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Biomedical subjects

B Catanese

Publications and source records attributed to B Catanese.

At least 19 recordsLinked to original sources
PubMed1992

A new protein antidenaturant agent, bindarit, reduces secondary phase of adjuvant arthritis in rats.

Bindarit (or 2-[(1-benzyl-indazol-3-yl)methoxy]-2-methyl propionic acid) reduces heat induced denaturation of bovine and rat serum albumin in vitro (EC50 = 8.5 and 65 micrograms/ml, respectively) and inhibits heat induced serum albumin denaturation after in vivo (12.5-25-50 mg/kg po) administration in rats. To assess the relationship between protein denaturation and the development of chronic inflammatory diseases, the drug (0.5 or 0.12% medicated diet) was studied in comparison with indomethacin (1 mg/kg po daily) in rats injected with complete Freund's adjuvant. Bindarit appeared different from aspirin-like drugs, antiinflammatory steroids and immunosuppressants because it does not reduce primary inflammation of arthritic rats and was shown to be completely inactive on cyclo and lipooxygenase activity in vitro and on immune reactions of mice in vivo. Nevertheless, the drug strongly reduced the development of the secondary phase of adjuvant induced arthritis. The most significant effect of bindarit in this phase was a strong inhibition of serum albumin denaturation in arthritic rats. Assessment of both electrophoretic and quantitative changes suggests that the reduction of albumin during inflammation is due, at least in part, to a denaturation of native albumin, which loses its electrophoretic mobility. The involvement of protein denaturation in the production of new antigenic determinants, their pathogenic relevance in the development of adjuvant arthritis and the possibility that protein stabilization by bindarit could be the mechanism of action of the drug are discussed.

Animals↗
PubMed1992

Validation of a HPLC method for the determination of bendazac and its main metabolite 5-hydroxybendazac in human plasma.

The purpose of this study was to validate an analytical method for the determination of bendazac and its main metabolite 5-hydroxybendazac in human plasma. The results obtained indicate that the method is reproducible, accurate, precise, sensitive and specific for the measurement of bendazac and 5-hydroxybendazac in the human plasma. Therefore it can be considered suitable for experimental purposes, routine application for drug monitoring and regulatory requirements.

Chromatography, High Pressure Liquid↗
PubMed1991

Pharmacokinetics of benzydamine after intravenous, oral, and topical doses to human subjects.

The pharmacokinetics of the anti-inflammatory drug benzydamine were determined after intravenous infusion of 5 mg to six healthy male subjects. Benzydamine was characterized as a drug of relatively low systemic clearance (ca. 160 ml min-1) but high volume of distribution (ca. 1101); the apparent terminal half-life in plasma was ca. 8 h. Benzydamine was well absorbed after oral administration, as indicated by a mean systemic availability of 87 per cent. However, absorption of the drug was low (less than 10 per cent of the dose) after its use by male subjects as a mouthwash, or after its application to female subjects as dermal cream and vaginal douche preparations. The data suggest that benzydamine is generally not well absorbed through the skin and non-specialized mucosae, thereby limiting unrequired systemic exposure to this drug when it is used by these routes.

Administration, Cutaneous↗
PubMed1991

Validation of a HPLC method for the determination of bendazac and its main metabolite 5-hydroxybendazac in rabbit aqueous humor and its applicability to human aqueous.

The purpose of this study was to validate an analytical method for the determination of bendazac and its main metabolite 5-hydroxybendazac in aqueous humor. The method was validated with rabbit aqueous but it can be used also for human aqueous since no differences between the two matrices were observed. The results obtained indicate that the method is reproducible, accurate, precise, sensitive and specific for the measurement of bendazac and 5-hydroxybendazac in the aqueous humor. Therefore it can be considered suitable for experimental purposes, drug monitoring and adequate for regulatory requirements.

Animals↗
PubMed1991

The pharmacokinetics of oral lonidamine in breast and lung cancer patients.

