臭化チオトロピウム

関: tiotropium

WordNet

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）』「2013/08/01 11:32:28」(JST)

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Tiotropium bromide (INN) is a long-acting, 24 hour, anticholinergic bronchodilator used in the management of chronic obstructive pulmonary disease (COPD). Tiotropium bromide capsules for inhalation are co-promoted by Boehringer-Ingelheim and Pfizer under the trade name Spiriva. It is also manufactured and marketed by Cipla under trade name Tiova.

Medical uses[edit]

Tiotropium is used for maintenance treatment of chronic obstructive pulmonary disease (COPD) which includes chronic bronchitis and emphysema.^[1] It is not however used for acute exacerbations.^[1]

Adverse effects[edit]

Adverse effects are mainly related to its antimuscarinic effects. Common adverse drug reactions (≥1% of patients) associated with tiotropium therapy include: dry mouth and/or throat irritation. Rarely (<0.1% of patients) treatment is associated with:urinary retention, constipation, acute angle closure glaucoma, palpitations (notably supraventricular tachycardia and atrial fibrillation) and/or allergy (rash, angioedema, anaphylaxis).^[2]

Tiotropium and another member of its class ipratropium were linked to increased risk of heart attacks, stroke and cardiovascular death.^[3] The FDA requested further trials; these are now complete, and adequately resolve the previous safety concerns.^[4]

Tiotropium mist inhaler (Respimat) has been found to be associated with an increase of all cause mortality in people with COPD.^[5]

Mechanism of action[edit]

Tiotropium is a muscarinic receptor antagonist, often referred to as an antimuscarinic or anticholinergic agent. Although it does not display selectivity for specific muscarinic receptors, on topical application it acts mainly on M₃ muscarinic receptors^[6] located on smooth muscle cells and submucosal glands leading to a reduction in smooth muscle contraction and mucus secretion, thus producing a bronchodilatory effect.

Mode of delivery[edit]

The patient removes one tiotropium capsule from the blister pack, places it into the piercing chamber of the inhalation device and closes the mouthpiece.

The capsule is manually pierced, and the medication is inhaled through the mouthpiece. It is recommended that inhalations are repeated 2 to 3 times to ensure all medication is drawn from the capsule. When properly done, the capsule will make a distinctive flutter or rattle, audible to the patient.

Once the powder capsules are removed from the blister pack, it should be taken immediately via the inhalation device. If a capsule is exposed to the air, it will rapidly degrade to the point the dose will become ineffective. Any previously exposed capsules should be discarded.

The capsules cannot be taken orally - they will not be effective as respiratory medication if absorbed through the gastrointestinal tract and may have side effects if absorbed via this route.

Front view

A previously pierced Spiriva capsule

Open (cleaning) view

References[edit]

^ ^a ^b "Spiriva Handihaler". The American Society of Health-System Pharmacists. Retrieved 3 April 2011.
^ Rossi S, ed. (2006). Australian Medicines Handbook. Adelaide.
^ Singh S, Loke YK, Furberg CD (September 2008). "Inhaled anticholinergics and risk of major adverse cardiovascular events in patients with chronic obstructive pulmonary disease: a systematic review and meta-analysis". JAMA 300 (12): 1439–50. doi:10.1001/jama.300.12.1439. PMID 18812535.
^ FDA. Follow-Up to the October 2008 Updated Early Communication about an Ongoing Safety Review of Tiotropium (marketed as Spiriva HandiHaler). FDA 2010
^ Singh, S; Loke, YK, Enright, PL, Furberg, CD (2011 Jun 14). "Mortality associated with tiotropium mist inhaler in patients with chronic obstructive pulmonary disease: systematic review and meta-analysis of randomised controlled trials.". BMJ (Clinical research ed.) 342: d3215. doi:10.1136/bmj.d3215. PMID 21672999.
^ Kato M, Komamura K, Kitakaze M (December 2006). "Tiotropium, a novel muscarinic M3 receptor antagonist, improved symptoms of chronic obstructive pulmonary disease complicated by chronic heart failure". Circ. J. 70 (12): 1658–60. doi:10.1253/circj.70.1658. PMID 17127817.

External links[edit]

Official SPIRIVA Site
Thomson CenterWatch

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. 思春期および成人における重症喘息の治療 treatment of severe asthma in adolescents and adults
3. 喘息治療の代替剤および経験的薬剤 alternative and experimental agents for the treatment of asthma
4. 安定した慢性閉塞性肺疾患（COPD）のマネージメント management of stable chronic obstructive pulmonary disease
5. 重度慢性閉塞性肺疾患（COPD）および心血管疾患患者のマネージメント management of the patient with severe copd and cardiovascular disease

English Journal

Aclidinium bromide / formoterol fumarate fixed-dose combination for the treatment of chronic obstructive pulmonary disease.

Cazzola M, Rogliani P, Matera MG.SourceUniversity of Rome, Department of System Medicine , Rome 'Tor Vergata' , Italy.
Expert opinion on pharmacotherapy.Expert Opin Pharmacother.2013 Apr;14(6):775-81. doi: 10.1517/14656566.2013.776539. Epub 2013 Mar 9.
Introduction: Combining a long-acting β2-agonist (LABA) and a long-acting antimuscarinic agent (LAMA) is potentially a good pharmacological approach to improve clinical results in stable moderate chronic obstructive pulmonary disease (COPD) patients when symptoms are not adequately controlled with
PMID 23472632

Safety and Efficacy of 12-Week or Longer Indacaterol Treatment in Moderate-to-Severe COPD Patients: A Systematic Review.

