Itrakonazola

Itrakonazola
Data klinikal
Nama dagang	Sporanox, Sporaz, Orungal, lain-lain
Nama lain	ITZ
AHFS/Drugs.com	Monograph
MedlinePlus	a692049
Data lesen	AS DailyMed: Itraconazole;
Kategori; kehamilan	AU: B3; ;
Kaedah; pemberian	Mulut (kapsul, larutan), setempat (faraj), intravena (IV)
Kod ATC	J02AC02 (WHO) ;
Status perundangan
Status perundangan	AU: S4 (Preskripsi sahaja) ; KA: Rx sahaja ; UK: POM (Preskripsi sahaja) ; AS: Rx sahaja ;
Data farmakokinetik
Bioketersediaan	~55%, maksimum jika dengan makan
Pengikatan protein	99.8%
Metabolisme	Meluas di hati (CYP3A4)
Metabolit	Hidroksiitrakonazola, ketoitrakonazola,; N-desalkilitrakonazola
Penyingkiran separuh hayat	21 jam
Perkumuhan	Air kencing (35%), tahi (54%)
Pengecam
	Nama IUPAC (±)-1-[(RS)-sec-butyl]-4-[p-[4-[p-[[(2R,4S)-rel-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-Δ2-1,2,4-triazolin-5-one;
Nombor CAS	84625-61-6 ;
PubChem CID	55283;
DrugBank	DB01167 ;
ChemSpider	49927 ;
UNII	304NUG5GF4;
KEGG	D00350 ;
ChEBI	CHEBI:6076 ;
ChEMBL	ChEMBL22587 ;
CompTox Dashboard (EPA)	DTXSID3023180 ;
ECHA InfoCard	100.123.596
Data kimia dan fizikal
Formula	C35H38Cl2N8O4
Jisim molar	705.64
Model 3D (JSmol)	Gambar interaktif;
Kekiralan	Campuran rasem
Takat lebur	165 °C (329 °F)
Keterlarutan dalam air	7.8 ± 0.4 × 10−6 mol/L (pH 1.6) mg/mL (20 °C)
	SMILES O=C1N(/N=C\N1c2ccc(cc2)N7CCN(c6ccc(OC[C@@H]3O[C@](OC3)(c4ccc(Cl)cc4Cl)Cn5ncnc5)cc6)CC7)C(C)CC;
	InChI InChI=1S/C35H38Cl2N8O4/c1-3-25(2)45-34(46)44(24-40-45)29-7-5-27(6-8-29)41-14-16-42(17-15-41)28-9-11-30(12-10-28)47-19-31-20-48-35(49-31,21-43-23-38-22-39-43)32-13-4-26(36)18-33(32)37/h4-13,18,22-25,31H,3,14-17,19-21H2,1-2H3/t25?,31-,35-/m0/s1 ; Key:VHVPQPYKVGDNFY-ZPGVKDDISA-N ;
	(verify)

Itrakonazol (R51211), dicipta pada 1984, ialah agen antikulat triazola dipreskripsi kepada pesakit dengan jangkitan kulat. Ubat ini boleh diberikan melalui mulut atau melalui intravena.

Lihat juga[sunting | sunting sumber]

Rujukan[sunting | sunting sumber]

^ ^a ^b "Itraconazole Use During Pregnancy". Drugs.com. 20 March 2019. Dicapai pada 15 May 2020.
^ "Sporanox 10 mg/mL Oral Solution - Summary of Product Characteristics (SmPC)". (emc). 1 February 2018. Dicapai pada 15 May 2020.
^ Isoherranen N, Kunze KL, Allen KE, Nelson WL, Thummel KE (October 2004). "Role of itraconazole metabolites in CYP3A4 inhibition". Drug Metabolism and Disposition. 32 (10): 1121–1131. doi:10.1124/dmd.104.000315. PMID 15242978. S2CID 6941636.
^ "Sporanox (itraconazole) Capsules. Full Prescribing Information" (PDF). Janssen Pharmaceuticals, Inc. Diarkibkan daripada yang asal (PDF) pada 17 May 2018. Dicapai pada 28 August 2016.
^ ^a ^b Vasilev NA, Surov AO, Voronin AP, Drozd KV, Perlovich GL (April 2021). "Novel cocrystals of itraconazole: Insights from phase diagrams, formation thermodynamics and solubility". International Journal of Pharmaceutics. 599: 120441. doi:10.1016/j.ijpharm.2021.120441. PMID 33675927. S2CID 232135660.

