anti inflammatories and related drugs (pharm at UVic) Flashcards

1
Q

which NSAIDs are nonselective COXinhibitors

A

ibuprofen
diclofenac
aspirin
naroxen

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2
Q

which NSAIDs are selective COX2 inhibitors

A

celecoxib

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3
Q

which conditions are treatee by ASA, NSAIDS, acetaminophen

A
Bursitis
Dysmenorrhea
Fibromyalgia
Gout
Migraine
Osteoarthritis
RA
Juvenile RA
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4
Q

which organ are NSAIDs hard on

A

kidneys

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5
Q

what is the prototype analgesic-antipyretic-antiinflm drug

A

ASA

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6
Q

other than ASA what drugs are analgesic-antipyretic-antiinflm drug

A

NSAIDs
acetaminophen

Drugs used to prevent or treat gout and migraine

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7
Q

are COX1 or COX 2 pathologic prostaglandins

what do they do

A

inflm

  • vasodilation
  • inc cap perm
  • edema
  • pain

leukocytosis\
activation of WBC to rel inflm cytokines

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8
Q

what does COX1 do and what are these aka

A

physiologica prostaglandins (aka)

GI protection

  • dec gastric acid secretion
  • inc mucus prod
  • maint of GI mucosal perfusion

renal protection
-maint of renal perfusion
maint of renal fx

relaxes sm muscle tone

  • vasodilation
  • bronchodilation

regs platelet aggregation

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9
Q

what is primary dysmenorrhea d/t?

how is this involved/produced and what effect does it have?

A

**inc prostaglandins and vasopressin in primary dysmenorrhea -> **inc muscle contractions (cramping) and pain (make the uterine muscles contract and help the uterus shed the lining that has built up during the menstrual cycle. )

the prostaglandins are made in the uterus

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10
Q

if pain during menses why is this? in r/t prostaglandins

A

too many prostaglandins produced

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11
Q

what other conditions can prostaglandins produce

A

Prostaglandins can also cause headaches, nausea, vomiting and diarrhea.

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12
Q

TX of primary dysmenorrhea (meds)

A

NSAIDs (prostaglandin inhibitor) eg aspirin or ibuprofen
-naproxen sodium is stronger but requires a prescription

-extended cycle oral contraceptive (prevents excessive growth of uterine lining)

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13
Q

Tx of primary dysmenorrhea nonpharm

A

Therapies for primary dysmenorrhea include rest, heating pad to the lower abdomen or back, proper nutrition, aerobic exercise and medication. Nutrition therapy includes a well-balanced diet with an adequate intake of calcium (1000 mg. per day) and fluid intake of two quarts of water each day. Vitamin E about 500 units a day, Vitamin B1 about 100mg a day and Vitamin B6, 200 mg. each day, may occasionally be helpful.

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14
Q

when taking NSAIDs is it best with or without food

A

take w food to prevent GI upset

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15
Q

taking NSAIDS for dysmenorrhea what part of cycle is best?

specific dose?

A
  • gen started 1-3 days prior to menstruation

- sometimes nec to take one of several NSAIDs until one with ma efficacy is found

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16
Q

how does hormonal alteration for dysmenorrhea alter pain

A

hormonal contraception prevents ovulation which dec thickness of uterine lining resulting in fewer prostaglandins

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17
Q

what is Depo-Provera and a consideration for this

A

it is a BC shot you get q10-12 wks

-MUST get adequate Ca2+ 1000mg

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18
Q

what kind of half-life do NSAIDs have

A

varies from short (less than hr) to longer than 12hrs

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19
Q

protein binding and NSAids

what % are bound

A

heavily bound

60-90%

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20
Q

metb of NSAIDs and ASA

A

in liver

21
Q

**what side effects do almost all NSAIDS cause

A

***Virtually all NSAIDs can cause dyspepsia and GI toxicity including ulceration. Except celecoxib

22
Q

aside from Gi upset what is a major consideration for almost all NSAIDs

what is exception to this

A

All except the nonacetylated salycilates? can effect bleeding time

23
Q

is the effect that NSaids have on bleeding time reversible? which drug is the exception?

A

generally reversible except for aspirin which lasts the life of the platelet

24
Q

where is Cox1 made

A

COX-1 is formed in all tissues and cells, especially platelets, endothelial cells, GI tract, and kidneys

25
Q

where is COX-2 found

A

COX-2 is present brain, bone, kidneys, GI tract and female reproductive system

26
Q

which dugs act on COX 1 or 2? what is the end result on the goal substance?

