PHARM_MSK_MS2

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Author:
soren101
ID:
119978
Filename:
PHARM_MSK_MS2
Updated:
2011-12-09 14:44:58
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PHARMACOLOGY MUSCULOSKELETAL MS2
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PHARM MSK MS2
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  1. DICLOFENAC
    NONSALICYLATE NSAID

    RELATIVELY SELECTIVE FOR COX-2

    • RA AND OA
    • --ALL NSAIDS EQUAL IN Tx

    ANKYLOSING SPONDYLITIS

    Tx ELDERLY w Hx OF GI BLEED CAUSED BY AN NSAID

    SOME INH OF LIPOXYGENASE

    SHORT t1/2 < 6hrs
  2. INDOMETHACIN

    for arth
    NONSALICYLATE NSAID

    SOME INH OF LIPOXYGENASE

    PHARM PROPERTIES UNRELATED TO INH OF PG SYNTHESIS

    HIGH INCIDENCE OF CNS SIDE EFFECTS, ESP IN ELDERLY

    SHORT t1/2 < 6hrs
  3. OXAPROZIN
    NONSALICYLATE NSAID

    LONG t1/2 > 15hrs
  4. CELECOXIB
    COX-2 INH

    t1/2 = 10hrs

    • THERA
    • --Tx OA and RA
    • --PRIMARY DYSMENNORHEA
    • --POST-OP SURG & DENTAL PAIN
    • --PREVENTION OF COLORECTAL CANCER & ALZ?
    • --NO EFFECT ON PLATELET AGG OR BLEEDING TIME
    • --NON INTERFERENCE w ANTIPLATELET ACT OF ASPIRIN

    COX-2 NEC FOR KIDNEY FUNCTION AND INVOLVED IN PULMONARY PHYSIOLOGY

    NO ANAPHYLACTOID-LIKE REACTIONS IN Pts w SUCH REACTION FROM NSAIDS

    MAY STILL CAUSE GI ULCERATION IN Pts w Hx OF GI BLEED FROM NSAIDS
  5. MISOPROSTOL
    PGE ANALOG

    • Tx GASTRIC EROSION AND ULCERATION CAUSED BY NSAIDS AND CORTICOSTEROIDS
    • --COMBO w DICLOFENAC

    • ADVERSE
    • --DIARRHEA
    • --ABD PAIN & CRAMPING

    • PGE
    • --INH RELEASE OF NE PRESYNAPTIC AND VASODILATE POSTSYNAPTIC TO ANTAGONIZE NE
    • --WORK TO ATTENUATE INC IN BP IN VASC SMOOTH MUSC
    • --IN KIDNEY: ATTENUATE EFFECT OF ADH ON COLLECTING DUCT TO PREVENT HYPONATREMIA

    • PGE IN STOMACH
    • --INH ACID SECRETION
    • --STIM MUCOUS SECRETION
    • --INC BICARB
    • --INC MUCOSAL BLD FLOW
    • --STIM CELL GROWTH & REPAIR
  6. ETANERCEPT
    "BIOLOGIC" DMARD

    MONOCLONAL Ab FOR Tx OF Rh

    SOLUBLE TNF RECEPTORS THAT BIND TNF-a IN THE BLD AND JOINTS

    • ADVERSE
    • --INC RISK OF INFEC
    • --REACTIVATION OF LATENT TB
    • --TRANSIENT NEUTROPENIA
  7. "BIOLOGIC" DMARDs
    • ETANERCEPT
    • INFLIXIMAB
    • ADALIMUMAB
    • ABATACEPT

    DISEASE MOD ANTI RHEUM DRUGS
  8. INFLIXIMAB
    ADALIMUMAB
    "BIOLOGIC" DMARDs

    MOA SAME AS ETANERCEPT -- BINDS TNF-a IN BLD & JOINTS

    Tx Rh AND PSORIATIC ARTH, ANK SPOND, CROHN'S Dz

    • ADVERSE
    • --INC RISK OF INFEC
    • --REACTIVATION OF LATENT TB
  9. ABATACEPT
    "BIOLOGIC" DMARD

    T-CELL CO-STIM BLOCKER

    COMBOs BINDING PORTION OF CTLA-4 TO Fc PART OF Ig --> INH OF T-CELL ACTIVATION BY BINDING TO APC

    USED ON Pts WHO FAILED THERAPY w OTHER DMARDs AND TNF-a ANTAGS

    • ADVERSE
    • --INC RISK OF INF

    nLLY CTLA-4 RELEASED BY ACTIVATED T-CELLS TO INH FURTHER T-CELL ACTIVATION AND BINDS TO CD80/86 (B7) ON APC

    T-CELL CD28 BINDS TO CD80/86 (B7) ON APC FOR ACTIVATION
  10. ANAKINRA
    "BIOLOGIC" DMARD

    IL-1 RECEPTOR ANTAGONIST

    Tx Rh

    • ADVERSE
    • --INC RISK INFEC

    nL -- IL-1 IS PROINFLAM THAT INC DEGRAD OF CART & STIMS OSTEOCLAST.

    IL-1 --> ATP --> INH IkK --> IkB PHOSED --> NFkB RELEASED AND ENTERS NUC
  11. COLCHICINE
    GOUT

    BINDS TUBULIN TO INH MICROTUBULES --> INH LEUKO MIGRATION AND PHAGO

    • TOXIC
    • --DIARRHEA
    • --ABD PAIN
    • --ALOPECIA
    • --BM DEPRESSION
    • --MYOPATHY
  12. INDOMETHACIN

    for gout
    NON SALICYLATE NSAID

    USED IN PLACE OF COLCHICINE FOR ACUTE ATTACKS

    INH OF PGs SYNTH PREVENTS PHAGO OF URATE CRYSTALS BY SYNOVIOCYTES AND MACROs
  13. PROBENECID
    GOUT

    INC RENAL EXCRETION OF URATE

    BEGIN 2-3 WEEKS AFTER ACUTE ATTACK
  14. ALLOPURINOL
    FEBUXOSTAT
    GOUT

    INH XANTHINE OXIDASE

    PREVENT HYPOXANTHINE AND XANTHINE CONVERSION TO URIC ACID

    FEBUXOSTAT MORE EFFECTIVE THAN ALLO IN DEC PLASMA URATE CONC

    SOME Pts THAT DON'T RESPOND TO ALLO WILL RESP TO FEBUX

    LONG-TERM FEBUX Tx DEC GOUT "FLARES" AND DEC SIZE & # OF TOPHI

    FEBUX MORE EXPENSIVE

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