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At least 73 records · Page 4Linked to original sources
PubMed1990

Levels of itraconazole in skin blister fluid after a single oral dose and during repetitive administration.

Oral itraconazole is effective in the treatment of mycoses. To measure its concentrations in the tissue, levels of total and non-protein-bound itraconazole were determined in serum, suction-induced blister fluid, and cantharides-induced blister fluid. Six healthy subjects received 200 mg as a single dose, followed by 100 mg/day for 10 days. Itraconazole binding in suction-induced blister fluid (99.54%) and cantharides-induced blister fluid (99.77%) was calculated from plasma protein binding (99.8%). The single-dose study showed the drug levels in blister fluid to increase more slowly than those in serum. The terminal half-life of itraconazole in serum was 22.5 +/- 3.2 hours. Suction- and cantharides-induced blister fluid levels declined in parallel. After the final dose, itraconazole penetration into cantharides-induced blister fluid was only 70%. Moreover, trough levels of unbound itraconazole in suction- and cantharides-induced blister fluid were 0.239 +/- 0.115 and 0.334 +/- 0.101 ng/ml and thus were significantly lower than free itraconazole levels in serum (0.422 +/- 0.125 ng/ml). Thus a distribution equilibrium between serum and blister fluids was not obtained. Free drug concentrations in suction- and cantharides-induced blister fluid were far lower than the minimal inhibitory concentration values for Candida ssp. and dermatophytes.

Administration, Oral↗
PubMed1989

Medical uses of mylabris in ancient China and recent studies.

Mylabris is the dried body of the Chinese blister beetle. The species used in medicine are Mylabris phalerata and M. cichorii. The use of mylabris as a traditional medicine in China can be traced back more than 2000 years, and it is still used as a folk medicine today. In recent studies, it has been found that mylabris possesses antitumor properties, increases the number of leucocytes, and has irritant effects on the urinary organs. The active constituent of mylabris is cantharidin. The synthesis of cantharidin is rather difficult. In order to find a less toxic analogue of cantharidin, its hydrolytic compound, disodium cantharidate, and its demethylated form, norcantharidin, were prepared. By biochemical and biological methods, it was found that these compounds may affect cancer cells in several ways. In clinical studies, antihepatoma effectiveness sequentially increased from cantharidin to disodium cantharidate to norcantharidin. Disodium cantharidate showed less urinary irritation than cantharidin while norcantharidin showed little to no such irritation. It appears that the two methyl groups of cantharidin are not the main functional groups for antitumor activity and for the stimulation of bone marrow but are associated with urinary irritation. Hydrocantharidimide, methylcantharidimide and dehydronorcantharidin have also been studied. All these compounds, except the last one, have been produced as antitumor agents in China. Since demethylated cantharidin may be prepared by total synthesis, it may be more suitable for medical investigation than cantharidin itself.

Animals↗
PubMed1999

Doxorubicin-resistant LoVo adenocarcinoma cells display resistance to apoptosis induction by some but not all inhibitors of ser/thr phosphatases 1 and 2A.

LoVo adenocarcinoma cells are fairly sensitive to cytostatic drugs, e.g. doxorubicin, but can develop drug resistance by expression of a P-glycoprotein-mediated MDR1 phenotype. LoVo cells respond with apoptosis to nanomolar concentrations of okadaic acid and micromolar concentrations of cantharidic acid. Interestingly, LoVoDx cells which had become about 10-fold less sensitive to doxorubicin by incubation in increasing concentrations of this cytostatic drug were also less sensitive to the toxicity of okadaic acid. Resistance to both agents was lost or significantly reduced by incubation in drug-free medium for about 4 months. On the other hand, LoVoDx cells did not lose responsiveness to the structurally different phosphatase inhibitor cantharidic acid but were about twofold more sensitive to the cytotoxic effect of this agent. Thus, MDR expression protects LoVo cells from the toxicity of phosphatase inhibitors that presumably are substrates of the P-glycoprotein, e.g. okadaic acid and its derivatives but not cantharidic acid, despite the fact that both agents are potent inducers of apoptotic cell death via ser/thr phosphatase inhibition.

ATP Binding Cassette Transporter, Subfamily B, Mem↗