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Therapeutics > Lecture 19: NSAIDs > Flashcards

Lecture 19: NSAIDs Flashcards

1
Q

NSAID activity

A

-anti-inflammatory
-analgesic
-antipyretic

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2
Q

NSAID use

A

-treat pain, fever, inflammation
-treat early rheumatoid arthritis and osteoarthritis
-cancer prevention

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3
Q

NSAID mech of action

A

-inhibit COX
=inhibit prostaglandin synthesis

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4
Q

Classes of NSAIDs

A

-salicylates
-arylacetic acids
-arylpropionic acids
-non-carboxylate
-COX-2 selective

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5
Q

Side effects of NSAIDs

A

-GI tract
-blood coagulation
-renal
-hypersensitivity
-Reye’s syndrome
-CNS

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6
Q

GI effects of NSAIDs

A

-dyspepsia, nausea, vomiting
-blood loss, ulcer, hemorrhage

-aspirin ~ indomethacin > naproxen > sulindac

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7
Q

Mech of NSAIDs on GI tract

A

-acidity
-inhibit protective PGEs in mucosa
-inhibit aggregation (increased tendency to bleed)

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8
Q

Side effects of NSAIDs on blood coagulation (ASPIRIN)

A

-Aspririn prolongs bleeding time by IRREVERSIBLE inhibition og COX-1 and reduced formation of TXA2
-don’t use before surgery
-can prevent coagulation in CV disease

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9
Q

Renal side effects of NSAIDs

A

-renal failure in patients with CV, hepatic, and renal disease

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10
Q

NSAID hypersensitivity

A

-skin rashes, hives, angioedema, asthma-like syndrome
-blocked by 5-lipooxygenase inhibitors
-0.3% of population 10% in asthmatics

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11
Q

Reye’s Syndrome (NSAID effects)

A

-only from salicylates
-rare life threatening
-vomiting, delirium, coma
-brain damage
-occurs in children who have had flu or pox
-do NOT give to anyone under 12 w a fever

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12
Q

CNS side effects of NSAIDs

A

-tinnitus
-dizziness
-headache

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13
Q

Prevention of GI side effects

A

-misoprostol
-proton-pump inhibitors
-combo products

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14
Q

Misoprostol

A

-synthetic PGE1 analog
-used to prevent gastric ulcers in high risk patients

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15
Q

Proton-pump inhibitors (esomeprazole)

A

-reduce acid secretion
-protect against ulceration in absence of COX-1 activity

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16
Q

Combo products for GI effects

A

-Naproxen/esomeprazole
-Naproxen/misoprostol
-NDicolfenac/misoprostol

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17
Q

Drug interactions of NSAIDs

A

-may compete for serum albumin binding sites with other drugs
-ex: anticoagulants

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18
Q

NSAID intereaction with anticoagulants

A

-inc plasma concentration of free anticoagulant
-and its WORSE bc salicylates promote bleeding

-must lower the dose of anticoagulant

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19
Q

SAR of NSAIDs

A

-acidic group off the ring
-add a methyl group to that C to increase activity (ibuprofen)
-another area of lipophilicity (another ring or alkyl) inc activity

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20
Q

Salicylates

A

-salicyclic acid
-acetylsalicylic acid (aspirin)
-salsalate
-diflunisal

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21
Q

Salicylic Acid

A

-from willow tree
-slightly acidic
-absorbed as ionic form in small intestine
-absorbed as acid form in stomach
-REVERSIBLE COX1/2 inhibiton
-may suppress COX-2 induction

22
Q

Aspirin (acetylsalicylic acid)

A

-IRREVERSIBLY inhibits COX
-acetylates serine in active site
-absorbed intact but hydrolyzed to salicylate by esterase
-2-fold more potent than salicylic acid ad analgesic/antipyretic
-blocks TXA2
-inc risk of bleeding
-reduces risk of MI
-not stable in solutions

23
Q

Salsalate

A

-dimer of salicylic acid
-hydrolyzed in SI
-does NOT cause GI bleeding

24
Q

Diflunisal

A

-better analgesic than aspirin
-fewer side effects
-less antipyretic activity
-longer half life
-F

