      Document 0202
 DOCN  DRG0202
 UNIQUE IDENTIFIER        DRG-0045
 NAME OF SUBSTANCE        Bleomycin [USAN 1996]
 REGISTRY NUMBER          11056-06-7
 RELATED REGISTRY NUMBER  9041-93-4 (sulfate)
 SYNONYMS                 Blenoxane [USAN 1996]
 SYNONYMS                 Bleo [Merck Index 1989]
 SYNONYMS                 Bleomycin sulfate [USAN 1996]
 PROTOCOL ID NUMBERS      NIAID ACTG 008
 PROTOCOL ID NUMBERS      NIAID ACTG 074
 PROTOCOL ID NUMBERS      NIAID ACTG 075
 PROTOCOL ID NUMBERS      NIAID ACTG 094
 PROTOCOL ID NUMBERS      NIAID ACTG 142
 PROTOCOL ID NUMBERS      NIAID ACTG 149
 PROTOCOL ID NUMBERS      FDA 121A
 PROTOCOL ID NUMBERS      FDA 134A
 PROTOCOL ID NUMBERS      FDA 134B
 PROTOCOL ID NUMBERS      NIAID ACTG 163
 PROTOCOL ID NUMBERS      NIAID ACTG 286
 SECONDARY SOURCE ID      DRG
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Affects the G2 phase of cell
                          division, possibly binding to DNA and
                          inducing lability of the DNA structure and
                          decreasing DNA synthesis. Following
                          intrapleural or intraperitoneal
                          administration about 45% of the dose is
                          absorbed. In patients with a creatinine
                          clearance greater than 35 ml/min the drug has
                          a half-life of 115 minutes. If the clearance
                          is less than this the half-life is increased
                          exponentially as the creatinine clearance
                          decreases. Renal excretion is 60-70%, mainly
                          as unchanged drug. [USP DI 1995]
 DISEASES STUDIED/TREATED Used alone or in combination chemotherapy for
                          various AIDS-related neoplasms [AHFS Drug
                          Information 1995]
 CLASSIFICATION CODE      Antineoplastic [USAN 1996]
 OTHER MAJOR USES         Used alone or in combination in palliative
                          cancer therapy for a variety of neoplasms
                          including squamous cell carcinoma, lymphomas
                          and testicular carcinomas [PDR 1995]
 SUBSTANCE INTERACTIONS   Interactions of bleomycin have been reported
                          with general anesthetics, other
                          antineoplastics, cisplatin, vincristine, and
                          with radiation therapy. [USP DI 1995]
 ADVERSE EFFECTS          May cause pneumonitis, occasionally
                          progressing to pulmonary fibrosis (this
                          occurs most frequently in elderly patients
                          and in those receiving > 400 units total
                          dose); an immediate hypersensitivity reaction
                          occurs in 1 percent of patients. The
                          following are the most frequently reported
                          side effects: erythema, rash, strial
                          vesiculation, hyperpigmentation, and
                          tenderness of the skin. Hyperkeratosis, nail
                          changes, alopecia, pruritus, and stomatitis
                          have also been reported. [PDR 1995]
 CONTRAINDICATIONS        Should not be used by patients who have
                          demonstrated a hypersensitive or
                          idiosyncratic reaction to bleomycin. Safe use
                          of blenoxane in pregnant women has not been
                          established. [PDR 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Bleomycin sulfate is a
                          mixture of basic cytotoxic glycopeptide
                          antibiotics produced by Streptomyces
                          verticillus. Bleomycin A2 and B2 are the
                          major components in this mixture [AHFS Drug
                          Information 1995]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C55H84N17O21S3 (Bleomycin
                          A2) [Merck Index 1983]. C55H84N17O21S3.xH2S04
                          (Bleomycin sulfate) [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY: Very soluble in water and
                          methanol, slightly soluble in ethanol,
                          insoluble in acetone, ethyl acetate, butyl
                          acetate, or ether [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: A cream colored
                          amorphous powder [AHFS Drug Information 1995]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: Colorless or yellowish
                          powder which becomes bluish depending on its
                          copper content [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   STABILITY: Hygroscopic; inactivated in vitro
                          by agents containing sulfhydryl groups,
                          hydrogen peroxide, and ascorbic acid [USP DI
                          1995]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Vial containing 15 units as
                          sterile bleomycin sulfate for parenteral
                          administration. [PDR 1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Intravenous, intramuscular,
                          subcutaneous, intra-arterial, intracavitary,
                          and intrapleural. [AHFS Drug Information
                          1995]
 SUBSTANCE DELIVERY DATA  STORAGE: Store under refrigeration (2-8 C);
                          stable at room temperature for 24 hours in
                          0.9 percent NaCl or 5 percent dextrose
                          solution, or for 14 or more days if
                          refrigerated. [USP DI 1995]
 MANUFACTURERS            Bristol-Myers
 REFERENCES               Opravil M, Hodapp K, Luthy R. Interferon
                          alpha-2a+zidovudine vs. bleomycin+zidovudine
                          for HIV-associated Kaposi's sarcoma. Int Conf
                          AIDS. 1994 Aug 7-12;10(1):179 (abstract no.
