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PubMedDate not supplied

Maximum bronchodilator effect of pirbuterol and procaterol administered as sprays with and without an aerochamber.

OBJECTIVE OF THE STUDY: To determine the maximal bronchodilator dose of procaterol and pirbuterol administered by inhalation with an without an aerochamber (Aerocâmera) to children with acute bronchial asthma attacks. TYPE OF STUDY: Prospective. 18 children (6-15 years of age) with acute bronchial asthma attacks (FEV1 < 80% of the predicted value) received pirbuterol (N = 10) or procaterol (N = 8) by metered-dose inhaler, one puff every 5 minutes, for a total of five doses. During another acute attack, the same patient received the same medication with the aid of a spacer (Aerocâmera). Clinical evaluation and pulmonary function tests were performed 5 minutes after each inhaled dose. RESULTS: For both drugs, maximal bronchodilation was obtained after the second dose. No significant side effects were observed even after procaterol doses of 50 micrograms or pirbuterol doses of 1000 micrograms. The results were unaffected by the use of the spacer. CONCLUSIONS: The doses that induced maximal bronchodilation were 400 micrograms pirbuterol and 20 micrograms procaterol. Although the spacer did not change the results, it is a valuable aid for patients who have difficulty in using the metered-dose inhaler (M.D.I.).

Administration, Inhalation↗
PubMedDate not supplied

Preparation of diastereomeric beta-d-glucuronides of the bronchodilator procaterol using immobilized rabbit liver microsomal enzymes.

Liver microsomal pellets from a phenobarbital induced New Zealand white male rabbit were prepared, solubilized, and reacted with cyanogen bromide activated Sepharose beads to form an immobilized microsomal enzyme preparation. Viability of bound enzymes was determined using established methods. Racemic erythro-[3H]-procaterol hydrochloride was incubated with immobilized microsomal enzymes at room temperature in 0.1 M potassium phosphate buffer (pH 7.4) together with cofactors magnesium chloride and UDPGA for 16 h. The incubation mixture was filtered and the filtrate fractionated by a C18 solid phase extraction procedure. Two polar reaction products were isolated and characterized by TLC, HPLC-RAM (homogeneous flow-through radioactivity detection), [1H]-NMR, and Fast-Atom Bombardment mass spectrometry as diastereomeric aryl-O-glucuronides of erythro-procaterol. Based on HPLC-RAM analysis, glucuronidation of racemic procaterol proceeds with regiostereoselectivity. In addition, both diastereomers are formed in nearly equal amounts indicating lack of enantioselectivity in this reaction. Combined yield of both diastereomers was approx. 60%.

Animals↗
PubMed1990

Evaluation of tremor and efficacy of oral procaterol in adult patients with asthma.

Tremor, the most common side effect of ordinary doses of beta 2-agonists, was evaluated in a quantitative manner and compared to improvement in pulmonary function in respect to time of onset, duration, peak effect, and tachyphylaxis with procaterol in adults. Forty-five adult patients with reversible obstructive airway disease were studied during administration of three different dosages of procaterol, 25 micrograms escalating to 100 micrograms, and 100 micrograms twice daily. Tremor was quantitatively evaluated with a Grass model accelerometer. The patients were evaluated during 8 hours approximately every 2 weeks for 8 weeks. Daily diaries of symptoms and side effects were also maintained. The study demonstrated no direct relationship between tremor and pulmonary function as far as time of onset, peak effect, or duration. Although tachyphylaxis was demonstrated, much of the tolerance developed to the tremor was explained by an increase in baseline tremor. Procaterol was demonstrated to be an effective bronchodilator, and tolerance to tremor was demonstrated to develop with time but is highly variable. There was not a direct relationship between tremor and pulmonary function, indicating possible differences between lung and peripheral muscle beta 2-receptors. It appeared that the best way to minimize the problem of tremor is to begin with a lower dose and increase the dose gradually during a period of weeks.

Administration, Oral↗
PubMed1981

erythro-5-[1-Hydroxy-2-(isopropylamino)butyl]-7-hydroxycarbostyril, a terbutaline-type derivative of the bronchodilator procaterol.

erythro-5-[1-Hydroxy-2-(isopropylamino)butyl]-7-hydroxycarbostyril (4), which is a terbutaline-type derivative of the bronchodilator procaterol, was synthesized by transfer of the 8-hydroxyl group of procaterol to the 7 position. Compound 4 showed less potent beta-adrenoceptor stimulant activities than procaterol or terbutaline in an in vitro test using guinea pig tracheal muscle and right atrium. In an in vivo assay on anesthetized dogs, compound 4 showed 42 times less bronchodilator activity and 87 times less effect on the heart rate than l-isoproterenol.

