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77 Cards in this Set
- Front
- Back
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Azathioprine is metabolized to what?
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Azathioprine is metabolized to 6-mercaptopurine- a purine anti-metabolite.
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How does Azathioprine/6-mercaptopurine exert its action
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A purine anti-metabolite, it inhibits DNA synthesis by inhibiting both the de novo and salvage pathways of DNA synthesis.
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What is azathioprine/6-mercaptopurine used for
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Inhibit rejection of transplanted organs
Autoimmune diseases (rheummatoid arthritis) |
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What drug could you give thats a purine anti-metabolite that inhibits rejection of transplanted organs and useful in treating autoimmune diseases
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Azathioprine
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How does cyclophosphamide work?
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Cyclophosphamide is an alkalating agent that cross links DNA to kill cells- this effect is more pronounced on B cells - > leads to humoral supression.
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What is cyclophosphamide used for?
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Autoimmune disease treatment in combination with other drugs.
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What drug could you give that would treat autoimmune diseases in combination with other drugs?
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Cyclophosphamide
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What drug is an alkylating agent that cross links DNA to kill cells and has a more pronounced effect on B cells?
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Cyclophosphamide
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How does methotrexate work?
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Methotrexate is a dihydrofolate reductase inhibitor -> this inhibits DNA synthesis due to no tetrahydrofolate formation
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What is methotrexate used for
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Methotrexate is used to treat autoimmune disease
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What drug inhibits dihydrofolate reductase and treats only autoimmune diseases?
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Methotrexate
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What does mycophenolate mofetil treat
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1) prevent renal allograft rejection with corticosteroids and cyclosporine
2) autoimmune diseases (rheumatoid arthritis, refractory psoriasis) |
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How doe mycophenolate mofetil work
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mycophenolate mofetil inhibits IMP dehydrogenase (which is needed to make GMP)
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Does mycophenolate mofetil work on inhibiting salvage or denovo pathways or both
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Mycophenolate mofetil inhibits only the de novo pathway. It has NO EFFECT on salvage pathway
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Which drug prevents renal allograft rejection and treats autoimmune diseases (rheumatoid arthritis and refractory psoriasis)
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Mycophenolate mofetil
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Which drug inhibits IMP dehydrogenase, having only an effect on the de novo pathway?
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Mycophenolate mofetil
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What does cyclosporine do?
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Prevents rejection of implanted organs
Helps in treating autoimmune diseases |
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How does cyclosporine work?
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It is an antibiotic that binds cyclophilin, which blocks activation of transcription factors needed to make IL-2- this inhibits t cell proliferation and cytotoxicity.
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Which drug binds cyclophilin, in turn inhibiting production of txn factors needed to make IL-2, ultimately inhibiting t cell proliferation and cytotoxicity.
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Cyclosporine
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What drugs have the effect of 1) inhibiting rejection of transplanted organs
2) treating autoimmune diseases |
azathioprine
and cyclosporine, tacrolimus, sirolimus |
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How does tacrolimus work?
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Binds FK binding protein and then has the same effect as cyclosporine, which is to inhibit IF-2 production that is needed for t cells to proliferate and be cytotoxic
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What is the difference between tacrolimus and cyclosporine if both have the same use
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Tacrolimus is more potent.
Tacrolimus binds FK binding protein rather than cyclophilin. |
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What is the use of tacrolimus
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1) Inhibit rejection of transplanted organs
2) Autoimmune disease tx |
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What additional therapeutic use does sirolimus have in addition to inhibiting organ transplant rejection and treating autoimmune disease
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It also coats cardiac stents to prevent restenosis
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How does sirolimus work
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Binds FK binding protein 12- it binds and inhibits mTOR, which blocks G1 -> S transition, inhibiting t cell response to IL-2
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What does sirolimus do
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1) prevent rejection of transplanted organs
2) treat autoimmune disease 3) coat cardiac stents to prevent restenosis |
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What is another name for Aspirin
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Acetylsalicylic acid
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What is the MOA of aspirin?
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Irreversible COX inhibitor (acetylation)
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Which NSAID is a uricosuric agent?
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Aspirin is a uricosuric agent at high doses. At low doses it increases serum uric acid.
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What are the therapeutic effects of aspirin
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1) anti-inflammatory, analgesic, anti-pyretic
2) reduce cancer risk, prevention of CV disease (low dose) |
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What is the toxicity of aspirin overdose
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CNS toxicity causing delirium, psychoses, nausea, vomitting, respiratory alkalosis and tinnitus
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Ibuprofen and naproxen work in what way?
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Reversible COX inhibitors
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What drug is an irreverisble cox inhibitor?
