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Heterocyclic Drugs from Plants
Published in Rohit Dutt, Anil K. Sharma, Raj K. Keservani, Vandana Garg, Promising Drug Molecules of Natural Origin, 2020
Debasish Bandyopadhyay, Valeria Garcia, Felipe Gonzalez
Fluconazole (Figure 8.13) is an antibiotic, frequently used in treating fungal and yeast infections (Fluconazole, 2018). This drug belongs to the triazole class of antifungal agents which works by inhibiting/reducing the fungal growth that causes infection in the human body. Substantial clinical studies demonstrated fluconazole’s effectiveness, its favorable pharmacokinetics, and safety profile; all these have a large contribution to its widespread uses (Cha et al., 2004). This drug works well in fungal meningitis and as a preventive medicine for infections due to chemotherapy, radiation therapy, or bone marrow transplant (Fluconazole, 2018). It also demonstrated activity up to a certain extent for the treatment of fungal infections in HIV positive patients. Fluconazole is taken orally but it some cases intravenous administration is preferred (Zervos et al., 1993).
Therapy For Skin, Hair and Nail Fungal Infections
Published in Raimo E Suhonen, Rodney P R Dawber, David H Ellis, Fungal Infections of the Skin, Hair and Nails, 2020
Raimo E Suhonen, Rodney P R Dawber, David H Ellis
Fluconazole is an oral synthetic bis-triazole compound that inhibits the cytochrome P450-dependent 14 alpha-demethylation step in the formation of ergosterol, which leads to alterations in a number of membrane-associated cell functions. Fluconazole has a broad spectrum of activity that includes both dermatophytes and yeasts. It is water soluble and is rapidly absorbed, with good penetration into all tissues and body fluids. Absorption is not dependent on acid conditions and is also unaffected by food intake. Unlike other azoles, fluconazole is not metabolised in humans and it is largely excreted unchanged in the urine. The usual adult doses range between 100 and 400 mg/day, depending on the immune status of the patient, the infecting organism and the patient’s response to therapy. With most mucocutaneous diseases, it is usual to start with a higher dose of 400 mg/day for the first two days and then reduce to 100–200 mg/day. Vaginal candidiasis usually responds to a single dose of 150 mg. Fluconazole is generally well tolerated. It has minor side-effects, such as nausea and vomiting, which occur in a few patients. Unlike ketoconazole and itraconazole, fluconazole has few significant drug interactions. However, the effects of warfarin, cyclosporin A, oral hypoglycaemics, phenytoin, midazolam and theophylline may be increased by fluconazole when given in doses of 200 mg/day or higher. Fluconazole has been proven to be particularly effective in the treatment of mucosal and cutaneous forms of candidiasis. It is currendy the drug of choice for controlling oropharyngeal candidiasis in AIDS patients.
Anti-Infective Agents
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: The use of Fluconazole should be avoided in pregnant women, especially during the 1st Trimester, because the pregnancy experience in humans has shown the risk of teratogenicity at doses ≥400 mg/day.
In vitro and in vivo anti-Candida activity of citral in combination with fluconazole
Published in Journal of Oral Microbiology, 2022
Katherine Miranda-Cadena, Cristina Marcos-Arias, Aitzol Perez-Rodriguez, Iván Cabello-Beitia, Estibaliz Mateo, Elena Sevillano, Lucila Madariaga, Guillermo Quindós, Elena Eraso
Fluconazole is one of the first-line antifungal agents for treating candidiasis. This triazole interferes with the biosynthesis of ergosterol inhibiting the lanosterol 14-α-demethylase (Erg11), an essential cytochrome P450 enzyme encoded by ERG11[8]. Fluconazole resistance of Candida biofilms is due to several complex mechanisms, including increased metabolic activity and genetic alterations, such as overexpression of genes implicated in efflux pumps in the early stages of biofilm formation [6,9]. In mature biofilms, resistance is associated with a variation in sterol composition of the extracellular polymeric matrix that hinders access and internalization of fluconazole in the sessile cell [10]. In the case of planktonic cells, several mechanisms have been described in C. albicans, including ERG11 point mutations, overexpression of Erg11 mediated by the zinc-cluster transcriptional regulator Upc2, overexpression of the Mdr1 and Cdr1p/Cdr2 efflux pumps, inactivation of the ERG3 gene, aneuploidy (related to Chr5) and/or loss of heterozygosity [8].
Effect of intravaginal gentian violet for acute vaginal candidiasis treated with a single dose oral fluconazole: a randomised controlled trial
Published in Journal of Obstetrics and Gynaecology, 2022
Chenchit Chayachinda, Manopchai Thamkhantho, Popchai Ngamsakulrungroj, Charussri Leeyaphan, Orwan Tulyaprawat
Outcomes measures included clinical cure rate, eradiation rate, time-to-cure, side effects, women’s satisfaction, lifestyle modification and subjective recurrent symptoms (SRS). Clinical cure was defined as absolute relief of symptoms at 2 weeks. Eradication was defined as conversion of positive fungal culture for any Candida spp. at enrolment to no growth at 2-week follow-up. Persistence of the same Candida spp. or detection of any Candida spp. at follow-up was considered as ‘not cure’. Time-to-cure was defined the duration (days) after treatment when the women reported a complete relief of symptoms. Possible side effects of fluconazole included headache, gastrointestinal symptoms and skin rash whereas the side effects of GV included vaginal irritation. Women’s satisfaction was graded into low, medium, high and very high. Lifestyle modification was focussed on intake of sugar-rich diet. SRS was a self-report of having new episodes of any symptoms and signs of VC.
Oral antifungal therapies for toenail onychomycosis: a systematic review with network meta-analysis toenail mycosis: network meta-analysis
Published in Journal of Dermatological Treatment, 2022
Maria L. D. Fávero, Aline F. Bonetti, Eric L. Domingos, Fernanda S. Tonin, Roberto Pontarolo
Rates of treatment failure with standard antifungal drugs range from 25% to 40%, and have been attributed, among others, to poor patient compliance, low bioavailability and lack of drug penetration into the nail (69). The most beneficial strategy to manage onychomycosis includes a correct diagnosis of the condition and its comorbidities, along with patient-tailored therapy with preferential use of oral drugs, and hygiene education/orientation (64,66). Patient expectations should be balanced between efficacy, therapy costs and avoidance of adverse events. Since treatment discontinuation is commonplace, the indication of pulse therapies or drugs with a long half-life that allows weekly dosing schedules, could be promising alternatives. We suggest albaconazole and posaconazole to be further investigated in well-design head-to-head trials compared to the current first-line therapies. Terbinafine remains effective approaches to manage onychomycosis. Patients requiring less adverse events may use fluconazole. The use of ravuconazole, ketoconazole or griseofulvin is hardly justified given the lack of expressive efficacy or high rates of medication related adverse events and discontinuation.