Mdcm - Nsaids

PGG2 and PGH2 are associated with what?  Select all that apply.

• A.

  Vasoconstriction

• B.

  Vasodilation

• C.

  Platelet aggregation

• D.

  Platelet aggregation inhibitor

• E.

  Pain

• F.

  Protects stomach

• G.

  Bronchoconstriction

Aspirin acetylates what enzyme?

• A.

  Thromboxane synthetase

• B.

  Prostacycline synthetase

What is used for the harvest and storage of platelets in renal dialysis and cardiopulmonary bypass?

• A.

  Thromboxanes

• B.

  Prostacyclins

• C.

  Prostaglandins

• D.

  Leukotrienes

Which enzyme is inducible?

• A.

  Cox-1

• B.

  Cox-2

Which of the following is true regarding COX-3?  Select all that apply.

• A.

  Involved in pain

• B.

  Involved in fever

• C.

  Involved in inflammation

• D.

  Inhibited by acetaminophen

• E.

  Inhibited by aspirin

• F.

  Inhibited by DMARDs

PGE2 and PGF2α biosynthesis is greatly increased hours before child birth.

• A.

  True

• B.

  False

How does PGE2 help the stomach?  Select all that apply.

• A.

  Inhibits gastric acid secretion

• B.

  Stimulates secretion of mucous

• C.

  Stimulates secretion of bicarb

This drug is available as a gel or vaginal suppository and is used to increase the frequency and amplitutde of uterine contractions.  Its onset is 10 minutes and a side effect is cramping.

• A.

  Misoprostol

• B.

  Alprostadil (PGE1)

• C.

  Dinoprostone (PGE2)

Which is is involved with platelet aggregation inhibition, vasodilation, and protecting the stomach?

• A.

  TXA2

• B.

  PGG2

• C.

  PGE2

• D.

  PGH2

Misoprostol is used vaginally in combination with __________ for termination of early pregnancy.

Which NSAID is the least renal toxic?

• A.

  Piroxicam

• B.

  Meloxicam

• C.

  Ibuprofen

• D.

  Indomethacin

• E.

  Sulindac

• F.

  Diclofenac

Sulindac undergoes in vivo _______ to form the sulfide form, the active drug,

• A.

  Oxidation

• B.

  Reduction

Unlike Aspirin, Salsalate does not inhibit thromboxane synthetase (does not acetylate), therefore, it has no effect on platelet function.

• A.

  True

• B.

  False

Piroxicam has less severe GI side effects than meloxicam.

• A.

  True

• B.

  False

Piroxicam undergoes what kind of metabolism?

• A.

  O-demethylation

• B.

  Hydroxylation of pyridine ring (5')

• C.

  Oxidation

• D.

  Phenyl ether cleavage

Which of the following is true regarding Meloxicam?  Select all that apply.

• A.

  It is 10 fold more selective for COX-2 than COX-1

• B.

  It is dosed twice daily

• C.

  It is part of an enolic class of NSAIDs

All NSAIDs can cause CNS effects such as dizziness, anxiety, and headaches.  Which of the following NSAIDs may cause severe CNS effects?

• A.

  Indomethacin

• B.

  Naproxen

• C.

  Tolmentin

• D.

  Diflunisal

Which of the following is true regarding ASA?  Select all that apply.

• A.

  Potency: COX-1 > COX-2

• B.

  Rapidly hydrolyzed by plasma esterases

• C.

  Stable in solution

• D.

  Prevents colon polyp formation

• E.

  The COOH has a direct corrosive effect in causing ulceration

• F.

  Oral bioavailability is 80 to 100%

• G.

  Short half life

Nabumetone's reduced GI side effects is probably due to its COX-2 selectivity and the fact that it has no acidic functional group.

• A.

  True

• B.

  False

Ketorolac is as effective as the opioids in the short term treatment of moderate to severe postoperative pain.

• A.

  True

• B.

  False

Which of the following is true regarding Ibuprofen?  Select all that apply.

• A.

  Sold as racemate. S-enantiomer is more active in vitro (but R-enantioner covered to S-enantiomer in vivo)

• B.

  Metabolism involves I-bu chain oxidation

• C.

  First member of its class (arylpropionic acids)

• D.

  Better tolerated then ASA or Indomethacin

Which drug is available as an opthalmic solution and topical gel?

• A.

  Ibuprofen

• B.

