Movatterモバイル変換


[0]ホーム

URL:


Jump to content
WikipediaThe Free Encyclopedia
Search

Ipratropium bromide

From Wikipedia, the free encyclopedia
Anticholinergic used in the treatment of asthma

Pharmaceutical compound
Ipratropium bromide
Clinical data
Trade namesAtrovent, others
AHFS/Drugs.comMonograph
MedlinePlusa618013
License data
Pregnancy
category
Routes of
administration
Inhalation,intranasal
Drug classAnticholinergic (muscarinic antagonist)
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding0–9%in vitro
MetabolismLiver
Onset of action15–30 minutes
Eliminationhalf-life2 hours
Duration of action3–5 hours
Identifiers
  • [8-methyl-8-(1-methylethyl)- 8-azoniabicyclo[3.2.1] oct-3-yl] 3-hydroxy-2-phenyl-propanoate
CAS Number
PubChemCID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard100.040.779Edit this at Wikidata
Chemical and physical data
FormulaC20H30BrNO3
Molar mass412.368 g·mol−1
3D model (JSmol)
  • CC(C)[N+]1(C2CCC1CC(C2)OC(=O)C(CO)C3=CC=CC=C3)C.[Br-]
  • InChI=1S/C20H30NO3.BrH/c1-14(2)21(3)16-9-10-17(21)12-18(11-16)24-20(23)19(13-22)15-7-5-4-6-8-15;/h4-8,14,16-19,22H,9-13H2,1-3H3;1H/q+1;/p-1/t16-,17+,18+,19?,21?;
  • Key:LHLMOSXCXGLMMN-WDTICOSOSA-M
 ☒NcheckY (what is this?)  (verify)

Ipratropium bromide, sold under the trade nameAtrovent among others, is a type ofanticholinergic medication which is applied by different routes:inhaler,nebulizer, ornasal spray, for different reasons.[1][2]

The inhalantopens up the medium and large airways in the lungs.[3] It is used to treat the symptoms ofchronic obstructive pulmonary disease (COPD) andasthma.[3] It is used byinhaler ornebulizer.[3] Onset of action is typically within 15 to 30 minutes and lasts for three to five hours.[3]

The nasal spray prevents the glands in the nose from producing large amounts of fluid.[4][5] It is used to treatrhinorrhea (runny nose) caused byallergic rhinitis,nonallergic rhinitis,[4] and the common cold.[6][2] It is used by metered-dose manual pump spray. Onset of action is within an hour.[6]

Common side effects of inhalant use includedry mouth,cough,inflammation of the airways,[3] andshortness of breath.[7] Potentially serious side effects includeurinary retention, worsening spasms of the airways, and asevere allergic reaction.[3] It appears to be safe inpregnancy andbreastfeeding.[3][8] Ipratropium is a short-actingmuscarinic antagonist,[9] which works by causingsmooth muscles to relax.[3]

Common side effects of nasal spray may includeheadache, dry nose, dry mouth or throat, nasal or throat irritation,nosebleeds, bad taste in mouth,nausea,dizziness, orconstipation.[6] Potentially serious side effects are unusual, but include severe allergic reaction, eye pain or change in vision, or urinary retention. It is considered safe during pregnancy, but it can pass into breast milk and may harm a nursing baby.[10]

Ipratropium bromide was patented in 1966, and approved for medical use in 1974.[11] It is on theWorld Health Organization's List of Essential Medicines, the most important medicines needed in ahealth system.[12] Ipratropium is available as a generic medication.[3] In 2023, it was the 268th most commonly prescribed medication in the United States, with more than 900,000 prescriptions.[13][14]

Medical uses

[edit]

Ipratropium as an inhalant can be used for the treatment ofchronic obstructive pulmonary disease (COPD) andasthma exacerbation.[15] It is supplied in a canister for use in aninhaler or in single dose vials for use in anebulizer.[16]

It is also used to treat and prevent minor and moderate bronchial asthma, especially asthma that is accompanied by cardiovascular system diseases, as it has been shown to produce fewer cardiovascular side effects.[17]

Combination withbeta-adrenergic agonists increases the dilating effect on the bronchi, as whenipratropium is combined with salbutamol (albuterolUSAN) under the trade names Combivent (a non-aerosolmetered-dose inhaler or MDI) and Duoneb (nebulizer) for the management of COPD and asthma, and withfenoterol (trade names Duovent and Berodual N) for the management of asthma.

