Dosing & Uses
Dosage Forms & Strengths
tablet: Schedule IV
- 75mg
- 100mg
Irritable Bowel Syndrome
Indicated for diarrhea-predominant irritable bowel syndrome (IBS-D) in adult men and women
100 mg PO BID with food
Discontinue in patients who develop severe constipation lasting >4 days
Dosage Modifications
Decrease dose to 75 mg PO BID in patients who
- are unable to tolerate the 100-mg dose
- are receiving concomitant OATP1B1 inhibitors
- have mild-to-moderate hepatic impairment
Renal Impairment
- Mild renal impairment: Dose adjustment not necessary
- Moderate or severe renal impairment and patients with ESRD not yet on dialysis: 75 mg PO BID
Hepatic impairment
- Mild-to-moderate (Child-Pugh A or B): Decrease dose to 75 mg PO BID; monitor for impaired mental or physical abilities needed to perform potentially hazardous activities
- Severe (Child-Pugh C): Contraindicated
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (85)
- alosetron
alosetron, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- alpelisib
eluxadoline will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.
- atazanavir
atazanavir increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- atorvastatin
atorvastatin increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- atropine
atropine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- bismuth subsalicylate
bismuth subsalicylate, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- brompheniramine
brompheniramine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions.
- buprenorphine
buprenorphine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- buprenorphine buccal
buprenorphine buccal, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- buprenorphine transdermal
buprenorphine transdermal, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- butorphanol
butorphanol, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- carbamazepine
carbamazepine increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- carbinoxamine
carbinoxamine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions.
- caspofungin
caspofungin increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- chlorpheniramine
chlorpheniramine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions.
- clarithromycin
clarithromycin increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- clemastine
clemastine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions.
- codeine
codeine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- cyclosporine
cyclosporine increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- cyproheptadine
cyproheptadine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions.
- dexchlorpheniramine
dexchlorpheniramine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions.
- digoxin
digoxin increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- dimenhydrinate
dimenhydrinate, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions.
- diphenhydramine
diphenhydramine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions.
- eltrombopag
eltrombopag increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- erythromycin base
erythromycin base increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- erythromycin ethylsuccinate
erythromycin ethylsuccinate increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- erythromycin lactobionate
erythromycin lactobionate increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- erythromycin stearate
erythromycin stearate increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- fentanyl
fentanyl, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- fentanyl intranasal
fentanyl intranasal, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- fentanyl transdermal
fentanyl transdermal, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- fentanyl transmucosal
fentanyl transmucosal, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- gemfibrozil
gemfibrozil increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- glyburide
glyburide increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- hydromorphone
hydromorphone, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- hydroxyzine
hydroxyzine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions.
- indinavir
indinavir increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- ketoconazole
ketoconazole increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- leniolisib
leniolisib will increase the level or effect of eluxadoline by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- lenvatinib
lenvatinib increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- levoketoconazole
levoketoconazole increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- levorphanol
levorphanol, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- loperamide
loperamide, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. Loperamide may be used occasionally for acute management of severe diarrhea but avoid chronic use. Discontinue loperamide immediately if constipation occurs.
- lopinavir
lopinavir increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- lovastatin
lovastatin increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- meperidine
meperidine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- methadone
methadone, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- metyrapone
metyrapone increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- mifepristone
mifepristone increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- morphine
morphine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- nalbuphine
nalbuphine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- nelfinavir
nelfinavir increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC)
ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC) increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- opium tincture
opium tincture, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- oxycodone
oxycodone, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- oxymorphone
oxymorphone, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- ozanimod
eluxadoline increases toxicity of ozanimod by Other (see comment). Avoid or Use Alternate Drug. Comment: Coadministration of ozanimod (a BCRP substrate) with BCRP inhibitors increases the exposure of the minor (RP101988, RP101075) and major active metabolites (CC112273, CC1084037) of ozanimod, which may increase the risk of ozanimod adverse reactions. .
- paclitaxel
paclitaxel increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- pazopanib
pazopanib increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- pentazocine
pentazocine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- pioglitazone
pioglitazone increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- pravastatin
pravastatin increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- promethazine
promethazine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions.
