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Definição e significado de Ipratropium_bromide

Definição

ipratropium bromide (n.)

1.an inhaled bronchodilator (trade name Atrovent)

Ipratropium Bromide (n.)

1.(MeSH)A muscarinic antagonist structurally related to ATROPINE but often considered safer and more effective for inhalation use. It is used for various bronchial disorders, in rhinitis, and as an antiarrhythmic.

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Dicionario analógico

Ipratropium Bromide (n.) [MeSH]



Wikipedia

Ipratropium bromide

                   
Ipratropium bromide
Systematic (IUPAC) name
[8-methyl-8-(1-methylethyl)- 8-azoniabicyclo[3.2.1] oct-3-yl] 3-hydroxy-2-phenyl-propanoate
Clinical data
AHFS/Drugs.com monograph
Pregnancy cat. B (US)
Legal status POM (UK) -only (US)
Routes Inhalation
Pharmacokinetic data
Protein binding 0 to 9% in vitro
Metabolism Hepatic
Half-life 2 hours
Identifiers
CAS number 22254-24-6
60205-81-4 (cation)
ATC code R01AX03 R03BB01
PubChem CID 657308
IUPHAR ligand 325
DrugBank DB00332
ChemSpider 19962157 YesY
UNII GR88G0I6UL YesY
ChEMBL CHEMBL541165 N
Chemical data
Formula C20H30BrNO3 
Mol. mass 412.37 g/mol
 N (what is this?)  (verify)

Ipratropium bromide (INN, trade names Atrovent, Apovent, and Aerovent) is an anticholinergic drug used for the treatment of chronic obstructive pulmonary disease and acute asthma. It blocks the muscarinic acetylcholine receptors in the smooth muscles of the bronchi in the lungs, opening the bronchi.[1]

Contents

  Uses

Ipratropium is administered by inhalation for the treatment of chronic obstructive pulmonary disease (COPD). For that purpose it is supplied in a canister for use in an inhaler or in single dose vials for use in a nebulizer.[2]

It is also combined with salbutamol (albuterol, USA) under the trade names Combivent (metered-dose inhaler or MDI) and Duoneb (nebulizer) for the management of COPD and asthma, and with fenoterol (trade names Duovent and Berodual N) for the management of asthma.

Ipratropium as a .03% nasal solution sprayed into the nostrils can reduce rhinorrhea but will not help nasal congestion.[3]

  Pharmacology

Ipratropium blocks muscarinic acetylcholine receptors, without specificity for subtypes, and therefore inhibits degradation of cyclic guanosine monophosphate (cGMP), resulting in an intracellular increase of cGMP concentration. Most likely due to actions of cGMP on intracellular calcium, this results in decreased contractility of smooth muscle in the lung, inhibiting bronchoconstriction and mucus secretion. It is a nonselective muscarinic antagonist,[4] and does not diffuse into the blood, which prevents systemic side effects. Ipratropium is a derivative of atropine[5] but is a quaternary amine and therefore does not cross the blood–brain barrier, which prevents central side effects (anticholinergic syndrome). Ipratropium is considered a short-acting bronchodilator.[6][7]

  Contraindications

There are no contraindications for inhaled ipratropium, apart from hypersensitivity to atropine and related substances. For oral administration, contraindications are similar to other anticholinergics; they include narrow angle glaucoma and obstructions in the gastrointestinal tract and urinary system.[8][4]

  Side effects

If ipratropium is inhaled, side effects resembling those of other anticholinergics are minimal. However, dry mouth and sedation have been reported. Also, effects such as skin flushing, tachycardia, acute angle-closure glaucoma, nausea, palpitations and headache have been observed. Inhaled ipratropium does not decrease mucociliary clearance.[8] The inhalation itself can cause headache and irritation of the throat in a few percent of patients.[4] Some studies suggest that patients with peanut allergies may have an anaphylactic response to atrovent.[citation needed] Urinary retention has been reported in patients receiving doses by nebulizer. As a result, caution may be warranted, especially by in men with prostatic hypertrophy.[9]

  Interactions

Combination with beta-adrenergic agonists, as well as theophylline and other xanthine derivatives, increases the dilating effect on the bronchi. Interactions with other anticholinergics like tricyclic antidepressants, antiparkinson drugs and quinidine, which theoretically increase side effects, are clinically irrelevant when ipratropium is administered as an inhalant.[8][4]

  See also

  References

  1. ^ Baigelman W, Chodosh S (March 1977). "Bronchodilator action of the anticholinergic drug, ipratropium bromide (Sch 1000), as an aerosol in chronic bronchitis and asthma". Chest 71 (3): 324–8. DOI:10.1378/chest.71.3.324. PMID 138578. http://www.chestjournal.org/cgi/pmidlookup?view=long&pmid=138578. 
  2. ^ Ipratropium Oral Inhalation PubMed Health Retrieved May 28, 2012
  3. ^ Atrovent Nasal Spray Drugs.com Retrieved May 28, 2012
  4. ^ a b c d Haberfeld, H, ed. (2009) (in German). Austria-Codex (2009/2010 ed.). Vienna: Österreichischer Apothekerverlag. ISBN 3-85200-196-X. 
  5. ^ Yamatake Y, Sasagawa S, Yanaura S, Okamiya Y (1977). "[Antiallergic asthma effect of ipratropium bromide (Sch 1000) in dogs (author's transl)]" (in Japanese). Nippon Yakurigaku Zasshi 73 (7): 785–91. PMID 145994. 
  6. ^ Kerstjens HA, Bantje TA, Luursema PB, et al. (2007). "Effects of short-acting bronchodilators added to maintenance tiotropium therapy". Chest 132 (5): 1493–9. DOI:10.1378/chest.06-3059. PMID 17890476. 
  7. ^ Knott L (November 20, 2007). "Antimuscarinic Bronchodilators". PatientUK. EMIS. http://www.patient.co.uk/showdoc/40025112/. Retrieved 2008-06-16. 
  8. ^ a b c Dinnendahl, V, Fricke, U, ed. (2010) (in German). Arzneistoff-Profile. 2 (23 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-9846-3. 
  9. ^ Afonso, A. S. M.; Verhamme, K. M. C.; Stricker, B. H. C.; Sturkenboom, M. C. J. M.; Brusselle, G. G. O. (2011). "Inhaled anticholinergic drugs and risk of acute urinary retention". BJU International 107 (8): 1265–1272. DOI:10.1111/j.1464-410X.2010.09600.x. PMID 20880196.  edit
   
               

 

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