  Aspirin

• C.

  Diclofenac

• D.

  Indomethacin

• E.

  Salsalate

Diflunisal is effective as an antipyretic.

• A.

  True

• B.

  False

NSAIDs _________ gestation.

• A.

  Shorten

• B.

  Prolong

Naproxen's half life is ___ hours.

• A.

  3

• B.

  13

• C.

  23

DMARDs include which of the following?  Select all that apply.

• A.

  Gold compounds

• B.

  Immunosupressants

• C.

  Anticancer agents

• D.

  Antimalarials

PGG2 is converted to PGH2 by which enzyme?

Which is involved in vasoconstriction, platelet aggregation, and bronchoconstriction...

• A.

  Prostacylins

• B.

  Prostaglandins

• C.

  Leukotrienes

• D.

  Thromboxanes

TXA2 has a half life of 30 seconds.

• A.

  True

• B.

  False

The aliphatic residue of this molecule is of smaller size and creates a side pocket.

• A.

  COX-1

• B.

  COX-2

Which enzyme is found in platelets?

• A.

  COX-1

• B.

  COX-2

Aspirin's major metabolic pathway occurs when this occurs.  Also, what percent of an ASA dose is excreted as salicylic acid?

• A.

  Oxidation, 1%

• B.

  Oxidation, 10%

• C.

  Oxidation, 20%

• D.

  When glycine complexes with the COOH, 1%

• E.

  When glycine complexes with the COOH, 10%

• F.

  When glycine complexes with the COOH, 20%

• G.

  Glucuronidation, 1%

• H.

  Glucuronidation, 10%

• I.

  Glucuronidation, 20%

Which of the following is true regarding this NSAID?  Select all that apply.

• A.

  Antipyretic, analgesic, and anti-inflammatory

• B.

  Causes less GI upset than ASA

• C.

  Available as oral liquid

• D.

  Inhibits thromboxane synthetase

• E.

  COX inhibitor (irreversible)

Diclofenac undergoes HYDROXYLATION at which position?

• A.

  1

• B.

  2

• C.

  3

• D.

  4

• E.

  5

• F.

  6

• G.

  7

Aspirin can prevent colon cancer by preventing polyp formation.

• A.

  True

• B.

  False

Metabolism of this drug primarily includes...

• A.

  Oxidation

• B.

  Glucuronidation

• C.

  O-demethylation

Which of the following drugs have no appreciable effect on platelets?  Select all that apply.

• A.

  Diflunisal

• B.

  Salsalate

• C.

  Piroxicam

• D.

  Celebrex

• E.

  Choline salicylate

• F.

  Aspirin

• G.

  Sodium salicylate

• H.

  Fenoprofen

• I.

  Naproxen

Diflunisal is 4 to 5x more potent than ASA, has neglible antipyretic effects, and has less GI side effects.

• A.

  True

• B.

  False

Diclofenac undergoes extensive ______ metabolism.

• A.

  Renal

• B.

  Hepatic

Which of the following drugs are pro-drugs?  Select all that apply.

• A.

  Sulindac

• B.

  Diclofenac

• C.

  Nabumetone

• D.

  Indomethacin

Ketorolac was the first parenteral NSAID.

• A.

  True

• B.

  False

Which useful group of NSAIDs is also known as "profens?"  They are potent anti-inflammatory drugs because of the addition of a methyl group.

• A.

  Arylacetic acid

• B.

  Pyrroleacetic acid

• C.

  Arylpropionic acid

Metabolism of ibuprofen involves the i-bu chain oxidation.

• A.

  True

• B.

  False

Naproxen is the top NSAID.

• A.

  True

• B.

  False

NSAIDs increase uterine motility.

• A.

  True

• B.

  False

________  increases celecoxib plasma two-fold.

Celebrex is approved for RA, OA, acute pain, and FAP.

• A.

  True

• B.

  False

Which of the following can safely be taken with methotrexate?  Select all that apply.

• A.

  NSAIDs

• B.

  Celebrex

• C.

  BRMs

Which DMARDs are used in mild cases of RA?  Select all that apply.

• A.

  Hydroxychloroquine

• B.

  Methotrexate

• C.

  Sulfasalazine

NSAIDs have the most rapid onset of action.  Between DMARDs and BRMs, which acts more quickly?

• A.

  DMARDs

• B.

  BRMs