Dosing & Uses
Dosage Forms & Strengths
tablet
- 0.5mg
- 1mg
Irritable Bowel Syndrome
Indicated only for women with severe diarrhea-predominant IBS who have: chronic IBS symptoms (generally lasting 6 months or longer), had anatomic or biochemical abnormalities of GI tract excluded, and not responded adequately to conventional therapy
Initial 0.5 mg PO q12hr for 4 weeks; if well tolerated, but inadequate control of IBS symptoms, increase up to 1 mg q12hr; discontinue if no improvement after 4 weeks
Renal Impairment
Dose adjustment not studied in the manufacturer's labeling
Hepatic Impairment
Moderate impairment (Child-Pugh score < 9): Use caution
Severe dysfunction (Child-Purgh score ≥ 10): Contraindicated
Not recommended
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (2)
- apomorphine
apomorphine, alosetron. Mechanism: unspecified interaction mechanism. Contraindicated. Profound hypotension and loss of consciousness reported when 5HT3 antagonists are coadministered with apomorphine. .
- fluvoxamine
fluvoxamine will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Contraindicated.
Serious - Use Alternative (28)
- abametapir
abametapir will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP1A2 substrates. If not feasible, avoid use of abametapir.
- amobarbital
amobarbital will decrease the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- armodafinil
armodafinil will decrease the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- butabarbital
butabarbital will decrease the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- butalbital
butalbital will decrease the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- carbamazepine
carbamazepine will decrease the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- cigarette smoking
cigarette smoking will decrease the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- cimetidine
cimetidine will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- ciprofloxacin
ciprofloxacin will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Alosetron is associated with potentially serious and life-threatening, dose-related gastrointestinal adverse effects, concomitant use with CYP450 1A2 inhibitors should generally be avoided if possible.
- eluxadoline
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. .
- erythromycin base
erythromycin base will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- erythromycin ethylsuccinate
erythromycin ethylsuccinate will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- erythromycin lactobionate
erythromycin lactobionate will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- erythromycin stearate
erythromycin stearate will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- givosiran
givosiran will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP1A2 substrates with givosiran. If unavoidable, decrease the CYP1A2 substrate dosage in accordance with approved product labeling.
- mexiletine
mexiletine will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Contraindicated.
- modafinil
modafinil will decrease the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- pefloxacin
pefloxacin will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- peginterferon alfa 2a
peginterferon alfa 2a will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- pentobarbital
pentobarbital will decrease the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- phenobarbital
phenobarbital will decrease the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- pipemidic acid
pipemidic acid will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Contraindicated.
- primidone
primidone will decrease the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- secobarbital
secobarbital will decrease the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- smoking
smoking will decrease the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- tobacco use
tobacco use will decrease the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- verapamil
verapamil will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- zileuton
zileuton will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
Monitor Closely (31)
- benzhydrocodone/acetaminophen
benzhydrocodone/acetaminophen, alosetron. Either increases effects of the other by serotonin levels. Use Caution/Monitor. Coadministration of drugs that affect the serotonergic neurotransmitter system may result in serotonin syndrome. If concomitant use is warranted, carefully observe the patient, particularly during treatment initiation and dose adjustment.
- carbamazepine
carbamazepine will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- cimetidine
cimetidine will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- clarithromycin
clarithromycin will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- deferasirox
deferasirox increases levels of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- efavirenz
efavirenz will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.
- erythromycin base
erythromycin base will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- erythromycin ethylsuccinate
erythromycin ethylsuccinate will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- erythromycin lactobionate
erythromycin lactobionate will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- erythromycin stearate
erythromycin stearate will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ethinylestradiol
ethinylestradiol will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- fenfluramine
alosetron decreases effects of fenfluramine by pharmacodynamic antagonism. Use Caution/Monitor. Potent serotonin receptor antagonists may decrease fenfluramine efficacy. If coadministered, monitor appropriately.
- fexinidazole
fexinidazole will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- fluoxetine
fluoxetine will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.
- fluvoxamine
fluvoxamine will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.
- hydrocodone
hydrocodone, alosetron. Either increases effects of the other by serotonin levels. Use Caution/Monitor. Coadministration of drugs that affect the serotonergic neurotransmitter system may result in serotonin syndrome. If concomitant use is warranted, carefully observe the patient, particularly during treatment initiation and dose adjustment.
- imatinib
imatinib will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.
