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32 Cards in this Set

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synth by fungus, has 9-carbon novel amino acid at position 1, where hydrogen bonds are formed.
Cyclosporine Mech of action
binds cyclophilin. The cyclosporin-cyclophilin complex then binds calcineurin, causing its inactivation, which is not then able to dephosphorylate NFAT, so NFAT can't enter the nucleus and IL-2 gene is not transcribed.
So Cyclosporine causes immunosupression how?
Since NFAT isn't able to turn on the IL-2 gene, there is low IL-2. IL-2 otherwise would cause CD4 and CD8 T cell proliferation.

So, it INHIBITS activatin and proliferation of T Cells.
Cyclosporine Metabolism
CYP3A4, largely hepatic. Increased clearance with phenytoin, phenobarbital. Decrease clearance with erythromycin, ketoconazole, amphotericin B or St John's wart.//

VERY narrow TI
Cyclosporine Toxicity
nephrotox, neurotox (tremor), hypertension, hirsutism, hyperlipidemia, gingival hyperplasia.
Tacrolimus (FK506)
a lactone-lactam antibiotic, structurally unrelated to cyclosporine, 50-100x more potent than cyclosporine, les nephrotoxicity. Also used topically to treat atopic dermatitis.//
Tacrolimus: Mech of action
It inactivates calcineurine by forming Tacrolimus-FKBP complex and binding calcineurin, unlike cyclosporine which binds 'cyclophilin'. The rest of the down stream consequence is the same, where then, calcineurin cannot be activated by calmodulin, thus no NFAT dephosphorylation and low IL-2 gene transcription.//
Tacrolimus: Pharmacology
used as prophylaxis after kidney and liver transplants, also as rescue therapy in pts experiencing graft rejections.//

Metabolized in liver, shorter half life than cyclosporine.//
Tacrolimus: Toxicity
nephro, neuro (tremor, headache, seizures, insomnia), GI disturbances, hyperglycemia, pancreatic beta cell function inhibition. INCREASED RISK OF malignant lymphomas.//
similar to tacrolimus, binds FKBP, used for topical treatment of atopic dermatitis. 2nd line b/c skin cancer risk
structurally related to tacrolimus. Mech: binds FKBP, which (this complex) then inhibits mTOR > no dephosphorylation and no transcription of IL-2 gene.

Inhibition of mTOR results in lack of response to growth stim. factors AND inhibition of T and B cell proliferation.
Sirolimus Pharmacology
metabolized by CYP3A4, same as cyclosporine and tacrolimus. Used as part of combo tx for renal transplant, and with islet cell transplantation.//

Has been used with stents in coronary arteries to prevent neointimal proliferation. *NOW WE THINK IT MAY NOT BE A GOOD THING*
Sirolimus Tox
anemia, thrombocytopenia, hyperlipidemia.

Mycophenolate mofetil
prodrug metabolized by liver to mycophenolic acid (MPA). Useful in pts in combo with cyclosporine or tacrolimus.
Mech of action of mycophenolate mofetil
once converted to MPA, it inhibits inosine monophosphate dehydrogenase, which is required for de novo PURINE synthesis. For B and T cells, the major source of PURINE is de novo synthesis instead of HPRT mediated salvage.
Mycophenolate mofetil pharmacology
recom. after renal and heart transplantation.//

Decrease absorption with mg or Al (so don't use these antacids).//

side effects: diarrhea, leakopenia
inhibits dihydroorotate dehydrogenase, essential for PYRIMIDINE biosynthesis.

EFFECTIVE in rheumatoid arthritis.
used for tx of erythema nodosum leprosum (type 2 leprosy rxn). Side effects: peripheral neuropathy. TERATOGENIC, NEVER use in pregnant women.
daclizumab and basiliximab
Ab against IL-2 receptor's (CD25) alpha chain > inhibits T cell activation. reduces incidence of acute rejection
Ab against epsilon chain of CD3 on T cell surface, blocks T cell receptor engagement. Indication: reversal of rejection of heart, liver and kidney transplant
Ab against TFNalpha. Tx of Crohn's dz, UC, rheumatoid and psoriatic arthritis, and ankylosing spondylitis.

Side effects: TB REACTIVATION, Hep B reactivatin, malignancies, heptotoxicities. anti-infliximab AB devp
chimeric recombinant of soluble p75-TFN receptor type II and Fc portion of human IgG. Acts by "soaking up" the free TNF.//

Used in RA, ankylosing spondylitis and plaque psoriasis.//

causes increase incidence of demyelinating dzs.
Ab against alpha4 subunit of Integrin. Inhibits lymphocyte migration to sites of inflamation. Used in Crohn's dz and MS. Use associated with PML.
Ab against CD11a, a subunit of LFA-1.

For tx of plaque psoriasis, blocks T Cell activation.
binds CD80 and CD86, blocking their binding to CD28 and T Cell activation. Works upstream from infliximab and etanercept.
purine analog, metabolized to 6-mercaptopurine, disrupts de no purine synthesis, and disrupts transcription when incorporated into DNA.

Used for RA in combo with cyclosporine,/tacrolimus plus prednisone.
antigenically similar to myelin basic protein, used for tx of remitting-relapsing MS.
Lymphocyte IGs: Ab to T cell surface Ag, depletes T Cells
IFN alpha
2a: hep C, KS, CML, hair cell leukemia.

2b: hep B, C and several malignancies.

n1, alfacon-1: Hep C

n3: chondyloma accuminata
IFN beta
1a, 1b: MS
IFN gamma
for chronic granulomatous dz and congenital osteopetrosis.

stim. of cytokine and IFN alpha synthesis. for tx of genital warts and actinic keratosis.