| Revision as of 14:23, 5 December 2011 editBeetstra (talk | contribs)Edit filter managers, Administrators172,074 edits Saving copy of the {{drugbox}} taken from revid 447386487 of page Progabide for the Chem/Drugbox validation project (updated: 'DrugBank'). |
Latest revision as of 01:33, 9 September 2024 edit 98.191.202.231 (talk) Cat. |
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{{Short description|Pharmaceutical drug}} |
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{{ambox | text = This page contains a copy of the infobox ({{tl|drugbox}}) taken from revid of page ] with values updated to verified values.}} |
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{{Drugbox |
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{{Drugbox |
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| Watchedfields = changed |
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| verifiedrevid = 427143655 |
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| verifiedrevid = 464215284 |
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| IUPAC_name = 4-aminobutanamide |
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| IUPAC_name = 4-aminobutanamide |
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| image = Progabide.svg |
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| image = Progabide structure.svg |
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<!--Clinical data--> |
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<!--Clinical data--> |
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| tradename = |
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| tradename = |
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| legal_status = Prescription only |
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| legal_status = Prescription only |
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| routes_of_administration = Oral |
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| routes_of_administration = Oral |
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<!--Pharmacokinetic data--> |
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<!--Pharmacokinetic data--> |
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| bioavailability = 60% |
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| bioavailability = 60% |
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| elimination_half-life = 4 hours |
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| elimination_half-life = 4 hours |
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| excretion = ] |
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| excretion = ] |
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<!--Identifiers--> |
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<!--Identifiers--> |
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| CASNo_Ref = {{cascite|correct|CAS}} |
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| CAS_number_Ref = {{cascite|correct|??}} |
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| CAS_number = 62666-20-0 |
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| CAS_number = 62666-20-0 |
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| ATC_prefix = N03 |
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| ATC_prefix = N03 |
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| ChEMBL_Ref = {{ebicite|correct|EBI}} |
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| ChEMBL_Ref = {{ebicite|correct|EBI}} |
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| ChEMBL = 287631 |
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| ChEMBL = 287631 |
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<!--Chemical data--> |
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<!--Chemical data--> |
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| C=17 | H=16 | Cl=1 | F=1 | N=2 | O=2 |
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| C=17 | H=16 | Cl=1 | F=1 | N=2 | O=2 |
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| molecular_weight = 334.772 g/mol |
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| smiles = Clc1ccc(cc1)/C(=N\CCCC(N)=O)c2cc(F)ccc2O |
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| smiles = Clc1ccc(cc1)/C(=N\CCCC(N)=O)c2cc(F)ccc2O |
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| InChI = 1/C17H16ClFN2O2/c18-12-5-3-11(4-6-12)17(21-9-1-2-16(20)23)14-10-13(19)7-8-15(14)22/h3-8,10,22H,1-2,9H2,(H2,20,23)/b21-17+ |
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| InChIKey = IBALRBWGSVJPAP-HEHNFIMWBY |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChI = 1S/C17H16ClFN2O2/c18-12-5-3-11(4-6-12)17(21-9-1-2-16(20)23)14-10-13(19)7-8-15(14)22/h3-8,10,22H,1-2,9H2,(H2,20,23)/b21-17+ |
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| StdInChI = 1S/C17H16ClFN2O2/c18-12-5-3-11(4-6-12)17(21-9-1-2-16(20)23)14-10-13(19)7-8-15(14)22/h3-8,10,22H,1-2,9H2,(H2,20,23)/b21-17+ |
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| StdInChIKey = IBALRBWGSVJPAP-HEHNFIMWSA-N |
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| StdInChIKey = IBALRBWGSVJPAP-HEHNFIMWSA-N |
