NSAIDs Notes PharmChem Sem VIiI

Follow the link
https://drive.google.com/file/d/1KGlx2HQ3T8dDm-Xs1LVhu_mklQL54w_g/view?usp=drivesdk

https://www.ispatula.com/file/n07-medicinal-chemistry-3-anti-inflammatory-notes-nsaid-steroids-pdf/

Topic:1 NSAIDS Test

Solve the following 

• 1.
  Match the description with the stage of inflammation: Acute transient phase, delayed subacute phase, and chronic proliferative phase.A. Infiltration of leukocytes and phagocytic cells to the site of inflammation; immunologicalB. tissue degradation and fibrocis; immunologicalC. local vasodilation of small vessels and increased capillary permeability; mediated by autacoids; characterized by redness (erythema), swelling (edema), and tenderness (hyperalgesia)
  • A. 
    Acute = A, Delayed = B, Chronic = C
  • B. 
    Acute = C, Delayed = A, Chronic = B
  • C. 
    Acute = B, Delayed = C, Chronic = A
• 2.
  Which mediators of inflammation are acted on by NSAIDs?
  • A. 
    Eicosanoids (arachidonic acid metabolites) such as prostaglandins, thromboxanes, and leukotrienes.
  • B. 
    Degradative enzymes such as proteases, hyaluronidases
  • C. 
    Vasoactive amines such as histamine and serotonin
  • D. 
    Biologically derived oxidants such as hydrogen peroxide and superoxide anion
  • E. 
    Plasma proteins and peptides such products of the complement and kinin
• 3.
  What are some mediators of pain?
  • A. 
    Histamine, 5-HT, bradykinin, LTC4, LTD4, PGE2, C3a, and C5a
  • B. 
    IL-1, IL-6, PGE2, IL-1beta, TNFalpha
  • C. 
    Histamine, 5-HT, PGE2, bradykinins
  • D. 
    Histamine, 5-HT, bradykinin, PGE2, and leukotrienes
• 4.
  What are some mediators for increased permeability (swelling)?
  • A. 
    Histamine, 5-HT, bradykinin, LTC4, LTD4, PGE2, C3a, and C5a
  • B. 
    IL-1, IL-6, PGE2, IL-1beta, TNFalpha
  • C. 
    Histamine, 5-HT, PGE2, bradykinins
  • D. 
    Histamine, 5-HT, bradykinin, PGE2, and leukotrienes
• 5.
  What are some mediators for pyrogens (immunologically)?
  • A. 
    Histamine, 5-HT, bradykinin, LTC4, LTD4, PGE2, C3a, and C5a
  • B. 
    IL-1, IL-6, PGE2, IL-1beta, TNFalpha
  • C. 
    Histamine, 5-HT, PGE2, bradykinins
  • D. 
    Histamine, 5-HT, bradykinin, PGE2, and leukotrienes
• 6.
  What are some mediators for smooth muscle contraction?
  • A. 
    Histamine, 5-HT, bradykinin, LTC4, LTD4, PGE2, C3a, and C5a
  • B. 
    IL-1, IL-6, PGE2, IL-1beta, TNFalpha
  • C. 
    Histamine, 5-HT, PGE2, bradykinins
  • D. 
    Histamine, 5-HT, bradykinin, PGE2, and leukotrienes
• 7.
  What mediator causes elevation of hypothalmic set-point for temperature control?
  • A. 
    Bradykinin
  • B. 
    5-HT
  • C. 
    PGE2
  • D. 
    Histamine
• 8.
  What mediator sensitizes the nerves to pain mediators?
  • A. 
    Bradykinin
  • B. 
    PGE2
  • C. 
    Histamine
  • D. 
    Serotonin
• 9.
  All of the following chemical mediators released at the sit of inflammation cause pain EXCEPT:
  • A. 
    Histamine
  • B. 
    PGE2
  • C. 
    Bradykinin
  • D. 
    Glucocorticoids
• 10.
  Acute transient phase of inflammation is accompanied by tissue degradation and fibrosis.
  • A. 
    True
  • B. 
    False
• 11.
  Which goal of treatment of inflammation is NOT met by NSAIDs?
  • A. 
    Arrest tissue damaging processes that accompany chronic inflammation.
  • B. 
    Relief of symptoms and maintenance of function.
  • C. 
    Both are met by NSAIDs.
• 12.
  What is an example of a pharmacological anti-inflammatory agent?
