Clotrimazole
Fenamates
Comparison of the toxicity of fluconazole and other azole antifungal drugs to murine and human granulocyte-macrophage progenitor cells in vitro. (1/56)
We studied the inhibitory effects on colony formation by granulocyte-macrophage colony forming units (cfu-gm) of eight azole antifungal agents in vitro. All agents, except fluconazole, inhibited colony formation dose-dependently with 50% inhibitory concentrations (IC50) in the range of 0.78-49 micromol/L in cultures of murine and human bone marrow. For human cells, the IC50 values were 0.553 mg/L for itraconazole, 1.24 mg/L for saperconazole, 2.58 mg/L for clotrimazole, 5.33 mg/L for miconazole, 6.17 mg/L for econazole, 6.27 mg/L for ketoconazole and 8.38 mg/L for oxiconazole. The IC50 of itraconazole for human cfu-gm in vitro was similar to the plasma level of this drug recommended for systemic antifungal therapy (>0.5 mg/L) thus indicating the potential clinical relevance of our data. The IC50 of ketoconazole for human cfu-gm in vitro may be exceeded by plasma levels produced in vivo by high (> or =400 mg) doses, whereas fluconazole failed to reduce colony formation by 50% even at 100 mg/L, a concentration not reached in vivo even after extremely high doses (2000 mg/day). To most of the drugs studied, murine progenitor cells seemed to be less sensitive than the human ones. There was, however, a close correlation between the murine and human log IC50 values of the drugs (r2 = 0.964, P< 0.001), suggesting that cultures of murine bone marrow may be suitable to predict the in-vitro toxicity of azole antifungals to human cfu-gm. (+info)In-vitro resistance to azoles associated with mitochondrial DNA deficiency in Candida glabrata. (2/56)
A commercially available disk diffusion procedure was used in a large-scale study to evaluate the susceptibility of a wide range of Candida isolates to polyenes and azoles. With almost all isolates of C. glabrata resistant colonies were present within the inhibition zones for the azole compounds fluconazole, ketoconazole and miconazole, and less frequently for isoconazole, econazole and clotrimazole. Ten randomly selected isolates were cloned by limiting dilution and the susceptibility of the resulting strains to polyenes and azoles was determined. All strains presented a similar susceptibility pattern with sensitivity to polyenes and the presence of resistant colonies for all azole compounds except tioconazole. For each strain and each antifungal agent, one of these resistant colonies was subcultured and studied for antifungal susceptibility. All these colonies showed similar properties regardless of which antifungal agent allowed their selection, with increased sensitivity to polyenes and cross-resistance to the azole compounds except tioconazole. Similar results were obtained on Shadomy's modified medium and on synthetic medium. Likewise, determination of MICs by the Etest method confirmed the resistance to fluconazole. Comparative growth studies revealed a respiratory deficiency in the mutants caused by mitochondrial DNA (mtDNA) deletions. In addition, 'petite' mutants were obtained from a wild-type strain by exposure to ethidium bromide, and these respiratory mutants were shown to be resistant to azoles. These results demonstrate the relationship between mtDNA deficiency and resistance to azoles, and provide an interesting model to study the mechanisms of action of these antifungal agents. (+info)In vitro activities of ketoconazole, econazole, miconazole, and Melaleuca alternifolia (tea tree) oil against Malassezia species. (3/56)
The in vitro activities of ketoconazole, econazole, miconazole, and tea tree oil against 54 Malassezia isolates were determined by agar and broth dilution methods. Ketoconazole was more active than both econazole and miconazole, which showed very similar activities. M. furfur was the least susceptible species. M. sympodialis, M. slooffiae, M. globosa, and M. obtusa showed similar susceptibilities to the four agents. (+info)Positive and negative control of multidrug resistance by the Sit4 protein phosphatase in Kluyveromyces lactis. (4/56)