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}} |
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}} |
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'''Progabide''' (]; trade name '''Gabrene''', ]) is an ] and ] of ] (GABA) used in the treatment of ]. Via conversion into GABA, progabide behaves as an ] of the ], ], and ]s. |
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==Uses== |
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Progabide is approved in ] for either monotherapy or adjunctive use in the treatment of epilepsy—specifically, generalized tonic-clonic, myoclonic, partial, and ] seizures—in both children and adults. |
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Progabide has been investigated for many diseases besides epilepsy, including ], ], ], ] and ] with various levels of success. |
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In 1987, Bartolini and colleagues reported progabide's actions on dopamine to be contradictory, decreasing dopamine release, dopamine receptor density and postsynaptic receptor responsivity to dopamine while reducing striatal cholinergic activity so as to increase dopaminergic effects.<ref name="Bartholini_et_al_1987">{{cite journal | vauthors = Bartholini G, Scatton B, Zivkovic B, Lloyd KG | title = GABA receptor agonists and extrapyramidal motor function: therapeutic implications for Parkinson's disease | journal = Advances in Neurology | year = 1987 | volume = 45 | pages = 79–83 | pmid = 3030072 }}</ref> Bartholini and colleagues concluded that it was this that caused Parkinson's patients in human clinical trials to either see an improvement in their Parkinson's with a worsening of L-dopa dyskinesia or an improvement in dyskinesia but with sometimes aggravated Parkinson's symptoms.<ref name="Bartholini_et_al_1987"/> The cholinergic effect takes only a single injection to achieve in rats; when given with ], the development of tolerance to haloperidol's ] effects did not develop.<ref name=Bartholini_et_al_1980>{{cite journal | vauthors = Bartholini G, Scatton B, Zivkovic B | title = Effect of the new gamma-aminobutyric acid agonist SL 76 002 on striatal acetylcholine: relation to neuroleptic-induced extrapyramidal alterations | journal = Advances in Biochemical Psychopharmacology | volume = 24 | pages = 207–13 | year = 1980 | pmid = 6105775 }}</ref> It was hoped that this would be effective for ]. However, Soares, Rathbone and Deeks wrote in the 2004 issue of ''The Cochrane Database of Systematic Reviews'' that "Any possible benefits are likely to be outweighed by the adverse effects associated with their use."<ref name=bust_for_TD>{{cite journal | vauthors = Soares K, Rathbone J, Deeks J | title = Gamma-aminobutyric acid agonists for neuroleptic-induced tardive dyskinesia | journal = The Cochrane Database of Systematic Reviews | issue = 4 | pages = CD000203 | date = October 2004 | pmid = 15494993 | doi = 10.1002/14651858.CD000203.pub2 | url = http://www.mrw.interscience.wiley.com/cochrane/clsysrev/articles/CD000203/frame.html | editor1-last = Soares-Weiser | editor1-first = Karla }}</ref> |
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In addition to being tested for antipsychotic-induced tardive dyskinesia, progabide was itself tested as an antipsychotic; as early as 1979, it was obvious that it was ineffective for ].<ref name=Bartholini_1979>{{cite journal | vauthors = Bartholini G | title = | journal = Schweizer Archiv für Neurologie, Neurochirurgie und Psychiatrie = Archives Suisses de Neurologie, Neurochirurgie et de Psychiatrie | volume = 125 | issue = 2 | pages = 265–9 | year = 1979 | pmid = 45343 }} (French)</ref> While progabide may have been devoid of antipsychotic effects, it did have the effect in schizoaffective and hebephrenic patients of improving environmental responsiveness and social interactions.<ref name=Lloyd_et_al_1983>{{cite journal | vauthors = Lloyd KG, Morselli PL, Depoortere H, Fournier V, Zivkovic B, Scatton B, Broekkamp C, Worms P, Bartholini G | display-authors = 6 | title = The potential use of GABA agonists in psychiatric disorders: evidence from studies with progabide in animal models and clinical trials | journal = Pharmacology, Biochemistry, and Behavior | volume = 18 | issue = 6 | pages = 957–66 | date = June 1983 | pmid = 6351106 | doi = 10.1016/S0091-3057(83)80021-5 | s2cid = 21297834 }}</ref> |
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==Synthesis== |
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] |
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== See also == |
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* ] (SL-75102), an ] of progabide |
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* ] |
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== References == |
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{{Reflist|2}} |
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{{Anticonvulsants}} |
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{{GABAergics}} |
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