhibition of gastric COX2 (...gastric COX1)
  98. All of the following are true of acetaminophen except:





    B. causes gastric irritation
  99. All of the following are true of ibuprofen and naproxen except:






    F. all of the above are true
  100. Which of the following is true of indomethacin:





    E. more than one of the above (b and d)
  101. Which of the following is true of Celebrax (celecoxib):





    D. linked to high incidence of myocardial infarction and sudden cardiac death
  102. All of the following are true of misoprostol except:




    B. can prevent gastric ulcers when used concurrently with a selective COX inhibitor (...non-selective COX inhibitors, like NSAIDS)
  103. All of the following are true of methotrexate except:





    E. it stimulates dihydrofolate reductase (DHFR) (...inhibits DHFR)
  104. All of the following are true of hydroxychloroquine except:





    D. should be avoided in pregnancy (safe to use in pregnancy)
  105. Which of the following is true of sulfasalazine:





    E. more than one of the above (c and d)
  106. All of the following are true of leflunomide except:





    C. stimulates p450 enzyme in liver (inhibits CYP2C9)
  107. Azathioprine is an inhibitor of several steps in _____ _____ that inhibit _____ synthesis.
    purine interconversions; DNA
  108. True or false. Azathioprine and methotrexate have similar effects.
    true
  109. Match the following.

    1. Enbrel (etanercept)
    2. Remicade (imfliximab)
    3. Humira (adalimumab)

    a. human antibody
    b. administered subQ
    c. human TNF receptor and Fc fragment of IgG
    d. produces effects similar to that of methotrexate
    e. chimeric human-mouse monoclonal anti-TNF
    f. administered IV
    • 1. Enbrel (etanercept) - b. administered subQ, c. human TNF receptor and Fc fragment of IgG, d. produces effects similar to that of methotrexate
    • 2. Remicade (imfliximab) - e. chimeric human-mouse monoclonal anti-TNF, f. administered IV
    • 3. Humira (adalimumab) - a. human antibody, b. administered subQ
  110. All of the following are true of Orencia (abatacept) except:





    D. principle untoward effect is renal failure (principle untoward effect is infection)
  111. All of the following are true of Rituxan (rituximab) except:





    A. it is a chimeric monoclonal antibody that targets T-cell antigen CD28 (...targets B-cell antigen CD20)
  112. All of the following are true of colchicine except:






    B. can be used for acute and chronic gout attacks (only used for acute gout attacks)
  113. All of the following are true of allopurinol except:





    E. none of the above (all of the above are true)
  114. All of the following are true of probenicid except:





    B. used to treat acute gout (used to treat chronic gout)
  115. All of the following are true of glucocorticoids except:






    F. once bound to its receptor a signaling cascade is initiated and tyrosine kinases are activated (once bound to its receptor, the activated receptor enters the nucleus and binds to GREs which leads to activation or inhibition of mRNA transcription)
  116. All of the following are drugs that are currently used to treat bronchial asthma and COPD except:







    C. ephedrine (not used anymore because of its undesirable cardiac stimulation and CNS effects (tremors))
  117. Match the following.

    1. bronchodilators
    2. non-selective beta-2-agonists
    3. selective beta-2-agonists
    4. anticholinergic agents
    5. anti-inflammatory agents
    6. prostaglandins
    7. leukotriene synthesis inhibitors
    8. leukotriene receptor blocker
    9. IgE antibody
    10. corticosteroid
    11. xanthine

    a. cromolyn sodium
    b. PGE1 and PGE2
    c. epinephrine
    d. prednisone
    e. Genentech (omalizumab)
    f. fluticasone
    g. theophylline
    h. Albuterol
    i. ephedrine
    j. Spiriva (tiotropium)
    k. Atrovent (ipratropium bromide)
    l. Advair
    m. zileuton
    n. Accolate (zafirleukast)
    • 1. bronchodilators - c. epinephrine, i. ephedrine
    • 2. non-selective beta-2-agonists - c. epinephrine, i. ephedrine
    • 3. selective beta-2-agonists - h. Albuterol
    • 4. anticholinergic agents - j. Spiriva (tiotropium), k. Atrovent (ipratropium bromide)
    • 5. anti-inflammatory agents - a. cromolyn sodium, d. prednisone, f. fluticasone, l. Advair
    • 6. prostaglandins - b. PGE1 and PGE2
    • 7. leukotriene synthesis inhibitors - m. zileuton
    • 8. leukotriene receptor blocker - n. Accolate (zafirleukast)
    • 9. IgE antibody - e. Genentech (omalizumab)
    • 10. corticosteroid - d. prednisone, f. fluticasone, l. Advair
    • 11. xanthine - g. theophylline
  118. _____ and _____ are two new therapeutic treatments for asthma and COPD that are still under development.
    IL-5 antibody; bacterial DNA induces TH1 response
  119. All of the following are true of selective beta-2-agonists used to treat asthma and COPD except:




    B. long-acting salmeterol and formoterol can be used as monotherapy (should be used in combination with an inhalation corticosteroid like fluticasone)
  120. All of the following are true of anticholinergic agents used to treat asthma and COPD except:





    A. Atrovent (ipratropium bromide) is used as a long-acting broncodilator for patients with chronic bronchitis and COPD (Atrovent is short-acting)
  121. All of the following are true of anticholinergic agents used to treat asthma and COPD except:






    A. possible side effects include seizures, arrhythmia, hypertension and cardiac arrest (possible side effects include seizures, arrhythmia, hypotension and cardiac arrest)
  122. All of the following are true of corticosteroids except:





    B. inhaled corticosteroids have a direct and immediate effect on airflow obstruction, similar to that of inhaled bronchodilators
  123. All of the following are true of corticosteroids except:





    E.  acts as a sodium channel blocker and is used exclusively for the prophylatic treatment of mild to moderate asthma (acts as a calcium channel blocker and is used exclusively for the prophylatic treatment of mild to moderate asthma)
  124. Singulair (montelukast) is most commonly used in the treatment of _____ _____ _____.
    seasonal allergic rhinitis
  125. _____ is a humanized monoclonal antibody given subQ that binds to IgE and is used in the treatment of moderate to severe asthma.
    Genentech (omalizumab)
  126. True or false. Oral administration is superior to IV administration if a patient has a functioning gut.
    true
  127. What are the 4 basic prescription laws?
    • max of 4 medications per Rx
    • no refills on C-IIs
    • up to 5 refills in 6 months for C-IIIs to C-Vs
    • DEA # is needed for all controlled substances
  128. What should always be included on a Rx?
    • Date/time
    • your name/pager #
    • height/weight of patient
    • allergies of patient
Author
davis.tiff
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176486
Card Set
HISTAMINE PHARMACOLOGY - RX WRITING AND DRUG COSTS (DR. TERLECKY, DR. WAKADE, DR. TODI, DR. WU AND D
Description
PHARM EXAM I
Updated