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Biomedical subjects

G Cauwenbergh

Publications and source records attributed to G Cauwenbergh.

53 records · Page 3Linked to original sources
PubMed1986

Itraconazole pharmacokinetics in the female genital tract: plasma and tissue levels in patients undergoing hysterectomy after a single dose of 200 mg itraconazole.

Twenty patients who underwent hysterectomy received a single dose of 200 mg itraconazole at different moments before surgery. At the moment of surgery, a urine sample, blood sample and tissue samples of different organs of the female genital tract were collected. Blood levels and tissue levels of itraconazole were measured by means of an HPLC method. Itraconazole blood levels were lower than the corresponding tissue levels in the various organs of the female genital tract. This finding for itraconazole is different from findings with ketoconazole, indicating that itraconazole has a higher affinity for tissue than ketoconazole. Urine levels of itraconazole were virtually undetectable in all samples. None of the patients complained of side-effects, and blood biochemical parameters all remained within the normal limits. The premedication with itraconazole had no effect whatsoever on the induction and maintenance of and recovery from the anaesthesia. No abnormal effects on ECG were observed.

Adult↗
PubMed1986

Itraconazole, a new orally active antifungal, in the treatment of pityriasis versicolor.

Itraconazole, a new orally active triazole antifungal, has been tested in patients with pityriasis versicolor. A comparison of different dose schedules was carried out in 73 patients. A regime of 100 mg itraconazole daily for 15 days gave a 100% response rate; 200 mg daily for 5 days gave an 80% response rate. Two patients, who had received 50 mg itraconazole for 14 days, relapsed within 2 months of finishing treatment. Only two patients reported minor side-effects.

Administration, Oral↗
PubMed1986

Itraconazole therapy in pityriasis versicolor.

The efficacy of itraconazole was assessed in an open trial in 30 patients with disseminated lesions of pityriasis versicolor confirmed by direct microscopy. The patients were allocated randomly to one of two treatment regimens, 200 mg once daily for 5 days or 100 mg once daily for 10 days. On assessment 3 weeks after the end of the treatment, 25 patients were healed, two patients had mild residual lesions, two had considerable residual lesions and one patient had relapsed. One patient reported dyspepsia and one patient reported stomach ache. One patient had asymptomatic elevation of serum transaminase (GOT and GPT) but this had returned to normal 3 weeks after the end of therapy.

Adolescent↗
PubMed1986

New and prospective developments in antifungal drugs.

In recent years many new antifungal compounds have been developed. Some of them are currently under investigation as orally or topically active drugs in human mycotic infections. The 3 main groups in this development are imidazoles, triazoles and allylamines. The group of imidazoles consists mainly of topical drugs with an activity comparable to that of miconazole, clotrimazole e.a. Besides ketoconazole, some other orally active imidazoles are currently under development e.g. SC38390. The chemical group of antifungals receiving the most attention at present is the tiazole family. Both topical (e.g. terconazole) as oral (e.g. R 51 211, Bay 7133) drugs are currently investigated. A third group consists of allylamines in which SF86-327 is developed for both oral and topical use.

Administration, Oral↗
PubMed1986

The pharmacology of agents used in the treatment of pulmonary mycoses.

The different antifungals currently used in pulmonary mycoses consist of polyene antibiotics, the antimetabolite 5-fluorocytosine, and azole derivatives. The pharmacologic profiles, mechanisms of action, pharmacokinetics, clinical indications for use, dosage recommendations, side effects, and drug interactions for these agents are presented.

Amphotericin B↗
PubMed1986

Prophylaxis of mycotic infections in immunocompromised patients: a review of 27 reports and publications.

During the last three years, several studies have investigated the potential of ketoconazole for antifungal prophylaxis in immunocompromised patients. Ketoconazole 200 mg o.d. seems to have some effect, but this daily dose is considered too low. Studies using higher doses suggest an increased prophylactic effect with 400 mg and adequate prophylaxis with 600 mg ketoconazole daily. When compared with other antifungals, ketoconazole seems to be superior to nystatin and as effective as amphotericin B (500 mg t.i.d.).

Amphotericin B↗
PubMedDate not supplied

Fungal cultures on cyanoacrylate skin surface strippings as a dose-finding method for topical antifungals. A placebo-controlled study with 0.25% and 0.50% itraconazole cream.