The nuclear gene encoding the Sit4 protein phosphatase was identified in the budding yeast Kluyveromyces lactis. K. lactis cells carrying a disrupted sit4 allele are resistant to oligomycin, antimycin, ketoconazole, and econazole but hypersensitive to paromomycin, sorbic acid, and 4-nitroquinoline-N-oxide (4-NQO). Overexpression of SIT4 leads to an elevation in resistance to paromomycin and to lesser extent tolerance to sorbic acid, but it has no detectable effect on resistance to 4-NQO. These observations suggest that the Sit4 protein phosphatase has a broad role in modulating multidrug resistance in K. lactis. Expression or activity of a membrane transporter specific for paromomycin and the ABC pumps responsible for 4-NQO and sorbic acid would be positively regulated by Sit4p. In contrast, the function of a Pdr5-type transporter responsible for ketoconazole and econazole extrusion, and probably also for efflux of oligomycin and antimycin, is likely to be negatively regulated by the phosphatase. Drug resistance of sit4 mutants was shown to be mediated by ABC transporters as efflux of the anionic fluorescent dye rhodamine 6G, a substrate for the Pdr5-type pump, is markedly increased in sit4 mutants in an energy-dependent and FK506-sensitive manner. (+info)Effect of cytochrome P-450 inhibitors econazole, bifonazole and clotrimazole on prostanoid formation. (5/56)
1. The present study was carried out to clarify the effect of the imidazole antimycotics econazole, bifonazole and clotrimazole on prostanoid biosynthesis. Osteoblast-like MC3T3-E1 cells stimulated by endothelin-1, melittin, ionomycin or arachidonic acid showed diminished prostaglandin E(2) (PGE(2)) production upon pretreatment with econazole. Following pretreatment with bifonazole, stimulation with ionomycin or arachidonic acid also resulted in decreased PGE(2) formation. Clotrimazole inhibited ionomycin but not arachidonic acid stimulated PGE(2) synthesis in MC3T3-E1 cells. 2. The results observed in osteoblast-like UMR-106 cells pretreated with econazole, bifonazole or clotrimazole and stimulated by arachidonic acid were similar with the exception of clotrimazole which was a more effective inhibitor of PGE(2) biosynthesis than in MC3T3-E1 cells. 3. Upon treatment with arachidonic acid thromboxane B(2) (TXB(2)) production in human platelets was abolished completely at concentrations of the three imidazole antimycotics higher than 5 microM (IC(50)<1 microM). 4. These data were confirmed by a direct assay using purified ram seminal vesicle prostaglandin H(2) synthase-1 (PGHS-1), which clearly showed inhibitory properties of econazole (IC(50) 4.7+/-2.3 microM), bifonazole (IC(50) 9.4+/-0.8 microM) and clotrimazole (IC(50) 4.4+/-0.6 microM). 5. Summarizing, these results indicate an inhibitory effect of econazole, bifonazole and clotrimazole on PGHS-1, varying in its potency dependent on the cell system used. In addition TXB(2) formation is affected at doses even lower than those needed to suppress PGE(2) biosynthesis. (+info)Activity of the Kluyveromyces lactis Pdr5 multidrug transporter is modulated by the Sit4 protein phosphatase. (6/56)
A possible role for posttranslational modifications in regulating the activity of ATP-binding cassette (ABC) transporters has not been well established. In this study, the drug efflux ABC transporter gene KlPDR5 was isolated from the budding yeast Kluyveromyces lactis, and it was found that the encoded KlPdr5 drug pump is posttranslationally regulated by the type 2A-related Ser/Thr protein phosphatase, Sit4p. The KlPdr5 transporter is a protein of 1,525 amino acids sharing 63.8% sequence identity with its Saccharomyces cerevisiae counterpart, ScPdr5p. Overexpression of the KlPDR5 gene confers resistance to oligomycin, antimycin, econazole, and ketoconazole, whereas cells with a disrupted allele of KlPDR5 are hypersensitive to the drugs and have a decreased capacity to carry out efflux of the anionic fluorescent dye rhodamine 123. It was found that a chromosomal disruption of KlPDR5 abolishes the drug-resistant phenotype associated with sit4 mutations and that a synergistic hyperresistance to the drugs can be created by overexpressing KlPDR5 in sit4 mutants. These data strongly indicate that the multidrug-resistant phenotype of sit4 mutants is mediated by negatively modulating the activity of KlPdr5p. As the transcriptional level of KlPDR5 and the steady-state level of KlPdr5p are not significantly affected by mutations in SIT4, the regulation by Sit4p appears to be a posttranslational process. (+info)Pharmacological modulation of monovalent cation currents through the epithelial Ca2+ channel ECaC1. (7/56)
