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114 Cards in this Set
- Front
- Back
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folic acid
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vitamin, hematologic agent; synthesis of pyrimidine/purine bases/AA and prevents/tx megaloblastic anemia, prevents neural tube defects and CAD
diet of organ meat, beans veggies dec in alcoholics, preg, poor diet homocysteine inc w/ deficiency MTX, trimethoprim, pyrimethamine, phenytoin |
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iron dextran
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IM/IV is ferric hydroxid and dextran (glucose); poss anaphylactic rxn in children and 10 tablets can be lethal
tx: iron deficiency |
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deferoxamine
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iron chelator to treat iron overdose and also a whole bowel irrigation; overload poss caused by hemochormatosis, excess storage, genetic, many RBC transfusions
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ferrous sulfate
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tx: iron deficiency orally 3x/day
food dec absorption but poss necessary b/c gastric distress intake from meat and vitamin C enhances; reduced form is ferrous that can bind to O2 w/ Hb and is oxidized as stored ferric; absorbed in duodenum and porx jejunum and bound to tranferrin; stored as ferritin; lasts 120 days adn degraded by reticuloendothelial cells; iron is recycled newborns, preg, menstration, female athlets, surgery, disease can cause iron def |
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ferrous gluconate
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tx: iron deficiency orally 3x/day
food dec absorption but poss necessary b/c gastric distress intake from meat and vitamin C enhances; reduced form is ferrous that can bind to O2 w/ Hb and is oxidized as stored ferric; absorbed in duodenum and porx jejunum and bound to tranferrin; stored as ferritin; lasts 120 days adn degraded by reticuloendothelial cells; iron is recycled newborns, preg, menstration, female athlets, surgery, disease can cause iron def |
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ferrous fumarate
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tx: iron deficiency orally 3x/day
food dec absorption but poss necessary b/c gastric distress intake from meat and vitamin C enhances; reduced form is ferrous that can bind to O2 w/ Hb and is oxidized as stored ferric; absorbed in duodenum and porx jejunum and bound to tranferrin; stored as ferritin; lasts 120 days adn degraded by reticuloendothelial cells; iron is recycled newborns, preg, menstration, female athlets, surgery, disease can cause iron def |
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cyanocobalamin
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inactive B12 (from meat and dairy); IF binds pareital cells to absorb
w/ B12 def inc methymalony-CoA and homocystine and dec succinyl coa - nasal spray less preferred |
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hydroxocobalamin
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for pernicious anemia defective IF give B12 parenterally IM daily for 2 wks then 1/mo for life if malabsortion;
-stays longer in circulation b/c highly bound to palsma proteins inactive B12 (from meat and dairy); IF binds pareital cells to absorb w/ B12 def inc methymalony-CoA and homocystine and dec succinyl coa |
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deoxyadenosylcobalamin
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active forms of B12
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methycobalamin
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active forms of B12
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epoietin a
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SE: HTN
poss dec need for transfusion and inc QOL; inc Hct or Hb dec EPO except in renal disease which a dec in EPO is concurrent w/ anemia tx: hematologic malignancies like lymphoma, HF, chemo, HIV therapy, chronic RF (add folate and iron) --recombanent human EPO |
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darbepoetin alfa
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3x longer HL b/c of inc in sialic acid content!!!!
