{"id":3752,"date":"2025-03-31T18:11:49","date_gmt":"2025-03-31T18:11:49","guid":{"rendered":"https:\/\/kidneydiseaseclinic.net\/kdc\/bosentan-txt\/"},"modified":"2025-03-31T18:11:49","modified_gmt":"2025-03-31T18:11:49","slug":"bosentan-txt","status":"publish","type":"post","link":"https:\/\/kidneydiseaseclinic.net\/kdc\/bosentan-txt\/","title":{"rendered":"Bosentan.txt"},"content":{"rendered":"

Bosentan<\/h1>\n

CLINICAL USE <\/H3>
\nTreatment of primary arterial pulmonary hypertension (PAH), and PAH secondary to scleroderma without significant interstitial pulmonary disease

DOSE IN NORMAL RENAL FUNCTION <\/H3>62.5\u2013250 mg twice daily

PHARMACOKINETICS <\/H3>
  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :551.6<\/li>\n
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :>98<\/li>\n
  • %Excreted unchanged in urine &nbsp &nbsp : <3<\/li>\n

  • Volume of distribution (L\/kg) &nbsp &nbsp &nbsp :18 litres<\/li>\n

  • half-life \u2013 normal\/ESRD (hrs)&nbsp &nbsp &nbsp :5\u20138\/Unchanged

    DOSE IN RENAL IMPAIRMENT <\/H3>

    GFR (mL\/MIN)<\/H4>
  • 20 to 50 &nbsp &nbsp : Dose as in normal renal function
  • 10 to 20 &nbsp &nbsp : Dose as in normal renal function
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES <\/H3>
  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Not dialysed. Dose as in normal renal function<\/p>\n
  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in normal renal function
  • HDF\/high flux &nbsp :Not dialysed. Dose as in normal renal function
  • CAV\/VVHD &nbsp &nbsp &nbsp:Not dialysed. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS <\/H3>Potentially hazardous interactions with other drugs\n
  • Antibacterials: concentration reduced by rifampicin \u2013 avoid concomitant use\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\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%\n
  • Lipid lowering agents: concentration of simvastatin reduced by 45% \u2013 monitor cholesterol levels and adjust dose of statin\n
  • Oestrogens and progestogens: may be failure of contraception \u2013 use alternative method

    ADMINISTRATION <\/H3>

    Reconstition<\/H4>\u2013

    Route <\/H4>Oral

    Rate of Administration <\/H4>\u2013

    Comments<\/H4>\u2013

    OTHER INFORMATION <\/H4>\n
  • Bosentan should only be used if the systemic systolic blood pressure is >85 mm\/Hg\n
  • Treatment with bosentan is associated with a dose-related, modest decrease in haemoglobin concentration\n
  • Bosentan is an inducer of CYP 3A4 and CYP 2C9Bosentan has been associated with dose-related elevations in liver aminotransferases\n
  • Side effects include leg oedema and hypotension
    \n","protected":false},"excerpt":{"rendered":"

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