ATC Group: R03A Adrenergics, inhalants

Clenbuterol is a direct-acting β2 sympathomimetic agent for the treatment of chronic obstructive airway diseases.

Epinephrine is a direct acting sympathomimetic agent, which exerts effects on both α and β adrenoceptors. It has more pronounced effects on β than on α adrenoceptors, although α effects prevail at high doses. The effects of adrenaline include increased rate and force of cardiac contraction, cutaneous vasoconstriction and broncho-dilatation.

Formoterol is a predominantly selective β₂-stimulator. Formoterol has bronchodilator activity in patients with reversible obstructive airway diseases. In humans formoterol is effective in the prophylaxis of bronchospasm induced by methacholine challenge.

Aclidinium is a long-acting muscarinic antagonist (also known as an anticholinergic) and formoterol is a long-acting β₂-adrenergic agonist. The combination of these substances with different mechanisms of action results in additive efficacy compared to that achieved with either component alone. Relaxation of both central and peripheral airways with combination treatment may contribute to the beneficial effects of aclidinium/formoterol combination on lung function.

Combination of two bronchodilators: glycopyrronium, a long-acting muscarinic antagonist (also referred to as an anticholinergic), and formoterol, a long-acting β₂-adrenergic agonist with a rapid onset of action.

Indacaterol is a partial agonist at the human beta₂-adrenergic receptor with nanomolar potency. When inhaled, indacaterol acts locally in the lung as a bronchodilator. In isolated human bronchus, indacaterol has a rapid onset of action and a long duration of action.

When inhaled, indacaterol acts locally in the lung as a bronchodilator. Indacaterol is a partial agonist at the human beta₂-adrenergic receptor with nanomolar potency. In isolated human bronchus, indacaterol has a rapid onset of action and a long duration of action. Mometasone furoate is a synthetic corticosteroid with high affinity for glucocorticoid receptors and local anti-inflammatory properties. In vitro, mometasone furoate inhibits the release of leukotrienes from leukocytes of allergic patients.

Isoprenaline is a potent non selective beta-adrenergic agonist with low affinity for alphaadrenergic receptors. Isoprenaline acts primarily on the heart and on smooth muscle of bronchi, skeletal muscle vasculature and the gastrointestinal tract.

Olodaterol has a high affinity and high selectivity to the human beta₂-adrenoceptor. The compound exerts its pharmacological effects by binding and activation of beta₂-adrenoceptors after topical administration by inhalation. Activation of these receptors in the airways results in a stimulation of intracellular adenyl cyclase, an enzyme that mediates the synthesis of cyclic-3',5' adenosine monophosphate (cAMP). Elevated levels of cAMP induce bronchodilation by relaxation of airway smooth muscle cells.

Fixed dose combination containing a long acting muscarinic receptor antagonist, tiotropium and a long acting beta₂-adrenergic agonist, olodaterol (LAMA/LABA). The two active ingredients provide additive bronchodilation due to their different mode of action. Since muscarinic receptors appear to be more prominent in the central airways while β₂ adrenoceptors have a higher expression level in the peripheral airways, a combination of tiotropium and olodaterol should provide optimal bronchodilatation in all regions of the lungs.

Orciprenaline sulphate is a bronchodilating agent. The bronchospasm associated with various pulmonary diseases-chronic bronchitis, pulmonary emphysema, bronchial asthma, silicosis, tuberculosis, sarcoidosis and carcinoma of the lung, has been successfully reversed by therapy with orciprenaline sulphate.

Procaterol is an intermediate-acting β2 adrenoreceptor agonist used for the treatment of dyspnea caused by bronchial asthma, chronic bronchitis, and pulmonary emphysema.

Salbutamol is a selective β₂-agonist providing short-acting (4-6 hour) bronchodilation with a fast onset (within 5 minutes) in reversible airways obstruction. At therapeutic doses it acts on the β₂-adrenoceptors of bronchial muscle. Salbutamol is administered for the symptomatic relief of bronchospasm associated with chronic or acute asthma, bronchitis or other obstructive pulmonary diseases.

Salmeterol is a selective long-acting (12 hour) β₂ adrenoceptor agonist. These pharmacological properties of salmeterol offer more effective protection against histamine-induced bronchoconstriction and produce a longer duration of bronchodilation, lasting for at least 12 hours, than recommended doses of conventional short-acting β₂ agonists.

Terbutaline is a selective beta₂-adrenoceptor agonist, thus producing relaxation of bronchial smooth muscle, inhibition of the release of endogenous spasmogens, inhibitions of oedema caused by endogenous mediators, increased mucociliary clearance and relaxation of the uterine muscle.

Vilanterol is a selective long-acting, beta₂-adrenergic agonist (LABA). The pharmacologic effects of beta₂-adrenoceptor agonist active substances, including vilanterol, are at least in part attributable to stimulation of intracellular adenylate cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.

Fluticasone furoate is a synthetic trifluorinated corticosteroid with potent anti-inflammatory activity. Vilanterol trifenatate is a selective long-acting, beta₂-adrenergic agonist (LABA). Molecular interactions occur between corticosteroids and LABAs, whereby steroids activate the beta₂-receptor gene, increasing receptor number and sensitivity and LABAs prime the glucocorticoid receptor for steroid-dependent activation and enhance cell nuclear translocation.

Umeclidinium/vilanterol is a combination inhaled long-acting muscarinic receptor antagonist/long-acting beta₂-adrenergic agonist (LAMA/LABA). Following oral inhalation both compounds act locally on airways to produce bronchodilation by separate mechanisms.