SE HTN poss dec need for transfusion and inc QOL; inc Hct or Hb dec EPO except in renal disease which a dec in EPO is concurrent w/ anemia tx: hematologic malignancies like lymphoma, HF, chemo, HIV therapy, chronic RF (add folate and iron) |
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epoetin beta
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SE: HTN
poss dec need for transfusion and inc QOL; inc Hct or Hb dec EPO except in renal disease which a dec in EPO is concurrent w/ anemia tx: hematologic malignancies like lymphoma, HF, chemo, HIV therapy, chronic RF (add folate and iron) |
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filgrastim
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hematopoietic GF; recombinant human granulocyte CSF
--by E coli dec infections esp after chemo SE: bone pain tx neutropenia assoc w/ cancer chemo and BM transplant |
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pegfilgrastim
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filgrastin + polyethylene glycol which inc HL to 42 hrs b/c inc size for renal clearance;
hematopoietic GF; recombinant human granulocyte CSF SE: bone pain tx neutropenia assoc w/ cancer chemo and BM transplant |
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sargramostim
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HL is 4; lymphoma pts; GM-CSF
SE: bone pain tx neutropenia assoc w/ cancer chemo and BM transplant |
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erythropoietin in renal disease
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dec w/ anemia (dec of hb and Hct)
also needs folate and iron |
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warfarin
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oral; delayed 3-5 days; inhib synthesis of 2, 7, 9, 10 by blocking vit K reductase; monitor w/ PT
NOT IN PREG; tx: articifical heart valve, log term prophylaxis, stroke/MI prevention; prevents embolism SE: bleeding poss hemorrhage, fetal warfarin syndrome (hemorrhage in fetus), chrondrodysplasia punctata (abnl bone formation) extrinsic pathway |
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coumarin
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warfain and dicumarol comes form it
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dicumarol
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warfarin but causes GI distress
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phytonadione
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antitode to warfarin toxicity; basically vit K1
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tx warfarin toxicity
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phytonadione, FFP, factor 9 conc
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side effects of warfarin
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SE: bleeding poss hemorrhage, fetal warfarin syndrome (hemorrhage in fetus), chrondrodysplasia punctata (abnl bone formation)
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warfarin drug interations
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inc PT (inc effects)- cimetidine, aspirin, cephalosproin, heaprin, sulfa, hepatic disease
dec PT- barbituates, fifampin, diruetic, vit k , hereditary resistance |
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heparin
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yes preg
antithrombotic agent active in vitro; not absorbed from gut (acidic) so parenteral IV/subQ; NOT IM; immediate effect inhibits thrombin and Xa slowly to prevent clotting SE: hemorrage in elderly/RF, TP hyperK (dec aldosterone), osteoporosis if chronic admin Tx: A-fib, STEMI, acute TE, acute therpay, DVt; pregnant woman, embolism, CV surgery, renal dialysis, blood transfusions, blood sampling **venous thromboembolism monitor w/ aPPT overdose-protamine sulfate effect inc by other thormbotic agents |
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enoxaparin
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yes preg
LMWH inact factor Xa (more bioavailable but less effective than HMW fractions) -prevent DVT, embolism, thormbosis in unstable angina, MI more predictable effects than heparin; no need to monitor w/ aPTT SE: bleeding TP (sufonated) |
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dalteparin
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yes preg
GI irritaiton; inact Factor Xa MWH (more bioavailable but less effective than HMW fractions) -prevent DVT, embolism, thormbosis in unstable angina, MI more predictable effects than heparin; no need to monitor w/ aPTT SE: bleeding TP (sufonated) |
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fondaprinux
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yes preg
heparin synthetic pentasaccharide inact Factor Xa MWH (more bioavailable but less effective than HMW fractions) -prevent DVT, embolism, thormbosis in unstable angina, MI more predictable effects than heparin; no need to monitor w/ aPTT SE: bleeding TP (sufonated) |
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bivalirudin
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hirudin analogue (leeches); direct thrombin inhib binds catalytic substract recognition sites; disrupt binding of fibirongen to thrombin
**no TP TX: acute coronary sydnrome an dheparine-induced TP lepirudin used over bivalirudin NOT used in active bleed preg yes |
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tx heparin toxicity
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protamine sulfate b/c highly alkaline or FFP
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protamine sulfate
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tx heparin toxicity
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lepirudin
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hirudin analogue (leeches); direct thrombin inhib binds catalytic substract recognition sites; disrupt binding of fibirongen to thrombin
**no TP TX: acute coronary sydnrome an dheparine-induced TP lepirudin used over bivalirudin NOT used in active bleed preg yes |
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aspirin
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inhibits COX-1 in plts; acetylates serine on plt irrev
dec TXA2 less effect on PGI2; prevent plt agg TX: unstable angina, TIA, stroke prevention, AMI, prevent rhombisis or dec enlargement, artificial heart valve, acute; low doses high doses: inflammatory disroders, pain, fever SE: GI bleed, heart burn, nausea, allegic, anaphylaxis; overdose=tinnitis, resp alkalosis and met acidosis inc effect by anticoag, thormbolytics, exretion inc by alkalinzing urine; ibuprofen can negate antiplt effect antiplt drugs |
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clopidogrel
