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Biomedical subjects

H Gastpar

Publications and source records attributed to H Gastpar.

At least 19 recordsLinked to original sources

Comparative efficacy of azelastine nasal spray and terfenadine in seasonal and perennial rhinitis.

The efficacy and tolerability of intranasal azelastine (0.14 mg/nostril twice daily) and oral terfenadine (60 mg twice daily) were compared under double-blind conditions in two 6-week, multicenter, parallel-group studies, including 167 patients suffering from seasonal and 52 patients suffering from perennial allergic rhinitis. In both studies, patients were symptomatic on entry and showed significant improvement on both treatments within the first 8 d of therapy, showing little further improvement with continued treatment. Symptoms most pronounced on entry--nasal itching, rhinorrhea, sneezing, and nasal obstruction--responded best to treatment (response rates 80-90%). Objective signs such as mucosal swelling and conjunctivitis improved in a manner parallel to symptoms. In perennial rhinitis, azelastine showed a trend to a superior relief of rhinorrhea and nasal obstruction, whereas terfenadine showed a trend toward better control of sneezing and nasal itchiness. No clinically relevant or statistically significant differences between treatments could be identified. The incidence of adverse effects of possible causal relationship to therapy was low. The most frequent effects in azelastine-treated patients were related to application site disorders, e.g., nasal irritation. Results indicate that with the dose used azelastine nasal spray is an effective treatment for both seasonal and perennial allergic rhinitis.

Administration, Intranasal↗

Investigation of long-term efficacy and tolerability of azelastine nasal spray in the treatment of perennial allergic rhinitis.

The long-term efficacy and tolerability of azelastine (CAS 58581-89-8) nasal spray (0.14 mg/nostril b.i.d.) was investigated in patients suffering from perennial allergic rhinitis. 185 patients entered an initial 6 months' study; 35 of them continued in a follow-up for a further 30 to 60 weeks' treatment. Azelastine both attenuated the severity and reduced the incidence of rhinitis symptoms, with the highest rate of improvement during the first month with some additional improvement during the following months. The most marked effects were on those symptoms which were initially most severe: nasal obstruction, mucosal swelling, rhinorrhoea, sneezing and nasal itching. Signs of rhinitis identified by rhinoscopic examination improved in parallel to symptoms. 84.1% of patients reported 'good' or 'very good' efficacy as did 94.3% during the follow-up. Approximately 96% of patients rated the tolerability of treatment as 'very good' or 'good'. The incidence of adverse events of possibly causal relationship to azelastine treatment was low during the first 6 months. The most frequent events were the experience of application site reactions (e.g. burning) and bitter or unpleasant taste, specific to azelastine. No unwanted effects were reported by patients continuing treatment. In addition, results of nasal biopsies indicate that with the dose used azelastine nasal spray is a safe drug for long-term treatment of perennial allergic rhinitis.

Administration, Intranasal↗

Intranasal treatment of perennial allergic rhinitis. Comparison of azelastine nasal spray and budesonide nasal aerosol.

The efficacy and tolerability of azelastine (CAS 58581-89-8) nasal spray (0.14 mg/nostril b.i.d.) and budesonide (CAS 51333-22-3) nasal aerosol (0.05 mg/nostril b.i.d.) were compared in a 6-week, multicentre, parallel group study of 193 patients suffering from perennial allergic rhinitis. Total rhinitis symptoms complex (TSC) scores derived from 10 rhinitis symptoms improved during treatment by a mean of 11.4 +/- 6.8 with azelastine and 10.8 +/- 6.4 with budesonide. Response rates, defined as a decrease in TSC of at least 50% at the end of therapy, was 79% with azelastine and 73% with budesonide. There were no significant differences between the treatment groups with respect to either target variable. Objective measurements of nasal flow rate showed a return to normal values during the 6-week therapy. Signs of rhinitis identified by rhinoscopic examination improved in parallel to symptoms. Both medications were well tolerated. The incidence of adverse events of possibly causal relationship to therapy was low. The most frequent event in azelastine treated patients was the experience of an "unpleasant" taste or smell. Occasional epistaxis occurred in both treatment groups but more frequently with budesonide. Results indicate that with the dose used azelastine nasal spray is an effective treatment for perennial allergic rhinitis comparable to that of budesonide nasal aerosol.

Administration, Intranasal↗

[NAAGA versus disodium cromoglycate in perennial allergic rhinopathy: results of a multicenter study].

The efficacy and tolerability of Naaga (the magnesium salt of N-acetyl-aspartyl-glutamate) and of sodium cromoglycate after intranasal application were tested and compared in 100 patients suffering from chronic allergic rhinitis. The study was conducted according to a randomized, double-blind design in four centers. The intensity and frequency of typical allergic symptoms such as nasal obstruction, sneezing, runny and itching nose, conjunctivitis, ocular itching and tear flow were recorded on a 4-point scale (absent, light, moderate and severe). The intensity of nasal and ocular symptoms was found to be marked for patients in two centers. For the patients in the other two centers the drugs' efficacy was difficult to assess because symptoms were not marked (rated either as absent or light) at the beginning of the study. Thus the assessment of efficacy was based on 60 patients (centers 1 and 2), while the assessment of tolerability was based on the whole patient sample (n = 100). There was no statistically significant difference between the two compounds in terms of efficacy. A total of five patients in each of both groups complained of moderate untoward effects (all patients from the same center).