- remifentanil
remifentanil, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- repaglinide
repaglinide increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- rifampin
rifampin increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- rimegepant
eluxadoline will increase the level or effect of rimegepant by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of rimegepant (a BCRP substrate) with inhibitors of BCRP.
- ritonavir
ritonavir increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- rosiglitazone
rosiglitazone increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- sacubitril/valsartan
sacubitril/valsartan increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- saquinavir
saquinavir increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- simvastatin
simvastatin increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- sufentanil
sufentanil, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- sufentanil SL
sufentanil SL, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- sulbactam/durlobactam
eluxadoline will increase the level or effect of sulbactam/durlobactam by Other (see comment). Avoid or Use Alternate Drug. Sulbactam is predicted to have active secretion by OATP1 as a significant portion of total clearance; therefore, inhibition of OAT1 may increase sulbactam plasma concentrations
- tacrolimus
tacrolimus increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- talazoparib
eluxadoline will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- tapentadol
tapentadol, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- telmisartan
telmisartan increases levels of eluxadoline by increasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- tipranavir
tipranavir increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- tramadol
tramadol, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- triprolidine
triprolidine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions.
- trofinetide
trofinetide will increase the level or effect of eluxadoline 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.
- valsartan
valsartan increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
Monitor Closely (114)
- abiraterone
abiraterone increases levels of eluxadoline by decreasing metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C8 inhibitors.
- alfentanil
eluxadoline increases levels of alfentanil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- alprostadil intracavernous/urethral
eluxadoline increases levels of alprostadil intracavernous/urethral by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- amiodarone
amiodarone increases levels of eluxadoline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP1A2 inhibitors.
- apalutamide
apalutamide will decrease the level or effect of eluxadoline by increasing elimination. Use Caution/Monitor. Apalutamide weakly induces OATP1B1 and may decrease systemic exposure of drugs that are OATP1B1 substrates.
- berotralstat
eluxadoline increases levels of berotralstat by Other (see comment). Modify Therapy/Monitor Closely. Comment: Reduced dose of berotralstat (a BCRP substrate) to 110 mg/day when coadministered with BCRP inhibitors.
- bupropion
bupropion increases levels of eluxadoline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2D6 inhibitors.
- capecitabine
capecitabine increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
- carbamazepine
eluxadoline increases levels of carbamazepine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- carboprost tromethamine
eluxadoline increases levels of carboprost tromethamine by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- chenodiol
eluxadoline increases levels of chenodiol by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- chloramphenicol
chloramphenicol increases levels of eluxadoline by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C19 inhibitors.
- chlorothiazide
eluxadoline increases levels of chlorothiazide by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates.
- chlorpromazine
chlorpromazine increases levels of eluxadoline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2D6 inhibitors.
- cholic acid
eluxadoline increases levels of cholic acid by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- cimetidine
cimetidine increases levels of eluxadoline by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C19 inhibitors.
eluxadoline increases levels of cimetidine by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates. - cinacalcet
cinacalcet increases levels of eluxadoline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2D6 inhibitors.
- ciprofloxacin
ciprofloxacin increases levels of eluxadoline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP1A2 inhibitors.
- clonidine
eluxadoline increases levels of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- cocaine topical
cocaine topical increases levels of eluxadoline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2D6 inhibitors.
- conjugated estrogens
eluxadoline increases levels of conjugated estrogens by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- cyclosporine
eluxadoline increases levels of cyclosporine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- daunorubicin
eluxadoline increases levels of daunorubicin by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates.
- dexmedetomidine
dexmedetomidine increases levels of eluxadoline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2D6 inhibitors.
- dihydroergotamine
eluxadoline increases levels of dihydroergotamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- dipyridamole
eluxadoline increases levels of dipyridamole by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates.
- disopyramide
eluxadoline increases levels of disopyramide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- doxorubicin
eluxadoline increases levels of doxorubicin by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates.
- duloxetine
duloxetine increases levels of eluxadoline by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP1A2 inhibitors.
- duvelisib
eluxadoline will increase the level or effect of duvelisib by Other (see comment). Use Caution/Monitor. Coadministration of duvelisib (a BCRP substrate) with a BCRP transport inhibitor may increase levels or effects of duvelisib.
- encorafenib
encorafenib will increase the level or effect of eluxadoline 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.