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block ADP receptors (which induces GP2b/3a for fibrinogen); inhib plt agg
Tx: prophylactic for ischemia; esp if person is allergic to aspirin additive effective w/ aspirin antiplt drugs |
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ticlodipine
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block ADP receptors (which induces GP2b/3a for fibrinogen); inhib plt agg
additive effects w/ aspirin MORE LIKELY TO CAUSE NEUTORPENIA; food intereferes w/ absorption Tx: prophylactic for ischemia; esp if person is allergic to aspirin antiplt drugs |
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abciximab
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plt GP receptor antag to 2b/3a;
mAb to GP Rc; irrev bind to GP2b3a; no agg; percutaneous coronary interventions for procedures -poss TP,bleeding; antiplt drugs |
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tiriofiban
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block Gp2b/3a R competitative rev fibirongen atag; minic fibriongen (analog)
tx: acute coronary syndrome (unstable angina and MI) antiplt drugs |
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eptifibatide
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block Gp2b/3a R competitative rev fibirongen atag; minic fibriongen (analog)
tx: acute coronary syndrome (unstable angina and MI) antiplt drugs |
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alteplast
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recombinant tPA- tissue palsminogen activatory- act fibirn bound plasinogen to palsmin
preferentioally act plaminogen tx: acute AMI, ischemia thrombotic stroke, pulm embosim, STEMI, hemipariesis, HA, blurred vision CI: active bleed; hemorrhagic stroke, sever HTN, intracrainial surgery/trauma, aneurysm, tumor SE: bleeding, reperfusion arrhythmias Inx: inc effect by antithormbotic agents |
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reteplase
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recombinant tPA- tissue palsminogen activatory- act fibirn bound plasinogen to palsmin
preferentioally act plaminogen tx: acute AMI, ischemia thrombotic stroke, pulm embosim, STEMI, hemipariesis, HA, blurred vision CI: active bleed; hemorrhagic stroke, sever HTN, intracrainial surgery/trauma, aneurysm, tumor SE: bleeding, reperfusion arrhythmias Inx: inc effect by antithormbotic agents |
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tenecteplase
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recombinant tPA- tissue palsminogen activatory- act fibirn bound plasinogen to palsmin
preferentioally act plaminogen tx: acute AMI, ischemia thrombotic stroke, pulm embosim, STEMI, hemipariesis, HA, blurred vision CI: active bleed; hemorrhagic stroke, sever HTN, intracrainial surgery/trauma, aneurysm, tumor SE: bleeding, reperfusion arrhythmias Inx: inc effect by antithormbotic agents |
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plasmin
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endogenous anti-plamsins preclude the use of palsmin...drugs are activated w/in clot ("protected")
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streptokinase
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indirect fibrionlytic drug; joins plsainogen to palsmin; lacks fibirn specificity; not enzymatic;
antistreplase=stretokinase +plasminogen activater-->thormbolysis INDICATED FOR PULMONARY EMBOLISM |
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urokinase
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catalytic; from human urine
plasminogen activater-->thormbolysis INDICATED FOR PULMONARY EMBOLISM |
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antiplasmins
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inactivates plasmin before it can become bound to fibirn;
so create clots |
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aminocaproid acid
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inhibits plasminogen for fibrinolytic drugs; tx toxicity
ex: anistreplase, reteplase, streptokinase, tencteplase, urokinase, alteplase |
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atorvastatin
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can take daily anytime, flourine #2 drug
- inhibit acetyl-Coa by blocking HMG-CoA reductase which prevents CH from being made; inc LDL Rc expression in liver; inc LDL remvoal form paslma; dec hepatic CH synthesis; inc clearance of cH; -act in GI tract dec mevalonic acid (CH precursor) inhibits rate-limiting enzyme in CH biosynthesis Tx: hypercholesterolemia 2a and atherosclerosis can combine w/ ezetimibe and bile acid-binding agents SE: myalgia, myositis, rhabodomyolysis; liver tox (hepatitis: GI distress; monitor urin and CK levels effects inc by cyclosporine, gemfibrozil, niacin, azole, antifungals, erythromycin, grafuit juice; inc warfarin inc HDL and dec TGs too **most have short HL 2-3 hrs w/ noctural peak CYP3A |
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fluvastatin
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active fluorine; least myopathy
- inhibit acetyl-Coa by blocking HMG-CoA reductase which prevents CH from being made; inc LDL Rc expression in liver; inc LDL remvoal form paslma; dec hepatic CH synthesis; inc clearance of cH; -act in GI tract dec mevalonic acid (CH precursor) inhibits rate-limiting enzyme in CH biosynthesis Tx: hypercholesterolemia 2a and atherosclerosis can combine w/ ezetimibe and bile acid-binding agents SE: myalgia, myositis, rhabodomyolysis; liver tox (hepatitis: GI distress; monitor urin and CK levels effects inc by cyclosporine, gemfibrozil, niacin, azole, antifungals, erythromycin, grafuit juice; inc warfarin inc HDL and dec TGs too **most have short HL 2-3 hrs w/ noctural peak CYP3A |
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lovastatin
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food inc absorption; (do NOT give if have GI probs); BBB cross-->sleep disturbances; Mevacor; inactive lactone prodrug (act in GI tract)
- inhibit acetyl-Coa by blocking HMG-CoA reductase which prevents CH from being made; inc LDL Rc expression in liver; inc LDL remvoal form paslma; dec hepatic CH synthesis; inc clearance of cH; -act in GI tract dec mevalonic acid (CH precursor) inhibits rate-limiting enzyme in CH biosynthesis Tx: hypercholesterolemia 2a and atherosclerosis can combine w/ ezetimibe and bile acid-binding agents SE: myalgia, myositis, rhabodomyolysis; liver tox (hepatitis: GI distress; monitor urin and CK levels effects inc by cyclosporine, gemfibrozil, niacin, azole, antifungals, erythromycin, grafuit juice; inc warfarin inc HDL and dec TGs too **most have short HL 2-3 hrs w/ noctural peak CYP3A |
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pravastatin
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pravachol; no drug intx!!!!
