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At least 19 recordsLinked to original sources
PubMed1987

Fenoterol depot and fenoterol in premature uterine contractions--a multicentric double-blind comparative study.

In a double-blind randomized study, the effect of a single dose of a fenoterol preparation with delayed release of active substance (designated as fenoterol depot) was compared with a fenoterol product with undelayed release of active substance (designated as fenoterol) in two groups respectively comprising 66 and 65 female patients with premature uterine contractions. The fenoterol depot was administered p.o. in a single total dose of 21 mg at the beginning of an investigation period of 360 minutes and the fenoterol was administered p.o. within 235 minutes in three identical consecutive doses resulting in a total dose of 22.5 mg. The increased uterine activity present at the beginning was markedly lowered by an initial intravenous infusion of Partusisten. After administration of the two oral preparations, the uterine contractions remained at the low level achieved. The fenoterol depot was slightly superior to fenoterol with regard to the reduction of the duration of contractions: the difference in the inhibition of the duration of the contraction between the two preparations was a maximum of 25.7% in favor of fenoterol depot. The frequency of uterine contraction was substantially reduced by both preparations, but to a greater extent by the depot form. The tocolytic efficacy and the tolerance were rated as "good" in 70% and 75% respectively with fenoterol depot and in 69% and in 71% respectively in the case of fenoterol. The maternal pulse rate remained at the level reached at the end of Partusisten infusion with the two preparation, and the blood pressure fluctuated slightly within the normal range.(ABSTRACT TRUNCATED AT 250 WORDS)

Blood Pressure↗
PubMed1986

Stereoselective formation of fenoterol-para-glucuronide and fenoterol-meta-glucuronide in rat hepatocytes and enterocytes.

The glucuronidation of fenoterol (Berotec, Partusisten) in isolated rat hepatocytes and enterocytes was investigated. Two different glucuronides, fenoterol para-glucuronide and fenoterol meta-glucuronide, were formed in proportions, that were constant over the concentration range investigated (0-1 mM). The fraction of para-glucuronide formed was 0.40 +/- 0.01 for hepatocytes and 0.54 +/- 0.01 for enterocytes. Fenoterol consists of a racemic mixture of SS'(+)fenoterol and RR'(-)fenoterol. The maximum glucuronidation rate of the (-)enantiomer (Vmax = 3.6 +/- 0.3 nmol/min/mg in hepatic microsomes and 3.4 +/- 0.1 nmol/min/mg in intestinal microsomes) is significantly lower than the same values of the (+)isomer (Vmax = 6.7 +/- 0.8 nmol/min/mg in hepatic microsomes and 5.8 +/- 0.4 nmol/min/mg in intestinal microsomes). Kmapp-values for the (-)enantiomer were lower than for the (+)enantiomer. Similar, but less pronounced, differences in Vmax were observed in isolated cells: Vmax = 148 +/- 13 and 372 +/- 50 pmol/min/mg [(-)fenoterol in hepatocytes and enterocytes], Vmax = 173 +/- 12 and 444 +/- 57 pmol/min/mg [(+)fenoterol in hepatocytes and enterocytes]. Calculation of intrinsic metabolic clearance (Clint = Vmax/Kmapp) from the cellular data suggests that the (+)enantiomer may be more efficiently eliminated by liver metabolism in vivo than the (-)enantiomer. This can result in stereoselective first-pass metabolism of the fenoterol enantiomers.

Animals↗
PubMed1999

Comparison between fenoterol and fenoterol plus oxitropium bromide delivered by metered-dose inhaler with InspirEase to relieve acute asthma attack.