1. The recent identification of the epithelial Ca(2+) channel, ECaC1, represents a major step forward in our knowledge of renal Ca(2+) handling. ECaC1 constitutes the rate-limiting apical Ca(2+) entry mechanism of active, transcellular Ca(2+) reabsorption. This unique highly selective Ca(2+) channel shares a low but significant homology with transient receptor potential (TRP) channels and vanilloid receptors (VR). 2. We have studied the pharmacological modulation of currents through ECaC1 heterologously expressed in HEK 293 cells. Monovalent cation currents were measured by use of the whole cell patch clamp technique in cells dialysed with 10 mM BAPTA or 10 mM EGTA to prevent the fast Ca(2+) dependent inactivation of ECaC1. 3. Several modulators were tested, including inorganic cations, putative store-operated Ca(2+) entry (SOC) blockers, the vanilloid receptor (VR-1) blocker capsazepine, protein tyrosine kinase blockers, calmodulin antagonists and ruthenium red. 4. Ruthenium red and econazole appeared to be the most effective inhibitors of currents through ECaC1, with IC(50) values of 111 nM and 1.3 microM, respectively, whereas the selective SOC inhibitor, SKF96365, was nearly ineffective. 5. The divalent cation current block profile for ECaC1 is Pb(2+)=Cu(2+) >Zn(2+) >Co(2+) >Fe(2+) with IC(50) values between 1 and approximately 10 microM. 6. In conclusion, ECaC activity is effectively inhibited by various compounds including ruthenium red, antimycotic drugs and divalent cations, which might be useful tools for pharmacological manipulation and several disorders related to Ca(2+) homeostasis could benefit from such developments. (+info)Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. (8/56)
Depletion of Ca(2+) from the endoplasmic reticulum (ER) induces large increases in cytoplasmic Ca(2+), mitochondrial Ca(2+) loading, protein synthesis inhibition, and cell death. To clarify the connections among these events, we have evaluated the effect of Ca(2+) mobilizing agents thapsigargin (Tg), econazole (Ec), and the growth factor Steel Factor (SLF) on bone marrow-derived mast cells (BMMCs). BMMC Ca(2+) stores were found to consist of a Tg-sensitive ER compartment, the Tg-insensitive SIC store, and mitochondrial stores. Low levels of Ec interfered with Tg-stimulated mitochondrial loading while promoting progressive leakage of Ca(2+) from the ER. Low levels of Ec completely reversed Tg toxicity while higher levels blocked store-operated influx and induced cell death in a SLF-enhanced manner. Both Ec and Tg inhibited protein synthesis, however, only SLF plus Tg or very high levels of Ec were able to significantly stimulate EIF-2alpha phosphorylation. Cycloheximide only partially protected BMMCs from Tg toxicity yet strongly synergized with Ec to induce cell death. These results therefore indicate that although both Tg and Ec deplete ER Ca(2+) levels, Ec-induced cell death results from sustained protein synthesis inhibition while Tg toxicity results primarily from mitochondrial Ca(2+) overload and secondarily from ER stress associated with Ca(2+) depletion. (+info)Econazole is an antifungal medication used to treat various fungal infections of the skin, nails, and mucous membranes. It works by inhibiting the synthesis of ergosterol, a key component of fungal cell membranes, thereby weakening the cell membrane and increasing permeability, ultimately leading to fungal cell death.
Econazole is available in various formulations, including creams, lotions, powders, and tablets. It is commonly used to treat conditions such as athlete's foot, jock itch, ringworm, candidiasis (yeast infection), and other fungal skin infections.
