Aclidinium bromide

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Aclidinium bromide
Aclidinium bromide.svg
Systematic (IUPAC) name
[(8R)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octan-8-yl] 2-hydroxy-2,2-dithiophen-2-ylacetate bromide
Clinical data
Trade names Bretaris Genuair, Eklira Genuair, Tudorza Pressair
Licence data US FDA:link
Pregnancy cat. C (US)
Legal status -only (US)
Routes Inhalational
Identifiers
CAS number 320345-99-1 N
ATC code R03BB05
PubChem CID 11519741
ChemSpider 9694529 N
UNII UQW7UF9N91 N
KEGG D08837 YesY
ChEBI CHEBI:65344 N
ChEMBL CHEMBL551466 N
Chemical data
Formula C26H30BrNO4S2 
Mol. mass 564.555 g/mol
 N (what is this?)  (verify)

Aclidinium bromide (INN) is a long-acting anticholinergic bronchodilator approved by the FDA in 2012 for use in the management of chronic obstructive pulmonary disease (COPD). Aclidinium bromide is an inhalation powder promoted by Forest Pharmaceuticals in the US under the trade name Tudorza Pressair. It is also manufactured and marketed by Menarini Pharmaceuticals in the EU under the trade name Bretaris Genuair, in the UK as Eklira Genuair and in the Canada as Tudorza Genuair.[1]

Medical Uses[edit]

Aclidinium bromide is used for maintenance treatment of chronic obstructive pulmonary disease (COPD), which includes chronic bronchitis and emphysema. It is not however used for acute exacerbations. [2]

Safety and Efficacy[edit]

Early clinical studies in healthy subjects have confirmed the low systemic bioavailability and favourable safety profile of single and multiple doses of aclidinium.[3] In a subsequent Phase IIb study, which included 464 patients with moderate to severe COPD, aclidinium displayed long-lasting bronchodilatory activity and was well tolerated.[4]

Adverse Effects[edit]

Adverse effects are mainly related to its antimuscarinic effects. Common adverse drug reactions (≥1% of patients) associated with alcidinium bromide therapy include: headache, diarrhea, vomiting, nasopharyngitis, cough, rhinitis, sinusitis, toothache, and falls. Disease-related concerns include: worsening symptoms of narrow-angle glaucoma, myasthenia gravis, and prostatic hyperplasia/bladder neck obstruction. Rarely (<1% of patients) treatment is associated with the following: AV block, cardiac failure, cardiopulmonary arrest, diabetes mellitus, osteoarthritis, xerostomia, and/or allergy (rash, angioedema, anaphylaxis). [5]

Dosage[edit]

The standard dose of Aclidinium Bromide is 400 mcg (one inhalation) twice daily, which is administered by a Pressair inhalation device. [6]

Mechanism of action[edit]

Aclidinium bromide is a muscarinic receptor antagonist, often referred to as an antimuscarinic or anticholinergic agent. It competitively and reversibly inhibits the action of acetylcholine at type 3 muscarinic (M3) receptors in bronchial smooth muscle. This leads to a reduction in smooth muscle contraction and mucus secretion and thus produces a bronchodilatory effect.[7][8]

Mode of Delivery[edit]

Administer via oral inhalation. Prior to first use, remove from sealed pouch immediately before use. Prior to each use, remove protective cap from Tudorza™ Pressair™ inhaler and prepare inhaler by pressing and releasing the green button (while keeping the green button straight up and avoiding tilting the inhaler). After this step, ensure that the inhaler is ready for use by the colored control window which should have changed from red to green. The green control window indicates the inhaler is ready for use. If the control window is red, retry activating the inhaler again by pressing and releasing the green button. Prior to inhaling the dose, exhale fully (do not exhale into the inhaler), then close lips tightly around the inhaler mouthpiece and inhale (rapidly, steadily, and deeply); do not hold the green button down while inhaling. Keep breathing in until a “click” is heard to ensure that the full dose has been given. Hold breath as long as possible, then breathe out slowly through nose. Ensure the dose was delivered correctly by observing the control window which should have changed from green to red. If the control window is still green, repeat inhalation steps. When control window has been verified as red, replace the protective cap for next use. [9]


References[edit]

  1. ^ http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm313052.htm
  2. ^ http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm313052.htm
  3. ^ Janset JM, Lamarca R, Garcia Gil E, Ferrer P. (2009). "Safety and pharmacokinetics of single doses of aclidinium bromide, a novel long-acting, inhaled antimuscarinic, in healthy subjects". Int J Clin Pharmacol Ther 47 (7): 460–468. PMID 19640353. 
  4. ^ Jones PW, Singh D, Bateman ED, Agusti A, Lamarca R, de Miquel G, Segarra R, Caracta C, Garcia Gil E. Efficacy and safety of twice-daily aclidinium bromide in COPD patients: the ATTAIN study. Eur Respir J. 2012 Oct;40(4):830-6. Epub 2012 Mar 22. PMID: 22441743
  5. ^ http://www.frx.com/pi/tudorza_pi.pdf
  6. ^ http://www.frx.com/pi/tudorza_pi.pdf
  7. ^ http://www.frx.com/pi/tudorza_pi.pdf
  8. ^ Cazzola M, Page CP, Calzetta L, Matera MG. Pharmacology and therapeutics of bronchodilators. Pharmacol Rev. 2012 Jul;64(3):450-504. doi: 10.1124/pr.111.004580. Epub 2012 May 18. PMID: 22611179
  9. ^ http://www.frx.com/pi/tudorza_pi.pdf