      Document 0113
 DOCN  DRG0113
 UNIQUE IDENTIFIER        DRG-0134
 NAME OF SUBSTANCE        Vinblastine sulfate [USAN 1996]
 REGISTRY NUMBER          143-67-9
 STANDARD CHEMICAL NAME   Vincaleukoblastine sulfate [USAN 1996]
 SYNONYMS                 Velban [USAN 1996]
 SYNONYMS                 Velsar [USAN 1993]
 PROTOCOL ID NUMBERS      NIAID ACTG 149
 SECONDARY SOURCE ID      NSC-49842 [USAN 1996]
 SECONDARY SOURCE ID      29060-LE [USAN 1996]
 PHARMACOLOGICAL ACTION   MODE OF ACTION: In vitro studies suggest an
                          interference with metabolic pathways of amino
                          acids leading from glutamic acid to the
                          citric acid cycle and to urea. In vivo
                          studies tend to confirm the in vitro results.
                          Other studies indicate that vinblastine
                          effects cell energy production required for
                          mitosis and interferes with nucleic acid
                          synthesis. In vitro, the drug arrests growing
                          cells in metaphase. Pharmacokinetic studies
                          in cancer patients have shown a triphasic
                          serum decay pattern following rapid
                          intravenous injection. The initial, middle,
                          and terminal half-lives are 3.7 minutes, 1.6
                          hours, and 24.8 hours, respectively. Major
                          route of excretion may be through the biliary
                          system; thus, toxicity may be increased in
                          patients with hepatic excretory
                          insufficiency. [PDR 1995]
 DISEASES STUDIED/TREATED Treatment of Hodgkin's disease in
                          HIV-infected patients [Int Conf AIDS 1993 Jun
                          6-11;9(1): (abstract no WS-B20-4)]
 DISEASES STUDIED/TREATED Kaposi's sarcoma [Int Conf AIDS 1993 Jun
                          6-11;9(1):(abstract no. WS-B20-4)]
 CLASSIFICATION CODE      Antineoplastic [USAN 1996]
 OTHER MAJOR USES         Treatment of generalized Hodgkin's disease;
                          lymphocytic lymphoma; histiocytic lymphoma;
                          mycosis fungoides; advanced carcinoma of the
                          testis; Kaposi's sarcoma; Letterer-Siwe
                          disease (histiocytosis X); choriocarcinoma
                          resistant to other chemotherapeutic agents;
                          and breast carcinoma unresponsive to
                          appropriate endocrine surgery and hormone
                          therapy [PDR 1995]
 SUBSTANCE INTERACTIONS   Phenytoin and antineoplastic chemotherapy
                          combinations including vinblastine have been
                          reported to reduce blood levels of the
                          anticoagulant and to increase seizure
                          activity. Possible interaction with
                          allopurinol, colchicine, probenecid,
                          sulfinpyrazone, blood dyscrasia-causing
                          medications, bone marrow depressants,
                          radiation therapy, killed-virus vaccines, and
                          live-virus vaccines. [PDR 1995] [USP DI 1995]
 ADVERSE EFFECTS          Adverse effects include leukopenia,
                          thrombocytopenia (generally in patients with
                          bone marrow impairment by prior therapy),
                          anemia, alopecia, constipation, anorexia,
                          nausea, vomiting, abdominal pain, other
                          gastrointestinal effects, hypertension,
                          neurologic effects, acute shortness of
                          breath, bronchospasm, malaise, bone pain,
                          pain in tumor-containing tissue, jaw pain.
                          [PDR 1995]
 CONTRAINDICATIONS        Contraindicated in patients with significant
                          granulocytopenia (unless caused by disease
                          being treated) or with bacterial infections.
                          Also contraindicated in pregnant women.