- inhibit acetyl-Coa by blocking HMG-CoA reductase which prevents CH from being made; inc LDL Rc expression in liver; inc LDL remvoal form paslma; dec hepatic CH synthesis; inc clearance of cH; -act in GI tract dec mevalonic acid (CH precursor) inhibits rate-limiting enzyme in CH biosynthesis Tx: hypercholesterolemia 2a and atherosclerosis can combine w/ ezetimibe and bile acid-binding agents SE: myalgia, myositis, rhabodomyolysis; liver tox (hepatitis: GI distress; monitor urin and CK levels effects inc by cyclosporine, gemfibrozil, niacin, azole, antifungals, erythromycin, grafuit juice; inc warfarin inc HDL and dec TGs too **most have short HL 2-3 hrs w/ noctural peak CYP3A |
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rosuvastatin
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crestor #1 drug; active fluourine; can take daily
- inhibit acetyl-Coa by blocking HMG-CoA reductase which prevents CH from being made; inc LDL Rc expression in liver; inc LDL remvoal form paslma; dec hepatic CH synthesis; inc clearance of cH; -act in GI tract dec mevalonic acid (CH precursor) inhibits rate-limiting enzyme in CH biosynthesis Tx: hypercholesterolemia 2a and atherosclerosis can combine w/ ezetimibe and bile acid-binding agents SE: myalgia, myositis, rhabodomyolysis; liver tox (hepatitis: GI distress; monitor urin and CK levels effects inc by cyclosporine, gemfibrozil, niacin, azole, antifungals, erythromycin, grafuit juice; inc warfarin inc HDL and dec TGs too **most have short HL 2-3 hrs w/ noctural peak CYP3A |
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simvastatin
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zocor; inactive lactone; GI probs; food inc absorption; BBB-sleep disturbances; must give food
- inhibit acetyl-Coa by blocking HMG-CoA reductase which prevents CH from being made; inc LDL Rc expression in liver; inc LDL remvoal form paslma; dec hepatic CH synthesis; inc clearance of cH; -act in GI tract dec mevalonic acid (CH precursor) inhibits rate-limiting enzyme in CH biosynthesis Tx: hypercholesterolemia 2a and atherosclerosis can combine w/ ezetimibe and bile acid-binding agents SE: myalgia, myositis, rhabodomyolysis; liver tox (hepatitis: GI distress; monitor urin and CK levels effects inc by cyclosporine, gemfibrozil, niacin, azole, antifungals, erythromycin, grafuit juice; inc warfarin inc HDL and dec TGs too **most have short HL 2-3 hrs w/ noctural peak CYP3A |
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bile acid bind resins
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colestipol, cholestyramine, colesevelam
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colesevelam
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bile acid binding resin
bile acids made from CH; bind and inhibit bile acid reabsorption form gut in jejunm an dileum which inc CH utilization; inc LDL Rc expression; these inhibit entero-hepatic cycling of bile almost no SE; poss constipation dec CH mainly Tx: hypercholesterolemia in persons not tolerating other drugs; additive esp w/ statins; NOT effective in homozygous familiar hypercholesterolemia b/c they lack LDL Rc!!! CI: inhib absroption of digoxin, TH, fat soluble vitamins, gemfibrozil, steroids |
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colestipol
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bile acid binding resin
bile acids made from CH; bind and inhibit bile acid reabsorption form gut in jejunm an dileum which inc CH utilization; inc LDL Rc expression; these inhibit entero-hepatic cycling of bile almost no SE; poss constipation dec CH mainly Tx: hypercholesterolemia in persons not tolerating other drugs; additive esp w/ statins; NOT effective in homozygous familiar hypercholesterolemia b/c they lack LDL Rc!!! CI: inhib absroption of digoxin, TH, fat soluble vitamins, gemfibrozil, steroids |
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cholestryamine
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bile acid binding resin
bile acids made from CH; bind and inhibit bile acid reabsorption form gut in jejunm an dileum which inc CH utilization; inc LDL Rc expression; these inhibit entero-hepatic cycling of bile almost no SE; poss constipation dec CH mainly Tx: hypercholesterolemia in persons not tolerating other drugs; additive esp w/ statins; NOT effective in homozygous familiar hypercholesterolemia b/c they lack LDL Rc!!! CI: inhib absroption of digoxin, TH, fat soluble vitamins, gemfibrozil, steroids |
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ezetimibe
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in brush border of SI; inhib absorption of CH; 50% even w/o CH in diet; dec LDL, TG, inc HDL; tx: multiple lipid disorders but mainly hyperCHOL; DISRUPTS ANNEXIN-CAVEOLIN COMPLEX; HL 20hr; metab by conj w/ glucoronate
SE: very few mostly dec LDL additive w/ statins (vytorin) |