Adolescent↗

[Effectiveness and tolerance of the C3 convertase inhibitor, N-acetyl-aspartyl-magnesium glutamate with anti-allergic action. Results of a double-blind study].

N-Acetyl-aspartyl magnesium glutamate (Rhinaaxia, NAAGA) is a topically active antiallergic dipeptide. The compound acts in two different ways. On the one hand NAAGA inhibits the mast cell-degranulation, on the other hand this compound blocks the activation of the C3-convertase, subsequently followed by a blocked cleavage of the fragments C3a and C5a, respectively. 20 patients suffering from pollinosis were treated for 2 weeks according to a randomized double-blind placebo-controlled study. Besides subjective complaints nasal obstruction was objectively documented via rhinomanometria. 9 out of 10 patients under placebo had to use the rescue drug tritoqualine, a histidine decarboxylase inhibitor, compared to none in the verum group (p less than 0.01). After 14 days of treatment with NAAGA the nasal peak flow rate increased by 21.5 l/min and 21.8 l/min in the tritoqualine/placebo group, respectively (not significant). Nasal obstruction improved statistically significantly after 7 and 14 days of treatment in both groups. Tolerance was reported to be good in either group.

Adolescent↗

[Administration of terfenadine in a single dose: comparison to standard treatment, as a double blind study, in patients presenting with allergic rhinitis].

This double-blind, randomized multicentre study was designed to compare efficacy and tolerability of 120 mg terfenadine taken once daily (in the morning) with the established regimen of 60 mg terfenadine taken twice daily in the treatment of seasonal rhinitis. Two comparable groups, a total of 191 hay fever patients, were treated for 1 week. Symptom severity was assessed by the investigators before and at the end of the treatment (visual analogue scale), and daily by the patient (four-point rating scale). All symptoms improved to a similar degree in both groups. Differences between the two groups were not statistically significant, except for nasal symptoms in three cases as assessed by the visual analogue scale in one centre (better relief in the group given 120 mg terfenadine once daily). Tolerability was good and similar in both groups. The data presented show that in the treatment of hay fever 120 mg terfenadine given once daily is an effective, convenient and well tolerated alternative to the regimen of 60 mg terfenadine given twice daily.

Benzhydryl Compounds↗

Studies on the vasoocclusive crisis of sickle cell disease IV. Mechanism of action of pentoxifylline (Trental).

Pentoxifylline was shown to prevent sickling induced by deoxygenation of SS-genotype blood from sickle cell disease patients. It also prevents development of cell stiffness, based on decreased membrane fluidity. This effect is related to increased red cell ATP content, decreased potassium loss during sickling and decreased attachment of hemoglobin to the red cell membrane during sickling. There was no effect on osmotic fragility or mean corpuscular volume. There was some increase in pH of blood from patients in vasoocclusive crisis of sickle cell disease under the effect of pentoxifylline. The consideration is discussed that pentoxifylline may prevent vasoocclusive crisis, but may not abort an existing process.

Adenosine Triphosphate↗

Studies on the vasoocclusive crisis of sickle cell disease. III. In vitro and in vivo effect of the pyrimido-pyrimidine derivative, RA-233: studies on its mechanism of action.

Red cell deformability was found to be impaired in SS- and SC-genotype and to a lesser extent SA-genotype red blood cells as compared with those of AA-genotype. RA-233 in vitro improved deformability according to a bell-shaped dose-response curve. RA-233 also prevented experimental vasoocclusive crisis in Macaca arctoides. Deoxygenation of SS-genotype red cells resulted in sickle shape transformation, ATP depletion, potassium efflux, and attachment of hemoglobin molecules to the membrane. These changes were prevented by RA-233. Suspending SS-genotype red blood cells in potassium rich tris-buffer also prevented potassium efflux during deoxygenation and also decreased cellular deformability. RA-233 had no effect on osmotic fragility of SS-genotype red blood cells.

Adult↗

Mechanism of the potentiation of thrombolysis by pentoxifylline (Trental).

Streptokinase induced thrombolysis of radioactive labeled human fibrin clots was potentiated by simultaneous treatment with pentoxifylline (Trental). This appears to be due in part to the prevention of platelet aggregation on the clot. In addition, release of t-PA and PgI2 from the endothelium and increases in red cell deformability may also play a role.

Animals↗

[Rhinomanometric measurements following intranasal allergen provocation].

Intranasal provocation tests followed by rhinomanometry were performed on 49 males with defined pollen allergy. Subsequently each patient took two tablets of tritoqualine, 100 mg each, three times daily for four or five days. Intranasal provocation was then repeated with the same allergen and flow again measured by rhinomanometry. There was a highly significant, treatment-induced rise in breath-flow through both nasal passages. The drug was well tolerated and no side effects, in particular no sedative action, were observed.

