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Pharmacology > NSAIDs/Gout/RA/Migraine > Flashcards

NSAIDs/Gout/RA/Migraine Flashcards

1
Q

aspirin

A
  • NSAID, non-selective, prostaglandin synthesis inhibitor
  • MOA: reversible COX 1 & 2 inhibitor–> inhibit inflammation, pain, and fever
  • uses: pain, fever, inflammation, antithrombotic, cramping, colorectal cancer prevention, Alzheimer’s disease, MI/stroke, anticoagulant
  • adverse effects: GI upset (Cox-1 inhibition), GI irritation (inhibition of PGs), platelet inhibition, hepatic and renal toxicity, hypersensitivity, tinnitus, Reye’s syndrome, drug interactions
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2
Q

indomethacin

A
  • NSAID, acetic acid, prostaglandin synthesis inhibitor
  • MOA: non-selective COX inhibitor
  • use: pain, fever, inflammation, antithrombotic, menstrual cramping, MI/stroke, prevention of colorectal cancer, Alzheimer’s, closure of patent ductus arteriosus
  • primary NSAID for gout and ankylosing spondylitis
  • adverse effects: GI upset (Cox-1 inhibition), GI irritation (inhibition of PGs), platelet inhibition, hepatic and renal toxicity, hypersensitivity
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3
Q

ketorolac

A
  • NSAID, acetic acid, prostaglandin synthesis inhibitor
  • MOA: non-selective Cox inhibitor
  • use: pain, fever, inflammation, antithrombotic, menstrual cramping, MI/stroke, prevention of colorectal cancer, Alzheimer’s, closure of patent ductus arteriosus
  • adverse effects: GI upset (Cox-1 inhibition), GI irritation (inhibition of PGs), platelet inhibition, hepatic and renal toxicity, hypersensitivity
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4
Q

naproxen

A
  • NSAID, prostaglandin synthesis inhibitor, propionic acid
  • MOA: non-selective COX inhibitor
  • use: pain, fever, inflammation, antithrombotic, menstrual cramping, MI/stroke, prevention of colorectal cancer, Alzheimer’s, closure of patent ductus arteriosus
  • used for gout
  • adverse effects: GI upset (Cox-1 inhibition), GI irritation (inhibition of PGs), platelet inhibition, hepatic and renal toxicity, hypersensitivity
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5
Q

oxaprozin

A
  • NSAID
  • MOA: non-selective COX inhibitor
  • use: pain, fever, inflammation, antithrombotic, menstrual cramping, MI/stroke, prevention of colorectal cancer, Alzheimer’s, closure of patent ductus arteriosus
  • adverse effects: GI upset (Cox-1 inhibition), GI irritation (inhibition of PGs), platelet inhibition, hepatic and renal toxicity, hypersensitivity
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6
Q

piroxicam

A
  • NSAID, prostaglandin synthesis inhibitor, oxicam
  • MOA: non-selective COX inhibitor
  • use: pain, fever, inflammation, antithrombotic, menstrual cramping, MI/stroke, prevention of colorectal cancer, Alzheimer’s, closure of patent ductus arteriosus
  • adverse effects: GI upset (Cox-1 inhibition), GI irritation (inhibition of PGs), platelet inhibition, hepatic and renal toxicity, hypersensitivity
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7
Q

sulindac

A
  • NSAID
  • MOA: non-selective COX inhibitor
  • use: pain, fever, inflammation, antithrombotic, menstrual cramping, MI/stroke, prevention of colorectal cancer, Alzheimer’s, closure of patent ductus arteriosus
  • used for gout
  • adverse effects: GI upset (Cox-1 inhibition), GI irritation (inhibition of PGs), platelet inhibition, hepatic and renal toxicity, hypersensitivity
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8
Q

celecoxib

A
  • NSAID
  • MOA: Cox-2 selective inhibitor
  • use: RA and osteoarthritis, analgesic, antipyretic, anti-inflammatory
  • less GI adverse effects
  • No impact on platelet aggregation
  • adverse effects: incidence of CV thrombotic events
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9
Q

etoricoxib

A
  • NSAID
  • MOA: cox-2 selective inhibitor
  • use: analgesic, antipyretic, anti-inflammatory
  • less GI adverse effects
  • No impact on platelet aggregation
  • adverse effects: incidence of CV thrombotic events
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10
Q

