Help
Options
Didn't know it?
click below
click below
Knew it?
click below
click below
Don't Know
Remaining cards (0)
Know
retry
shuffle
restart
0:00
Embed Code - If you would like this activity on your web page, copy the script below and paste it into your web page.
Normal Size Small Size show me how
Normal Size Small Size show me how
mskt1
pharm--antiarthritis
| Question | Answer |
|---|---|
| when is tylenol useful? | -Samter's sndrome -Hemphilia -active PUD -children w/viral infxns |
| metab of tylenol? | -hepatically conjugated=>sulfate/glucuronide -high doses=>iminoquinone=>overwhemls glutath=>hepatic tox |
| ae of tylenol? | -LFTs -LT: renal impair -pts w/liver dz: hemolytic anemia, methemoglobinemia |
| why is Phenacetin banend in us? | -carcinogenicc -nephrotox |
| use of Chlorquine/hydroxy? | -FDA: RA...used for others like SLE, Sjoegrens -pts w/ MILD dz w/o bony erosions (not help w/bone damage) |
| metab of chloroquine? | -oral ->plasma proteins -> esp taken up by melanin-tissues like eyes -> slow liver metab (1/2= 40 d!) |
| shortcoming of chlorquien? | -takes months to work and for mild dz only |
| ae of chlorquine? | -ocular toxicity -GI effects, rash, nightmares |
| chlloroquine + preg? | 0ok |
| name the types of DMARDs | -glucocorticoids -immunosuppresants -gold, penicillamine -biologicals -tnf-a blockers |
| typical use of glucocorticois? | -most pts -esp early and in acute flares -esp intra-articularly -and for extra-articular manifestations |
| moa of mtx? | -inhib of AICAR ribonucleotide transformylase and thymidine synthase and leukocyte chemotaxis (high doses: inhib dihydrofolate reductase) ..mostly inhibits prolif/form of proinflam cytokines and ->apoptosis of inflam cells (vs DHFR=>lymphos and MOs) |
| metab of mtx? | -oral-> liver metab ->distrib widely= polyglutamated resorvoir -urine > bile excretion |
| hydroxychorquine + mtx? | reduced mtx renal clearance... |
| ae of mtx? | -nausea, apthous ulcers = MC -pneumonitis, pseudolymphomatous rxns -rarely cirrhosis (biopsy every 5 yrs) |
| c/i of mtx? | preg |
| use of leucovorin w/ mtx? | -reduces GI/liver tox, but decreases drug efficacy |
| moa of cyclophosphamide? | -prodrug -> phoshoramide mustard => akylates and x-links DNA=> prevents cell replication -suppresse T-cell (some B-cell) fxn in AI dzs |
| ae of cyclophos? | hemorrhagic cystitis...rare w/low doses used for AI dzs |
| moa of cyclosporine? | -inhibits IL-1 and IL-2 RECEPTOR produc and fxns of T-cells |
| use of cyclosproine? | -FDA: RA...used in others though (sle, juvenile, wegerns) |
| problems w/ cyclosporine? | -erratic biavail..use microemulsion formul -cyp3a4 metab...drug-drug |
| ae of cycloporine? | -NEPHROTOX (monitor BP and SCr) -hyperkalemia -gingival hyperplasia -hirsuitism -rarely hepatotox ...MONITOR WHOLE BLOOD LEVELS to avoid tox |
| moa of sulfasalazine? | -reduces produc of Rhematoid factor, suppresses T-cell fxn and B-cell prolif (decrease rlease/produc of inflam cytokines) |
| metab of sulfasalzine | -hydrolyzed in GI=> Sulfapyridine (RA, ankyl spond) and 5-aminosalicylic acid (IBD) -only 20% bioavail after oral, but some goes->enterohepatic recirculation=>hydrolysis via intestinal bacterial =>sulfpyradine liberation=>hepatic metab |
| ae of sulfasalazine? | -GI, h.a., rash -1/3 d/c -neutropenia, hemolytic anemia -pulm tox -methemoglobinbemia -REVERSIBLE INFERTILITY IN MEN! but non-teratogenic |
| moa of leflunomide | -prodrug to dihydroorotate dehydrogase inhib => decrease ribonucleotide synth and => cell cycle arrest in G1 ...=>inhib of T-cell prolif and B-cell auto-AB produc |
| use of LEflunomide? | mostly RA...as effective as MTX...oftne used as combo w/ MTX |
| metab of Leflunomide? | -oral => plasma and GI=>active drug =>enteroheptic circulation |
| drug itneractions w/ leflunomide? | -cholestyramine and resin binders can interrupt the meteab (enterohepatic circ) => increased clearance |
| ae of leflunomide? | -diarrhea -LFTs -alopecia -wt gain -htn |
| c/i of leflunomide? | preg |