- epoprostenol
eluxadoline increases levels of epoprostenol by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- ergotamine
eluxadoline increases levels of ergotamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- erythromycin base
eluxadoline increases levels of erythromycin base by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- erythromycin ethylsuccinate
eluxadoline increases levels of erythromycin ethylsuccinate by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- erythromycin lactobionate
eluxadoline increases levels of erythromycin lactobionate by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- erythromycin stearate
eluxadoline increases levels of erythromycin stearate by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- everolimus
eluxadoline increases levels of everolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- fentanyl
eluxadoline increases levels of fentanyl by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- fentanyl intranasal
eluxadoline increases levels of fentanyl intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- fentanyl transdermal
eluxadoline increases levels of fentanyl transdermal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- fentanyl transmucosal
eluxadoline increases levels of fentanyl transmucosal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- fexofenadine
eluxadoline increases levels of fexofenadine by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- fluconazole
fluconazole increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
fluconazole increases levels of eluxadoline by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C19 inhibitors. - fluorouracil
fluorouracil increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
- fluoxetine
fluoxetine increases levels of eluxadoline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2D6 inhibitors.
- flurbiprofen
flurbiprofen increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
- fluvoxamine
fluvoxamine will increase the level or effect of eluxadoline by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Use caution when coadministering with strong CYP1A2 inhibitors; Not studied
fluvoxamine will increase the level or effect of eluxadoline by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Use caution when coadministering with CYP2C19 inhibitors; not studied - fostemsavir
fostemsavir will increase the level or effect of eluxadoline 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.
- gemfibrozil
gemfibrozil increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
gemfibrozil increases levels of eluxadoline by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C19 inhibitors. - glecaprevir/pibrentasvir
eluxadoline will increase the level or effect of glecaprevir/pibrentasvir by Other (see comment). Use Caution/Monitor. Glecaprevir/pibrentasvir is an OATP1B1 inhibitor, BCRP substrate and inhibitor, and glecaprevir is a OAT1B1/3 substrate. Eluxadoline is an OATP1B1 substrate and BCRP inhibitor. Glecaprevir/pibrentasvir may decrease the therapeutic effects of eluxadoline. Eluxadoline may increase the plasma levels of glecaprevir/pibrentasvir.
- glyburide
eluxadoline increases levels of glyburide by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates.
- ibuprofen
ibuprofen increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
- ibuprofen IV
ibuprofen IV increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
- iloprost
eluxadoline increases levels of iloprost by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- imatinib
eluxadoline increases levels of imatinib by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 or BCRP substrates.
- indomethacin
indomethacin increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
- irinotecan
eluxadoline increases levels of irinotecan by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates.
- irinotecan liposomal
eluxadoline increases levels of irinotecan liposomal by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates.
- isoniazid
isoniazid increases levels of eluxadoline by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C19 inhibitors.
- itraconazole
itraconazole increases levels of eluxadoline by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP3A4 inhibitors.
- ketoconazole
ketoconazole increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
- lapatinib
eluxadoline increases levels of lapatinib by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates.
- leflunomide
eluxadoline increases levels of leflunomide by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates.
- lenvatinib
eluxadoline increases levels of lenvatinib by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 or BCRP substrates.
- letermovir
letermovir increases levels of eluxadoline by Other (see comment). Use Caution/Monitor. Comment: Letermovir, an OATP1B1/3 inhibitor may increase plasma concentrations of coadministered OATP1B1/3 substrates.
- letrozole
letrozole increases levels of eluxadoline by decreasing metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2A6 inhibitors.
- levofloxacin
eluxadoline increases levels of levofloxacin by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- levoketoconazole
levoketoconazole increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
levoketoconazole increases levels of eluxadoline by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP3A4 inhibitors. - levothyroxine
eluxadoline increases levels of levothyroxine by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- liothyronine
eluxadoline increases levels of liothyronine by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- lopinavir
lopinavir increases levels of eluxadoline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2D6 inhibitors.
- lorcaserin
lorcaserin increases levels of eluxadoline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2D6 inhibitors.
- mefenamic acid
mefenamic acid increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
- methotrexate
eluxadoline increases levels of methotrexate by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates.
- methoxsalen
methoxsalen increases levels of eluxadoline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP1A2 inhibitors.
- mexiletine
mexiletine increases levels of eluxadoline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP1A2 inhibitors.
- midazolam
eluxadoline increases levels of midazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- mitoxantrone
eluxadoline increases levels of mitoxantrone by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates.