meloxicam

A
  • NSAID
  • MOA: prostaglandin synthesis inhibitor, Cox-2 selective inhibitor
  • use: analgesic, antipyretic, anti-inflammatory
  • less GI adverse effects
  • No impact on platelet aggregation
  • adverse effects: incidence of CV thrombotic events
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11
Q

acetaminophen

A
  • no anti-inflammatory effect, inhibition of platelet aggregation, or GI tract irritation
  • actions: angalgesic, antipyretic
  • MOA: unclear
  • use: mild-to-moderate pain, post-op pain, children and elderly
  • adverse effects: hepatotoxicity at high doses w/ alcohol abuse
  • narrow therapeutic index with liver necrosis
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12
Q

salicylic acid

A
  • NSAID, prostaglandin synthesis inhibitor
  • MOA: reversible COX 1 & 2 inhibitor–> inhibit inflammation, pain, and fever
  • uses: pain, fever, inflammation, antithrombotic, cramping, colorectal cancer prevention, Alzheimer’s disease, MI/stroke, anticoagulant
  • adverse effects: GI upset (Cox-1 inhibition), GI irritation (inhibition of PGs), platelet inhibition, hepatic and renal toxicity, hypersensitivity, tinnitus, Reye’s syndrome, drug interactions
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13
Q

ibuprofen

A
  • NSAID, propionic acid
  • MOA: non-selective Cox inhibitor, prostaglandin synthesis inhibitor
  • use: pain, fever, inflammation, antithrombotic, menstrual cramping, MI/stroke, prevention of colorectal cancer, Alzheimer’s, closure of patent ductus arteriosus
  • used for gout
  • adverse effects: GI upset (Cox-1 inhibition), GI irritation (inhibition of PGs), platelet inhibition, hepatic and renal toxicity, hypersensitivity
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14
Q

capsaicin

A
  • active spice substance in various chili peppers
  • MOA: bind vanilloid receptors heat activated Ca2+ channels on afferent nociceptive neurons–> release of Substance P–> depletes and prevents reaccumulation of Substance P
  • use: topically for RA, osteoarthritis, neuralgia, shingles, diabetic neuropathy
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15
Q

NSAID interactions

A
  • displacement of protein binding–> increase free fraction of drug
  • diuretics: attenuate effects via action on Na+ transport
  • anticoagulants: antithrombotic effect
  • GI effects (upset, ulcer, bleeding): anticoagulants (bleeding risk), enhanced effects of alcohol and glucocorticoids
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16
Q

acute gout tx

A
  • NSAIDs: idomethacin, colchicine, ibuprofen, naproxen, or sulindac
  • NOT aspirin–>renal retention of uric acid
  • corticosteroids (fail w/ NSAID/colchicine)
  • intra-articular steroid injection (1 or 2 joints affected or elderly)
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17
Q

colchicin

A
  • primary tx for acute gout before idomethacin
  • reduce pain and inflammation w/o altering metabolism or excretion of uric acid
  • inhibit leukocyte migration and phagocytosis–> anti-inflammatory
  • adverse effects: severe diarrhea, nausea, vomiting
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18
Q

allopurinol

febuxostat

A
  • gout prophylaxis
  • MOA: inhibit xanthine oxidase–> block conversion of xanthin to uric acid–> lower uric acid conc.
  • use: agents for periods b/t acute gout attacks
  • febuxostat more selective and well tolerated
19
Q

probenecid

sulfinpyrazone

A
  • gout prophylaxis
  • uricosuric drugs
  • MOA: increase renal clearance of uric acid by inhibiting tubular absorption–> decrease body pool of urate
  • adverse effects: GI and kidney stone
  • not effective in acute attacks of gout
20
Q

Treatment of RA

A
  • NSAIDs: 1st line drugs-reduce inflammation and pain
  • glucocorticoids: reduce inflammation, dramatic improvement in RA
  • disease-modifying anti-rheumatic drugs (DMARDs): reduc inflammation, improve symptoms, slow bone damage
21
Q

NSAIDs for RA

A

aspirin, acetaminophen, indomehacin, ibuprofen, naproxen, sulindac, celecoxib, etoricoxib, meloxicam, valdecoxib

