Dictionary:
ble·o·my·cin (blē'ə-mī'sĭn)  |
[Alteration of phleomycin, a related antibiotic : phleo-, of unknown meaning + -MYCIN.]
| 5min Related Video: bleomycin |
| Oncology Encyclopedia: Bleomycin |
Key Terms: DNA.
Definition
Bleomycin (Blenoxane) kills cancer cells by damaging the genetic material known as DNA, thus preventing cells from repairing themselves.
Purpose
Bleomycin is used in the treatment of a number of different cancers, including cancer of the head and neck, skin, esophagus, lung, testis, penis, vulva, cervix, and genitourinary tract. In addition, it is used in the treatment of Hodgkin's disease and non-Hodgkin's lymphomas. It may also be used to treat Kaposi's sarcoma.
Because bleomycin is used in the treatment of so many different cancers, only a sampling of its uses can be provided here. In the treatment of Hodgkin's disease, one chemotherapy regimen used is the so-called ABVD, which consists of doxorubicin, bleomycin, vinblastine, and dacarbazine. Another regimen is called MOPP/ABV, which consists of mechlorethamine, vincristine, prednisone, procarbazine, doxorubicin, bleomycin, and vinblastine.
A treatment used for stage III and IV non-Hodgkin's lymphoma is the CHOP-bleomycin regimen, which consists of cyclophosphamide, hydroxydaunomycin, vincristine, prednisone, and bleomycin. Another approach to the same illness involves the m-BACOD chemotherapy regimen, which consists of methotrexate, bleomycin, doxorubicin, cyclophosphamide, vincristine, and dexamethasone. Yet another approach to treating this disease is called ProMACE-CytaBOM, and consists of cyclophosphamide, doxorubicin, etoposide, prednisone, cytarabine, bleomycin, vincristine, methotrexate, and leucovorin.
Description
Bleomycin is an antitumor antibiotic that fights cancer by attacking the DNA in cancerous cells, thus interfering with cell growth.
Recommended Dosage
A dose of 0.25-0.50 units/kg (10-20 units per square meter) is given once or twice a week either intravenously, intramuscularly, or subcutaneously. A small test dose should be given first to test for a possible severe allergic reaction.
Precautions
Patients who receive certain forms of oxygen therapy while taking bleomycin or who receive anesthesia while taking bleomycin are at increased risk for developing serious lung problems.
Patients given bleomycin may develop an acute allergic reaction that may be fatal in rare cases. Therefore, a patient should only receive a small test dose of bleomycin the first time the drug is administered. After this initial dose the patient is observed carefully for one hour. Assuming no further problems appear, the patient may then receive a standard dose.
The likelihood that lung damage will occur increases if a patient receives more than 450–500 units of the drug during an entire lifetime. So, it is prudent to limit the amount of this medication given. Furthermore, it may be unwise to give bleomycin in regimens containing cyclophosphamide, as this combination also increases the likelihood that lung damage will occur.
Side Effects
Lung problems are a serious side effect affecting some patients who receive bleomycin. While lung problems can appear regardless of how much of the medicine is given, they are more likely to appear if a patient receives more than a certain amount of the medicine—250 units according to some authorities and 450–500 units according to others. The appearance of a dry cough may indicate the development of lung problems. Lung damage can be assessed by measuring the rate at which the patient is able to transfer gas across the lung membranes (DLCO or diffusion lung capacity).
Other side effects of bleomycin may include skin problems and alteration of skin color, allergic reactions, Raynaud's phenomenon, and hair loss (alopecia). In addition, headache, and nausea and vomiting may occur. Rheumatoid arthritis may worsen during bleomycin therapy. Patients with testicular tumors who receive multiple chemotherapy agents including bleomycin may develop Raynaud's phenomenon and cardiovascular disease. Raynaud's phenomenon, which affects the fingers and toes, may involve pain, pale color, and abnormal sensation (for instance, burning or prickling).
Approximately 1 out of every 100 patients who takes bleomycin experiences a reaction that involves chills, fever, wheezing, low blood pressure, and mental confusion. Unlike many other cancer drugs, bleomycin is not likely to cause any damage to the bone marrow.
