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34 Cards in this Set

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  • Back
Mycophenolate Mofetil
converted to MPA to inhibit IMPDH, dec. guanine, inc. adenosine

lowers adhesion molecules, apoptosis in activated T-cells

prevent acute organ transplant rejection (better than AZA), RA, lupus nephritis, psoriasis
Sodium Mycophenolate
converted to MPA to inhibit IMPDH, dec. guanine, inc. adenosine

lowers adhesion molecules, apoptosis in activated T-cells

prevent acute organ transplant rejection (better than AZA), RA, lupus nephritis, psoriasis
Azathioprine
6-MP prodrug, inhibits IMP conversion to IMODH and forms 6-TG to disrupt DNA synthesis dec. IgG and IL-2

renal transplant (worse than MMF), RA, lupus, Behcet's disease

slow release, so less toxic and longer lasting
6-Mercaptopurine
inhibits IMP conversion to IMODH and forms 6-TG to disrupt DNA synthesis dec. IgG and IL-2

renal transplant (worse than MMF), RA, lupus, Behcet's disease

Preferred as anti-neoplastic
Methotrexate
Inhibits DHFR to stop denovo purine synthesis, adenosine builds up, apoptosis in T-cells and dec. adhesion

RA and psoriasis

careful in liver disease & alcoholism
Leflunomide
Inhibits pyrimidine synthesis and blocks dihydroorotate dehydrogenase to dec B and T cells

RA
Cyclophosphamide
alkylates DNA to decrease B-cells but inc. T-cell proliferation

systemic lupus
Cyclosporine A
Inhibits calcineurin, no NFAT phosphorylation and no IL-2 production and blunts anti-apoptotic proteins

organ transplant, psoriasis, RA, keratoconjunctivitis sicca
Tacrolimus
Inhibits calcineurin, no NFAT phosphorylation and no IL-2 production and blunts anti-apoptotic proteins and binds FKBP to inhibit inflammatory mediators

organ transplant, eczema

50-100x more potent than CSA
Everolimus
binds FKBP and inhibits mTOR, T-cell arrests in G1, IL-2 is inhibited

kidney/liver transplants
Sirolmus
binds FKBP and inhibits mTOR, T-cell arrests in G1, IL-2 is inhibited

organ transplant, CAD elutingstent

NO nephrotoxicity
Etanercept
TNF-alpha and beta inhibitor through complement activation fusion protein

RA, PSA, kids >2 yo, plaque psoriasis, spondylitis
Infliximab
Chimeric IgG mAb TNF-a inhibitor through complement activation

RA, plaque psoriasis, spondylitis, Chron's
Adalimumab
Recombinant IgG mAb TNF-a inhibitor through complement activation

RA, PSA, kids >4 yo, plaque psoriasis, spondylitis, chron's
Golimumab
Recombinant IgG mAb TNF-a inhibitor NO compliment activation

RA, PSA, spondylitis

***CAN use with other non-biologic DMARDS, NSAIDS, corticosteroids
Certolizumab Pegol
Recombinant humanized Fab fragment from e. coli NO complement activation

RA and Chron's disease
Tocilizumab
recombinant IL-6

RA, kids >2 yo

**monitor LFT, platelets, neurtophils, lipids
Anakinra
Recombinant IL-1 from e. coli blocks IL-1b from accessing receptor

RA, CAPS, NOMID, dec. bony erosions
Rilonacept
Fusion protein of IL-1 and IgG

CAPS, FCAS, MWS, kids >12 yo

**monitor lipids, LFT's
Canakinumab
Recombinant anti-human IL-1 mAb

CAPS, FCAS, MWS, kids >4 yo

**monitor LFT's
Ustekinumab
Human IgG 1a mAb, preventing IL-12 & 2 activity

plaque psoriasis
Tofacitinib
JAK 1&3 inhibitor to block IL 2,4,7,9,15,21

RA pts intolerant to MTX

***monitor LFT, platelets, neutrophils, lipids
Belimumab
Human IgG gamma, blocks BLyS and BAFF

systemic lupus

***WORSE than Rituximab
Antithymocyte Globulin (ATG)
gamma globulin from human thymocytes in all T-cells

organ transplant

can cause cytokine release syndrome
Muromonab CD3
mouse mAb, binds e-chain to activate complement and phagocytosis of T-cells

2nd line organ transplant when CSA fails

**cytokine release syndrome
Rituximab
chimeric antibody to CD on B-cells causing lysis

2nd line RA

less risk of infection
Basiliximab
chimeric blocker of CD25 on T-cells with MHC antigen stimulation

Acute organ rejection prophylaxis w/ CSA/glucocorticoids
Daclizumab
humanized blocker of CD25 on T-cells with MHC antigen stimulation

Acute organ rejection prophylaxis w/ CSA/glucocorticoids
Alemtuzumab
humanized, binds CD52 on T&B cells

lymphocytic leukemia
Alefacept
human fusion binds CD2 to inhibit T-cells

plaque psoriasis
Abatecept
binds B7 on APC to block T-cell activation

RA
Efalizumab
no longer allowed in US
Natalizumab
humanized, inhibits movement of immune cells to inflammed site

VCAM-1 is MS madCAM-1 is Chrons

causes PML blackbox
Eculizumab
blocks C5 and MAC to decrease lysing of RBC's

PNH, atypical hemolytic-uremic syndrome