Biomaterial Database

Pharmacokinetics of the oral iron chelator deferiprone (L1) in patients with iron overload. 1995

F N al-Refaie, and L N Sheppard, and P Nortey, and B Wonke, and A V Hoffbrand

Department of Haematology, Royal Free Hospital School of Medicine, London.

Single oral dose pharmacokinetics of the iron chelator deferiprone (L1) were studied in 24 patients with chronic iron overload and correlated with 24 h urinary iron excretion (UIE) and creatinine clearance. Absorption of L1 was rapid with a t1/2 of 22.2 +/- 17.7 (mean +/- SD) min. The elimination half-life (elt1/2) of the drug was 91.1 +/- 33.1 min and of its metabolite, L1-glucuronide (L1G) 147.7 +/- 52.0 min. Creatinine clearance of the patients correlated significantly with the elimination t1/2 of L1G (r = -0.79, P = 0.002). There was also a significant correlation between 24 h UIE in the 14 patients studied and L1 versus time area under the curve (AUC) (P = 0.007). The total amount of L1 recovered in urine in 24 h comprised 77.9 +/- 13.3% of the L1 dose. L1 efficiency (the 24 h UIE divided by the amount of iron the oral dose of L1 is capable of binding) in the 14 patients was 3.8 +/- 1.9%. These data show for the first time that the urinary elimination of L1G is influenced by the renal function of the patient. Although no significant accumulation of L1 and L1G will occur in most of the patients if L1 is given more than once daily, in some patients with impaired renal function, L1G may accumulate.

UI	MeSH Term	Description	Entries
D007501	Iron	A metallic element with atomic symbol Fe, atomic number 26, and atomic weight 55.85. It is an essential constituent of HEMOGLOBINS; CYTOCHROMES; and IRON-BINDING PROTEINS. It plays a role in cellular redox reactions and in the transport of OXYGEN.	Iron-56,Iron 56
D008297	Male		Males
D008875	Middle Aged	An adult aged 45 - 64 years.	Middle Age
D011728	Pyridones	Pyridine derivatives with one or more keto groups on the ring.	Pyridinones
D005260	Female		Females
D006402	Hematologic Diseases	Disorders of the blood and blood forming tissues.	Blood Diseases,Hematological Diseases,Blood Disease,Disease, Blood,Disease, Hematologic,Disease, Hematological,Diseases, Blood,Diseases, Hematologic,Diseases, Hematological,Hematologic Disease,Hematological Disease
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000077543	Deferiprone	A pyridone derivative and iron chelator that is used in the treatment of IRON OVERLOAD in patients with THALASSEMIA.	1,2-Dimethyl-3-hydroxy-4-pyridinone,1,2-Dimethyl-3-hydroxypyrid-4-one,1,2-Dimethyl-3-hydroxypyridin-4-one,3-Hydroxy-1,2-dimethyl-4-pyridinone,DMOHPO,Ferriprox,HDMPP,1,2 Dimethyl 3 hydroxy 4 pyridinone,1,2 Dimethyl 3 hydroxypyrid 4 one,1,2 Dimethyl 3 hydroxypyridin 4 one,3 Hydroxy 1,2 dimethyl 4 pyridinone
D000284	Administration, Oral	The giving of drugs, chemicals, or other substances by mouth.	Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D000293	Adolescent	A person 13 to 18 years of age.	Adolescence,Youth,Adolescents,Adolescents, Female,Adolescents, Male,Teenagers,Teens,Adolescent, Female,Adolescent, Male,Female Adolescent,Female Adolescents,Male Adolescent,Male Adolescents,Teen,Teenager,Youths