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European Journal of Clinical... Dec 2010To investigate if the ordinary use of a vaginal suppository containing miconazole results in systemic absorption that is sufficient to affect the activities of CYP1A2...
PURPOSE
To investigate if the ordinary use of a vaginal suppository containing miconazole results in systemic absorption that is sufficient to affect the activities of CYP1A2 and CYP3A4, which are major drug- and steroid-metabolising enzymes.
METHODS
In 20 healthy non-pregnant women aged 18-45 years, the serum concentration of miconazole was determined following the use of a vaginal suppository containing 1,200 mg miconazole. Enzyme activities of CYP1A2 and CYP3A4 were determined as metabolic ratios of caffeine (CMR = (AFMU + 1MU + 1MX)/17DMU) and quinidine (QMR = 3-hydroxy-quinidine/quinidine) respectively before and 34 h after insertion of the suppository. Miconazole was analysed by LC-MS/MS, while caffeine and metabolites were analysed by HPLC-UV and quinidine and hydroxy-quinidine were analysed by HPLC fluorescence.
RESULTS
All 20 women had measurable concentrations of miconazole in serum (mean ± SD: 12.9 ± 5.6 μg/L; range: 3.5-24.6 μg/L). Although not statistically significant, an association between the serum concentrations of miconazole and the inhibition of CYP1A2 activity was indicated. No relation was observed between the CYP3A4 activity and the miconazole serum concentration.
CONCLUSIONS
Miconazole is absorbed via the vaginal mucosa to the systemic circulation in measurable concentrations. Our data indicate a concentration-dependent inhibition of CYP1A2, but the effect is negligible compared with the variation in the activity of CYP1A2 and is regarded to be of no clinical significance to the women. However, further studies on the ability of miconazole to be transferred across the placenta or to interfere with the placental function are warranted to secure safe use during pregnancy.
Topics: Adult; Antifungal Agents; Cytochrome P-450 CYP1A2; Cytochrome P-450 CYP3A; Female; Humans; Miconazole; Suppositories; Vagina
PubMed: 20924570
DOI: 10.1007/s00228-010-0906-2 -
The British Journal of Dermatology Jul 1975A double-blind trial of 2% miconazole in a cream and in a powder base and of the respective vehicles was done in a group of forty-five young sportsmen regularly training... (Clinical Trial)
Clinical Trial
A double-blind trial of 2% miconazole in a cream and in a powder base and of the respective vehicles was done in a group of forty-five young sportsmen regularly training and using the showers in a gymnasium. After 4 weeks treatment, the mycological cure rate using the active preparation was 60% compared to 24% for the placebo (P less than 0-05).
Topics: Adult; Clinical Trials as Topic; Humans; Imidazoles; Male; Miconazole; Ointments; Powders; Sports Medicine; Tinea Pedis; Trichophyton
PubMed: 1103934
DOI: 10.1111/j.1365-2133.1975.tb06480.x -
Journal of Chromatography Jan 1982
Topics: Chromatography, High Pressure Liquid; Humans; Imidazoles; Miconazole; Saliva; Time Factors
PubMed: 7056815
DOI: 10.1016/s0378-4347(00)80377-1 -
BMJ Open May 2024To evaluate the efficacy of topical miconazole or amorolfine compared to placebo for mild to moderately severe onychomycosis. (Randomized Controlled Trial)
Randomized Controlled Trial
How effective is topical miconazole or amorolfine for mild to moderately severe onychomycosis in primary care: the Onycho Trial - a randomised double-blind placebo-controlled trial.
OBJECTIVES
To evaluate the efficacy of topical miconazole or amorolfine compared to placebo for mild to moderately severe onychomycosis.
DESIGN
Randomised, double-blind, placebo-controlled trial, with computer-generated treatment allocation at a 1:1:1 ratio.
SETTING
Primary care, recruitment from February 2020 to August 2022.
PARTICIPANTS
193 patients with suspected mild to moderately severe onychomycosis were recruited via general practices and from the general public, 111 of whom met the study criteria. The mean age of participants was 51 (SD 13.1), 51% were female and onychomycosis was moderately severe (mean OSI 12.1 (SD 8.0)).
INTERVENTIONS
Once-daily miconazole 20 mg/g or once-weekly amorolfine 5% nail lacquer solution was compared with placebo (denatonium benzoate solution).
MAIN OUTCOME MEASURES
Complete, clinical and mycological cure at 6 months. Secondary outcomes were clinical improvement, symptom burden, quality of life, adverse effects, compliance, patient-perceived improvement and treatment acceptability.
