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vinblastine; vincaleukoblastine (Velban, Velsar, Alkaban-AQ)

C46-H58-N4-O9. Tradenames: Velban, Velsar, Alkaban-AQ. Indications: - Hodgkin's disease - non-Hodgkin's lymphoma - lymphocytic lymphomas including mycosis fungoides - Kaposi's sarcoma - breast cancer - non-small cell lung cancer - chronic lymphocytic leukemia (CML) - advanced testicular germ cell tumors - bladder cancer - head & neck cancer [6] - neuroblastoma - Letterer-Siwe syndrome - gestational trophoblastic disease - testicular cancer [6] Contraindications: 1) severe bone marrow suppression 2) bacterial infection not under control Dosage: 1) IV: 6-10 mg/m2 every 2-4 weeks - 2 mg/m2/day IV continuously over 96 hours 2) SC: (Kaposi's sarcoma): 0.1 mg/mL in 2% lidocaine injected into each lesion every 2-4 weeks Injection: 1 mg/mL (10 mL). Pharmacokinetics: 1) metabolized by the liver by cyt P450 3A4 -> active & inactive metabolites 2) excreted through the biliary system 3) elimination 1/2life is approximately 20 hours Adverse effects: 1) common (> 10%) a) alopecia b) myelosuppression - dose-limiting toxicity - WBC & platelets moderate to severe - onset 4-7 days - nadir 4-10 days - recovery 17 days 2) less common (1-10%) - tachycardia, orthostatic hypotension, depression, malaise, seizures, headache, rash, paralytic ileus, stomatitis, jaw pain, muscle pain, urinary retention, hyperuricemia, photosensitivity 3) uncommon (< 1%) - hemorrhagic colitis, neurotoxicity*, alopecia, bronchospasm, dermatitis, paresthesias, pain, photosensitivity, muscle pain, hyperuricemia 4) other - extravasation: vesicant; tissue irritation & necrosis can occur with extravasation - emetic potential moderate (30-60%) - neurotoxicity rare at clinical doses - peripheral neuropathy - loss of deep tendon reflexes (DTR) - weakness - constipation - ileus - urinary retention - SIADH - ototoxicity Toxicology: 1) treatment is symptomatic 2) no known antidotes Drug interactions: 1) aminoglycosides: increased risk of ototoxicity given within 3-5 days 2) zalcitabine: in combination increases neurotoxicity 3) mitomycin -C in combination may result in severe bronchospasm 4) any drug that inhibits cyt P450 3A4 may increase levels of vinblastine 5) any drug that induces cyt P450 3A4 may diminish levels of vinblastine Test interactions: increases serum K+ Mechanism of action: 1) vinka alkaloid 2) inhibits microtubule formation in the mitotic spindle arresting cell division

Related

cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4) intravenous (IV) extravasation

General

antimitotic agent; mitotic inhibitor (antineoplastic agent) vinca alkaloid

Properties

SIZE: MW = 811 G/M MISC-INFO: elimination route LIVER pregnancy-category D 1/2life 20 HOURS

Database Correlations

PUBCHEM correlations

References

  1. Merck tenth ed. (1983)
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 529
  5. Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: 220233 (subscription needed) http://www.prescribersletter.com
  6. Deprecated Reference

Component-of

brentuximab vedotin/doxorubicin/vinblastine/dacarbazine (A+AVD) doxorubicin (Adriamycin)/bleomycin/vinblastine/dacarbazine (ABVD)