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Phar 507 > Pharmacology of NSAIDs > Flashcards

Pharmacology of NSAIDs Flashcards

1
Q

What are the properties of NSAIDS

A

Analgesisa, antipyresis, anti-inflammatory

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2
Q

What type of prostaglandins are produced by COX-1

A

support platelets and protect the stomach

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3
Q

Which COX enzymes are active under healthy conditions, expressed in inflammatory cells

A

COX-1 (constitutive), COX-2 (inducible)

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4
Q

Which COX-2 selective enzyme inhibitor reduces hormones causing inflammation and pain in the body, the biggest drawback

A

Celecoxib, increase cardiovascular thrombotic events

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5
Q

T/F: Ibuprofen is COX-1 selective

A

False: Ibuprofen is nonselective for COX-1 and COX-2

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6
Q

What is the product of the COX-1 isoform and what are the functions

A

Thromboxane (TXA2): vasoconstriction and platelet aggregation (thrombosis)

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7
Q

What is the product of the COX-2 isoform and what are the functions

A

Prostacyclin (PGI2): vasodilator and inhibits platelet aggegation

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8
Q

How do selective COX-2 inhibitors increase cardiac events

A

Homeostatic balance between TXA2 and PGI2 shifts to cause more thrombosis

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9
Q

T/F: NSAID anti-inflammatory effects require higher doses compared with analgesic doses

A

True

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10
Q

What are characteristics that NSAIDs have that opiates don’t

A

Ceiling effect, anti-inflammation, antiplatelet effect

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11
Q

In peripheral pain what are the steps prostaglandins make to increase pain

A

Arachidonic acid is released during tissue damage, arachidonic acid is then metabolized to prostaglandin, prostaglandin blocks the potassium efflux released from nociceptors following damage resulting in additional depolarization making the nociceptor more sensitive

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12
Q

How do NSAIDS cause analgesia

A

Reduces sensitization of nociceptive nerve ending to mediators like bradykinin and histamine

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13
Q

Which prostaglandin increases body temperature, how

A

PGE2, Receptors on neurons in hypothalamus recognize PGE2 and the body temperature resets to a few degrees higher than normal

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14
Q

What are the effects NSIADs have on fever

A

Innhibit PGE2 synthesis at thermoregulatory centers in the hypothalamus leading to body temperature resetting to normal, sweating, vasodilation

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15
Q

T/F: NSAIDs taken when a patient has normal body temperature casues them to be colder

A

False: NSAIDs has little effect on “normal” body temperature

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16
Q

Which prostaglandins csensitize skin pain receptors

A

PGE2 and PGI2

17
Q

How do prostaglandins cause inflammation

A

Direct vasodilation and potentiation of other vasodilatiors (bradykinin and histamine) increasing blood flow, potentiation of effects of bradykinin and histamine on vascular permeability lead to edema and swelling

18
Q

Which NSAID is most effective as antifinflammaotry and is used to close the ductus arteriosus

A

Indomethacin

19
Q

What are the propionic acids

A

Ibuprofen, ketoprofen, and naproxen

20
Q

What are the acetic acid derivatives

A

Indomethcin, Etodolac, ketorolac, sulindac, diclofenac

21
Q

What are the fenmates

A

Mefenamic acid and meclofenamic acid

22
Q

What are the oxicams

A

Meloxicam and piroxicam

23
Q

What is the non acidic compound NSAID

A

Nabumetone

24
Q

Which NSAIDs are most COX-2 selective

A

Etodolac and Meloxicam

25
Q

What are the topical NSIADS

A

Diclofenac and ketoprofen

26
Q

T/F: Mefenamic is needs no dose reduction required for renal impairment

A

True

27
Q

What are the formulations for ketorolac, when is it used, cautious tip

A

oral, IV and IM/ postoperations for analgesia/ causes ulcers more frequently so use no more than 5 days

28
Q

Which NSAID is once daily dosing

A

Piroxicam

29
Q

T/F: Selective COX-2 inhibitors are useful in patient unable to tolerate conventional NSAIDs

A

True

30
Q

What is the active metabolite of acetaminophen (paracetamol)

A

Phenacetin

31
Q

What are the proposed ways APAP works

A

inhibits COX-3, work in the CNS

32
Q

What are properties APAP has, normal dose

A

Analgesic and antipyretic/ 2-4 grams per day (no more than 4)

33
Q

Why does acetaminopehn cause toxicity

A

NAPQI binds with hepatocytes leading to liver injury

34
Q

What is the most common cause of death ffollowing an aspirin oversoe

A

Cadiopulmonary arrest usually due to pulmonary edema (respiratory and renal depression)

35
Q

Which NSAID is associated with ringing in the ear, which is the safest non-selective NSAID for people iwth CAD

A

Aspirin, Naproxen

Phar 507 (33 decks)

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