AdultPediatricDosage Forms & Strengths tablet 5mg 10mg Pulmonary Arterial Hypertension Indicated for treatment of pulmonary arterial hypertension (PAH) (WHO Group 1) to improve exercise ability and delay clinical worsening or in combination with tadalafil to reduce the risks of disease progression and hospitalization for worsening PAH, and to improve exercise ability Initiate treatment at 5 mg PO qDay, with or without tadalafil 20 mg PO qDay At 4-week intervals, either ambrisentan or tadalafil dose can be increased, as needed and tolerated, not to exceed ambrisentan 10 mg/day or tadalafil 40 mg/day Dosage Modifications Coadministration with cyclosporine: Limit ambrisentan to 5 mg/day Renal impairment Mild-to-moderate: No dosage adjustment required Severe: Not studied Hemodialysis: Not studied Hepatic impairment Pre-existing Mild: No information available Moderate-to-severe: Not recommended Elevated LFTs after initiating LFTs >5x ULN: Discontinue LFTs increased and accompanied by bilirubin >2x ULN (or signs/symptoms of liver dysfunction): Discontinue Dosing Considerations Studies establishing effectiveness included predominantly patients with WHO functional Class II–III symptoms and etiologies of idiopathic or heritable PAH (60%) or PAH associated with connective tissue diseases (34%) Initiate treatment with ambrisentan in females of reproductive potential only after a negative pregnancy test; obtain monthly pregnancy tests during treatmentSafety and efficacy not establishedInteraction CheckerEnter a drug name and ambrisentanNo Results No Interactions Found Interactions FoundContraindicatedSerious - Use AlternativeSignificant - Monitor CloselyMinorAll Interactions Sort By: SeverityName Contraindicated (1)sparsentansparsentan, ambrisentan. 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).Serious - Use Alternative (9)apalutamideapalutamide will decrease the level or effect of ambrisentan by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP2C19 inducer, with drugs that are CYP2C19 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.apalutamide will decrease the level or effect of ambrisentan 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.cyclosporinecyclosporine will increase the level or effect of ambrisentan by Other (see comment). Avoid or Use Alternate Drug. may increase plasma concentrations of OATP substratesidelalisibidelalisib will increase the level or effect of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrateslasmiditanlasmiditan increases effects of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.leniolisibleniolisib will increase the level or effect of ambrisentan by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates lonafarniblonafarnib will increase the level or effect of ambrisentan by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Lonafarnib may increase the AUC and peak concentration of CYP2C19 substrates. If coadministration unavoidable, monitor for adverse reactions and reduce the CYP2C19 substrate dose in accordance with its approved product labeling.sotorasibsotorasib will decrease the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If use is unavoidable, refer to the prescribing information of the P-gp substrate for dosage modifications.tepotinibtepotinib will increase the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If concomitant use unavoidable, reduce the P-gp substrate dosage if recommended in its approved product labeling.trofinetidetrofinetide will increase the level or effect of ambrisentan by Other (see comment). Avoid or Use Alternate Drug. Trofinetide (an OATP131 and OATP13B inhibitor) may increase plasma levels of OATP131 or OATP13B substrates. Avoid coadministration with sensitive substrates.Monitor Closely (36)apalutamideapalutamide will decrease the level or effect of ambrisentan by increasing elimination. Use Caution/Monitor. Apalutamide weakly induces OATP1B1 and may decrease systemic exposure of drugs that are OATP1B1 substrates.bazedoxifene/conjugated estrogensambrisentan will increase the level or effect of bazedoxifene/conjugated estrogens by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.ambrisentan will increase the level or effect of bazedoxifene/conjugated estrogens by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.berotralstatberotralstat will increase the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor or titrate P-gp substrate dose if coadministered.cannabidiolcannabidiol will increase the level or effect of ambrisentan by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider reducing the dose of sensitive CYP2C19 substrates, as clinically appropriate, when coadministered with cannabidiol. cenobamatecenobamate will increase the level or effect of ambrisentan by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider a dose reduction of CYP2C19 substrates, as clinically appropriate, when used concomitantly with cenobamate. conjugated estrogensambrisentan will increase the level or effect of conjugated estrogens by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.ambrisentan will increase the level or effect of conjugated estrogens by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.conjugated estrogens, vaginalambrisentan will increase the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.ambrisentan will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.crofelemercrofelemer increases levels of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Crofelemer has the potential to inhibit CYP3A4 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.cyclosporinecyclosporine will increase the level or effect of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. 2-fold increase in ambrisentan exposure; limit ambrisentan dose to 5 mg/day when coadministered with cyclosporinedabrafenibdabrafenib will decrease the level or effect of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.elagolixelagolix will increase the level or effect of ambrisentan by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak CYP2C19 inhibitor. Caution with sensitive CYP2C19 substrates.elagolix will increase the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.eliglustateliglustat increases levels of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Monitor therapeutic drug concentrations, as indicated, or consider reducing the dosage of the P-gp substrate and titrate to clinical effect.elvitegravir/cobicistat/emtricitabine/tenofovir DFelvitegravir/cobicistat/emtricitabine/tenofovir DF increases effects of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Cobicistat is a CYP3A4 inhibitor; contraindicated with CYP3A4 substrates for which elevated plasma concentrations are associated with serious and/or life-threatening events.encorafenibencorafenib will increase the level or effect of ambrisentan by Other (see comment). Modify Therapy/Monitor Closely. Encorafenib (a OATP1B1 inhibitor) may increase the concentration and toxicities of OATP1B1 