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any of the salts of hydrobromic acid; formerly used as a sedative but now generally replaced by safer drugs

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〈U〉臭化物(鎮静剤・睡眠剤として用いる) / 〈C〉《話》陳腐なことば

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/03/23 14:58:53」(JST)

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Ipratropium bromide, sold under the trade name Atrovent among others, is a medication which opens up the medium and large airways in the lungs.^[1] It is used to treat the symptoms of chronic obstructive pulmonary disease and asthma. It is used by inhaler or nebulizer. Onset of action is typically within 15 to 30 minutes and lasts for three to five hours.^[1]

Common side effects include dry mouth, cough, and inflammation of the airways. Potentially serious side effects include urinary retention, worsening spasms of the airways, and a severe allergic reaction.^[1] It appears to be safe in pregnancy and breastfeeding.^[1]^[2] Ipratropium is an anticholinergic and muscarinic antagonist which works by causing smooth muscles to relax.^[1]

Ipratropium bromide was developed in Germany in 1976.^[3] It was approved for medical use in the United States in 1986.^[1] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.^[4] Ipratropium is available as a generic medication.^[1] The wholesale price in the developing world is about 6.60 USD for a 200 dose inhaler.^[5] In the United States, a month worth of medication costs 100 to 200 USD.^[6]

Medical 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.^[7]

It is also used to treat and prevent minor and moderate bronchial asthma, especially asthma that is accompanied by cardiovascular system diseases.^{[citation needed]}

It is also combined with salbutamol (albuterol — USAN) 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 nasal solution sprayed into the nostrils can reduce rhinorrhea but will not help nasal congestion.^[8]

Combination with beta-adrenergic agonists, increases the dilating effect on the bronchi.

Contraindications

The main contraindication for inhaled ipratropium is 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.^[9]^[10]

Peanut allergy

Previously atrovent inhalers used chlorofluorocarbon (CFC) as a propellant and contained soy lecithin in the propellant ingredients. In 2008 all CFC inhalers were phased out and hydrofluoroalkane (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.^[11]

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.^[10] The inhalation itself can cause headache and irritation of the throat in a few percent of patients.^[9]

Urinary retention has been reported in patients receiving doses by nebulizer. As a result, caution may be warranted, especially by men with prostatic hypertrophy.^[12]

Interactions

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.^[9]^[10]

Pharmacology

Ipratropium exhibits broncholytic action by reducing cholinergic influence on the bronchial musculature. It blocks muscarinic acetylcholine receptors, without specificity for subtypes, and therefore promotes the degradation of cyclic guanosine monophosphate (cGMP), resulting in a decreased intracellular concentration of cGMP.^[13] 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,^[9] and does not diffuse into the blood, which prevents systemic side effects. Ipratropium is a derivative of atropine^[14] but is a quaternary amine and therefore does not cross the blood–brain barrier, which prevents central side effects (anticholinergic syndrome). Ipratropium is not considered a short-acting bronchodilator and should never be used in place of salbutamol (albuterol) as a rescue medication.

References

^ ^a ^b ^c ^d ^e ^f ^g "Ipratropium Bromide". The American Society of Health-System Pharmacists. Retrieved Dec 2, 2015.
^ Yaffe, Gerald G. Briggs, Roger K. Freeman, Sumner J. (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 9781608317080.
^ Ravina, Enrique (2011). The evolution of drug discovery : from traditional medicines to modern drugs (1. Aufl. ed.). Weinheim: Wiley-VCH. p. 144. ISBN 9783527326693.
^ "WHO Model List of Essential Medicines (19th List)" (PDF). World Health Organization. April 2015. Retrieved 8 December 2016.
^ "Ipratropium Bromide". International Drug Price Indicator Guide. Retrieved 5 December 2015.
^ Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 455. ISBN 9781284057560.
^ Ipratropium Oral Inhalation PubMed Health Retrieved May 28, 2012
^ Atrovent Nasal Spray Drugs.com Retrieved May 28, 2012
^ ^a ^b ^c ^d Haberfeld, H, ed. (2009). Austria-Codex (in German) (2009/2010 ed.). Vienna: Österreichischer Apothekerverlag. ISBN 3-85200-196-X.
^ ^a ^b ^c Dinnendahl, V; Fricke, U, eds. (2010). Arzneistoff-Profile (in German). 2 (23 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-9846-3.
^ Ipratropium Soybean and Nuts Allergy EMSMedRx Retrieved April 6, 2013
^ 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.
^ Ipratropium Drugs.com
^ 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. doi:10.1254/fpj.73.785. PMID 145994.