- isoniazid
isoniazid will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
isoniazid will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - itraconazole
itraconazole will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ketoconazole
ketoconazole will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- levoketoconazole
levoketoconazole will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nefazodone
nefazodone will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ribociclib
ribociclib will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- rifabutin
rifabutin will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- rifampin
rifampin will decrease the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
rifampin will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - rucaparib
rucaparib will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP1A2 substrates, if clinically indicated.
- saquinavir
saquinavir increases levels of alosetron by decreasing metabolism. Use Caution/Monitor.
- St John's Wort
St John's Wort will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- stiripentol
stiripentol, alosetron. affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP1A2 inhibitor and inducer. Monitor CYP1A2 substrates coadministered with stiripentol for increased or decreased effects. CYP1A2 substrates may require dosage adjustment.
- sufentanil SL
sufentanil SL, alosetron. Either increases effects of the other by serotonin levels. Use Caution/Monitor. Coadministration of drugs that affect the serotonergic neurotransmitter system may result in serotonin syndrome. If concomitant use is warranted, carefully observe the patient, particularly during treatment initiation and dose adjustment.
- teriflunomide
teriflunomide decreases levels of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
Minor (70)
- amiodarone
amiodarone will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
- amobarbital
amobarbital will decrease the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
amobarbital will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. - aprepitant
aprepitant will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- armodafinil
armodafinil will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- artemether/lumefantrine
artemether/lumefantrine will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- atazanavir
atazanavir will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- bosentan
bosentan will decrease the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
bosentan will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. - budesonide
budesonide will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- butabarbital
butabarbital will decrease the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
butabarbital will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. - butalbital
butalbital will decrease the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
butalbital will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. - carbamazepine
carbamazepine will decrease the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
- cimetidine
cimetidine will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
- conivaptan
conivaptan will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- cortisone
cortisone will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- cyclosporine
cyclosporine will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- darifenacin
darifenacin will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- darunavir
darunavir will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- dasatinib
dasatinib will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- dexamethasone
dexamethasone will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- DHEA, herbal
DHEA, herbal will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- disulfiram
disulfiram will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
- dronedarone
dronedarone will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- efavirenz
efavirenz will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- esomeprazole
esomeprazole will decrease the level or effect of alosetron by increasing metabolism. Minor/Significance Unknown.
- etravirine
etravirine will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
etravirine will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. - felbamate
felbamate will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
- fluconazole
fluconazole will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
fluconazole will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. - fludrocortisone
fludrocortisone will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- fosamprenavir
fosamprenavir will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- fosphenytoin
fosphenytoin will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- grapefruit
grapefruit will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- griseofulvin
griseofulvin will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- hydrocortisone
hydrocortisone will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- indinavir
indinavir will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- ketoconazole
ketoconazole will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
- lapatinib
lapatinib will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- leflunomide
leflunomide will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
- levoketoconazole
levoketoconazole will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
- lumefantrine
lumefantrine will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- marijuana
marijuana will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- methylprednisolone
methylprednisolone will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- metronidazole
metronidazole will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
metronidazole will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. - miconazole vaginal
miconazole vaginal will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
miconazole vaginal will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. - nateglinide
nateglinide will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
- nelfinavir
nelfinavir will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- nevirapine
nevirapine will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- nifedipine
nifedipine will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- nilotinib
nilotinib will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
nilotinib will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. - omeprazole
omeprazole will decrease the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.
- oxcarbazepine
oxcarbazepine will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- pentobarbital
pentobarbital will decrease the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
pentobarbital will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. - phenobarbital
phenobarbital will decrease the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
phenobarbital will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. - phenytoin
phenytoin will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- posaconazole
posaconazole will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- prednisone
prednisone will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- primidone
primidone will decrease the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
primidone will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. - quinupristin/dalfopristin
quinupristin/dalfopristin will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- rifampin
rifampin will decrease the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
- rifapentine
rifapentine will decrease the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
rifapentine will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. - ritonavir
ritonavir will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- rufinamide
rufinamide will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- secobarbital
secobarbital will decrease the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
secobarbital will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. - sulfamethoxazole
sulfamethoxazole will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
- ticlopidine
ticlopidine will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
- topiramate
topiramate will decrease the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- valproic acid
valproic acid will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
- verapamil
verapamil will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- voriconazole
voriconazole will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
voriconazole will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. - zafirlukast
zafirlukast will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.
