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Candida and parasitic infection: Helminths, trichomoniasis, lice, scabies, and malaria
Published in Hung N. Winn, Frank A. Chervenak, Roberto Romero, Clinical Maternal-Fetal Medicine Online, 2021
Treatment of Candida vulvovaginitis in pregnancy is typically limited to topical azoles and nystatin (16,25). For many years, nystatin was the primary drug used for Candida vulvovaginitis in pregnancy because its extremely poor absorption was felt to improve its safety (pregnancy category B) (25). As studies have proven, the increased efficacy of the azole antifungal agents, miconazole, clotrimazole, butoconazole, and terconazole, has become the mainstays of therapy in pregnancy. They have been used extensively in human pregnancy with no adverse effects or increase in congenital malformations noted, but most remain pregnancy category C due to the absence of adequate controlled human studies. There is no clear leader from this group in terms of efficacy and patient satisfaction, so selection may be based on availability and cost. Seven-day treatment is usually needed in pregnancy due to the higher rates of treatment failure and recurrence. Cure rates are typically 5% to 10% lower than those in nonpregnant women for the same dosing regimen.
Terconazole
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Terconazole is a synthetic triazole derivative structurally related to fluconazole. This antifungal seems to disrupt cell wall synthesis by inhibiting biosynthesis of ergosterol or other sterols, damaging the fungal cell membrane, altering its permeability, and promoting loss of essential intracellular elements. Terconazole is active against Candida species and is available in cream and suppository forms (1).
Topical Azoles
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Joanne L. Sharp, Michael A. Pfaller
Terconazole is an effective agent for vaginal candidiasis. Comparative trials of terconazole 80-mg pessaries with clotrimazole vaginal tablets revealed equivalent mycologic efficacy (95% and 85%) and a more rapid onset of symptomatic relief for terconazole-treated women (Kjaeldgaard and Larsson, 1985).
PLGA-modified Syloid®-based microparticles for the ocular delivery of terconazole: in-vitro and in-vivo investigations
Published in Drug Delivery, 2022
Nada Zaghloul, Azza A. Mahmoud, Nermeen A. Elkasabgy, Nada M. El Hoffy
A triazole ketal derivative, terconazole proved its efficacy on a various range of yeasts and mycelium-forming fungi upon its in-vivo investigations. It acts as a powerful antifungal agent, preventing the yeast from morpho-genetically transforming into the highly infectious filamentous form of Candida albicans known as pseudomycelium. Additionally, it is highly active in topical treatment of numerous experimental models of dermatophytosis and candidosis (Heeres et al., 1983). Terconazole is white to almost white powder with a molecular weight of 532.47 Da. It has a log P and Pka of 5.37 and 8, respectively. Unfortunately, its poor aqueous solubility limits its ocular application. The literature sheds the light on several studies investigating the use of terconazole for ocular delivery applying various formulation techniques, including the fabrication of silica/chitosan nanoparticles (Zaghloul et al., 2022) and cationic polymeric nanoparticles (Mohsen, 2022).
Development of bifunctional vaginal suppositories by joint use terconazole and probiotic for treatment and prophylaxis of vulvovaginal candidiasis
Published in Drug Development and Industrial Pharmacy, 2021
Maria M. Pashayan, Hrachya G. Hovhannisyan
Terconazole is an antifungal triazole intended for treating vaginal yeast infections. It has shorter treatment regimens, lower relapse rates, better mycologic clinical cure rates, higher efficiency, tolerability, and high safety level compared with other imidazole antifungal agents in the treatment of VVC [11,12]. The results of numerous short- and long-term evaluations confirm the efficacy of 80 mg terconazole cocoa butter base suppositories with 92.2% cure rate after three days. It has been also shown that women diagnosed with Candida spp. who perorally received single doses of terconazole (80 mg) supplemented every morning with two probiotic capsules containing Lactobacillus rhamnosus GR‐1 and Lactobacillus reuteri RC‐14 for the four weeks showed significant reduction in Candida in the vaginal discharge [13]. Many clinical studies have also found that probiotic lactobacilli augment antifungal treatment of VVC [14,15]. This finding can improve the effectiveness of treatment by antifungal pharmaceutical agents, especially when a limited number of new drugs are in the pipeline and resistant microorganisms are increasingly emerging.
Formulation and in vivo assessment of terconazole-loaded polymeric mixed micelles enriched with Cremophor EL as dual functioning mediator for augmenting physical stability and skin delivery
Published in Drug Delivery, 2018
Wessam H. Abd-Elsalam, Sally A. El-Zahaby, Abdulaziz M. Al-Mahallawi
Besides the development of efficient dosage forms of the highly potential available anti-fungal agents; the lately sudden increase in the use of antimycotic drugs resulted in the emergence of resistant strains. Hence an urgent medical need for novel antifungals has been arised. Terconazole (TCZ) is a new broad-spectrum antifungal agent that belongs to the class of triazoles and is mainly used for the treatment of vulvovaginal candidiasis. The main mechanism of action of TCZ simulates that of imidazoles through inhibition of the fungal cytochrome P-450 but it is documented to be more active than imidazoles (Cauwenbergh & Vanden, 1989). The poor permeability characters of TCZ limit its clinical use. To overwhelmed this problem, TCZ were incorporated in bilosomes (Abdelbary et al., 2016) and proniosomal gel (Abdou & Ahmed, 2016).