Ipratropium as a nasal solution sprayed into the nostrils can reducerhinorrhea (runny nose) but will not helpnasal congestion.[18] It is supplied in a metered-dose manual pump spray.[6]

Contraindications

[edit]

The main contraindication for ipratropium in any form ishypersensitivity toatropine and related substances.[19][20]

Conditions such as narrow-angle glaucoma, prostatic hyperplasia, or bladder neck obstruction are not necessarily contraindicators, but should be taken into account, particularly if the patient is receiving an anticholinergic by another route.[2]

Peanut allergy

[edit]

Previously, Atrovent inhalers usedchlorofluorocarbon (CFC) as a propellant and containedsoy lecithin in the propellant ingredients. In 2008 all CFC inhalers were phased out andhydrofluoroalkane (HFA) inhalers replaced them.Allergy to peanuts was noted for the inhaler as a contraindication but now is not. It has never been a contraindication when administered as a nebulized solution.[21]

Side effects

[edit]

If ipratropium is inhaled, side effects resembling those of otheranticholinergics are minimal. However,dry mouth andsedation have been reported. Also, effects such asskin flushing,tachycardia, acute angle-closureglaucoma,nausea,palpitations, andheadache have been observed. Inhaled ipratropium does not decreasemucociliary clearance.[20] The inhalation itself can cause headache and irritation of the throat in a few percent of patients.[19]

Urinary retention has been reported in patients receiving doses by nebulizer. As a result, caution may be warranted, especially by men with prostatic hypertrophy.[22]

Common side effects of nasal spray are experienced at a rate of 1-6% (versus the control group of 0-3%), and may include headache, dry nose, dry mouth or throat, nasal or throat irritation,nosebleeds, bad taste in mouth, nausea,dizziness, orconstipation.[6][23] Potentially serious side effects from nasal spray are rare, but include severe allergic reaction, eye pain or change in vision, or difficulty urinating.[5]

Accidental contact with the eye should be avoided.

Interactions

[edit]

Interactions with other anticholinergics liketricyclic antidepressants,anti-Parkinson drugs andquinidine, which theoretically increase side effects, are clinically irrelevant when ipratropium is administered as an inhalant.[19][20]

Ipratropium nasal spray may interact with certain medications fordepression,anxiety, or other mental health conditions, certain medications forParkinson's disease such asbenztropine andtrihexyphenidyl,atropine, certainantihistamines forallergy,cough, andcold, certain medications for bladder problems such asoxybutynin andtolterodine, certain medications for stomach problems such asdicyclomine andhyoscyamine, and certain medications for motion sickness such asscopolamine.[5]

Pharmacology

[edit]

Chemically, ipratropium bromide is a quaternary ammonium compound (which is indicated by the-ium per theBAN and theUSAN)[24] obtained by treatingatropine withisopropyl bromide, thus the name:isopropyl +atropine.[citation needed] It is chemically related to components of the plantDatura stramonium, which was used in ancient India for asthma.[25]

Ipratropium exhibitsbroncholytic action by reducing cholinergic influence on the bronchial musculature. It blocks muscarinic acetylcholine receptors, without specificity for subtypes, and therefore promotes the degradation ofcyclic guanosine monophosphate (cGMP), resulting in a decreased intracellular concentration of cGMP.[26] Most likely due to actions of cGMP on intracellular calcium, this results in decreased contractility of smooth muscle in the lung, inhibitingbronchoconstriction andmucussecretion. It is a nonselectivemuscarinicantagonist,[19] and does not diffuse into the blood, which prevents systemic side effects. Ipratropium is a derivative ofatropine[3] but is aquaternary amine and therefore does not cross theblood–brain barrier, which prevents central side effects. Ipratropium should never be used in place ofsalbutamol (albuterol) as a rescue medication.

