Exam 4 Analgestics Flashcards

1
Q

cox1

A

constitutive, housekeeping, all tissues

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2
Q

cox2

A

constitutive in kidney, otherwise inducable

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3
Q

NSAIDS prototype

A

aspirin (prototype)

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4
Q

What enzyme releases arachidonic acid? what is it inhibited by?

What are two pathways?

A

phospholipase A2; inhibited by glucocoticoids

1) lipooxygenase -> leukotrienes (bronchoconstrictor, inflammation)
2) cyclooxygenase -> prostaglandins, prostacyclins, and thromboxane

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5
Q

cox1 response

A

1) thromboxane: inhibit cox1 > inhibit thromboxane> inhibit clot formation (why aspirin works)
2) prostacyclins: inhibit cox1 > limit acid secretion control > thinner mucin layer > lining exposure and pain (NSAIDs cause stomach pain)
3) prostaglandins: help fluid movement inkidney

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6
Q

cox 2 constitutive response

A

prostacyclin in vasculature prevents platlet aggregation and micro clots
so inhibit cox2 > remove micro clot inhibition > you GET clots (why cox2 selective was a bad idea)

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7
Q

cox2 inducible

A

fever, pain, inflammation

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8
Q

name of aspirin?

A

acetyl salicyclic acid

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9
Q

basic therapuetic effect of NSAIDs

A

analgesic
antipyretic
anti-inflam

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10
Q

what is only NSAID to permanently inhibit platlets?

A

aspirin

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11
Q

1) aspirin lowers ____ plasma levels to reduce inflame?

2) does aspirin have uricosuric action?

A

1) C-reactive protein due to prostaglandin synthesis inhibition
2) only in high doses

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12
Q

adverse aspirin

A
respiratory alkalosis
"ringing in ears" = tinnitus
ulcers
hypertension
rare hypersenstivity
REYE SYNDROME
*premature closure of ductus arterisus*
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13
Q

low dose aspirin

A

aka baby aspirin = 1/4 normal, 82mg

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14
Q

what drug is used to prevent ulcers in pts on NSAIDs?

A

misoprostol (Cytotec)

  • inhibits acid secretion and stimulates mucus production
  • get diarrhea
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15
Q

ionized or un-ionized passes through membrane?

A

UN-ionized, lower pH has more un-ionized so it is absorbed more

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16
Q

why moniter pH in pts of aspirin overdose?

A

switch from alkalosis to acidosis

17
Q

why not give a person with gout aspirin?

A

at low levels it decreases secretion of uric acid making the gout worse

18
Q

clinical uses of aspirin

A
pain
RA
fever
cardiovascular prevention
dysmenorrhea
patent ductus arteriosus
reduce cancer and alzheimer's risk
19
Q

what NSAIDs are approved for pharmacotherapy of patent ductus arteriosus?

A

indomethacin and ibuprofin

20
Q

what is the derivative of salicyclic acid?

A

difluorophenyl

21
Q

difluorophenyl

A

long 1/2 life

– similar side effects as aspirin bit more stomach friendly

22
Q

acetaminophen pathway

A

acetaminophen converted in liver by CY2E1 into toxic, converted from toxic metabolite by GLUTATHIONE to inactive
* don’t drink alcohol with acetaminophen UNLESS you are an alcoholic, bc they have increased levels of 2E1 and alcohol is it’s preferred substrate

23
Q

acetaminophen vs aspirin

A

aspirin pKA=3

  • stomach probs
  • cox responds in PNS
  • more cox1 effects

acetaminophen pka= 9.5, so FASTER bc more un-ionized in stomach

  • NOT an NSAID
  • no anti-inflam, but has equal analgestic and anti-pyretic to aspirin
  • cox responds in CNS
  • SEVERE liver toxicity (4g per day FDA) = black box
  • equal cox1 & 2
  • – CYP2E1 enzyme
24
Q

avoid acetaminophen with?

A

alcohol, codeine (depleits liver of glutathione) and warfarin (increases INR and anticoagulation)

25
gold standard for pain control
400mn of Ibuprofen
26
what is name for ibuprofen?
propionic acid
27
ibuprofen has cross-reactivity to?
aspirin (salicylates)
28
motrin is?
ibuprofen
29
what is sister drug to ibuprofen
naproxen
30
ibuprofen vs naproxen
ibuprofen- rapidly absorbed, 1/2 life is 2 hrs, 6x daily naproxen- 1/2 life of 12 hrs, 2x daily, and safety concern due to hypertension
31
propionic acid drugs
ibuprofen naproxen ketoprofen
32
Celecoxib (celebrex)
used for osteoarthritis and acute pain - long 1/2 dose - stomach friendlier than aspirin - CAUSES HEART ATTACKS
33
meloxicam (Mobic)
cox2 preferrential | - black box: heart probs
34
List cox2 blockers
Celecoxib (celebrex) | meloxicam (Mobic)