Histamine H1 Antagonists↗

[Drug side effects on the nasal mucosa and sense of smell].

Several drugs may induce pathologic changes of the nasal mucosa, especially at a long-term treatment. The clinical appearance of an allergic or vasomotoric rhinopathy, a chronical hyperplastic or an atrophic rhinitis, hemorrhagic changes of the mucosa with the incidence of epistaxis or smelling disorders may be caused by several drugs. The ENT-specialist, therefore, should always take in consideration the various drugs, which the patient received but mostly have been prescribed by another doctor.

Administration, Intranasal↗

Red cell flexibility and platelet aggregation in patients with chronic obstructive vascular disease (COAD) and study of therapeutic approaches.

The red blood cell flexibility was studied in the blood of twenty patients with severe peripheral vascular disease and twenty matched controls. Patients exhibited significantly less red cell flexibility than controls. In both groups there was an inverse relationship between age and red cell flexibility. No correlation was found between red cell flexibility and sex or smoking history. Pentoxifylline, a xanthine derivative which inhibits phosphodiesterases and platelet aggregation, was found to increase red cell flexibility. This effect of the drug was greater on red cells with imparied flexibility than on normal cells. Various prostaglandins by contrast were found to decrease red cell flexibility, this could be compensated for by pentoxifylline. Forty patients with COAD were treated intravenously with PgE1. Significant inhibition of platelet aggregation and clinical improvement was noticed. It is suggested that combinations of PgE1 and pentoxifylline should be explored in clinical studies.

Adult↗

The role of fibrinolysis in the therapy of peripheral vascular disease.

In vivo thrombolytic studies in stumptailed monkeys indicated that pentoxifylline potentiates thrombolysis induced by urokinase activated human plasmin. Pentoxifylline as well as prostaglandin E1 released plasminogen activators and activated the fibrinolysin system. From this point of view pentoxifylline and prostaglandin E1 synergized with each other. Pentoxifylline potentiated the thrombolytic effect of prostaglandin E1 in vivo.

Alprostadil↗

Efficacy and tolerability of glaucine as an antitussive agent.

One hundred and thirty out-patients, affected by acute and chronic cough caused by upper respiratory tract inflammation, took part in two clinical studies aimed at evaluating the efficacy and tolerability of glaucine , a new antitussive agent. The first study involved 90 patients in a double-blind comparative trial of glaucine and codeine: both treatments were administered as a syrup at a dosage of 30 mg 3-times daily for 7 days. The cough suppressant effect of the two treatments was checked by the physician and the patient using a 4-point scale (from absent to severe), and by the patient using a visual analogue scale. Mean scores of the physician's evaluation decreased from 3.0 to 1.10 after codeine and from 3.0 to 0.47 after glaucine (p less than 0.001 between treatments). Mean values of the patients' visual analogue scales decreased from 83 mm to 17 mm after codeine, and from 85 mm to 7 mm after glaucine (p less than 0.001 between treatments). Constipation and nausea were reported by 9 patients on codeine and by no patient on glaucine (p less than 0.01). One patient on codeine was withdrawn from the study after 3 days because of vomiting, constipation and nausea. The second study was an open trial in 40 patients who received glaucine capsules at a dosage of 30 mg 3-times daily for 28 days. The antitussive effect of the treatment was evaluated on the basis of the same criteria as in the first study. The mean score of the physician's evaluation decreased from 3.0 to 0.15 (p less than 0.001); the mean value of the patients' visual analogue scales decreased from 93 mm to 1 mm (p less than 0.001).(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗

Effect of second tumors and of prostaglandin-leukotriene inhibitors on radiation therapy of transplanted rodent tumors.

The prostaglandin and leukotriene inhibitor sodium meclofenamate (SM) failed to influence radiation therapy induced regression of 6C3HED Gardner lymphosarcoma in C3H mice. Recurrence after radiation therapy, however, was reduced by treatment with SM. During these experiments, we observed that if a tumor was "cured" by radiation therapy, it required inoculation of a larger number of cells to establish a second tumor. Presumably, a certain degree of immunity has developed. On the other hand, if a second tumor was already established, less tumor cells were needed to establish a third tumor. This may be related to immuno-suppressor products of the second tumor. This effect could be partly inhibited by SM, suggesting that prostaglandins and leukotrienes may be involved in this phenomenon.

Animals↗

Antineoplastic effect of the xanthine derivative Trental.

The xanthine derivative, Trental (pentoxifylline) was found to inhibit several human leukemic and lymphoma cell lines in tissue cultures. Optimal concentrations were less inhibitory for a normal B-lymphocyte cell line then for the neoplastic cell lines. In fact, small concentrations stimulated DNA synthesis in the normal cell line. Trental and beta-interferon appeared to be additive synergists at certain dosages. Possible mechanisms are discussed.

B-Lymphocytes↗