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Pharma 2nd semester > B.28.NSAID's, except acetylsalicylic acid. gout+pain > Flashcards

B.28.NSAID's, except acetylsalicylic acid. gout+pain Flashcards

1
Q

list the non-selective NSAID’s

A 
Ibuprofen
Indomethacin 
Naproxen 
Diclofenac
Metamizole
Ketoprofen
Phenylbutazone 
Meloxicam
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2
Q

what are the contraindications for NSAID’s?

A 
GI bleeding 
allergy, asthma, angioedema 
impaired renal function 
congestive heart failure (COX- 2 inhibition ↑ effect)
pregnancy (specifically 3rd trimester)
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3
Q

what are the uses of Ibuprofen?

A

analgesic in children

induction of ductus arteriosus closure

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4
Q

what is the recommended dose for Ibuprofen?

A

child :5mg/kg

adult: 400mg
max. 2400 mg per day

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5
Q

what is the uses of Indomethacin?

A

1st line agent for acute gout attack

induction of ductus arteriosus closure

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6
Q

what are the side effects of Indomethacin?

A
  1. bone marrow suppression–>thrombocytopenia, agranulocytosis
  2. aplastic anemia

*rarely used for inflammation

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7
Q

when do we give Naproxen?

A 
menstrual cramps (management of dysmenorrhea)--> uterine relaxation 
control of acute gout
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8
Q

how is diclofenac given?

A

topical or oral

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9
Q

what are the functions of diclofenac?

A
  1. accumulates in synovial fluid–> used for musculoskeletal pain (back pain, disc herniation, osteoarthritis)
  2. gastroprotective- releases NO
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10
Q

what is risk of taking diclofenac?

A

prothrombotic risk

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11
Q

which NSAID causes hematotoxicity (granulocytosis)?

A

Metamizole (אופטלגין)

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12
Q

what is the function of ketoprofen?

A

inhibit LOX enzyme (↓ leukotrienes)

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13
Q

what is Phenylbutazone?

A

pyrazole derivative

potent anti-inflammatory effect

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14
Q

a severe side effect of Phenylbutazone

A

aplastic anemia

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15
Q

what is the inhibitory effect of Meloxicam?

A

COX-2>COX-1

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16
Q

other SE of NSAID’s

A
  1. in combination with ACE inhibitors–> renal papillary necrosis
  2. ↑ lithium concentrations
  3. hyperkalemia
  4. GI bleeding
  5. ↑BP
  6. ↓GFR
17
Q

What is Celecoxib

A

selective, reversible inhibition of COX-2 enzyme

18
Q

what are the functions of Celecoxib?

A

analgesic
anti-pyretic
anti-inflammatory

19
Q

what are the adverse effects of Celecoxib

A

GI irritation (milder effect compared to the non-selective)
renal damage
prothrombotic effect
sulfonamide hypersensitivity

20
Q

at what doses are acetaminophen safe?

A

<4g/day (adult)

21
Q

what is the #1 cause of acute liver failure in western countries?

A

Acetaminophen

22
Q

management of acetaminophen toxicity

A

N-acetylcysteine

*within 12 hours of overdose

23
Q

indications for Acetaminophen (Paracetamol)

A
  1. analgesic and antipyretic effect (inhibits cyclooxygenases in the CNS)
  2. aspirin substitute
  3. osteoarthritis and RA–> slight anti-inflammatory effect (no COX inhibition in the periphery)

NO anti-platelet effects

24
Q

what drug for pain can be given to pregnant women?

A

acetaminophen

*NSAID’s shouldn’t be given!!

25
Q

list the agents used for acute gout attack

A
  1. NSAID’s: indomethacin, Naproxen
  2. Corticosteroids: prednisone
  3. microtubule assembly inhibitors: colchicine
26
Q

how is colchicine given?

A

oral or parenteral

27
Q

what is the mechanism of colchicine (as a microtubule assembly inhibitor)?

A

bind to tubulin–> altered microtubular polymerization–> LTB₄ ↓–> altered leukocyte and granulocyte migration

28
Q

what agent has a more potent effect- indomethacin or Naproxen

A

indomethacin

29
Q

when do we give prednisone in acute gout attacks?

A

when NSAID’S are contraindicated

30
Q

how is prednisone given for acute gout?

A

intra-articular injection

oral (up to 5 days course treatment)

31
Q

what are the indications of colchicine other than acute gout

A

chronic gout-low doses
familial Mediterranean fever
management of pericardial diseases (pericarditis, pericardial effusion)

32
Q

side effects of colchicine

A

acute: severe diarrhea, GI pain

longer use: hematuria, alopecia, myelosuppression gastritis, peripheral neuropathy

33
Q

what are the agents used for chronic gout?

A
  1. Xanthine oxidase inhibitors: Allopurinol

2. recombinant urate oxidase: Rasburicase

34
Q

what are the indications for giving allopurinol and Rasburicase?

A

chronic gout
adjunct to cancer chemotherapy and radiotherapy
(‘tumor lysis syndrome’ may precipitate gout attack)

35
Q

side effects of allopurinol

A

GI irritation
hypersensitivity reaction, SJS syndrome
bone marrow suppression

36
Q

what are the side effects of Rasburicase?

A

anaphylactic reaction

methemoglobinemia in patients with G6PD

37
Q

allopurinol inhibits the metabolism of..

A

6-MP

38
Q

What is the mechanism of allopurinol?

A

inhibit xanthine oxidase–> ↓ purine metabolism –> serum uric acid ↓

39
Q

what is the mechanism of Rasburicase

A

it’s a urate oxidase enzyme that catalyzes the metabolism of uric acid to allantoin–> ↓ serum uric acid

Pharma 2nd semester (49 decks)

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