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Biomedical subjects

F Jané

Publications and source records attributed to F Jané.

At least 55 records · Page 3Linked to original sources
PubMed1989

Bioavailability study of fosfosal and codeine administered alone or in combination.

Fosfosal (2-phosphonoxybenzoic acid) is a new salicylic acid derivative which is used for treating inflammatory disease as well as in analgesic therapy. On the other hand, codeine together with acetylsalicylic acid is widely used in patients who require analgesic treatment for mild to moderate pain. The present study was carried out in ten healthy subjects to assess the pharmacokinetic profiles of single oral doses of fosfosal (1,200 mg) and codeine (30 mg) when administered alone or in combination. Blood samples were drawn on each study day and salicylic acid and codeine plasma concentrations were determined by HPLC and enzyme immunoassay methods, respectively. Individual pharmacokinetic parameters were calculated according to standard procedures and the magnitude and rate of bioavailability were tested using a 95% confidence internal approach. Results indicated no statistical differences in any of the kinetic parameters studied except for tmax values which were higher for fosfosal combined with codeine (2 +/- 0.39 h) when compared to fosfosal alone (1.55 +/- 0.35 h). Regarding codeine compared in combination with fosfosal, no significant differences were observed in Cmax and AUC values, while tmax showed a higher value for the combination (1.75 +/- 0.6 vs 0.85 +/- 0.32 h). Although statistical differences in the elimination constant rate and MRT were found between both codeine administrations, these cannot be considered significant in clinical terms. The changes in bioavailability rate observed for both drugs when administered together provide support for the use of this combination in a single formulation.

Adult↗
PubMed1988

Comparison between apomorphine and amphetamine-induced rotational behaviour in rats with a unilateral nigrostriatal pathway lesion.

Apomorphine and amphetamine-induced rotational behaviour in 310 rats with a unilateral 6-OHDA nigrostriatal pathway lesion has been studied. Animals presenting an apomorphine-induced contralateral rotation with a "two-peak" pattern, showed a greater number of contralateral turns induced by apomorphine and fewer ipsilateral turns induced by amphetamine than rats without this pattern. In addition, we have not found any correlation between apomorphine and amphetamine-induced turning behaviour.

Amphetamine↗
PubMed1988

Lack of correlation between lithium pharmacokinetic parameters obtained from plasma and saliva.

One tablet containing 755 mg of lithium tryptophanate (10.8 mEq of lithium) was administered to eight healthy volunteers. The main pharmacokinetic parameters for the group of subjects were estimated. Pharmacokinetic parameters (mean +/- SD) from plasma and saliva were respectively: half life (t1/2) 17 +/- 6 vs. 21.8 +/- 14 h; mean residence time 23.7 +/- 7.4 vs. 24.4 +/- 15.3 h; total clearance 30.6 +/- 9.3 vs. 28.6 +/- 6.2 ml/h/kg; and apparent volume of distribution 0.71 +/- 0.20 vs. 0.84 +/- 0.37 L/kg. Although the mean pharmacokinetic parameters in plasma and saliva were similar, there was no significant correlation between the calculated parameters in the individual subject (p greater than 0.05). The usefulness of monitoring salivary levels of lithium is questionable.

Adult↗
PubMed1988

Lack of antihistamine properties of single dose cinnarizine in man.

A simple way to study a histamine antagonist in man is to observe the effect it has on the magnitude of the skin reaction to intradermal histamine. The aim of the present study was to evaluate the antihistamine activity of single oral doses of 75 mg cinnarizine using 75 mg diphenhydramine as control, both being compared to placebo. The study was performed with two groups of 5 healthy subjects, each group receiving one of the active treatments or placebo randomly under blind conditions. All subjects received intradermal injections on the forearm of a 0.05 ml saline solution containing 5 micrograms of histamine before and at different times after drug intake. The histamine-induced wheal area was measured and, after drug administration, the percent decrease of the wheal area was calculated. Results showed that diphenhydramine produced a significant inhibition of the histamine-induced wheal size at 1.5 h which lasted up to 4 h after drug administration, reaching maximum inhibition at 2.5 h. After cinnarizine treatment no significant decrease of the histamine-induced wheal area was observed at any time.

Adult↗
PubMed1988

UV-induced erythema model: a tool in dermatopharmacology for testing the topical activity of non-steroidal anti-inflammatory agents in man.

