AdultPediatricDosage Forms & Strengths tablet 62.5 mg 125 mg tablet, for oral suspension 32 mg Pulmonary Arterial Hypertension (PAH) Indicated to improve exercise ability and decrease worsening of PAH; effectiveness shown in NYHA II-IV, idiopathic or heritable PAH, connective tissue diseases that result in PAH, and PAH associated with congenital heart disease with left-to-right shunts <40 kg: Maintain dose at 62.5 mg PO q12hr >40 kg: 62.5 mg PO q12hr for 4 weeks and then increased to maintenance dosage 125 mg PO q12hr Discontinuation of treatment: Consider a reduction in dosage to 62.5 mg PO q12hr for 3-7 days See Administration Dosage Modifications Elevated ALT/AST levels Discontinue if elevated ALT/AST levels are accompanied with clinical symptoms of hepatotoxicity (eg, nausea, vomiting, fever, abdominal pain, jaundice, unusual lethargy, fatigue) or bilirubin ≥2X ULN; reintroduction studies have not been established Confirm test, if confirmed, reduce/hold dose as described below >12 years and >40 kg: Reduce dose to 62.5 mg PO q12hr or interrupt treatment and monitor liver tests at least q2weeks; if levels return to pretreatment values, continue or reintroduce treatment at 62.5mg PO q12hr; reassess levels within 3 days >5 and <8X ULN Interrupt treatment and monitor AST/ALT at least q2weeks >12 years and >40 kg: If levels return to pretreatment values, consider reintroducing dose to 62.5 mg PO q12hr; reassess levels within 3 days >8X ULN Stop treatment; reintroduction should not be considered Liver impairment Mild: No dose adjustment required Moderate or severe: Avoid use AST/ALT >3X ULN: Avoid use Coadministration with ritonavir Have been receiving ritonavir for at least 10 days: Initiate bosentan at the recommended starting dose qDay or every other day based on tolerability Have been receiving bosentan: Discontinue bosentan <36 hr prior to initiating ritonavir; resume bosentan at recommended initial dose qDay or every other day after at least 10 days of ritonavir treatment Idiopathic Pulmonary Fibrosis (Orphan) Orphan indication sponsor Actelion Pharmaceuticals Ltd; Gewerbestrasse 16, CH-4123; Switzerland Systemic Sclerosis (Orphan) Reduction of the number (treatment) of new digital ulcers in patients with systemic sclerosis Orphan indication sponsor Actelion Pharmaceuticals Ltd; Gewerbestrasse 16, CH-4123; Switzerland Dosage Strengths & Forms tablet, film-coated 62.5mg 125 mg tablet, for oral suspension 32 mg Pulmonary Arterial Hypertension (PAH) Indicated in children and adolescents aged ≥3 years with idiopathic or congenital PAH to improve pulmonary vascular resistance (PVR) See Administration <3 years: Safety and efficacy not established 3 to ≥12 years ≥4-8 kg: Maintain dose at 16 mg PO q12hr >8-16 kg: Maintain dose at 32 mg PO q12hr >16-24 kg: Maintain dose at 48 mg PO q12hr >24-40 kg: Maintain dose at 64 mg PO q12hr >12 years <40 kg: Maintain dose at 62.5mg PO q12hr >40 kg: 62.5mg PO q12hr initially for 4 weeks, then increase to maintenance dose 125 mg PO q12hr Dosage Modifications Discontinue if elevated ALT/AST levels are accompanied with clinical symptoms of hepatotoxicity (eg, nausea, vomiting, fever, abdominal pain, jaundice, unusual lethargy, fatigue) or bilirubin ≥2X ULN; reintroduction should not be considered Elevated ALT/AST levels Confirm test, if confirmed >3 and <5X ULN >12 years and >40 kg: Reduce dose to 62.5 mg PO q12hr or interrupt treatment and monitor liver tests at least q2weeks; if levels return to pretreatment values, continue or reintroduce treatment at 62.5mg PO q12hr; reassess levels within 3 days ≥3-12 years and <40 kg: Interrupt treatment; if levels return to pretreatment values, consider reintroduction of initial dose; reassess levels within 3 days >5 and <8X ULN Interrupt treatment and monitor AST/ALT at least q2weeks >12 years and >40 kg: If levels return to pretreatment values, consider reintroducing dose to 62.5 mg PO q12hr; reassess levels within 3 days ≥3-12 years and <40 kg: If levels return to pretreatment values, consider reintroduction of initial dose; reassess levels within 3 days >8X ULN Stop treatment; reintroduction should not be considered Coadministration with ritonavir Have been receiving ritonavir for at least 10 days: Initiate bosentan at the recommended starting dose qDay or every other day based on tolerability Have been receiving bosentan: Discontinue bosentan <36hr prior to initiation of ritonavir treatment; resume bosentan at recommended initial dose qDay or every other day after at least 10 days of ritonavir treatment Interaction CheckerEnter a drug name and bosentanNo Results No Interactions Found Interactions FoundContraindicatedSerious - Use AlternativeSignificant - Monitor CloselyMinorAll Interactions Sort By: SeverityName Contraindicated (23)artemether/lumefantrinebosentan will decrease the level or effect of artemether/lumefantrine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration with strong CYP3A4 inducers can result in decreased serum concentrations and loss of antimalarial efficacycariprazinebosentan will decrease the level or effect of cariprazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. CYP3A4 is responsible for the formation and elimination of cariprazine's active metabolites. The effect of CYP3A4 inducers on cariprazine exposure has not been evaluated and the net effect is unclear.cobimetinibbosentan will decrease the level or effect of cobimetinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Avoid coadministration. Strong or moderate CYP3A inducers may decrease cobimetinib systemic exposure by >80% and reduce its efficacy.cyclosporinecyclosporine will increase the level or effect of bosentan by Other (see comment). Contraindicated. may increase plasma concentrations of OATP substratesdienogest/estradiol valeratebosentan will decrease the level or effect of dienogest/estradiol valerate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Women should not choose estradiol valerate/dienogest as their contraceptive while using strong CYP3A4 inducers due to potential decrease in contraceptive efficacy. Estradiol valerate/dienogest should not be used for at least 28 days after discontinuation of the inducer due to possibility of decreased contraceptive efficacy. doravirinebosentan will decrease the level or effect of doravirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration of doravirine with a strong CYP3A inducer may decrease doravirine plasma concentrations and/or effects. Potential for loss of virologic response and possible resistance to doravirine. elvitegravir/cobicistat/emtricitabine/tenofovir