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bexarotene (Rx)Brand and Other Names:Targretin

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 75mg

gel

  • 1%
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Cutaneous T-Cell Lymphoma

300 mg/sq.meter PO qDay with food; titrate based on response or toxicity 

Topical: initial apply to lesions qOD x 1 week, THEN increase qWeek up to QID

Monitor: WBC, LFTs, lipids, thyroid function

Safety & efficacy not established

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Interactions

Interaction Checker

bexarotene and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Oral (CTCL trial)

            • Peripheral edema (11-13%)
            • Headache (30-42%), fever (5-17%), chills (10-13%), insomnia (5-11%)
            • Exfoliative dermatitis (10-28%), rash (16-23%), alopecia (4-12%), dry skin (10-11%)
            • Diarrhea (7-41%), nausea (8-16%), vomiting (4-13%), abdominal pain (4-11%)
            • Bacterial infection (1-13%), flu syndrome (4-13%), infections (13-23%)
            • Leukopenia (17-47%), anemia (6-25%), lactic dehydrogenase increased (7-13%), hypochromic anemia (4-13%)
            • Hyperlipidemia (78-79%), hypercholesteremia (32-62%), hypothyroidism (29-52%)
            • Back pain (2-11%)

            Topical

            • Rash (72%)
            • Pruritus (36%)
            • Pain (30%)
            • Infection (18%)
            • Contact dermatitis (14%)
            • Headache (14%)

            1-10%

            Oral

            • Hemorrhage, hypertension
            • Hypothyroidism
            • Pharyngitis, rhinitis
            • Arthralgia
            • Blephartis, corneal lesion
            • Renal dysfunction

            Topical

            • Edema (10%)
            • Hyperlipemia (10%)
            • Asthenia (6%)
            • Exfoliative dermatitis (6%)
            • Leukopenia (6%), lymphadenopathy (6%), WBC changes (6%)
            • Cough increased (6%), pharyngitis (6%)
            • Sweating (6%)
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            Warnings

            Black Box Warnings

            Bexarotene is a retinoid

            Retinoids are associated with birth control defects in humans and are contraindicated during pregnancy

            Effective contraception must be in place 1 month before initiation of therapy, during therapy, and for at least 1 month after discontinuation of therapy

            Contraindications

            Hypersensitivity to retinoids

            Pregnancy (use 2 forms of contraception)

            Cautions

            Do not use occlusive dressings w/ gel

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            Pregnancy & Lactation

            Pregnancy Category: X

            Lactation: It is not known whether bexarotene is excreted in human milk. Because of the potential for serious adverse reactions in nursing infants from bexarotene, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

            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

            Half-Life: 7 hr

            Peak Plasma Time: 2 hr

            Protein Bound: >99%

            Metabolism: by CYP3A4

            Metabolites: 6- & 7- hydroxy- bexarotene, 6- & 7- oxo- bexarotene

            Excretion: bile

            Mechanism of Action

            Retinoid X receptor activator, regulates genes that control cell differentiation

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            Images

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            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

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            • View the formulary and any restrictions for each plan.
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            • 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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