It is important to follow the instructions of a healthcare provider when using econazole or any medication, and to report any side effects or concerns promptly.
Miconazole is an antifungal medication used to treat various fungal infections, including those affecting the skin, mouth, and vagina. According to the Medical Subject Headings (MeSH) database maintained by the National Library of Medicine, miconazole is classified as an imidazole antifungal agent that works by inhibiting the synthesis of ergosterol, a key component of fungal cell membranes. By disrupting the structure and function of the fungal cell membrane, miconazole can help to kill or suppress the growth of fungi, providing therapeutic benefits in patients with fungal infections.
Miconazole is available in various formulations, including creams, ointments, powders, tablets, and vaginal suppositories, and is typically applied or administered topically or vaginally, depending on the site of infection. In some cases, miconazole may also be given intravenously for the treatment of severe systemic fungal infections.
As with any medication, miconazole can have side effects and potential drug interactions, so it is important to use it under the guidance of a healthcare professional. Common side effects of miconazole include skin irritation, redness, and itching at the application site, while more serious side effects may include allergic reactions, liver damage, or changes in heart rhythm. Patients should be sure to inform their healthcare provider of any other medications they are taking, as well as any medical conditions they have, before using miconazole.
Clotrimazole is an antifungal medication used to treat various fungal infections such as athlete's foot, jock itch, ringworm, candidiasis (yeast infection), and oral thrush. It works by inhibiting the growth of fungi that cause these infections. Clotrimazole is available in several forms, including creams, lotions, powders, tablets, and lozenges.
The medical definition of Clotrimazole is:
A synthetic antifungal agent belonging to the imidazole class, used topically to treat various fungal infections such as candidiasis, tinea pedis, tinea cruris, and tinea versicolor. It works by inhibiting the biosynthesis of ergosterol, a key component of fungal cell membranes, leading to increased permeability and death of fungal cells.
Fenamates is a term used to refer to a group of non-steroidal anti-inflammatory drugs (NSAIDs) that have a chemical structure related to fenamic acid. This group includes medications such as mefenamic acid, flufenamic acid, and tolfenamic acid, among others.
Fenamates are used to relieve pain, reduce inflammation, and lower fever. They work by inhibiting the activity of cyclooxygenase (COX) enzymes, which play a key role in the production of prostaglandins, hormone-like substances that mediate various physiological processes, including inflammation and pain perception.
Like other NSAIDs, fenamates can cause gastrointestinal side effects such as stomach ulcers, bleeding, and perforation, especially when taken in high doses or for prolonged periods. They may also increase the risk of cardiovascular events such as heart attack and stroke, particularly in people with pre-existing cardiovascular disease or other risk factors.
It is important to use fenamates only under the supervision of a healthcare provider and to follow their dosage instructions carefully to minimize the risk of adverse effects.
Vulvovaginal candidiasis is a medical condition that refers to an infection in the vagina and vulva caused by Candida fungus, most commonly Candida albicans. This type of infection is also commonly known as a yeast infection. The symptoms of vulvovaginal candidiasis can include itching, redness, swelling, pain, and soreness in the affected area, as well as thick, white vaginal discharge that may resemble cottage cheese. In some cases, there may also be burning during urination or sexual intercourse. Vulvovaginal candidiasis is a common condition that affects many women at some point in their lives, and it can be treated with antifungal medications.
Antifungal agents are a type of medication used to treat and prevent fungal infections. These agents work by targeting and disrupting the growth of fungi, which include yeasts, molds, and other types of fungi that can cause illness in humans.
There are several different classes of antifungal agents, including:
1. Azoles: These agents work by inhibiting the synthesis of ergosterol, a key component of fungal cell membranes. Examples of azole antifungals include fluconazole, itraconazole, and voriconazole.
2. Echinocandins: These agents target the fungal cell wall, disrupting its synthesis and leading to fungal cell death. Examples of echinocandins include caspofungin, micafungin, and anidulafungin.
