Cyclooxygenase inhibitors

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Author:
dbrattebo
ID:
96950
Filename:
Cyclooxygenase inhibitors
Updated:
2011-08-14 11:37:48
Tags:
pharm
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Description:
ch. 70
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  1. Nonsteroidal Anti-Inflammatory Drug (NSAID)

    Prototype: Aspirin
    • Nonsteroidal Anti-Inflammatory Drug(NSAID)Prototype: Aspirin
    • MECHANISM OF ACTION:
    • -irreversible inhibition of cyclooxygenase (COX-1 and COX-2)
    • -suppresses platelet aggregation
    • -decreases prostaglandin synthesis
    • -reduces inflammation, pain, and fever

    • USES:
    • -suppression of inflammation
    • -analgesia (pain reduction)
    • -reduction of fever in adults
    • -dysmenorrhea
    • -suppression of platelet aggregation to protect against MI and stroke
    • -prevention of colorectal cancer

    • ADVERSE EFFECTS:
    • -gastric distress (heartburn and nausea)
    • -GI bleeding, gastric ulceration and perforation
    • -not used in children b/c of the risk of Reye's syndrome
    • -fetal harm (prolongs labor, premature closing of the patent ductus)
    • -hypersensitivity in patients with allergies
    • -renal impairment
    • -bleeding
  2. First Generation - Nonaspirin NSAIDs

    Prototype: Ibuprofen (Advil, Motrin)

    Other NSAIDs:
    -Fenoprofen (Nalfon)
    -Flurbiprofen (Ansaid)
    -Ketoprofen
    -Naproxen (Aleve, Anaprox, Naprelan, Naprosyn)
    -Oxaprozin (Daypro)
    -Diclofenac (Voltaren, Cataflam) - risk of liver failure
    -Voltaren gel and Flector patch
    -Diclofenac plus Misoprostol (Arthrotec)
    -Diflunisal (Dolobid)
    -Etodolac
    -Indomethacin (Indocin)
    -Ketorolac (Toradol) - available IM or IV
    -Mefenamic acid (Ponstel)
    • MECHANISM OF ACTION:
    • -reversible inhibition of COX-1 and COX-2
    • -inhibits prostaglandin synthesis
    • -has anti-inflammatory, analgesic, and antipyretic actions

    • USES:
    • -fever
    • -pain
    • -arthritis
    • -dysmenorrhea
    • -closure of the ductus arteriosus in preterm infants

    • ADVERSE EFFECTS:
    • -bleeding
    • -gastric ulceration
    • -renal impairment
    • -cross-hypersensitivity with aspirin
    • -may precipitate Reye's syndrome
  3. Second Generation NSAID (COX-2 Inhibitor)

    Prototype: Celecoxib (Celebrex)
    • MECHANISM OF ACTION:
    • -selective inhibition of COX-2
    • -decreases prostaglandin synthesis at the site of injury
    • -reduces pain and inflammation
    • -spares COX-1 inhibition
    • -minimal gastric, renal, and platelet effect

    • USES:
    • -osteoarthritis
    • -rheumatoid arthritis
    • -dysmenorrhea
    • -acute pain

    • ADVERSE EFFECTS:
    • -dyspepsia
    • -mild renal impairment
    • -not used in patients with sulfonamide allergy
    • -premature closure of ductus arteriosus
    • -no inhibition of platelets
    • -increased risk of MI and stroke
  4. Acetaminophen (Tylenol)

    Analgesic and Antipyretic
    • MECHANISM OF ACTION:
    • -reduces prostaglandin synthesis in the CNS
    • -has no anti-inflammatory properties

    • USES:
    • -pain and fever
    • -preferred in children
    • -no GI injury, no effect of platelets or kidneys

    • ADVERSE EFFECTS:
    • -toxic metabolite builds up in ETOH abusers
    • -hepatic necrosis can occur
    • -max dose is 4 grams/day
    • -acetylcysteine (mucomyst) given for overdose

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