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fenofibrate
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inc absorption w/ food; HL 20 hrs
fibric acid drug; inc; PPAR-a ligand binds promoter region of gene to transcriptional induct of LPL...inc; FFA into fat tissue to become TG dec VLDL secertion inc clearance ***dec TG levels; blocks secretin Tx: hypertriglercidemia and low HDL levels CI: statins NO! same MOA and SE SE: myopathy, rhabdomyolysis, BM suppresion, exfoliative dermatitis, fibrates potentiate warfarin **monitor LFTs |
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gemfibrozil
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fibric acid drug; inc; PPAR-a ligand binds promoter region of gene to transcriptional induct of LPL...inc; FFA into fat tissue to become TG
dec VLDL secertion inc clearance ***dec TG levels; blocks secretin Tx: hypertriglercidemia and low HDL levels CI: statins NO! same MOA and SE SE: myopathy, rhabdomyolysis, BM suppresion, exfoliative dermatitis, fibrates potentiate warfarin **monitor LFTs |
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niacin
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B3 is incorporated into NAD in oxidation rxn; GPCR ligand inhibits lipolysis in adipose tissue and release of FA; dec TG syn and dec VLDL
B3 prevents atherosclerotic damage by inc ABCA1 w/ HDL act LPL best effect on CH dec CV mortality tx: hypercholesterolemai, hyperTG, low HDL SE: flusing, VD, GI distress; inc blood glc; aggrevate peptic ulcer (CI PUD); myopathy, rhabdomyolysis (do NOT combo w/ statin) asprin pretx reduces VD and flushing |
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tx hyperCH
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statin (HMG coa reductase inhib); bile acid binding resins (combo w/ statin), niacin (GCPR B3), ezetimibe (combo w/ statin; on brush border disrupts annexin-caveolin complex)
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hyperTG and low HDL
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gemfibrozil-fibrate blocks PPAR-a RE on gene inc LPL); Niacin- in NAD
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tx high levels of both TG/CH
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niacin
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inc LDL, dec HDL, inc TG and has T1DM
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use gemfibrozil NOT niacin
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SE using gemfibrozil and statin
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rhabdomyalysis
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inc TG, nl HDL, high B band electorphoresis, fam hx MI w/ itraconazole
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hyperlipproteiniemia so no LDLR can't use statins b/c of itraconazole and not bile acid b/c of no LDLRc so use niacin
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adult male w/ inc VLDL, TG, LDL norm and dec HDL
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niacin
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NSAIDS tx:
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inhib COX
tx: inflammation, pain, fever |
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Cox-1 is
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consitutive (always there in kidneys, plt, GI tract); inability to form stomach protecting PG; dec TxA2
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Cox-2 is
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inducible and assoc w/ inflammation, less GI distress
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aspirin
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acetysalicylic acid ASA absorb in stomach, low gastric pH so in non-ionized form which enhances absorption can irritate mucosal lining; buffering can dec irritation by slowing absorption rate
Phase 1 metab- hydrolyzed acetic acid and salicylate by esterase in tissues and blood Phase 2: conjugate w/ glycine; water-soluble inhib TxA2 more than PGI2 tx: pain and fever at low dose and inflammation at high dose NSAID; tx: MI TIA, stroke SE: GI bleed, epigastric distress, heartburn, nausea, allgery, overedose=tinnitus and resp alk intx: inc by anticoags; inc excretion by alkalinizing urin; ibuprofen can negate antiplt effect 15 mins; 1-2 hrs as salycylate high dose 15hrs sat at phase 2 becomes zero order and subsequrent small dose inc result to build up serum salicylate irrevercsible COX inhibitor |
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salicylate
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rev COX inhibtor;
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aspirin SE
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low dose-GI distress w/ inc BT
high dose- tinnitis; resp depression as resp alkylosis to met acidosis |
