Antiasthmatics properties, effects & ideal usage
Antiasthmatics are medicines used to prevent and treat bronchial asthma. Today a distinction is made between two groups of drugs. The first group leads to rapid symptom relief. These include beta2 sympathomimetics such as salbutamol. The second group enables a longer-term control of the complaints. These include, for example, inhaled glucocorticoids, such as budesonide.
Synonymous words used: asthma medication.
1. Treatment of symptoms
Beta2 sympathomimetics are derived from adrenaline. They selectively stimulate the adrenergic β2 receptors of the bronchial muscles and thus have a bronchospasmolytic effect. For rapid symptom relief, fast-acting active ingredients are usually administered by inhalation, for example with a metered dose aerosol or a powder inhaler. These type of antiasthmatics should only be used when necessary. An increase in administration suggests deterioration and insufficient control:
1- Fenoterol (Berodual®, combination)
2- Salbutamol (Ventolin®, generics)
3- Terbutaline (Bricanyl®)
Nonspecific sympathomimetics are not selective for beta2 receptors and can therefore cause more adverse effects. They are mainly used as a solution for injection to treat acute, severe asthma attacks:
Systemic glucocorticoids have anti-inflammatory properties and are used to prevent further progression in the event of acute deterioration. They are poorly tolerated when applied in the long term:
Cortisone tablets such as prednisolone (Spiricort®, generics)
Parasympatholytics are muscarinic receptor antagonists that neutralize the effects of the neurotransmitter acetylcholine and, thus, cause bronchodilation. They are derived from the tropane alkaloid atropine and are administered by inhalation. Parasympatholytics are less effective than sympathomimetics.
Ipratropium bromide (Atrovent®, generics)
2. Basic therapy
Inhaled glucocorticoids are anti-inflammatory agents which are used as first-choice antiasthmatics for the long-term treatment of bronchial asthma and are mainly administered locally as inhalations. They have immunosuppressive properties and can cause mouth fungus. Therefore, inhalation should be done before eating or the mouth should be rinsed after inhalation. Local application is better tolerated than systemic. Inhaled glucocorticoids are also combined with long-acting beta2 sympathomimetics.
1- Beclometasone (Qvar®)
2- Budesonide (Pulmicort®, generics)
3- Ciclesonide (Alvesco®)
4- Fluticasone Propionate (Axotide®)
5- Fluticasone Fuorate (Arnuity® Ellipta®)
6- Mometasone furoate (Atectura® Breezhaler®, combination)
7- Systemic glucocorticoids (see above)
Long-acting beta2 sympathomimetics are effective between 12 to 24 hours and enable a long-lasting effect. They should not be used as monotherapy in the long term:
1- Formoterol (Foradil®, Oxis®)
2- Indacaterol (Atectura® Breezhaler®, combination)
3- Salmeterol (Serevent®)
Note: The long-acting vilanterol is only available as a combination preparation (Relvar® Ellipta® with fluticasone furoate).
Leukotriene antagonists are anti-inflammatory and anti-allergic. These antiasthmatics bind to the CysLT1 receptor and thereby inhibit the effects of cysteinyl leukotrienes. These are strong inflammatory mediators that cause respiratory reactions such as constriction of the bronchi, mucus secretion, permeability of the blood vessels and the recruitment of inflammatory cells. They are given orally and are commonly used in children (montelukast):
1- Montelukast (Singulair®, generics)
2- Zafirlukast (Accolate®, out of trade)
3- Leukotriene synthesis inhibitors inhibit the formation of leukotrienes. They are not available in Switzerland: Zileuton (Zyflo®, USA)
Mast cell stabilizers prevent mast cell degranulation and thus counteract the release of inflammatory mediators that are involved in the inflammation of the mucous membranes and the narrowing of the airways. The drugs must be inhaled four times a day and are intended for long-term therapy:
1- Cromoglicic acid for asthma (Lomudal®, in Switzerland out of trade)
2- Nedocromil (in Switzerland out of trade)
3- Phosphodiesterase inhibitors are anti-inflammatory and / or bronchodilator. The effects are based on the inhibition of phosphodiesterases in inflammatory cells and the resulting increase in cAMP. This reduces the release of inflammatory mediators and the migration of neutrophils and eosinophils into the airways. Theophylline has a narrow therapeutic index and is toxic in overdose:
4- Theophylline (Euphyllin®, Unifyl®)
Monoclonal antibodies are specific antibodies that bind to human immunoglobulin E (IgE) or interleukin-5 (IL-5) and inactivate them:
1- Omalizumab (Xolair®) binds to IgE
2- Mepolizumab (Nucala®) and reslizumab (Cinqair® / Cinqaero®) bind to interleukin-5 and are given to treat eosinophilic asthma.
3- Benralizumab (Fasenra®) binds to the alpha subunit of the interleukin-5 receptor and is also injected into eosinophilic asthma.
Inhaled glucocorticoids and beta2 sympathomimetics:
1- Fluticasone Propionate and Salmeterol (Seretide®)
2- Fluticasone Propionate and Formoterol (Flutiform®)
3- Fluticasone furoate and vilanterol (Relvar® Ellipta®)
4- Budosenid and Formoterol (Symbicort®, Vannair®)
5- Beclometasone and Formoterol (Foster®)
6- Mometasone furoate and indacaterol (Atectura® Breezhaler®)
7- Parasympatholytics and Beta2-Sympathomimetics:
Ipratropium bromide and salbutamol (Dospir®, Ipramol®)
Ipratropium bromide and fenoterol (Berodual N®)
Parasympatholytics, beta2-sympathomimetics and inhaled glucocorticoids:
Glycopyrronium bromide, indacaterol and mometasone furoate (Enerzair® Breezhaler®)
Magistral formulations such as inhalation solution B are not commercially available as finished medicinal products and are prepared in a pharmacy on a doctor’s prescription. The active ingredients contained include sodium chloride, salbutamol, ipratropium bromide and dexpanthenol.
I hope this article was enabling you to understand the different properties and effects of antiasthmatics better.
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