Source: Health Products Regulatory Authority (IE) Revision Year: 2011 Publisher: Teva Pharma B.V. Computerweg 10 3542 DR Utrecht Netherlands
Pharmacotherapeutic group: Anthracyclines and related substances
ATC code: L01D B01
Doxorubicin belongs to the group of anthracyclines and is a cytostatic antibiotic that has been isolated from cultures of Streptomyces peucetius var. caesius. It is now prepared semi-synthetically from daunorubicin. Doxorubicin is a strong tissue irritant.
The biological activity of doxorubicin is attributed to its DNA-binding property, which results in inhibition of the enzymatic system, vital for the DNA-replication and the DNA-transcription. The blocking of the cellular cycle seems to be maximal during S phase and mitosis, but inhibition has also been observed during other cell cycle phases.
After intravenous administration, doxorubicin elimination is characterized by a tri-phasic elimination from plasma with a terminal half life of approximately 30 hours. The distribution volume is approximately 25 L/kg. The degree of protein binding in plasma is approximately 70%.
Highest drug concentrations are attained in the lung, liver, spleen, kidney, heart, small intestine and bone-marrow. Doxorubicin does not cross the blood-brain barrier.
Doxorubicin is rapidly metabolised, and the main metabolite is the less active 13-dihydroderivative *doxorubicin*ol. Within five days approximately 5% is recovered in the urine, whilst 40-50% is excreted through the bile within 7 days. Reduced liver functions results in a slower elimination of the substance.
Animal studies from literature show that doxorubicin affects the fertility, is embryo- and fetotoxic and teratogenic. Other data shows that doxorubicin is mutagenic.
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