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Pharm > Exam 4 Analgestics > Flashcards

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
Q

gold standard for pain control

A

400mn of Ibuprofen

26
Q

what is name for ibuprofen?

A

propionic acid

27
Q

ibuprofen has cross-reactivity to?

A

aspirin (salicylates)

28
Q

motrin is?

A

ibuprofen

29
Q

what is sister drug to ibuprofen

A

naproxen

30
Q

ibuprofen vs naproxen

A

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
Q

propionic acid drugs

A

ibuprofen
naproxen
ketoprofen

32
Q

Celecoxib (celebrex)

A

used for osteoarthritis and acute pain

  • long 1/2 dose
  • stomach friendlier than aspirin
  • CAUSES HEART ATTACKS
33
Q

meloxicam (Mobic)

A

cox2 preferrential

- black box: heart probs

34
Q

List cox2 blockers

A

Celecoxib (celebrex)

meloxicam (Mobic)

Pharm (15 decks)

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