ICD-10 Specific code J45: Asthma

Budesonide is a glucocorticosteroid with a high local anti-inflammatory effect. At doses clinically equivalent to systemically acting glucocorticosteroids, budesonide gives significantly less HPA axis suppression and has a lower impact on inflammatory markers.

Choline theophyllinate is the choline salt of theophylline. It has a strong bronchodilator action, due to the relaxation of the smooth muscle fibers of the bronchi.

Ciclesonide exhibits low binding affinity to the glucocorticoid-receptor. Once orally inhaled, ciclesonide is enzymatically converted in the lungs to the principal metabolite (C21-des-methylpropionyl-ciclesonide) which has a pronounced anti-inflammatory activity and is thus considered as the active metabolite.

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

Sodium cromoglicate (Cromoglicic acid) inhibits the activation of many of the cell types involved in the development and progression of asthma. Thus, sodium cromoglicate inhibits the release of inflammatory mediators including cytokines from mast cells and reduces the chemotactic activity of eosinophils and neutrophils.

Diprophylline is a xanthine derivative with pharmacologic actions similar to theophylline and other members of this class of drugs. Its primary action is that of bronchodilation, but it also exhibits peripheral vasodilatory and other smooth muscle relaxant activity to a lesser degree. The bronchodilatory action of dyphylline, as with other xanthines, is thought to be mediated through competitive inhibition of phosphodiesterase with a resulting increase in cyclic AMP producing relaxation of the bronchial smooth muscle. Diprophylline exerts its bronchodilatory effects directly and, unlike theophylline, is excreted unchanged by the kidneys without being metabolized by the liver. Because of this, dyphylline pharmacokinetics and plasma levels are not influenced by various factors that affect liver function and hepatic enzyme activity, such as smoking, age, congestive heart failure, or concomitant use of drugs which affect liver function.

Fluticasone has anti-inflammatory and vasoconstrictive features. Fluticasone given by inhalation at recommended doses has a potent glucocorticoid anti-inflammatory action within the lungs, resulting in a reduction of both symptoms and exacerbations of asthma, with a lower incidence and severity of adverse effects than those observed when corticosteroids are administered systemically.

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.

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.

Ipratropium is a quaternary ammonium compound with anticholinergic (parasympatholytic) properties. Ipratropium appears to inhibit vagally mediated reflexes by antagonising the action of acetylcholine, the transmitter agent released from the vagus nerve. Anticholinergics prevent the increase in intracellular concentration of Ca++, which is caused by interaction of acetylcholine with the muscarinic receptor on bronchial smooth muscle. Ca++ release is mediated by the second messenger system consisting of IP3 (inositol triphosphate) and DAG (diacylglycerol).

Ketotifen is a histamine H₁-receptor antagonist. In vivo animal studies and in vitro studies suggest the additional activities of mast cell stabilisation and inhibition of infiltration, activation and degranulation of eosinophils.

Methylprednisolone is a synthetic glucocorticoid and a methyl derivative of prednisolone. Methylprednisolone is a potent anti-inflammatory agent with the capacity to profoundly inhibit the immune system.

Nedocromil is a non-steroidal agent, which has anti-inflammatory properties when administered topically in the lung. In the treatment of bronchial asthma, nedocromil sodium reduces bronchospasm, cough and bronchial hyperreactivity and improves objective measurements of lung function.

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.

Prednisolone is a glucocorticoid which has anti-inflammatory activity. Naturally occurring glucocorticoids (hydrocortisone and cortisone), which also have salt-retaining properties, are used as replacement therapy in adrenocortical deficiency states. Their synthetic analogs are primarily used for their potent anti-inflammatory effects in disorders of many organ systems.

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.

Tiotropium is a long-acting, specific, muscarinic receptor antagonist, in clinical medicine often called an anticholinergic. By binding to the muscarinic receptors in the bronchial smooth musculature, tiotropium inhibits the cholinergic (bronchoconstrictive) effects of acetylcholine, released from parasympathetic nerve endings.

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.