Alosetron

Indications

Alosetron is used for: Irritable Bowel Syndrome

Adult Dose

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 Hepatic Impairment Moderate impairment (Child-Pugh score < 9): Use caution Severe dysfunction (Child-Purgh score ? 10): Contraindicated

Child Dose

Renal Dose

Renal Impairment Dose adjustment not studied in the manufacturer's labeling

Administration

Contra Indications

Hypersensitivity Rectal bleeding, history of chronic or severe current constipation History of ischemic colitis, intestinal obstruction, stricture, toxic megacolon, GI perforation or adhesion, thrombophlebitis, 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

Precautions

Discontinue if inadequate control after 4 weeks of q12hr dosing Discontinue immediately if symptoms of constipation or ischemic colitis occurs Risk of complications from constipation higher in the elderly Use with caution in breast-feeding women Use caution in mild-to-moderate hepatic impairment

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

Interactions

Adverse Effects

Side effects of Alosetron : >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

Mechanism of Action

5-HT3 receptor antagonist; modulates enteric nervous system