Pautan luar[sunting | sunting sumber]

Maklumat farmokologi umum tentang itrakonazol, Institut Kesihatan Negara
Laluan Mulut Itrakonazol, Mayo Clinic

[Drugs.com_pregnancy-1] "Itraconazole Use During Pregnancy". Drugs.com. 20 March 2019. Dicapai pada 15 May 2020.

[2] "Sporanox 10 mg/mL Oral Solution - Summary of Product Characteristics (SmPC)". (emc). 1 February 2018. Dicapai pada 15 May 2020.

[3] Isoherranen N, Kunze KL, Allen KE, Nelson WL, Thummel KE (October 2004). "Role of itraconazole metabolites in CYP3A4 inhibition". Drug Metabolism and Disposition. 32 (10): 1121–1131. doi:10.1124/dmd.104.000315. PMID 15242978. S2CID 6941636.

[Sporanox_PI-4] "Sporanox (itraconazole) Capsules. Full Prescribing Information" (PDF). Janssen Pharmaceuticals, Inc. Diarkibkan daripada yang asal (PDF) pada 17 May 2018. Dicapai pada 28 August 2016.

[NikitaVas-5] Vasilev NA, Surov AO, Voronin AP, Drozd KV, Perlovich GL (April 2021). "Novel cocrystals of itraconazole: Insights from phase diagrams, formation thermodynamics and solubility". International Journal of Pharmaceutics. 599: 120441. doi:10.1016/j.ijpharm.2021.120441. PMID 33675927. S2CID 232135660.

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l b s Piperazina
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Benzilpiperazina	2C-B-BZP 3-Metilbenzilpiperazina Befuralina Bifeprunoks Buklizina BZP DBZP Fipeksida Klorbenzoksamina Imatinib MBZP MDBZP Meklozina Metoksipiperamida NSI-189 Piberalina Piribedil RN-1747 Sunifiram Trimetazidina Vesnarinon
Difenilalkilpiperazina (benzhidrilalkilpiperazina)	AD-1211 Almitrina Amperozida BRL-15,572 Buklizina BW373U86 DBL-583 Difenpipenol Difenilmetilpiperazina Dotarizina DPI-221 DPI-287 DPI-3290 GBR-12,783 GBR-12,935 GBR-13,069 GBR-13,098 GBR-13,119 Hidroksizina Klorbenzoksamina Klorsiklizina Klosinizina Lidoflazina Manidipina Meklozina MT-45 Oksatomida Setirizina Sinarizina Siklizina SNC-80 Vanokserina
Pirimidinilpiperazina	Buspiron Dasatinib Eptapiron Gepiron Ipsapiron Piribedil Praziton Pirimidinilpiperazina Revospiron Tandospiron Tirilazad Trimazosin Umespiron Zalospiron
Piridinilpiperazina	Atevirdina Azaperon Delavirdina Mirtazapina ORG-12962 Piridinilpiperazina
Benzo(iso)tiazolil piperazina	Lurasidon Perospiron Revospiron Tiospiron Ziprasidon
Trisiklik (piperazina dipasang dengan rantai sisi)	Amoksapina Doklotepin Dokloksitepin Flupentiksol Flufenazina Klopentiksol Klorotepina Klozapina Isofloksitepin Loksapina Meperatiepin Metitepina Oktometotepin Olanzapina Opipramol Oksiklotepin Oksiprotepin Peraditiepin Peratiepin Perazina Perfenazina Pirenzepina Proklorperazina Sianotepin Tietilperazina Tiotiksena Trifluoperazina Triflutepin Zuklopentiksol
Lain-lain/Tidak dikelaskan	6-Nitrokuipazina AP-238 Azimilida Businazina CPD-1 EGIS-7625 Heksosiklium Indinavir JNJ-7777120 Lodenafil MK-212 Mirodenafil PB-28 Kuipazina Ranolazina SA-4503 Sinepazet Asid sinepazik Sinepazida Sikloheksilpiperazina Sildenafil Tadalafil Vardenafil VUF-6002 WY-46824 Zipeprol