References

[edit]
  1. ^Rxlist.com: Search Atrovent
  2. ^abcRx.com: Ipratropium
  3. ^abcdefghij"Ipratropium Bromide". The American Society of Health-System Pharmacists.Archived from the original on 8 December 2015. Retrieved2 December 2015.
  4. ^abMayo Clinic: Ipratropium (Nasal Route)
  5. ^abcCleveland Clinic: Ipratropium Nasal Spray
  6. ^abcdeRxlist.com: Atrovent Nasal Spray
  7. ^RxList.com: Atrovent HFA
  8. ^Briggs G, Freeman RK, Yaffe SJ (2011).Drugs in pregnancy and lactation : a reference guide to fetal and neonatal risk (9th ed.). Philadelphia: Wolters Kluwer Health/Lippincott Williams & Wilkins. p. 763.ISBN 978-1-60831-708-0.
  9. ^Ritter J, Flower RJ, Henderson G, Loke YK, MacEwan DJ, Rang HP (2020).Rang and Dale's pharmacology (9th ed.). Edinburgh. p. 377.ISBN 978-0-7020-8060-9.OCLC 1081403059.{{cite book}}: CS1 maint: location missing publisher (link)
  10. ^Drugs.com: Ipratropium nasal
  11. ^Fischer J, Ganellin CR (2006).Analogue-based Drug Discovery. John Wiley & Sons. p. 446.ISBN 978-3-527-60749-5.
  12. ^World Health Organization (2019).World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization.hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  13. ^"The Top 300 of 2023".ClinCalc.Archived from the original on 17 August 2025. Retrieved17 August 2025.
  14. ^"Ipratropium Drug Usage Statistics, United States, 2014 - 2023".ClinCalc. Retrieved17 August 2025.
  15. ^Aaron SD (October 2001). "The use of ipratropium bromide for the management of acute asthma exacerbation in adults and children: a systematic review".The Journal of Asthma.38 (7):521–530.doi:10.1081/jas-100107116.PMID 11714074.S2CID 7335677.
  16. ^"Ipratropium Oral Inhalation".PubMed Health. Archived fromthe original on 2 September 2012. Retrieved28 May 2012.
  17. ^"Ipratropium Bromide 0.5 mg/Albuterol Sulfate 3.0 mg"(PDF).FDA. 2004. Archived fromthe original(PDF) on 27 February 2017. Retrieved4 January 2021.
  18. ^"Atrovent Nasal Spray".Drugs.com.Archived from the original on 11 January 2012. Retrieved28 May 2012.
  19. ^abcdHaberfeld, H, ed. (2009).Austria-Codex (in German) (2009/2010 ed.). Vienna: Österreichischer Apothekerverlag.ISBN 978-3-85200-196-8.
  20. ^abcDinnendahl, V, Fricke, U, eds. (2010).Arzneistoff-Profile (in German). Vol. 2 (23 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag.ISBN 978-3-7741-9846-3.
  21. ^"Ipratropium Soybean and Nuts Allergy".EMSMedRx. 21 March 2011. Archived fromthe original on 13 May 2012. Retrieved6 April 2013.
  22. ^Afonso AS, Verhamme KM, Stricker BH, Sturkenboom MC, Brusselle GG (April 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.S2CID 29516074.
  23. ^Drugs.com: Ipratropium nasal
  24. ^"The Use of Common Stems in the Selection of International Nonproprietary Names (INN) for Pharmaceutical Substances".who.int. World Health Organization. 2000. Archived fromthe original on 7 March 2012. Retrieved18 July 2018.
  25. ^"History of Asthma".Allergy And Asthma. 21 December 2017. Archived fromthe original on 11 November 2020. Retrieved2 September 2020.... India, smoking the herb stramonium (an anticholinergic agent related to ipratropium and tiotropium currently used in inhalers) was used to relax the lungs.
  26. ^"Ipratropium".Drugs.com. Archived fromthe original on 19 May 2012.
Decongestants and other nasal preparations (R01)
Topical
Sympathomimetics, plain
Antiallergic agents,
excluding corticosteroids
Corticosteroids
Other nasal preparations
Combination products
Systemic use:
Sympathomimetics
Adrenergics,inhalants
Short-acting β2 agonists
Long-acting β2 agonists
Ultra-long-acting β2 agonists
Other
Glucocorticoids
Anticholinergics/
muscarinic antagonist
Mast cell stabilizers
Xanthines
Eicosanoid inhibition
Leukotriene antagonists
Arachidonate 5-lipoxygenase inhibitors
Thromboxane receptor antagonists
Non-xanthinePDE4 inhibitors
Others/unknown
Combination products
mAChRsTooltip Muscarinic acetylcholine receptors
Agonists
Antagonists
Precursors
(andprodrugs)
Portal:
Retrieved from "https://en.wikipedia.org/w/index.php?title=Ipratropium_bromide&oldid=1311870423"
Categories:
Hidden categories:

[8]ページ先頭

©2009-2025 Movatter.jp