Antimycotic effects

The main advantage of this ointment is its low price. This combination has now been replaced by more active modern antimycotics. Long ago, the antimycotic effect of aUphatic carboxyUc acids with an increasing number of C-atoms was discovered. The optimum is 11 C-atoms and CH2=CH(CH2)gCOOH, undecylenic acid [112-38-9] C22H2QO2, is used in several ointments. 

Cleary, K. and McFeeters R.F., Effects of oxygen and turmeric on the formation of oxidative aldehydes in fresh-pack dill pickles, J. Agric. Food Chem., 54, 3421, 2006. Lean, L.P. and Mohamed S., Antioxidative and antimycotic effects of turmeric, lemon-grass, betel leaves, clove, black pepper leaves and Garcinia atriviridis on butter cakes, J. Sci. Food Agric., 79, 1817, 1999. 

Azzouz, M.A. and Bullerman, L.B. 1982. Comparative antimycotic effects of selected herbs, spices, plant components and commercial antifungal agents. J. Food Protection. 45 1298-1301. 

Flucytosine (5-FC) is an analogue of the natural pyrimidine cytosine that is converted to 5-fluorouracil (5-FU) in susceptible fungi. Formation of 5-FU is essential to the antimycotic effect of 5-FC 5-FU acts as a pyrimidine antimetabolite and is phosphorylated to the cytotoxic agent 5-fluorodeoxyuridine monophosphate. All of these facts are commonly emphasized in a medicinal chemistry sequence, and readers probably are aware that 5-FU is a chemotherapeutic agent that causes myelosuppression as its major toxicity. Therefore, it should not be surprising that the same side effect can be seen in patients receiving 5-FC. 

The observation that a patient had an allergic reaction to hydroxyquinoline in ointments with a paiafQn base, but not a zinc oxide base, prompted further study of a possible incompatibility. The subsequent study in 13 patients confirmed that zinc oxide reduces the eczematogenic (allergic) properties of the hydroxyquinoline. However, it also inhibits its antibacterial and antimycotic effects, and appears to stimulate the growth of Candida albicans. ... 

The antimycotic effect of straight chain carboxylic acids has long been known. In particular the unsaturated acids, for example crotonic acid and its homologues, are very active. Sorbic acid (2-trans, 4-trans-hexadienoic acid pK = 4.76) has the advantage that it is odorless and tasteless at the levels of use (0.3% or less). The acid is obtained by several syntheses ... 

Older Compounds. Some antimycotics have been used for a long time Whitfield s ointment is a typical example (1907). The ointment usually contains 6% ben2oic acid [65-85-0] and 3% sahcyhc acid [69-72-7] C H O. The action is attributed to the keratolytic effect of the sahcyhc acid... 

Because of their limited, activity, small spectmm, and side effects, the older topical antimycotics have generally been surpassed by newer antimycotic chemotherapeutic agents. These newer antimycotics for topical use iaclude the imida2ole derivatives clotrimazole, miconazole, econazole, isoconazole, sulconazole, fenticonazole, oxiconazole, bifonazole, butoconazole, ziaoconazole, tioconazole, and the triazole derivative, terconazole (Table 2) (5—7). The iatroduction of the azole derivatives represents a milestone ia the treatment of mycoses. 

With the aid of cytosine permease, flucytosine reaches the fungal cell where it is converted by cytosine deaminase into 5-fluorouracil [51-21-8]. Cytosine deaminase is not present in the host, which explains the low toxicity of 5-FC. 5-Fluorouracil is then phosphorylated and incorporated into RNA and may also be converted into 5-fluorodeoxyuridine monophosphate, which is a potent and specific inhibitor of thymidylate synthetase. As a result, no more thymidine nucleotides are formed, which in turn leads to a disturbance of the DNA-synthesis. These effects produce an inhibition of the protein synthesis and cell repHcation (1,23,24). 5-Fluorouracil caimot be used as an antimycotic. It is poorly absorbed by the fungus to begin with and is also toxic for mammalian cells. 

Some of the N-alkylated narceine amides and imides were tested for antibacterial effectiveness and showed activity of medium potency against Mycobacterium tuberculosis H37 Rv. Their antimycotic activity was also of medium strength. Coccidiostatic screening showed some effectiveness (100). 

Triazolylcyclopropane derivatives are endowed with antimycotic properties [125]. They are also prepared as plant growth regulators and fungicides for instance 93 (R = unsubstituted and substituted aryl, heteroaryl) markedly inhibited the growth of rice, cotton and soybeans in hot tests [126]. l-(l,2,4-Triazolyl)-2-(2,4-dichlorophenyl)cyclopropane 94, is a more effective fungicide against Podosphaera leucotricha and a better growth retardant in rice and soybeans than the (l,2,4-triazolyl)pentenone 95, Eq. (36) [127]. 

Olkkola KT, Ahonen J, Neuvonen PJ. The effect of systemic antimycotics, itraconazole and fluconazole, on the pharmacokinetics and pharmacodynamics of intravenous and oral midazolam. Anesth Analg 1996 82 511-516. 

Management For intertrigo, local antimycotic therapy has to be combined with drying of this region (e.g. linen strips, use of an antimycotic paste), local therapy with potassium permanganate deals with this aspect and is effective against concomitant bacteria as well. In the treatment of diaper candidiasis these points of view are important as well (e.g. frequent changes of napkins) steroids should be avoided if possible. 

Niphimycin, an antimycotic antibiotic derived from Actinomyces hygroscopicus, is effective against both der-matomycosis and onychomycosis, with a 16-26% success rate in the latter. Tolerance is reportedly good, but there is a notable lack of recent data (SEDA-12, 236). 

Ibrahim SA, Hafez E, El-Shanawany SM, et al. Eormulation and evaluation of some topical antimycotics. Part 3. Effect of promoters on the in vitro and in vivo efficacy of clotrimazole ointment. Bull Pharm Sci Assiut XJniv 1991 14(1-2) 82-94. Swafford SK, Bergmann WR, Migliorese KG, et al. Characterization of swollen micelles containing linoleic acid in a microemulsion system. / Soc Cosmet Chem 1991 42 235-247. 

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