Although the inhalation of beta2-agonists has frequently been used to relieve acute asthma attacks, the efficacy of anticholinergic agents for acute asthma attacks still remains unclear. This study was designed to compare the inhalation of fenoterol and the inhalation of fenoterol plus oxitropium bromide delivered by a metered-dose inhaler with holding chamber (InspirEase) to relieve acute asthma attacks. To accomplish this, 69 patients who had presented with an acute asthma attack were randomized to receive either fenoterol (1 puff [200 microg/puff] every 1 min for 5 min; total 1000 microg) or fenoterol plus oxitropium bromide (2 puffs [100 microg/puff] every 1 min for 5 min; total 1000 microg). The peak expiratory flow (PEF) and forced expiratory volume in 1 sec (FEV1) values were measured before treatment, and 1, 15, 30, and 60 min after the inhalation therapy. The ratios of improvement, PEF (or FEV1) after treatment divided by PEF (or FEV1) before treatment, were also calculated. Thirty-three patients were evaluated in the combination group and 31 patients were evaluated in the fenoterol group. The PEF value at 60 min after inhalation therapy of the fenoterol plus oxitropium bromide group (261 +/- 18 L/min, mean +/- standard error) was significantly higher compared to that of the fenoterol group (210 +/- 17 L/min). In addition, the ratios of improvement of PEF at 1, 15, 30, and 60 min after inhalation therapy were significantly higher in the fenoterol plus oxitropium bromide group compared with the fenoterol group.

Acute Disease↗
PubMed1990

Radioimmunological determination of fenoterol. Part II: Antiserum and tracer for the determination of fenoterol.

A radioimmunological method for the determination of the concentration of fenoterol in biological samples is described. The mixture of antibodies against the enantiomers of fenoterol obtained with the selected hapten shows a high affinity for racemic fenoterol and for the monoiodo125-fenoterol used as a tracer, which is also present as a racemate. The limit of detection of the radioimmunoassay for fenoterol (racemate) in biological samples (plasma, urine) is 10-20 pg/ml. The precision and accuracy of the radioimmunoassay, in the presence of racemic fenoterol, are sufficient for an analysis and meaningful interpretation of samples from human pharmacokinetic studies. A relationship between the cross-reactivity of the antibodies against fenoterol and a preferred conformation of the fenoterol molecule in aqueous solution is discussed.

Animals↗
PubMedDate not supplied

[Tocolysis with fenoterol suppositories--a comparison with oral administration of fenoterol tablets].

A new application form of fenoterol (Partusisten) as 15 mg suppositories from Boehringer Ingelheim was tested for its tocolytic effect, tolerance and the main side effects under usual clinical conditions in a prospective study in 50 pregnant patients with premature labour in 24-36th week of gestation. During one week's treatment 25 pregnant women received 3 to 4 15 mg fenoterol suppositories and 25 patients 6 to 8 5 mg fenoterol tablets. Beginning on the second day of treatment until the end of therapy in both groups a reduction of the uterine activity of at least 50 percent was achieved. The uterine relaxant effect was sufficient until 3 to 4 hours after the application of fenoterol tablets and 6 to 8 hours after the application of fenoterol suppositories. Side effects were mainly limited to cardiovascular complaints, restlessness and tremor, and we found no significant difference between tablets and suppositories. The maternal heart rate reached its highest level on the second day of treatment. Fenoterol suppositories can be recommended in all cases, where an oral tocolytic therapy is not possible e.g. in cases of vomiting or before operations. Here the application of fenoterol suppositories can replace in some cases the intravenous infusion of fenoterol.

Administration, Oral↗
PubMed1980

[Efficency of tocoylsis by fenoterol and fenoterol in combination with a beta-1-blocking compound (author's transl)].

In 35 pregnant women threatening premature labour and cervic dilatation indicated therapy by a beta-mimetic compound (fenoterol) for tocolysis. 17 patients (group I) got fenoterol-monotherapy; in 18 patients (group II) fenoterol was combined with the cardioselective beta-1-blocking agent metoprolol. There were no differences in age, bodyweight and time of gestation in both groups before therapy; also the obstetric states--as compared by pelvic score (Bishop) and tocolysis index (Baumgarten)--were nearly identical. Efficiency of tocolytic therapy was evaluated by prolongation index (Richter) and tocolysis-success-score (Weidinger). Statistical analysis comparing these parameters in both groups showed no significant differences. Heartrate, however, was significantly (p > 0,005) lower in patients treated by fenoterol and metoprolol, thus indicating less cardial stress induced by fenoterol. In conclusion the combination of the semiselective beta-2-stimulating compound fenoterol with the beta-1-blocking agent metoprolol is proposed for tocolytic therapy because of less cardial stress but identical tocolytic efficiency as compared with fenoterol-monotherapy.

