Antiasthmatics

1. symptom treatment

Beta2-sympathomimetics are derived from epinephrine. They selectively stimulate the adrenergic β2-receptors of bronchial muscles and thus have a bronchospasmolytic effect. For rapid symptom relief, fast-acting agents are usually administered by inhalation, for example, with a metered-dose inhaler or a powder inhaler. They should be used only when needed. An increase in administration suggests worsening and inadequate control:

Nonspecific sympathomimetics are not selective for beta2 receptors and therefore may cause more adverse effects. They are mainly used as injectable solutions to treat acute, severe asthma attacks:

  • Epinephrine
  • Ephedrine
  • Isoprenaline

Systemic glucocorticoids have anti-inflammatory properties and are used in acute exacerbations to prevent further progression. They are poorly tolerated when used in the longer term:

Parasympatholytics are muscarinic receptor antagonists that abolish the effects of the neurotransmitter acetylcholine, causing bronchodilatation. They are derived from the tropane alkaloid atropine and are administered by inhalation. Parasympatholytics are considered less effective than sympathomimetics.

Theophylline non-retarded, see below.

2. basic therapy

Inhaled glucocorticoids are anti-inflammatory agents that are used as 1st-line agents for the long-term treatment of bronchial asthma and are administered primarily locally as inhalations. They have immunosuppressive properties and can cause oral 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.

  • Beclometasone (Qvar)
  • Budesonide (Pulmicort, generic).
  • Ciclesonide (Alvesco)
  • Fluticasone propionate (Axotide)
  • Fluticasone fuorate (Arnuity Ellipta)
  • Mometasone furoate (Atectura Breezhaler, combination).

Systemic glucocorticoids (see above) Long-acting beta2-sympathomimetics are effective between 12 to 24 hours and provide a long-lasting effect. They should not be used as monotherapy in the longer term:

Note: The long-acting vilanterol is available only as a combination preparation (Relvar Ellipta with fluticasone furoate). Leukotriene antagonists are anti-inflammatory and anti-allergic. They bind to the CysLT1 receptor, thereby inhibiting the effects of cysteinyl leukotrienes. These are potent inflammatory mediators that cause airway responses such as bronchoconstriction, mucus secretion, blood vessel permeability, and inflammatory cell recruitment. They are administered orally and are often used in children (montelukast):

Leukotriene synthesis inhibitors inhibit the formation of leukotrienes. They are not available in many countries:

Mast cell stabilizers prevent degranulation of mast cells, thereby counteracting the release of inflammatory mediators involved in mucosal inflammation and airway constriction. The drugs must be inhaled four times daily and are intended for continuous therapy:

  • Cromoglicic acid for asthma (Lomudal, out of trade in many countries).
  • Nedocromil (out of trade in many countries).

Phosphodiesterase inhibitors are anti-inflammatory and/or bronchodilators. The effects are based on the inhibition of phosphodiesterases in inflammatory cells and the consequent increase in cAMP. This decreases the release of inflammatory mediators and the migration of neutrophils and eosinophils into the airways. Theophylline has a narrow therapeutic range and is toxic in overdose:

  • Theophylline (Euphyllin, Unifyl)

Monoclonal antibodies are specific antibodies that bind to and inactivate human immunoglobulin E (IgE) or interleukin-5 (IL-5):

  • Omalizumab (Xolair) binds to IgE.
  • Mepolizumab (Nucala) and reslizumab (Cinqair / Cinqaero) bind to interleukin-5 and are administered to treat eosinophilic asthma.
  • Benralizumab (Fasenra) binds to the alpha subunit of the interleukin-5 receptor and is also injected for eosinophilic asthma.

Combinations

Inhaled glucocorticoids and beta2-sympathomimetics:

Parasympatholytics and beta2-sympathomimetics:

Parasympatholytics, beta2-sympathomimetics, and inhaled glucocorticoids:

Extemporaneous preparations, such as inhalation solution B, are not commercially available as finished medicinal products and are prepared in a pharmacy on prescription. The active ingredients contained include sodium chloride, salbutamol, ipratropium bromide and dexpanthenol.