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Aspirin/acetylsalicylic acid
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What drug is an uricosuric agent at high does
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Acetylsalicylic acid/ aspirin
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What NSAID is used to prevent CV disease at low doses as well as cancer prevention
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Acetylsalicylic acid/aspirin
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What NSAID causes delirium.psychoses, vomitting, nausea, resp alkalosis, tinnitus at high doses
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Aspirin/acetylsalicylic acid
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In addition to anti-inflammatory, analgesic, and anti-pyretic activities, what else does ibuprofen and naproxen be used for?
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dysmenorrhea treatment
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Which NSAID can treat dysmenorrhea
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Ibuprofen and Naproxen
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What does indomethacin treat, in addition to anti-inflammatory, antipyretic, analgesic
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gout
and closes Ductus arteriosus |
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Which NSAID can treat gout and close a Ductus arteriosus
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Indomethacin
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What NSAIDS do not have all 3 of the properties: analgesic, anti-inflammatory, anti-pyretic
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ketorlac (isnt anti-inflammatory)
nabumetome (isnt anti-pyretic) |
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What is ketorlac mechanism of action
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Reversible cox inhibitor
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What does ketorlac do
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ketorlac is anti-pyretic and analgesic. It is NOT anti-inflammatory. It treats post operative pain
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Which NSAID is useful in treating post operative pain
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ketorlac
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How does piroxicam work?
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It is a reversible cox inhibitor
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What does piroxicam do in addition to its anti-inflammatory, anti-pyretic, and analgesic qualities
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Treats Osteoarthritis since it has a t1/2 of 50 hours!
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What drug can treat osteoarthritis because it has a half life of 50 hours
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Piroxicam
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What drug is a reversible cox inhibitor but has more action on cox 2 inhibition
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Nabumetone
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What does nabumetone treat
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NOT anti-pyretic
treats osteoarthritis and rheumatoid arthritis |
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What NSAID treats osteoarthritis and rheumatoid arthritis and inhibits cox 2 > cox 1
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Nabumetone
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What are the uses of celecoxib besides the standard ones?
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Rheumatoid and osteoarthritis
Primary dysmenorrhea Reduces polyp number in familial adenomatous polyposis |
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Which drug is used in treating familial adenomatous polypopsis
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Celecoxib
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What is celecoxib's mechanism of action
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Allosteric cox-2 inhibitor
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Which NSAID is an allosteric cox-2 inhibitor
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celecoxib
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What is acetaminophens mechanism of action
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Not really understood, but inhibits the reduction of COX enzyme to its peroxidase form (peroxidase form needed to make PGs)
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Which drug inhibits the reduction of COX enzyme to peroxidase form?
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Acetaminophen
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What are the therapeutic effects of acetaminophen
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Analgesic and antipyretic ONLY. NOT ANTIINFLAMMATORY!!!
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How to treat acetaminophen OD
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N-acetylcysteine
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What are the drugs used to treat Gout
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NSAIDS (indomethacin),
Colchicine, Allopurinol, Probenecid |
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How does Colchicine work?
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Treats gout by inhibiting inflammatory cells by interfering with microtubule formation.
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What is colchicine used for?
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Treatment of acute gout flares (if given in first few hours)
Otherwise prophylactic treatment of gout |
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What drug can treat gout by inhibiting inflammatory cells by inhibiting microtubule formation
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Colchicine
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What is allopurinol used to treat
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Treats chronic gout
Also prophylaxis in patients with leukemia to prevent gout development |
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How does allopurinol work
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Xanthine oxidase inhibitor (blocks uric acid synthesis)
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What drug blocks xanthine oxidase
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Allopurinol
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Which drug is given as prophylaxis during leukemia to prevent gout formation
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Allopurinol
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What is probenecid
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Treats chronic gout (not in patients with kidney stones); use colchicine to prevent this.
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How does probenacid work
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Probenacid is an organic acid transporter inhibitor (OAT)
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Which drug is an OAT inhibitor
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Probenecid
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Which drug do you not want to give to a patient who has kidney stones
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Probenecid.
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What does etanercept treat
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rheumatoid arthritis
crohns disease |
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How does etanercept work
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Etanercept treats RA and crohns by :
recombinant TNF receptor fusion protein with IgG -> binds TNF. |
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Which drug is a recombinant TNF receptor fusion protein with IgG ?
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Etanercept
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What is infliximab
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Treats rheumatoid arthritis
Crohns disease |
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How does infliximab work
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Monoclonal antibody against TNF alpha
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Which drug is a MAB against TNF-alpha
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Infliximab
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What drugs could you give to treat RA and crohns disease
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Etanercept
and Infliximab |