- modafinil
modafinil increases levels of eluxadoline by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C19 inhibitors.
- nicardipine
nicardipine increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
- nitrofurantoin
eluxadoline increases levels of nitrofurantoin by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates.
- ofloxacin
ofloxacin increases levels of eluxadoline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP1A2 inhibitors.
- omeprazole
omeprazole increases levels of eluxadoline by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C19 inhibitors.
- paroxetine
paroxetine increases levels of eluxadoline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2D6 inhibitors.
- pimozide
eluxadoline increases levels of pimozide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- piroxicam
piroxicam increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
- pitavastatin
eluxadoline increases levels of pitavastatin by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- primaquine
primaquine increases levels of eluxadoline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP1A2 inhibitors.
- quinidine
quinidine increases levels of eluxadoline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2D6 inhibitors.
eluxadoline increases levels of quinidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline. - quinine
eluxadoline increases levels of quinine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- riociguat
eluxadoline increases levels of riociguat by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates.
- ritonavir
ritonavir increases levels of eluxadoline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2D6 inhibitors.
- rosuvastatin
eluxadoline increases levels of rosuvastatin by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 or BCRP substrates. Potential for increased risk of myopathy/rhabdomyolysis with rosuvastatin. Decrease rosuvastatin to lowest effective dose.
- saquinavir
eluxadoline increases levels of saquinavir by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- selexipag
eluxadoline will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- simvastatin
eluxadoline increases levels of simvastatin by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates. .
- sirolimus
eluxadoline increases levels of sirolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- sofosbuvir/velpatasvir
sofosbuvir/velpatasvir increases levels of eluxadoline by Other (see comment). Use Caution/Monitor. Comment: Velpatasvir inhibits OATP1B1, OATP1B3, and OATP2B1 transporters. .
- sulfadiazine
sulfadiazine increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
- sulfamethoxazole
sulfamethoxazole increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
- sulfasalazine
eluxadoline increases levels of sulfasalazine by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates. .
- tacrolimus
eluxadoline increases levels of tacrolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- thiotepa
thiotepa increases levels of eluxadoline by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2B6 inhibitors.
- thyroid desiccated
eluxadoline increases levels of thyroid desiccated by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- ticlopidine
ticlopidine increases levels of eluxadoline by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C19 inhibitors.
- tolbutamide
tolbutamide increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
- topotecan
eluxadoline increases levels of topotecan by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates. .
- tranylcypromine
tranylcypromine increases levels of eluxadoline by decreasing metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2A6 inhibitors.
- treprostinil
eluxadoline increases levels of treprostinil by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- triazolam
eluxadoline increases levels of triazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- ursodiol
eluxadoline increases levels of ursodiol by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- voriconazole
voriconazole increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
- zileuton
zileuton increases levels of eluxadoline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP1A2 inhibitors.
Minor (1)
- voclosporin
voclosporin will increase the level or effect of eluxadoline by Other (see comment). Minor/Significance Unknown. Information suggests voclosporin (an OATP1B1 inhibitor) may increase in the concentration of OATP1B1 substrates is possible. Monitor for adverse reactions of OATP1B1 substrates when coadministered with voclosporin.
