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PubMedDate not supplied

Inhibition of interferon-gamma production from lymphocytes stimulated with food antigens by a beta 2-agonist, procaterol, in patients with food-sensitive atopic dermatitis.

Procaterol hydrochloride is a relatively new beta 2-selective agonist with a unique carbostyril nucleus. In this study, procaterol dose-dependently inhibited IFN-gamma production of peripheral blood mononuclear cells stimulated with ovalbumin in patients with hen's egg-sensitive atopic dermatitis, without inhibition of proliferative responses of peripheral blood mononuclear cells. Our results suggest that procaterol also has an effect as an immunomodulator, in addition to its effect as a beta 2-selective agonist.

Adrenergic beta-Agonists↗
PubMed1990

Agonist-induced desensitization of beta-adrenoceptor function in humans. Subtype-selective reduction in beta 1- or beta 2-adrenoceptor-mediated physiological effects by xamoterol or procaterol.

We investigated the effects of beta 2- (procaterol 2 x 50 micrograms/day for 9 days) and beta 1- (xamoterol 2 x 200 mg/day for 14 days) adrenoceptor agonists on lymphocyte beta 2-adrenoceptor density and beta 1- and beta 2-adrenoceptor in vivo function (assessed as isoprenaline-infusion-evoked hemodynamic effects and exercise-induced tachycardia) in healthy volunteers. Procaterol decreased lymphocyte beta 2-adrenoceptor density and all beta 2-adrenoceptor-mediated in vivo effects but did not affect beta 1-adrenoceptor-mediated in vivo effects. In contrast, xamoterol neither affected lymphocyte beta 2-adrenoceptors nor beta 2-adrenoceptor-mediated in vivo effects but decreased beta 1-adrenoceptor-mediated in vivo effects. It is concluded that in humans, generally long-term application of beta 1- or beta 2-adrenoceptor agonists causes desensitization of beta-adrenoceptor function but in a beta-adrenoceptor subtype-selective fashion.

Adrenergic beta-Agonists↗
PubMed2005

Pharmacodynamic equivalence study of CFC-free and CFC-containing procaterol hydrochloride metered-dose inhalers.

Equivalence between a CFC-free procaterol hydrochloride metered-dose inhaler using HFA-227 as a propellant (Meptin [HFA]) and a CFC-containing procaterol hydrochloride metered-dose inhaler (Meptin [CFC]) was assessed in 28 patients with bronchial asthma. The study was conducted in a randomized, double-dummy, double-blind crossover manner, using forced expiratory volume in the first second (FEV1) as an index of bronchodilatory effect. In Period I, the patients received 20 microg of either Meptin [HFA] or Meptin [CFC] and then crossed over in Period II after a washout interval of 3-28 days. Pharmacodynamic equivalence was assessed using AUC (FEV1)/h and peak FEV1 as indices, and the data was analyzed by analysis of variance. Factors used for the analysis were the treatment group and/or carryover effect, patients within each group, period, and treatment. The 90% confidence intervals for the differences between the two treatments were -0.0507 to 0.0039 (L) for mean AUC (FEV1)/h and -0.056 to 0.026 (L) for mean peak FEV1, both within the acceptance criteria of -0.15 to 0.15 (L). Meptin [HFA] was therefore assessed as being equivalent to the current Meptin [CFC].

Administration, Inhalation↗
PubMed1989

Inhibitory actions of procaterol, a beta-2 stimulant, on substance P-induced cough in normal subjects during upper respiratory tract infection.

We studied substance P (SP)-induced cough in normal subjects without and with colds, and the effects of orally administered procaterol on SP-induced cough in normal subjects with colds. SP aerosols caused cough at a concentration of approximately 10(-15) M in subjects with colds whereas it did not cause cough at a concentration of up to 10(-5) M in subjects without colds. Procaterol (50 micrograms) completely inhibited SP-induced cough in normal subjects with colds. These results suggest that cough response to SP remarkably increases during colds and that beta-2 stimulant may be a useful tool for treatment of cough during colds in normal subjects.

Adrenergic beta-Agonists↗
PubMed2002

[beta 2-adrenoceptor polymorphism and effect of inhaled beta 2-stimulant (procaterol) on airway resistance measured by body plethysmography in healthy volunteers].

