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Home / Drugs / Starting with D / Dactinomycin
 
Dactinomycin
 

A compound composed of a two cyclic peptides attached to a phenoxazine that is derived from streptomyces parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015)
BrandsChounghwamycin B
Cosmegen
Lyovac Cosmegen
Meractinomycin
CategoriesAntineoplastic Agents
Anti-Bacterial Agents
Nucleic Acid Synthesis Inhibitors
Antibiotics
Antibiotics, Antineoplastic
Protein Synthesis Inhibitors
ManufacturersLundbeck inc
Bedford laboratories div ben venue laboratories inc
PackagersLundbeck Inc.
Merck & Co.
SynonymsActD
Actinomycin C1
Actinomycin D
Dactinomicina [INN-Spanish]
Dactinomycine [INN-French]
Dactinomycinum [INN-Latin]

indication

For the treatment of Wilms' tumor, childhood rhabdomyosarcoma, Ewing's sarcoma and metastatic, nonseminomatous testicular cancer as part of a combination chemotherapy and/or multi-modality treatment regimen

pharmacology

Generally, the actinomycins exert an inhibitory effect on gram-positive and gram-negative bacteria and on some fungi. However, the toxic properties of the actinomycins (including dactinomycin) in relation to antibacterial activity are such as to preclude their use as antibiotics in the treatment of infectious diseases. Because the actinomycins are cytotoxic, they have an antineoplastic effect which has been demonstrated in experimental animals with various types of tumor implant. This cytotoxic action is the basis for their use in the treatment of certain types of cancer. Dactinomycin is believed to produce its cytotoxic effects by binding DNA and inhibiting RNA synthesis.

mechanism of action

Good evidence exists that this drug bind strongly, but reversibly, to DNA, interfering with synthesis of RNA (prevention of RNA polymerase elongation) and, consequently, with protein synthesis.

toxicity

hepatoxicity

biotransformation

hepatic

absorption

poorly absorbed from gastrointestinal tract

half life

36 hours