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tx aspirin toxicity
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gstric lavage; sodium bicarb alkalinizes
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ibuprofen
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2 hr HL NSAID; tx pain/inflammation assoc w/ trauma/infection; potency 3
inhib COX1/2 nonselective; synthesis of PG causing pain, fever and inflammation tx: mild to mod pain or dysmenorrhea; infalmmatory disorders; osteoarthritis and RA reduces risk of colon, breast, lung, prostate cancer SE: GI bleed, N/V, dyspepsia, allergic rxn poss hepatitis, RF Inx: NOT w/ GI probs inc renal tox; dec effect of antiHTNs; inc lithium; aspirin dec effects |
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diclofenac
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approx 2 hr NSAID; pain/inflammation assoc w/ trauma/infection; potency 3
inhib COX1/2 nonselective; synthesis of PG causing pain, fever and inflammation tx: mild to mod pain or dysmenorrhea; infalmmatory disorders; osteoarthritis and RA reduces risk of colon, breast, lung, prostate cancer SE: GI bleed, N/V, dyspepsia, allergic rxn poss hepatitis, RF Inx: NOT w/ GI probs inc renal tox; dec effect of antiHTNs; inc lithium; aspirin dec effects |
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etodolac
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approx 2 hr NSAID; pain/inflammation assoc w/ trauma/infection; potency 3
inhib COX1/2 nonselective; synthesis of PG causing pain, fever and inflammation tx: mild to mod pain or dysmenorrhea; infalmmatory disorders; osteoarthritis and RA reduces risk of colon, breast, lung, prostate cancer SE: GI bleed, N/V, dyspepsia, allergic rxn poss hepatitis, RF Inx: NOT w/ GI probs inc renal tox; dec effect of antiHTNs; inc lithium; aspirin dec effects |
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fenoprofen
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NSAID; pain/inflammation assoc w/ trauma/infection; potency 3
inhib COX1/2 nonselective; synthesis of PG causing pain, fever and inflammation tx: mild to mod pain or dysmenorrhea; infalmmatory disorders; osteoarthritis and RA reduces risk of colon, breast, lung, prostate cancer SE: GI bleed, N/V, dyspepsia, allergic rxn poss hepatitis, RF Inx: NOT w/ GI probs inc renal tox; dec effect of antiHTNs; inc lithium; aspirin dec effects |
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flubiprofen
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NSAID; pain/inflammation assoc w/ trauma/infection; potency 3
inhib COX1/2 nonselective; synthesis of PG causing pain, fever and inflammation tx: mild to mod pain or dysmenorrhea; infalmmatory disorders; osteoarthritis and RA reduces risk of colon, breast, lung, prostate cancer SE: GI bleed, N/V, dyspepsia, allergic rxn poss hepatitis, RF Inx: NOT w/ GI probs inc renal tox; dec effect of antiHTNs; inc lithium; aspirin dec effects |
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meloxicam
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approx 2 hr NSAID; pain/inflammation assoc w/ trauma/infection; potency 3
inhib COX1/2 nonselective; synthesis of PG causing pain, fever and inflammation tx: mild to mod pain or dysmenorrhea; infalmmatory disorders; osteoarthritis and RA reduces risk of colon, breast, lung, prostate cancer SE: GI bleed, N/V, dyspepsia, allergic rxn poss hepatitis, RF Inx: NOT w/ GI probs inc renal tox; dec effect of antiHTNs; inc lithium; aspirin dec effects |
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ketoprofen
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2 hr HL; pain/ inflammation assoc w/ traum/infection
NSAID; pain/inflammation assoc w/ trauma/infection; potency 3 inhib COX1/2 nonselective; synthesis of PG causing pain, fever and inflammation tx: mild to mod pain or dysmenorrhea; infalmmatory disorders; osteoarthritis and RA reduces risk of colon, breast, lung, prostate cancer SE: GI bleed, N/V, dyspepsia, allergic rxn poss hepatitis, RF Inx: NOT w/ GI probs inc renal tox; dec effect of antiHTNs; inc lithium; aspirin dec effects |
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nabumetone
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approx 2 hr NSAID; pain/inflammation assoc w/ trauma/infection; potency 3
inhib COX1/2 nonselective; synthesis of PG causing pain, fever and inflammation tx: mild to mod pain or dysmenorrhea; infalmmatory disorders; osteoarthritis and RA reduces risk of colon, breast, lung, prostate cancer SE: GI bleed, N/V, dyspepsia, allergic rxn poss hepatitis, RF Inx: NOT w/ GI probs inc renal tox; dec effect of antiHTNs; inc lithium; aspirin dec effects |
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naproxen
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****14 hr HL potency is 4
