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At least 19 recordsLinked to original sources
PubMed1982

Does cantharides blister fluid provide access to the peripheral compartment?

The pharmacokinetics of bendroflumethiazide (BFT) was investigated following the oral administration of 10 mg to 3 healthy volunteers. Each subject participated twice in the study. BFT was determined in plasma and cantharides blister fluid from 1/2 to 30 h post administration. Blister fluid was obtained from blisters 10-22 h old. Plasma levels were fitted to a tri-exponential equation and the concentration of the drug in the peripheral compartment was calculated from the microscopic rate constants. In 5 of 6 cases investigated, cantharides blister fluid levels paralleled the concentration of the drug in the peripheral compartment. The mean blister fluid levels exceeded the calculated concentration in Compartment 2 1.46 fold. In one case, the blister fluid level paralleled the plasma level. This subject clearly differed from the others as more than 10 h were required for blister formation in her. The results suggest that following the administration of BFT, cantharides blister fluid behaves as part of the peripheral compartment. The possible value of studying blister fluid levels in pharmacokinetic investigations is discussed.

Adult↗
PubMed1988

Cantharide acantholysis: endogenous protease activation leading to desmosomal plaque dissolution.

Using a method which allowed us to study the morphological consequences of the expression and the inhibition of proteases in living tissues, we demonstrated that the primary detectable cellular event in cantharide acantholysis is the dissolution of the dense plaque, leading to the detachment of tonofilaments from desmosomes. This process is inhibited by neutral serine protease inhibitors. This suggests that the desmosome-tonofilament complex, more precisely the desmosomal dense plaque, is the primary target of activated proteases during cantharide acantholysis, and can be disrupted by a specific epidermal protease-anti protease system. Cantharide acantholysis may be useful model for studying desmosomal turnover.

Acantholysis↗
PubMed1987

Comparison of the acute toxicity of endothal and cantharidic acid on mouse liver in vivo.

Endothal and cantharidic acid were administered intraperitoneally to mice at 75 and 10 mg/kg, respectively, to compare their acute toxicity on liver tissue in vivo. Within 45 min both treatments caused extreme liver enlargement and congestion. Hepatic glycogenolysis was increased as evidenced by elevations in blood glucose and hepatic glycogen phosphorylase levels and by corresponding reductions in hepatic glycogen content and glycogen synthase activity. Endothal decreased hepatic ATP concentrations, although neither compound altered mitochondrial Mg2+-ATPase activity. Microsomal Mg2+-ATPase levels, however, were reduced by both treatments. There were no indications that reactive intermediates were involved in the toxicity of either compound. The results show that endothal and cantharidic acid act directly and cause similar biochemical changes in mouse liver in vivo.

Animals↗
PubMed1998

Direct assessment of peripheral pharmacokinetics in humans: comparison between cantharides blister fluid sampling, in vivo microdialysis and saliva sampling.

AIMS: Skin blister fluid sampling, in vivo microdialysis and saliva sampling are commonly employed as surrogates for the measurement of drug concentrations in peripheral compartments. Although expected to exhibit comparable results, data derived from these techniques have never been directly compared. Thus, the aim of the present study was to evaluate the comparability of these techniques. METHODS: Paracetamol, a model drug with low protein binding, was administered to seven healthy volunteers at an oral dose of 2000 mg. Subsequently, tissue kinetics were measured simultaneously in cantharides induced skin blisters, microdialysates of subcutaneous- and skeletal muscle-tissue and saliva and compared to serum concentrations. RESULTS: Mean ratio (AUCblister/AUCserum) was 0.88 (95% CI, 0.50-1.26), mean ratio (AUCmuscle/AUCserum) was 1.08 (0.67-1.49), mean ratio (AUCsubcutaneous/AUCserum) was 0.96 (0.41-1.51) and mean ratio (AUCsaliva/AUCserum) was 1.83 (1.39-2.27). In this study the concentration profiles after single oral administration differed among the three methods. The time course of the concentration (peripheral compartment)/concentration (serum)-ratios showed that cantharides blister and microdialysate concentrations closely paralleled serum levels. An equilibration period of less than 2 h had to be taken into account for blister measurements. In contrast, saliva concentrations were significantly higher than corresponding serum concentrations. CONCLUSIONS: Skin blister sampling and microdialysis closely mirrored corresponding serum concentrations and, thus, proved to be suitable techniques for the assessment of peripheral compartment pharmacokinetics. In contrast, saliva data overestimated the corresponding serum concentrations.

Acetaminophen↗
PubMed1992

Correlations between theophylline concentrations in plasma, erythrocytes and cantharides-induced blister fluid and peak expiratory flow in asthma patients.

Theophylline levels in plasma, erythrocytes and cantharides-induced blister fluid (BF) have been correlated with peak expiratory flow (PEF) in asthmatic patients. Nine asthmatic men received an IV infusion of 240 mg theophylline at a constant rate for 30 min. The theophylline concentrations in erythrocytes and blister fluid were 37% and 78% of those in plasma. There was not a strong correlation between erythrocyte or blister fluid penetration and the clinical effect of theophylline.

Asthma↗
PubMed1987

Digoxin concentrations in serum and cantharides blister fluid: correlations with cardiac response.

