Capreomycin
J04AB30
Colorless solid
Antibiotics
Inhibitors of protein biosynthesis
Soluble in water, insoluble in organic solvents
Risk
250 mg · kg -1 ( LD50, mouse, i.v.)
Template: Infobox chemical / molecular formula search available
Capreomycin (trade name Capastat ®; initial manufacturer Eli Lilly) is a drug from the group of polypeptide antibiotics, which is used as second choice in the treatment of multidrug-resistant tuberculosis.
- 2.1 Mechanism of action ( pharmacodynamics )
- 2.2 Absorption and distribution in the body ( pharmacokinetics )
- 3.1 Chemical and pharmaceutical information
- 3.2 History
Clinical information
Areas of application (indications )
Capreomycin is used in combination with other antituberculous drugs in the treatment of pulmonary tuberculosis, when a primary treatment with isoniazid, rifampicin and ethambutol was not effective and also fails in a combination therapy with aminosalicylic acid and streptomycin. The sensitivity of the pathogen Mycobacterium tuberculosis compared to capreomycin should be determined in each patient.
Adverse effects (side effects)
Very common side effects include damage to the kidneys and the inner ear ( ototoxicity ). Accordingly, the kidney function, and the hearing function should be monitored before and during the treatment. Also, liver damage and changes in the blood count occur. Hypersensitivity reactions are rare.
Pharmacological properties
Mechanism of action ( pharmacodynamics )
Capreomycin acts through the inhibition of protein synthesis in the bacterial cells by binding to both the 16S and the 23S rRNA, an unusual, both subunits of the ribosome of respective mechanism of action that was otherwise only described for the structurally related viomycin. Mycobacteria, which are resistant to capreomycin, have an inactive tlyA gene; This gene encodes a methyltransferase that modifies both the 16S and the 23S rRNA of the binding site for capreomycin, whereby the ribosome is sensitive to the inhibition by the antibiotic. Since only a few genera of bacteria have a tlyA gene, the effect of capreomycin is essentially limited to mycobacteria.
Uptake and distribution in the body ( pharmacokinetics )
The absorption of the drug after oral administration is very low, so the gift is always intramuscularly or intravenously. With normal renal function, approximately 50 % of the drug is excreted within 12 hours unchanged in the urine.
Other Information
Chemical and pharmaceutical information
Capreomycin is a cyclic peptide from streptomycetes bacteria of the species Streptomyces capreolus obtained. The substance used in drugs is a complex of four antimicrobial active components: capreomycin IA, IB, IIA and IIB .. The antibiotic is sometimes counted due to the similar effect to the bacterial translation to the aminoglycosides, although there is no structural relationship exists.
History
The antibiotic was developed in the 1960s at Eli Lilly; regulatory approval in the United States took place on 2 June 1971. In Germany no drugs are approved with this drug.