zafirlukast will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
Adverse Effects
>10%
Constipation (29%)
1-10%
Abdominal pain (7%)
Nausea (6%)
Headache (≥3%)
GI discomfort and pain (5%)
Fatigue (≥3%)
Gastroenteritis (>3%)
Abdominal distention (2%)
Flatulence (1-3%)
Regurgitation and reflux (2%)
Abdominal distension (2%)
Hemorrhoids (2%)
Urinary tract infection (≥3%)
Muscle spasm (≥3%)
Cough (≥3%)
Nasopharyngitis (≥3%)
<1%
Ischemic colitis
Anxiety
Bone pain
Colitis
Diverticulitis
Cholecystitis
GI impaction
GI spasms
GI ulceration
Warnings
Black Box Warnings
Infrequent but serious GI adverse reactions (eg, ischemic colitis, serious complications of constipation) reported; some have resulted in hospitalization and, rarely, blood transfusion, surgery, or death
In order to prescribe, physicians must be enrolled in Prescribing Program for Lotronex (see cautions)
Indicated only for women with severe diarrhea-predominant irritable bowel syndrome that has not responded adequately to conventional therapy
Discontinue immediately in patients who develop constipation or symptoms of ischemic colitis; do not resume in those who develop ischemic colitis
Patients who have constipation should immediately contact their prescriber if constipation does not resolve after therapy is discontinued; patients with resolved constipation should resume only on the advice of their treating prescriber
Contraindications
Hypersensitivity
Rectal bleeding, history of chronic or severe current constipation
History of ischemic colitis, intestinal obstruction, stricture, toxic megacolon, GI perforation or adhesion, thrombophlebitis, diverticulitis, hypercoagulable state, history of or current Crohn's disease or ulcerative colitis
Coadministration with apomorphine; combination reported to cause profound hypotension and loss of consciousness
Inability to comply with the Patient-Physician Agreement for Lotronex
Severe hepatic impairment
Impaired intestinal circulation
Concomitant administration with fluvoxamine
Thrombocytopenia
Cautions
Discontinue if inadequate control after 4 weeks of q12hr dosing
Use with caution in breast-feeding women
Use caution in mild-to-moderate hepatic impairment
Withdrawn from U.S. market in Nov. 2000 due to cases of severe ischemic colitis, obstructed or ruptured bowel, and death; reinstated in June 2002 on a limited basis
Constipation
- Serious complications of constipation, including obstruction, ileus, impaction, toxic megacolon, and secondary bowel ischemia, reported with use
- Complications of constipation reported with use of 1 mg twice daily and with lower doses
- Rare cases of perforation and death reported from postmarketing clinical practice; in some cases, complications of constipation required intestinal surgery, including colectomy
- Patients who are elderly, debilitated, or taking additional medications that decrease gastrointestinal motility may be at greater risk for complications of constipation; discontinue therapy immediately in patients who develop constipation
Ischemic colitis
- Ischemic colitis reported with use of 1 mg twice daily and with lower doses; a dose-response relationship has not been established; ischemic colitis was reported in one patient receiving placebo; the patient experience in controlled clinical trials is insufficient to estimate incidence of ischemic colitis in patients taking this medication for longer than 6 months
- Treatment should be discontinued immediately in patients with signs of ischemic colitis such as rectal bleeding, bloody diarrhea, or new or worsening abdominal pain; because ischemic colitis can be life-threatening, patients with signs or symptoms of ischemic colitis should be evaluated promptly and have appropriate diagnostic testing performed; treatment should not be resumed in patients who develop ischemic colitis
Pregnancy & Lactation
Pregnancy
The available data with use in pregnant women are insufficient to draw conclusions about any drug-associated risks for major birth defects, miscarriage, or adverse maternal or fetal outcomes
Animal data
- In animal reproduction studies, no adverse developmental effects were observed with oral administration of alosetron in rats and rabbits during organogenesis at doses 160 to 240 times, respectively, the recommended human dosage
Lactation
There are no data regarding presence of drug in human milk, effects on breastfed infant, or on milk production; the drug and/or metabolites of the drug are present in breast milk of lactating rats; when a drug is present in animal milk, it is likely that the drug will be present in human milk; the developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and any potential adverse effects on the breastfed infant from therapy or from the underlying maternal condition
Monitor infants exposed to drug through breast milk for severe constipation and blood in stools
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
5-HT3 receptor antagonist; modulates enteric nervous system
Pharmacokinetics
Half-life: 1.5 hr
Peak plasma time: 0.5-1.7 hr
Bioavailability: 50-60%, food decreases absorption
Protein bound: 82%
Vd: 65-95 L
Excretion: Urine (74%); feces (11%)
Metabolites: 6-hydroxyl metabolite, 6-O-glucuronide metabolite, bis-oxidized dicarbonyl metabolite, N-demethylated alosetron [all are inactive]
