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At least 19 recordsLinked to original sources
PubMed1991

Budesonide and terbutaline or terbutaline alone in children with mild asthma: effects on bronchial hyperresponsiveness and diurnal variation in peak flow.

The effects of treatment with budesonide (200 micrograms twice daily) and terbutaline (500 micrograms four times daily) has been compared with the effects of placebo and terbutaline in 27 children with mild asthma, aged 7-14 years, in a double blind, randomised placebo controlled study over eight weeks. Bronchial responsiveness (PC20 histamine), lung function, the amplitude of diurnal variation in peak expiratory flow (PEF), and symptom scores were measured. Baseline FEV1 was over 70% predicted and PC20 histamine less than 8 mg/ml. Twelve children were treated with budesonide and terbutaline and 15 with placebo and terbutaline. After four and eight weeks of treatment the change in PC20 was significantly greater after budesonide and terbutaline than after terbutaline alone by 2.1 (95% CI 0.5-3.8) and 1.3 (95% CI 0.1-2.5) doubling doses respectively. Mean FEV1 did not change in either group. The change in afternoon and nocturnal PEF was significantly greater after budesonide and terbutaline than after terbutaline alone. The amplitude of diurnal variation in PEF did not change significantly in either group. Peak flow reversibility decreased in the budesonide group. There were no differences between treatments for cough and dyspnoea, but wheeze improved in the budesonide group. The children with mild asthma treated with budesonide and terbutaline showed improvement in bronchial responsiveness, afternoon and nocturnal PEF, and symptoms of wheeze and a fall in peak flow reversibility by comparison with those who received terbutaline alone.

Administration, Inhalation↗
PubMedDate not supplied

A comparison of gestational days gained with oral terbutaline versus continuous subcutaneous terbutaline in women with twin gestations.

OBJECTIVE: To compare gestational days gained with oral versus subcutaneous terbutaline for maintenance tocolysis. STUDY DESIGN: In retrospective fashion 386 women enrolled in an outpatient preterm labor identification program met the following criteria: twin gestation, development of threatened preterm labor resulting in treatment with oral terbutaline, and subsequent recurrence of threatened preterm labor resulting in treatment with continuous subcutaneous terbutaline. The primary outcome was gestational days gained with oral terbutaline versus gain with continuous subcutaneous terbutaline. RESULTS: There were significantly more days gained during subcutaneous treatment than during oral treatment (34.0 +/- 19.8 versus 19.3 +/- 15.3 days). Thirty-three percent of desired prolongation was achieved with oral terbutaline, whereas 79% of desired prolongation was achieved with subcutaneous terbutaline (p < 0.001). Patients gained a mean of 53.4 +/- 21.4 days overall with outpatient tocolysis. The mean gestational age at delivery was 35.2 +/- 1.9 weeks. CONCLUSION: Continuous subcutaneous terbutaline was superior to oral terbutaline in prolonging gestation in women with twin gestations.

Administration, Oral↗
PubMedDate not supplied

Beta1-adrenoceptor stimulation by high-dose terbutaline downregulates terbutaline-stimulated alveolar fluid clearance in ex vivo rat lung.

Because high-dose terbutaline and isoproterenol (10(-3) M), beta2-adrenergic agonists, failed to increase alveolar fluid clearance, the mechanisms responsible for this effect were examined in ex vivo rat lungs. An isosmolar 5% albumin solution with Evans blue dye was instilled into the distal airspaces in isolated rat lungs that were then inflated with 100% oxygen at an airway pressure of 8 cm H2O in a 37 degrees C incubator. Alveolar fluid clearance was measured by the progressive increase in dye concentrations over 1 hour. The results indicated that: (1) although 10(-5) M terbutaline or isoproterenol increased alveolar fluid clearance, 10(-3) M terbutaline or isoproterenol did not; (2) both concentrations of terbutaline (10(-5), 10(-3) M) increased intracellular adenosine 3',5'-cyclic monophosphate in cultured type II alveolar epithelial cells; (3) instillation of atenolol, a selective beta1-adrenergic antagonist, in the presence of either 10(-3) M terbutaline or isoproterenol was associated with an increase in alveolar fluid clearance. These results suggested that beta1-adrenoceptor stimulation prevented the normal response to a beta2-adrenergic agonist. To further test this hypothesis, a selective beta1-adrenergic agonist, denopamine, was administered; these results showed that (4) 10(-3) M denopamine, a selective beta1-adrenergic agonist, inhibited the increase in alveolar fluid clearance in the presence of 10(-5) M terbutaline; (5) hypoxia for 2 hours did not alter the effects of terbutaline on alveolar fluid clearance. The mechanism for the inability of the alveolar epithelium to respond to high-dose terbutaline or isoproterenol with the normal upregulation of alveolar fluid clearance in ex vivo rats lungs appears to be mediated by beta1-adrenoceptor stimulation that subsequently suppresses the beta2-adrenergic response.