NSAID; pain/inflammation assoc w/ trauma/infection; potency 3 inhib COX1/2 nonselective; synthesis of PG causing pain, fever and inflammation tx: mild to mod pain or dysmenorrhea; infalmmatory disorders; osteoarthritis and RA reduces risk of colon, breast, lung, prostate cancer SE: GI bleed, N/V, dyspepsia, allergic rxn poss hepatitis, RF Inx: NOT w/ GI probs inc renal tox; dec effect of antiHTNs; inc lithium; aspirin dec effects |
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oxaprozin
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approx 2 hr
NSAID; pain/inflammation assoc w/ trauma/infection; potency 3 inhib COX1/2 nonselective; synthesis of PG causing pain, fever and inflammation tx: mild to mod pain or dysmenorrhea; infalmmatory disorders; osteoarthritis and RA reduces risk of colon, breast, lung, prostate cancer SE: GI bleed, N/V, dyspepsia, allergic rxn poss hepatitis, RF Inx: NOT w/ GI probs inc renal tox; dec effect of antiHTNs; inc lithium; aspirin dec effects |
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piroxicam
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57 HL used to Tx RA b/c of its long HL; potency 200
NSAID; tx: mild to mod pain or dysmenorrhea; infalmmatory disorders; osteoarthritis and RA reduces risk of colon, breast, lung, prostate cancer SE: GI bleed, N/V, dyspepsia, allergic rxn poss hepatitis, RF Inx: NOT w/ GI probs inc renal tox; dec effect of antiHTNs; inc lithium; aspirin dec effects |
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sulindac
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approx 2 hr HL
NSAID; pain/inflammation assoc w/ trauma/infection; potency 3 inhib COX1/2 nonselective; synthesis of PG causing pain, fever and inflammation tx: mild to mod pain or dysmenorrhea; infalmmatory disorders; osteoarthritis and RA reduces risk of colon, breast, lung, prostate cancer SE: GI bleed, N/V, dyspepsia, allergic rxn poss hepatitis, RF Inx: NOT w/ GI probs inc renal tox; dec effect of antiHTNs; inc lithium; aspirin dec effects |
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tolmetin
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approx 2 hr HL
NSAID; pain/inflammation assoc w/ trauma/infection; potency 3 inhib COX1/2 nonselective; synthesis of PG causing pain, fever and inflammation tx: mild to mod pain or dysmenorrhea; infalmmatory disorders; osteoarthritis and RA reduces risk of colon, breast, lung, prostate cancer SE: GI bleed, N/V, dyspepsia, allergic rxn poss hepatitis, RF Inx: NOT w/ GI probs inc renal tox; dec effect of antiHTNs; inc lithium; aspirin dec effects |
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indomethacin
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5 hr HL; toxic, short term in severe cond; tx serious infection (gouty arthritis, osteoarthritis, RA, ankylosing spondylitis); used in closure of PDA in infants
more GI and CNS SE nonselective NSAID reserved for pts not responding to less toxic drugs SE: GI bleed, N/V, dyspepsia, allergic, dizzy, drowsy, HA adverse effect inc by other NSAIDs; acetaminophen inc renal tox; dec effect of antihtn; inc lithium; aspirin dec effects of both; hyperK w/ K sparking diruetics |
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ketorolac
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4-10 hr HL; post-op pain, similar analgesis effect as morphine but w/o N/V; IV or IM SHORT TERM
TX: MIGRAINS AND GLAUCOMA MORE HEMOLYTIC TOX nonselective NSAID; inc BT limit to <5 days SE: inc risk allergic rxn w/ asthma; nasal polyps adverse GI effect inc by NSAIDs, use w/ acetaminophen inc renal tox; dec effect of antiHTN agens; inc lithium; aspirin dec effets of both; inc risk of bleed w/ thormbolytics |
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celecoxib
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inhib COX-2 NSAID; and PG
Tx: osteoarthritic RA easily absorbed; 3 hrs; p-450; SE: abdominal pain, dyspepsia, diarrhea; GI ulcers; inc stroke an dMI intx: P450 dec effects of ACEi and diuetics and inc lithium |
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acetaminophen
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tylenol; inhib COX3; inhib synthesis of PG causing pain and fever; NOT affect inflammation; inhib by peroxides so only in CNS not periphery
tx: mild to mod pain; fever SE: overdose fatal hepatic fialure glutitione clears inx: inc hepatotoxicity w/ alcohol use; add salicylates an dNSAID additive renal toxicity |
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man has peptic ulcers, mm pain and family hx of AMI
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tx w/ acetaminophen NOT COX nonsp b/c GI distress; no COX2 due to family hx
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fever, aching mm tx w/
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acetaminophen
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twisten ankle, HA, fever tx w/ acetamiophen what happens?
