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Spironolakton Садржај Mehanizam dejstva Sinteza Reference Spoljašnje veze Мени за навигацијуМонографијаa68262752-01-7WHO5833APRD01234562827O7W4T232D00443CHEBI:9241CHEMBL1393Goodman & Gilman's The Pharmacological Basis of Therapeutics10.1036/0071422803PDR: Physicians Desk Reference 2010 (Physicians' Desk Reference (Pdr))10.1021/jo01090a019Spironolaktonуу

Антагонисти алдостеронаАнтиандрогениЕсенцијални лекови Светске здравствене организацијеФурониСпиро једињењаПрегнаниАгонисти прегнанског X рецептора


diuretikantiandrogenlaktonantagonist aldosteronakalijumzatajenja srcaascitareninskehipertenzijehipokalemijeKonovog sindromahipertenzijomantiandrogenskoghirsutizmagubitka koseaknićelavostisindroma policističnih jajnikaterapije korekcije polatransženatestosteronaginekomastijuimpotencijaerektilnu disfunkcijugubitak seksualnog nagonatestosteronahipogonadizamhiperkalemijualdosteronske receptoresistemu prikupljajućih kanalaENaCROMKSpironolactone synth.pngMENDanatphysdevphormcellnocodcongtumrsysieponproclekA10H1H2H3H5MVASanathucalvhutlfizrazvnocosyvacongtumrsysieponprocC3C4C5C9










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Spironolakton




Из Википедије, слободне енциклопедије






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Spironolakton (Aldakton, Novo-Spiroton, Aldaktazid, Spiraktin, Spiroton, Verospiron, Berlakton) je diuretik i antiandrogen. On se često pojednostaljeno naziva spiro.[1][2]


Ovaj leki je sintetički 17-lakton. On je renalno kompetitivni antagonist aldosterona iz klase diuretika koji pošteđuju kalijum. On se prvenstveno koristi za lečenje zatajenja srca, ascita kod pacijenata sa oboljenjem jetre, niskoreninske hipertenzije, hipokalemije, sekundarnog hiperaldosteronizma (koji se javlja sa hepatičkom cirozom), i Konovog sindroma (primarnog hiperaldosteronizma). Sam spironolakton je slab diuretik jer deluje na distalni nefron (tubule za prikupljanje), gde se zapremina urina može samo neznatno promeniti. Međutim on se može kombinovati sa drugim diureticima da bi mu se povećala potentnost. Aproksimativno jedna osoba od stotine sa hipertenzijom ima povišene nivoe aldosterona. Kod tih osoba antihipertenzivno dejstvo spironolaktona može da nadmaši od kompleksne kombinacije drugih antihipertenziva.


Usled njegovog antiandrogenskog dejstva, on se takođe koristiti za lečenje hirsutizma. On nalazi primenu u lečenju gubitka kose i akni kod žena, i može se koristiti kao topikalni lek za tretman muške ćelavosti. On se često upotrebljava za tretiranje simptoma sindroma policističnih jajnika kao što su višak dlake na licu i akne. On može da bude deo terapije korekcije pola transžena.


Spironolakton redukuje telesnu produkciju testosterona i blokira testosteronske receptore, te kod muškaraca može da prouzrokuje ginekomastiju, impotencija, erektilnu disfunkciju, gubitak seksualnog nagona i druge poremećaje, kao što su gubitak mišićne mase, umor i fizička slabost, koji su generalno vezani za niske nivoe testosterona i hipogonadizam kod muškaraca. Iz tog razloga, muškarcima se tipično ne propisuje spironolakton za dugotrajnu upotrebu. Kalijumski suplementi se ne propisuju za upotrebu sa spironolaktonom jer bi to uzrokovalo hiperkalemiju, koja je potencijalno smrtonosna. Nivoi kalijuma se moraju oprezno pratiti kod muškaraca i žena tokom upotrebe spironolaktona, posebno tokom prvih dvanaest meseci i nakon povećanja doze.




