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Pharmacology > NSAIDs > Flashcards

NSAIDs Flashcards

1
Q

NSAIDs - MoA

A

Inhibition of prostaglandin synthesis by competitive cyclooxygenase (COX) inhibition

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2
Q

NSAIDs - Clinical use

A 
Low dose: mild-moderate pain, antipyretic 
Higher doses: inflammation. 
Postop pain (often combined with opioid) 
Chronic pain
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3
Q

NSAIDs - Contraindications

A

Contraind: previous severe hypersensitivity to salicylates (cross-sensitivity)

Generally not recommended for second half of pregnancy

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4
Q

NSAIDs - Adverse effects

A 
GI bleeding, Peptic ulcers
Renal and hepatic dysfunction. 
Lithium toxicity. 
Hyperkalemia 
Platelet inhibition 
Premature closure of ductus arteriosus
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5
Q

NSAIDs - Interactions

A

Inhibit renal excretion of lithium.

Reduced clearance of aminoglycosides & methotrexates.

Interfere with antihypertensive effect of: diuretics, β-adrenoceptor antagonists, angiotensin inhibitors & others.

Potassium-sparing diuretics: hyperkalemia

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6
Q

Salicylates - MoA

A

Nonspecific inhibition of COX

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7
Q

Salicylates - Clinical use

A

Pain, fever, inflammation

Prophylaxis for MI, stroke, thromboembolic disorders

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8
Q

Salicylates - Contraindication

A

Avoid in children: Reye syndrome (in virus infected children).

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9
Q

Salicylates - Overdose treatment

A

Vomiting
IV sodium bicarbonate (alkalization of the urine, increases ionization and elimination)
Fluids, electrolytes

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10
Q

Salicylates - Adverse effects

A

Reye syndrome

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11
Q

Aspirin - MoA

A

Forms covalent, irreversible inhibition of COX in platelets

Nonspecific inhibition of COX in peripheral tissues and CNS

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12
Q

Aspirin - Clinical use

A

Analgesic
Antipyretic
Anti-inflammatory

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13
Q

Aspirin - Special considerations

A

Longer thromboxane effect than other salicylates.

Inhibits platelet aggregation

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14
Q

Aspirin - Adverse

A

Aspirin toxicity
High dose: Tinnitus (early sign of salicylate toxicity)

Hyperventilation
Fever, dehydration, severe metabolic acidosis
If not treated: Shock, coma, organ system failure, death

Hypoprothrombinemia – impairment of hemostatis and bleeding

Hypersensitivity – anaphylaxis (mostly pt with asthma, nasal polyps, chronic urticaria)

Symptoms of aspirin intolerance: vasomotor rhinitis, angioedema, urticaria

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15
Q

Aspirin - Interactions and contraindication

A

Adm with antacids: slows absorption rate

Contraindication: Persons who have has severe hypersensitivity reaction to aspirin or another salicylate should not be treated with another type of NSAID (cross-sensitivity)

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16
Q

Ibuprofen - MoA

A

Reversible and nonselective inhibition of COX

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17
Q

Ibuprofen, Ketoprofen, Naproxen - Clinical use

A

Analgesic, antipyretic and anti-inflammatory effects
Low dose: mild pain and inflammation
Higher dose: arthritis

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18
Q

Ibuprofen - Special considerations

A

Combo with H2 receptor antagonist famotidine for RA and OA (less GI ulcers)

Half-life: 2h

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19
Q

Ibuprofen - Adverse effects

A

GI irritation, nausea, dyspepsia, bleeding.

Long-term: PUD, Hepatotoxicity, renal toxicity

Failure of ingesting adequate fluid: acute renal failure

20
Q

Naproxen - Special considerations

A

Combo with esomeprazole: arthritis, reduces risk of ulcers

Longer halflife (14h)

21
Q

Acetaminophen - MoA

A

COX3 inhibitor

22
Q

Acetaminophen - Clincal use

A

Mild fever and pain
Mild arthritis
Analgesic and antipyretic effects via inhibitor of COX

23
Q

Acetaminophen - Special considerations

A

Safe for children with viral infection

24
Q

Acetaminophen - Overdose treatment

A

Acetylcysteine

25
Q

Acetaminophen - Adverse effects

A

Fewer GI problems

High dose: hepatic necrosis, hepatotoxicity

Long-term use: Increased risk of renal dysfunction

26
Q

Acetaminophen - Interactions

A

Small amount converted by CYT P-450 to potentially hepatotoxic quinone intermediate

Patients at risk for hepatotoxicity (f.ex. overdose): given acetylcysteine (conjugates quinone and renders it harmless)

27
Q

Indomethacin - Clinical use

A

Reserved for moderate/severe inflammation disorders

Patent ductus arteriosus (indomethacin inhibit synthesis of prostaglandins and causes the closure)

28
Q

Indomethacin - Adverse effects

A

Nephrotoxicity with triamterene
Highest incidence of GI and CNS side effects
Hematologic toxicity

29
Q

Indomethacin - Interaction

A

Reduces natriuretic effect of diuretics.

With triamterene: nephrotoxicity

30
Q

Sulindac - MoA

A

Prodrug converted to active sulfide metabolite. Parent compound sulindac sulfoxide is inactive in COX inhibition

31
Q

Sulindac - Clinical use

A

RA

Adenomas in polyp disease

32
Q

Ketorolac - Clinical use

A

Analgesic activity
Post-op moderate pain in dentistry
Allergic conjunctivitis
Post-op ocular infl.

33
Q

Ketorolac - Special considerations and Caution

A 
Potent analgesic (comparable to morphine) Ophthalmic solution of ocular inflammation. 
Treatment limited to 5 days

Caution in patients with renal/hepatic disease

34
Q

Ketorolac - Adverse effects

A

Fewer GI and CNS effects than opioids.
Hematologic toxicity
Increased risk of renal or hepatic impairment

35
Q

Piroxicam - Clinical use

A

Anti-inflammatory

Chronic RA treatment

36
Q

Piroxicam - Special considerations

A

Long half-life (50h)

37
Q

Nabumetone - MoA

A

Weak COX inhibitory activity in vitro, but converted to active metabolites with potent inhibition in vivo

38
Q

Etodolac, meloxicam - MoA

A

More selective for COX-2 than typical NSAIDs

39
Q

Diclofenac - Clinical use

A

Osteoarthritis

40
Q

Selective COX-2 inhibitors

A

Celecoxib
Rofecoxib (Removed from market)
Valdecoxib (Removed from market)

41
Q

Selective COX-2 inhibitors - MoA

A

Potent anti-inflammatory action

42
Q

Selective COX-2 inhibitors - Special

A

Decreased risk of cancer (esp colon cancer)

43
Q

Celecoxib - Clinical use

A

Rheumatoid arthritis

Osteoarthritis

44
Q

Celecoxib - MoA

A

Selective COX-2 inhibition

Analgesic
antipyretic
antiinflammatory

45
Q

Celecoxib - Special

A

Does not inhibit platelet aggregation (platelet contain only COX-1)

46
Q

Celecoxib - Adverse effects

A

Increased risk of cardiovascular events

Low incidence: diarrhea, dyspepsia, abd pain

47
Q

Celecoxib - Interactions

A

Metabolized by CYT P-450

Metabolism is inhibited and increased serum levels by fluconazole, fluvastatin, zafirlukast.

Pharmacology (55 decks)

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