Fenoterol

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[edit] BRAND NAMES

[edit] STRUCTURE

Fenoterol.jpg

[edit] MECHANISM OF ACTION

Fenoterol is a short-acting Beta2 adrenergic receptor agonist.

Beta2 receptors are the predominant adrenergic receptors in bronchial smooth muscle. The binding of Fenoterol to Beta2 adrenergic receptors in bronchial smooth muscle, activates the intracellular adenylate cyclase, an enzyme which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP). The increase of cAMP determines:

  • Bronchodilation: Increased intracellular cyclic AMP (cAMP), increases the activation of cAMP-dependent protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellular calcium levels within the muscle. Lower levels of calcium cause relaxation of the smooth muscle and therefore bronchodilatation.
  • Inhibition of the release of mast cell mediators.
  • Increased mucociliary clearance.

In high doses fenoterol also affects the striated muscles (tremor) and the the β1-receptors (heart side effects) and has an influence on lipid and sugar metabolism (lipolysis, glycogenolysis and hyperglycaemia) and relative hypokalaemia due to increased K+ uptake in the skeletal muscle.
Due to the density of β2-receptors in the myometrium, fenoterol also relaxes the uterine muscles. This effect is particularly pronounced in the pregnant uterus and at considerably higher doses.

Following inhalation, bronchodilatation is induced within a few minutes and the effect persists for 3 – 5 hours.

[edit] INDICATIONS

Fenoterol is used to relieve and prevent bronchospasm associated with asthma, chronic bronchitis, emphysema and other pulmonary disorders where bronchospasm is a complicating factor.

[edit] DOSAGE

A single dose of one or two inhalations (0.2-0.4 mg) to control bronchospasm. If required, this dose of 1 or 2 inhalations may be repeated up to 4 times daily. With repeated dosing, drug should not be given more often than every 4 hours. Patients should not exceed a total of 8 inhalations per day

[edit] CONTRAINDICATIONS

[edit] PRECAUTIONS

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

[edit] SIDE EFFECTS

Generally, fenoterol is well tolerated and many people will not experience unwanted effects. The severity and duration of these effects are dependant on many factors including duration of therapy, dose, route of administration and individual response. Possible unwanted effects include:

  • nervousness
  • slight palpitations
  • fine tremor
  • headache
  • dizziness
  • cough
  • bad taste

Uncommon:

  • increased heart rate
  • nausea
  • muscle cramps
  • weakness

Many of these unwanted effects, especially the most common ones, may disappear with continued use.

Rare:

  • restlessness
  • irritability

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Asthma / Chronic obstructive pulmonary disease (COPD)
Adrenergics, inhalants Short acting β2-agonists Fenoterol (Berotec)   Levosalbutamol (Xopenex)   Salbutamol (Ventolin)   Terbutaline (Bricanyl)
Long acting β2-agonists (LABA) Arformoterol (Brovana)   Clenbuterol (Spiropent)   Formoterol (Foradil)   Salmeterol (Serevent)
Ultra long acting β2-agonists Indacaterol   Olodaterol   Vilanterol
Inhaled corticosteroids Beclomethasone (Inhaler)   Budesonide (Inhaler)   Ciclesonide (Inhaler)   Flunisolide (Inhalation suspension)   Fluticasone (Inhaler)   Mometasone (Inhaler)
Anticholinergics (Muscarinic antagonists) Aclidinium bromide   Glycopyrronium bromide   Ipratropium bromide   Oxitropium bromide (Inhalation suspension)   Tiotropium bromide
Mast cell stabilizers Cromoglicate   Nedocromil
Monoclonal anti-IgE antibody Omalizumab
Xanthine derivatives Aminophylline   Bamifylline   Doxofylline   Dyphylline   Theophylline
Eicosanoid inhibition Leukotriene antagonists Montelukast   Pranlukast   Zafirlukast
Thromboxane receptor antagonists Ramatroban   Seratrodast
Non-xanthine PDE4 inhibitors Ibudilast   Roflumilast
Combination products Corticosteroid + Long acting Beta2 agonist Beclomethasone/Formoterol (Inhaler)   Fluticasone/Salmeterol (Inhaler)   Fluticasone/Vilanterol   Mometasone/Formoterol
Corticosteroid + Short acting Beta2 agonist Beclomethasone/Salbutamol   Salbutamol/Flunisolide (Inhalation suspension)   Salbutamol/Flunisolide (Inhaler)
Short acting Beta2 agonist + Muscarinic antagonist Fenoterol/Ipratropium bromide (Inhaler)   Levosalbutamol/Ipratropium   Salbutamol/Ipratropium bromide