Adverse Effects
1-10%
Constipation (7-8%)
Nausea (7-8%)
Abdominal pain (6-7%)
URT infection (3-5%)
Vomiting (4%)
Nasopharyngitis (3-4%)
Abdominal distention (3%)
Bronchitis (3%)
Dizziness (3%)
Flatulence (3%)
Rash (3%)
Increased ALT (2-3%)
Fatigue (2-3%)
Viral gastroenteritis (1-3%)
≤2%
- Gastrointestinal: GERD
- General disorders: Feeling drunk
- Investigations: Increased AST
- Nervous system: Sedation, somnolence
- Psychiatric disorders: Euphoric mood
- Respiratory: Asthma, bronchospasm, respiratory failure, wheezing
<1%
Severe constipation
Postmarketing Reports
Hypersensitivity: anaphylaxis, angioedema (e.g. swollen face and throat), dyspnea, throat tightness, and chest pain/tightness
Warnings
Contraindications
Documented hypersensitivity to drug or components of the formulation
Patients who do not have a gallbladder
Known or suspected gallbladder obstruction, biliary duct obstruction or sphincter of Oddi disease or dysfunction; increased risk for sphincter of Oddi spasm
Alcoholism, alcohol abuse, alcohol addiction, or in patients who drink >3 alcoholic beverages/day; increased risk of pancreatitis
History of pancreatitis, pancreatic duct obstruction, or structural diseases of the pancreas; increased risk of acute pancreatitis
Severe hepatic impairment (Child-Pugh C); risk of significantly increased eluxadoline plasma concentrations
History of chronic or severe constipation or sequelae from constipation, or known mechanical GI obstruction; increased risk of bowel obstruction
Cautions
Eluxadoline is a mu opioid receptor agonist; because of this mechanism of action, the potential for increased risk of sphincter of Oddi spasm exists, resulting in pancreatitis or hepatic enzyme elevation associated with acute abdominal pain (see Contraindications)
There is risk of sphincter of Oddi spasm, resulting in pancreatitis or hepatic enzyme elevation associated with acute abdominal pain (e.g., biliary-type pain) in patients receiving therapy; instruct patients to immediately stop therapy and seek medical attention if they experience symptoms suggestive of sphincter of Oddi spasm such as acute worsening of abdominal pain
Increased risk of pancreatitis not associated with sphincter of Oddi spasm reported; most cases were associated with excessive alcohol use
In patients with a gallbladder, evaluate a patient’s alcohol intake prior to starting therapy; instruct patients to avoid chronic or acute excessive alcohol use while in therapy; monitor for new or worsening abdominal pain that may radiate to back or shoulder, with or without nausea and vomiting; instruct patients to immediately stop therapy and seek medical attention if they experience symptoms suggestive of pancreatitis such as acute abdominal or epigastric pain radiating to back or shoulder associated with elevations of pancreatic enzymes with or without nausea and vomiting
Constipation requiring hospitalization reported; severe cases with development of intestinal obstruction, intestinal perforation, and fecal impaction, requiring intervention, also reported; instruct patients to stop therapy and immediately contact their healthcare provider if they experience severe constipation; avoid use with other drugs that may cause constipation
In postmarketing experience, serious hypersensitivity reactions (including anaphylaxis) reported; some of these reactions occurred after first one or two doses of treatment; instruct patients to immediately stop therapy and seek medical attention if they experience symptoms suggestive of a hypersensitivity reaction
Patients who do not have a gallbladder
- Monitor patients without a gallbladder for new or worsening abdominal pain, with or without nausea and vomiting, or acute biliary pain with liver or pancreatic enzyme elevations
- Discontinue therapy and seek medical attention if symptoms develop
- March 2017: An FDA review found patients who do not have a gallbladder are at increased risk of developing serious pancreatitis that could result in hospitalization or death
- Symptoms of pancreatitis have occurred with just 1 or 2 doses of eluxadoline at the recommended dosage for patients who do not have a gallbladder (75 mg) and who do not consume alcohol
- Pancreatitis, with or without sphincter of Oddi spasm, reported in patients taking either the 75 mg or 100 mg dosage, including serious cases resulting in hospitalization, primarily in patients without a gallbladder; fatal cases also reported in patients without a gallbladder
The FDA is recommending the following
- Physicians should not prescribe eluxadoline to patients without a gallbladder
- Patients taking eluxadoline who do not have a gallbladder should talk to their health care professional to consider other treatment options
Data summary
- From May 2015 through February 2017, the FDA received reports of 120 serious cases of pancreatitis or death; 76 of these cases resulted in hospitalization, of which 2 patients died
- Among the 68 cases that reported gallbladder status, 56 cases of pancreatitis or death occurred in patients who do not have a gallbladder
- The majority of patients (n=44/56) received the currently recommended dosage (75 mg) for patients who do not have a gallbladder
- Of the 56 cases in patients who do not have a gallbladder, 21 reported that the patient did not abuse alcohol and 35 did not report alcohol use status
Drug interaction overview
- OATP1B1 inhibitors may increase systemic exposure to eluxadoline
- Strong CYP inhibitors may increase systemic exposure to eluxadoline
- Risk of constipation increased when coadministered with other drugs that cause constipation