                          PB0141).
 REFERENCES               Reddy M, Remick S, Herman D, Willis K, et al.
                          Continuous infusion (CI) bleomycin in
                          AIDS-related Kaposi's sarcoma (KS) (Meeting
                          Abstract). Proc Annu Meet Am Assoc Cancer
                          Res. 1993;34:A1118.
 REFERENCES               Von Gunten CF, Roth EL, Von Roenn JH. Raynaud
                          phenomenon in three patients with acquired
                          immune deficiency syndrome-related Kaposi's
                          sarcoma treated with bleomycin. Cancer. 1993
                          Sep 15;72(6):2004-6.
 REFERENCES               Schurmann D, Weiss R, Jautzke G, Pohle HD,
                          Ruf B. Intensive treatment of AIDS-related
                          non-Hodgkin's lymphomas with the MACOP-B
                          protocol. Int Conf AIDS. 1993 Jun
                          6-11;9(1):404 (abstract no. PO-B13-1616).
 REFERENCES               Lipman MC, Swaden LS, Sabin CA, Collis C,
                          Johnson MA. Kaposi's sarcoma in HIV infection
                          treated with vincristine and bleomycin
                          [letter; comment]. AIDS. 1993 Apr;7(4):592-3.
 REFERENCES               Taillan B, Pesce A, Garnier G, Vinti H,
                          Fuzibet JG, Cassuto JP, Dujardin P. AIDS
                          related malignant lymphoma: results of MACOP
                          B chemotherapy. Int Conf AIDS. 1992 Jul
                          19-24;8(2):B108 (abstract no. PoB 3127).
 REFERENCES               Dormann A, Gruenewald T, Ross ME, Pohle HD,
                          Ruf B, Schueler W. Liposomal-encapsulated
                          cytotoxic agent daunorubicin (LD) versus
                          conventional three-drug chemotherapy (CC) in
                          AIDS patients with Kaposi's sarcoma
                          (KS)--preliminary results. Int Conf AIDS.
                          1992 Jul 19-24;8(1):Th74 (abstract no. ThD
                          1545).
 REFERENCES               Gill PS, Rarick M, McCutchan JA, Slater L,
                          Parker B, Muchmore E, Bernstein-Singer M,
                          Akil B, Espina BM, Krailo M, et al. Systemic
                          treatment of AIDS-related Kaposi's sarcoma:
                          results of a randomized trial. Am J Med. 1991
                          Apr;90(4):427-33.
 REFERENCES               Gisselbrecht C, Tirelli U, Oksenhendler E,
                          Gabarre J, Gastaldi R, Farcet JP, Lepage E,
                          Raphael M, Monfardini S. TREATMENT OF
                          NON-HODGKIN'S LYMPHOMAS (NHL) AND HUMAN
                          IMMUNODEFICIENCY VIRUS (HIV) (MEETING
                          ABSTRACT). Fifteenth Symposium of the
                          International Association for Comparative
                          Research on Leukemia and Related Diseases.
                          October 6-11, 1991, Padova/Venice, Italy, p.
                          30. 1991.
 REFERENCES               Guermonprez G, Katlama C, Caumes E, Brucker
                          G, Kosenheim M, Gentilini M. Bleomycin in
                          treatment of AIDS related Kaposi's sarcoma.
                          Int Conf AIDS. 1990 Jun 20-23;6(3):213
                          (abstract no. S.B.511).
 ENTRY MONTH              8906
 LAST REVISION DATE       950908
 

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