The plasma levels of lonidamine have been studied in 24 breast or lung cancer patients as part of the Phase II evaluation of the drug. The pharmacokinetic studies were performed when the patients had been on oral lonidamine therapy for 27 to 47 days (mean 32 days) and the studies were conducted over a 24 hour period. Lonidamine was administered in three divided doses of 150 mg (t = 0h), 150 mg (t = 7h), and 150 mg or 300 mg (t = 14h). Plasma levels of lonidamine were determined by high-performance liquid chromatography (HPLC) with fluorescence detection. Lonidamine was detected in the plasma of all patients studied, and the absolute range for the peak plasma levels of the drug following the first and second doses were 4.6-33.8 and 4.8-33.3 micrograms/ml, respectively. The range of times after administration at which the peak occurred was 0.5 to 4.2 hours for the first dose and 0.5 to 4.1 hours for the second. The absolute range for the trough levels observed over the 24-hour study period was 1.0 to 12.6 micrograms/ml and in 19 of the patients it was possible to define the apparent half life of lonidamine that was found to be within the range 2.5 to 11.7 hours. In addition to lonidamine, a number of fluorescent components were detected in the plasma of patients following lonidamine treatment that were not detected in pretreatment plasma samples. One component, a compound that eluted from the HPLC more rapidly than lonidamine, was found in some patients to be sensitive to hydrolysis with beta-glucuronidase. Comparison of the pharmacokinetic data with patient characteristics and clinical biochemistry results failed to establish any clear relationship. Similarly there was no relationship between lonidamine pharmacokinetics and either drug-induced myalgia or testicular pain. Insufficient responses were seen in the patient group studied to allow the relationship between lonidamine pharmacokinetics and response to be evaluated.

Absorption↗
PubMed1989

Time-course of aspirin and salicylate in ocular tissues of rabbits.

The time courses of aspirin and salicylate in plasma and ocular tissues of rabbits were investigated after the i.v. administration of aspirin. Unhydrolyzed aspirin rapidly disappears from plasma and many ocular compartments but persists up to 4 hours in aqueous and vitreous humours. Salicylate decreases in plasma follow an exponential kinetics; in aqueous humour and in vascularized tissues the behaviour is similar but with a half-life longer than in plasma. In the cornea, lens and vitreous humour, the concentration of salicylate reaches a peak between 2 and 4 hours, then it decreases very slowly. Our results show that aspirin is protected from the hydrolytic action of plasmatic esterases in aqueous and vitreous humours but is rapidly hydrolyzed in the cornea and lens by local esterases present in these tissues. It is possible that both aspirin and salicylate leave the eye by means of an active transport. Our results also indicate that salicylate can accumulate in the cornea, lens and retina when aspirin is administered repeatedly.

Animals↗
PubMed1987

Absorption of bendazac lysine after topical application to the rabbit eye.

A water solution of 0.5% 14C-3-bendazac lysine was administered to the rabbit eye. Following single application to the cornea, the drug was found in different ocular compartments including the lens. Although in the lens the concentrations are lower as compared to the iris, retina ciliary bodies and aqueous humor, they last longer.

Absorption↗
PubMed1987

Pharmacokinetics of benzydamine.

Benzydamine is a non-steroidal anti-inflammatory drug especially used topically for the treatment of primary or normoreactive types of inflammation. The pharmacokinetics of benzydamine are reported after both topical and systemic administration, and the available data are reviewed with particular reference to its topical use.

Absorption↗
PubMed1986

Ocular pharmacokinetics of dapiprazole.

Dapiprazole is a drug having specific alpha 1 adrenergic blocking properties. Following topical instillation on the eye, it crosses the corneal epithelium reaching high concentrations in the ocular tissue and producing a prompt miotic and hypotensive effect. The high concentration ratio between ciliary bodies and iris versus aqueous humor suggests a peculiar affinity for these structures containing adrenoceptors of the alpha type. The very low concentrations in the plasma, as compared to those after systemic administration, and in the fellow eye indicate that the systemic absorption is negligible.

Administration, Topical↗
PubMed1986

HPLC determination of benzydamine and its metabolite N-oxide in plasma following oral administration or topical application in man, using fluorimetric detection.

A method for the extraction and quantification of benzydamine and its metabolite N-oxide by liquid chromatography with fluorescence detection in plasma samples is described. This method has adequate sensitivity, specificity and is reproducible. The use of the extraction column allowed a recovery of both benzydamine and its metabolite of over 97% to be obtained. The plasma levels of benzydamine and its metabolite N-oxide were studied after oral administration as sugar-coated tablets or topical application to the vaginal mucosa as a cream to 6 healthy volunteers. After topical application, the plasma concentrations of the unchanged drug and its metabolite are lower than those obtained following oral administration. These data further stress the concept that, whenever possible, topical use should be considered the treatment of choice since, along with a more selective therapy, the incidence of systemic side effects can be considerably reduced.

Administration, Oral↗
PubMed1985

Effect of benzydamine on exocytosis and respiratory burst in human neutrophils and mononuclear phagocytes.

