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Biomedical subjects

P Placheta

Publications and source records attributed to P Placheta.

At least 19 recordsLinked to original sources

Enflurane alters compensatory hemodynamic and humoral responses to hemorrhage.

This study examined the impact of enflurane (3%) on the hemodynamic and humoral defense mechanisms in a canine model of hemorrhagic shock. In order to obtain reasonable reference values with confounding influences of anesthesia and recent surgical preparation, the dogs were chronically instrumented 8-10 days prior to the experiments enabling measurements in the conscious state. While arterial pressure, cardiac output, and the corresponding derivatives were recorded continuously, plasma catecholamines and plasma renin activity were determined intermittently. As anticipated, the conscious dogs were able to tolerate considerable more severe levels of hemorrhage than the dogs anesthetized with enflurane. This finding is associated with reciprocal responses of both the renin-angiotensin system and the sympathoadrenal system in the conscious and anesthetized states. While the sympathoadrenal system prevailed in the conscious dogs, the renin-angiotensin system predominated during enflurane anesthesia. Despite the augmented response of the renin-angiotensin system, the activation of this defense mechanism was not sufficiently powerful enough to prevent overall hemodynamic deterioration with hemorrhage in the animals anesthetized with enflurane.

Anesthesia, Inhalation

B-HT 920 and B-HT 958: presynaptic effects on electrically evoked 3H-dopamine release from slices of rat nucleus accumbens.

The effects of two thiazoloazepine derivatives, B-HT 920 (6-allyl-2-amino-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepine) and B-HT 958 (2-amino-6-(p-chloro-benzyl)-4H-5,6,7,8-tetrahydrothiazolo[5,4-d]a zepine) on electrically evoked overflow of 3H-dopamine were studied. Slices from nucleus accumbens of the rat were preincubated with 3H-dopamine and superfused at 23 degrees C or 37 degrees C. Electrical field stimulation was applied using frequencies of 0.5 or 5 Hz. At 37 degrees C/5 Hz, B-HT 920 markedly and dose-dependently (0.01-0.1 mumol/l) reduced the stimulation evoked overflow of tritium. Its dose-response curve was shifted to the right at 23 degrees C/0.5 Hz and 23 degrees C/5 Hz, respectively. A similar result was obtained with the dopamine receptor agonist, apomorphine (1 mumol/l). B-HT 958 (0.1-10 mumol/l) also reduced electrically induced overflow of tritium at 37 degrees C/5 Hz, had no effect at 23 degrees C/0.5 Hz, and facilitated tritium overflow at 23 degrees C/5 Hz. Sulpiride (10 mumol/l) completely prevented the effects of B-HT 920 (1 mumol/l) or B-HT 958 (1 mumol/l) at 37 degrees C/5 Hz, whereas phentolamine (1 mumol/l) had no effect on the actions of the two drugs under these experimental conditions. From the patterns of effects obtained under the different experimental conditions it is concluded that B-HT 920 acts as full agonist at presynaptic dopamine autoreceptors whereas B-HT 958 acts as partial agonist.

Adrenergic alpha-Agonists

Effects of clonidine on the stimulation-evoked release of 3H-noradrenaline from superfused rat brain slices as a function of the biophase concentration. Temperature dependent widening of extracellular space.

The influence of clonidine on the stimulation-evoked overflow of tritium was studied in brain slices preincubated with 3H-noradrenaline. The slices were prepared from parietal cortex (Cx), nucleus anterior hypothalami (nah) and nucleus tractus solitarii (nts). After preincubation, the tissues were superfused at 23 degrees C or 37 degrees C with a medium containing the noradrenaline uptake inhibitor desipramine. Electrical field stimulation was applied using stimulation frequencies of 0.3-10 Hz. At 23 degrees C/0.3 Hz, clonidine concentration-dependently inhibited the evoked overflow of tritium in all three brain regions. In contrast, at 23 degrees C/3 Hz the inhibitory effect of the drug in the Cx was abolished and a facilitation was observed in the nah and nts. When tested at increasing frequencies of stimulation in the nts at 23 degrees C, clonidine exerted a dual action, characterized by a reduction of electrically evoked responses at frequencies below 1 Hz and a facilitation at frequencies above 1 Hz. At 37 degrees C, clonidine concentration-dependently decreased the evoked overflow in all brain regions studied, this effect being more pronounced at 0.3 Hz than at 3 Hz. The apparent lack of an effect of clonidine on the stimulation-evoked overflow of tritium in the Cx at 23 degrees C/3 Hz was turned to a facilitation when noradrenaline (0.01 mumol/l) was included in the superfusion medium. Conversely, an inhibitory effect of clonidine was seen when the uptake blocker desipramine (as well as noradrenaline) was omitted from the superfusion medium.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals

Properties of [3H]taurine release from crude synaptosomal fractions of rat cerebral cortex.