UpToDate Contents

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1. 慢性閉塞性肺疾患（COPD）における抗コリン療法の役割 role of anticholinergic therapy in copd
2. Acute asthma exacerbations in children: Emergency department management
3. 成人における感冒：治療および予防 the common cold in adults treatment and prevention
4. 12歳未満の小児における慢性喘息：初回評価および診断 asthma in children younger than 12 years rescue treatment for acute symptoms
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English Journal

Novel relaxant effects of RPL554 on guinea pig tracheal smooth muscle contractility.

Venkatasamy R1, Spina D1.
British journal of pharmacology.Br J Pharmacol.2016 Aug;173(15):2335-51. doi: 10.1111/bph.13512. Epub 2016 Jul 7.
BACKGROUND AND PURPOSE: We investigated the effectiveness of RPL554, a dual PDE3 and 4 enzyme inhibitor, on airway smooth muscle relaxation and compared it with that induced by salbutamol, ipratropium bromide, glycopyrrolate or their combination on bronchomotor tone induced by different spasmogenic
PMID 27174172

Oronasal and Tracheostomy Delivery of Soft Mist and Pressurized Metered-Dose Inhalers With Valved Holding Chamber.

Berlinski A1, Cooper B2.
Respiratory care.Respir Care.2016 Jul;61(7):913-9. doi: 10.4187/respcare.04575. Epub 2016 Mar 22.
BACKGROUND: Some pediatric tracheostomized patients who receive inhaled drugs undergo decannulation, and it is unknown whether the dose has to be adjusted. Pressurized metered-dose inhalers (pMDIs) and soft mist inhalers (SMIs) used with valved holding chambers (VHCs) made of non-electrostatic mater
PMID 27006348

[Asthma bronchiale - Emergency medical treatment].

Hansen M1, Hachenberg T1.
Anästhesiologie, Intensivmedizin, Notfallmedizin, Schmerztherapie : AINS.Anasthesiol Intensivmed Notfallmed Schmerzther.2016 Jun;51(6):412-20. doi: 10.1055/s-0041-107624. Epub 2016 Jun 30.
Treatment of patients with acute severe or life-threatening asthma in the emergency department or in rescue services is a challenge for the physician. The decision on which therapy is needed depends on the clinical assessment of severity. Early administration of bronchodilators, ipratropium bromide
PMID 27359240

Japanese Journal

Standard dose of inhaled albuterol significantly increases QT dispersion compared to low dose of albuterol plus ipratropium bromide therapy in moderate to severe acute asthma attacks in children

COSKUN SENOL,YUKSEL HASAN,TIKIZ HAKAN,DANAHALILOGLU SELAHATTIN
Pediatrics international : official journal of the Japan Pediatric Society 43(6), 631-636, 2001-12-01
NAID 10010092789

コリン反応性鼻粘膜の鼻腔抵抗に及ぼすメサコリンの効果

臼井信朗,吉野由紀子,大木幹文
日本鼻科学会会誌 38(1), 27-32, 1999-04-15
NAID 10009521645

The role of ipratropium bromide in the emergency management of acute asthma exacerbation ; a meta-analysis of randomized clinical trials

STOOLDEY RG
Ann Emerg Med 34, 8-18, 1999
NAID 30016781314

★リンクテーブル★

リンク元	「イプラトロピウム」
関連記事	「bromide」「bromides」

「イプラトロピウム」

Ipratropium bromide
Clinical data
Trade names	Atrovent, Apovent, Ipraxa, Rinatec, other
AHFS/Drugs.com	Monograph
Pregnancy; category	US: B (No risk in non-human studies); ;
Routes of; administration	Inhalation
ATC code	R01AX03 (WHO) R03BB01 (WHO);
Legal status
Legal status	UK: POM (Prescription only); US: ℞-only;
Pharmacokinetic data
Protein binding	0 to 9% in vitro
Metabolism	Hepatic
Biological half-life	2 hours
Identifiers
	IUPAC name [8-methyl-8-(1-methylethyl)- 8-azoniabicyclo[3.2.1] oct-3-yl] 3-hydroxy-2-phenyl-propanoate;
CAS Number	22254-24-6;
PubChem CID	657308;
IUPHAR/BPS	325;
DrugBank	DB00332;
ChemSpider	10481997;
UNII	GR88G0I6UL;
ChEMBL	CHEMBL1464005 ;
ECHA InfoCard	100.040.779
Chemical and physical data
Formula	C20H30BrNO3
Molar mass	412.37 g/mol
3D model (Jmol)	Interactive image;
	SMILES CC(C)[N+]1([C@@H]2CC[C@H]1C[C@H](C2)OC(=O)C(CO)C3=CC=CC=C3)C.[Br-] ;
	InChI 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 ;
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