A

Aspirin, NSAIDs and acetaminophen inactivate cyclooxygenases, effectively blocking prostaglandin formation.

27
Q

Does aspirin or NSAIDs

  • act both centrally and periph to black pain impulses
  • act periph to block pain impulses
A

aspirin-act both centrally and periph to black pain impulses

NSAIDs–act periph to block pain impulses

28
Q

Does aspirin or NSAIDs

Act on hypothalamus to decrease temperature and reset thermostat

A

both do this

29
Q

Does aspirin or NSAIDs

Prevents prostaglandins from increasing pain and edema

A

both do but I think NSAIDs more…it was **Prevents prostaglandins from increasing pain and edema

30
Q

what is the antiplatelet activity of aspirin vs NSAIDs

which is longer acting

A

aspirinAntiplatelet effects by preventing synthesis of throboxane A2

NSAID-Antiplatelet effects bind reversibly with platelet COX-1 (shorter acting than aspirin)

31
Q

Indications: celecoxib

A

elecoxib used to treat familial adenomatous polyposis

(some kind of lg intestine thing)

32
Q

indications of NSAIDs and other antipyretic, anti inflm meds

A

Treat mild-moderate pain (may be combined with oral opioid)

  • *Anti-inflammatory
  • *Antipyretic
  • *Antiplatelet - low dose cardioprotective
33
Q

what is relationship of NSAIDs to eyes

A

may be used for eye disorders

but all NSAIDs cause dry eyes

34
Q

contraindications

general

A

GI disorders
Hypersensitivity
Renal disease

35
Q

*contraindication for aspirin

A

Aspirin is *****contraindicated for children in presence of viral infection due to association with Reye’s Syndrome

36
Q

**celecoxib contra when..

A

pt is allergic to sulfonamides

37
Q

what are the general categories of NSAIDs eg ..acid

A
  • propionic acid derivatives
  • acetic acid..
  • mefenamic acid
  • oxicam
  • diclofenac
  • celecoxib
38
Q

which of these is ibuprofen and what the max dose

  • propionic acid derivatives
  • acetic acid..
  • mefenamic acid
  • oxicam
  • diclofenac
  • celecoxib
A

its a type of propionic acid derivative

the max is 2x400-3x200mg/day

so…800mg/day max?

39
Q

what are the consequences of the acetic acid derivatives

A
  • indomethacine and sulindac

- -GI ulceration, bone marrow depression, hemolytic anemia, mental confusion, depression and psychosis

40
Q
Mefenamic acid (Ponstan): 
Oxicam drugs: 

whih has a long half life and which causes GI upset

A
Mefenamic acid (Ponstan): GI upset
Oxicam drugs: long half-lives
41
Q

what is another major concern w celecoxib ** and wht is the dose

A

dose 100-400mg/day, iincreased risk of cardiovascular events such as MI and stroke with COX-2 inhibitors.

42
Q

what is max dose for acetaminophen

A

4g

43
Q

what are the names of the drugs used to treat gout and hyperuricemia

A

Allopurinol (Zyloprim)
Colchicine
Probenecid (Benemid)
Sulfinpyrazone (Anturan)

44
Q

how do allopurinol and colchicine work (tx of gout)

A

Allopurinol prevents formation of uric acid by inhibiting xanthine oxidase.

Colchicine decreases inflm by decreasing the movement of leukocytes into body tissues containing urate crystals. It has no analgesic or anti-pyretic effects.

45
Q

howdo probenecid and sulfinpyrazone work

A

Probenecid (Benemid) increases the urinary excretion of uric acid. This uricosuric action is used therapeutically to treat hyperuricemia and gout.

Sulfinpyrazone (Anturan) is a uricosuric agent similar to probenecid. It is not effective in acute gout but prevents or decreases tissue changes of chronic gout.

46
Q

what is arthrotec and a consideration with this

A

arthrotec contains diclofenac and misoprostol (since this s protective of the stomach)
BUT! this will induce abortion so need to know if pregnant or trying to get pregnant

47
Q

what are the two ways that drugs to treat migraines will help with them

A

medications used to treat acute pain,

medications used to prevent migraine headaches from occurring.

48
Q

how should we think of a migraine

A

a neurovascular headache