25
Q

Arylacetic Acids

A

-indomethacin
-sulindac
-etodolac
-diclofenac

26
Q

Indomethacin

A

-v potent
-lots side effects
-do NOT use long term
-not atble in solution (hydrolysis of amide bond)

27
Q

Sulindac

A

-prodrug (sulfoxide reduced to active sulfide intermediate in circulatory system
-less side effects
-ok for long term use

28
Q

Etodolac

A

-pyranocarboxylic acid
-almost as potent as indomethacin
-a lil selective for COX2
-less GI bleeding
-long term use for osteoarthritis

29
Q

Diclofenac

A

-most widely used NSAID in the world
-as potent as indomethacin
-lil selective for COX-2
-inhibits COX and lipoxygenase pathways

30
Q

Arylpropionic Acids

A

-ibuprofen
-naproxen
-ketorolac

31
Q

Ibuprofen

A

-OTC analgesic
-more potent than aspirin
-less potent than indomethacin
-some GI irritation

32
Q

Ibuprofen SAR

A

-a-methyl group enhances activity and reduced side effects
-racemic mix
-R is converted to S in vivo

33
Q

Naproxen

A

-S enantiomer
-more potent than ibuprofen
-GI irritation
-treat rheumatoid arthritis and osteoarthritis

34
Q

Ketorolac

A

-cyclized heteroarylpropionic acid derivative
-short-term
-analgesic activity similar to centrally acting analgesics
-alt to narcotics

35
Q

Non-carboxylates

A

-nabumetone
-meloxicam

36
Q

Nabumetone

A

-nonacidic prodrug
-metabolized to 6-MNA which is effective inhibitor of COX
-minimum effects
potent anti-inflammatory
-weak analgesic

37
Q

Meloxicam

A

-belongs to oxicam class
-resembles peroxy radical intermediate in COX
-enolic acid
-long acting, qd dose
-as potent as indomethacin
-a lil selective for COX-2

38
Q

Doses

A

slide 33

39
Q

Effects of COX-1 Inhibition

A

-stomach irritation
-ulceration
-block aggregation
-block uterine motility
-blovk prostaglandin-mediated renal function
-hypersensitivity

40
Q

Preferential inhibition of COX-2 gives

A

anti-inflammatory effects with lower incidence of gastric ulceration

41
Q

Selective COX-2 Inhibitor drugs

A

-Celecoxib
-rofecoxib (disc)
-valdecoxib (disc)

42
Q

Selective COX-2 inhibitors

A

-valine in NSAID binding site of COX-2 is swapped for isoluecine in COX-2
-exploit larger binding sire in COX-2 with big substituents

43
Q

Side effects of selective COX-2 inhibtion

A

-inc BP
-atherogenesis
-no PGI2 production
-does NOT affect TXA2 production by COX-2
-BUT TXA2 inc in response to plaque
-inc risk of heart attack/strokeq

44
Q

Celecoxib

A

-first COX-2 inhibitor NSAID
-use for osteoarthritis and rheumatoid arthritis
-fights pain, inflammation, and fever
-as potent as naproxen
-less GI side effects
-NO antiplatelet activity

45
Q

Acetaminophen activity

A

-analgesic and antipyretic effects like aspririn
-weaker as an anti-inflammatory

46
Q

Acetaminophen mech of action

A

-does NOT inhibit arachidonic acid binding to PGHS
-Scavenges peroxynitrite required for PGHS activity

47
Q

Peroxynitrite

A

-major oxidant for PGHS in the CNS
-concentration is high in inflammation and acetaminophen scavenging is overwhelmed

48
Q

Acetaminophen effects

A

-less GI
-tolerated in blood coagulation diseases
-no reye’s syndrome
-maybe a rash but not rlly hypersensitivity
-does not cross-react w aspirin

49
Q

Acetaminophen hepatotoxicity

A

-CYP450 hydroxylation forms N-acetylimidoquinone
-reacts w glutathione
-high doses overload glutathione and cell damage occurs in liver

50
Q
A

Therapeutics (78 decks)

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