Pharmacokinetics of vindesine given as an intravenous bolus and 24-hour infusion in humans. 1985

T Ohnuma, and L Norton, and A Andrejczuk, and J F Holland

The pharmacokinetics of vindesine was examined after the determination of serum drug levels by radioimmunoassay in patients who received the drug either as an i.v. bolus or a 24-hr infusion. After i.v. bolus, vindesine was eliminated from the serum by triphasic decay. The central compartment was approximately 6 times the serum volume. The peak serum level achieved by i.v. bolus was approximately 16 times that achieved by the 24-hr infusion. The post-24-hr-infusion serum decay followed biphasic decay. Pharmacokinetic modeling, assuming a prolonged infusion period, resulted in a triphasic decay curve, with an extremely short distribution phase which would not be clinically detectable. This was due to the incorporation of the distribution phase into the infusion period. This explains the experimental data of a biphasic decay curve observed after 24-hr infusion. Pharmacokinetic parameters for the two phases observed after 24-hr infusion were similar to values calculated from i.v. bolus data. The c X t for 24-hr infusion was identical to that after i.v. bolus; theoretically, the c X t appears constant regardless of infusion time. It is concluded that the rate of elimination and/or the c X t, rather than the peak serum level, played a role in the degree of hematological toxicity.

UI MeSH Term Description Entries
D007263 Infusions, Parenteral The administration of liquid medication, nutrient, or other fluid through some other route than the alimentary canal, usually over minutes or hours, either by gravity flow or often by infusion pumping. Intra-Abdominal Infusions,Intraperitoneal Infusions,Parenteral Infusions,Peritoneal Infusions,Infusion, Intra-Abdominal,Infusion, Intraperitoneal,Infusion, Parenteral,Infusion, Peritoneal,Infusions, Intra-Abdominal,Infusions, Intraperitoneal,Infusions, Peritoneal,Intra Abdominal Infusions,Intra-Abdominal Infusion,Intraperitoneal Infusion,Parenteral Infusion,Peritoneal Infusion
D007275 Injections, Intravenous Injections made into a vein for therapeutic or experimental purposes. Intravenous Injections,Injection, Intravenous,Intravenous Injection
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008433 Mathematics The deductive study of shape, quantity, and dependence. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed) Mathematic
D008657 Metabolic Clearance Rate Volume of biological fluid completely cleared of drug metabolites as measured in unit time. Elimination occurs as a result of metabolic processes in the kidney, liver, saliva, sweat, intestine, heart, brain, or other site. Total Body Clearance Rate,Clearance Rate, Metabolic,Clearance Rates, Metabolic,Metabolic Clearance Rates,Rate, Metabolic Clearance,Rates, Metabolic Clearance
D008954 Models, Biological Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment. Biological Model,Biological Models,Model, Biological,Models, Biologic,Biologic Model,Biologic Models,Model, Biologic
D009369 Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms. Benign Neoplasm,Cancer,Malignant Neoplasm,Tumor,Tumors,Benign Neoplasms,Malignancy,Malignant Neoplasms,Neoplasia,Neoplasm,Neoplasms, Benign,Cancers,Malignancies,Neoplasias,Neoplasm, Benign,Neoplasm, Malignant,Neoplasms, Malignant
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000964 Antimetabolites, Antineoplastic Antimetabolites that are useful in cancer chemotherapy. Antineoplastic Antimetabolites
D014747 Vinblastine Antitumor alkaloid isolated from Vinca rosea. (Merck, 11th ed.) Vincaleukoblastine,Cellblastin,Lemblastine,Velban,Velbe,Vinblastin Hexal,Vinblastina Lilly,Vinblastine Sulfate,Vinblastinsulfat-Gry,Sulfate, Vinblastine

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