The release of previously accumulated [3H]taurine and [14C]GABA from crude synaptosomal (P2) fractions isolated from rat cerebral cortex was studied using a superfusion system. The spontaneous efflux of [3H]taurine and [14C]GABA was stimulated by elevated concentrations of K+ (15--133 mM) in a concentration-dependent manner. This K+-stimulated relase of [14C]Gaba but not of [3H]taurine was enhanced in the presence of Ca2+. However, addition of 3 mM Ca2+ to the superfusion medium in the presence of the ionophore A 23187 resulted in a stimulation of the release of both [3H]taurine and [14C]GABA. These results are discussed in connection with the cellular localization of taurine in the central nervous system.

Animals

IgG levels in maternal and umbilical cord serum after vaginal delivery and after elective Caesarean section.

Concentrations of IgG is maternal serum and in umbilical cord blood were determined in two groups of patients: one group had spontaneous vaginal deliveries and the other elective Caesarean sections. Mean umbilical cord serum IgG after vaginal delivery was significantly higher than the mean value after elective Caesarean section. The difference between the maternal serum IgG livel and the umbilical cord serum IgG level increased as did the duration of labour.

Cesarean Section

[Long-term comparative study: diclofenac (voltaren) and naproxen (proxen) in arthritis].

Two non-steroidal antirheumatic drugs, diclofenac (Voltaren) and naproxen (Proxen), were compared with respect to their analgesic effect and the observed improvement in joint mobility in two groups of patients, each consisting of 20 males with either cox-arthrosis or gonarthrosis. The duration of treatment was up to six months. The therapeutic response was assessed by the mean scores of spontaneous and exercise-induced pain, the clinical state of joints and painfree time of walking. Both drugs led to a persistent improvement in the condition of most patients, but the clinical impression would appear to point to a more marked analgesic effect of diclofenac. The daily maintenance dosage from the fourth week of treatment onwards was 75 mg diclofenac and 500 mg naproxen. Both drugs were generally well tolerated. Occasionally gastrointestinal side effects were observed (more frequently in the naproxen group). Laboratory controls were carried out periodically, but no evidence of organ toxicity or hemotoxic effects was found.

Arthritis

Fluvoxamine, a specific 5-hydroxytryptamine uptake inhibitor.

1. On the basis of both in vitro and in vivo experiments fluvoxamine has been characterized as a potential anti-depressant drug with almost exclusively 5-hydroxytryptamine (5-HT) uptake inhibiting properties. 2. Fluvoxamine is effective in inhibiting 5-ht uptake by blood platelets and brain synaptosomes. Due to inhibition of the membrane pump the compound prevents 5-HT depletion by the tyramine-derivatives H 75/12 and H 77/77. As a result of the interference with the neuronal re-uptake mechanism for 5-HT, fluvoxamine produces a decreased 5-HT turnover in the brain. Effects of 5-hydroxytryptophan (5-HTP) are potentiated in mice and in combination with pargyline, fluvoxamine induces 5-HT-like behavioural effects. 3. In contrast to tricyclic antidepressants, noradrenaline uptake processes are either unaffected or only slightly inhibited by fluvoxamine. The noradrenaline depleting effects of tyramine derivates are not influenced by fluvoxamine. Reserpine effects, such as ptosis are affected only at very high doses of the test compound. The antagonism by fluvoxamine of the reserpine-induced lowering of the pentamethylenetetrazole convulsive threshold can be regarded as due to an effect upon 5-HT uptake. In contrast to the effects of desmethylimipramine and imipramine, no stimulatory effects are found in rats when rapidly acting reserpine-like compounds are given following a dose of fluvoxamine.

5-Hydroxytryptophan

[Effect of the beta-adrenergic blocking agent bupranolol on the plasma renin activity in normotensive rats].

