1,2-Dimethyl-3-hydroxypyrid-4-one, an orally active chelator for treatment of iron overload

Subcutaneous desferrioxamine, though effective in preventing or reducing iron overload in transfusion-dependent refractory anaemia, is expensive and inconvenient. One potentially cheaper and orally active alternative is 1,2-dimethyl-3-hydroxypyrid-4-one (L1). This drug has been tested in three multi...

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Veröffentlicht in:	The Lancet (British edition) 1987-06, Vol.1 (8545), p.1294
Hauptverfasser:	Kontoghiorghes, G J, Aldouri, M A, Sheppard, L, Hoffbrand, A V
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Aged Aged, 80 and over Capsules Deferiprone Dose-Response Relationship, Drug Humans Iron - poisoning Iron - urine Iron Chelating Agents - administration & dosage Male Neural Tube Defects - complications Pyridones - administration & dosage
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creator	Kontoghiorghes, G J Aldouri, M A Sheppard, L Hoffbrand, A V
description	Subcutaneous desferrioxamine, though effective in preventing or reducing iron overload in transfusion-dependent refractory anaemia, is expensive and inconvenient. One potentially cheaper and orally active alternative is 1,2-dimethyl-3-hydroxypyrid-4-one (L1). This drug has been tested in three multiply transfused patients with myelodysplasia. Gelatin capsules were taken at doses ranging from 0.5 g to 3.0 g. Urinary iron excretion increased substantially in all three patients and in the one tested was equal to that achieved with comparable doses of subcutaneous desferrioxamine. The amounts of iron excreted were related to the dose of L1 administered and the iron load of the patients. The urinary excretion of zinc, magnesium, and calcium did not increase, and the drug was well tolerated.
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One potentially cheaper and orally active alternative is 1,2-dimethyl-3-hydroxypyrid-4-one (L1). This drug has been tested in three multiply transfused patients with myelodysplasia. Gelatin capsules were taken at doses ranging from 0.5 g to 3.0 g. Urinary iron excretion increased substantially in all three patients and in the one tested was equal to that achieved with comparable doses of subcutaneous desferrioxamine. The amounts of iron excreted were related to the dose of L1 administered and the iron load of the patients. The urinary excretion of zinc, magnesium, and calcium did not increase, and the drug was well tolerated.</description><identifier>ISSN: 0140-6736</identifier><identifier>PMID: 2884415</identifier><language>eng</language><publisher>England</publisher><subject>Administration, Oral ; Aged ; Aged, 80 and over ; Capsules ; Deferiprone ; Dose-Response Relationship, Drug ; Humans ; Iron - poisoning ; Iron - urine ; Iron Chelating Agents - administration & dosage ; Male ; Neural Tube Defects - complications ; Pyridones - administration & dosage</subject><ispartof>The Lancet (British edition), 1987-06, Vol.1 (8545), p.1294</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2884415$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kontoghiorghes, G J</creatorcontrib><creatorcontrib>Aldouri, M A</creatorcontrib><creatorcontrib>Sheppard, L</creatorcontrib><creatorcontrib>Hoffbrand, A V</creatorcontrib><title>1,2-Dimethyl-3-hydroxypyrid-4-one, an orally active chelator for treatment of iron overload</title><title>The Lancet (British edition)</title><addtitle>Lancet</addtitle><description>Subcutaneous desferrioxamine, though effective in preventing or reducing iron overload in transfusion-dependent refractory anaemia, is expensive and inconvenient. One potentially cheaper and orally active alternative is 1,2-dimethyl-3-hydroxypyrid-4-one (L1). This drug has been tested in three multiply transfused patients with myelodysplasia. Gelatin capsules were taken at doses ranging from 0.5 g to 3.0 g. Urinary iron excretion increased substantially in all three patients and in the one tested was equal to that achieved with comparable doses of subcutaneous desferrioxamine. The amounts of iron excreted were related to the dose of L1 administered and the iron load of the patients. The urinary excretion of zinc, magnesium, and calcium did not increase, and the drug was well tolerated.