Patients may be given steroids before bleomycin therapy is started in an effort to reduce the side effects of the drug.
Interactions
Bleomycin is often given in combination with with other anticancer drugs, for example cisplatin, vinblastine, and etoposide. Such combinations have been found to be more effective than single drug therapy.
—Bob Kirsch
| Drug Info: Bleomycin |
Brand names: Blenoxane®
Chemical formula:
Bleomycin Sulfate Solution for injection
What is this medicine?
BLEOMYCIN is a chemotherapy drug. It is used to treat many kinds of cancer like lymphoma, cervical cancer, head and neck cancer, and testicular cancer. It is also used to prevent and to treat fluid build-up around the lungs caused by some cancers.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•cigarette smoker
•kidney disease
•lung disease
•recent or ongoing radiation therapy
•an unusual or allergic reaction to bleomycin, other chemotherapy agents, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
This drug is given as an infusion into a vein or a body cavity. It can also be given as an injection into a muscle or under the skin. It is administered in a hospital or clinic by a specially trained health care professional.
Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What if I miss a dose?
If you miss a dose, use it as soon as you can. If it is almost time for your next dose, useWhat may interact with this medicine?
•certain antibiotics given by injection
•cisplatin
•cyclosporine
•diuretics
•foscarnet
•medicines to increase blood counts like filgrastim, pegfilgrastim, sargramostim
•vaccines
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Visit your doctor for checks on your progress. This drug may make you feel generally unwell. This is not uncommon, as chemotherapy can affect healthy cells as well as cancer cells. Report any side effects. Continue your course of treatment even though you feel ill unless your doctor tells you to stop.
Call your doctor or health care professional for advice if you get a fever, chills or sore throat, or other symptoms of a cold or flu. Do not treat yourself. This drug decreases your body's ability to fight infections. Try to avoid being around people who are sick.
Avoid taking products that contain aspirin, acetaminophen, ibuprofen, naproxen, or ketoprofen unless instructed by your doctor. These medicines may hide a fever.
Do not become pregnant while taking this medicine. Women should inform their doctor if they wish to become pregnant or think they might be pregnant. There is a potential for serious side effects to an unborn child. Talk to your health care professional or pharmacist for more information. Do not breast-feed an infant while taking this medicine.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing problems
•chest pain
•confusion
•cough
•fast, irregular heartbeat
•feeling faint or lightheaded, falls
•fever or chills
•mouth sores
•pain, tingling, numbness in the hands or feet
•trouble passing urine or change in the amount of urine
•yellowing of the eyes or skin
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•darker skin color
•hair loss
•irritation at site where injected
•loss of appetite
•nail changes
•nausea and vomiting
•weight loss
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
This drug is given in a hospital or clinic and will not be stored at home.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
| Veterinary Dictionary: bleomycin |
A polypeptide antibiotic mixture having antineoplastic properties, obtained from cultures of Streptomyces verticellus. Evidence indicates that bleomycin inhibits cell division, thymidine incorporation into DNA, and DNA synthesis. Has been used in dogs and cats in the treatment of squamous cell carcinoma, but side-effects, including pneumonia or pulmonary scarring, limit its use.
