Formoterol 3-agonist

Salmeterol and formoterol are long-acting inhaled p2-agonists that provide up to 12 hours of bronchodilation after a single dose. Both agents are approved for the chronic prevention of... 

Long-Acting p2 Agonists Formoterol Inhalation 1-3 minutes 1-3 hours 12 hours Powder (12 mcg/inhalation)... 

Several recent articles describe the ring-opening of chiral epoxides under microwave irradiation conditions (see also Scheme 6.103). In the context of the preparation of novel /32-adrenoceptor agonists related to formoterol and salmeterol, Fairhurst and a team from Novartis have described the synthesis of chiral ethanolamines by solvent-free microwave-assisted ring-opening of a suitable chiral epoxide precursor with secondary benzylated amines (Scheme 6.129) [262]. At 110 °C, the reaction occurred... 

P-Agonists Albuterol Sahneterol Formoterol P -adrenergic receptor ADRp2... 

Orciprenaline is a partially selective adrenoceptor-agonist and hence it is more likely to have effects on the cardiovascular system, such as arrhythmias, than the selective adrenoceptor-agonists, such as salbutamol, terbutaline and the long-acting beta-agonists salmeterol and formoterol. Orciprenaline is available only as tablets or syrup and can be prescribed to 4-year-old children. 

The majority of the marketed products are used for asthma and COPD. Typical agents that are used for these indications are fl2-agonists such as salbutamol (albuterol), Terbutalin or formoterol, corticosteroids such as budesonide, FUxotide or beclomethasone and mast-cell stabilizers such as sodium cromoglycate or nedocromil. 

Concomitant therapy-Can be used concomitantly with short-acting 2-agonists, inhaled or systemic corticosteroids, and theophylline therapy. A satisfactory clinical response to formoterol does not eliminate the need for continued treatment with an anti-inflammatory. 

When beginning treatment with formoterol, instruct patients who have been taking inhaled, short-acting 2-agonists on a regular basis (eg, 4 times/day) to... 

Patients receiving fluticasone propionate/salmeterol twice daily should not use salmeterol or other inhaled, long-acting 2-agonists (eg, formoterol) for... 

Budesonide/Formoterol (Symbicort) [Anti-inflammatory> Bronchodilator/Beta-2-Agonist] WARNING Long-acting... 

If asthma control is not optimal, conventional advice was to increase the ICS dose. However, it is now apparent, that the dose-response effect of ICS is rather flat, so that there is little improvement in lung function after doubling the dose of inhaled steroid. An alternative strategy is to add some other class of controller drug. Several studies have shown that the combination of ICS and salmeterol or formoterol was more effective than increasing the dose of inhaled corticosteroid in terms of lung function improvement, rescue /32-agonist use, symptom control, and frequency of mild and severe asthma exacerbations. 

A fixed combination of ICS plus long-acting P2-agonist, such as fluticasone/salmeterol or budes-onide/formoterol, is available and may simplify therapy. However, new insights in treating patients with these combinations on an as needed regimen in combination with a daily low dose maintenance therapy, is still debated. 

Formoterol is a long-acting selective beta2-adrenoceptor agonist that is more potent than salmeterol (1) and has a similar duration of action (12 hours) but a rapid onset of effect similar to that of salbutamol. It is available as a multidose, pressurized aerosol and as a dry powder inhaler, delivering 0.006 or 0.012 mg per dose. The usual dose is 0.012 mg bd. 

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