Jiang FM, Liang ZA, Zheng QL, Wang RC, Luo J, Li CT.SourceDepartment of Respiratory Medicine, West China Medical School and West China Hospital, Sichuan University, Chengdu, 610000, Sichuan, China.
Lung.Lung.2013 Apr;191(2):135-46. doi: 10.1007/s00408-012-9444-2. Epub 2013 Jan 10.
BACKGROUND: This is a meta-analysis of the safety and efficacy of indacaterol in chronic obstructive pulmonary disease (COPD) with treatment duration of ≥12 weeks.METHODS: Randomized controlled trials (RCTs) reported in English (to September 30, 2012) were identified from PubMed, the Cochrane Lib
PMID 23306410

Japanese Journal

非発作時に閉塞性換気障害を呈する気管支喘息患者に対する吸入抗コリン薬の長期効果

野上裕子,本荘哲,岩永知秋
アレルギー 61(11), 1675-1682, 2012-11
NAID 40019515638

IP-3 Effects of Tiotropium bromide on Chronic Murine Asthma Model

Ohta Shin,Minoguchi Kenji,Oda Naruhito,Yokoe Takuya,Xu Xun,Chen Xiaoyang,Yamamoto Yoshitaka,Yamamoto Mayumi,Watanabe Yoshio,Nagase Hiroyuki,Ohta Ken,Adachi Mitsuru
アレルギー 57(9・10), 1384, 2008-10-30
NAID 110007012453

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★リンクテーブル★

リンク元	「チオトロピウム」
関連記事	「bromide」「bromides」

「チオトロピウム」

Tiotropium
Systematic (IUPAC) name
	(1α,2β,4β,7β)-; 7-[(hydroxidi-2-thienylacetyl)oxy]-9,9-dimethyl-; 3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide
Clinical data
MedlinePlus	a604018
Pregnancy cat.	B1 (AU)
Legal status	Prescription Only (S4) (AU) POM (UK) ℞-only (US)
Routes	Inhalation (oral)
Pharmacokinetic data
Bioavailability	19.5% (inhalation)
Metabolism	Hepatic 25%; (CYP2D6, CYP3A4)
Half-life	5–6 days
Excretion	Renal
Identifiers
CAS number	136310-93-5; 186691-13-4 (cation)
ATC code	R03BB04
PubChem	CID 5487426
IUPHAR ligand	367
DrugBank	DB01409
ChemSpider	10482095
UNII	XX112XZP0J
ChEMBL	CHEMBL1201307
Chemical data
Formula	C19H22BrNO4S2
Mol. mass	472.416 g/mol
	SMILES C[N+]1(C2CC(CC1C3C2O3)OC(=O)C(C4=CC=CS4)(C5=CC=CS5)O)C.[Br-];
	InChI InChI=1S/C19H22NO4S2/c1-20(2)12-9-11(10-13(20)17-16(12)24-17)23-18(21)19(22,14-5-3-7-25-14)15-6-4-8-26-15/h3-8,11-13,16-17,22H,9-10H2,1-2H3/q+1/t11?,12-,13+,16-,17-/m0/s1 ; Key:LERNTVKEWCAPOY-MCGYIYAPSA-N ;
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　　[★]

英: tiotropium
化: 臭化チオトロピウム tiotropium bromide、
商: スピリーバ

抗コリン薬;慢性閉塞性肺疾患治療;長時間持続型

「bromide」

　　[★]

n.

臭化物、ブロム剤

「bromides」

　　[★]

n.

臭化物、ブロム剤

[AHFS-1] "Spiriva Handihaler". The American Society of Health-System Pharmacists. Retrieved 3 April 2011.

[2] Rossi S, ed. (2006). Australian Medicines Handbook. Adelaide.

[3] Singh S, Loke YK, Furberg CD (September 2008). "Inhaled anticholinergics and risk of major adverse cardiovascular events in patients with chronic obstructive pulmonary disease: a systematic review and meta-analysis". JAMA 300 (12): 1439–50. doi:10.1001/jama.300.12.1439. PMID 18812535.

[4] FDA. Follow-Up to the October 2008 Updated Early Communication about an Ongoing Safety Review of Tiotropium (marketed as Spiriva HandiHaler). FDA 2010

[5] Singh, S; Loke, YK, Enright, PL, Furberg, CD (2011 Jun 14). "Mortality associated with tiotropium mist inhaler in patients with chronic obstructive pulmonary disease: systematic review and meta-analysis of randomised controlled trials.". BMJ (Clinical research ed.) 342: d3215. doi:10.1136/bmj.d3215. PMID 21672999.

[pmid17127817-6] Kato M, Komamura K, Kitakaze M (December 2006). "Tiotropium, a novel muscarinic M3 receptor antagonist, improved symptoms of chronic obstructive pulmonary disease complicated by chronic heart failure". Circ. J. 70 (12): 1658–60. doi:10.1253/circj.70.1658. PMID 17127817.

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案内

案内

tiotropium bromide