</description><subject>Administration, Oral</subject><subject>Aged</subject><subject>Aged, 80 and over</subject><subject>Capsules</subject><subject>Deferiprone</subject><subject>Dose-Response Relationship, Drug</subject><subject>Humans</subject><subject>Iron - poisoning</subject><subject>Iron - urine</subject><subject>Iron Chelating Agents - administration & dosage</subject><subject>Male</subject><subject>Neural Tube Defects - complications</subject><subject>Pyridones - administration & dosage</subject><issn>0140-6736</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1987</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNotj71qwzAURjW0pGnaRyjoASKQLFlSxpL-BQJd2qlDuLausItsGVkN1dvX0AyHbzl8cK7ImgvFmTZS35Dbef7mnCvN6xVZVdYqJeo1-RLbij31A-auBCZZV1yKv2UqqXdMsTjilsJIY4IQCoU292ekbYcBckzUL-SEkAccM42e9iku8hlTiODuyLWHMOP9ZTfk8-X5Y__Gju-vh_3jkU1C2sykkHIHntfcG7sztcXKALRcWmwaI8AoJzi0jfcIHlvrpdRLCQqptbMW5YY8_P9OP82A7jSlfoBUTpdI-QdFyU1J</recordid><startdate>19870606</startdate><enddate>19870606</enddate><creator>Kontoghiorghes, G J</creator><creator>Aldouri, M A</creator><creator>Sheppard, L</creator><creator>Hoffbrand, A V</creator><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope></search><sort><creationdate>19870606</creationdate><title>1,2-Dimethyl-3-hydroxypyrid-4-one, an orally active chelator for treatment of iron overload</title><author>Kontoghiorghes, G J ; Aldouri, M A ; Sheppard, L ; Hoffbrand, A V</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p138t-31339af050f789758e27aac038ebb71a74d10acbffeafec8f336000e1366d88e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1987</creationdate><topic>Administration, Oral</topic><topic>Aged</topic><topic>Aged, 80 and over</topic><topic>Capsules</topic><topic>Deferiprone</topic><topic>Dose-Response Relationship, Drug</topic><topic>Humans</topic><topic>Iron - poisoning</topic><topic>Iron - urine</topic><topic>Iron Chelating Agents - administration & dosage</topic><topic>Male</topic><topic>Neural Tube Defects - complications</topic><topic>Pyridones - administration & dosage</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kontoghiorghes, G J</creatorcontrib><creatorcontrib>Aldouri, M A</creatorcontrib><creatorcontrib>Sheppard, L</creatorcontrib><creatorcontrib>Hoffbrand, A V</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><jtitle>The Lancet (British edition)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kontoghiorghes, G J</au><au>Aldouri, M A</au><au>Sheppard, L</au><au>Hoffbrand, A V</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>1,2-Dimethyl-3-hydroxypyrid-4-one, an orally active chelator for treatment of iron overload</atitle><jtitle>The Lancet (British edition)</jtitle><addtitle>Lancet</addtitle><date>1987-06-06</date><risdate>1987</risdate><volume>1</volume><issue>8545</issue><spage>1294</spage><pages>1294-</pages><issn>0140-6736</issn><abstract>Subcutaneous desferrioxamine, though effective in preventing or reducing iron overload in transfusion-dependent refractory anaemia, is expensive and inconvenient. One potentially cheaper and orally active alternative is 1,2-dimethyl-3-hydroxypyrid-4-one (L1). This drug has been tested in three multiply transfused patients with myelodysplasia. Gelatin capsules were taken at doses ranging from 0.5 g to 3.0 g. Urinary iron excretion increased substantially in all three patients and in the one tested was equal to that achieved with comparable doses of subcutaneous desferrioxamine. The amounts of iron excreted were related to the dose of L1 administered and the iron load of the patients. The urinary excretion of zinc, magnesium, and calcium did not increase, and the drug was well tolerated.</abstract><cop>England</cop><pmid>2884415</pmid></addata></record>
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subjects	Administration, Oral Aged Aged, 80 and over Capsules Deferiprone Dose-Response Relationship, Drug Humans Iron - poisoning Iron - urine Iron Chelating Agents - administration & dosage Male Neural Tube Defects - complications Pyridones - administration & dosage
title	1,2-Dimethyl-3-hydroxypyrid-4-one, an orally active chelator for treatment of iron overload
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