22
Q

methotrexate

A
  • synthetic DMARD
  • antimetabolite and antifolate agent
  • MOA: inhibit AICAR transformylase–> increase extracellular adenosine–> inhibit T-cell actiavtion
  • use: 1st line DMARD for treatment of RA
  • adverse effects: myelosuppresion
23
Q

cyclosporine

A
  • synthetic DMARD
  • polypeptide antibiotic
  • MOA: inhibit IL-1 and IL-2 receptor production
24
Q

cyclophosphamide

A
  • synthetic DMARD
  • cytostatic/cytotoxic agent
  • MOA: cytotoxic cross-link DNA to prevent cell replication
25
Q

azathioprine

A
  • synthetic DMARD
  • cytostatic/cytotoxic agent
  • MOA: interferes w/ nucleic acid metabolism/synthesis–> inhibit cell proliferation–> suppress B and T cell function, Ig production, and IL-2 secretion
26
Q

leflunomide

A
  • synthetic DMARD
  • MOA: inhibits ribonucleotid synthesis–> cell cycle arrest
  • 1st agent for RA for symptomatic improvement and retardation of structural joint damage
27
Q

chloroquine

hydroxychlorine

A
  • synthetic DMARD
  • anti-malarial agent
  • MOA: anti-inflammatory action of drugs in RA unclear
28
Q

aurothigluclose

auranofin

A
  • synthetic DMARD
  • gold compounds
  • MOA: alter morphology and functional capabilities of human macrophages
29
Q

sulfasalazine

A
  • synthetic DMARD

- IgA and IgM rheumatoid factor production increased

30
Q

etanercept

A
  • biologic DMARD
  • anti-TNF agent
  • MOA: cytokine receptor fusion protein
31
Q

infliximab

A
  • biologic DMARD
  • anti-TNF agent
  • MOA: anti-TNF chimeric monoclonal antibody
32
Q

anakinra

A
  • biologic DMARD
  • IL-1 inhibitor
  • MOA: IL-1 cytokine receptor decoy
33
Q

propranolol

metoprolol

A
  • beta-adrenergic receptor antagonists
  • preventive therapy of migraine
  • MOA: beta 1 and beta 2 antagonist (pro), beta 1 antagonist (met)
  • adverse effects: reduced energy, postural symptoms
  • contraindicated in pts w/ asthma
34
Q

amitriptyline

A
  • preventive therapy of migraine
  • antidepressant
  • adverse effects: drowsiness
35
Q

valproic acid

topiramate

A
  • preventive therapy of migraine
  • anticonvulsants
  • adverse effects: drowsiness, weight gain, tremor, hair loss, hemotological and liver abnormalities, teratogenicity
36
Q

flunarizine

A
  • preventative therapy of migraine
  • Ca-channel blocker
  • adverse effects: tiredness, weight gain, depression, parkinsonism
37
Q

verapamil

A
  • preventative therapy of migraine
  • Ca2+ channel blocker
  • adverse effects: constipation, leg swelling, atrioventricular conduction distrubances
38
Q

fluoxetine

A
  • preventive therapy of migraine
  • selective serotonin-reuptake inhibitor
  • adverse effect: anxiety, insomnia
39
Q

NSAIDs for migraines

A
  • acute migraine attack
  • aspirin, naproxen, ibuprofen, acetaminophen
  • avoid overuse: limit drug tx to 2-3 days
40
Q

meperidine
butorphanol
oxycodone
hydromorphone

A
  • tx of acute migraine attack
  • opiate analgesics
  • risk of dependence and tolerance (not used much)
  • adverse effects: rebound headaches, dizziness, nausea, vomiting, impaired cognitive function
41
Q

metoclopramide
chlorpromazine
prochlorperazine

A
  • acute migraine attacks
  • antiemetics
  • adjunctive therapy to combat nausea and vomiting
  • MOA: dopamine receptor antagonist (D2)
  • metoclopramide also weak 5-HT3 receptor antagonist
42
Q

ergotamine

dihydroergotamine

A
  • acute migraine attacks
  • ergot derivatives
  • MOA: stimulation of alpha-adrenergic and 5-HT receptors–> vasoconstriction
  • dural and cerebral vessels very sensitive
  • cerebral vasoconstriction by agonist effects on neuronal or vascular 5-HT1D receptors
  • effective, low cost, high experience
  • adverse effects: GI disturbance, potent and sustained vasoconstrictor effect
43
Q

sumatriptan

zolmitriptan

A
  • acute migraine attack
  • the “triptans”
  • MOA: selective 5-HT1D and 5-HT1B receptor agonists–> cranial/dural vasoconstriction
  • higher cost, resricted on use in CV disease
  • adverse effects: mild, nausea, dizziness, drowsiness, muscle weakness
  • safety: safe, some angina, MI rare
  • tolerability: irritating adverse effects (tingling, warmth in head, neck, chest, and limbs)

Pharmacology (34 decks)

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