{"id":4189,"date":"2025-03-31T18:12:00","date_gmt":"2025-03-31T18:12:00","guid":{"rendered":"https:\/\/kidneydiseaseclinic.net\/kdc\/mercaptopurine-txt\/"},"modified":"2025-03-31T18:12:00","modified_gmt":"2025-03-31T18:12:00","slug":"mercaptopurine-txt","status":"publish","type":"post","link":"https:\/\/kidneydiseaseclinic.net\/kdc\/mercaptopurine-txt\/","title":{"rendered":"Mercaptopurine.txt"},"content":{"rendered":"

CLINICAL USE <\/H3>
\nAntineoplastic agent:Acute leukaemias Inflammatory bowel disease (unlicensed)

DOSE IN NORMAL RENAL FUNCTION <\/H3>Usual dose is 2.5 mg\/kg\/day, but the dose and duration of administration depend on the nature and dosage of other cytotoxic agents given in conjunction

PHARMACOKINETICS <\/H3>
  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :170.2<\/li>\n
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :20<\/li>\n
  • %Excreted unchanged in urine &nbsp &nbsp : 7<\/li>\n

  • Volume of distribution (L\/kg) &nbsp &nbsp &nbsp :0.1\u20131.7<\/li>\n

  • half-life \u2013 normal\/ESRD (hrs)&nbsp &nbsp &nbsp :1\u20131.5\/\u2013

    DOSE IN RENAL IMPAIRMENT <\/H3>

    GFR (mL\/MIN)<\/H4>
  • 20 to 50 &nbsp &nbsp : Caution \u2013 reduce dose.
  • 10 to 20 &nbsp &nbsp : Caution \u2013 reduce dose.
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : Caution \u2013 reduce dose.

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES <\/H3>
  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR <10 mL\/min <\/p>\n
  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Dialysed. Dose as in GFR
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL\/min
  • HDF\/high flux &nbsp :Dialysed. Dose as in GFR
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL\/min
  • CAV\/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR 10 to 20 mL\/min

    IMPORTANT DRUG INTERACTIONS <\/H3>Potentially hazardous interactions with other drugsAllopurinol: decreased rate of metabolism of mercaptopurine \u2013 reduce dose of mercaptopurine to a quarter of normal dose\n
  • Antibacterials: increased risk of haematological toxicity with co-trimoxazole and trimethoprim\n
  • Anticoagulants: possibly reduced anticoagulant effect of coumarins\n
  • Antipsychotics: avoid concomitant use with clozapine (increased risk of agranulocytosis)

    ADMINISTRATION <\/H3>

    Reconstition<\/H4>\u2013

    Route <\/H4>Oral

    Rate of Administration <\/H4>\u2013

    Comments<\/H4>\u2013

    OTHER INFORMATION <\/H4>Absorption of an oral dose is incomplete, averaging ~50%. This is largely due to first pass metabolism in the liver (less when given with food). There is enormous inter-individual variability in absorption, which can result in a 5-fold variations in AUCIt is extensively metabolised (by intracellular activation). At conventional doses clearance is primarily hepatic. Renal clearance may become important at high dosesThe active metabolites have a longer half- life than the parent drugWellcome UK recommend consideration be given to reducing the dose in patients with impaired hepatic or renal function, although no specific dosing guidelines are availableWith renal impairment, the following dosing intervals have been suggested: 24\u201336 hrs for CrCl of 50\u201380 mL\/min, and 48 hrs for CrCl of 10\u201350 mL\/min. (Summerhayes M, Daniels S (eds). Practical Chemotherapy \u2013 A Multidisciplinary guide. 1st ed. Abingdon: Radcliffe Medical Press Ltd. 2003. p. 384)A recent study on anti-cancer drug renal toxicity and elimination concluded that the dose of 6-mercaptopurine does not require modification in patients with decreased renal function (except in conjunction with allopurinol). This study also gives % excreted unchanged in urine as 21%.
    \n","protected":false},"excerpt":{"rendered":"

    CLINICAL USE Antineoplastic agent:Acute leukaemias Inflammatory bowel disease (unlicensed) DOSE<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"","ping_status":"","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[1],"tags":[7],"class_list":["post-4189","post","type-post","status-publish","format-standard","hentry","category-blog","tag-post-by-auto-php"],"_links":{"self":[{"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/posts\/4189","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/comments?post=4189"}],"version-history":[{"count":0,"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/posts\/4189\/revisions"}],"wp:attachment":[{"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/media?parent=4189"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/categories?post=4189"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/tags?post=4189"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}