Ipratropium bromide
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| Routes of administration | Inhalation |
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| Protein binding | 0 to 9% in vitro |
| Metabolism | Hepatic |
| Elimination half-life | 2 hours |
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| ECHA InfoCard | 100.040.779 |
| Chemical and physical data | |
| Formula | C20H30BrNO3 |
| Molar mass | 412.37 g/mol g·mol−1 |
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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]
Uses
It is administered by inhalation for the treatment of chronic obstructive pulmonary disease (COPD).
Ipratropium 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 can reduce rhinorrhea but will not help nasal congestion.
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.[2][3]
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. Inhaled ipratropium does not decrease mucociliary clearance.[2] The inhalation itself can cause headache and irritation of the throat in a few percent of patients.[3]
Pharmacology
It blocks muscarinic acetylcholine 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 nonselective muscarinic antagonist, and does not diffuse into the blood, which prevents systemic side effects. Ipratropium is a derivative of atropine[4] 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.[5][6]
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.[2][3]
See also
References
- ^ Baigelman W, Chodosh S (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.
{{cite journal}}: Unknown parameter|month=ignored (help) - ^ a b c Dinnendahl, V, Fricke, U, ed. (2010). Arzneistoff-Profile (in German). Vol. 2 (23 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-98-46-3.
{{cite book}}: CS1 maint: multiple names: editors list (link) - ^ a b c Haberfeld, H, ed. (2009). Austria-Codex (in German) (2009/2010 ed.). Vienna: Österreichischer Apothekerverlag. ISBN 3-85200-196-X.
- ^ Yamatake Y, Sasagawa S, Yanaura S, Okamiya Y (1977). "[Antiallergic asthma effect of ipratropium bromide (Sch 1000) in dogs (author's transl)]". Nippon Yakurigaku Zasshi (in Japanese). 73 (7): 785–91. PMID 145994.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ 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.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link) - ^ Knott L (November 20, 2007). "Antimuscarinic Bronchodilators". PatientUK. EMIS. Retrieved 2008-06-16.