  • A. 
    Antihistamines
  • B. 
    Immunosuppressants
  • C. 
    Antibiotics
  • D. 
    Analgesics
  • E. 
    All of the above
  • F. 
    A, B, C
• 13.
  NSAIDs can be divided into:
  • A. 
    Non-selective COX inhibitors
  • B. 
    COX-2 selective inhibitors
  • C. 
    CINODs; Nitroaspirins
  • D. 
    All of the above.
• 14.
  Put these drugs in the order they would be given based on the amount of pain felt by the patients - from lowest amount of pain to highest.
  • A. 
    NSAID, morphine, codeine
  • B. 
    Codeine, NSAID, morphine
  • C. 
    NSAID, codeine, morphine
• 15.
  Which COX enzyme are aspirin, indomethacin, and sulindac more selective for?
  • A. 
    COX-1
  • B. 
    COX-2
  • C. 
    They are equally selective for COX-1 and COX-2
• 16.
  Which COX enzyme are piroxicam, ibuprofen, flurbiprofen and mefenamic acid more selective for?
  • A. 
    COX-1
  • B. 
    COX-2
  • C. 
    They are equally selective for COX-1 and COX-2
• 17.
  Which COX enzyme is naproxen and diclofenac more selective for?
  • A. 
    COX-1
  • B. 
    COX-2
  • C. 
    They are equally selective for COX-1 and COX-2.
• 18.
  What is special about CINODs?
  • A. 
    They are COX-2 inhibitors.
  • B. 
    They are COX-1 inhibitors.
  • C. 
    They can release NO.
  • D. 
    They are extremely potent NSAIDs.
• 19.
  What are the anti-inflammatory actions of NSAIDs?
  • A. 
    Decrease in vasodilator prostaglandins (PGE2, PGI2) means less vasodilation and, indirectly, less edema.
  • B. 
    Inhibit the migration of polymorphonuclear leukocytes and macrophages into the site of inflammation.
  • C. 
    Stabilize lysosomal membranes, thereby preventing release of inflammatory mediators.
  • D. 
    All of the above.
• 20.
  What are the analgesic actions of NSAIDs?
  • A. 
    Decreased PG generation means less sensitization of nociceptive nerve endings to inflammatory mediators
  • B. 
    Decreased PG-mediated vasodilation (in headache relief)
  • C. 
    All of the above.
• 21.
  How do NSAIDs cause an anticoagulation effect?
  • A. 
    By binding already formed platelets and preventing aggregation.
  • B. 
    By vasodilating the vessels.
  • C. 
    By inhibiting platelet thromboxane A2 production.
• 22.
  What can be done to prevent the GI side effects of NSAIDs?
  • A. 
    Co-administration of NSAID with PPI.
  • B. 
    Enteric coated tablets.
  • C. 
    Prescribe CINODs instead.
  • D. 
    All of the above.
• 23.
  Why don't you want to give NSAIDs to pregnant women, especially in the third trimester?
  • A. 
    It causes spina bifida in the fetus.
  • B. 
    It causes excess bleeding during delivery.
  • C. 
    It causes prolongation of gestation or delayed spontaneous labor.
• 24.
  The changes in renal failure of congestive heart failure patients, hepatic cirrhosis patients, chornic renal disease patients and hypovolemic patients given NSAIDs include:
  • A. 
    A decrease in renal blood flow and glomerular filtration rate due to unopposed vascoconstriction.
  • B. 
    Promote retention of salt and water by inhibiting PG-induced inhibition of the reabsorption of Cl- and the action of ADH. (may cause drug-induced edema)
  • C. 
    Promote hypokalemia via: increased reabsorption of K+ and suppression of PG-induced secretion of renin.
  • D. 
    All of the above.
• 25.
  Which drugs require a "black box warning"?
  • A. 
    All NSAIDs
  • B. 
    Aspirins
  • C. 
    Coxibs
  • D. 
    NANSAIDs
  • E. 
    B and C
  • F. 
    C and D
• 26.
  Antipyretic effect of NSAIDs is due to the inhibitory effect of NSAIDs on biosynthesis of thromboxane A2.
  • A. 
    True
  • B. 
    False
• 27.
  NSAIDs decrease renal blood flow and glomerular filtration rate in patients with normal kidney function.
  • A. 
    True
  • B. 
    False
• 28.
