Source: Health Products Regulatory Authority (IE) Revision Year: 2014 Publisher: Aspen Pharma Trading Limited 3016 Lake Drive Citywest Business Campus Dublin 24 Ireland
Group + ATC code: Antineoplastic and Immunomodulating Agents (Nitrogen mustard analogues) L01AA03.
Mode of Action: Melphalan is a bifunctional alkylating agent. Formation of carbonium intermediates from each of the two his- 2- chloroethyl groups enables alkylation through covalent binding with the 7-nitrogen of guanine on DNA, cross-linking two DNA strands and thereby preventing cell replication.
The absorption of oral melphalan is highly variable with respect to both the time to first appearance of the drug in plasma and peak plasma concentration.
In studies of the absolute bioavailability of melphalan the mean absolute bioavailability ranged from 56 to 85%.
Intravenous administration can be used to avoid variability in absorption associated with myeloablative treatment.
In a study of 18 patients administered melphalan 0.2 to 0.25 mg/kg bodyweight orally, a maximum plasma concentration (range 87 to 350 nanograms/ml) was reached within 0.5 to 2.0 h.
The administration of melphalan tablets immediately after food delayed the time to achieving peak plasma concentrations and reduced the area under the plasma concentration-time curves by between 39 and 45%.
In 18 patients administered melphalan 0.2 to 0.25 mg/kg bodyweight orally, the mean elimination half-life was 1.12 ± 0.15 h.
Special Patient Populations
Melphalan is mutagenic in animals.
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