| Wikipedia: Bleomycin |
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Bleomycin
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| Systematic (IUPAC) name | |
| (3-{[(2'-{(5S,8S,9S,10R,13S)-15-{6-amino-2- [(1S)-3-amino-1-{[(2S)-2,3-diamino-3-oxopropyl]amino}-3-oxopropyl] -5-methylpyrimidin-4-yl}-13-[{[(2R,3S,4S,5S,6S)-3- {[(2R,3S,4S,5R,6R)-4-(carbamoyloxy)-3,5-dihydroxy-6- (hydroxymethyl)tetrahydro-2H-pyran-2-yl]oxy} -4,5-dihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl]oxy} (1H-imidazol-5-yl)methyl]-9-hydroxy-5-[(1R)-1-hydroxyethyl]-8,10-dimethyl-4,7,12,15-
tetraoxo-3,6,11,14-tetraazapentadec-1-yl}-2,4'-bi-1,3- thiazol-4-yl)carbonyl]amino}propyl)(dimethyl)sulfonium |
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| Identifiers | |
| CAS number | 11056-06-7 |
| ATC code | L01DC01 |
| PubChem | 456190 |
| DrugBank | APRD00453 |
| ChemSpider | 401687 |
| Chemical data | |
| Formula | C55H84N17O21S3 |
| Mol. mass | 1415.551 |
| SMILES | eMolecules & PubChem |
| Pharmacokinetic data | |
| Bioavailability | well absorbed |
| Metabolism | ? |
| Half life | 2 hours |
| Excretion | renal (60-70%) |
| Therapeutic considerations | |
| Pregnancy cat. |
D(US) |
| Legal status |
? |
| Routes | intramuscular and subcutaneous |
 (what is this?) (verify) |
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Bleomycin is a glycopeptide antibiotic produced by the bacterium Streptomyces verticillus. Bleomycin refers to a family of structurally related compounds. When used as an anti-cancer agent, the chemotherapeutical forms are primarily bleomycin A2 and B2. Bleomycin A2 is shown in the image. The drug is used in the treatment of Hodgkin lymphoma (as a component of the ABVD regimen), squamous cell carcinomas, and testicular cancer, as well as in the treatment of pleurodesis[1] and plantar warts. [2]
Contents |
Bleomycin was first discovered in 1966 when the Japanese scientist Hamao Umezawa found anti-cancer activity while screening culture filtrates of S. verticullus. Umezawa published his discovery in 1966.[3] The drug was launched in Japan by Nippon Kayaku in 1969. In the US bleomycin gained Food and Drug Administration (FDA) approval in July 1973. It was initially marketed in the US by the Bristol-Myers Squibb precursor Bristol Laboratories under the brand name Blenoxane.
Bristol-Myers Squibb still supplies Blenoxane. There are also generic versions of bleomycin available from APP Pharmaceuticals, Bedford, Sicor (Teva) and Hospira.
Bleomycin acts by induction of DNA strand breaks.[4] Some studies suggest that bleomycin also inhibits incorporation of thymidine into DNA strands. DNA cleavage by bleomycin depends on oxygen and metal ions, at least in vitro. It is believed that bleomycin chelates metal ions (primarily iron) producing a pseudoenzyme that reacts with oxygen to produce superoxide and hydroxide free radicals that cleave DNA. In addition, these complexes also mediate lipid peroxidation and oxidation of other cellular molecules.
Bleomycin is a nonribosomal peptide that is a hybrid peptide-polyketide natural product. The peptide/polyketide/peptide backbone of the bleomycin aglycon is assembled by the bleomycin megasynthetase, which is made of both nonribosomal peptide synthetase (NRPS) and polyketide synthase (PKS) modules. Nonribosomal peptides and polyketides are synthesized from amino acids and short carboxylic acids by NRPSs and PKSs, respectively. These NRPSs and PKSs use similar strategies for the assembly of these two distinct classes of natural products. Both NRPs and type I PKSs are organized into modules. The structural variations of the resulting peptide and polyketide products are determined by the number and order of modules on each NRPS and PKS protein.
The biosynthesis of the bleomycin aglycon can be easily visualized in three stages (see Figure 2):
On the basis of the bleomycin structure and the deduced functions of individual NRPS and PKS domains and modules, a linear model for the bleomycin megasynthetase-templated assembly of the bleomycin peptide/polyketide/peptide aglycon was proposed from nine amino acids and one acetate.
The most serious complication of bleomycin is pulmonary fibrosis and impaired lung function. It has been suggested that bleomycin induces sensitivity to oxygen toxicity[5] and recent studies support the role of the proinflammatory cytokines IL-18 and IL-1beta in the mechanism of bleomycin-induced lung injury.[6] Past history of treatment with bleomycin should therefore always be disclosed to the anaesthetist prior to undergoing a procedure requiring general anaesthesia.
Other side effects include fever, rash, dermatographism, hyperpigmentation, alopecia and Raynaud's phenomenon.
This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)
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 | Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved. Read more |
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| Oncology Encyclopedia. Gale Encyclopedia of Cancer. Copyright © 2006 by The Gale Group, Inc. All rights reserved. Read more |
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| Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved. Read more |
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| Veterinary Dictionary. Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved. Read more |
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| Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Bleomycin". Read more |
