{"id":1681,"date":"2023-06-25T17:31:26","date_gmt":"2023-06-25T17:31:26","guid":{"rendered":"https:\/\/kidneydiseaseclinic.net\/kdc\/bosentan\/"},"modified":"2023-06-25T19:46:27","modified_gmt":"2023-06-25T19:46:27","slug":"bosentan","status":"publish","type":"post","link":"https:\/\/kidneydiseaseclinic.net\/kdc\/bosentan\/","title":{"rendered":"Bosentan"},"content":{"rendered":"

<\/p>\n

Bosentan<\/h1>\n

CLINICAL USE<\/h3>\n

Treatment of primary arterial pulmonary hypertension (PAH), and PAH secondary to scleroderma without significant interstitial pulmonary disease<\/p>\n

DOSE IN NORMAL RENAL FUNCTION<\/h3>\n

62.5\u2013250 mg twice daily<\/p>\n

PHARMACOKINETICS<\/h3>\n
  • Molecular weight                           :551.6<\/li>\n
  • %Protein binding                           :>98<\/li>\n
  • %Excreted unchanged in urine     : <3<\/li>\n
  • Volume of distribution (L\/kg)       :18 litres<\/li>\n
  • half-life \u2013 normal\/ESRD (hrs)      :5\u20138\/Unchanged
    \n

    DOSE IN RENAL IMPAIRMENT<\/h3>\n

    GFR (mL\/MIN)<\/h4>\n<\/li>\n
  • 20 to 50     : Dose as in normal renal function<\/li>\n
  • 10 to 20     : Dose as in normal renal function<\/li>\n
  • <10           : Dose as in normal renal function
    \n

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES<\/h3>\n<\/li>\n
  • CAPD                :Not dialysed. Dose as in normal renal function<\/li>\n
  • HD                     :Not dialysed. Dose as in normal renal function<\/li>\n
  • HDF\/high flux   :Not dialysed. Dose as in normal renal function<\/li>\n
  • CAV\/VVHD      :Not dialysed. Dose as in normal renal function
    \n

    IMPORTANT DRUG INTERACTIONS<\/h3>\n

    Potentially hazardous interactions with other drugs<\/li>\n

  • Antibacterials: concentration reduced by rifampicin \u2013 avoid concomitant use<\/li>\n
  • Antidiabetics: increased risk of hepatoxicity with glibenclamide \u2013 avoid concomitant useAntifungals: fluconazole, ketoconazole and itraconazole cause large increases in plasma concentrations of bosentan \u2013 avoid concomitant useAntivirals: ritonavir causes greatly increased bosentan levels \u2013 avoid concomitant use<\/li>\n
  • Ciclosporin: co-administration of ciclosporin and bosentan is contraindicated. When ciclosporin and bosentan are co-administered, initial trough concentrations of bosentan are 30 times higher than normal. At steady state, trough levels are 3\u20134 times higher than normal. Blood concentrations of ciclosporin decreased by 50%<\/li>\n
  • Lipid lowering agents: concentration of simvastatin reduced by 45% \u2013 monitor cholesterol levels and adjust dose of statin<\/li>\n
  • Oestrogens and progestogens: may be failure of contraception \u2013 use alternative method
    \n

    ADMINISTRATION<\/h3>\n

    Reconstition<\/h4>\n

    \u2013<\/p>\n

    Route<\/h4>\n

    Oral<\/p>\n

    Rate of Administration<\/h4>\n

    \u2013<\/p>\n

    Comments<\/h4>\n

    \u2013<\/p>\n

    OTHER INFORMATION<\/h4>\n<\/li>\n
  • Bosentan should only be used if the systemic systolic blood pressure is >85 mm\/Hg<\/li>\n
  • Treatment with bosentan is associated with a dose-related, modest decrease in haemoglobin concentration<\/li>\n
  • Bosentan is an inducer of CYP 3A4 and CYP 2C9Bosentan has been associated with dose-related elevations in liver aminotransferases<\/li>\n
  • Side effects include leg oedema and hypotension<\/li>\n","protected":false},"excerpt":{"rendered":"

    Bosentan CLINICAL USE Treatment of primary arterial pulmonary hypertension (PAH),<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[1],"tags":[7],"class_list":["post-1681","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\/1681","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=1681"}],"version-history":[{"count":1,"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/posts\/1681\/revisions"}],"predecessor-version":[{"id":2863,"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/posts\/1681\/revisions\/2863"}],"wp:attachment":[{"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/media?parent=1681"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/categories?post=1681"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/tags?post=1681"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}