Peringatan Keamanan

Miconazole overdose has not been reported.L14021 Patients experiencing an overdose are at an increased risk of severe adverse effects such as headache, skin irritation, diarrhea, nausea, vomiting, abdominal pain, and dysgeusia. Symptomatic and supportive measures are recommended.

Miconazole has an oral LD50 of 500 mg/kg in rats.MSDS

Miconazole

DB01110

small molecule approved investigational vet_approved

Deskripsi

Miconazole is a broad-spectrum azole antifungal with some activity against Gram-positive bacteria as well.A203636 It is widely used to treat mucosal yeast infections, including both oral and vaginal infections; although intravenous miconazole is no longer available, a wide variety of suppositories, creams, gels, and tablet-based products are available.L14021, L14024, L14027, L14033, L14396 Miconazole is thought to act primarily through the inhibition of fungal CYP450 14?-lanosterol demethylase activity.A203636, A203639

Miconazole was first synthesized in 1969 and first granted FDA approval on January 8, 1974, for sale by INSIGHT Pharmaceuticals as a topical cream.A214523, L14021 It is currently available as a variety of prescription and over the counter products. Despite having been in clinical use for an extended period, resistance to miconazole among susceptible organisms is relatively low.A203636

Struktur Molekul 2D

Berat 416.129
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Miconazole has a terminal half-life of 24 hours.[L14021]
Volume Distribusi A 1200 mg miconazole vaginal suppository resulted in a calculated apparent volume of distribution of 95 546 L while a 100 mg vaginal cream yielded an apparent volume of distribution of 10 911L.[A203657]
Klirens (Clearance) -

Absorpsi

Miconazole given to healthy volunteers as a single 50 mg oral tablet produced a mean Cmax of 15.1 ± 16.2 mcg/mL, a mean AUC0-24 of 55.2 ± 35.1 mcg\*h/mL, and a median Tmax of 7 hours (range 2.0-24.1). In these patients measurable plasma concentrations ranged from 0.5 to 0.83 mcg/mL.L14021 Topical miconazole is absorbed poorly into the systemic circulation.A203636 In pediatric patients aged 1-21 months given multiple topical applications of miconazole ointment for seven days, the plasma miconazole concentration was less than 0.5 ng/mL in 88% of the patients, with the remaining patients having a concentration of 0.57 and 0.58 ng/mL, respectively.L14024 Similarly, patients. administered with a vaginal 1200 mg ovule had a mean Cmax of 10.71 ng/mL, mean Tmax of 18.4 hours, and mean AUC0-96 of 477.3 ng\*h/mL.A203657

Metabolisme

Miconazole is metabolized in the liver and does not give rise to any active metabolites.L14021

Rute Eliminasi

Miconazole is excreted through both urine and feces; less than 1% of unchanged miconazole is recovered in urine.L14021

