- 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

- 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

- 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

- 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

- 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

- 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

- 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

- 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

- 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

- 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

- 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

- 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

- 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

- 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

- 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

- 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)

- 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

NSAIDs/Gout/RA/Migraine Flashcards by Blair Tilkens

aspirin

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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indomethacin

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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ketorolac

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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naproxen

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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oxaprozin

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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piroxicam

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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sulindac

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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celecoxib

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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etoricoxib

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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meloxicam

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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acetaminophen

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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salicylic acid

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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ibuprofen

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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capsaicin

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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NSAID interactions

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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acute gout tx

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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colchicin

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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allopurinol

febuxostat

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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

probenecid

sulfinpyrazone

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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

Treatment of RA

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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

NSAIDs for RA

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

methotrexate

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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

cyclosporine

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synthetic DMARD
polypeptide antibiotic
MOA: inhibit IL-1 and IL-2 receptor production

cyclophosphamide

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

azathioprine

- 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

leflunomide

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

chloroquine | hydroxychlorine

- synthetic DMARD - anti-malarial agent - MOA: anti-inflammatory action of drugs in RA unclear

aurothigluclose | auranofin

- synthetic DMARD - gold compounds - MOA: alter morphology and functional capabilities of human macrophages

sulfasalazine

- synthetic DMARD | - IgA and IgM rheumatoid factor production increased

etanercept

- biologic DMARD - anti-TNF agent - MOA: cytokine receptor fusion protein

infliximab

- biologic DMARD - anti-TNF agent - MOA: anti-TNF chimeric monoclonal antibody

anakinra

- biologic DMARD - IL-1 inhibitor - MOA: IL-1 cytokine receptor decoy

propranolol | metoprolol

- 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

amitriptyline

- preventive therapy of migraine - antidepressant - adverse effects: drowsiness

valproic acid | topiramate

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

flunarizine

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

verapamil

- preventative therapy of migraine - Ca2+ channel blocker - adverse effects: constipation, leg swelling, atrioventricular conduction distrubances

fluoxetine

- preventive therapy of migraine - selective serotonin-reuptake inhibitor - adverse effect: anxiety, insomnia

NSAIDs for migraines

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

meperidine butorphanol oxycodone hydromorphone

- 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

metoclopramide chlorpromazine prochlorperazine

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

ergotamine | dihydroergotamine

- 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

sumatriptan | zolmitriptan

- 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)

NSAIDs/Gout/RA/Migraine Flashcards

(43 cards)