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Pharmacology > 03 Inflammation and anti-inflammatory drugs > Flashcards

03 Inflammation and anti-inflammatory drugs Flashcards

1
Q

3.01 NSAIDs

Ibuprofen - actions

A

reduces inflammation
analgesic for inflammatory pain
antipyretic

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2
Q

3.01 NSAIDs

Ibuprofen - MOA

A

reversible inhibition of COX-1
weak inhibition of COX-2

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3
Q

3.01 NSAIDs

Ibuprofen - abs/distrib/elim

A

given orally
half-life 2h

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4
Q

3.01 NSAIDs

Ibuprofen - clinical use

A

inflammatory conditions (e.g. rheumatoid disease, osteoarthritis, musculoskeletal disorders)
dysmenorrhoea

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5
Q

3.01 NSAIDs

Ibuprofen - adverse effects

A

GIT disturbances, including gastric bleeding
headache
dizziness less commonly
allergic reactions occasionally
renal toxicity rarely

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6
Q

3.01 NSAIDs

Ibuprofen - special points

A

increased adverse effects if combined with other NSAIDs
used to close patent ductus arteriosus

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7
Q

3.01 NSAIDs

Ibuprofen - similar drugs

A

diclofenac (moderate potency, half-life 1-2h)
ketoprofen (half-life ~2h)
naproxen (more potent, half-life 10-14h)
ketorolac (half-life 4-10h, COX-1 selective)
piroxicam (half-life 57h, GIT toxicity common, COX non-selective)

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8
Q

3.02 NSAIDs

Aspirin - actions

A

reduces inflammation
analgesic for inflammatory pain
antipyretic
inhibits platelet aggregation

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9
Q

3.02 NSAIDs

Aspirin - MOA

A

irreversible acetylation of cyclooxygenases
weakly COX-1 selective

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10
Q

3.02 NSAIDs

Aspirin - abs/distrib/elim

A

given orally, but also available as suppository
rapid hydrolysis (30min) to salicylate but effects last longer because the COX has been inactivated and new enzyme must be produced

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11
Q

3.02 NSAIDs

Aspirin - clinical use

A

antithrombotic in MI (main use)
other NSAIDs are preferred for anti-inflammatory action and analgesia in musculoskeletal conditions

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12
Q

3.02 NSAIDs

Aspirin - adverse effects

A

GIT disturbances, especially gastric bleeding
in high dosage can cause ‘salicylism’ (tinnitus, vertigo, reduced hearing)
allergic reactions occasionally
renal toxicity rarely
can cause the potentially fatal Reye’s syndrome (encephalopathy and liver disorder) in children after a viral infection

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13
Q

3.02 NSAIDs

Aspirin - special points

A

should not be used in children
can cause increased effect of warfarin resulting in bleeding
should not be used for gout because it reduces urate excretion and interferes with the action of uricosuric agents

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14
Q

3.03 NSAIDs

Paracetamol - actions

A

analgesic
antipyretic
has little anti-inflammatory action

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15
Q

3.03 NSAIDs

Paracetamol - MOA

A

inhibition of COX-1, COX-2 and also the recently identified COX-3 which occurs predominantly in the CNS

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16
Q

3.03 NSAIDs

Paracetamol - abs/distrib/elim

A

given orally
half-life 2-4h
inactivated in the liver

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17
Q

3.03 NSAIDs

Paracetamol - clinical use

A

mild to moderate pain, especially headache
it is the most commonly used NSAID

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18
Q

3.03 NSAIDs

Paracetamol - adverse effects

A

few and uncommon with therapeutic doses
toxic doses cause firstly nausea and vomiting and then 24h later potentially fatal liver toxicity

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19
Q

3.04 COX-2 INHIBITORS

Celecoxib, etoricoxib, parecoxib - actions

A

analgesic, antipyretic and anti-inflammatory actions
no antiplatelet action

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20
Q

3.04 COX-2 INHIBITORS

Celecoxib, etoricoxib, parecoxib - MOA

A

selective inhibition of COX-2 - the enzyme that is induced in areas of inflammation
celecoxib is 10-20 × more active on COX-2 than COX-1 - the constitutive enzyme that generates physiologically important prostaglandins

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21
Q

3.04 COX-2 INHIBITORS

Celecoxib, etoricoxib, parecoxib - abs/distrib/elim

A

given orally
half-life ~11h
inactivated in the liver

22
Q

3.04 COX-2 INHIBITORS

Celecoxib, etoricoxib, parecoxib - clinical use

A

rheumatoid arthritis, osteoarthritis, ankylosing spondylitis
offered to patients for whom treatment with conventional NSAIDs would pose high probability of serious gastrointestional side effects - although they can still occur with COX-2 inhibitors (coxibs)

23
Q

3.04 COX-2 INHIBITORS

Celecoxib, etoricoxib, parecoxib - adverse effects

A

several coxibs have been withdrawn following claims of cardiovascular and other toxicity (renal and liver)
new-onset hypertension, fluid retention
celecoxib, etericoxib and parecoxib are currently available for clinical use in the United Kingdom

24
Q

3.05 DMARDs

Immunosuppressive disease-modifying anti-rheumatoid drug: methotrexate - actions

A

marked anti-inflammatory action in rheumatoid disease
cytotoxic in the larger doses used to treat cancer

25
Q

3.05 DMARDs

Immunosuppressive disease-modifying anti-rheumatoid drug: methotrexate - MOA

A

folate antagonist and thus interferes with thymidylate synthesis (which is essential for DNA synthesis)