Metabolism
- Extensively undergoes first-pass metabolism
- Metabolized by Cytochrome (CYP) P450: CYP2C9 (30%), 3A4 (18%), 1A2 (10%), and non-CYP mediated phase I metabolism (11%)
Clearance
- Renal: 94 mL/min
- Total body: 1190 mL/min
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Lotronex oral - | 1 mg tablet |  | |
| Lotronex oral - | 0.5 mg tablet |  | |
| alosetron oral - | 1 mg tablet |  | |
| alosetron oral - | 1 mg tablet |  | |
| alosetron oral - | 0.5 mg tablet |  | |
| alosetron oral - | 1 mg tablet |  | |
| alosetron oral - | 0.5 mg tablet |  | |
| alosetron oral - | 1 mg tablet |  | |
| alosetron oral - | 0.5 mg tablet |  | |
| alosetron oral - | 1 mg tablet | | |
| alosetron oral - | 0.5 mg tablet | | |
| alosetron oral - | 1 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
alosetron oral
ALOSETRON - ORAL
(al-OH-se-tron)
COMMON BRAND NAME(S): Lotronex
WARNING: Alosetron has rarely caused serious, sometimes fatal side effects of the intestines. These effects include reduced blood flow to the large intestine (ischemic colitis) and serious complications of constipation. If you have constipation, new or worsening stomach/abdominal pain, or bloody diarrhea/stools, stop taking this medication and get medical help right away. If your constipation does not go away after stopping alosetron, again tell your doctor right away. Do not take this medication again unless your doctors tells you to do so.This medication should only be used by women with severe irritable bowel syndrome (IBS) whose main problem is diarrhea. Only carefully selected patients may use this medication. Consult your doctor or pharmacist for more information about the risks and benefits of using alosetron.
USES: Alosetron is used to treat women with severe irritable bowel syndrome (IBS) who have diarrhea as the main problem. It is not a cure, but it may help to decrease abdominal pain, sudden urges to have a bowel movement, and diarrhea.This medication is not recommended for use by children because of the serious side effects that have been seen in adults.
HOW TO USE: Read the Medication Guide provided by your pharmacist before you start taking alosetron and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with or without food as directed by your doctor, usually once or twice daily. The dosage is based on your medical condition and response to treatment. Do not start taking this medication if you are constipated.Tell your doctor if your condition does not get better or if it gets worse.
SIDE EFFECTS: See also Warning section.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.Stop taking this medication and get medical help right away if any of these very serious side effects occur: constipation, bloody diarrhea/stools, new or worsening stomach/abdominal pain.This medication may increase serotonin and rarely cause a very serious condition called serotonin syndrome/toxicity. The risk increases if you are also taking other drugs that increase serotonin, so tell your doctor or pharmacist of all the drugs you take (see Drug Interactions section). Get medical help right away if you develop some of the following symptoms: fast heartbeat, hallucinations, loss of coordination, severe dizziness, severe nausea/vomiting/diarrhea, twitching muscles, unexplained fever, unusual agitation/restlessness.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, such as: 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 alosetron, 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: constipation, other bowel/intestinal disorders (such as bowel blockage, ischemic colitis, Crohn's disease, ulcerative colitis, diverticulitis), liver disease, blood clots.Before having surgery, tell your doctor or dentist about all the products you use (such as prescription drugs, nonprescription drugs, and herbal products).Older adults may be more sensitive to the side effects of this drug, especially constipation.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if this drug 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 (such as 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.A product that may interact with this drug is: apomorphine.Other medications can affect the removal of alosetron from your body, which may affect how alosetron works. Examples include fluvoxamine, viloxazine, among othersThe risk of serious complications of constipation increases if you are also taking other drugs that may cause constipation. Ask your doctor or pharmacist about the safe use of all the products you may take.The risk of serotonin syndrome/toxicity increases if you are also taking other drugs that increase serotonin. Some examples are street drugs such as MDMA/ "ecstasy," St. John's wort, certain antidepressants (such as SSRIs like fluoxetine/paroxetine, SNRIs like duloxetine/venlafaxine), among others. The risk of serotonin syndrome/toxicity may be more likely when you start or increase the dose of these drugs.
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.
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 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 August 2021. Copyright(c) 2022 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.
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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.
