Anti-fungal agents/drugs

Certain APIs are administered topically, e.g., topical anti-inflammatory steroids and topical anti-fungal agents. The release of these APIs from their formulation was thought to be maximized when the solution of the drug in the vehicle is just saturated (27). However, Davis and Hadgraft (28) have shown that supersaturation can increase the penetration even further. The interaction of the moisture present in the skin with the topical formulation can be used to change the degree of saturation of the formulation and thereby enhance the release of the API from the formulation into the skin. 

Itraconazole, a widely used broad-spectrum anti-fungal agent has been used as an example (De Beule and Van Gestel, 2001 Peeters et al., 2002). As indicated in Figure 3, the compound is predicted to have extremely low water solubility but useful intestinal permeability. The parameter sensitivity analysis indicated that fraction absorbed could be substantially increased if the apparent solubility of the drug could be increased to 100 pg/mL or greater. Such manipulation is possible through the use of hydrophilic cyclodextrins such as 2-hydroxypropyl-... 

Similar oxidative metabolism was observed for premazepam, an antianxiety drug, in the rat and the dog prinomide, an anti-inflammatory agent, in six i ecies of laboratory animals" and pyrrolnitrin, an anti-fungal agent, in rats. ... 

Goodman and Gilman, 1980) and also in the anti-cancer drug, fluorouracil (Section 4.0.2) and the anti-fungal agent, flucytosine 4.23). Many such drugs are used in human medicine, but (a note of caution) the substitution of fluoro-citric acid for citric acid is disastrous (Section 13.5). 

Amphotericin B is the mainstay of treatment of patients with severe endemic fungal infections. The conventional deoxycholate formulation of the drug can be associated with substantial infusion-related adverse effects (e.g., chills, fever, nausea, rigors, and in rare cases hypotension, flushing, respiratory difficulty, and arrhythmias). Pre-medication with low doses of hydrocortisone, acetaminophen, nonsteroidal anti-inflammatory agents, and meperidine is common to reduce acute infusion-related reactions. Venous irritation associated with the drug can also lead to thrombophlebitis, hence central venous catheters are the preferred route of administration in patients receiving more than a week of therapy. 

Nonsteroidal anti-inflammatory agents are used extensively as nonprescription drugs, and residues of these compounds have been detected ubiquitously in WWTP effluents at the pg L 1 levels, and they also frequently occur at the ng L 1 level in the aquatic environment (see [2], this volume). As a result, many researchers have focused on the degradation of these pharmaceuticals, which are one of the most studied groups of therapeutic agents in terms of fungal transformation. 

Steroid creams will often clear the condition and hydrocortisone can be prescribed under a variety of trade names such as Alphaderm. More powerful are the creams based on betamethasone esters, of which Betnovate is the best known and has been used for more than 40 years. If this does not work then the doctor can prescribe even stronger drugs based on clobetasol propionate, such as Dermovate, or similar active agents. There are several such creams now available and it is rare for eczema not to respond to one of them and be cured - and kept at bay. If the eczema is infected then various antibiotics, antivirals, and anti-fungals can be given to clear up the infection. Very... 

Biodiversity New Leads for the Pharmaceutical and Agrochemical Industries reviews and discusses aspects of modern natural products research. The central theme of many articles is the sustainable use of global biodiversity. Microbial, plant and marine products are presented as the sources of new drugs, including anti-fungal products, antibiotics, anti-cancer agents and animal health products. There is also coverage of the biosynthesis of polyketides and the chemical synthesis of natural products and their derivatives. 

Among the drugs employed in the treatment of fungal infections are the anti-fungal antibiotics, such as anphotericin and nystatin, and synthetic anti-fnngal agents such as flucytosine, tolnaftate, and the azoles. 

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