Animals↗
PubMed2001

Beta2-adrenergic receptor genotype-related changes in cAMP levels in peripheral blood mononuclear cells after multiple-dose oral procaterol.

PURPOSE: To evaluate the beta2-adrenergic receptor (beta2AR) genotype frequency in the Japanese population and the relationship between beta2AR genotype at amino acid position 16 (beta2AR-16) and desensitization to beta2-agonist ex vivo. METHODS: The beta2AR genotypes at amino acid positions 16, 27, and 164 of 92 healthy Japanese subjects were determined by polymerase chain reaction-restriction fragment-length polymorphism. The relationship between the beta2AR-16 genotype and the desensitization to beta2-agonist was examined in 10 male subjects ex vivo. Procaterol tablet (HCl salt, 50 microg, Meptin) was given orally for 5 days, and peripheral blood was obtained before and after 5 days of consecutive medications followed by the assessment of the intracellular cAMP levels in peripheral blood mononuclear cells after incubation with or without procaterol hydrochloride (0-1000 ng/mL). RESULTS: Allele frequency was Arg16:Gly16 = 46%:54%, Gln27: Glu27 = 92%:8%, and Thr164:Ile164 = 100%:0%, respectively. The cAMP levels were increased by incubation with procaterol hydrochloride, and the increase was suppressed after 5 days of consecutive medications. The suppression was more significant in the homozygote for Gly16 than the homozygote for Arg16. CONCLUSIONS: The desensitization to beta2-agonist was associated more frequently with the mutation at beta2AR-16 (Gly16).

Administration, Oral↗
PubMed1998

Inhaled procaterol inhibits histamine-induced airflow obstruction and microvascular leakage in guinea-pig airways with allergic inflammation.

BACKGROUND: Beta2-adrenoceptor agonists (beta2-agonists) are shown to inhibit airway microvascular leakage in experimental animals. This effect may change in animals with chronic airway inflammation. OBJECTIVE: We examined whether inhaled beta2-agonists inhibit microvascular leakage in guinea-pig airways with chronic allergic inflammation. METHODS: Three weeks after the sensitization with ovalbumin (OA; 6 mg/mL), each guinea pig was challenged with inhaled OA once a day for 1 or 3 weeks. Control animals without sensitization with OA also inhaled vehicle for OA (saline) for 3 weeks. One day after the last challenge, different doses of inhaled procaterol (1, 3 or 10 microg/mL) or vehicle was given to animals for 10 min after an anaesthesia. Fifteen minutes after the end of inhalation, the animals were given i.v. Evans blue dye (EB dye; 20 mg/kg), a marker of microvascular leakage, and then i.v. histamine (3 or 30 microg/kg) or vehicle. Lung resistance, a parameter of airflow obstruction, was measured for 6 min and the lungs were removed to calculate the amount of extravasated EB dye into the airways. RESULTS: A significant increase in eosinophil infiltration into the airways was seen in sensitized and challenged animals compared with control animals without sensitization. Among animals receiving antigenic exposure for either 0 (control), 1 or 3 weeks, 10 microg/mL procaterol significantly inhibited 30 microg/kg histamine-induced increase in EB dye extravasation to a similar degree (ranged from 28.7 to 69.8% inhibition) as well as that in lung resistance (more than 90% inhibition in all groups). The minimal dose of procaterol to inhibit 3 microg/kg histamine-induced microvascular leakage was not different between nonsensitized control animals and those sensitized and challenged for 3 weeks at all airway levels. CONCLUSION: Inhaled beta2-adrenoceptor agonists may be also potent in attenuating microvascular leakage even in the airways with chronic allergic inflammation.

Administration, Inhalation↗
PubMed1992

Effects of methacholine induced bronchoconstriction and procaterol induced bronchodilation on cough receptor sensitivity to inhaled capsaicin and tartaric acid.