- Eluxadoline may increase systemic exposure of coadministered OATP1B1 and BCRP substrates
- Eluxadoline may increase systemic exposure of coadministered CYP3A substrates with a narrow therapeutic index
Pregnancy & Lactation
Pregnancy
No studies in pregnant women
Animal reproduction studies
- Oral and SC administration of eluxadoline to rats and rabbits during organogenesis at doses approximately 51 and 115 times the human exposure after a single oral dose of 100 mg, respectively, demonstrated no teratogenic effects. In a prenatal and postnatal development study in rats
- No adverse effects were observed in offspring with oral administration of eluxadoline at doses approximately 10 times the human exposure
Lactation
Unknown if distributed in human breast milk
Secreted in rat milk
Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Mu opioid receptor agonist; it also is a delta opioid receptor antagonist and a kappa opioid receptor agonist
The multiple opioid activity is designed to treat the symptoms of IBS-D while reducing the incidence of constipation that can occur with unopposed mu opioid receptor agonists
Absorption
Peak plasma time: 1.5 hr (with food); 2 hr (fasting)
Peak plasma concentration: 2-4 ng/mL (decreased by 50% with high-fat meal)
AUC: 12-22 ng•hr/mL (decreased by 60% with high-fat meal)
Distribution
Protein bound: 81%
Metabolism
Not clearly established; eluxadoline may decrease elimination of CYP3A, OATP1B1, and BCRP substrates
OATP1B1 inhibitors and strong CYP inhibitors may decrease elimination of eluxadoline
Evidence exists that glucuronidation can occur to form an acyl glucuronide metabolite
Elimination
Half-life: 3-7-6 hr
Excretion: 82.2% feces; <1% urine
Administration
Instructions
Take with food
If a dose is missed, take the next dose at the regular time; do not take 2 doses at the same time to make up for a missed dose
Discontinue with severe constipation that lasts >4 days
Storage
Store at controlled room temperature (20-25°C [68-77°F]); excursions permitted to 15-30°C (59-86°F)
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Viberzi oral - | 75 mg tablet |  | |
| Viberzi oral - | 100 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
eluxadoline oral
ELUXADOLINE - ORAL
(EL-ux-AD-oh-leen)
COMMON BRAND NAME(S): Viberzi
USES: This medication is used to treat a certain stomach/abdominal disorder (irritable bowel syndrome with diarrhea, or IBS-D). It works by slowing down the motion in your gut. This effect helps lessen symptoms such as belly pain and diarrhea.
HOW TO USE: Read the Medication Guide provided by your pharmacist before you start taking eluxadoline and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with food as directed by your doctor, usually 2 times a day. The dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of side effects will increase. Properly stop the medication when so directed.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.If you are also taking loperamide to help control diarrhea, do not take it on a regular schedule or you may become constipated. However, you may take it occasionally if needed for severe diarrhea. If you develop constipation, stop taking loperamide and tell your doctor right away.Though it helps many people, this medication may sometimes cause addiction. This risk may be higher if you have a substance use disorder (such as overuse of or addiction to drugs/alcohol). Take this medication exactly as prescribed to lower the risk of addiction. Ask your doctor or pharmacist for more details.Tell your doctor if you do not get better or if you get worse.
SIDE EFFECTS: Constipation, nausea, vomiting, abdominal pain, or drowsiness may occur. If any of these effects last or get worse, tell your doctor or pharmacist right away. If you have severe constipation, stop taking eluxadoline and tell your doctor or pharmacist right away.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: symptoms of pancreatitis or sphincter of Oddi spasm (such as nausea/vomiting that doesn't stop, new or suddenly worse stomach/abdominal pain that may move to your back or shoulder).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking eluxadoline, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: personal or family history of a substance use disorder (such as overuse of or addiction to drugs/alcohol), gallbladder removal surgery, liver disease, kidney disease, pancreatitis, other stomach/abdominal problems (such as blockage, sphincter of Oddi disease/dysfunction, previous long-lasting or severe constipation).This drug may make you drowsy. Alcohol or marijuana (cannabis) can make you more drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis). Drinking a lot of alcohol while taking this medication may increase the risk of pancreatitis.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Older adults may be more sensitive to the side effects of this drug, especially constipation or stomach/abdominal pain.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if eluxadoline passes into breast milk. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Do not share this medication with others. Sharing it is against the law.Lab tests (such as liver function tests, lipase levels) may be done while you are taking this medication. Keep all medical and lab appointments.
MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep this medicine in a safe place to prevent theft, misuse, or abuse. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised April 2022. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
