Difference between revisions of "Thioguanine (Tabloid)"
Warner-admin (talk | contribs) m (Text replacement - "Category:Acute lymphocytic leukemia medications" to "Category:B-cell acute lymphoblastic leukemia medications") |
m |
||
| Line 1: | Line 1: | ||
| − | |||
| − | |||
==General information== | ==General information== | ||
Class/mechanism: Purine (guanine) analog, antimetabolite that interferes with DNA synthesis. Thioguanine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is converted to 6-thioguanylic acid (TGMP). TGMP interferes with several processes involving the synthesis of guanine nucleotides. It exerts pseudo-feedback inhibition of glutamine-5-phosphoribosylpyrophosphate amidotransferase, an early enzyme in the de novo pathway for purine ribonucleotide synthesis. TGMP is a competitive inhibitor of inosinic acid (IMP) dehydrogenase, interfering with the conversion of IMP to xanthylic acid (XMP). Thioguanylic acid is converted to thioguanosine diphosphate (TGDP) and thioguanosine triphosphate (TGTP), and they are eventually incorporated into RNA and DNA, which may cause additional cytotoxicity. Thioguanine is structurally and functionally similar to [[Mercaptopurine (Purinethol)]].<ref name="insert">[http://us.gsk.com/products/assets/us_tabloid.pdf Thioguanine (Tabloid) package insert]</ref><ref>[http://hemonc.org/docs/packageinsert/thioguanine.pdf Thioguanine (Tabloid) package insert (locally hosted backup)]</ref> | Class/mechanism: Purine (guanine) analog, antimetabolite that interferes with DNA synthesis. Thioguanine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is converted to 6-thioguanylic acid (TGMP). TGMP interferes with several processes involving the synthesis of guanine nucleotides. It exerts pseudo-feedback inhibition of glutamine-5-phosphoribosylpyrophosphate amidotransferase, an early enzyme in the de novo pathway for purine ribonucleotide synthesis. TGMP is a competitive inhibitor of inosinic acid (IMP) dehydrogenase, interfering with the conversion of IMP to xanthylic acid (XMP). Thioguanylic acid is converted to thioguanosine diphosphate (TGDP) and thioguanosine triphosphate (TGTP), and they are eventually incorporated into RNA and DNA, which may cause additional cytotoxicity. Thioguanine is structurally and functionally similar to [[Mercaptopurine (Purinethol)]].<ref name="insert">[http://us.gsk.com/products/assets/us_tabloid.pdf Thioguanine (Tabloid) package insert]</ref><ref>[http://hemonc.org/docs/packageinsert/thioguanine.pdf Thioguanine (Tabloid) package insert (locally hosted backup)]</ref> | ||
| Line 9: | Line 7: | ||
==Diseases for which it is used== | ==Diseases for which it is used== | ||
| − | *[[Acute | + | *[[Acute myeloid leukemia]] |
*[[Acute promyelocytic leukemia]] | *[[Acute promyelocytic leukemia]] | ||
| + | *[[B-cell acute lymphoblastic leukemia]] | ||
==Patient drug information== | ==Patient drug information== | ||
| Line 18: | Line 17: | ||
==History of changes in FDA indication== | ==History of changes in FDA indication== | ||
* 1/18/1966: Initial FDA approval | * 1/18/1966: Initial FDA approval | ||
| + | |||
| + | ==Also known as== | ||
| + | *'''Generic names:''' 6-TG, 6-thioguanine, 2-Amino-6-Mercaptopurine | ||
| + | *'''Brand name:''' Tabloid | ||
==References== | ==References== | ||
| Line 23: | Line 26: | ||
[[Category:Drug index]] | [[Category:Drug index]] | ||
| − | |||
[[Category:Oral medications]] | [[Category:Oral medications]] | ||
| Line 29: | Line 31: | ||
[[Category:Purine analogues]] | [[Category:Purine analogues]] | ||
| + | [[Category:Acute myeloid leukemia medications]] | ||
| + | [[Category:Acute promyelocytic leukemia medications]] | ||
[[Category:B-cell acute lymphoblastic leukemia medications]] | [[Category:B-cell acute lymphoblastic leukemia medications]] | ||
| − | |||
[[Category:Drugs FDA approved in 1966]] | [[Category:Drugs FDA approved in 1966]] | ||
[[Category:WHO Essential Cancer Medicine]] | [[Category:WHO Essential Cancer Medicine]] | ||
Revision as of 20:38, 3 March 2018
General information
Class/mechanism: Purine (guanine) analog, antimetabolite that interferes with DNA synthesis. Thioguanine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is converted to 6-thioguanylic acid (TGMP). TGMP interferes with several processes involving the synthesis of guanine nucleotides. It exerts pseudo-feedback inhibition of glutamine-5-phosphoribosylpyrophosphate amidotransferase, an early enzyme in the de novo pathway for purine ribonucleotide synthesis. TGMP is a competitive inhibitor of inosinic acid (IMP) dehydrogenase, interfering with the conversion of IMP to xanthylic acid (XMP). Thioguanylic acid is converted to thioguanosine diphosphate (TGDP) and thioguanosine triphosphate (TGTP), and they are eventually incorporated into RNA and DNA, which may cause additional cytotoxicity. Thioguanine is structurally and functionally similar to Mercaptopurine (Purinethol).[1][2]
Route: PO
Extravasation: n/a
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]
Diseases for which it is used
Patient drug information
- Thioguanine (Tabloid) patient drug information (Chemocare)[3]
- Thioguanine (Tabloid) patient drug information (UpToDate)[4]
History of changes in FDA indication
- 1/18/1966: Initial FDA approval
Also known as
- Generic names: 6-TG, 6-thioguanine, 2-Amino-6-Mercaptopurine
- Brand name: Tabloid