BACKGROUND: The direct effect of bronchoconstriction on cough receptor sensitivity is unknown, and the antitussive effect of beta 2 adrenergic agonists in man has been controversial. This study was designed to throw light on these questions. METHODS: The threshold of the cough response to inhaled capsaicin, a stimulant acting on C fibre endings, and tartaric acid, a chemostimulant, was measured before and 10 minutes after inhalation of methacholine, which caused a nearly 20% fall in forced expiratory volume in one second (FEV1), in 14 normal subjects (study 1), and also before and 30 minutes after inhalation of procaterol (30 micrograms), placebo, and saline in eight normal subjects (study 2). Progressively increasing concentrations of capsaicin and tartaric acid solutions were inhaled for 15 seconds by mouth tidal breathing at one minute intervals and cough threshold was defined as the lowest concentration of capsaicin and tartaric acid that elicited five or more coughs. RESULTS: In study 1 the geometric mean values of the cough threshold of response to capsaicin and tartaric acid before methacholine callenge, 2.98 (GSE 1.30) micrograms/ml and 46.6 (1.22) mg/ml, were not significantly different from those of the response to methacholine inhalation, 3.45 (1.33) micrograms/ml and 32.9 (1.37) mg/ml. In study 2 the geometric mean value of the cough threshold of response to capsaicin before inhalation of procaterol (4.61 (GSE 1.84) micrograms/ml) was not different from that after inhalation of procaterol (4.61 (GSE 1.84) micrograms/ml), which had significant bronchodilator effects. The cough threshold was not altered by placebo or saline. CONCLUSIONS: These findings suggest that muscarinic receptor stimulation, bronchoconstriction, beta 2 receptor stimulation, or bronchodilation might have no direct effect on the sensitivity of the cough receptors in normal subjects.

Adult↗
PubMed1994

Changes in pulmonary function and cross-sectional area of trachea and bronchi in asthmatics following inhalation of procaterol hydrochloride and ipratropium bromide.

To determine the sites of action of inhaled adrenergic and anticholinergic bronchodilators, we used the acoustic reflection technique to measure airway area before and after administration of beta 2-selective adrenoreceptor agonist (procaterol hydrochloride) and quaternary anticholinergic agent (ipratropium bromide). Eight stable individuals with asthma (five men and three women; mean age, 34 +/- 12.7 yr) were studied on 2 days in single-blind randomized crossover fashion when they self-administered (using metered-dose inhaler) two puffs of either procaterol hydrochloride hemihydrate (10 micrograms/puff) or ipratropium bromide (20 micrograms/puff). Maximal expiratory flow-volume curve, specific airway resistance, and cross-sectional areas of three airway segments (extrathoracic tracheal, intrathoracic tracheal, and bronchial) were recorded at baseline and 15, 30, 60, and 120 min after drug administration. Both agents produced significant improvements in FEV1, FVC and forced expiratory flow at 50% of vital capacity (V50), and specific airway resistance (SRaw) as early as 15 min after drug administration. These effects were sustained for the 120 min monitoring period. However, all improvements were significantly greater for procaterol than for ipratropium. By contrast, there was no significant difference between drugs in the increased production in the cross-sectional areas of the three airway segments although there was a nonsignificant trend toward greater increases in tracheal area produced by the anticholinergic agent.(ABSTRACT TRUNCATED AT 250 WORDS)

Acoustics↗
PubMed1985

Effects of the selective beta 2-adrenergic agonists, procaterole and terbutaline, on protein secretion by rat submandibular glands.

We examined the secretory effects of two beta 2-adrenergic agonists, procaterole and terbutaline, on the submandibular glands of anesthetized rats. After stimulation with these agents with and without a range of antagonists (non-specific alpha- and beta-adrenergic blockers), submandibular saliva was collected. The flow rate, protein concentration, the electrophoretic patterns, and amino acid composition of saliva were examined. These parameters were compared with their counterparts in saliva stimulated with isoproterenol (IPR), with and without antagonists. Assessed by these criteria, secreted proteins were classified as the alpha- or beta-type. In addition, IPR-stimulated proteins were compared in submandibular saliva of rats chronically treated with IPR or procaterole. Both beta 2-agonists were potent secretagogues for the submandibular glands of rats. All beta-antagonists completely abolished the secretory effects elicited by both beta 2-agonists, with the exceptions of carteolol and propranolol. However, no blocking agent abolished the secretory effects of IPR (60 mg/kg). The types of proteins in all submandibular saliva samples elicited by both beta 2-agonists with and without antagonists were the beta-type. Enlargement of the submandibular glands was not observed in rats subjected to chronic administration of procaterole, nor were abnormal and additional proteins observed, as confirmed by electrophoresis and by the amino acid analyses.

