Cyclosporine 16

shevyatiwari's version from 2015-08-13 13:40

Section 1

Question Answer
CsA cytotoxic, does not suppress bone marrow and is not teratogenic ?F. NOT cytotoxic, does NOT suppress bone marrow and NOT teratogenic
Neoral less bioavailable and less well absorbed microemulsion form of CsA?F. More bioavailable and more consistently absorbed form of CsA
Neutral cyclic peptide composed of 12 amino acids?F. Neutral cyclic polypeptid composed of 11 amino acids
Should be diluted in grapefruit juice to aid absorption?F. Grapefruit juice intereferes with metabolism . Dilute in OJ or apple juice
Neoral immediately forms a microemulsion in an aqueous enviroment?True
Sandimmune bioavailability equal to Neoral?False. Neoral 10-54% greater bioavailable
Neoral is predigested form of CsA?True
Neoral more dependent on bile, food, diet and GI tract for proper absorption?False. Neoral pregdigested form - LESS dependent on bile/food/diet/GIT for absorption
CsA not excreted in human breast milk?False: Excreted in breast milk. AVOID while breastfeeding
Generic CsA is bioequivalent to gengraf and neoralTrue

Section 2

Question Answer
CsA extensively metabolised by Cytochrome P450 in the liver?True
Primarily renally excreted?False. Primarily bile through faeces only 6% urine (parent drug and metabolites)
Hepatic insufficency does not effect half life?F. May prolong half life and requires dosage adjustment
Effect on T lymphocytes important for psorisis treatment?True
Acts via inhibition of intracellular enzyme calcineurin?True. CsA forms a complex with cyclophilin and inhibits calcineurin
Calcineurin inhibition leads to increased activity of transcription factor NFAT -1 ?F. DECREASED ACTIVITY OF NFAT-1
Inhibits the production of IL-6 by inhibiting calcineurin?F Inhibits production of IL-2 by inhibiting calcineurin
Inhibition of IL-2 causes increased T-cell proliferation upon activation? F. Inhibition of IL-2 causes DECREASED T-cell proliferation
Calcineurin inhibition leads to reduced activity of NFAT-1 and inhbitis T cell proliferation?True
Inhibits IFN-alpha production by T-lympohcytes F . Inhibits IFN-GAMMA production by t -lymphocytes. Reduced HLA-DR positivity and reduced keratinocyte proliferation
Binds to steroid receptor associated heat-shcok protein 56?Ttrue. inhibits transcription of pro-inflamm cytokines eg. GM-CSF, il1, il-3, 4, 5, 6, 8, NOT il2
Does not affect antigen presenting cells eg, langerhans, mast and keratinocytes?F. DOES affect APC'S

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