Azathioprine Chapter 14

shevyatiwari's version from 2015-04-19 09:07


Question Answer
Azathioprine is the prodrug of 6-MPT
Azathioprine's absorption is 50%F. >88%
Azathioprine is similar to Mtx and does not cross the BBBT
Azathioprine does not cross the placentaF
Peak plasma levels occur in 0.75 hoursF 2 hours
The metabolism of Azt is slowF
6-TG is not activeF, is the active metabolite
Maximum clinical immunosuppression is 6 weeksF. 8-12 weeks
Azathioprine is rapidly converted to 6-TG on absorptionF. To 6-MP
Azathioprine is converted to 6-TG in erythrocytesF. To 6-MP
Azt is converted to 6-TG by TPMTF. HGPRT
Art's pathway via TPMP produces inactive metabolitesT
Azt's pathway via XO produces inactive metabolitesT
6-TG, diphosphate and triphosphate metabolites are all activeT
Azt is 30% protein boundT
Allopurinol or febuxostat require a 75% dose reduction of aztT
Azt is similar to endogenous purinesT
Azt has no effect on T cell but does affect B cell functionF. Affects both as well as antigen presenting cell
Azt is FDA approved for psoriasisF. No dermatological FDA approved indications
Azt is C/I in pregnancy T
Azt is cat xF. D
Active infections are a relative C/IF. Absolute
Previous use of alkylating agents is a relative C/I to aztT
Increased risk of lymphoproliferative malignancyT
No increased risk of NMSCSF
Severe myelosuppression is a common S/EF, rare
Live vaccines should not be administeredT
Azt is found in breastmilkT
Azt drug hypersensitivity is characterised by CV collapse, cutaneous eruptions, fever, leukocytosis, GI discomfort, pancreatitis, arthralgia, myalgia, rhabdo, headaches, renal impairment, respiratory involvementT
The cutaneous eruption of Azt hypersensitivity includes macular erythema, maculopapular, macular eruptions with vesicles and pustules, purpuric or petechialT
Hypersensitivity reactions occur after 4 weeks of therapyF. 1-4 weeks
Cyclosporin or Mtx increases the likelihood of hypersensitivity syndromeT
Rechallenge post azt hypersensitivity is the best diagnostic toolF. C/I
GI effects are the most common S/E of aztT
Taking azt with food helps manage GI S/ET
Life threatening LFT derangement is uncommonT
ACE inhibitors interact with AztT. Increase risk of leukpenia
Warfarin interacts with AztT. less effective
Sulfasalazine inhibits TPMPTT. Increased risk of toxicity
Pancuronium requirements are lower in those on AztF. Higher
Cotrimoxazole and penicillamine can cause increased hepatotoxicity in those taking AztF. Increased haematological toxicity
Cyclosporine levels are increased with concomitant useF, decreased
Half life of 5 hoursT

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