NSAIDs

Question 1

Signs of inflammation

Answer 1

SLHRP
Swelling, Loss of function, heat, redness and pain

Question 2

Fill in the Eicosanoids Effects

Answer 2

Question 3

When Eicosanoids bind to GPCRs in the target cells, the generation of what causes dilation? Constriction?

Answer 3

Generation of cAMP (Gs) = dilation
Release of calcium (Gq) = constriction

Question 4

20-carbon polyunsaturated fatty acid that is the most abundant and important precursor of eicosanoids

Answer 4

Arachidonic acid

Question 5

On Arachidonic acid, which carbon has an inflammatory effect?

Answer 5

6 carbon

Question 6

PGH synthase has both ____ & _____ activities

Answer 6

COX and hydroperoxidase

Question 7

“Housekeeping” function; COX 1
Constitutively expressed in various tissues

Answer 7

PGH synthase-I

Question 8

Expressed upon stimulus in inflammatory and immune cells
COX 2
Stimulated by growth factors, tumor promoters, and cytokines

Answer 8

PGH synthase-2

Question 9

What are PGH synthase 1 and 2 inhibited by?

Answer 9

NSAIDS

Question 10

Synthesis of prostaglandins

Answer 10

Question 11

What classification of drug is this?
PGE1
Relaxes smooth muscles and expand blood vessels
Used for erectile dysfunction by injection or as a suppository

Answer 11

Alprostadil
Eicosanoid drugs

Question 12

What classification of drug is this?
PGE1 derivative; Cytoprotective
Prevents peptic ulcer
Terminates early pregnancy in combo with mifepristone

Answer 12

Misoprostol
Eicosanoid drugs

Question 13

What classification of drug is this?
Topically active PGF2a derivative (prodrug)
Constrict blood vessels
Used in ophthalmology to treat high pressure inside the eye

Answer 13

Latanoprost
Eicosanoid drugs

Question 14

What classification of drug is this?
PGI2; powerful vasodilator
Inhibitor of platelet aggregation
Used to treat pulmonary arterial hypertension by IV injection or inhalation
Should not be used with anticoagulants

Answer 14

Prostacyclin (epoprostenol)
Eicosanoid drugs

Question 15

NSAIDs mechanism of action: inhibition of ____ & _______

Answer 15

prostaglandin and COX 1 and 2

Question 16

Side effects of NSAIDs

Answer 16

Blood coagulation, hypersensitivity, Reye’s

Question 17

Synthetic PGE1 analog
Used prophylactically to prevent NSAID-induced gastric ulcers in patients at high risk

Answer 17

Misoprostol

Question 18

Many NSAIDs are highly bound to _____ ______

Answer 18

serum albumin

Question 19

Absorbed as an ionic form from the small intestine and, to lesser extend, from the stomach as an acid form
Inhibits COX 1 and 2 reversibly
May suppress COX-2 induction

Answer 19

salicylates

Question 20

The only NSAID that irreversibly inhibits COX by acetylating a serine residue in the active site

Answer 20

Aspirin (acetylsalicylic acid)

Question 21

What classification of drug is this?
Dimer of this group
Hydrolyzed to two salicylates in the small intestine and absorbed
Does not cause GI bleeding

Answer 21

Salsalate (Disalcid)
Salicylates

Question 22

What classification of drug is this?
More potent analgeic than aspirin but produces fewer side effects
Less antipyretic activity than aspirin
3-4 fold longer half life than aspirin

Answer 22

Diflunisal (Dolobid)
Salicylates

Question 23

What classification of drug is this?
One of the most potent NSAIDs in use
High incidence of side effects; not suitable for a long-term use
Not stable in solution due to the hydrolysis of the amide bond

Answer 23

Indomethacin
Arylacetic acid

Question 24

What classification of drug is this?
Prodrug; the sulfoxide group id reduced to the active sulfide intermediate in the circulatory system
Less GI side effects
Suitable for a long-term use to treat chronic inflammation

Answer 24

Sulindac
Arylacetic acids

Question 25

What classification of drug is this? Pyranocarboxylic acid As potent as indomethacin Somewhat selective for COX-2 Less GI bleeding; suitable for long-term use to manage osteoarthritis

Answer 25

Etodolac Arylacetic acids

Question 26

What classification of drug is this? The most widely used NSAID in the world As potent as indomethacin Somewhat selective for COX-2 Inhibits both COX and lipoxygenase pathways

Answer 26

Diclofenac Arylpropionic acid

Question 27

Popular OTC analgesic More potent than aspirin, but less than indomethacin Moderate degrees of gastric irritation Bioequivalent racemic mixture

Answer 27

Ibuprofen Arylpropionic acid

Question 28

S-(+)-enantiomer; more potent than ibuprofen Moderate degrees of gastric irritation Used to treat rheumatoid arthritis and osteoarthritis

Answer 28

Naproxen (Aleve)

Question 29

Cyclized heteroarylpropionic acid derivative Short-term management of moderate to severe pain Analgesic activity similar to centrally acting analgesics Widely accepted alternative to narcotic analgesics

Answer 29

Ketorolac

Question 30

What classification of drug is this? Nonacidic prodrug Metabolized rapidly which is an effective inhibitor of COX Minimum gastric side effects Potent anti-inflammatory, but weak analgesic activity

Answer 30

Nabumetone Non-carboxylate

Question 31

What classification of drug is this? Belongs to the oxicam class, which resembles the peroxy radical intermediate in COX Enolic acid Long acting; single daily dose; somewhat COX-2 selective As potent as indomethacin

Answer 31

Meloxicam

Question 32

Preferential inhibition of _____ gives anti-inflammatory effects with lower incidence of gastric ulceration

Answer 32

COX-2

Question 33

What is the suffix for COX-2 inhibitors?

Answer 33

(-coxib)

Question 34

First NSAID to be marketed as selective COX-2 inhibitor Used for osteoarthritis and rheumatoid arthritis Good efficacy against pain, inflammation, and fever As potent as naproxen; less risk of GI side effects; no antiplatelet activity

Answer 34

Celecoxib (Celebrex)

Question 35

Analgesic and antipyretic effects similar to aspirin but with fewer adverse effects not NSAID Much weaker as an anti-inflammatory agent

Answer 35

Acetaminophen