The relationship between the pharmacokinetics and dynamics of digoxin was investigated using a skin blistering technique that allows experimental access to tissue fluid concentrations. Eight healthy volunteers received digoxin, 1.0 mg, and placebo intravenously according to a double-blind crossover design. Drug concentrations were determined during a 72-hour period in serum, urine, and cantharides blister fluid (CBF). Digoxin levels in the hypothetic peripheral compartments were calculated from serum concentrations. Digoxin effects (total electromechanical systole [QS2c], left ventricular ejection time [LVETc], preejection period [PEPc], QTc time, heart rate, and T wave amplitude) were measured simultaneously. Peak levels in the shallow and deep compartments occurred at 12 1/2 to 20 minutes and 3 hours and the maximum concentration in CBF (2.75 +/- 0.48 ng/ml) occurred at 1 hour. Digoxin effects on QS2c, PEPc, and the ratio PEP/LVET were not related to serum concentrations but were closely related to CBF concentrations (r = 0.90). CBF concentrations were then within the range of serum digoxin concentrations usually associated with the treatment of heart failure. Thus, CBF allows experimental access to active drug concentrations after a single intravenous dose.

Adult↗
PubMed1986

Bactericidal activity of cefotiam and ceftizoxime against Neisseria gonorrhoeae in an in vitro model simulating plasma and cantharidal blister fluid levels after the single intramuscular application of one gram.

Two gonococcal strains with differing susceptibility to cefotiam and ceftizoxime, as expressed by the minimum inhibitory concentration (MIC), are exposed to continuously changing concentrations of these antibiotics as they are found in plasma and skin cantharidal blister fluid (CBF) after a single intramuscular application of 1 g. Under the conditions of the plasma level profiles, bacterial density is always greatly but not totally reduced, already during the first 1-1.5 h it declines by 99%. The effect is the more marked the quicker and higher the levels increase. In this respect, facing the less favorable CBF level profiles, a 99% reduction of gonococci takes much longer. While the degree of bacterial susceptibility plays no major role as long as the MIC is highly exceeded, as during invasion, it becomes important when the actual levels come more or less close to the MIC. Then the decline of bacterial density can slow down and even the maximum relative reduction can be affected. Under the condition of equivalent in vitro activity, the superior plasma kinetics of cefotiam leads to better antimicrobial activity, an effect no longer found facing similar CBF kinetics. This demonstrates the need for the inclusion of tissue level data, in so far as infection sites other than blood are simulated. The high degree of antigonococcal activity of the drug concentration time curves for plasma and CBF after cefotiam and ceftizoxime (1 g) allow the expected high cure rates in uncomplicated gonorrhoea.

Blister↗
PubMed1990

Post-mortem serum concentration of cantharidin in a fatal case of cantharides poisoning.

A patient admitted to hospital died shortly after admission without a proper diagnosis having been made. Symptoms as well as the presence of a brown powder found in the possession of the deceased indicated the possibility of cantharidin intoxication. Cantharidin was positively identified by means of a GC/MS analysis, utilizing the selected ion monitoring technique (SIM), for m/z = 197.0813, (M + H+) for cantharidin, under positive chemical ionization conditions at a resolution of 7000 and a mass window of 30 ppm. Quantitation was done by means of a GC/MS SIM analysis of a toluene extract of acidified post-mortem serum under El+ conditions at a resolution of 3000, using clofibrate as internal standard and monitoring m/z = 128.0473 and 128.0029 for cantharidin and clofibrate respectively. The post-mortem serum was found to contain cantharidin at a concentration of 72.3 ng/ml whilst the cantharides powder contained 0.87% cantharidin.

Adult↗
PubMed1990

A fatality due to the use of cantharides from Mylabris phalerata as an abortifacient.

A fatal case of attempting to procure abortion by the ingestion of the crude extract of cantharides from over 200 dried Mylabris phalerata is presented. The quantification of catharidin in blood, urine and liver by gas chromatography using trichloroacetic acid in the extraction process and butobarbitone as the internal standard is described. Ante- and post-mortem blood levels were found to be 0.27 and 0.11 micrograms/ml respectively. To conclude, the lack of legislative control in Hong Kong over Chinese herbal medicines is highlighted.

Abortion, Induced↗
PubMed1984

Plasma, cantharides blister fluid, and suction blister fluid levels of ceftizoxime after single intramuscular application for gonorrhea.

Following a single intramuscular application of 1 g ceftizoxime, levels of the drug were determined in plasma as well as in suction blister fluid (SBF) and cantharides blister fluid (CBF). This regimen invariably led to both high and long-lasting plasma levels: 81 +/- 16 min post dose maximum plasma levels of 17.5 +/- 3.1 micrograms/ml were reached; 6 h post dose levels of 4.6 +/- 0.4 micrograms/ml were still found, i.e., 4375 and 1150 times, respectively, the MIC90% of Neisseria gonorrhoeae. The high plasma levels were parallelled by high concentrations in SBF, with peaks amounting to 8.4 +/- 1.0 micrograms/ml. Peak concentrations in CBF ranged from 8.1 to 15.7 micrograms/ml. Thus, the pharmacokinetic behavior of ceftizoxime given as a single intramuscular injection of 1 g explained the excellent clinical results of this regimen in uncomplicated gonorrhea.

Adult↗
PubMed1995

[Therapy of cantharides extract for perennial allergic rhinitis and its effect on total IgE in serum].

The therapy of 10% Cantharides extract in treating 50 cases of perennial allergic rhinitis (PAR) was studied. The extract was plastered and blistered on Dazhui, Neiguan point. It was observed by nasal mucosa provocative test, cells in nasal secretion test and serum total IgE test. The results showed that its effective rate was 88%, the allergic nasal mucosa provocative test of treated group alleviated obviously after the treatment (P < 0.01), the number of eosinophil and basophil in nasal secretion decreased (P < 0.01, P < 0.05); and the serum total IgE also reduced significantly (P < 0.01).

Acupuncture Points↗