The antimycotic activities of 0.25% and 0.50% itraconazole cream were compared in the stratum corneum after once-daily applications for 1 week. Two groups of 12 healthy volunteers applied either itraconazole or placebo on the inner side of each forearm, in a double-blind design. Cyanoacrylate skin surface strippings (CSSS) were taken on days 8, 11 and 21. Conidia or yeasts of selected fungi (Trichophyton rubrum, Trichophyton metagrophytes, Microsporum canis and Candida albicans) were deposited on CSSS. Fungal growth on CSSS was assessed in time by computerized image analysis to derive the inhibitory effect of the previously applied antifungal preparations. Comparable antimycotic activity was found against dermatophytes for both concentrations. Itraconazole 0.50% appeared to be more active than 0.25% against C. albicans. The 0.50% concentration yielded prominent fungitoxic effect after 1 week of treatment, and showed a lingering effect in the stratum corneum for at least 3 days. This method could be useful in a pre-clinical setting and serve as a predictive tool for further clinical dose-finding studies with topical antimycotics.

Adult↗
PubMedDate not supplied

Itraconazole in the treatment of human mycoses: review of three years of clinical experience.

During the first three years of clinical investigation of itraconazole, more than 1,000 patients with mycoses were treated with the drug. Almost 50% were women with vaginal candidosis; a dosage of 200 mg per day for three days appeared to be optimal for their treatment. Several treatment regimens were tested for pityriasis versicolor; the minimum total dose necessary for optimal results was 1 g. A randomized comparison of 50-mg and 100-mg daily doses for the treatment of skin mycoses indicated that the optimal dosage is 100 mg. The results of short courses of treatment for superficial dermatophytoses suggest that such regimens may be effective, and the results of an ongoing double-blind comparison of itraconazole and griseofulvin suggest that itraconazole is superior in these infections. The outcome of treatment of systemic mycoses with itraconazole, especially sporotrichosis, chromomycosis, and aspergillosis, indicates that itraconazole may be useful in therapy for life-threatening fungal infections when standard therapy has failed.

Antifungal Agents↗
PubMedDate not supplied

Itraconazole: pharmacologic studies in animals and humans.

Several pharmacologic studies of itraconazole, an orally active antifungal triazole, were conducted in humans and animals. In dogs and rats, no significant toxic effects were seen at doses of up to 40 mg/kg. Endocrinologic studies demonstrated that itraconazole, unlike ketoconazole, does not significantly affect human testicular and adrenal steroidogenesis. Pharmacokinetic studies indicated that itraconazole has a high tissue affinity and a longer half-life than ketoconazole. These pharmacologic observations suggest that itraconazole has a broader spectrum of activity than ketoconazole and a lower potential for producing adverse effects.

Adrenal Glands↗
PubMedDate not supplied

Ketoconazole vs. itraconazole for antifungal prophylaxis in patients with severe granulocytopenia: preliminary results of two nonrandomized studies.

The efficacies of antifungal prophylaxis with ketoconazole and itraconazole, a new triazole, in patients with prolonged granulocytopenia were evaluated in two nonrandomized studies. The conditions other than the drug administered for prophylaxis were equivalent in the two studies. The incidence of fatal fungal infections was significantly higher among patients given ketoconazole than among those given itraconazole (P = .02); this trend was especially evident with fatal infections due to Aspergillus (P = .0045). The level of protection from fatal fungal infection afforded by itraconazole was highly significant among patients who were granulocytopenic for more than 25 days (P less than .0001) and among patients with acute lymphoblastic leukemia (P = .008). Failures of prophylaxis with itraconazole may have been due to inadequate levels of drug in plasma. Although these results must be interpreted with caution because they were obtained in consecutive nonrandomized studies, the use of itraconazole for antifungal prophylaxis in granulocytopenic patients seems to be a major advance and to be especially advantageous in hospitals, where the incidence of fatal aspergillosis in these patients is high.

Adolescent↗
PubMedDate not supplied

Oral candidosis: treatment with absorbable and non-absorbable antifungal agents in children.

Oral candidosis in neonates and children is a common infection which occurs often during the first few months after birth, but occasionally also in older children with certain predisposing factors. In neonates, oral candidosis is usually benign, although the symptoms of such an acute infection can be disturbing to both the patient and the parents. In older children developing oral candidosis, specific predisposing factors may be present (e.g. immunodeficiency, chemotherapy, etc.). In such cases, the infection may constitute a source for further dissemination, leading to occasionally fatal Candida sepsis or to widespread chronic mucocutaneous candidosis. Treatment modalities to date include drugs with limited or no absorption from the gastrointestinal tract (e.g. nystatin and miconazole) and agents that are absorbed, combining local effect with systemic therapy (e.g. clotrimazole, ketoconazole, itraconazole and fluconazole). Overall, it appears that treatment of neonatal oral candidosis should be performed with non-absorbable drugs, while the systemically active agents should be used primarily if a risk of dissemination exists or if widespread disease is present. In general, side-effects and toxicity are not major causes of concern with non-absorbed or absorbed antifungals in children with oral candidosis, since treatment is usually of relatively short duration. When the systemically active agents are used in premature infants with sub-optimal liver function, the risk of drug-induced liver toxicity may be increased.

