Aclidinium bromide

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[edit] BRAND NAMES

[edit] STRUCTURE

Aclidinium bromide.jpg

[edit] MECHANISM OF ACTION

Aclidinium bromide is a competitive, selective muscarinic receptor antagonist (also known as an anticholinergic), with a longer residence time at the M3 receptors than the M2 receptors. M3 receptors mediate contraction of airway smooth muscle. Inhaled aclidinium bromide acts locally in the lungs to antagonise M3 receptors of airway smooth muscle and induce bronchodilation. Nonclinical in vitro and in vivo studies showed rapid, dose-dependent and long-lasting inhibition by aclidinium of acetylcholine-induced bronchoconstriction. Aclidinium bromide is quickly broken down in plasma, the level of systemic anticholinergic side effects is therefore low.

[edit] INDICATIONS

Aclidinium bromide is indicated as a maintenance bronchodilator treatment to relieve symptoms in adult patients with chronic obstructive pulmonary disease (COPD).

[edit] DOSAGE

The recommended dose is one inhalation of 322 µg aclidinium twice daily.

If a dose is missed the next dose should be taken as soon as possible. However, if it is nearly time for the next dose, the missed dose should be skipped.

Elderly population No dose adjustments are required for elderly patients

[edit] CONTRAINDICATIONS

Hypersensitivity to aclidinium bromide, atropine or its derivatives, including ipratropium, oxitropium or tiotropium, or to the excipients

[edit] PRECAUTIONS

  • Asthma: Aclidinium bromide should not be used in asthma; clinical trials of aclidinium bromide in asthma have not been conducted
  • Paradoxical bronchospasm: As with other inhalation therapies, administration of Aclidinium bromide may cause paradoxical bronchospasm. If this occurs, treatment with Aclidinium bromide should be stopped and other treatments considered.
  • Deterioration of disease: Aclidinium bromide is a maintenance bronchodilator and should not be used for the relief of acute episodes of bronchospasm, i.e. as a rescue therapy. In the event of a change in COPD intensity while the patient is being treated with aclidinium bromide so that the patient considers additional rescue medication is required, a re-evaluation of the patient and the patients’ treatment regimen should be conducted.
  • Cardiovascular effects: Cardiovascular safety profile is characterized by the anticholinergic effects. Aclidinium bromide should be used with caution in patients with a myocardial infarction during the previous 6 months, unstable angina, newly diagnosed arrhythmia within the previous 3 months, or hospitalisation within the previous 12 months for heart failure functional classes III and IV as per the “New York Heart Association”. Such patients were excluded from the clinical trials and these conditions may be affected by the anticholinergic mechanism of action.
  • Anticholinergic activity: Dry mouth, which has been observed with anticholinergic treatment, may in the long term be associated with dental caries.
    Consistent with its anticholinergic activity, aclidinium bromide should be used with caution in patients with symptomatic prostatic hyperplasia or bladder-neck obstruction or with narrow-angle glaucoma (even though direct contact of the product with the eyes is very unlikely).

[edit] INTERACTIONS

Co-administration of aclidinium bromide with other anticholinergic-containing medicinal products has not been studied and is not recommended.

Although no formal in vivo drug interaction studies have been performed, inhaled aclidinium bromide has been used concomitantly with other COPD medicinal products including sympathomimetic bronchodilators, methylxanthines, and oral and inhaled steroids without clinical evidence of drug interactions.

In vitro studies have shown that aclidinium bromide or the metabolites of aclidinium bromide at the therapeutic dose are not expected to cause interactions with P-glycoprotein (P-gp) substrate drugs or drugs metabolised by cytochrome P450 (CYP450) enzymes and esterases

[edit] PREGNANCY AND LACTATION

  • Pregnancy: Aclidinium bromide should only be used during pregnancy if the expected benefits outweigh the potential risks.
  • Breast-feeding: It is unknown whether aclidinium bromide and/or its metabolites are excreted in human milk. As animal studies have shown excretion of small amounts of aclidinium bromide and/or metabolites into milk, a decision must be made whether to discontinue breast-feeding or to discontinue therapy with aclidinium bromide taking into account the benefit of breast-feeding for the child and the benefit of long-term aclidinium bromide therapy to the woman.

[edit] SIDE EFFECTS

The most frequently reported adverse reactions with Aclidinium bromide were headache (6.6%) and nasopharyngitis (5.5%).

[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