Source: Health Products Regulatory Authority (IE) Revision Year: 2016 Publisher: NordMedica A/S, Jaegersborg, Alle 164, DK-2820, Gentofte, Denmark
Amsidine is a sterile antitumour chemotherapeutic agent for intravenous infusion. Although not completely clarified, the mode of action of amsacrine is related to its property of binding the DNA through intercalation and external (electrostatic) forces. Amsacrine inhibits the synthesis of DNA while the RNA may not be directly affected. An additional mode of action, involving modification of cell membrane function, has been suggested.
Amsidine is administered by intravenous infusion. Amsidine has a low lipid solubility, and a relatively high molecular weight, so that it is unlikely that it would cross the blood-brain barrier. Amsidine distributes well in the body, except to the brain and CSF, and is therefore inactive against cerebral tumours.
Studies have shown that the plasma concentration time profiles of Amsidine in man are best described using a three compartment open model. The terminal half-life was found to be prolonged in patients with severe hepatic dysfunction. Work in animals has shown that after biotransformation in the liver, the metabolites of Amsidine are finally excreted in the bile by an active transport mechanism. The majority of Amsidine is excreted in its metabolised form. Studies in man have shown that 20% of the administered drug (free and metabolised) was eliminated in the urine within the first 8 hours, and a total of about 42% within 72 hours in one patient with normal renal function.
No additional data of relevance.
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