3. Polyenes: These agents bind to ergosterol in the fungal cell membrane, creating pores that lead to fungal cell death. Examples of polyene antifungals include amphotericin B and nystatin.
4. Allylamines: These agents inhibit squalene epoxidase, a key enzyme in ergosterol synthesis. Examples of allylamine antifungals include terbinafine and naftifine.
5. Griseofulvin: This agent disrupts fungal cell division by binding to tubulin, a protein involved in fungal cell mitosis.
Antifungal agents can be administered topically, orally, or intravenously, depending on the severity and location of the infection. It is important to use antifungal agents only as directed by a healthcare professional, as misuse or overuse can lead to resistance and make treatment more difficult.
Econazole
Exophiala
Folliculitis
Topical antifungal drugs
Tineola bisselliella
Tinea cruris
ATC code G01
Pseudogymnoascus destructans
List of MeSH codes (D03)
TRPV6
Antifungal
List of drugs: E-El
Prototheca zopfii
ATC code D01
TRPV5
Imidazole
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Parasites: Using Prescription Drugs Against Parasites Description
Clotrimazole1
- If the chapped lips are caused by yeast, the medical professional will prescribe a topical antifungal such as nystatin, clotrimazole, or econazole. (skinsight.com)
Topical5
- After topical application to the skin of normal subjects, systemic absorption of econazole nitrate is extremely low. (nih.gov)
- econazole topical will increase the level or effect of warfarin by anticoagulation. (medscape.com)
- Monitor Closely (1) econazole topical will increase the level or effect of warfarin by anticoagulation. (medscape.com)
- The aim of this study was to determine the corneal delivery of econazole using a novel topical enhancement approach using a composite delivery system based upon cyclodextrins and soft hydrogel contact lenses. (swan.ac.uk)
- after 2 weeks of therapy with this cream, continue therapy as needed with a preparation containing econazole or econazole nitrate alone.Pediatric Use: Pediatric patients may demonstrate greater susceptibility to topical corticosteroid-induced HPA axis suppression and Cushing's syndrome than mature patients because of a larger skin surface area to body weight. (medeasy.health)
Triamcinolone acetonide2
- Fass environmental information for Pevisone (econazole, triamcinolone acetonide) from Janssen (downloaded 2018-07-12). (janusinfo.se)
- Read moreEconazole Nitrate & Triamcinolone Acetonide indicated for the treatment of: Eczematous Mycoses Psoriasis Tinea Pedis (Athlete's foot) Tinea Corporis (Ring worm) Tinea Cruris (Jock itch) Inflammatory Intertrigo Diaper Dermatitis Onychomycoses- for the treatment of onychomycoses, local therapy with Econazole/Triamcinolone cream, combined with an oral antimycotic, is recommended. (medeasy.health)
Pevisone1
- It is a component of Pevisone, Ecoderm-TA and ECOSONE (econazole/triamcinolone). (wikipedia.org)
Nitrate exhibits1
- citation needed] Econazole nitrate exhibits strong anti-feeding properties against the keratin-digesting common clothes moth Tineola bisselliella. (wikipedia.org)
Antifungal medication2
- Econazole is an antifungal medication of the imidazole class. (wikipedia.org)
- Econazole nitrate lotion is a commonly used antifungal medication that efficiently treats numerous fungal infections of the skin. (graficodo.com)
Cream9
- Econazole is used as a cream to treat skin infections such as athlete's foot, tinea, pityriasis versicolor, ringworm, and jock itch. (wikipedia.org)
- About 3% of patients treated with econazole nitrate cream reported side effects. (wikipedia.org)
- Econazole comes as a cream to apply to the skin. (medlineplus.gov)
- Econazole Nitrate Cream, 1% is contraindicated in individuals who have shown hypersensitivity to any of its ingredients. (nih.gov)
- Econazole Nitrate Cream, 1% is not for ophthalmic use. (nih.gov)
- Avoid introduction of Econazole Nitrate Cream into the eyes. (nih.gov)
- Econazole nitrate cream is a medication generally utilized to treat numerous fungal infections of the skin. (graficodo.com)
