Demeklociklin

Demeklociklin
(IUPAC) ime
	(2E,4S,4aS,5aS,6S,12aS)-2-[amino(hydroxy)methylidene]-7-chloro-4-(dimethylamino)-6,10,11,12a-tetrahydroxy-1,2,3,4,4a,5,5a,6,12,12a-decahydrotetracene-1,3,12-trione
Klinički podaci
Identifikatori
CAS broj	127-33-3 ; 64-73-3 (HCl)
ATC kod	D06AA01 J01AA01
PubChem	5311063
DrugBank	APRD00272
ChemSpider	10482117
UNII	5R5W9ICI6O
KEGG	D03680
ChEMBL	CHEMBL1591
Hemijski podaci
Formula	C21H21ClN2O8
Mol. masa	464.853 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C21H21ClN2O8/c1-24(2)14-7-5-6-10(16(27)12-9(25)4-3-8(22)11(12)15(6)26)18(29)21(7,32)19(30)13(17(14)28)20(23)31/h3-4,6-7,14-15,25-26,28-29,32H,5H2,1-2H3,(H2,23,31)/t6-,7-,14-,15-,21-/m0/s1 ; Key: FMTDIUIBLCQGJB-SEYHBJAFSA-N
Farmakokinetički podaci
Bioraspoloživost	60–80%
Vezivanje za proteine plazme	41–50%
Metabolizam	Hepatički
Poluvreme eliminacije	10–17 časa
Izlučivanje	Renalno
Farmakoinformacioni podaci
Trudnoća	D(US)
Pravni status	℞ Prescription only
Način primene	Oralno

Demeklociklin (Deklomicin, Deklostatin i Ledermicin) je tetraciklinski antibiotik. On je izolovan iz aktinobakterijske vrste Streptomyces aureofaciens.^[6]

Upotreba

Infekcije

Demeklociklin je odobren za lečenje raznih tipova bakterijskih infekcija.^[7]

On se koristi u lečenju Lajmske bolesti^[8], akni i bronhitisa.^[9] Otpornot na ovaj antibiotik postepeno postaje sve zastupljenija.

Sindrom neodgovarajućeg izlučivanja antidiuretskog hormona

On je u upotrebi (mada nije odobren za tu namenu u mnogim zemljama) u lečenju hiponatremije (niske koncentracije krvnog natrijuma) uzrokovane sindromom neodgovarajućeg izlučivanja antidiuretskog hormona (SIADH) kad sama restrikcija fluida nije efektivna.^[10]

Mehanizam dejstva

Poput drugih tetraciklinskih antibiotika demeklociklin deluje putem vezivanja za 30S- i 50S-RNK, čime se ometa sinteza proteina bakterija. On je bakteriostatik (on ometa bakterijski rast, ali direktno ne ubija bakterije).

Nije potpuno razjašnjeno zašto demeklociklin ometa dejstvo antidiuretskog hormona. Smatra se da blokira vezivanje hormona za njegov receptor.^[11]

Reference

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.
↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit
↑ Keith Parker; Laurence Brunton; Goodman, Louis Sanford; Lazo, John S.; Gilman, Alfred (2006). Goodman & Gilman's The Pharmacological Basis of Therapeutics (11 izd.). New York: McGraw-Hill. ISBN 0-07-142280-3.
↑ „DailyMed: About DailyMed”. Pristupljeno 20. 12. 2008.
↑ Bryan Rosner, Julie Byers and Michael Huckleberry (Apr 2, 2007). The Top 10 Lyme Disease Treatments: Defeat Lyme Disease with the Best of Conventional and Alternative Medicine (1st edition izd.). BioMed Publishing Group. ISBN 0976379716.
↑ „Antibiotics versus placebo and versus other treatments”. ^{[mrtav link]}
↑ Goh KP (May 2004). „Management of hyponatremia”. American Family Physician 69 (10): 2387–94. PMID 15168958. Arhivirano iz originala na datum 2008-10-16. Pristupljeno 2014-04-05.
↑ De Troyer A, Demanet JC (1975). „Correction of antidiuresis by demeclocycline”. N Engl J Med 293 (18): 915–8. DOI:10.1056/NEJM197510302931809. PMID 170519.

Literatura

Spoljašnje veze

	Portal Medicina
	Portal Hemija

Šablon:Diuretici Šablon:Neuropeptidni ligandi

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[4] Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.

[5] Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[6] Keith Parker; Laurence Brunton; Goodman, Louis Sanford; Lazo, John S.; Gilman, Alfred (2006). Goodman & Gilman's The Pharmacological Basis of Therapeutics (11 izd.). New York: McGraw-Hill. ISBN 0-07-142280-3.

[urlDailyMed:_About_DailyMed-7] „DailyMed: About DailyMed”. Pristupljeno 20. 12. 2008.

[8] Bryan Rosner, Julie Byers and Michael Huckleberry (Apr 2, 2007). The Top 10 Lyme Disease Treatments: Defeat Lyme Disease with the Best of Conventional and Alternative Medicine (1st edition izd.). BioMed Publishing Group. ISBN 0976379716.

[9] „Antibiotics versus placebo and versus other treatments”. ^{[mrtav link]}

[Goh-10] Goh KP (May 2004). „Management of hyponatremia”. American Family Physician 69 (10): 2387–94. PMID 15168958. Arhivirano iz originala na datum 2008-10-16. Pristupljeno 2014-04-05.

[11] De Troyer A, Demanet JC (1975). „Correction of antidiuresis by demeclocycline”. N Engl J Med 293 (18): 915–8. DOI:10.1056/NEJM197510302931809. PMID 170519.

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