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Drugs reference index «Vorinostat»

Vorinostat

Pronunciation: (vore-IN-oh-stat)Class: Multikinase inhibitor

Trade Names:Zolinza- Capsules 100 mg

Pharmacology

Inhibits enzymatic activity of histone deacetylases (HDACs) at nanomolar concentrations. These enzymes catalyze the removal of acetyl groups from the lysine residue of proteins, including histones and transcription factors.

Pharmacokinetics

Absorption

When administered with high-fat meal, C max is 1.2 mcM and T max is 4 h. The extent of absorption is increased 33% when taken with a high-fat meal.

Distribution

Plasma protein binding is approximately 71%.

Metabolism

Metabolism involves glucuronidation and hydrolysis followed by beta-oxidation.

Elimination

Less than 1% of an administered dose is recovered unchanged in the urine. Total urinary recovery of vorinostat and 2 inactive metabolites averages 52%. Mean terminal t ½ is 2 h.

Indications and Usage

Treatment of cutaneous manifestation in patients with cutaneous T-cell lymphoma who have progressive, persistent, or recurrent disease during or following 2 systemic therapies.

Contraindications

Standard considerations.

Dosage and Administration

Adults

PO 400 mg once daily with food, continued as long as there is no evidence of progressive disease or unacceptable toxicity. If a patient is intolerant to therapy, the dose may be reduced to 300 mg once daily with food for 5 consecutive days each wk, as necessary.

General Advice

  • Take with food and drink at least 8 oz of liquid.

Storage/Stability

Store at 59° to 86°F.

Drug Interactions

Coumarin-derivative anticoagulants (eg, warfarin)

Prolongation of PT and INR may be prolonged.

Other HDAC inhibitors (eg, valproic acid)

The risk of GI bleeding and severe thrombocytopenia may be increased. Monitor platelet count every 2 wk for the first 2 mo.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Fatigue (52%); dizziness (15%); headache (12%); pyrexia (11%).

Dermatologic

Alopecia (19%); pruritus (12%).

GI

Diarrhea (52%); nausea (41%); dysgeusia (28%); anorexia (24%); dry mouth (16%); constipation, vomiting (15%); decreased appetite (14%).

Hematologic-Lymphatic

Thrombocytopenia (26%); anemia (14%).

Lab Tests

Increased serum glucose (69%); proteinuria (51%); increased serum creatinine (46%); increased blood creatinine (16%).

Metabolic-Nutritional

Decreased weight (21%).

Musculoskeletal

Muscle spasms (20%).

Respiratory

Cough, upper respiratory tract infection (11%); pulmonary embolism (5%).

Miscellaneous

Chills (16%); peripheral edema (13%); squamous cell carcinoma (4%).

Precautions

Monitor

Monitor CBC and blood chemistry, including electrolytes, glucose, and serum creatinine every 2 wk during the first 2 mo of therapy and every mo thereafter. Perform ECGs during treatment.

Pregnancy

Category D .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

Not evaluated; use with caution.

Hepatic Function

Not evaluated; use with caution.

GI

GI disturbances, including diarrhea, nausea, and vomiting, may occur. Antiemetic and antidiarrheal medications may be needed.

Hematologic

Dose-related thrombocytopenia and anemia may occur.

Hyperglycemia

May occur. Monitor serum glucose.

QTc prolongation

Although not studied, QTc prolongation has been reported.

Thromboembolism

Pulmonary embolism and deep vein thrombosis may occur.

Overdosage

Symptoms

No information is available.

Patient Information

  • Advise patient to read the patient information leaflet before using product the first time and with each refill.
  • Instruct patient to take exactly as prescribed and not to change the dose or discontinue therapy unless advised by health care provider.
  • Instruct patient to take the medicine with food and to drink at least 8 oz of liquid when taking the capsule.
  • Instruct patient to drink at least 2 L/day of fluid to prevent dehydration.
  • Advise patient to swallow capsule whole and not to open or crush capsule.
  • Instruct patient to report excessive diarrhea or vomiting to health care provider.
  • Instruct patient to seek immediate medical attention if unusual bleeding occurs.
  • Advise patient that if a dose is missed to take it as soon as they remember. If it is almost time for the next dose, skip the missed dose and go back to regular dosing schedule. Do not to take 2 doses at the same time.
  • Advise patient to keep all appointments and that blood cell counts, blood sugar, and other chemistries will be monitored every 2 wk for the first 2 mo of treatment then every mo thereafter.

Copyright © 2009 Wolters Kluwer Health.

  • Vorinostat MedFacts Consumer Leaflet (Wolters Kluwer)
  • vorinostat Advanced Consumer (Micromedex) - Includes Dosage Information
  • Zolinza Prescribing Information (FDA)
  • Zolinza Consumer Overview

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