Adrenergic beta-Agonists↗
PubMed1989

Pharmacokinetics of the enantiomers of terbutaline after repeated oral dosing with racemic terbutaline.

Terbutaline is a beta 2-agonist and administered as the racemic mixture. The pharmacokinetics of the separate enantiomers differ with respect to degree of absorption and clearance. In the present study, repeated doses of racemic terbutaline were given to six healthy volunteers. Plasma was analyzed for the concentrations of the two enantiomers. The observed plasma concentrations at steady state differed from those predicted from the values observed after single dose administration of the separate enantiomers. The difference between the observed and predicted values can be tentatively explained by a combined influence of (-)-terbutaline on the absorption of (+)-terbutaline and the influence of (+)-terbutaline on the elimination of (-)-terbutaline. The results have implications for the interpretation of effect/concentration studies with terbutaline, but do not affect the doses used in clinical practice.

Adult↗
PubMed1992

Influence of beta-adrenergic receptor function during terbutaline treatment on allergen sensitivity and bronchodilator response to terbutaline in asthmatic subjects.

Nine asthmatic patients with an allergy to birch or timothy underwent bronchial allergen provocations on three different trial days, with intervals of 2 to 5 wk. Two weeks prior to one of the provocations, no medication was allowed. Before the other two provocations the patients had been on continuous treatment with oral terbutaline (7.5-mg slow-release pill bid) for 2 wk, which was discontinued 12 or 48 h before the allergen provocation. After allergen challenges, terbutaline was inhaled in increasing doses (0.5 mg, 1.0 mg, and 2.0 mg), and pulmonary function was measured after each dose. Before each allergen provocation, blood samples were drawn for measurements of catecholamine and terbutaline concentrations and for in vitro measurements of beta-adrenergic receptor function on lymphocytes (isoproterenol-induced accumulation of cyclic AMP). Beta-adrenergic receptor function on blood lymphocytes was impaired after the two treatment periods, compared with the drug-free period, and was significantly more depressed at 12 h than 48 h after dosing. The bronchial responsiveness to allergen, defined as PC20PEF (median values), was 1,700 biologic units (BU) after the period of no treatment and 220 BU and 445 BU at 12 and 48 h after discontinuation of the terbutaline treatment (p less than 0.1 after 48 h). Five of the nine patients exhibited increased bronchial responsiveness 48 h after treatment, compared to results without treatment. The responsiveness was similar on all occasions in three patients. The bronchodilator response to inhaled terbutaline after allergen-induced bronchoconstriction was attenuated (p less than 0.01) at both 12 and 48 h after terbutaline, compared to results without treatment, indicating desensitization also of the bronchial beta-adrenergic receptors. We conclude that the early bronchial responsiveness to allergen is increased following a period of continuous treatment with a beta-adrenergic receptor agonist in some asthmatic patients and that the capability of a beta-agonist to reverse allergen-induced bronchoconstriction is attenuated after beta-agonist treatment.

Adult↗
PubMed1985

Indomethacin, (-)-terbutaline (beta 2 agonist), and (+)-terbutaline in acute inflammation induced by repeated ischemia in hamster cheek pouch.

A mild and controlled acute inflammatory reaction in hamster cheek pouch was created without any exogenous, but rather by locally activated and liberated, mediators. A pressure of 60 mm Hg was applied to part of the everted cheek pouch eight times with a 10-min recovery period in between. The microvascular response was followed by intravital microscopy and the permeability changes were monitored with intravital fluoroscopy and intravenous FITC dextran (mol wt 150,000). The number of extravasated polymorphonuclear leukocytes (PMNLs) was calculated by a new, whole tissue, histological technique. In three experimental groups (-)-terbutaline (beta 2-receptor agonist) 0.05 mg/100 g body wt., (+)-terbutaline 0.05 mg/100 g body wt., and indomethacin 2 mg/100 g body wt. was given intravenously before pressure was applied. A fourth group, with no drug given, served as control. There was a rapid increase in the number of FITC dextran leakages and extravasated PMNLs in the control group. Indomethacin almost completely inhibited FITC dextran permeability and extravasation of PMNLs. The beta 2 agonist markedly diminished the number of FITC dextran leakages for 75 min. The number of extravasated PMNLs was also reduced. Treatment with (+)-terbutaline, which is supposed to have no beta 2-receptor effect, gave a slight reduction in number of FITC dextran leakages and almost a complete inhibition of PMNL extravasation. Thus we conclude that indomethacin is a very potent antiinflammatory agent even in the early phase of inflammation. (-)-Terbutaline diminished the inflammatory response, probably by preventing endothelial gap formation. (+)-Terbutaline prevented PMNL extravasation either by interaction with the PMNL itself or with the endothelium.