Drug Therapy, Combination↗
PubMed1986

Bronchodilator effects of a fenoterol metered dose inhaler and fenoterol powder in asthmatics with poor inhaler technique.

Thirty-seven per cent of 204 consecutive asthmatic patients using metered dose inhalers (MDI) regularly had faulty inhaler technique. Twenty patients with poor technique volunteered for bronchomotor tests. The bronchodilator effects of 0.2 mg of fenoterol in MDI form, 0.2 mg of fenoterol in powder form and a placebo powder were compared. Mean peak expiratory flow (PEF) and forced expiratory volume in 1 s (FEV1) values after 0.2 mg of fenoterol in MDI form were only slightly different from those after placebo. Inhalation of 0.2 mg of fenoterol powder was, however, followed by a highly significant (p less than 0.001) increase in measured expiratory indices. PEF and FEV1 values were significantly higher after fenoterol powder than after fenoterol in MDI form (PEF, p less than 0.01 at 5 min, p less than 0.001 at 15 min, and p less than 0.05 at 60 min, FEV1, p less than 0.01 1 h after drug administration). Poor MDI technique can severely impair the effect of bronchodilator drugs. Use of a bronchodilator in powder form is more reliable in these patients.

Adolescent↗
PubMed1988

[Comparison of protective effects induced by the ultrasonic mist of nicardipine + fenoterol versus nicardipine + fenoterol + ipratropium bromide].

A comparison is presented of the protective effect of ultrasound mist induced by nicardipine + fenoterol and nicardipine + fenoterol + ipratropium bromide in a group of 11 patients with chronic bronchial asthma in a phase of relative clinical stability. The data collected show that the three-drug combination was more effective than the use of nicardipine and fenoterol.

Aerosols↗
PubMed1984

A comparison of effects of inhaling a combined preparation of fenoterol with ipratropium bromide (Duovent) with those of fenoterol and salbutamol.

The effects of inhaling an aerosol preparation containing fenoterol 200 micrograms and ipratropium bromide 80 micrograms were compared with those of inhaling 200 micrograms of salbutamol and a similar dose of fenoterol on 20 patients with chronic bronchitis and four patients with chronic stable asthma. The dose of each drug was contained in 2 puffs taken from a metered-dose inhaler. Changes in airways function were assessed by measuring peak expiratory flow rate. Pulse, blood pressure and presence of any tremor were monitored to detect drug-induced side effects. No significant difference was found in the onset of action and overall bronchodilator effects between the three drugs. The combined preparation was found to have a significantly greater bronchodilator action three and four hours after inhalation compared to the other two drugs. A significant effect lasting six hours was found with salbutamol and fenoterol, but the combined preparation had an effect which was significant up to seven hours. There was no significant difference in the side effects which were minimal for all three drugs.

Adult↗
PubMed1992

Treatment of acute wheezing and dyspnea attacks in children under 2 years old: inhalation of fenoterol plus ipratropium bromide versus fenoterol.

Two treatment regimens for the initial treatment of acute wheezing were evaluated in 61 wheezing infants. Thirty-one patients received fenoterol (F) (0.1 mg/kg) and placebo (P) and 30 patients received fenoterol (F) (0.1 mg/kg) plus a fixed dose of ipratropium bromide (IB) (50 micrograms). Both groups received the drugs by inhalation using an ultrasonic nebulizer and face mask. A clinical score system based on wheezing and rib cage retraction was established and evaluations were performed before and at 15, 30, and 45 minutes after treatment. After the last evaluation based on the clinical score, it was decided whether to repeat or not to repeat the treatment. Our results showed that a combination of a beta agonist and ipratropium bromide (FB) was more effective than a beta agonist alone (F) in reducing wheezing and dyspnea during an acute attack (63.4 versus 25.8%; p less than 0.05).