RESULTS
Based on intention-to-treat analysis, none of the participants receiving miconazole or amorolfine reached complete cure compared with two in the placebo group (OR not estimable (n.e.), p=0.493 and OR n.e., p=0.240, respectively). There was no evidence of a significant difference between groups regarding clinical cure (OR n.e., p=0.493 and OR 0.47, 95% CI 0.04 to 5.45, p=0.615) while miconazole and amorolfine were less effective than placebo at reaching both mycological cure (OR 0.25, 95% CI 0.06 to 0.98, p=0.037 and OR 0.23, 95% CI 0.06 to 0.92, p=0.029, respectively) and clinical improvement (OR 0.26, 95% CI 0.08 to 0.91, p=0.028 and OR 0.25, 95% CI 0.07 to 0.85, p=0.021, respectively). There was no evidence of a significant difference in disease burden, quality of life, adverse reactions, compliance, patient-perceived improvement or treatment acceptability.
CONCLUSIONS
Topical miconazole and amorolfine were not effective in achieving a complete, clinical or mycological cure of mild to moderately severe onychomycosis, nor did they significantly alleviate the severity or symptom burden. These treatments should, therefore, not be advised as monotherapy to treat onychomycosis.
TRIAL REGISTRATION NUMBER
WHO ICTRP NL8193.
Topics: Humans; Miconazole; Onychomycosis; Female; Double-Blind Method; Male; Middle Aged; Antifungal Agents; Administration, Topical; Treatment Outcome; Adult; Primary Health Care; Quality of Life; Aged; Severity of Illness Index; Morpholines
PubMed: 38702077
DOI: 10.1136/bmjopen-2023-081914 -
BMC Oral Health Feb 2024Oral thrush is the most common occurring fungal infection in the oral cavity in uncontrolled diabetic patients, it is treated by various antifungal drugs according to... (Randomized Controlled Trial)
Randomized Controlled Trial
The anti-fungal effect of miconazole and miconazole-loaded chitosan nanoparticles gels in diabetic patients with Oral candidiasis-randomized control clinical trial and microbiological analysis.
BACKGROUND
Oral thrush is the most common occurring fungal infection in the oral cavity in uncontrolled diabetic patients, it is treated by various antifungal drugs according to each case. This study aimed to evaluate the therapeutic effects of topical application of miconazole and miconazole-loaded chitosan nanoparticles in treatment of diabetic patients with oral candidiasis.
METHODS
In this randomized controlled clinical trial. A total of 80 diabetic patients presenting with symptomatic oral candidiasis were randomly assigned into two treatment groups: miconazole and miconazole-loaded chitosan nanoparticles. The patients were treated for 28 days, and clinical assessments were conducted at baseline, 7, 14, 21 and 28 days. Clinical parameters, including signs and symptoms of oral candidiasis were evaluated and microbiological analysis was performed to determine the Candida species and assess their susceptibility to the antifungal agents. Statistical analysis was done to the categorical and numerical data using chi-square test and Kruskal Wallis test.
RESULTS
The antifungal efficacy between the miconazole and miconazole-loaded chitosan nanoparticles (CS-MCZ) groups insignificant difference (P > 0.05) was observed. Both treatment modalities exhibited comparable effectiveness in controlling oral candidiasis symptoms and reducing Candida colonization as miconazole-loaded chitosan nanoparticles group showed a significant difference in the clinical improvement in respect of both signs and symptoms from baseline (70%) until the end of study at 28 days (5%) (P < 0.05) Moreover, miconazole-loaded chitosan nanoparticles, there was a significant reduction in the number of colonies forming units of Candida albicans from baseline until the end of the study at 28-day with P value < 0.000.
CONCLUSIONS
This randomized controlled clinical trial and microbiological analysis demonstrate that both miconazole and miconazole-loaded chitosan nanoparticles are effective in the treatment of oral candidiasis in diabetic patients with no adverse reactions.
TRIAL REGISTRATION
NCT06072716 with first registration first registration in 10/10/2023.
Topics: Humans; Miconazole; Antifungal Agents; Candidiasis, Oral; Chitosan; Candida; Nanoparticles; Gels; Diabetes Mellitus
PubMed: 38321454
DOI: 10.1186/s12903-024-03952-0 -
Congenital Anomalies Mar 2004Miconazole cream is used in Hungary to treat fungal genital and skin infections in pregnant women, but it causes anxiety for both patients and medical doctors due to the...
Miconazole cream is used in Hungary to treat fungal genital and skin infections in pregnant women, but it causes anxiety for both patients and medical doctors due to the category C classification of the drug regarding teratogenic or fetotoxic risk. The objective of this case-control study was to analyze the teratogenic potential of topical miconazole used during pregnancy in the mothers of babies with congenital abnormalities and in matched control mothers of babies without congenital abnormalities. The population-based data set of the Hungarian Case-Control Surveillance of Congenital Abnormalities between 1980 and 1996 included 22 843 women who had newborns or fetuses with congenital abnormalities, and 38 151 pregnant women who had newborn infants without any defects (controls). In the case group, 24 (0.11%) and in the control group, 46 (0.12%) pregnant women were treated with miconazole (crude odd ratio [OR]: 0.9 with 95% confidence interval [CI]: 0.6-1.6). Different congenital abnormality groups were evaluated in case-control pairs and a higher prevalence of miconazole treatment was not found during the second or third month of pregnancy. Thus, treatment with topical miconazole during pregnancy does not increase the risk of congenital abnormalities.