  NSAIDs are capable of delaying progression of bone and cartilage deformation that is characteristic of chronic inflammatory conditions such as arthritis.
  • A. 
    True
  • B. 
    False
• 29.
  Mr. X has been suffering from congestive heart failure. A few weeks ago, he started experiencing pain in his finger joints. His wife who has a long history of arthritis gave him several doses of the NSAID tablets she has been taking. Mr. X is likely to experience:
  • A. 
    Frequent urination
  • B. 
    Increased retention of fluids
  • C. 
    Hypokalemia
• 30.
  Which NSAID binds irreversibly to COX?
  • A. 
    Ibuprofen
  • B. 
    Aspirin
  • C. 
    Celebrex
• 31.
  A single dose of aspirin can prolong the bleeding time of normal persons for how long?
  • A. 
    5-8 hours
  • B. 
    3-4 weeks
  • C. 
    4-7 days
• 32.
  Salicylates have the following effects on respiration:
  • A. 
    Direct
  • B. 
    Indirect
  • C. 
    Both direct and indirect
• 33.
  Aspirin can be used in the treatment of gout.
  • A. 
    True
  • B. 
    False
• 34.
  Salicylates are contraindicated in pregnancy.
  • A. 
    True
  • B. 
    False
• 35.
  Rate of urinary excretion of salicylates is higher in:
  • A. 
    Alkaline urine
  • B. 
    Acidic urine
• 36.
  At low and high toxic salicylate levels, repiratory alkalosis may occur as a result of increased ventilation and the body is able to compensate.
  • A. 
    True
  • B. 
    False
• 37.
  Drug Interactions: Salicylates can displace all of the following drugs EXCEPT:
  • A. 
    Tolbutamide
  • B. 
    Methotrexate
  • C. 
    Penicillins
  • D. 
    Phenytoin
  • E. 
    Warfarin
  • F. 
    Ibuprofen
• 38.
  What is the first sign/symptom of salicylate intoxication we were told to look for?
  • A. 
    Headache
  • B. 
    Dizziness
  • C. 
    Ringing in the ears
  • D. 
    Hyperventilation
• 39.
  What is the antidote for aspirin overdose?
  • A. 
    Snake venom
  • B. 
    Protamine
  • C. 
    Diclofenac
  • D. 
    There is no antidote
• 40.
  The acetic acid derivatives (indomethacin, sulindac, and etodolac) are more or less potent than aspirin?
  • A. 
    More.
  • B. 
    Less.
• 41.
  Indomethacin can cause CNS disturbances such as depression, psychosis and hallucinations and is therefore contraindicated in psychiatric disorders.
  • A. 
    True
  • B. 
    False
• 42.
  Which acetic acid derivative is used to accelerate the closure of patent ductus arteriosus (hole in the heart)?
  • A. 
    Etodolac
  • B. 
    Indomethacin
  • C. 
    Sulindac
• 43.
  Propionic acid derivatives (ibuprofen, naproxen, ketoprofen, fenoprofen, oxaprozin, and flurbiprofen) are better tolerated by patients than aspirin, phenylbutazone or indomethacin.
  • A. 
    True
  • B. 
    False
• 44.
  Which propionic acid derivative accumulates in synovial fluids and is therefore useful in the treatment of arthritis?
  • A. 
    Ketoprofen
  • B. 
    Naproxen
  • C. 
    Flurbiprofen
  • D. 
    Ibuprofen
• 45.
  Absorption of propionic acid derivatives is retarded by what?
  • A. 
    Concurrent aspirin usage.
  • B. 
    Intake of large amounts of water.
  • C. 
    Food in the stomach.
  • D. 
    An empty stomach.
• 46.
  The oxicams (piroxicam, tenoxicam, and meloxicam) are similar to the salicylates EXCEPT they:
  • A. 
    Do not possess anti-inflammatory actions.
  • B. 
    Do not possess analgesic actions.
  • C. 
    Do not possess antipyretic actions.
  • D. 
    Have less GI side effects.
• 47.
  In addition to inhibition of COX, fenamates (mefenamic acid and meclofenamate) can also:
  • A. 
    Block prostaglandin receptors
  • B. 
    Block histamine receptors
  • C. 
    Block serotonin receptors
• 48.
  Fenamates are used as first-line therapy.
  • A. 
    True
  • B. 
    False
• 49.
  Which NSAID is a prodrug?
  • A. 
    Ibuprofen
  • B. 
    Aspirin
  • C. 