Animals↗
PubMed1993

Synthesis and pharmacological evaluation of 7-substituted procaterol derivatives.

A series of procaterol derivatives having a substituent at the 7-position of the carbostyril moiety was synthesized. Halogenation of procaterol and its homologues gave the 7-halogeno derivatives (3). Nitration of the procaterol analogues afforded the 7-nitro derivatives (4), and the catalytic reduction of 4 gave the 7-amino derivatives (5). These compounds showed weak beta-adrenoceptor stimulant activities in anesthetized dog.

Adrenergic beta-Agonists↗
PubMed1989

New assessment of airway responsiveness. Effect of pretreatment with procaterol on allergen-induced bronchoconstriction.

We examined airway responsiveness to allergen inhalation using a novel technique by which dynamic compliance (Cdyn) and pulmonary resistance (Rl) are simultaneously calculated by Fourier-series analysis of flow and transpulmonary pressure during tidal breathing. C0 and C0.5 (Cdyn at the frequency of zero and 0.5 Hz, respectively) were computed using the regression line of Cdyn versus frequency measured at the fundamental and first three harmonics in each breathing cycle. First, the validity of this system was tested by comparing Rl, C0 and C0.5 during five consecutive breaths with those obtained by the conventional method. A good correlation was seen in Rl, C0 and C0.5 between the two methods. Second, we studied airway response to allergen inhalation before and after oral administration of a long-acting beta 2-stimulant (procaterol, 50 micrograms or 100 micrograms) or placebo in a double-blind crossover trial in six atopic asthmatic subjects. In control allergen inhalation tests by administration of placebo, Rl increased progressively, and C0.5, expressed as percentage of control compliance at zero frequency (C0.5/COcont), decreased progressively. After 100 micrograms procaterol, Rl response to allergen was almost completely inhibited. However, a decrease in C0.5/C0cont was still observed. These findings suggest that pretreatment of asthmatic patients with procaterol can release allergen-induced bronchoconstriction of the central airways, but cannot release that of the peripheral airways.

Adult↗
PubMed1993

Bronchial hyperresponsiveness changes after 5 months of regular procaterol inhalation therapy in asthmatic children.

It is well known that procaterol has more potent antiallergic properties than previous beta-stimulants. Thirteen children with asthma who could be controlled for 2 months with a regular procaterol aerosol given 4 times/day (10 micrograms/dose) were studied. Histamine challenges were performed before and an average of 5 months after the consecutive treatment. No significant differences were seen in peak expiratory flow values. PC20 increased significantly from 132.9 +/- 127.7 micrograms/ml to 762.4 +/- 1205.7 micrograms/ml after 5 months. These results suggest that asthmatic children who can be controlled with regular use of the beta-stimulant procaterol are likely to have a decreased bronchial hyperresponsiveness.

Administration, Inhalation↗
PubMed1989

[Comparative study of procaterol and salbutamol in single inhaled doses].

The bronchodilator effect of 0.02 mg of procaterol compared to 0.2 mg of salbutamol as a reference drug administered by single dose inhalation, has been tested in 15 asthmatic patients with a stable clinical situation, using a double-blind study. The clinical value of the administered dose was determined by FEV1, FEV 25-75%, PEF, MEF 50% FVC, SRaw, VC and FRC. These functional tests together with the evaluation of secondary and cardiovascular effects were performed every hour during a 12 hour period. The results revealed that the procaterol aerosol was more potent (although not statistically significant) than the salbutamol, and had a longer activity time. There were no differences in the secondary effects which were mild and transitory. These results suggest that procaterol is a potent bronchodilator, with a long-lasting activity and minimal cardiovascular and adverse side effects.

Adult↗
PubMedDate not supplied

[Procaterol in the prevention of recurrent asthmatic bronchitis. Double-blind study].

In a study in double-blind it has considered if the procaterol, given for a month, had been able to develop a preventive action in children affected from relapsing asthmatic bronchitis. For that the clinical symptomatology, the number of the contagious events and the consumption of the drugs have been valued for two following months. The patients who had taken the procaterol, presented a reduction of the contagious events, of the consumption of the drugs and of the spastic bronchus symptomatology in the first month of the treatment which continued in the second month. In spite of the development of the contagious events, in the third month, the pulmonary symptomatology resulted inferior in comparison with the group of check. It is likely than the treatment with procaterol avoids the arisen of the spastic-bronchus symptomatology for a rise of the threshold of bronchial re-established, consequent to the re-establishment of the mucous lesions.

