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Pharmacology: Bronchodilative Action: The bronchodilative action of procaterol HCl was comparable to or more potent than that of isoproterenol, and more potent than that of salbutamol and orciprenaline, as determined by inhibition on increased pulmonary resistance in dogs, cats and guinea pigs.
The onset of the bronchodilative action is observed 1-5 min after inhalation in conscious guinea pigs and anesthesized dogs, indicating much faster onset of action than the tablet formulation.
Inhaled procaterol HCl dilates not only the central airway but also peripheral airways in pediatric asthma patients.
Duration of Bronchodilative Action: Procaterol HCl had a longer duration of brochodilative action than isoproterenol, trimetoquinol, orciprenaline, and salbutamol in dogs, cats and guinea pigs.
The potency with which procaterol HCl at 10 mcg by inhalation inhibits the increase in airway resistance due to histamine is equal to that of salbutamol at 200 mcg by inhalation in anesthesized dogs. However, procaterol is longer-acting than salbutamol.
Selectivity for β2-Adrenergic Receptors (Organ Selectivity): The selectivity of procaterol HCl for β-adrenergic receptors in the respiratory system was greater than that for such receptors in the cardiovascular system, as compared to isoproterenol, trimetoquinol, orciprenaline, and salbutamol in dogs, cats and guinea pigs.
Antiallergic Action: Procaterol HCl exhibited a definite antiallergic action by inhibiting antigen-induced increase in airway resistance, the passive cutaneous anaphylaxis (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 allergen inhalation in bronchial asthma patients, as compared to isoproterenol, trimetoquinol, orciprenaline and salbutamol.
Effects on the Respiratory Tract System: Procaterol HCl accelerated ciliary movement in airways of pigeons.
Effect on Exercised-Induced Asthmatic Attacks: Procaterol HCl suppressed treadmill exercise-induced asthmatic attacks in patients with bronchial asthma.
Pharmacokinetics: Plasma Concentrations: When Meptin Air was administered by inhalation to 6 healthy male subjects as 4 doses (40 mcg per subject as procaterol HCl*), a peak plasma concentration of 128 pg/mL was attained at 15 min post-dosing followed by a gradual decline.
Urinary Excretion: When Meptin Air was administered by inhalation as 4 doses (40 mcg per subject as procaterol HCl), 14.36% of the dose was excreted in the urine within 24 hrs post-dosing.
Cytochrome (CYP)-450 Isoenzyme for Hepatic Oxidized Metabolism of Drugs: The enzyme is mainly CYP3A4 (in vitro).
*The approved dose for a single administration of Meptin Air is 20 mcg.