DFbosentan decreases levels of elvitegravir/cobicistat/emtricitabine/tenofovir DF by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. May lead to loss of virologic response and possible resistance.fostemsavirbosentan will decrease the level or effect of fostemsavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration of fostemsavir (prodrug) with strong CYP3A4 inducers significantly decreases temsavir (active moiety) plasma concentrations, which may lead to loss of virologic response and resistance.glyburidebosentan, glyburide. Either decreases levels of the other by increasing metabolism. Contraindicated.bosentan, glyburide. Either increases toxicity of the other by Other (see comment). Contraindicated. Comment: Coadministration increases risk of liver enzyme elevations; alternative hypoglycemic agents should be considered.isavuconazonium sulfatebosentan will decrease the level or effect of isavuconazonium sulfate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.lonafarnibbosentan will decrease the level or effect of lonafarnib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Lonafarnib is a sensitive CYP3A4 substrate. Coadministration with strong or moderate CYP3A4 inducers is contraindicated.lorlatinibbosentan will decrease the level or effect of lorlatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration of lorlatinib with strong CYP3A inducers is contraindicated. Discontinue the strong CYP3A inducer for 3 plasma half-lives before initiating lorlatinib.lumacaftor/ivacaftorbosentan will decrease the level or effect of lumacaftor/ivacaftor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A inducers have minimal effect on lumacaftor exposure, but decreased ivacaftor exposure (AUC) by 57%. This may reduce the effectiveness of lumacaftor/ivacaftor. Therefore, coadministration is not recommended.lumefantrinebosentan will decrease the level or effect of lumefantrine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration with strong CYP3A4 inducers can result in decreased serum concentrations and loss of antimalarial efficacymavacamtenbosentan will decrease the level or effect of mavacamten by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.naloxegolbosentan will decrease the level or effect of naloxegol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of naloxegol with strong CYP3A4 inducers is not recommendedombitasvir/paritaprevir/ritonavir & dasabuvir (DSC)bosentan will decrease the level or effect of ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC) by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers may reduce partiaprevir and ritonavir levels, and therefore decreased efficacy of Viekira Pakpanobinostatbosentan decreases levels of panobinostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers can reduce panobinostat levels by ~70% and lead to treatment failure.praziquantelbosentan decreases levels of praziquantel by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP450 inducers significantly decrease praziquantel blood levels.regorafenibbosentan, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.roflumilastbosentan will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectivenesssparsentansparsentan, bosentan. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Coadministration of endothelin antagonists with sparsentan is associated with increased risks of hypotension, syncope, hyperkalemia, and changes in renal function (eg, acute renal failure).vandetanibbosentan decreases levels of vandetanib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Avoid coadministration with potent CYP3A4 inducers; these drugs reduce exposure to vandetanib by up to 40%.Serious - Use Alternative (130)abametapirabametapir will increase the level or effect of bosentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.abemaciclibbosentan will decrease the level or effect of abemaciclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of abemaciclib with strong CYP3A4 inducers reduces plasma concentration of abemaciclib and its metabolites.alpelisibbosentan will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.apalutamideapalutamide will decrease the level or effect of bosentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.apremilastbosentan will decrease the level or effect of apremilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration with strong CYP inducers results in a significant decrease of systemic exposure of apremilast, which may result in loss of efficacyatazanavirbosentan will increase the level or effect of atazanavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Do not coadminister unless atazanavir boosted with ritonaviravapritinibbosentan will decrease the level or effect of avapritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.axitinibbosentan decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.bedaquilinebosentan will decrease the level or effect of bedaquiline by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of bedaquiline with strong CYP3A4 inducers due to potential for decreased therapeutic effectbenzphetaminebosentan will decrease the level or effect of benzphetamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.bosutinibbosentan decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85% .brigatinibbosentan will decrease the level or effect of brigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration with strong CYP3A4 inducers may decrease brigatinib efficacy.cabozantinibbosentan will decrease the level or effect of cabozantinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of cabozantinib with strong CYP3A4 inducers. If a strong CYP3A4 inducer is required, increase cabozantinib dose by 40 mg/day (Cometriq) or by 20 mg/day (Cabometyx). Resume previous dose 2-3 days after strong CYP3A4 inducer discontinued.capmatinibbosentan will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.ceritinibbosentan decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.cobicistatcobicistat will increase the level or effect of bosentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Bosentan dose reduction requiredcopanlisibbosentan will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.cyclosporinecyclosporine will increase the level or effect of bosentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.dabrafenibbosentan decreases levels of dabrafenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.daridorexantbosentan will decrease the level or effect of daridorexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.darunavirbosentan will decrease the level or effect of darunavir by