substrates. Closely monitor for signs and symptoms of increased exposure and consider adjusting the dose of these substrates.eslicarbazepine acetateeslicarbazepine acetate will increase the level or effect of ambrisentan by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.etonogestrelambrisentan will increase the level or effect of etonogestrel by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.fedratinibfedratinib will increase the level or effect of ambrisentan by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP2C19 substrates as necessary.fexinidazolefexinidazole will increase the level or effect of ambrisentan by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.fostamatinibfostamatinib will increase the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Concomitant use of fostamatinib may increase concentrations of P-gp substrates. Monitor for toxicities of the P-gp substrate drug that may require dosage reduction when given concurrently with fostamatinib.fostemsavirfostemsavir will increase the level or effect of ambrisentan by Other (see comment). Modify Therapy/Monitor Closely. Fostemsavir inhibits OATP1B1/3 transporter. If possible, avoid coadministration or modify dose of OATP1B1/3 substrates coadministered with fostemsavir. glecaprevir/pibrentasvirglecaprevir/pibrentasvir will increase the level or effect of ambrisentan by Other (see comment). Use Caution/Monitor. Coadministration with glecaprevir/pibrentasvir may increase plasma concentration of drugs that are substrates of OATP1B1 or OATP1B3glecaprevir/pibrentasvir will increase the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely.iloperidoneiloperidone increases levels of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Iloperidone is a time-dependent CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by CYP3A4.istradefyllineistradefylline will increase the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of P-gp substrates in clinical trials. Consider dose reduction of sensitive P-gp substrates.ivacaftorivacaftor increases levels of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Ivacaftor and its M1 metabolite has the potential to inhibit P-gp; may significantly increase systemic exposure to sensitive P-gp substrates with a narrow therapeutic index.letermovirletermovir increases levels of ambrisentan by Other (see comment). Use Caution/Monitor. Comment: Letermovir, an OATP1B1/3 inhibitor may increase plasma concentrations of coadministered OATP1B1/3 substrates.lumacaftor/ivacaftorlumacaftor/ivacaftor, ambrisentan. affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. In vitro studies suggest that lumacaftor may induce and ivacaftor may inhibit CYP2C19 substrates. .mitotanemitotane decreases levels of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.ponatinibponatinib increases levels of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.rifampinrifampin will decrease the level or effect of ambrisentan by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.rifampin will decrease the level or effect of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration was associated with a transient 2-fold increase in ambrisentan AUC; however, by day 7, rifampin had no clinically important effect on ambrisentan. Use with caution.rucaparibrucaparib will increase the level or effect of ambrisentan by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP2C19 substrates, if clinically indicated.sarecyclinesarecycline will increase the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor for toxicities of P-gp substrates that may require dosage reduction when coadministered with P-gp inhibitors.sofosbuvir/velpatasvirsofosbuvir/velpatasvir increases levels of ambrisentan by Other (see comment). Use Caution/Monitor. Comment: Velpatasvir inhibits OATP1B1, OATP1B3, and OATP2B1 transporters. .stiripentolstiripentol will increase the level or effect of ambrisentan by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider reducing the dose of CYP2C19 substrates, if adverse reactions are experienced when administered concomitantly with stiripentol.stiripentol will increase the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Consider reducing the dose of P-glycoprotein (P-gp) substrates, if adverse reactions are experienced when administered concomitantly with stiripentol.tecovirimattecovirimat will increase the level or effect of ambrisentan by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Tecovirimat is a weak inhibitor of CYP2C8 and CYP2C19. Monitor for adverse effects if coadministered with sensitive substrates of these enzymes.triclabendazoletriclabendazole will increase the level or effect of ambrisentan by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. If plasma concentrations of the CYP2C19 substrates are elevated during triclabendazole, recheck plasma concentration of the CYP2C19 substrates after discontinuation of triclabendazole. tucatinibtucatinib will increase the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Consider reducing the dosage of P-gp substrates, where minimal concentration changes may lead to serious or life-threatening toxicities.Minor (47)acetazolamideacetazolamide will increase the level or effect of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.amiodaroneamiodarone will increase the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Minor/Significance Unknown.anastrozoleanastrozole will increase the level or effect of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.atazanaviratazanavir will increase the level or effect of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.bosentanbosentan will decrease the level or effect of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.carbamazepinecarbamazepine will decrease the level or effect of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.clarithromycinclarithromycin will increase the level or effect of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.clarithromycin will increase the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Minor/Significance Unknown.cyclophosphamidecyclophosphamide will increase the level or effect of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.dexamethasonedexamethasone will decrease the level or effect of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.dronedaronedronedarone will increase the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Minor/Significance Unknown.efavirenzefavirenz will decrease the level or effect of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.erythromycin baseerythromycin base will increase the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Minor/Significance Unknown.erythromycin ethylsuccinateerythromycin ethylsuccinate will increase the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Minor/Significance Unknown.erythromycin lactobionateerythromycin lactobionate will increase the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Minor/Significance Unknown.erythromycin