The effects of the beta-adrenergic blocking agent 3-tert.-butyl-amino-1-(6'-chloro-3'-methylphenoxy)-propan-2-ol hydrochloride (bupranolol; KL 255; Betadrenol) on the plasma renin activity (PRA) of normotensive rats were studied in comparison to propranolol. Bupranolol (10--100 microgram/kg) reduced basal PRA and inhibited the isoproterenol as well as dihydralazine induced increase of PRA in a dose dependent fashion. Bupranolol exhibited an effect 2--4 times stronger than that of propranolol. The PRA inhibiting effects of bupranolol seem to be linked to its beta-receptor blocking properties.

Adrenergic beta-Antagonists

[Concentration of pregnancy-specific-beta-1-protein sp1 in amniotic fluid in normal and pathologic pregnancies (author's transl)].

The concentration of the pregnancy specific protein SP-1 in amniotic fluid was determined in normal and pathologic pregnancies. SP-1 concentrations in amniotic fluid of normal pregnancies amounted to one percent of the maternal serum concentrations. In cases with diabetes mellitus intrauterine death and rhesus incompatibility SP-1 levels were increased significantly.

Amniocentesis

[Double-blind trial: ketoprofen versus phenylbutazone in acute gouty arthritis (author's transl)].

A double-blind study was carried out to compare the effects of ketoprofen and phenylbutazone in acute gouty arthritis. Two groups of patients, each consisting of 23 males, received intramuscular injections of either phenylbutazone (2 X 300 mg daily) or ketoprofen (2 X 50 mg daily) for a period of 7 days. The drug effects were assessed both subjectively and objectively. There was an excellent therapeutic effect in both groups. In general, no statistically-significant differences were detected between the two preparations. However, ketoprofen appears to be slightly better tolerated with respect to the incidence of systemic and local side effects. Thus, the administration of ketoprofen can be recommended in cases of acute gouty arthritis.

Acute Disease

Mepiprazole, a new psychotropic drug: effects on uptake and retention of monoamines in rat brain synaptosomes.

The influence of mepiprazole (EMD 16,923), a new pyrazol-ylalkyl-piperazine derivative, on the uptake of 3H-norepinephrine (NE), 3H-dopamine (DA), and 3H-serotonin (5-HT) into rat brain synaptosomes from cerebral cortex, corpus striatum, and hypothalamus was investigated in comparison with several psychotropic drugs, including oxypertine, d-amphetamine, imipramine, desipramine, chlorimipramine, amitriptyline, and chlorpromazine in vitro. Mepiprazole was a relatively weak inhibitor of monoamine uptake and exhibited its strongest action on the hypothalamic 5-HT uptake, being almost equipotent with desipramine (IC50 = 0.9 MUM). Furthermore, the influence of the drugs on the retention of 3H-amines previously taken up by whole rat brain synaptosomes was studied. Unlike the tricyclic antidepressants, mepiprazole as well as oxypertine and d-amphetamine markedly increased the efflux of radioactivity during a 20-min incubation at 37 degrees C at low concentrations (10(-6) to 10(-5) M), whereas at 10(-4) M all drugs greatly enhanced the efflux. The ability of mepiprazole to increase 5-HT concentration at the receptor level by a combination of neuronal uptake inhibition and release is discussed in relationship to the central actions of the drug.

Animals

[Plasma renin activity in essential hypertension: different short- und long-term effects of diuretics (author's transl)].

In an acute clinical trial 12 patients with essential hypertension on a standardized sodium and potassium dietary intake were given either amilorid (10 mg daily, orally) or potassium canrenoate (200 mg daily, i.v.) for two days. Either treatment caused a significant decrease in blood pressure and an increase in plasma renin activity (PRA). The aldosterone excretion rate was elevated only in the patients receiving amilorid. Furthermore potassium retention and sodium loss were more pronounced in the amilorid group. Long-term treatment (up to 14 weeks) with amilorid (10 mg daily), spironolactone (200 mg daily) or chlortalidone (50 mg daily) significantly lowered the blood pressure of patients with essential hypertension. Plasma potassium and PRA rose significantly in patients receiving either amilorid or spironolactone. However, after three weeks of therapy the mean PRA returned to the pretreatment level in patients on amilorid while it remained persistently elevated in the spironolactone group. On the other hand, chlortalidone caused potassium loss and persistent elevation of PRA. A possible relationship between the changes in plasma potassium levels and PRA in response to diuretics is discussed.

Adult