26
Q

3.05 DMARDs

Immunosuppressive disease-modifying anti-rheumatoid drug: methotrexate - abs/distrib/elim

A

given orally
has active metabolite
both MTX and metabolite are poly-glutamated (PgMTX)
half-life 6-9h

27
Q

3.05 DMARDs

Immunosuppressive disease-modifying anti-rheumatoid drug: methotrexate - clinical use

A

drug of first choice for rheumatoid arthritis
used in psoriasis, ankylosing spondylitis, polymyositis and vasculitis
also an anti-cancer agent

28
Q

3.05 DMARDs

Immunosuppressive disease-modifying anti-rheumatoid drug: methotrexate - adverse effects

A

GIT disturbances
dose-related liver toxicity
bone marrow depression and pneumonitis can occur

29
Q

3.06 DMARDs

Immunosuppressive disease-modifying anti-rheumatoid drug: sulfasalazine - actions

A

produces remission of active rheumatoid arthritis
according to X-rays, disease progression is reduced

30
Q

3.06 DMARDs

Immunosuppressive disease-modifying anti-rheumatoid drug: sulfasalazine - MOA

A

in the colon, the salicylic acid moiety is released, absorbed and has anti-inflammatory action

31
Q

3.06 DMARDs

Immunosuppressive disease-modifying anti-rheumatoid drug: sulfasalazine - abs/distrib/elim

A

given orally
only ~15% is absorbed in the GIT
half-life 6-16h

32
Q

3.06 DMARDs

Immunosuppressive disease-modifying anti-rheumatoid drug: sulfasalazine - clinical use

A

rheumatoid arthritis, juvenile arthritis
inflammatory bowel disease

33
Q

3.06 DMARDs

Immunosuppressive disease-modifying anti-rheumatoid drug: sulfasalazine - adverse effects

A

nausea and vomiting, headaches, rashes
rarely bone marrow dyscrasias, liver dysfunction
about a third of patients discontinue the drug because of adverse effects

34
Q

3.07 DMARDs

Immunosuppressive disease-modifying anti-rheumatoid drug: leflunomide - actions

A

modifies the immune reaction underlying rheumatoid arthritis through an inhibitory action on activated T cells

35
Q

3.07 DMARDs

Immunosuppressive disease-modifying anti-rheumatoid drug: leflunomide - MOA

A

gives rise to a metabolite that inhibits dihydrooratate dehydrogenase
this results in inhibition of T cell proliferation and decreased production of autoantibodies by B cells

36
Q

3.07 DMARDs

Immunosuppressive disease-modifying anti-rheumatoid drug: leflunomide - abs/distrib/elim

A

absorbed orally
the metabolite undergoes enterohepatic cycling
half-life thus ~18 days

37
Q

3.07 DMARDs

Immunosuppressive disease-modifying anti-rheumatoid drug: leflunomide - clinical use

A

rheumatoid arthritis
particularly effective in combination with methotrexate

38
Q

3.07 DMARDs

Immunosuppressive disease-modifying anti-rheumatoid drug: leflunomide - adverse effects

A

~25% of patients get diarrhoea
increased BP, weight gain can occur
the long half-life can lead to cumulative toxicity

39
Q

3.08 URICOSURIC AGENTS

Allopurinol, febuxostat - actions

A

reduces uric acid concentration in the body

40
Q

3.08 URICOSURIC AGENTS

Allopurinol, febuxostat - MOA

A

inhibits xanthine oxidase and also the biotransformation of purines to xanthine

41
Q

3.08 URICOSURIC AGENTS

Allopurinol, febuxostat - abs/distrib/elim

A

given orally, well absorbed
converted to alloxanthine which has a half-life of ~18-30h and is the moiety that inhibits xanthine oxidase

42
Q

3.08 URICOSURIC AGENTS

Allopurinol, febuxostat - clinical use

A

to prevent episodes of gout

43
Q

3.08 URICOSURIC AGENTS

Allopurinol, febuxostat - adverse effects

A

GIT disturbances
rashes and blood dyscrasias can occur

44
Q

3.08 URICOSURIC AGENTS

Allopurinol, febuxostat - special points

A

allopurinol is not used to treat acute attacks of gout - these are treated with NSAIDs
allopurinol interferes with the metabolism of oral anticoagulants and can increase the effect of azathioprine and cyclophosphamide

45
Q

3.08 URICOSURIC AGENTS

Allopurinol, febuxostat - similar drugs

A

probenecid is similar in that it is also uricosuric but it acts by increasing uric acid excretion through an effect on the proximal tubule in the nephron - only used to prevent gouty attacks

46
Q

3.09 Antigout: colchicine - actions

A

it decreases the pain and inflammation of gouty arthritis

47
Q

3.09 Antigout: colchicine - MOA

A

inhibits migration of neutrophils into gouty joints by binding to tubulin and preventing its polymerisation into microtubules
neutrophils are reduced to moving with a ‘drunken walk’
it also decreases production of the chemokine leukotriene B4

48
Q

3.09 Antigout: colchicine - abs/distrib/elim

A

given orally, well absorbed
half-life 9h

49
Q

3.09 Antigout: colchicine - clinical use

A

to treat acute episodes of gout
also used in treatment of pericarditis

50
Q

3.09 Antigout: colchicine - adverse effects

A

diarrhoea, sometimes nausea and vomiting
blood dyscrasias can occur

51
Q

3.09 Antigout: colchicine - special points

A

it can increase the bone marrow depression caused by other drugs

Pharmacology (34 decks)

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