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still swollen b/c periphery peroxides degrade
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acetycysteine
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tx acetaminophen toxicity which inc GSH
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RA first choice for pain relief
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Gluycocorticoids and maybe prednisone (lipocortin) and NSAIDS
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methotrexate
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immunosuppressant; inhibits AICAR in purine synthesis; thymidylate synthetase in DNA synthesis; can be long term; dose lower than that in cancer chemo
folate reductase inhibitor tx: RA SE: N/V, hepatotox, anemia, leukopenia, TP, nephropathy itx: sufas, Trimethoprim |
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chlorambucil
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inhibtis cell replication; immunosuppresant; cross links DNA
tx: RA SE: N/V, anorexia, hemorrhage, TP, leukopenia, anemia intx: rifampin, doxorubicin |
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cyclophosphamide
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inhibtis cell replication; immunosuppresant; cross links DNA
tx: RA SE: N/V, anorexia, hemorrhage, TP, leukopenia, anemia intx: rifampin, doxorubicin |
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cyclosporine
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immunosuppresent; inhibitos IL-2; disrupts T cell
Tx: RA SE: nephrotixic, HTN, GI distress, gingival hyperplasia intx: CYP450 drugs |
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infliximab
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disease mod antirheumatic durg; monoclonal Ab to TNFa
inac TNFa and dec joint inflammation pain destruction Tx: RA and crohns IV every 4 wks sometimes combine w/ MTX- 8 wks so don't intx w// mouth Ab SE: n/v, fatique, URT infection |
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adalimumab
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give subQ every 2 wks
disease mod antirheumatic durg; monoclonal Ab to TNFa inac TNFa and dec joint inflammation pain destruction Tx: RA and crohns SE: n/v, fatique, URT infection |
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etanercept
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recombinant fusion protein TNFa Rc-IgG binds TNFa; recetpor for cytokines; expencive
dec joint inflammation an dpain; slows RA sub Q twice wkly SE: URT infeciton, HA can dec Ab response to live virus vaccines |
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Leflunomide
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inhib ribonucleotide synthesis; inhib T cell prliv
act in intestine/plasma; inhibits dihydro dehydrogenase disease mod antirheumatic durg; monoclonal Ab to TNFa inac TNFa and dec joint inflammation pain destruction Tx: RA and crohns SE: n/v, fatique, URT infection |
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anakinra
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recombinant IL-1B Rc antag; locks cytokine induced inflammaiton given subQ
TNF a blocking agent Tx: RA |
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arthrocentesis
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remove fluid form joint for inspection of crystals
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allopurinal
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stops production of uric acid; inhib xanthine oxidase which catabolizes purines
prevent hyperuricemia NOT for acute attaks of gout SE: rask intx: inhibtis metab of mercaptopurine and inc mercaptopurine BM suppresion; inc effects of warfarin and hypoglycemic agents; ampicillin inc risk of rash |
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probenecid
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highdose salicyclate inc uric acid clearance
antigout; uricosuric agent tx: and prevents gouty arhtritis; inhibits renal tubular secretion of penicillins an dused to inc penicillin serum levels SE: diarrhea, n/v poss agranulocytosis, aplstic anemia inx: colchicine additive bm suppresion combo colchicine prevents leukocyte respones to urate cystals |
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sulfinpyrazone
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highdose salicyclate inc uric acid clearance
antigout; uricosuric agent tx: and prevents gouty arhtritis; inhibits renal tubular secretion of penicillins an dused to inc penicillin serum levels SE: diarrhea, n/v poss agranulocytosis, aplstic anemia |
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diretics and low-dose salicylates do what to uric acid
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uric acid rtn
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colchicine
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used for acute attacts and prophylacxis; prevents plymerizaiton of tubulin into MT; inhib leukocyte migration into affected area; inhib synthesis an drlease of leuktirenes
combine w/ probenecid for gout |
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pripionic acid derivative in GOUT
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ibuprofen, naproxen, kepprofen all given in first acute gout attack due to toxicity of colchicines NOT aspirin
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probenecid or allopurionol
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observe 24 hr uric acid excretion rate less than 800 mg too little excretion; give probenecid
gtrs than 800 mg give allopurinol |
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F w/ RA, NSAIDS then MTX given drug Sub Q
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TNFa ineffective is adalimumab???
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