Peringatan Keamanan

Symptoms of overdose include erythema, stinging, blistering, peeling, edema, pruritus, urticaria, burning, and general irritation of the skin, and cramps. As with all topical agents, skin sensitization may result F3088.

Oral LD50 (rat): 708 mg/kg; Intraperitoneal LD50 (rat): 445 mg/kg; Subcutaneous LDLO (rat): 10 g/kg; Oral LD50 (mouse): 761 mg/kg; Subcutaneous LDLO (mouse): 10 g/kg; Intraperitoneal LD50 (mouse): 108 mg/kg;F3124

Overdose

This drug poses no risk of acute intoxication, as it is unlikely to occur following a single vaginal or dermal application of an overdose (application over a large area under conditions favorable to absorption) or accidental oral ingestion. There is no specific antidote F3100.

Effects on Fertility

No human studies of the effects of clotrimazole on fertility have been conducted; however, animal studies have not shown any effects on the drug on fertility F3088.

Use in Pregnancy

There are limited data regarding the use of clotrimazole in pregnant women. Animal studies do not show direct or indirect harmful effects on reproduction. Although the topical application of clotrimazole may result in very low serum and tissue levels, the use of clotrimazole topical cream by pregnant women is not recommended unless it is advised by the prescribing physician. Clotrimazole topical cream should not be used in the first trimester of pregnancy unless it is considered by the physician to be essential to patient well-being F3088.

Use in Breastfeeding

Available pharmacodynamic/toxicological studies in animals have shown excretion of clotrimazole/metabolites in breastmilk. Clotrimazole should not be administered during breastfeeding. Although the topical application of clotrimazole has resulted in very low serum and tissue levels, the use of clotrimazole topical cream by lactating women is not recommended unless it recommended by the prescribing physician F3088.

Clotrimazole

DB00257

small molecule approved vet_approved

Deskripsi

This drug is a broad spectrum antimycotic or antifungal agent. Clotrimazole's antimycotic properties were discovered in the late 1960s A174094. Clotrimazole falls under the imidazole category of azole antifungals, possessing broad-spectrum antimycotic activity A174094. It is available in various preparations, including creams, pessaries, and troche formulations (slowly dissolving tablets). As well as its antifungal activity, clotrimazole has become a drug of interest in treating several other diseases such as sickle cell disease, malaria and some cancers A174094. The minimal side effect profile of this drug and its uncomplicated metabolic profile have led it to gain widespread acceptance for the treatment of mycotic outbreaks such as vaginal yeast infections as well as athlete's foot A174097.

Struktur Molekul 2D

Berat 344.837
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi The topical form is minimally absorbed in the serum and tissues [F3088]. Clotrimazole is a lipophilic drug [A174118], and has been shown to be secreted in breastmilk in animal studies [F3088]. There are limited data available regarding the volume of distribution following oral troche administration.
Klirens (Clearance) -

Absorpsi

Because clotrimazole is generally not significantly absorbed, drug interactions are not a major issue with its use A174094.

Metabolisme

Hepatic (metabolized to inactive metabolites) L5173.

Rute Eliminasi

Mainly hepatic L5173.

