alosetron (Rx)

Brand and Other Names:Lotronex
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 0.5mg
  • 1mg
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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

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Interactions

Interaction Checker

and alosetron

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            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

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            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

            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, 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

            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

            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

            Physicians must enroll in GlaxoSmithKline's Prescribing Program for Lotronex 1-888-825-5249 or www.lotronex.com

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            Pregnancy & Lactation

            Pregnancy Category: B

            Lactation: Not known whether drug distributed into breast milk, use caution

            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.

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            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
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            Formulary

            FormularyPatient Discounts

            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.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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