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Klozapin Садржај Hemija Reference Literatura Spoljašnje veze Мени за навигацијуMonografijaa6910015786-21-0WHO281838DB0036310442628J60AR2IKICD00283CHEBI:3766CHEMBL42„Clozapine prescribing information”оригинала„Awakenings Schizophrenia a New Drug Brings Patients Back to Life”„Clozaril (Clozapine) drug description - FDA approved labeling for prescription drugs and medications at RxList”оригинала„What medications are used to treat schizophrenia?”„Frequency of Monitoring based on Stage of Therapy or Results from WBC Count and ANC Monitoring Tests”оригиналаCase report: rapidly fatal bowel ischaemia on clozapine treatmentClozapine‐related seizures„Prescribing Information”10.1002/hlca.19670500618FR 1334944U.S. Patent 3.539.573GB 98085310.1177/0957154X07070335KlozapinVikimedijinoj ostaviKlozarilKlozapinUputstva za upotrebuуууууу

Атипични антипсихотициДопамински антагонистиДопамински агонистиСеротонински антагонистиПиперазиниХлороарениДибензодиазепини5-ХТ6 антагонисти5-ХТ7 антагонисти


antipsihotikšizofrenijemanično-depresivne psihozeatipični antipsihotik19711975agranulocitozubelih krvnih zrnacaFDA1989.agranulocitozemiokarditisaagranulocitozeagranulocitozadijabeteshipersalivacijudibenzodiazepinloksapinomacetonuhloroformuAzaperonBenperidolBromperidolDroperidolFluanizonHaloperidolLenperonMoperonPipamperonSpiperonTimiperonTrifluperidolKlopimozidFluspirilenPenfluridolPimozidAcepromazinAcetofenazinButaperazinKarfenazinHloracizinHlorproetazinHlorpromazinCijamemazinDiksirazinFluacizinFlufenazinLevomepromazin/MetotrimeprazinMezoridazinPerazinPericijazinPerfenazinPiperacetazinPipotiazinProhlorperazinPromazinPrometazinPropiomazinSulforidazinTietilperazinTiopropazatTioproperazinTioridazinTrifluoperazinTriflupromazinHlorprotiksenKlopentiksolFlupentiksolTiotiksenZuklopentiksolButaklamolFluotracenLoksapinTrimipraminCinuperonMelperonSetoperonIloperidonOkaperidonPaliperidonRisperidonLurasidonePerospironRevospironTiospironZiprasidonAmperozidAripiprazolBifeprunoksBrekspiprazolElopiprazolUmespironAmoksapinAsenapinKarpipraminKlocapraminKlorotepinKlotiapinKlozapinFluperlapinGevotrolinMetitepinMosapraminNDMCOlanzapinPihindonKvetijapinTenilapinZotepinWHO-EMPovučeniKlinička ispitivanjaFaza IIINije dospeo do faze IIIMPSOPSImeprdsrdodbpasspecspvoprocN5A5B5C6A6B6DAkrivastinAlinastinAstemizolAzelastinBamirastinBarmastinBepiastinBepotastinBilastinKabastinenKarebastinKetirizinKlemastinKlemizolKlobenztropinDorastinEbastinEmedastinEpinastinFlezelastinKetotifenLatrepirdinLevokabastinLinetastinLoratadinMapinastinMebhidrolinMizolastinMoksastinNoberastinOktastinOlopatadinPerastinPiklopastinRokastinRupatadinSetastinTalastinTemelastinTerfenadinZepastinDesloratadinFeksofenadinCetirizin‎‎LevocetirizinBelarizinEfletirizinElbanizinFlotrenizinMedrilaminNapaktadinPibaksizinTagorizinTrelnarizinTrenizinVapitadinMDIGtgpphysdevpenzynococongtumrsysieponprocdrugA2A2B345671416blte










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Klozapin




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Klozapin
Clozapine.svg
Clozapine-3D-vdW.png

IUPAC ime
8-hloro-11-(4-metilpiperazin-1-il)-
5H-dibenzo[b,e][1,4]diazepin
Klinički podaci
Prodajno imeKlozaril
Drugs.comMonografija
MedlinePlusa691001
Kategorija trudnoće

  • B
Način primeneOralno
Pravni status
Pravni status

  • Lek na recepat, specijalne restrikcije se primenjuju u mnogim zemljama


Farmakokinetički podaci
Bioraspoloživost60 do 70%
Metabolizam
Hepatički, posredstvom nekoliko CYP izozima
Poluvreme eliminacije6 do 26 sata (prosečna vrednost 14.2 sata pri stabilnim uslovima)
Izlučivanje80% u metabolisanom stanju: 30% bilijarno i 50% renalno

Identifikatori
CAS broj
5786-21-0 ДаY
ATC kod
N05AH02 (WHO)
PubChemCID 2818
IUPHAR/BPS38
DrugBank
DB00363 ДаY
ChemSpider
10442628 ДаY
UNII
J60AR2IKIC ДаY
KEGG
D00283 ДаY
ChEBI
CHEBI:3766 ДаY
ChEMBL
CHEMBL42 ДаY
Hemijski podaci
Formula
C18H19ClN4
Molarna masa326,823 g/mol



Fizički podaci
Tačka topljenja
183 °C (361 °F)
Rastvorljivost u vodi0,1889[1] mg/mL (20 °C)

Klozapin (Klozaril, Azaleptin, Leponeks, Fazaklo, Froidir, Denzapin, Zaponeks, Klozapol, Klopin) je antipsihotik koji se koristi za lečenje šizofrenije. Poznato je da se primenjuje i za lečenje manično-depresivne psihoze, mada za tu indikaciju nije odobren.