                          Toxicity of the drug is enhanced in the
                          presence of hepatic insufficiency. [PDR 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Alkaloid extracted from
                          Vinca rosea Linn, commonly known as
                          periwinkle [PDR 1995]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C46H58N4O9.H2SO4 [USAN
                          1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 909.07 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: White to off-white
                          powder [PDR 1995]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY: Freely soluble in water, soluble
                          in methanol, slightly soluble in ethanol,
                          insoluble in benzene, ether and naphtha [PDR
                          1995]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: 10 mg vials. [PDR 1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Intravenous. FATAL IF GIVEN
                          INTRATHECALLY. [PDR 1995] [Int Conf AIDS 1993
                          Jun 6-11;9(1): (abstract no. WS-B20-4)]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Intralesionally for
                          Kaposi's sarcoma. [PDR 1995] [Int Conf AIDS
                          1993 Jun 6-11;9(1): (abstract WS-B20-4)]
 SUBSTANCE DELIVERY DATA  STORAGE: Store at 2-8 C (36-46 F) for a
                          maximum of 28 days. [PDR 1995]
 REFERENCES               Tirelli U, Errante D, Dolcetti R, Gloghini A,
                          Serraino D, Vaccher E, Franceschi S, Boiocchi
                          M, Carbone A. Hodgkin's disease and human
                          immunodeficiency virus infection:
                          clinicopathologic and virologic features of
                          114 patients from the Italian Cooperative
                          Group on AIDS and Tumors. J Clin Oncol. 1995
                          Jul;13(7):1758-67.
 REFERENCES               Tami TA, Sharma PK. Intralesional vinblastine
                          therapy for Kaposi's sarcoma of the
                          epiglottis. Otolaryngol Head Neck Surg. 1995
                          Sep;113(3):283-5.
 REFERENCES               Conant MA. Management of human
                          immunodeficiency virus-associated
                          malignancies. Recent Results Cancer Res.
                          1995;139:423-32.
 REFERENCES               Errante D, Tirelli U, Gastaldi R, Milo D,
                          Nosari AM, Rossi G, Fiorentini G, Carbone A,
                          Vaccher E, Monfardini S. Combined
                          antineoplastic and antiretroviral therapy for
                          patients with Hodgkin's disease and human
                          immunodefiency virus infection. A prospective
                          study of 17 patients. The Italian Cooperative
                          Group on AIDS and Tumors (GICAT). Cancer.
                          1994 Jan 15;73(2):437-44.
 REFERENCES               von Gunten CF, Roth EL, Von Roenn JH. Raynaud
                          phenomenon in three patients with acquired
                          immune deficiency syndrome-related Kaposi
                          sarcoma treated with bleomycin. Cancer. 1993
                          Sep 15;72(6):2004-6.
 REFERENCES               Moyle G, Youle M, Barton S. Intralesional
                          vinblastine in the treatment of oral Kaposi's
                          sarcoma. Br J Clin Pract. 1993
                          Mar-Apr:47(2):79-80.
 REFERENCES               Nichols M, Flaitz C, Hicks J. Intraoral
                          Kaposi's sarcoma in AIDS and intralesional
                          vinblastine treatment. Int Conf AIDS 1993 Jun
                          6-11;9(1):63 (abstract no. WS-B20-4).
 REFERENCES               Epstein JB. Treatment of oral Kaposi sarcoma
                          with intralesional vinblastine. Cancer 1993
                          Mar 1;71(5):1722-5.
 REFERENCES               Boudreaux AA, Smith LL, Cosby CD, Bason MM,
                          et al. Intralesional vinblastine for
                          cutaneous Kaposi's sarcoma associated with
                          acquired immunodeficiency syndrome. A
                          clinical trial to evaluate efficacy and
                          discomfort associated with infection. J Am
                          Acad Dermatol 1993 Jan;28(1):61-5.
 REFERENCES               Vaccher E, Tirelli U, Milo D, Chieppa F,
                          Alberici F, Branz F, Ambrosini G, Giudici M,
                          Lazzarin A, Cargnel A, et al. Hodgkin's
                          disease and HIV infection (HD-HIV): a report
                          of 92 patients from the GICAT (Italian
                          Cooperative Group on AIDS and Tumors), with
                          emphasis on prospective study with combined
                          chemotherapy and zidovudine (AZT) in 16
                          patients. Int Conf AIDS. 1992 Jul
                          19-24;8(1):Mo16 (abstract no. MoB 0059).
 ENTRY MONTH              9201
 LAST REVISION DATE       960111
 

SOURCE: National Library of Medicine, Bethesda, MD.  Distributed by AEGIS.