Acute Disease↗
PubMed1983

A comparison of fenoterol powder capsules and fenoterol metered dose spray in bronchial asthma.

In the present investigation the effect of fenoterol powder for inhalation has been compared to that of fenoterol spray in 20 adult patients with reversible obstructive lung disease. No difference could be demonstrated between the two forms of the drug in a randomized cross-over study. Neither was it possible to demonstrate any difference between the two preparations following the use of the drug at home over a minimum of four days, with regard to daily PEF registration and symptom scores. Nine of the patients preferred spray, six powder.

Adult↗
PubMed1982

The short-term bronchodilator effects of fenoterol and ipratropium in asthma.

We studied the bronchodilator effects of inhaled fenoterol, a relatively selective beta-2 adrenergic agent, and ipratropium an anticholinergic drug, singly and in combination in 10 patients with asthma. The period of observation was 6 hr after aerosol administration. The six drug regimens used were fenoterol 100 micrograms, fenoterol 200 micrograms fenoterol 50 micrograms combined with 20 micrograms of ipratropium, fenoterol 100 micrograms combined with 40 micrograms of ipratropium, 40 micrograms of ipratropium, and placebo. Measurements consisted of spirometry with determination of forced expiratory volume in one second (FEV1), maximal expiratory flow at 50% of vital capacity (V50), specific airway conductance, lung volumes, and heart rate. Bronchodilation with regimens containing fenoterol was rapid, with 75% of the maximum response achieved by 5 min, while the peak effect of ipratropium was delayed for 1 to 2 hr. Fenoterol 100 micrograms produced approximately half the degree of improvement in FEV1 and V50 compared with 200 micrograms of fenoterol. The addition of 40 micrograms of ipratropium to 100 micrograms of fenoterol resulted in bronchodilation equivalent to 200 micrograms fenoterol and was associated with a more prolonged effect than fenoterol 100 micrograms. Tremor was observed in two-subjects inhaling fenoterol 200 micrograms but was not observed with any other regimen. It is concluded that the combination of inhaled ipratropium and fenoterol is an effective bronchodilator in asthma, achieving efficacy similar to that of fenoterol alone but with fewer side effects.

Adult↗
PubMed1996

Cardiovascular safety of high doses of inhaled fenoterol and albuterol in acute severe asthma.