Interaksi Obat

1026 Data
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Miconazole.
Amphotericin B The therapeutic efficacy of Amphotericin B can be decreased when used in combination with Miconazole.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Miconazole.
Clopidogrel The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Miconazole resulting in a loss in efficacy.
Didanosine Didanosine can cause a decrease in the absorption of Miconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Miconazole.
Everolimus The metabolism of Everolimus can be decreased when combined with Miconazole.
Flibanserin The metabolism of Flibanserin can be decreased when combined with Miconazole.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Miconazole.
Ivabradine The metabolism of Ivabradine can be decreased when combined with Miconazole.
Ivacaftor The metabolism of Ivacaftor can be decreased when combined with Miconazole.
Lurasidone The metabolism of Lurasidone can be decreased when combined with Miconazole.
Naloxegol The metabolism of Naloxegol can be decreased when combined with Miconazole.
Olaparib The metabolism of Olaparib can be decreased when combined with Miconazole.
Ranolazine The metabolism of Ranolazine can be decreased when combined with Miconazole.
Sonidegib The metabolism of Sonidegib can be decreased when combined with Miconazole.
Avanafil The metabolism of Avanafil can be decreased when combined with Miconazole.
Eplerenone The metabolism of Eplerenone can be decreased when combined with Miconazole.
Sildenafil The serum concentration of Sildenafil can be increased when it is combined with Miconazole.
Colchicine The metabolism of Colchicine can be decreased when combined with Miconazole.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Miconazole.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Miconazole.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Miconazole.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Miconazole.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Miconazole.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Miconazole.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Miconazole.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Miconazole.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Miconazole.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Miconazole.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Miconazole.
Sucralfate Sucralfate can cause a decrease in the absorption of Miconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Miconazole.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Miconazole.
Phenytoin The serum concentration of Phenytoin can be increased when it is combined with Miconazole.
Fosphenytoin The serum concentration of Fosphenytoin can be increased when it is combined with Miconazole.
Warfarin The metabolism of Warfarin can be decreased when combined with Miconazole.
Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Miconazole.
(R)-warfarin The metabolism of (R)-warfarin can be decreased when combined with Miconazole.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be decreased when combined with Miconazole.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be decreased when combined with Miconazole.
(S)-Warfarin The metabolism of (S)-Warfarin can be decreased when combined with Miconazole.
Glimepiride The serum concentration of Glimepiride can be increased when it is combined with Miconazole.
Acetohexamide The serum concentration of Acetohexamide can be increased when it is combined with Miconazole.
Chlorpropamide The serum concentration of Chlorpropamide can be increased when it is combined with Miconazole.
Tolazamide The serum concentration of Tolazamide can be increased when it is combined with Miconazole.
Glyburide The serum concentration of Glyburide can be increased when it is combined with Miconazole.
Glipizide The serum concentration of Glipizide can be increased when it is combined with Miconazole.
Gliclazide The serum concentration of Gliclazide can be increased when it is combined with Miconazole.
Tolbutamide The serum concentration of Tolbutamide can be increased when it is combined with Miconazole.
Gliquidone The serum concentration of Gliquidone can be increased when it is combined with Miconazole.
Glisoxepide The serum concentration of Glisoxepide can be increased when it is combined with Miconazole.
Glibornuride The serum concentration of Glibornuride can be increased when it is combined with Miconazole.
Carbutamide The serum concentration of Carbutamide can be increased when it is combined with Miconazole.
Metahexamide The serum concentration of Metahexamide can be increased when it is combined with Miconazole.
Pantoprazole The metabolism of Pantoprazole can be decreased when combined with Miconazole.
Pentobarbital The metabolism of Pentobarbital can be decreased when combined with Miconazole.
Clobazam The serum concentration of Clobazam can be increased when it is combined with Miconazole.
Carisoprodol The metabolism of Carisoprodol can be decreased when combined with Miconazole.
Quinine The metabolism of Quinine can be decreased when combined with Miconazole.
Albendazole The metabolism of Albendazole can be decreased when combined with Miconazole.
Voriconazole The metabolism of Voriconazole can be decreased when combined with Miconazole.
Doxazosin The metabolism of Doxazosin can be decreased when combined with Miconazole.
Thiopental The metabolism of Thiopental can be decreased when combined with Miconazole.
Thioridazine The metabolism of Thioridazine can be decreased when combined with Miconazole.
Esomeprazole The metabolism of Esomeprazole can be decreased when combined with Miconazole.
Primidone The metabolism of Primidone can be decreased when combined with Miconazole.
Methylphenobarbital The metabolism of Methylphenobarbital can be decreased when combined with Miconazole.
Zonisamide The metabolism of Zonisamide can be decreased when combined with Miconazole.
Ramelteon The metabolism of Ramelteon can be decreased when combined with Miconazole.
Praziquantel The metabolism of Praziquantel can be decreased when combined with Miconazole.
Rabeprazole The metabolism of Rabeprazole can be decreased when combined with Miconazole.
Escitalopram The metabolism of Escitalopram can be decreased when combined with Miconazole.
Lapatinib The metabolism of Lapatinib can be decreased when combined with Miconazole.
St. John's Wort The metabolism of St. John's Wort can be decreased when combined with Miconazole.
Barbital The metabolism of Barbital can be decreased when combined with Miconazole.
Methsuximide The metabolism of Methsuximide can be decreased when combined with Miconazole.
Dexlansoprazole The metabolism of Dexlansoprazole can be decreased when combined with Miconazole.
Lacosamide The metabolism of Lacosamide can be decreased when combined with Miconazole.
Etizolam The metabolism of Etizolam can be decreased when combined with Miconazole.
Triclabendazole The metabolism of Triclabendazole can be decreased when combined with Miconazole.
Dexrabeprazole The metabolism of Dexrabeprazole can be decreased when combined with Miconazole.
Paroxetine The metabolism of Paroxetine can be decreased when combined with Miconazole.
Pentamidine The metabolism of Pentamidine can be decreased when combined with Miconazole.
Fedratinib The metabolism of Fedratinib can be decreased when combined with Miconazole.
Labetalol The metabolism of Labetalol can be decreased when combined with Miconazole.
Nebivolol The metabolism of Nebivolol can be decreased when combined with Miconazole.
Vilazodone The metabolism of Vilazodone can be decreased when combined with Miconazole.
Esketamine The metabolism of Esketamine can be decreased when combined with Miconazole.
Cenobamate The metabolism of Cenobamate can be decreased when combined with Miconazole.
Valproic acid The metabolism of Valproic acid can be decreased when combined with Miconazole.
Ticlopidine The metabolism of Ticlopidine can be decreased when combined with Miconazole.
Nilutamide The metabolism of Nilutamide can be decreased when combined with Miconazole.
Stiripentol The metabolism of Miconazole can be decreased when combined with Stiripentol.
Moclobemide The metabolism of Moclobemide can be decreased when combined with Miconazole.
Methylene blue The metabolism of Methylene blue can be decreased when combined with Miconazole.
Benzocaine The metabolism of Benzocaine can be decreased when combined with Miconazole.
Rilpivirine The metabolism of Rilpivirine can be decreased when combined with Miconazole.
Dronabinol The serum concentration of Dronabinol can be increased when it is combined with Miconazole.
Ethinylestradiol The metabolism of Ethinylestradiol can be decreased when combined with Miconazole.

