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The Development of Beta Receptor Agonist Drugs
Published in Richard Beasley, Neil E. Pearce, The Role of Beta Receptor Agonist Therapy in Asthma Mortality, 2020
Some of the newer beta2-selective drugs, for example, procaterol (OPC-2009),79-80 were shown to have significantly greater affinity for beta2 than beta1 receptors in vitro, but this was not paralleled by any major improvement in selectivity in in vivo experiments and the drug still caused cardiovascular side effects in clinical trials.81 Nevertheless, procaterol, because of its potency and good beta2-betai selectivity in vitro, also proved to be a useful pharmacological tool. It was used in functional studies designed to detect small populations of beta2 receptors in tissues containing predominantly betat receptors.80
Drug Targeting to the Lung: Chemical and Biochemical Considerations
Published in Anthony J. Hickey, Sandro R.P. da Rocha, Pharmaceutical Inhalation Aerosol Technology, 2019
Peter A. Crooks, Narsimha R. Penthala, Abeer M. Al-Ghananeem
β2-receptor agonists such as soterenol (2), fenoterol (3), and salbutamol (4) bind with approximately equal affinity to both β1- and β2-receptors, but apparently owe their selectivity to greater efficacy at the latter receptor (Minneman et al. 1979), whereas other agonists, such as procaterol (5), show greater affinity for β2-receptors (Rugg et al. 1978). In fact, procaterol is a particularly selective β2-adrenoceptor drug.
Adrenergic Agonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Other short-acting β2 adrenergic agonists are levalbuterol, bitolterol, fenoterol, isoetharine, metaproterenol, and procaterol. Levalbuterol is a dextro isomer of albuterol, which is a racemic mixture. It is β2 selective and formulated and used as an inhalation. Bitolterol is a β2 receptor selective agonist and a prodrug of the active colterol. After inhalation, duration of activity is 3–6 h. Fenoterol, a β2 receptor selective agonist, has duration of activity of 4–6 h, the effect of the drug starts immediately after inhalation. It binds to β1 receptors producing cardiac effects. It is discontinued from the market. Isoetharine is a β2 receptor selective agonist. MAO does not affect the drug and the metabolism is by COMT. It is formulated as an inhalation and is used in treating bronchoconstriction. Metaproterenol, a β2 receptor selective agonist belonging to the category of resorcinol bronchodilators is used long-termly for treating COPD, asthma, and bronchospasm. After administering orally, approximately 40% drug absorption takes place as the active form. It is usually resistant to COMT. It is not much β2 selective in comparison to terbutaline, so it may cause cardiac stimulation. While taking orally, the drug has a slow onset of action and the effect lasts up to 3 to 4 h. Inhalation produces an immediate effect. It may be used via oral route or by inhalation. Pirbuterol is a β2 receptor selective agonist and it is almost similar to albuterol. It is administered as an inhalation and effect lasts up to 3–4 h. Procaterol is a β2 receptor selective agonist and is administered as an inhalation. It has an immediate onset of activity and a 5-h duration of action (Brunton et al., 2011; Barisione et al., 2010).
Association of upper and lower airway eosinophilic inflammation with response to omalizumab in patients with severe asthma
Published in Journal of Asthma, 2020
Makoto Kurokawa, Toshiyuki Koya, Hiroyuki Takeuchi, Masachika Hayashi, Takuro Sakagami, Kojiro Ishioka, Yasuhiro Gon, Takashi Hasegawa, Toshiaki Kikuchi
Pulmonary function tests were performed using a spirometer (SpiroSift SP-470; Fukuda Densi, Tokyo, Japan) in accordance with the American Thoracic Society (ATS) guidelines. The FeNO was measured using an nitric oxide analyzer (Kimoto Denshi, Osaka, Japan) with an online method, which was consistent with a previous mutual consensus statement from the ATS/European Respiratory Society [13]. Sputum induction and processing were performed as previously described [14]. In brief, the participants received a procaterol (200 μg) pretreatment and subsequently inhaled a hypertonic saline solution (3% w/v) delivered with an ultrasonic nebulizer for 15 min. Cell differentials were calculated as the percentage of cells in the total sputum. The diagnosis of chronic rhinosinusitis (CRS) was judged by otologists, based on symptoms and CT findings according to the Lund–Mackay score.
Rocuronium anaphylaxis in a 7-year-old boy during the induction of anesthesia
Published in Immunological Medicine, 2018
Yoshiko Morimoto, Sakiko Satake, Aguri Kamitani, Manabu Yamada, Mutsumi Saitou, Yuki Torii, Rokuro Shiba, Chika Hadase, Toru Yamamoto
Eleven minutes after rocuronium administration, his lungs became difficult to ventilate with a bag and his airway pressure elevated to 25 mmHg. Bronchodilator procaterol hydrochloride (β2 stimulator) at 10 µg was inhalated. The patient’s lungs were hand-ventilated with 100% oxygen at 40 mmHg, and the fentanyl and remifentanil infusion were paused as the next arterial blood pressure reading was 61/26 mmHg. His oxygen saturation was noted to have decreased to 86%. Subcutaneous injection of 0.2 mg adrenaline with venous injection of 50 mg methylprednisolone was administered and signs of bronchospasm resolved. After intravenous injection of ephedrine at 0.4 mg/kg, his blood pressure normalized. By removing the sheets for surgery, urticarial eruptions on his trunk became apparent. A diagnosis of anaphylaxis was made. He received a bolus of hydroxyzine 10 mg and skin rash disappeared. Surgery was postponed about 1 h and the orthopedic surgeon and anesthetist reported the clinical course to his parent and the pediatric division. We proposed the plan to keep any pin tip over the patient’s skin (not internal) for the purpose of extracting pins without anesthesia next month. After reinitiation, surgery proceeded without incident. The next day, his pulse and blood pressure remained stable and he was successfully liberated from the ventilator support (Figure 1). He was discharged home on the fifth hospital day. The orthopedist extracted all pins without anesthesia next month.
Effect of pulmonary rehabilitation with assistive use of short-acting β2 agonist in COPD patients using long-acting bronchodilators
Published in Physiotherapy Theory and Practice, 2021
Yasuhiko Tsujimura, Tetsuo Hiramatsu, Eiji Kojima, Kazuyuki Tabira
Procaterol hydrochloride (Meptin® 10 µg, Otsuka Pharmaceutical Industry, Tokyo, Japan) was used as the SABA in this study. Prior to activities that would be expected to cause breathlessness, subjects were instructed to inhale 20 µg of procaterol hydrochloride. Subjects were instructed to inhale this medication a maximum of 2 inhalations 4 times per day, with at least 4 hours between uses. Subjects were also instructed to record when and how many times each day they used procaterol hydrochloride. Before the start of the study, each patient was instructed on how to inhale SABA and use the inhalation device properly.