BACKGROUND: It has been suggested that overuse of fenoterol metered-dose inhalers (MDIs) may increase the risk of death from asthma due to cardiac arrhythmias. Our primary objective was to compare the cardiovascular safety of fenoterol and albuterol MDIs when administered in maximal bronchodilating or maximal tolerated doses to an absolute maximum of 16 puffs, for the emergency department (ED) treatment of acute severe asthma. METHODS: Asthmatic patients presenting to the ED with acute severe asthma (FEV1 less than 50% of predicted) were enrolled in a multicenter, randomized, double-blind, parallel-group study. Following baseline measurements, (medical history, physical examination, determination of serum potassium and serum theophylline levels, oximetry, 12-lead ECG, and spirometry), each patient received 4 puffs of either fenoterol, 200 micrograms per puff, or albuterol, 100 micrograms per puff, 1 puff every 30 s via an MDI attached to a holding chamber. Additional doses of inhaled beta 2-agonist were administered by dose titration, 2 puffs every 10 min to a maximal cumulative dose of 16 puffs of albuterol or fenoterol, side effects were intolerable to the patient, or an FEV1 plateau (i.e., < 10% improvement for 2 consecutive doses) occurred. ECG was recorded continuously via Holter monitor, and respiratory rate, BP, dyspnea (Borg scale), and FEV1 were assessed after each dose. RESULTS: 128 patients were randomized to receive fenoterol and 129 to receive albuterol. Overall, fenoterol increased FEV1 160 mL more than albuterol. The mean (SEM) FEV1 increase from baseline was 0.75 +/- 0.06 L in the fenoterol group and 0.59 +/- 0.06 L in the albuterol group (p < 0.03). Both beta 2-agonists caused a decrease in serum potassium level that was significantly greater in the fenoterol (0.23 +/- 0.04 mmol/L) than in the salbutamol (0.06 +/- 0.03 mmol/L) group (p = 0.0002). There was also a greater increase in the Q-Tc interval in the fenoterol group, 0.011 +/- 0.003 s compared with 0.003 +/- 0.003 s in the albuterol group (p < 0.05). Differences in hypokalemia and Q-Tc prolongation associated with fenoterol and albuterol were significantly different only after 8 puffs of fenoterol had been given. 32 patients exhibited ventricular premature beats, 14 in the fenoterol group and 18 in the albuterol group. There were 34 patients with episodes of supraventricular premature beats, 17 in each group. No episodes of sustained ventricular tachycardia were detected in either group. CONCLUSIONS: In adequately oxygenated patients, using dose titration of fenoterol, in a formulation of 200 micrograms per puff by MDI valved holding chamber and mask, to a total dose of 3,200 micrograms and salbutamol (100 micrograms per puff) to a total dose of 1,600 micrograms over 90 min, showed cardiovascular safety in acute severe asthma. This was evidenced by absence of cardiovascular mortality or clinically significant arrhythmias in either group. The 100% greater dose of fenoterol improved FEV1 significantly more than salbutamol and was associated with a relatively small but significantly greater prolongation of the Q-Tc interval and decrease in serum potassium level. This study does not exclude the possibility that adverse cardiac events could occur with severe hypoxemia.

Acute Disease↗
PubMed1994

Determination of fenoterol and ractopamine in urine by enzyme immunoassay.

Fenoterol and ractopamine are phenethanolamines with beta-adrenergic agonist activity. An enzyme immunoassay (EIA) for these compounds was developed using antibodies raised in a New Zealand white rabbit against fenoterol-bovine serum albumin and fenoterol coupled to horseradish peroxidase (HRP). The calibration graphs of fenoterol and ractopamine showed linearity over the concentration ranges 0.1-5 and 0.2-25 ng ml-1, respectively. Isoxsuprine showed a cross-reactivity of 0.7% while the cross-reactivity of other beta-agonists was < 0.1%. The screening assay was used to detect fenoterol in urine samples obtained from an animal experiment in which male calves were treated with fenoterol (100 micrograms of fenoterol per kg of bodymass per meal for a period of four weeks). Using a direct method, without sample preparation, fenoterol concentrations ranged from 22 to 210 ng ml-1. The mean concentration of fenoterol after extraction in isobutanol was 3.5 times lower compared with the direct method. On applying enzymic hydrolysis in combination with isobutanol extraction, the mean concentration was eight times higher than that obtained when using extraction only. Gas chromatography-mass spectrometry (GC-MS) analysis confirmed the presence of fenoterol in most of these samples. However, probably owing to the absence of a proper GC-MS internal standard, the correlation between GC-MS and EIA concentrations was low (r = 0.7976). In general, the concentrations found by the EIA are much higher than those found by GC-MS, which might be caused by the presence of metabolites detected with the EIA. Fenoterol is excreted in urine mostly (about 85%) as glucuronidated-sulfated conjugate. The antibodies partly recognize the conjugated fenoterol, which makes it possible to use a direct screening assay. In blank calf urine the detection limits, mean background +3 times the standard deviation, are 1.3 (fenoterol) and 2.6 ng ml-1 (ractopamine). In bovine urine, however, owing to matrix effects, the detection limits are 20 times higher.

Administration, Oral↗