vinblastine; vincaleukoblastine (Velban, Velsar, Alkaban-AQ)
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Introduction
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
- severe bone marrow suppression
- bacterial infection not under control
Dosage
- IV: 6-10 mg/m2 every 2-4 weeks
- 2 mg/m2/day IV continuously over 96 hours
- SC: (Kaposi's sarcoma): 0.1 mg/mL in 2% lidocaine injected into each lesion every 2-4 weeks
Pharmacokinetics
- metabolized by the liver by cyt P450 3A4
- active & inactive metabolites
- excreted through the biliary system
- elimination 1/2life is approximately 20 hours
elimination via liver
1/2life = 20 hours
Adverse effects
- common (> 10%)
- less common (1-10%)
- uncommon (< 1%)
- hemorrhagic colitis, neurotoxicity*, alopecia, bronchospasm, dermatitis, paresthesias, pain, photosensitivity, muscle pain, hyperuricemia
- 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:
- treatment is symptomatic
- no known antidotes
Drug interactions
- aminoglycosides: increased risk of ototoxicity given within 3-5 days
- zalcitabine: in combination increases neurotoxicity
- mitomycin -C in combination may result in severe bronchospasm
- any drug that inhibits cyt P450 3A4 may increase levels of vinblastine
- any drug that induces cyt P450 3A4 may diminish levels of vinblastine
Test interactions
increases serum K+
Mechanism of action
- vinka alkaloid
- inhibits microtubule formation in the mitotic spindle arresting cell division
More general terms
Additional terms
- cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
- intravenous (IV) extravasation
Component of
- brentuximab vedotin/doxorubicin/vinblastine/dacarbazine (A+AVD)
- doxorubicin (Adriamycin)/bleomycin/vinblastine/dacarbazine (ABVD)
References
- ↑ Merck tenth ed. (1983)
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 529
- ↑ Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 6.0 6.1 6.2 Deprecated Reference
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=8935
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=241903
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=13342
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=241902
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5147170
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5315216
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5667
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=657289