tretinoin (Rx)

Brand and Other Names:Vesanoid
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 10mg

Acute Promyelocytic Leukemia

For use in patients with APL classification M3, which is characterized by the presence of t(15;17) translocation and/or the presence of the PML/RAR-alpha gene, who are refractory to, or have relapsed from, anthracycline chemotherapy, as well as for use in patients for whom anthracycline-based chemotherapy is contraindicated

Remission Induction

  • 45 mg/m²/day PO divided q12hr  
  • Discontinue 30 days after complete remission or 90 days after start of treatment (whichever comes first)

Remission Induction In Combination with an Anthracycline

  • 45 mg/m²/day PO divided q12hr  
  • Discontinue 30 days after complete remission or 90 days after start of treatment (whichever comes first)

Consolidation Therapy (Off-label)

  • Intermediate and high risk patients: 45 mg/m² PO divided q12hr for 15 days/month for 3 months

Maintenance of Remission (Off-label)

  • 45 mg/m²/day PO divided q12hr for 15 days every 3 months for 2 years

Dosing Adjustment (Toxicity)

APL differentiation syndrome: 10 mg dexamethasone IV q12hr for 3-5 days; consider interrupting tretinoin until resolution of hypoxia

Liver function tests >5 times upper limit of normal: Consider withholding treatment temporarily

Patient Monitoring

Monitor CBC, coagulation, liver function tests, serum lipids

Dosage Forms & Strengths

capsule

  • 10mg

Acute promyelocytic leukemia

For use in patients with APL classification M3, which is characterized by the presence of t(15;17) translocation and/or the presence of the PML/RAR-alpha gene, who are refractory to, or have relapsed from, anthracycline chemotherapy, as well as in patients in whom anthracycline-based chemotherapy is contraindicated

Remission Induction

  • 45 mg/m²/day PO divided q12hr  
  • Discontinue 30 days after remission or 90 days after start of treatment (whichever comes first)

Remission Induction with an Anthracycline

  • 25 mg/m²/day PO divided q12hr until complete remission or 90 days

Consolidation Therapy (Off-label)

  • Intermediate and high risk patients: 25 mg/m² PO divided q12hr for 15 days/month for 3 months

Maintenance of Remission (Off-label)

  • 25 mg/m²/day PO divided q12hr for 15 days every 3 months for 2 years

Dosing Adjustment (Toxicity)

APL differentiation syndrome: 10 mg dexamethasone IV q12hr for 3-5 days; consider interrupting tretinoin until resolution of hypoxia

Liver function tests >5 times upper limit of normal: Consider withholding treatment temporarily

Patient Monitoring

Monitor CBC, coagulation, liver function tests, serum lipids

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Interactions

Interaction Checker

and tretinoin

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     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Headache (86%)

            Fever (83%)

            Bone pain (77%)

            Dry mucous membranes (77%)

            Malaise (67%)

            URI (63%)

            Shivering (60%)

            Dyspnea (60%)

            Hemorrhage (60%)

            Elevated liver function tests (50-60%)

            Hyperlipidemia (60%)

            Infections (58%)

            Nausea and vomiting (57%)

            Rash (54%)

            Peripheral edema (52%)

            Leukocytosis (40%)

            Pain (37%)

            Abdominal pain (31%)

            DIC (26%)

            Respiratory insufficiency (26%)

            Mucositis (26%)

            GI disorder (26%)

            Retinoic acid-APL syndrome (25%)

            Ear ache (23%)

            Diarrhea (23%)

            Pleural effusion (20%)

            Dizziness (20%)

            Pruritus (20%)

            Sweating (20%)

            Anxiety (17%)

            Paresthesia (17%)

            Constipation (17%)

            Vision changes (17%)

            Dyspepsia (14%)

            Rales (14%)

            Depression (14%)

            Insomnia (14%)

            Alopecia (14%)

            Skin changes (14%)

            Confusion (11%)

            Abdominal distention (11%)

            Renal insufficiency (11%)

            1-10% (selected)

            Cardiac failure (6%)

            Pallor (6%)

            Cardiac arrest (3%)

            Cardiomyopathy (3%)

            Myocarditis (3%)

            Stroke (3%)

            Heart murmur (3%)