| moa of mycophenolate mofetil? | -prodrug -> immed hydrolyzed to mycophenolic acid -> inhib iosine monophosphate dehydrogenase =>T_cell prolif/leukocyte adhesion inhib via ICAM-1 inhib.... |
| use for mycophenolate mofetil? | -mc in Lupus nephritis, s.t. vasculitis/wegeners -NOT usually for RA |
| moa of azathioprine? | -hepatic metab=> 6-thioguanine, which inhibits INOSINIC ACID and then PURINE synth, then reduces B- and T_cell fxn , IG produc, IL-2 secretion |
| metab of aza? | -genetically based...10% have less fxn of thiopurine s-methytransferase and .3% have hardly any fxn...high rx of myelosuppression if dont reduce dose |
| use of aza? | fda: RA...also used for psoraitic arth , lupus, behcet dzs |
| ae of aza? | BM SUPPRESSION....GI, infxn, lyymphoma Allergy: fever/rash/LFTs |
| problem w/ D-penicillamine? what to do if you do use it? | -slow, not that effective, Lupus like illness, leukopenia (and bad GI effects) -must monitor: temp, cbc, renal fxn |
| problem w/ gold tx? | -limited efficcy, unk moa, IM -apthous ulcers!...thrymobocyto, proteinuria, leukppenia, anemia, NITRITOID RXN , chronic=>ligh blue skin |
| name the biologicals | abatacept anakinra rituximab |
| moa of abatacept | -costim modulation: binds CD80 and CD86 on APC => prevents t-cell binding to cd28 and stops t-cell activatilon |
| dosing of abatacept | -IV, based on body wt, every 2 wks |
| use of abatcept | mod-sever dz when other DMARDs ineffecctive |
| ae of abatacept | -rx of infxn, infusion rxn, hypersens, lymphoma -synergetist w/ tnf-a inhibs=>HIGH rx of infxn |
| moa of anakinra | -human recomb (IL-1 receptor antag -has N-terminal methionine=> block receptor w/o activation |
| use and admin of anakinra | -daily SQ; combo w/ other DMARDs (NOT tnf-a! infxns!) |
| ae of anakinra | -injection site rxns are very common, but resolve -less serious infxns than tnf-a inhibs -neutropenia s.t. occurs |
| moa of rituximab | -chimeric monoclonal AB targers cd20 b-lymphos...reduces inflam of cell- and compelment-mediated cytotix, tim apoptosis, inhib secretion of coytokines, dcreases antigen present to T_cells |
| admin and use of ritux | -IV post-pretx w/ IV steroid to prevent infusion rxns -used post-failure of tnf-a blockers |
| ae of ritux | -rashes, reduced w/each admin -NOT assoc w/ infxn/lmphoma! but decrases IgG and IgM |
| name the tnf-a blockers | -adalimumab -infliximab -etanercept |
| tnf approved for | ra |
| moa of adalimumab? | -IgG monoclonal ab: prevents soluble tnfa from interacting w/ p55 and p75 cell surface receptors -> MO and T-cell downregulation |
| admin and use of adalimbum | -sq every 2 wks (longer if w/MTX) -FDA: arthritis, psoraisa, crohns |
| ae of adalimbumab | -infxn, lymphoma (but not solid tumors) -ana abs, ds-dna abs, leukopenia, vasculitis |
| moa of infliximab | -chimeric IgG monoclonal ab: binds soluble AND bound tnf-a=> downregul MO and T_cell fxn |
| admin and use of infliximab | -IV q8wks usu w/ mtx -fda: ra, sporiatic arth, anyl spon, crohns...used for others though |
| ae of of inflixmab | -infxn, TB REACTIVATION,hbv reactiv -lymphoma? -infusion site rxns (pre-tx w/ h1 and h2 blockers and steroids) |
| moa of etanercept | -recomb fusion protein: links 2 extracel doamins of TNF p75 w/ Fc of IgG = binding of tnfa-a AND tnf-b |
| admin and use of etanercept | -sq q1wk usu w/ mtx (less AB formation to the drug) -fda: ra, psoiatic arth, JUVENILE, ankyl, psori |
| ae of etanercept | -injfec site rxns -LESS reactivation TB -infxns, lymphoma -ab formation to the drug if not used w/ mtx |
| what is tofacitinib? use? | -inhib of JAK ...st. in combo w/ MTX/nonbiologics -2x/d oral for mod-severe RA unresponsive to mtx |
| ae of tofac? | -uri, h.a., gi -infxns, lymphoma, cancers, GI perforations -LFTs, cholesteral increase, lowers leukocutes -$$$ |
| what not to combine tofac w/ ? | -immunosuppres or bioligicals |
| metab of tofac? | -mostly cyp3a4 and cyp2c19, then renal excetion...reduce if ckd |
| if you use tofac you must | monitor freq |
| mc combo for ra | mtx + cyclosporine/antimalarial/leflu/ritux/anti-tnf...not aza, gold, sulfasal w/ mtx...not useful |
Created by:
geil