Absorption↗
PubMedDate not supplied

Cryptococcal meningitis: the place of itraconazole.

Itraconazole, an orally active broad-spectrum triazole antimycotic, has demonstrated anti-Cryptococcus activity in vitro and in animal models of cryptococcal meningitis. The drug has been used by a number of clinical groups for the treatment of cryptococcal meningitis, predominantly in AIDS patients. A problem that has been found with ketoconazole is the relatively low absorption of the drug in AIDS patients. This has resulted in ketoconazole plasma levels below the MIC90 (1-5 micrograms ml-1) needed to eliminate Cryptococcus neoformans. In addition, tissue levels of ketoconazole are lower than plasma levels. For itraconazole, the required MIC90 for Cr. neoformans is 0.1 microgram ml-1, and the plasma levels in AIDS patients receiving 200-400 mg daily, even in the case of reduced absorption, are well above this MIC90. The itraconazole levels in the brain and in the meninges are higher than the plasma levels. Consequently, itraconazole has been considered a valid candidate for studies in patients with cryptococcal meningitis. Various treatment modalities have been used: primary oral therapy alone or in combination with amphotericin B or 5-fluorocytosine (5-FC); maintenance oral therapy after initial treatment with amphotericin B (with or without 5-FC); and first-line intravenous treatment in severely ill patients. The results were evaluated in four different groups. When the drug was given as primary oral therapy without combination with amphotericin B or 5-FC, the results depended greatly on the dose administered and on the life expectancy of the patient at inclusion. In general, daily doses of 400 mg were better than 200-mg doses.(ABSTRACT TRUNCATED AT 250 WORDS)

AIDS-Related Opportunistic Infections↗
PubMedDate not supplied

Corneofungimetry bioassay on Malassezia spp. under ketoconazole and desonide influences.

BACKGROUND: Glucocorticoids can boost some Malassezia-driven dermatoses. However, both antifungals and topical corticosteroids improve lesions of seborrheic dermatitis. OBJECTIVE: To revisit the topical activity of the antifungal ketoconazole and the corticosteroid desonide on Malassezia growth on human stratum corneum. MATERIAL AND METHODS: The computer-assisted corneofungimetry bioassay was used to compare the growth of M. furfur, M. globosa and M. restricta on human stratum corneum coated with olive oil. Four blinded gel formulations were tested. They contained either 2% ketoconazole, 0.05% desonide or a combination of 2% ketoconazole and 0.05% desonide; one gel was unmedicated. Untreated stratum corneum and specimens coated with a 2% ketoconazole cream were used as negative and positive comparators, respectively. A total of 45 samples (15 M. furfur, 15 M. globosa, and 15 M. restricta) were used for each test formulation in this randomized, double-blind study. RESULTS: The 2% ketoconazole gel and cream and the combination of 2% ketoconazole and 0.05% desonide formulation abated similarly and significantly the M. furfur, M. globosa and M. restricta growth. The 3 species were similarly sensitive to these formulations. By contrast, no significant inhibitory effect was yielded by the 0.05% desonide gel and the vehicle. CONCLUSION: The presence of 0.05% desonide does not impair or improve the Malassezia susceptibility to 2% ketoconazole when growing on lipid-enriched human stratum corneum.

Administration, Topical↗
PubMedDate not supplied

A randomized, placebo-controlled trial of topical retinol in the treatment of cellulite.

BACKGROUND: Cellulite occurs to varying degrees on the thighs and buttocks of many otherwise healthy women. Among the many purported treatments for cellulite, only a handful have been tested in clinical trials. OBJECTIVE: The aim of this study was to critically explore the reputed effect of topical retinol in the treatment of cellulite. MATERIALS AND METHODS: The study compared the effect of topical retinol to a placebo formulation in a left-right randomized trial in order to eliminate the massage-effect. The study was conducted in 15 women aged from 26 to 44 years who had requested liposuction to improve mild to moderate cellulite. RESULTS: After 6-months of treatment, skin elasticity was increased by 10.7% while viscosity was decreased by 15.8% at the retinol-treated site. Such an effect on the tensile properties of skin was more prominent where the mattress phenomenon was the only evidence of cellulite. The lumpy-bumpy appearance of the skin showed either little response or was not responsive to the treatment. Although gross microanatomical differences were not disclosed between the comparative sites at completion of the study, evidence for a shift in the phenotype of connective tissue cells was obtained. The main retinol-related change consisted of a 2- to 5-fold increase in the number of factor XIIIa+ dendrocytes both in the dermis and fibrous strands of the hypodermis. CONCLUSIONS: We hypothesize that the functional and phenotypic changes seen in this study were linked and represent the result of a direct or indirect modulating effect of retinol on cellulite. Such features ultimately improve the resting tensions inside the skin which should in turn smooth the skin surface.

Adipose Tissue↗