Bleomycine

Bleomycine Uses, Dosage, Side Effects, Food Interaction and all others data.

Although the exact mechanism of action of bleomycin sulfate is unknown, available evidence indicates that the main mode of action is the inhibition of DNA synthesis with some evidence of lesser inhibition of RNA and protein synthesis.

Bleomycine is known to cause single, and to a lesser extent, double-stranded breaks in DNA. In in vitro and in vivo experiments, bleomycin has been shown to cause cell cycle arrest in G2 and in mitosis. When administered into the pleural cavity in the treatment of malignant pleural effusion, bleomycin sulfate acts as a sclerosing agent.

Bleomycine is an antibiotic which has been shown to have antitumor activity. Bleomycine selectively inhibits the synthesis of deoxyribonucleic acid (DNA). The guanine and cytosine content correlates with the degree of mitomycin-induced cross-linking. At high concentrations of the drug, cellular RNA and protein synthesis are also suppressed. Bleomycine has been shown in vitro to inhibit B cell, T cell, and macrophage proliferation and impair antigen presentation, as well as the secretion of interferon gamma, TNFa, and IL-2. The antibiotic antitumor drugs are cell cycle-nonspecific except for Bleomycine (which has major effects in G2 and M phases).

Bleomycine
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Bleomycine
Availability	Prescription only
Generic	Bleomycin
Bleomycin Other Names	Bleocin, Bleomicin, Bleomicina, Bleomycin, Bleomycine, Bleomycinum
Related Drugs	methotrexate, Keytruda, rituximab, pembrolizumab, Rituxan, doxorubicin, cisplatin, cyclophosphamide, Opdivo, nivolumab
Type
Formula	C₅₅H₈₄N₁₇O₂₁S₃
Weight	Average: 1415.552 Monoisotopic: 1414.518979905
Protein binding	1%
Groups	Approved, Investigational
Therapeutic Class	Cytotoxic Chemotherapy
Manufacturer
Available Country	Netherlands
Last Updated:	September 19, 2023 at 7:00 am

Uses

Bleomycine is used for Malignant effusions, Lymphoma, Squamous cell or testicular tumours

Bleomycine is also used to associated treatment for these conditions: Cervical Cancers, Head and Neck Carcinoma, Intracranial Germ Cell Tumors, Lymphoma, Hodgkins, Malignant Pleural Effusions, Non-Hodgkin's Lymphoma (NHL), Ovarian Cancer, Penile Cancer, Pneumothorax, Testicular Cancer, Vulvar Cancers, Early Kaposi's sarcoma

How Bleomycine works

Although the exact mechanism of action of bleomycin is unknown, available evidence would seem to indicate that the main mode of action is the inhibition of DNA synthesis with some evidence of lesser inhibition of RNA and protein synthesis. As evident in in vitro studies, the DNA-cleaving actions of bleomycin is dependent on oxygen and metal ions. 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.

Dosage

Bleomycine dosage

Squamous cell carcinoma:

Over 80 years: 15 mg per week (in a single or divided doses), total 100 mg
70-79 years: 30 mg/week, total 150-200 mg
60-69 years: 30-60 mg/week, total 200-300 mg
Under 60 years: 30-60 mg/wk, total 500 mg. All to be applied through slow intravenous or intravenous infusion.

Malignant lymphomas: 15 mg once or twice a week to a total dose of 225 mg.

CrCl 20-40 mcg/ml: Admin 50% of normal dose.

IM/SC: Add 1-5 mL or 2-10 mL of sterile water for inj, NaCl 0.9% inj, or bacteriostatic water for inj to the vial labelled as containing 15 IU or 30 IU of bleomycin, respectively, to provide a soln containing 3-15 IU/mL.

IV: Add 5 mL or 10 mL of NaCl 0.9% into the vial labelled as containing 15 IU or 30 IU of bleomycin, respectively, to provide a soln containing ≤3 IU/mL. Admin slowly over a 10-min period. Intrapleural: Dissolve 60 IU of bleomycin in 50-100 mL NaCl 0.9% inj.

Side Effects

Common side effects of Bleomycine Sulfate include injection site reactions (pain, redness, warmth, itching, or swelling), fever, chills, vomiting, loss of appetite, weight loss, darkening or discoloration of the skin, changes in fingernails or toenails, itching, or pain near your tumor.

Toxicity

Excessive exposure may cause fever, chills, nausea, vomiting, mental, confusion, and wheezing. Bleomycine may cause irritation to eyes, skin and respiratory tract. It may also cause a darkening or thickening of the skin. It may cause an allergic reaction.

Precaution

Caution should be taken in patient with severe heart disease, Renal impairment, Elderly & Pregnancy.

Interaction

Increased incidence and severity of lung toxicity with previous or concurrent radiotherapy to the chest. Combination with vinca alkaloids may result to a syndrome corresponding to morbus Raynaud, ischaemia which can lead to necrosis of peripheral parts of the body (fingers, toes, nose tip). May reduce the absorption of phenytoin. Increased risk of agranulocytosis with clozapine.

Food Interaction

No interactions found.

Bleomycine Drug Interaction

Moderate: doxorubicin, doxorubicin, cyclophosphamide, cyclophosphamide, etoposide, etoposideUnknown: arginine, arginine, levocarnitine, levocarnitine, vincristine, vincristine, valproic acid, valproic acid, cyanocobalamin, cyanocobalamin, pyridoxine, pyridoxine, cholecalciferol, cholecalciferol

Bleomycine Disease Interaction

Major: pulmonary infiltrates/fibrosis, renal dysfunctionModerate: hepatic impairment

Elimination Route

Systemic absorption is approximately 45%.

Half Life

115 minutes

Elimination Route

It was reported that patients with moderately severe renal failure excreted less than 20% of the dose in the urine.

Pregnancy & Breastfeeding use

Pregnancy Category D. There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk.