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Pharmacology: Bronchodilator Action: Bronchodilator action of procaterol HCl was determined to be equipotent or more potent than that of isoproterenol and more potent than salbutamol and orciprenaline in terms of its inhibitory activity on an increase in pulmonary resistance in dogs, cats and guinea pigs.
Duration of Action: The duration of action of procaterol HCl was longer than that of isoproterenol, trimetoquinol, orciprenaline and salbutamol in dogs, cats and guinea pigs.
Selectivity for β2-Adrenergic Receptors: Procaterol HCl showed a greater selective action for β2-receptors in the respiratory system than on those in the cardiovascular system in comparison to isoproterenol, trimetoquinol, orciprenaline and salbutamol in dog, cat and guinea pig studies.
Antiallergic Action: Procaterol HCl exhibited a definite antiallergic action by inhibiting antibody-induced increases in airway resistance, the PCA reaction and histamine release from sensitized lung tissues in guinea pigs and rats, as well as allergen-induced skin reactions, and increases in asthmatic responses to antibody inhalation in bronchial asthma patients, as compared to isoproterenol, trimetoquinol, orciprenaline and salbutamol. Procaterol HCl also inhibited allergen-induced delayed-type and immediate-type bronchial responses.
Effect on Accelerated Airway Hypersensitivity: Procaterol HCl inhibited airway hypersensitivity accelerated by the inoculation of influenza virus C in dogs.
Inhibitory Effect on Exercise-Induced Asthma Episodes: The results of treadmill or ergometer exercise or methacoline loading tests suggest that procaterol HCl suppresses exercise-induced asthma attacks in patients with bronchial asthma.
Pharmacokinetics: Plasma Concentrations: When procaterol HCl was administered orally to 6 healthy male subjects at single doses of 50 and 100 mcg/subject, the following plasma concentration curves and pharmacokinetic parameters were obtained. (See table and figure.)
Click on icon to see table/diagram/image
Click on icon to see table/diagram/imageUrinary Excretion: When procaterol HCl was administered orally as single doses of 50 and 100 mcg/subject, 9.93% and 11.65% of the dose were excreted in the urine within 24 hrs post-dosing, respectively.