This study was designed to evaluate, in healthy volunteers, differences of bronchodilator responsiveness to a beta 2-agonist between those with the Arg 16/Gly 16 allele and those with the Gly 16/Gly 16 allele at codon 16 of beta 2 adrenoceptor polymorphism. Peak flow and pulmonary functions were measured by body plethysmography after the inhalation of procaterol. In the Arg 16/Gly 16 group, the resulting acute increase of V 25 and acute decrease of airway resistance were greater, and the bronchodilator effect of a single inhaled beta 2-agonist was longer, than those observed in the Gly 16/Gly 16 group. The present study showed that a single inhalation of procaterol has a varying bronchodilator effect on healthy adults, depending on the genotype of beta 2 adrenoceptor polymorphism at codon 16.

Administration, Inhalation↗
PubMed1985

Therapeutic efficacy and equivalence of tablet and syrup formulations of procaterol hydrochloride in childhood asthma.

It has been reported that albuterol syrup produces more improvement in pulmonary function and greater increases in heart rate than an equal dose of albuterol tablets in asthmatic children. Consequently, tablet and syrup formulations of a new beta 2-adrenergic drug, procaterol hydrochloride, were tested for efficacy and equivalence. The two formulations were compared after the first dose and after 1 week of double-blind treatment in 11 children. Statistical analyses indicated that there were few significant differences in the bronchodilating efficacy of the tablet and syrup formulations. Improvement in pulmonary function began within one-half hour postdose and continued until four to six hours postdose. Increases in heart rate were small. Adverse effects were similar for the two formulations. Five patients showed minimal electrocardiogram changes. Tremor, reported by four patients, was the only other adverse effect. In conclusion, the tablet and syrup formulations of procaterol hydrochloride were equivalent in bronchodilating efficacy and safety in childhood asthma.

Adrenergic beta-Agonists↗
PubMed1985

Procaterol metered-dose inhaler in adults with asthma.

Procaterol hydrochloride is a new sympathomimetic amine which is highly selective for beta-2 receptors. The drug has been previously studied in the oral dosage form and has been found to be an effective bronchodilator with a prolonged duration of action. The present study evaluated the procaterol metered-dose inhaler (in comparison to placebo) in 30 adult patients with asthma during a 2-week treatment period. The drug was shown to be an effective bronchodilator with a prolonged duration of action.

Adult↗
PubMed1987

[Comparison of the bronchodilating activity of procaterol and nicardipine in chronic forms of bronchial asthma].

The bronchodilatory activity of one beta 2-stimulation (procaterol) and one calcium antagonist (nicardipine) both recently introduced was compared in a group of chronic asthmatics in the clinical remission phase. The experiment took the form of the randomised double blind administration of procaterol or nicardipine or a placebo twice a day for 15 days with spirometric tests being performed before, during and after the experiment. The results show that nicardipine does have a bronchodilatory effect though less than the beta 2-stimulant.

Adult↗
PubMed1993

Preventive effect and duration of action of disodium cromoglycate and procaterol on exercise-induced asthma in asthmatic children.

We evaluated the preventive effect and duration of action of disodium cromoglycate (DSCG) and procaterol nebulizer solutions on exercise-induced asthma (EIA) in 14 asthmatic patients. Disodium cromoglycate solution prevented EIA one hour after inhalation in 11 out of 14 (78.6%), and in some patients after four (36.5%) and eight hours (15.4%). The preventive effect and duration of action of DSCG depended on the severity of EIA in each subject. Procaterol solution had a greater effect than DSCG at any time point in the study. With both drugs, however, the effect decreased four and eight hours after inhaling and was related to the severity of the EIA.

Administration, Inhalation↗
PubMed1996

Effect of paper spacer (spader) in conjunction with procaterol metered dose inhaler in the treatment of acute asthma.

Thirty acute asthmatic patients (mean age 35.6 +/- 13.5 years, mean FEV1 0.97 +/- 0.95 L) in the emergency room were evaluated for airway response to procaterol administered by metered-dose inhaler (MDI) compared to MDI with auxiliary device (a paper spacer) in a randomised cross over study. Bronchodilator response to procaterol delivered by MDI, with paper spacer was significantly greater than that by MDI without spacer (mean maximal increment of FEV1, 0.67 +/- 0.46 vs 0.59 +/- 0.46 L, p = 0.016, mean maximal increment of PEFR, 112 +/- 62.3 vs 86.7 +/- 61.3 L/min, p = 0.003) but there was no difference in dyspnoea score, wheezing score and heart rate. This collapsible and portable auxiliary device (paper spacer) can increase therapeutic efficacy of bronchodilator response in asthmatic patients.