    Acetaminophen
  • D. 
    Nabumetone
  • E. 
    Meclofenamate
• 50.
  Which drug listed below is the only non-acid NSAID?
  • A. 
    Celecoxib
  • B. 
    Ketoprofen
  • C. 
    Nabumetone
  • D. 
    Indomethacin
• 51.
  Aspirin is a reversible inhibitor of both isoforms of COX enzyme.
  • A. 
    True
  • B. 
    False
• 52.
  Cardiotoxic effect of coxibs is partly due to their ability to inhibit the biosynthesis of vascular PGI2.
  • A. 
    True
  • B. 
    False
• 53.
  Coxibs exhibit a potent antiplatelet effect.
  • A. 
    True
  • B. 
    False
• 54.
  Mr. X has had a history of hemophilia all of his life. He was recently diagnosed with gout. As his pharmacist, which of the following NSAIDs would you recommend and why?
  • A. 
    Aspirin
  • B. 
    A CINOD such as NO-naproxen
  • C. 
    A coxib such as celecoxib
• 55.
  Which NSAID does not inhibit neutrophil activation?
  • A. 
    Indomethacin
  • B. 
    Celecoxib
  • C. 
    Acetaminophen
• 56.
  Which NSAID has a toxic intermediate?
  • A. 
    Acetaminophen
  • B. 
    Ibuprofen
  • C. 
    Motrin
  • D. 
    Aspirin
• 57.
  What is the drug of choice for treatment of Acetaminophen toxicity?
  • A. 
    Protamine
  • B. 
    Warfarin
  • C. 
    Mucomyst
• 58.
  What is the preferred NSAID for children?
  • A. 
    Ketoprofen
  • B. 
    Acetaminophen
  • C. 
    Aspirin
• 59.
  Which of the following is NOT an option for the treatment of gout?
  • A. 
    Inhibiting uric acid synthesis
  • B. 
    Increasing uric acid secretion
  • C. 
    Inhibiting leukocyte migration into the joint
  • D. 
    General anti-inflammatory and analgesic effects
  • E. 
    All of the above are ways to treat gout
• 60.
  Which drug used in the treatment of gout acts by decreasing the migration of neutrophiles into the inflammed area?
  • A. 
    Probenecid
  • B. 
    Febuxostat
  • C. 
    Allopurinol
  • D. 
    Colchicine
• 61.
  Which drug used in the treament of gout can cause alopecia in long term use?
  • A. 
    Probenecid
  • B. 
    Allopurinol
  • C. 
    Colchicine
• 62.
  Which drug used in the treatment of gout acts by inhibiting xanthine oxidase?
  • A. 
    Probenecid
  • B. 
    Allopurinol
  • C. 
    Sulfinpyrazone
• 63.
  Neither allopurinol or its metabolite is bound to plasma proteins.
  • A. 
    True
  • B. 
    False
• 64.
  Which drug used in the treatment of gout in the first nonpurine inhibitor of xanthine oxidase?
  • A. 
    Allopurinol
  • B. 
    Febuxostat
  • C. 
    Probenecid
  • D. 
    Sulfinpyrazone
• 65.
  Which drug used in the treatment of gout acts by inhibiting proximal tubular reabsorption of uric acid leading to increased urate excretion?
  • A. 
    Probenacid
  • B. 
    Allopurinol
  • C. 
    Sulfinpyrazone
• 66.
  Probenacid is used for acute gouty attacks.
  • A. 
    True
  • B. 
    False
• 67.
  Which drug used in the treatment of gout is highly bound to plasma proteins?
  • A. 
    Sulfinpyrazone
  • B. 
    Allopurinol
  • C. 
    Probenacid
• 68.
  Match the following descriptors with the drugs they are describing:1. Anti-gout drug that inhibits mitosis.2. Anti-gout drugs that have no effect on uric acid levels in blood.3. Anti-gout drug that is not protein bound.4. A non-purine xanthine oxidase inhibitor.5. Anti-gout drug that causes an increase in uric acid excretion.
  • A. 
    1 = Allopurinol, 2 = Colchicine and Aspirin, 3 = Febuxostat, 4 = NSAIDs and corticosteroids, 5 = uricosuric agents.
  • B. 
    1 = colchicine, 2 = colchicine and NSAIDs and corticosteroids, 3 = allopurinol, 4 = Febuxostat, 5 = Uricosuric agents, and aspirin.