vorinostat (Rx)

Brand and Other Names:Zolinza
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 100mg

Cutaneous T-cell Lymphoma

Indicated for treatment of cutaneous manifestations in patients with cutaneous T-cell lymphoma who have progressive, persistent, or recurrent disease during or following 2 systemic therapies

400 mg PO qDay

May reduce to 300 mg qDay, and then to 300 mg qDay for 5 days/wk if intolerant

Monitor: CBC, electrolytes, serum glucose and creatinine q2week during first 2 months and monthly thereafter

Dosage Modifications

Hepatic impairment

  • Mild/moderate (Child-Pugh A or B): Use with caution
  • Severe (Child-Pugh C): Contraindicated

Multiple Myeloma (Orphan)

Orphan designation for treatment of multiple myeloma

Sponsor

  • Merck Research Laboratories; Merck & Co Inc; PO Box 2000, RY 33-212; Rahway, NJ 07065-0900

Melanoma (Orphan)

Orphan designation for treatment of advanced melanoma (stages IIb, IIc, III, and IV)

Sponsor

  • Qameleon Therapeutics; Moslaan 32, 1433 WJ; Kudelstaart, Netherlands

Safety and efficacy not established

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Interactions

Interaction Checker

and vorinostat

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Diarrhea (52%)

            Fatigue (52%)

            Nausea (41%)

            Dysguesia (28%)

            Thrombocytopenia (26%)

            Anorexia (24%)

            Weight loss (20.9%)

            Muscle spasms (19.8%)

            Alopecia (18.6%)

            Chills (16%)

            Dry mouth (16%)

            Increase serum Cr (16%)

            Dizziness (15%)

            Constipation (15%)

            Vomiting (15%)

            Anemia (14%)

            Peripheral edema (12.8%)

            Headache (11.6%)

            Pruritus (11.6%)

            Cough (10.5%)

            Upper respiratory infection (10.5%)

            Decreased appetite

            Pyrexia

            1-10%

            Prolonged QT interval (3.5-6%)

            Pulmonary embolism (4.7%)

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            Warnings

            Contraindications

            Severe hepatic Impairment

            Cautions

            Congenital long QT syndrome, drugs/conditions that prolong QT interval; correct hypokalemia or hypomagnesemia before commencing treatment

            Thrombocytopenia and anemia may require dose modification or discontinuation; monitor blood counts every 2 weeks during first 2 months of therapy and monthly thereafter

            Severe thrombocytopenia with gastrointestinal bleeding reported with other HDAC inhibitors (e.g., valproic acid); monitor platelet counts more frequently

            Monitor for pertinent signs and symptoms of pulmonary embolism and deep vein thrombosis

            Potential for hyperglycemia; caution in diabetes; monitor blood glucose every 2 weeks during first 2 months of therapy and monthly thereafter

            Dose related anemia and thrombocytopenia may occur; modify dose or discontinue if reduction in platelets or Hgb

            Concomitant valproic acid

            May cause dizziness or fatigue

            Concomitant coumarin-derived anticoagulants

            Hepatic/renal impairment

            Nausea, vomiting and diarrhea; patients may require antiemetics, antidiarrheals, and fluid and electrolyte replacement to prevent dehydration

            Avoid pregnancy

            Drink at least 2 L of fluids daily

            Measure and correct abnormal electrolytes, creatinine, magnesium and calcium at baseline; monitor every 2 weeks during first 2 months of therapy and at least monthly during treatment

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            Pregnancy & Lactation

            Pregnancy

            Based on mechanism of action and findings from animal studies, therapy can cause fetal harm when administered to a pregnant woman

            There are insufficient data in pregnant women to inform a drug-associated risk of major birth defects and miscarriage

            Advise pregnant women of potential risk to fetus

            Animal data

            • In animal reproduction studies, administration of drug to pregnant rats and rabbits during period of organogenesis caused adverse developmental outcomes at maternal exposures approximately 0.5 times the human exposure based on AUC0-24 hours

            Reproductive potential

            • Can cause fetal harm when administered to a pregnant woman

            Pregnancy testing

            • Perform pregnancy testing in females of reproductive potential within 7 days prior to initiating therapy

            Contraception

            • Females: Advise patients of reproductive potential to use effective contraception during treatment and for at least 6 months after the last dose
            • Males: Advise males with female partners of reproductive potential to use effective contraception and to avoid fathering a child during treatment with ZOLINZA and for at least 3 months after the last dose

            Infertility

            • Based on findings in animals, therapy has the potential to affect female fertility

            Lactation

            There are no data on presence of drug or its metabolites in human milk, effects on a breastfed child, or on milk production; because many drugs are excreted in human milk and because of potential for serious adverse drug reactions in a nursing child, advise lactating women not to breastfeed during treatment and for at least 1 week after last dose

            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

            Histone deacetylase inhibitor for enzymes HDAC1, HDAC2, HDAC3, and HDAC6, which in turn alters chromatin structure and transcription factor activation; as a result, cell growth is terminated and apoptosis occurs

            Absorption

            Peak plasma time: 4 hr

            Peak plasma concentration (400 mg dose): 1.2±0.62 umol/L

            Fasted state has quicker peak time, but lower AUC and peak concentration

            Taken with a high fat meal increases extent of absorption by 33%

            Bioavailability: 43%

            Distribution

            Protein Bound: 71%

            Metabolism

            Liver

            Metabolites: Inactive

            Elimination

            Half-Life, Terminal: 2 hr

            Excretion: Urine 52%

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            Administration

            Oral Administration

            Take with food

            Drink at least 2 L of fluids daily

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            Formulary

            FormularyPatient Discounts

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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.