Acute Disease↗
PubMed1979

Alterations in blood levels of carbohydrate and lipid metabolites and of cyclic AMP mediated by beta1- and beta2-adrenoceptors in beagle dogs: effects of procaterol, a new selective beta2-adrenoceptor agonist.

The intravenous injection of isoprenaline (10 nmole/kg) into conscious beagle dogs caused significant increases in the blood level of lactate, glucose, FFA, insulin and cyclic AMP. These metabolic alterations induced by isoprenaline were blocked completely by pretreatment of the dog with propranolol (1 mg/kg). Butoxamine (10 mg/kg) antagonized isoprenaline-induced increases in glucose, lactate and insulin, but not the increases in FFA. Practolol (10 mg/kg) diminished the increase in blood FFA very strongly. Salbutamol, which is known to be an agonist of the beta 2-subtype in its bronchomotor and cardiovascular actions, produced marked increases in the blood concentrations of lactate, glucose and insulin but were without effect on the FFA level. Thus metabolic responses of conscious beagle dogs to beta-adrenoceptor agonists appeared to depend differentially on two types of beta-adrenoceptors: beta1-adrenoceptors are largely involved in lipolysis while beta2-adrenoceptors are involved in the regulation of blood glucose metabolism and insulin secretion. A new beta-adrenoceptor agonist, 5-(1-hydroxy-2-isopropylaminobutyl)-8-hydroxycarbostyril hydrochloride hemihydrate (Procaterol), was classified as a beta 2-agonist, because it markedly increased plasma concentrations of glucose, lactate and insulin but increased the plasma level of FFA to a lesser degree. The order of potency of beta2-agonists was procaterol greater than salbutamol greater than trimetoquinol. Metabolic responses of beagle dogs would be useful for appreciating the selectivity and potency of beta-adrenoceptor agonists and antagonists.

Adrenergic beta-Agonists↗
PubMedDate not supplied

Efficacy and duration of action of procaterol, a new bronchodilator.

Procaterol, a new beta-adrenergic agonist, was tested in two different doses in patients with reversible airway obstruction. Single oral doses of 0.05 or 0.1 mg produce an increase in measured expiratory flow rates, and the peak and duration of action are both dose related. Side effects reported during this one-day study were similar to those described with other compounds of this class; they were considered to be mild by the patients and the investigator. From these results, further investigation of this agent in bronchoconstrictive disease appears warranted.

Adult↗
PubMed1987

Kinetics of procaterol auto-oxidation in buffered acid solutions.

The kinetics of procaterol (1) degradation in buffered acidic solutions (pH 4-6) was investigated using an HPLC procedure. The effect of temperature and ferric ions on the reaction rate was estimated. In acidic solutions, 1 undergoes pseudo first-order degradation with an induction period. The first-order rate constant for degradation increased and the induction period decreased with an increase in pH. Ferric ions catalyzed the degradation reaction and decreased the induction period. At pH 6, the activation energy of the reaction was 34.5 kcal/mol/deg. The results of this study indicate that 1 in solution is more stable at acidic pH, in the absence of heavy metal ions, and protected from air.

Bronchodilator Agents↗
PubMed2002

Airway responsiveness and airway remodeling after chronic exposure to procaterol and fenoterol in guinea pigs in vivo.

