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Pulmonary – Treatable traits
Published in Vibeke Backer, Peter G. Gibson, Ian D. Pavord, The Asthmas, 2023
Vibeke Backer, Peter G. Gibson, Ian D. Pavord
Short-acting beta2 agonists called SABA (Salbutamol, Terbutaline) are widely used as rescue symptomatic therapy. Long-acting beta2 agonists called LABA (Salmeterol, Formoterol, Vilanterol) are currently generally recommended as the first choice for patients who have symptoms that persist despite regular inhaled corticosteroids. Salmeterol is a partial agonist of the beta2 receptor whilst formoterol is a full agonist. Both appear to have similar clinical effects, but formoterol has a more rapid onset of action. Side effects of tachycardia, tremor and muscle cramps are rarely a problem unless given in high doses. Clinically important tachyphylaxis to the airway smooth muscle effects of LABA is not thought to occur.
The Pharmacotherapy of Rhinitis and Asthma
Published in Pudupakkam K Vedanthan, Harold S Nelson, Shripad N Agashe, PA Mahesh, Rohit Katial, Textbook of Allergy for the Clinician, 2021
Amanda Grippen Goddard, Harold S. Nelson, Rohit Katial, Flavia Hoyte
Step 2 in the GINA report suggests using daily low dose ICS with as needed SABA or as needed low dose ICS-formoterol for preferred controller treatment. The preferred reliever treatment for both Step 1 and Step 2 is as needed low dose ICS-formoterol.
Long-Acting Inhaled Beta2 Receptor Agonist Drugs
Published in Richard Beasley, Neil E. Pearce, The Role of Beta Receptor Agonist Therapy in Asthma Mortality, 2020
Salmeterol has been shown to have a relaxant effect on isolated guinea pig trachea and human bronchial tissue lasting for many hours.20 A prolonged bronchodilator effect of formoterol has also been demonstrated in vitro. In one study,19 the remaining beta-stimulating effect on isolated guinea pig trachea after washout and continuous flushing of the organ baths for 1 h for salbutamol (0.1 μM) was only 9 ± 4%, whereas for formoterol (10 nM) it was 78 ± 7% and for salmeterol (50 nAf) it was 93 ± 7%. In this study, the duration of the relaxation after continuous washing was longer for salmeterol than for formoterol.19 In other in vitro experimental models and with different choices of doses, the difference between salmeterol and formoterol has been more pronounced with a longer relaxant effect for salmeterol than for formoterol.18,21,22 In a study of the effects of salmeterol, formoterol, and salbutamol on the binding of [125I]iodopindolol ([125I]PIN), a beta antagonist, in rat lung membranes, both salmeterol and formoterol had similar affinities (53 and 76 nM, respectively) compared with 2.5 μM for salbutamol. Preincubation of membranes with salmeterol prevented [125I]PIN binding, but both salbutamol and formoterol were rapidly displaced by [125I]PIN.22 Similar studies are needed in human lung membrane preparations.
Investigation of potential substandard dry powder inhalers on EU and North African markets – evaluation of the delivered and fine particle doses
Published in Journal of Drug Assessment, 2022
Yue Zhang, Philippe Hubert, Cédric Hubert
Since the discovery of falsified Symbicort 320/9 Turbohaler in the UK, no cases of substandard or falsified inhaler formulations have been reported to European health authorities. Statistically, due to their high profitability, the pharmaceuticals most affected by falsification or poor quality are antibiotics, antiretrovirals, antimalarials, anticancer drugs and vaccines. Despite the limited data available on the inhalers, the risk of poor quality or falsified products is perhaps low but still present, therefore this work aimed to investigate the current situation of formoterol-containing inhalers in Europe and North Africa. It also extended the examination of potential falsified or substandard DPIs to a different formulation: capsule-based DPIs. More specifically, this work focused on formoterol fumarate delivered by Aerolizer. Formoterol is a long-acting ß-agonist indicated in asthma and COPD treatments3,6. It can be administrated in monotherapy or combined with another active molecule within the same formulation, e.g. in combination with an inhaled corticosteroid (ICS) when the ICS monotherapy can no longer control asthma3,6.
Impact of chronic medications in the perioperative period: mechanisms of action and adverse drug effects (Part I)
Published in Postgraduate Medicine, 2021
Ofelia Loani Elvir-Lazo, Paul F White, Hillenn Cruz Eng, Firuz Yumul, Raissa Chua, Roya Yumul
Beta agonists exert their clinical effects by mimicking effects of the endogenous catecholamines (e.g. norepinephrine, epinephrine, and dopamine) on adrenergic receptors. As inhaled agents, they have greater selectivity for β2-adrenergic receptors located on the airway of smooth muscles. The activation of these receptors leads to a cascade of intracellular signaling, resulting in the inhibition of myosin light-chain phosphorylation producing bronchodilation and airway smooth muscle dilation [36]. Inhaled beta agonists are mainstays for the treatment of respiratory disorders, including asthma and COPD. Salmeterol is metabolized by cytochrome P450 CYP3A4, and formoterol CYP2D6, 2C9, and 2C19. Salmeterol should be used with caution in patients taking strong 3A4 inhibitors. Formoterol should be used with caution when combined with drugs that prolonged the QT interval [37].
Step-up and step-down approaches in the treatment of asthma
Published in Expert Review of Respiratory Medicine, 2021
Mario Cazzola, Maria Gabriella Matera, Paola Rogliani, Luigino Calzetta, Josuel Ora
The available literature indicates the advantage of using what is now defined as ‘anti-inflammatory reliever therapy’ compared to SABAs in both intermittent and mild asthma [16]. The recommendation to use ICS/formoterol as needed or, alternatively, an ICS whenever a SABA is taken in Step 1 is due to the need to avoid severe exacerbations and also to standardize the approach to the patient with mild asthma, regardless whether at Step 1 or Step 2 [14]. Actually, since ICSs cause rapid clinical effects and can suppress airway inflammation within hours [17], there are clinical advantages over the traditional as-needed inhaled rapid-onset β2-agonists alone in patients with different degrees of asthma severity when an ICS is combined with a rapid-onset β2-agonist [18]. Formoterol has a rapid onset of action like salbutamol with the additional benefit of longer-lasting bronchodilation [19].