- Econazole nitrate cream is made to fight different types of fungi that cause skin infections. (graficodo.com)
- Some medicines might interact with econazole nitrate cream, possibly influencing its effectiveness or boosting the threat of side effects. (graficodo.com)
Indications1
- Econazole nitrate has been shown to be active against most strains of the following microorganisms, both in vitro and in clinical infections as described in the INDICATIONS AND USAGE section. (nih.gov)
Allergic2
- tell your doctor and pharmacist if you are allergic to econazole or any other drugs. (medlineplus.gov)
- Individuals with a known allergic reaction or hypersensitivity to econazole nitrate or any of its elements should stay clear of using this drug. (graficodo.com)
Topically1
- Econazole nitrate lotion is very easy to use topically to the afflicted location. (graficodo.com)
Medication1
- While econazole nitrate lotion is generally taken into consideration secure for use during pregnancy and breastfeeding, it is a good idea to speak with a health care professional before using any type of medication during these periods. (graficodo.com)
Dose1
- and achieved both a more rapid and a higher cure rate compared with a triple dose of econazole. (curehunter.com)
Pregnancy1
- Econazole nitrate should be used in the first trimester of pregnancy only when the physician considers it essential to the welfare of the patient. (nih.gov)
Pregnant1
- If you become pregnant while using econazole, call your doctor. (medlineplus.gov)
Adverse2
- Intravaginal administration in humans has not shown prolonged gestation or other adverse reproductive effects attributable to econazole nitrate therapy. (nih.gov)
- When made use of as directed, econazole nitrate lotion generally has marginal adverse effects. (graficodo.com)
Infections1
- By utilizing econazole nitrate lotion as routed, individuals can successfully manage and also deal with fungal infections, advertising healthier skin. (graficodo.com)
Differences1
- Yeast Yhb and Ralstonia eutropha flavoHb both structurally studied in complex with econazole indicate conformational differences between the inhibitors and the polypeptide primarily caused by stable binding of a phospholipid to the latter and by distinct loop D structures. (rcsb.org)
Side effects1
- Econazole may cause side effects. (medlineplus.gov)
Warfarin1
- Econazole: compound metabolized by CYP3A4/2C9 oral anticoagulants (warfarin & acenocoumarol).Triamcinolone: lowering of plasma salicylates levels. (medeasy.health)
Symptoms1
- If you still have symptoms of infection after you finish econazole, call your doctor. (medlineplus.gov)
Clinical1
- In summary, the results in this study have demonstrated that a composite drug delivery system based upon econazole-HP-β-CD inclusion complexes loaded into contact lenses can achieve significantly greater corneal drug delivery with the potential for improved clinical responses. (swan.ac.uk)
Continue1
- Continue to use econazole even if you feel well. (medlineplus.gov)
Eyes1
- Do not let econazole get into your eyes or mouth, and do not swallow it. (medlineplus.gov)
Effect1
- Effect of econazole and benzydamine on sensory neurons in culture. (nih.gov)
External2
- Econazole is for external use only. (medlineplus.gov)
- Econazole nitrate lotion is suggested for external usage only. (graficodo.com)
Made1
- Acceptable predictions were made for Econazole, Methoxsalen, Flurbiprofen and ketoprofen with adjustments to the diffusivity of the stratum corneum. (cdc.gov)
Safety1
- This write-up will certainly delve into the usages, advantages, and safety measures connected with econazole nitrate lotion. (graficodo.com)
Data3
- It cannot be excluded that econazole is persistent, due to the lack of data. (janusinfo.se)
- The use of econazole (sales data Sweden 2015) has been considered to result in low environmental risk. (janusinfo.se)
- The minimum inhibitory concentration (MIC) of econazole was determined against four fungal species associated with keratitis, and these data were then related to the amount of drug delivered to the cornea, using an average corneal volume of 0.19 mL. (swan.ac.uk)