Topics: Abnormalities, Drug-Induced; Administration, Topical; Adult; Antifungal Agents; Case-Control Studies; Female; Humans; Miconazole; Pregnancy
PubMed: 15008899
DOI: 10.1111/j.1741-4520.2004.00007.x -
Life Sciences Mar 2005The effect of miconazole, an anti-fungal drug, on cytoplasmic free Ca2+ concentrations ([Ca2+]i) in human osteosarcoma cells (MG63) was explored by using the...
The effect of miconazole, an anti-fungal drug, on cytoplasmic free Ca2+ concentrations ([Ca2+]i) in human osteosarcoma cells (MG63) was explored by using the Ca2+-sensitive dye fura-2. Miconazole acted in a concentration-dependent manner with an EC50 of 75 microM. The Ca2+ signal comprised a gradual rise and a sustained elevation. Removal of extracellular Ca2+ reduced 50% of the signal. In Ca2+-free medium, the [Ca2+]i rise induced by 1 microM thapsigargin (an endoplasmic reticulum Ca2+ pump inhibitor) was completely inhibited by pretreatment with 20 microM miconazole. Pretreatment with thapsigargin partly inhibited miconazole-induced Ca2+ release. The miconazole-induced Ca2+ release was not changed by inhibition of phospholipase C with 2 microM U73122. By using tetrazolium as a fluorescent probe, it was shown that 10-100 microM miconazole decreased cell proliferation rate in a concentration-dependent manner. Collectively, this study shows that miconazole induces [Ca2+]i rises in human osteosarcoma cells via releasing Ca2+ mainly from the endoplasmic reticulum in a manner independent of phospholipase C activity, and by causing Ca2+ influx. Furthermore, miconazole may be cytotoxic to the cells at higher concentrations.
Topics: Bone Neoplasms; Calcium; Calcium Channel Blockers; Cell Proliferation; Humans; Inositol 1,4,5-Trisphosphate; Miconazole; Osteoblasts; Osteosarcoma; Tumor Cells, Cultured
PubMed: 15826876
DOI: 10.1016/j.lfs.2004.09.033 -
Lancet (London, England) Jan 1982
Topics: Candidiasis; Endophthalmitis; Humans; Imidazoles; Miconazole
PubMed: 6119450
DOI: 10.1016/s0140-6736(82)92602-2 -
Mykosen Oct 1980
Topics: Adult; Aged; Candidiasis, Oral; Female; Gels; Humans; Imidazoles; Male; Miconazole; Middle Aged
PubMed: 7442707
DOI: 10.1111/j.1439-0507.1980.tb02561.x -
Pediatric Surgery International Oct 2016Intestinal perforation (IP) is a fatal complication in extremely low birth weight infants (ELBWI). We started administrating enteral miconazole (MCZ) to ELBWI in 2002....
PURPOSE
Intestinal perforation (IP) is a fatal complication in extremely low birth weight infants (ELBWI). We started administrating enteral miconazole (MCZ) to ELBWI in 2002. Since then, the incidence of IP has significantly decreased. The aim of this study was to elucidate the prophylactic effect of MCZ for the treatment of neonatal IP, and to establish a new prophylactic concept for this disease.
METHODS
In in vivo experiments, the effects of MCZ were examined histopathologically using a mouse model of intestinal ischemia. In in vitro experiments, the cytoprotective effect of MCZ against hypoxia was evaluated using Caco-2 intestinal cells, and its anti-inflammatory potential using a co-culture model of Caco-2 and HL60 cells.
RESULTS
MCZ showed a tissue protective effect against intestinal ischemia. MCZ reduced high mobility group-box 1 (HMGB1) release in Caco-2 cells under hypoxic stress and attenuated the potential to activate co-cultured HL60 leukocytes with Caco-2 cells by suppressing interleukin-8 (IL-8).
CONCLUSION
MCZ may have preventive roles in the clinical management of IP in ELBWI by the suppression of IL-8 and HMGB-1.
Topics: Animals; Caco-2 Cells; Cytochrome P-450 CYP2C9 Inhibitors; Disease Models, Animal; Humans; Intestinal Perforation; Intestines; Male; Mice; Mice, Inbred BALB C; Miconazole; Treatment Outcome
PubMed: 27473010
DOI: 10.1007/s00383-016-3946-6