            Hemmorrhage (9%)

            Facial edema (6%)

            Intracranial hypertension (9%)

            Hypotaxia (3%)

            Seizure (3%)

            Somnolence (3%)

            Facial paralysis (3%)

            Spinal cord disorder (3%)

            Light reflex absent (3%)

            Ulcer (3%)

            Cellulitis (8%)

            Hepatosplenomegaly (9%)

            Dysuria (9%)

            Enlarged prostate (3%)

            Ascites (3%)

            Hepatitis (3%)

            Tremor (3%)

            Bone inflammation (3%)

            Hearing loss (6%)

            <1%

            Arterial thrombosis

            Hypercalcemia

            Myositis

            Pancreatitis

            Thrombocytosis

            Venous thrombosis

            Irreversible hearing loss

            Genital ulceration

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            Warnings

            Black Box Warnings

            Administration: Administered under the supervision of an experienced cancer chemotherapy physician in a facility equipped to diagnose and manage complications

            Teratogenic effects: High risk of severe infant deformity if administered during pregnancy; if treatment with tretinoin is required in women of childbearing potential, 2 reliable forms of contraception should be used during, and for 1 month after, therapy; if it is determined that tretinoin represents the best available treatment for a pregnant woman, patients should be informed of the risk to the fetus

            Retinoic acide-APL syndrome: About 25% of patients with APL treated with tretinoin experience a syndrome called the retinoic acid-APL syndrome, which can be fatal and is characterized by fever, dyspnea, acute respiratory distress, weight gain, radiographic pulmonary infiltrates, pleural or pericardial effusions, edema, and hepatic, renal, and/or multiorgan failure; this syndrome has occasionally been accompanied by impaired myocardial contractility and episodic hypotension; management has not been defined rigorously, but high-dose steroids given at the first suspicion of the RA-APL syndrome appear to reduce morbidity and mortality

            Rapidly evolving leukocytosis: About 40% of patients will develop rapidly evolving leukocytosis; those who present with high WBC at diagnosis (ie, >5 x10^9/L) have an increased risk; if signs and symptoms of the RA-APL syndrome are present together with leukocytosis, treatment with high-dose steroids should be initiated immediately

            Contraindications

            Hypersensitivity to retinoids, parabens, or formulation components

            Cautions

            Teratogenic and embryotoxic in animal studies and is expected to cause fetal harm in pregnant women; effective contraception must be used by all females of childbearing potential during and for 1 month after discontinuation (see Black Box Warnings)

            Microdosed progesterone oral contraception (“minipill”) may not be adequate for contraception during tretinoin therapy

            Patients without the t(15;17) translocation genetic marker should be considered for alternative treatment

            Retinoic acid-APL syndrome, which can be fatal, has been reported (see Black Box Warnings)

            Leukocytosis may occur (see Black Box Warnings)

            Pseudotumor cerebri associated with retinoids, especially in pediatric patients; dizziness or severe headache may be symptoms

            Up to 60% incidence of hypercholesterolemia and/or hypertriglyceridemia; reversible upon completion of treatment

            Elevated liver function tests may occur in 50-60% of patients during treatment

            Increased risk of thrombosis during first month of treatment

            Do not coadminister with other retinoids or in combination with vitamin A because symptoms of hypervitaminosis A

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            Pregnancy & Lactation

            Pregnancy category: D (systemic)

            Lactation: Unknown if excreted in breast milk; do not breast-feed, because of potential for serious adverse reactions in infant

            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

            Retinoid, induces differentiation and decreased proliferation of APL cells; produces an initial maturation of promyelocytes, followed by a repopulation of the bone marrow and peripheral blood by normal polyclonal hematopoietic cells in patients achieving complete remission

            Absorption

            Peak plasma time: 1-2 hours

            Peak plasma concentration: 347 ng/mL

            Distribution

            Protein bound: 95%

            Metabolism

            Metabolized by hepatic cytochrome 450

            Metabolites: 13-cis retinoic acid, 4-oxo trans retinoic acid, 4-oxo cis retinoic acid, 4-oxo trans retinoic acid glucuronide

            Elimination

            Half-life: 0.5-2 hours

            Excretion: urine 63%; feces 30%

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

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            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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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.