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Ipratropium
Systematic (IUPAC) name
[8-methyl-8-(1-methylethyl)- 8-azoniabicyclo[3.2.1] oct-3-yl] 3-hydroxy-2-phenyl-propanoate
Identifiers
CAS number 60205-81-4
ATC code R01AX03 R03BB01
PubChem 43232
DrugBank APRD00537
Chemical data
Formula C 20H30NO3  
Mol. mass 332.457 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Protein binding 0 to 9% in vitro
Metabolism Hepatic
Half life 2 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat. B(US)
Legal status POM (UK)
Routes Inhalation
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Ipratropium (Atrovent, Apovent) is an anticholinergic drug.[1] It blocks the muscarinic cholinergic receptors in the smooth muscles of the bronchi in the lungs. This opens the bronchi, and provides relief in chronic obstructive pulmonary disease.

Contents

Uses

It is administered by inhalation for the treatment of obstructive lung diseases.

Ipratropium is also combined with albuterol (salbutamol) (trade names Combivent and Duoneb, in Italy known as Breva) for the management of chronic obstructive pulmonary disease (COPD) and asthma.

Ipratropium is also combined with fenoterol (trade names Duovent and Berodual N) for the management of asthma.

Ipratropium can reduce rhinorrhea but will not help nasal congestion.

Pharmacology

It blocks muscarinic cholinergic receptors, without specificity for subtypes, resulting in a decrease in the formation of cyclic guanosine monophosphate (cGMP). 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 non-selective muscarinic antagonist, and does not diffuse into the blood, which prevents systemic side-effects. Ipratropium is a derivative of atropine[2] 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.[3][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 ocular dislocure, nausea, palpitations and headache have been observed.

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. PMID 138578. http://www.chestjournal.org/cgi/pmidlookup?view=long&pmid=138578.  
  2. ^ 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.  
  3. ^ 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.  
  4. ^ Knott L (November 20, 2007). "Antimuscarinic Bronchodilators". PatientUK. EMIS. http://www.patient.co.uk/showdoc/40025112/. Retrieved 2008-06-16.  







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