Target Protein

Lanosterol 14-alpha demethylase ERG11
Nitric oxide synthase 3 NOS3
Nitric oxide synthase, inducible NOS2
Nuclear receptor subfamily 1 group I member 2 NR1I2
Calcium-activated potassium channel KCNMA1
Voltage-gated Potassium Channels KCND1
Inward rectifier potassium channel KCNJ12
Voltage gated L-type calcium channel CACNA1C

Referensi & Sumber

Synthesis reference: Godefroi EF, Heeres J, Van Cutsem J, Janssen PA: The preparation and antimycotic properties of derivatives of 1-phenethylimidazole. J Med Chem. 1969 Sep;12(5):784-91. doi: 10.1021/jm00305a014.
Artikel (PubMed)
  • PMID: 31287594
    Taudorf EH, Jemec GBE, Hay RJ, Saunte DML: Cutaneous candidiasis - an evidence-based review of topical and systemic treatments to inform clinical practice. J Eur Acad Dermatol Venereol. 2019 Oct;33(10):1863-1873. doi: 10.1111/jdv.15782. Epub 2019 Jul 30.
  • PMID: 6364994
    Tanenbaum L, Anderson C, Rosenberg MJ, Akers W: 1% sulconazole cream v 2% miconazole cream in the treatment of tinea versicolor. A double-blind, multicenter study. Arch Dermatol. 1984 Feb;120(2):216-9.
  • PMID: 22568580
    Pierard GE, Hermanns-Le T, Delvenne P, Pierard-Franchimont C: Miconazole, a pharmacological barrier to skin fungal infections. Expert Opin Pharmacother. 2012 Jun;13(8):1187-94. doi: 10.1517/14656566.2012.687047. Epub 2012 May 8.
  • PMID: 185515
    De Nollin S, Borgers M: An ultrastructural and cytochemical study of Candida albicans after in vitro treatment with imidazoles. Mykosen. 1976 Sep;19(9):317-28. doi: 10.1111/j.1439-0507.1976.tb01469.x.
  • PMID: 12234832
    Kobayashi D, Kondo K, Uehara N, Otokozawa S, Tsuji N, Yagihashi A, Watanabe N: Endogenous reactive oxygen species is an important mediator of miconazole antifungal effect. Antimicrob Agents Chemother. 2002 Oct;46(10):3113-7. doi: 10.1128/aac.46.10.3113-3117.2002.
  • PMID: 15155241
    Hornby JM, Nickerson KW: Enhanced production of farnesol by Candida albicans treated with four azoles. Antimicrob Agents Chemother. 2004 Jun;48(6):2305-7. doi: 10.1128/AAC.48.6.2305-2307.2004.
  • PMID: 21768514
    Sharma M, Prasad R: The quorum-sensing molecule farnesol is a modulator of drug efflux mediated by ABC multidrug transporters and synergizes with drugs in Candida albicans. Antimicrob Agents Chemother. 2011 Oct;55(10):4834-43. doi: 10.1128/AAC.00344-11. Epub 2011 Jul 18.
  • PMID: 17553796
    Thevissen K, Ayscough KR, Aerts AM, Du W, De Brucker K, Meert EM, Ausma J, Borgers M, Cammue BP, Francois IE: Miconazole induces changes in actin cytoskeleton prior to reactive oxygen species induction in yeast. J Biol Chem. 2007 Jul 27;282(30):21592-7. doi: 10.1074/jbc.M608505200. Epub 2007 Jun 6.
Menampilkan 8 dari 12 artikel.

Contoh Produk & Brand

Produk: 723 • International brands: 10
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Menampilkan 8 dari 723 produk.
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  • Zimycan

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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