Садржај





  • 1 Mehanizam dejstva


  • 2 Sinteza


  • 3 Reference


  • 4 Spoljašnje veze




Mehanizam dejstva


Spironolakton inhibira dejstvo aldosterona putem kompeticije za intracelularne aldosteronske receptore u sistemu prikupljajućih kanala. Time se umanjuje reapsorpcija natrijuma i vode, dok se snižava sekrecija kalijuma. Spironolakton ima prilično spor početak dejstva. Potrebno je nekoliko dana da se razvije, isto tako njegovi efekti sporo iščezavaju. Razlog su steroidni putevi nakon transkripcije gena. Potrebno je nekoliko dana da bi došlo do promene genskih proizvoda (u ovom slučaju ENaC i ROMK kanali su umanjeni).



Sinteza


Spironolactone synth.png[3]



Reference




  1. ^ Hardman JG, Limbird LE, Gilman AG (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10. изд.). New York: McGraw-Hill. ISBN 0071354697. doi:10.1036/0071422803. 


  2. ^ Pdr Staff (2009). PDR: Physicians Desk Reference 2010 (Physicians' Desk Reference (Pdr)). Rozelle, N.S.W: Thomson Reuters. ISBN 1-56363-748-0. 


  3. ^ Cella John A., Tweit Robert C. (1959). „Steroidal Aldosterone Blockers. II”. Journal of Organic Chemistry. 24 (8): 1109. doi:10.1021/jo01090a019. 



Spoljašnje veze



  • Spironolakton
Spironolakton
Spironolactone structure.svg

IUPAC ime
7α-Acetiltio-3-okso-17α-pregn-4-en-21,17-karbolakton
ili
(1' S,2R,2' R,9' R,10' R,11' S,15' S)-9'-(acetilsulfanil)-2',15'-dimetilspiro[oksolan-2,14'-tetraciklo[8.7.0.02,7.011,15]heptadekan]-6'-en-5,5'-dion
Klinički podaci
Prodajno imeAldakton
Drugs.comМонографија
MedlinePlusa682627
Kategorija trudnoće


  • AU: B3


  • US: C (Mogući rizik)


Način primeneOralno
Pravni status
Pravni status


  • UK: POM (Samo na recepat)


  • US: ℞-only



Farmakokinetički podaci
MetabolizamHepatički
Poluvreme eliminacije1.3-2 h
Izlučivanje
Urin, žuč

Identifikatori
CAS broj
52-01-7 ДаY
ATC kod
C03DA01 (WHO)
PubChemCID 5833
DrugBank
APRD01234 ДаY
ChemSpider
5628 ДаY
UNII
27O7W4T232 ДаY
KEGG
D00443 ДаY
ChEBI
CHEBI:9241 ДаY
ChEMBL
CHEMBL1393 ДаY
SinonimiAldakton
Spiroton
Spirolakton
Hemijski podaci
Formula
C24H32O4S
Molarna masa416.574 g/mol















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u vezi sa temama iz oblasti medicine (zdravlja).








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Mentenanță CS1: Dată și anMentenanță CS1: Utilizare explicită a lui et al.IsraelȚări în Orientul MijlociuRepubliciSionismState membre ale Organizației Națiunilor Unite ebraicăarabărepublică parlamentarăOrientul MijlociuMării MediteraneLibanulSiriaIordaniaCisiordaniaEgiptFâșia GazaIerusalimTel AvivOrganizației Națiunilor Unite14 mai1948Mandatului britanic pentru PalestinaDavid Ben-GurionOrganizației SionisteAgenției Evreiești pentru PalestinaStatului IsraelONULiga ArabăpalestinieneRăzboiul arabo-israelian din 1948Conflict arabo-israelianTransiordaniaEgiptulRăzboiului de Șase ZileCisiordaniaPeninsula SinaiFâșia GazaÎnălțimile GolanBiroului Central de Statisticădruzicerchezisamariteniarmenidemocrație reprezentativăsistem parlamentarvot universalKnessetulgaze naturaleIndicelui Dezvoltării UmaneOCDEȚara I...
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Кастелфранко ди Сопра Становништво Референце Спољашње везе Мени за навигацију43°37′18″ СГШ; 11°33′32″ ИГД / 43.62156° СГШ; 11.55885° ИГД / 43.62156; 11.5588543°37′18″ СГШ; 11°33′32″ ИГД / 43.62156° СГШ; 11.55885° ИГД / 43.62156; 11.558853179688„The GeoNames geographical database”„Istituto Nazionale di Statistica”проширитиууWorldCat156923403n850174324558639-1cb14643287r(подаци)

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