Interaksi Obat

22 Data
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Clotrimazole.
Sirolimus The serum concentration of Sirolimus can be increased when it is combined with Clotrimazole.
Dicoumarol The therapeutic efficacy of Dicoumarol can be increased when used in combination with Clotrimazole.
Phenindione The therapeutic efficacy of Phenindione can be increased when used in combination with Clotrimazole.
Phenprocoumon The therapeutic efficacy of Phenprocoumon can be increased when used in combination with Clotrimazole.
4-hydroxycoumarin The therapeutic efficacy of 4-hydroxycoumarin can be increased when used in combination with Clotrimazole.
Coumarin The therapeutic efficacy of Coumarin can be increased when used in combination with Clotrimazole.
Ethyl biscoumacetate The therapeutic efficacy of Ethyl biscoumacetate can be increased when used in combination with Clotrimazole.
Fluindione The therapeutic efficacy of Fluindione can be increased when used in combination with Clotrimazole.
Clorindione The therapeutic efficacy of Clorindione can be increased when used in combination with Clotrimazole.
Diphenadione The therapeutic efficacy of Diphenadione can be increased when used in combination with Clotrimazole.
Tioclomarol The therapeutic efficacy of Tioclomarol can be increased when used in combination with Clotrimazole.
Warfarin The therapeutic efficacy of Warfarin can be increased when used in combination with Clotrimazole.
Acenocoumarol The therapeutic efficacy of Acenocoumarol can be increased when used in combination with Clotrimazole.
(R)-warfarin The therapeutic efficacy of (R)-warfarin can be increased when used in combination with Clotrimazole.
(S)-Warfarin The therapeutic efficacy of (S)-Warfarin can be increased when used in combination with Clotrimazole.
Lemborexant The serum concentration of Lemborexant can be decreased when it is combined with Clotrimazole.
Clindamycin The metabolism of Clindamycin can be increased when combined with Clotrimazole.
Rimegepant The metabolism of Rimegepant can be increased when combined with Clotrimazole.
Capmatinib The serum concentration of Capmatinib can be decreased when it is combined with Clotrimazole.
Selpercatinib The serum concentration of Selpercatinib can be decreased when it is combined with Clotrimazole.
Rilpivirine The serum concentration of Rilpivirine can be decreased when it is combined with Clotrimazole.

Target Protein

C-X-C chemokine receptor type 2 CXCR2
Lanosterol 14-alpha demethylase ERG11
Intermediate conductance calcium-activated potassium channel protein 4 KCNN4
Ergosterol
Nuclear receptor subfamily 1 group I member 2 NR1I2
Hydroxycarboxylic acid receptor 2 HCAR2

Referensi & Sumber

Synthesis reference: Buechel, K.H., et al; South African Patent 69/0039; January 3, 1969; assigned to Farben- Buechel, K.H., Regel, E. and Plempel, M.; US. Patent 3,660,577; May 2,1972; and U.S. fabriken Bayer AG, Germany. Patent 3,705,172; Dec. 5,1972; both assigned to Farbenfabriken Bayer A.G. (Germany).
Artikel (PubMed)
  • PMID: 4025444
    Ritter W: Pharmacokinetic fundamentals of vaginal treatment with clotrimazole. Am J Obstet Gynecol. 1985 Aug 1;152(7 Pt 2):945-7.
  • PMID: 24863842
    Crowley PD, Gallagher HC: Clotrimazole as a pharmaceutical: past, present and future. J Appl Microbiol. 2014 Sep;117(3):611-7. doi: 10.1111/jam.12554. Epub 2014 Jun 30.
  • PMID: 26819835
    S K, C S, Cs K, S W: Clotrimazole as a Cancer Drug: A Short Review. Med Chem (Los Angeles). 2014;4(11):722-724. doi: 10.4172/2161-0444.1000219.
  • PMID: 21725708
    Hashem FM, Shaker DS, Ghorab MK, Nasr M, Ismail A: Formulation, characterization, and clinical evaluation of microemulsion containing clotrimazole for topical delivery. AAPS PharmSciTech. 2011 Sep;12(3):879-86. doi: 10.1208/s12249-011-9653-7. Epub 2011 Jul 2.

Contoh Produk & Brand

Produk: 492 • International brands: 9
Produk
  • 1MED Clotrimazole 1% Antifungal Cream
    Cream • 1 g/100g • Topical • US • OTC
  • 1MED Clotrimazole 1% Antifungal Cream
    Cream • 1 g/100g • Topical • US • OTC
  • Akin Anti-fungal
    Solution • 10 mg/1mL • Topical • US • OTC
  • Alevazol
    Ointment • 10 mg/1g • Topical • US • OTC
  • Anti Fungal
    Liquid • 1 g/100mL • Topical • US • OTC
  • Anti-Fungal
    Cream • 10 mg/1g • Topical • US • OTC
  • Anti-Fungal Cream
    Cream • 1 g/100g • Topical • US • OTC
  • Antifungal
    Cream • 1 g/100g • Topical • US • OTC
Menampilkan 8 dari 492 produk.
International Brands
  • Canesten — Bayer
  • Canifug — Dr. August Wolff
  • Clotrimaderm — Taro
  • Empecid — Bayer
  • FemCare
  • Fungicip — Cipla
  • Gyne-Lotrimin — Schering-Plough
  • Myclo-Derm
  • Myclo-Gyne

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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