Klozapin je bio prvi atipični antipsihotik. On je prvo uveden u Evropi 1971, ali je bio dobrovoljno povučen sa tržišta 1975, nakon što je pokazano da uzrokuje agranulocitozu, oboljenje koje je karakterisano opasnim smanjenjem broja belih krvnih zrnaca, što može da ima smrtni ishod. Nakon što je pokazano da je efektivniji od drugih antipihotika u lečenju šizofrenije, FDA je 1989. odobrila upotrebu klozapina za lečenje te bolesti u slučajevima kad postoji rezistencija na druge lekove. FDA zahteva testiranje krvi kod pacijenata na klozapinu.[2][3] Takođe se zahteva da pakovanja klozapina budu obležena upozorenjem za moguću pojavu agranulocitoze, epileptičkih napada, miokarditisa, drugih nepoželjnih kardiovaskularnih i respiratornih efekata, kao i da dovodi do povišenja mortaliteta kod starijih pacijenata sa psihozom vezanom za demenciju.[4]


Klozapin se obično koristi kao lek zadnjeg izbora kod pacijenata koji ne odgovaraju na druge antipsihotičke tretmane zbog mogućeg uzrokovanja agranulocitoze i zbog troškova testiranja krvi, mada je on jedan od veoma efektivnih antipsihotika.[5] Pacijenti se prate na nedeljnoj bazi tokom prvih šest meseci. Ako ne dolazi do pojave umanjenja broja belih krvnih zrnaca, pacijent se može testirati svake dve nedelje tokom narednih šest meseci. Nakon toga, pacijent može da pređe na testiranje svake četvrte nedelje.[6] Klozapin ima brojne ozbiljne nuspojave, među kojima su agranulocitoza, iritacija creva,[7] epileptički napadi,[8] miokarditis, i dijabetes. Osim toga, on često uzrokuje hipersalivaciju i uvećanje telesne težine.




Садржај





  • 1 Hemija


  • 2 Reference


  • 3 Literatura


  • 4 Spoljašnje veze




Hemija


Klozapin je dibenzodiazepin. On je strukturno srodan sa loksapinom. Klozapin je u maloj meri rastvoran u vodi, rastvoran je u acetonu, i veoma rastvoran u hloroformu. Njegova rastvorljivost u vodi je 188,9 mg/L (25 C).[1][9][10] Jedan od mogućih sintetičkih puteva je:[11][12][13]


Clozapine Production.png


Reference




  1. ↑ 1,01,1 Hopfinger A, Esposito EX, Llinas A, Glen RC, Goodman JM (2009). „Findings of the Challenge To Predict Aqueous Solubility”. Journal of Chemical Information and Modeling. 49: 1—5. 


  2. ^ „Clozapine prescribing information” (PDF). Архивирано из оригинала (PDF) на датум 27. 02. 2012. Приступљено 23. 03. 2012. 


  3. ^ CLAUDIA WALLIS & JAMES WILLWERTH (6. 7. 1992). „Awakenings Schizophrenia a New Drug Brings Patients Back to Life”. Time. Приступљено 09. 10. 2008. 


  4. ^ „Clozaril (Clozapine) drug description - FDA approved labeling for prescription drugs and medications at RxList”. Rxlist.com. Архивирано из оригинала на датум 15. 06. 2008. Приступљено 09. 10. 2008. 


  5. ^ National Institute of Mental Health. „What medications are used to treat schizophrenia?”. 


  6. ^ „Frequency of Monitoring based on Stage of Therapy or Results from WBC Count and ANC Monitoring Tests” (PDF). Архивирано из оригинала (PDF) на датум 27. 02. 2012. Приступљено 23. 03. 2012. 


  7. ^ Case report: rapidly fatal bowel ischaemia on clozapine treatment


  8. ^ Clozapine‐related seizures


  9. ^ Novartis Pharmaceuticals (април 2006). „Prescribing Information” (PDF). Novartis Pharmaceuticals. стр. 36. Приступљено 29. 06. 2007. CS1 одржавање: Формат датума (веза)


  10. ^ Hunziker F.; Fischer E.; Schmutz J. (1967). „11-Amino-5H-dibenzo[b, e]-1, 4-diazepine. 10. Mitteilung �ber siebengliedrige Heterocyclen”. Helvetica Chimica Acta. 50: 1588. doi:10.1002/hlca.19670500618.  replacement character у |title= на позицији 58 (помоћ)


  11. ^ S.A.A. Wander, FR 1334944  (1963).


  12. ^ F. Hunziker, J. Schmutz, U.S. Patent 3.539.573 (1970).


  13. ^ S.A.A. Wander, GB 980853  (1961).



Literatura


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  • Benkert, Hippius: Kompendium der Psychiatrischen Pharmakotherapie (German), 4th. ed., Springer Verlag

  • B. Bandelow, S. Bleich, and S. Kropp: Handbuch Psychopharmaka (German), 2nd. ed. Hogrefe

  • Crilly JF (2007). The history of clozapine and its emergence in the US Market: A review and Analysis. History of Psychiatry, 18(1): 39–60. doi:10.1177/0957154X07070335



Spoljašnje veze





  • Klozaril

  • Klozapin

  • Uputstva za upotrebu









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19. јануар Садржај Догађаји Рођења Смрти Празници и дани сећања Види још Референце Мени за навигацијуу

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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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