UV-induced erythema is a well known inflammatory model applied both in animal and human skin to test the activity of topical non-steroidal anti-inflammatory compounds in a great variety of pharmaceutical formulations. The aim of this study was to evaluate the inhibitory efficacy of piroxicam in two different topical formulations (cream 0.5, 1 and 1.5% and gel 1%) as compared to three non-steroidal compounds, benzydamine, etofenamate and indomethacin (cream 5%), on erythema induced after UV-injury on the back of 5 healthy subjects. The results showed that piroxicam in cream formulation, indomethacin cream and etofenamate gel have a similar effect, decreasing the erythema size 7 h after irradiation. However, benzydamine cream and piroxicam gel showed no effect with this method. We may conclude that this model is adequate and precise for selecting the most appropriate galenic dosage form for an active compound in terms of its clinical efficacy when topically administered.

Administration, Topical↗
PubMed1987

Influence of renal function on the pharmacokinetics of ramipril (HOE 498).

The pharmacokinetics of ramipril (HOE 498) were studied after oral administration of a single 10 mg dose to 24 hypertensive patients with different degrees of renal function. The creatinine clearance ranged between 4.1 and 126 ml/min/1.73 m2 and was below 35 ml/min/1.73 m2 in 16 patients. Angiotensin converting enzyme activity and the concentrations of ramipril and its active diacid metabolite ramiprilat were measured in plasma up to 10 days after drug intake. Urine levels of ramipril, ramiprilat, their glucuronides and 2 major metabolites (a diketopiperazine and a diketopiperazine acid) were measured up to 4 days after medication. The plasma concentration-time curve of ramiprilat was polyphasic with an initial steep decline after the peak level and a subsequent very long terminal phase at low concentrations. Impaired renal function resulted in higher peak levels of ramiprilat, longer times to peak and a markedly slower decline of plasma ramiprilat levels. Hence, the duration of angiotensin converting enzyme inhibition was considerably prolonged in renal failure and depended on the severity of renal impairment. The urinary excretion of ramipril and its metabolites decreased with decreasing renal function and was linearly related to the creatinine clearance, suggesting an alternative pathway of elimination. The pattern of excretion rates of ramipril and its various metabolites was not affected by renal failure. In contrast to the marked changes in the renal elimination, no relevant differences were observed in the absorption of ramipril from the gastrointestinal tract. Systolic and diastolic blood pressure decreased in all groups. The single 10 mg dose of ramipril was well tolerated.

Adult↗
PubMed1985

Pharmacokinetics and absolute bioavailability of intramuscular tranexamic acid in man.

The bioavailability of tranexamic acid after the administration of a single intramuscular dose was estimated in three healthy male volunteers. 500 mg tranexamic acid were given intramuscularly and intravenously, as a bolus injection, to each subject on separate occasions. Following intramuscular administration, the peak plasma concentrations were attained after approximately one hour and the apparent elimination half-life was about two hours. The absolute bioavailability was 105.2 +/- 10.7% (mean +/- SD). At the dose given, the bioavailability of tranexamic acid after intramuscular administration is fast and complete.

Adult↗
PubMed1984

Beta-adrenergic blocking effects and cardiodepressant activity of penbutolol and its two optical isomers in the guinea-pig left atrium.

The beta-adrenoceptor blocking potency and cardiodepressant activity of penbutolol and its two isomers have been evaluated in the guinea-pig left atrium in order to determine if the two properties are related. While (-)-penbutolol was ten times more potent than (+)-penbutolol and three times more potent than (+/-)-penbutolol as a beta-adrenoceptor antagonist, the three compounds showed a similar activity as cardiodepressant agents. These results seem to demonstrate that it is unlikely that this depressant action can be related to the antagonism of beta adrenoceptors.

Animals↗
PubMed1982

Effect of reserpine on body temperature in the rat after pretreatment with amphetamine and monoamineoxidase inhibitors.

Intravenous injection of reserpine produced a small but significant hyperthermic effect which is followed by a persistent decrease in temperature. Amphetamine, tranylcypromine and pargyline administered intraperitoneally caused a fall in body temperature. The decrease was higher after pargyline than after amphetamine and tranylcypromine. The initial increase in temperature that was seen immediately after reserpine administration in unanaesthetized and anaesthetized rats was significantly potentiated in the animals pretreated with amphetamine and monoamineoxidase (MAO) inhibitors. The decrease in temperature occurring afterwards is not significantly different from that seen after reserpine alone in conscious rats. However, in anaesthetized rats the hypothermic response was delayed and was not as marked as in conscious animals. The changes in the transient hyperthermic response to reserpine obtained with pretreatment with these drugs are roughly reminiscent of the modification of the effect on blood pressure. In conclusion, the present results confirm that the simple and objective determination of drug induced changes on reserpine effects on temperature may equal the results obtained on blood pressure.

Amphetamine↗