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Pharm - AntiArrhythmic/Opiods > Pharmacology of non-opiate analgesics > Flashcards

Pharmacology of non-opiate analgesics Flashcards

1
Q

amine autocoids

A

histamine

serotonin

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2
Q

lipid derived autocoids

A

prostaglandins

leukotrienes

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3
Q

peptide hormones

A

bradykinin

angiotensin

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4
Q

non classified class of autocoids

A

cytokines

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5
Q

timeline of non-opioids for pain

A 
aspirin
acetaminophen
paracetamol
ibuprofen
indomethacin
diclofenac
naproxen
piroxicam
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6
Q

Salicylates class of NSAIDs

A

aspirin

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7
Q

Arylpropionic acids class of NSAIDs

A

ibuprofen

naproxen

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8
Q

Arylacetic acids class of NSAIDs

A

indomethacin
diclofenac
ketorolac
etodolac

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9
Q

Enolic acids class of NSAIDs

A

piroxicam

meloxicam

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10
Q

2nd class of non-opioid that isn’t NSAID

A

p-Aminophenols

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11
Q

Only drug of p-aminophenols

A

acetaminophen

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12
Q

NSAIDs for analgesic

A

> headache: tylenol
chronic postsurgical pain: tylenol + opioid
myalgias/arthralgias/sprains/strains: ibuprofen
inflammatory pain: ibuprofen
dysmenorrhea(specific PGE effect): ibuprofen

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13
Q

NSAIDs for antipyretic

A

> fever: acetaminophen

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14
Q

NSAIDs for anti-inflammatory

A 
bursitis and tendonitis
osteoarthritis
RA including ankylosing spondylitis
gout and hyperuricemia
rib fractures
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15
Q

5 symptoms of inflammation

A

rubor: redness
tumor: swelling
calor: heat
dolor: pain
…and loss of function

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16
Q

3 phases of inflammation

A

acute; vasodilation and increased permeability
subacute; infiltration
chronic; proliferation

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17
Q

mediators that recruit inflammatory cells

A 
eicosanoids
> arachidonic acid metabolites
> PG; redness, heat
> thromboxanes
> leukotrienes; swelling
> cytokines; pain
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18
Q

main function of NSAIDs; inhibit what and what pathway

A

cox inhibitors in the arachidonic pathway

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19
Q

cox-1 produces

A

prostanoids from arachadonic acid

20
Q

prostanoids metabolites include

A

TXA2
PGE2
PGI2

21
Q

function of TXA2

A

> prothombotic; increase platelet activation and clotting via gp2b3a
vasoconstriction
inhibitor acts as blood thinner

22
Q

function of PGE2 and PGI2

A

> protect stomach lining cox 1 GI expression
inhibit acid secretion
promote mucus secretion
inhibition can lead to stomach ulcers

23
Q

cox-1 expressed where

A

platelets, kidneys, stomach

24
Q

function of PGI2 in vasculature

A

vasodilation

reduce platelet aggregation

25
Q

cox-2 expressed where

A

brain

spinal cord

26
Q

function of cox-2

A

> induced in setting of inflammation

> induced by cytokines and inflammatory mediators

27
Q

MOA of aspirin

A

irreversibly inhibits cox-1 and modifies cox-2 by acetylation

28
Q

Aspirin and cox-2

A

modified by acetylation to turn off its ability to produce PGE and activate its ability to produce protective lipid mediators

29
Q

Arylacetic acids that inhibit leukotriene synthesis

A

indomethacin

diclofenac

30
Q

Absorption of salicylates

A

> rapidly absorbed from stomach and jejunum
passive diffusion of free acid; gastric pH
delayed by presence of food

31
Q

distribution of salicylates

A

> throughout most tissues and fluids
readily crosses placenta
competes with many drugs for protein binding sites

32
Q

metabolism and excretion of salicylates

A

> aspirin t1/2 15min
salicylate t1/2 12hrs
active secretion and passive reabsorption in renal tubule
increased excretion with increased urinary pH

33
Q

absorption of non-salicylate NSAIDs

A

> well absorbed from GI tract

34
Q

metabolism of non-salicylate NSAIDs

A

> little first pass metabolism

> oxidation, demethylation, conjugation for metabolism

35
Q

excretion of non-salicylate NSAIDs

A

> drugs and metabolites excreted primarly as conjugates

> active secretion of parent drug in renal tubule

36
Q

Aspirin general use

A

> analgesia, antipyresis, anti-inflammatory
main use of anti-coagulation
no tolerance development
risk in treating children; Reye’s syndrome(rash, vomitting, liver necrosis)

37
Q

Arylpropionic acids half life

A

Ibuprofen: 2hr
Naproxen: 14hr

38
Q

NSAID for coronary artery disease

A

safest is naproxen

39
Q

Diclofenac use

A

gel for arthritic pain

40
Q

risk of diclofenac

A

> increased risk of peptic ulcer and renal dysfunction with prolonged use

41
Q

Arthrotec description

A

> diclofenac/misoprostol mix

> misoprostol = PGE1 analog

42
Q

indomethacin MOA

A

potent reversible inhibitors of PG biosynthesis

43
Q

use for indomethacin

A

acute gouty arthritis, ankylosing spondylitis, pericarditis

44
Q

ketorolac

A

> should not be given longer than 5 days

> available as IV

45
Q

Use of enolic acids(Meloxicam, Piroxicam)

A

> treat arthritis
great joint penetration
one of the least GI side effects

46
Q

Half lives of enolic acids

A

> Meloxicam: 20hrs
Piroxicam: 57hrs

low dose meloxicam is cox-2 selective

47
Q

ended on page 18

A

aa

Pharm - AntiArrhythmic/Opiods (4 decks)

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