Animals↗
PubMed1986

Downgrading of biochemical and cardiovascular responses to an intravenous infusion of terbutaline following chronic treatment with oral terbutaline.

Beta 2-agonists are known to cause a range of unwanted biochemical and cardiovascular responses. The present study was designed to investigate the effect of chronic exposure to beta 2-stimulation on the magnitude of these responses produced by an acute challenge with a beta 2-agonist. In this single blind placebo controlled study in six healthy male volunteers, we have compared the effects of chronic dosing with either oral terbutaline (5 mg three times daily for two weeks) or placebo on a number of these responses produced by an intravenous infusion of terbutaline (6 micrograms per kilogram over 1 hour). The infusion was given twenty-four hours after the last dose of oral terbutaline or placebo. The rise in pulse rate, systolic blood pressure and plasma glucose and the fall in serum potassium during terbutaline infusion, although still demonstrable, were significantly reduced following treatment with oral terbutaline compared to placebo. This suggests downgrading of beta-receptor function after chronic beta 2-stimulation.

Administration, Oral↗
PubMed1989

Comparison of inhaled terbutaline and terbutaline injection in treatment of acute asthmatic attacks in children.

Thirty asthmatic children, aged 4 to 13 years, 22 boys and 8 girls, were studied during acute asthmatic attacks. Each group of 15 children received either a 0.01 mg/kg subcutaneous injection of terbutaline or 2 puffs from terbutaline pressurized aerosol (0.25 mg/puff) inhaler through a 750-ml volumetric spacer. A slightly greater increase in PEFR following injection compared with inhalation throughout the 6 hours study period was observed. Significant increases in systolic blood pressure and pulse rate were observed only after injection. Therefore, it was concluded that inhaled terbutaline is safe and effective for treating children over 4 years of age with acute bronchospasm and has less cardiovascular side effects than injected terbutaline.

Acute Disease↗
PubMed1987

Terbutaline sustained-release treatment during one week 5 mg b.i.d. compared to one week placebo: terbutaline plasma levels, c-AMP plasma levels, lung function and tremor measurement.

In a group of ten patients with chronic asthmatic bronchitis, a good improvement of the lung function was achieved by a sustained-release terbutaline preparation (Bricanyl Retard) in a dosage of 5 mg twice daily. Tremor measurements and c-AMP plasma level showed a statistically significant increase. A good patient compliance was achieved with this dosage of terbutaline two times daily. The sustained-release preparation caused a rather constant and low terbutaline plasma level. We think that this relative low terbutaline plasma level is the most important reason for the lack of side effects.

Adult↗
PubMed1982

Cumulative dose-response study comparing terbutaline pressurized aerosol administered via a pearshaped spacer and terbutaline in a nebulized solution.

The bronchodilator effects of cumulative doses of terbutaline 0.125 mg, 0.125 mg and 0.250 mg administered as a pressurized aerosol via a pear shaped spacer were compared with those of terbutaline 1.25 mg, 1.25 mg and 2.50 mg administered as a nebulized solution via a PARI-inhaler Boy. FEV1.0 and flow-volume curves in 13 patients were measured. Initial placebo treatment of both groups resulted in a significant increase in FEV1.0, especially when it was given in nebulized form. The increase after active drug was significant after 15 min, with only minor changes during the rest of the trial. The log-dose/increase in FEV1.0 showed that equipotent doses of pressurized and nebulized terbutaline were in the ratio 1 to 4. Administration by nebulization offered no clear advantage over use of a pressurized aerosol with a pearshaped spacer.

Adult↗
PubMed1986

Terbutaline slow-release tablets in children with bronchial asthma. Effect and pharmacokinetics compared with plain terbutaline tablets.