Adrenergic beta-Agonists↗
PubMed1986

Protection against non-specific bronchial hyperreactivity and bronchodilating action of procaterol in atopics.

The efficacy of procaterol, a new selective beta 2-stimulant (by pressurized aerosol), and its protection against the effects of non-specific bronchial stimulation (fog test) was evaluated in ten hyperreactive seasonal atopics in an open trial of twelve days duration. Preliminary results had proved that single (10 micrograms) and repetitive (10 micrograms t.i.d.) doses of procaterol induced a strong bronchodilation. Accordingly the pre-medication with procaterol (10 micrograms) completely prevents the flow limitation subsequent to the non-specific bronchial stimulation.

Adult↗
PubMed1995

Effect of procaterol, a beta 2-adrenoceptor agonist, on skin whealing response caused by inflammatory mediators in asthmatic children.

BACKGROUND: Beta 2-adrenoceptor agonists have been shown to reduce allergen-induced skin whealing responses via inhibition of mediator release. OBJECTIVE: To study whether beta 2-adrenoceptor agonists have a direct action against inflammatory mediator-induced skin whealing responses. METHODS: We examined the effect of procaterol, a beta 2-adrenoceptor agonist, on skin whealing responses to histamine, platelet-activating factor (PAF), substance P, or bradykinin in eight asthmatic children in a double-blind, randomized, cross-over study. Two hours after taking procaterol (50 micrograms) or placebo orally, the subjects were given these mediators intradermally at a concentration of 10(-5) M. RESULTS: Procaterol has a small but significant inhibitory effect on wheal formation following the intradermal injection of histamine and PAF by an average of 15% (P < .05) and 18% (P < .05) respectively but not against substance P or bradykinin. CONCLUSIONS: Our results suggest that although beta 2-adrenoceptor agonists may have an inhibitory effect against plasma exudation from microvasculature in the human skin, bronchodilatory effects are more prominent.

Adolescent↗
PubMed1995

[Effects of dopexamine on the electrophysiologic changes during myocardial ischemia and comparison with fenoldopam and procaterol].

The effects of dopexamine (DPX), a new dopamine receptor agonist, on transmembrane potential and effective refractory period (ERP) of isolated guinea pig ventricular muscle superfused either with hypoxia or mimic ischemia perfusates were investigated by using intracellular microelectrode technique and compared with fenoldopam (FODA) and procaterol. DPX (3 x 10(-6) mol.L-1) was found to significantly reduce both the extent of decrease of resting potential, action potential amplitude and maximal upstroke velocity and the degree of shortening of action potential duration caused by hypoxia or ischemia. These effects of DPX were significantly greater than those of FODA and procaterol albeit the latter showed effects similar to DPX. DPX could not only lengthen the abbreviated ERP resulting from hypoxia, but also shorten the prolonged ERP caused by ischemia. This action of DPX was more evident than that of FODA and procaterol. The results reveal the potential advantages of DPX over other dopaminergic agonists in the antiarrhythmic activity during myocardial ischemia.

Action Potentials↗
PubMed1993

Prolonged bronchodilating effect of formoterol versus procaterol in bronchial asthma.

The tolerability and the duration of effect of 12 micrograms of formoterol and 25 micrograms of procaterol administered via metered-dose aerosol to 12 stable asthmatic patients were evaluated in a double-blind, placebo controlled trial. FEV1, pulse rate, and blood pressure were measured at baseline and every two hours after dosing for 12 hours. The bronchodilation peak was observed after two hours for both drugs. Formoterol induced a significant bronchodilating effect for 12 hours compared with both baseline and placebo values. With procaterol, significant bronchodilation occurred for six hours compared with baseline values and four hours compared with placebo. No significant changes were observed in pulse rate and blood pressure with either drug. Four subjects complained of muscle tremor after procaterol administration. We conclude that in subjects with stable asthma, inhaled formoterol at a dose of 12 micrograms maintains significant bronchodilation for 12 hours after dosing and is very well tolerated. Further studies are required to evaluate effectiveness and tolerability of high dose formoterol treatment in acute severe asthma therapy.

Adolescent↗