The effect of benzydamine on stimulus-dependent respiratory burst activity and enzyme release was tested in human neutrophils, monocytes and monocyte-derived macrophages. Established anti-inflammatory compounds, indomethacin, phenylbutazone and bufexamac, were tested for comparison. Care was taken to avoid cytotoxic or cytolytic concentrations of the test compounds, and their effect on release of lactate dehydrogenase was also tested. Release of specific and azurophil granules contents were induced in human neutrophils by A23187, PMA and fMLP with and without cytochalasin B pretreatment. Benzydamine inhibited stimulus-dependent release of vitamin B12-binding proteins, a marker for the specific granules, in a concentration-dependent fashion. By contrast, phenylbutazone and bufexamac were practically inactive. The effect of benzydamine on exocytosis of azurophil granules was tested in cytochalasin B-pretreated neutrophils. Benzydamine, again in contrast to the two reference anti-inflammatory compounds, inhibited release concentration-dependently also under these conditions. The concentration of the compound which inhibited exocytosis by 50% was 30-100 microM in normal and 3-10 microM in cytochalasin B-treated neutrophils. The effect of benzydamine and reference compounds on the respiratory burst was tested by assaying for superoxide formation in neutrophils and H2O2 formation in mononuclear phagocytes. Benzydamine was inactive on neutrophils and inhibited slightly the burst response of monocytes and macrophages. Two reference compounds, bufexamac and phenylbutazone, were generally more active. The strongest inhibitory effect was that of phenylbutazone on fMLP-stimulated cells. Benzydamine lacked activity under these conditions, indicating that it does not bind to the receptor of formylated chemotactic peptides.(ABSTRACT TRUNCATED AT 250 WORDS)

Benzydamine↗
PubMed1985

Distribution and excretion of 3H-dapiprazole in the rat.

Tissue distribution as well as biliary, urinary and fecal excretion of 3H-dapiprazole was studied in the rat. The product is found in many tissues, including the brain. About 23 and 57% of the dose is excreted in the urine and feces and about 65% is eliminated in the bile.

Animals↗
PubMed1985

Tissue distribution, urinary, fecal and biliary excretion of 14C bendazac L-lysine salt in rats.

The distribution of bendazac in the plasma and some rat tissues was studied after single oral administration of 14C bendazac L-lysine salt. The drug is distributed in varying amounts in the liver, kidneys, spleen, muscle, plasma and lens. In these tissues, the drug kinetics is similar, except for the lens where elimination of the drug is slower. More than 80% of the radioactivity administered is excreted through the urine and feces. Fecal excretion is due to the high biliary excretion.

Animals↗
PubMed1985

Pharmacokinetics of benzydamine.

Clinically, benzydamine can exert its action locally or systemically. Consequently the pharmacokinetics of this drug have been studied after its administration by several different routes. Oral doses of benzydamine are apparently well absorbed and plasma drug concentrations reach a peak fairly rapidly (e.g. 0.8 micrograms/ml after a 100-mg dose) and then decline with a half-life of about 13 h. Less than 20% of the drug is bound to plasma proteins. Assuming complete oral systemic availability, values of 193 ml/min and 213 litres respectively were calculated for the systemic clearance and volume of distribution of benzydamine. Cutaneous doses of benzydamine are more slowly absorbed and lead to peak drug levels about three-fold lower, but more persistent than those after oral administration. Although local drug concentrations are relatively large, the systemic absorption of mouthwash-gargle, vaginal and rectal doses of benzydamine is relatively low compared to oral doses: this lower absorption should greatly diminish the potential for any systemic drug side-effects when benzydamine is administered by these routes. Benzydamine is metabolized primarily by oxidation, conjugation and dealkylation.

Absorption↗
PubMed1984

Pharmacokinetics of Lonidamine after oral administration in cancer patients.

The pharmacokinetics of Lonidamine has been studied in cancer patients after single and chronic oral administrations. After single administration the plasma kinetics are highly variable, while the dose eliminated in the urine is over 70% in all subjects. This suggests an active but interindividually variable first-pass effect. After repeated administrations, both the residual plasma concentration before administration (C infinity min) and that obtained after drug intake (C infinity max) have been studied. The C infinity max values range from 4.5 to 25 micrograms/ml and C infinity min values from 0.4 to 7 micrograms/ml. In patients where a therapeutic response was noted, a mean value of 2.98 micrograms/ml for C infinity min was measured. In patients unresponsive to drug therapy the mean C infinity min was 1.5 micrograms/ml.

Absorption↗