The effect of terbutaline sulphate in slow-release (SR) tablets (Bricanyl Depot), 5 mg twice daily, was compared with that of terbutaline sulphate in ordinary tablets (Bricanyl), 2.5 mg three times daily, in a double-blind, randomized, cross-over study during 2 consecutive weeks in 10 asthmatic children. Plasma concentrations and urinary excretion of terbutaline were measured at various times during both treatment periods. The SR tablets produced a higher mean plasma concentration in the morning and a smaller peak-trough variation over the day than the ordinary ones. No differences between the two treatments were observed concerning FEV1 (forced expiratory volume in 1 s). Tremor, measured with an opto-electronic tremorgraph, was about the same for two treatments and not significantly different from tremor seen in healthy children. The reported side effects were less frequent in the SR tablet period.

Adolescent↗
PubMed1989

Terbutaline as powder inhalation from Bricanyl Turbuhaler compared to terbutaline as nebulizer solution in severe chronic airways obstruction.

Twenty two adults with severe chronic airways obstruction--FEV1 from 14 to 57% of predicted--participated on two consecutive days in an open cross over comparison of inhalation of 2 mg terbutaline powder by Bricanyl Turbuhaler and 5 mg terbutaline by a conventional jet nebulizer (Pari Inhalierboy). All participants were domiciliary users of nebulized terbutaline previous to inclusion in this study. The mean (SD) maximal increase in FEV1 within the 60 minutes following inhalation by Turbuhaler and by Pari Inhalierboy was 27% (15%) and 28% (15%). The mean (SD) maximal increase in FVC was 30% (20%) and 29% (16%). The differences were not statistically significant. All participants were able to produce inspiratory flows high enough to use the Turbuhaler. The study suggests that it will be possible to replace the use of nebulizers with powder inhalations, as far as the bronchodilating effects are concerned.

Administration, Inhalation↗
PubMedDate not supplied

Terbutaline increases survival after endotoxin shock. A comparative study of methyl prednisolone, isoprenaline and terbutaline in rats.

Since beta 2-receptor agonists and corticosteroids can counteract inflammatory mediator induced protein leakage and corticosteroids have been proposed as effective in treatment of experimental septic shock, we compared the effects of these agents on rats in endotoxin shock. Sixty adult wistar rats were anaesthetised with thiopentone sodium intra-peritoneally (i.p.), before shock was induced by E coli endotoxin (3 mg/kg bwt i.v.). Ten minutes later the rats were divided into four groups (n = 15 in each) and received either normal saline (controls) 4 ml/kg i.p., methyl prednisolone (MP) 40 mg/kg i.p., isoprenaline (ISO) 200 micrograms/kg i.p. or terbutaline (TER) 200 micrograms/kg i.p. 25% of the initial dose was repeated after 15, 60 and 120 minutes. After 2 hours observation 3-5 animals had died in each group (n.s.), but at the end of the observation period (96 hrs), 87% of the controls, 73% of the MP-group, 53% of the ISO-group and 20% of the TER-group had died. At this time all the surviving animals were looking well and behaving normally. It was concluded that terbutaline significantly increased the survival of rats exposed to a lethal dose of endotoxin compared with controls (p less than 0.001) and compared with methyl prednisolon (p less than 0.05). The mechanism may be that of decreased pulmonary capillary leakage with terbutaline. However, the survival rate was not significantly improved with methyl prednisolon or isoprenaline.

Animals↗
PubMed1990

Comparison of inhaled terbutaline and inhaled terbutaline plus ipratropium bromide in acute asthmatic children.

Twenty asthmatic children, aged 4 to 15 years, consisting of 14 boys and 6 girls, were studied during acute episodes of asthmatic attacks. A group of 10 children each received either inhaled terbutaline 0.5 mg or inhaled terbutaline 0.5 mg followed by ipratropium bromide 0.04 mg 15 minutes later through a 750-ml volumetric spacer. Significant increases in FEV1 over the baseline were observed from 2 minutes to 2 hours and from 2 minutes to 6 hours following the first and second regimen respectively. A slightly greater increase and longer duration in FEV1 were observed in the combined drug treatment and very slight decreases in systolic and diastolic blood pressure below the base-line were observed. Neither regimen showed any serious adverse effect on the heart rate and respiratory rate.

Acute Disease↗
PubMed1982

A comparison of sustained-release terbutaline and ordinary terbutaline in bronchial asthma.

The effects and side effects in steady state of a sustained-release preparation of terbutaline 7.5 mg twice daily were compared with ordinary tablets 5 mg three times daily. The study performed for two weeks was double-blind, double-dummy, cross-over with randomized allocation of the drugs. 20 patients completed the trial and the results show higher mean morning PEFR values and a tendency to milder side effects with depot tablets.

Adult↗