BACKGROUND: Chronic exposure to fenoterol (FEN), a beta(2)-adrenergic receptor (beta(2)-AR) agonist, was shown to induce both airway hyperresponsiveness and airway remodeling in experimental animals. OBJECTIVE: We wanted to know the effects of chronic exposure to procaterol (PRO), a beta(2)-AR agonist, on airway function and structure, because this agent is widely used as a bronchodilator in Japan. For comparison, the effects of FEN were also examined. METHODS: Aerosolized PRO (0.1 or 1 mg/ml), FEN (1 mg/ml) or vehicle (0.9% NaCl) was given to guinea pigs 3 times a day for 6 weeks. Sublaryngeal deposition of these agents was calculated using radioisotopes. At 72 h after the last inhalation of PRO, FEN or vehicle, the dose-response relationship between lung resistance (R(L)) and intravenously administered acetylcholine (ACh) was measured. After measuring R(L), histological changes in noncartilaginous airway dimensions were evaluated. RESULTS: The amount of sublaryngeal deposition of 0.1 mg/ml PRO in the present study was speculated to be 100 times larger than that of therapeutic dose. ACh concentrations causing 2-fold, 10-fold and maximal increases in R(L) were not different in 4 groups tested. In the smaller membranous airways (<0.4 mm in diameter), but not the larger ones, thickening of adventitial areas was significantly greater in animals treated with beta(2)-AR agonists than in control animals (23 and 25, and 96% higher in animals treated with 0.1 and 1 mg/ml PRO or 1 mg/ml FEN, respectively). The degree of the increase was significantly less in PRO-treated animals than in FEN-treated animals (p < 0.01). CONCLUSION: Our results did not provide any evidence that regular inhalation of PRO at the therapeutic dose might induce bronchial hyperresponsiveness. In addition, huge amounts of PRO only caused a mild thickening of the adventitial areas, suggesting that PRO may be a weak inducer of airway remodeling compared with FEN.

Administration, Inhalation↗
PubMed1984

Inhibition of exercise-induced asthma by oral procaterol, a new beta 2-adrenergic drug.

8 asthmatics were studied for 2 consecutive days in order to assess the preventive effect of a new oral beta 2-sympathomimetic, procaterol hydrochloride, against exercise-induced asthma. Statistical analysis of the resulting data showed that this preparation, unlike other oral beta 2-sympathomimetics, affords good protection against exercise-induced asthma.

Adolescent↗
PubMed1992

Comparison of the modulatory effect of ketotifen, sodium cromoglycate, procaterol and salbutamol in human skin, lung and tonsil mast cells.

To assess the influence of mast cell heterogeneity on the inhibition of mediator release by drugs, the effects of ketotifen, sodium cromoglycate and beta-adrenoceptor agonists were examined against IgE-dependent histamine and prostaglandin D2 release from enzymatically dispersed human skin, lung and tonsillar mast cells. At high concentrations, ketotifen was an inhibitor of histamine and prostaglandin D2 release from lung and tonsillar mast cells. No cross-tachyphylaxis with sodium cromoglycate was seen. In skin mast cells no inhibition of mediator release was observed with 1.0 microM ketotifen, above which histamine release was induced. Sodium cromoglycate was a weak inhibitor of histamine and prostaglandin D2 release from lung and tonsillar mast cells and showed tachyphylaxis. Sodium cromoglycate did not inhibit histamine and prostaglandin D2 release from skin mast cells. On the other hand, no heterogeneity was observed with the beta-adrenoceptor agonists, procaterol and salbutamol. beta-Adrenoceptor stimulants were significantly more effective in inhibiting prostaglandin D2 than histamine release. No tachyphylaxis was seen with prolongation of the incubation time before challenge. Our results suggest that human mast cells are heterogeneous with respect to the modulation of mediator release by ketotifen and sodium cromoglycate but not beta-adrenoceptor agonists.

Albuterol↗
PubMed1989

Synthesis and pharmacological evaluation of procaterol derivatives having a tert-amino group.

A series of procaterol derivatives having a tert-amino group was synthesized. Among them, a morpholino derivative (4a, R1 = H, NR2R3 = morpholino) showed beta-selective and rather potent adrenoceptor stimulant activities in an in vivo assay using anesthetized dogs. On the other hand, a morpholinopropanol analogue (4j, R1 = CH3, NR2R3 = morpholino) showed 400 times less potent bronchodilator activity than that of 4a. Some of the compounds showed weak bronchodilator activities and weak effects on the heart. It seems that steric hindrance around the nitrogen atom of catecholamines has a significant influence on beta-adrenoceptor stimulant activities. Compound 4a also showed anti-allergic action estimated in terms of the inhibition of homologous passive cutaneous anaphylaxis in rats.

Adrenergic beta-Agonists↗
PubMed1989

Synthesis of procaterol derivative having a piperidylmethanol group and its beta-adrenoceptor stimulant activities.

A procaterol derivative (6) having a piperidylmethanol group was synthesized by the nucleophilic reaction of a 5-formylcarbostyril derivative with pyridyllithium, followed by selective catalytic reductions to afford the erythro-isomer. Compound 6 showed non-selective beta-adrenoceptor agonist activities like those of l-isoproterenol in an in vivo assay using anesthetized dogs.

Adrenergic beta-Agonists↗