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a complex consisting of an organic base in association with hydrogen chloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/09/17 10:52:21」(JST)

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Ritodrine (discontinued preparation: Yutopar) is a tocolytic drug, used to stop premature labor.^[1] This drug has been removed from the US market, according to FDA Orange Book. It was available in oral tablets or as an injection and was typically used as the hydrochloride salt, ritodrine hydrochloride.

Mechanism

Ritodrine is a beta-2 adrenergic receptor agonist - a class of medication used for smooth muscle relaxation (other similar drugs are used in asthma or other pulmonary diseases such as salbutamol). Since ritodrine has a bulky N-substituent, it has high β2-selectivity. Also, the 4'-hydroxy on the benzene ring is important for activity as it is needed to form hydrogen bonds. However, the 4'-hydroxy makes it susceptible to metabolism by COMT. Since it is β2-selective it is used for premature labor.^[2]

Side effects and potential contraindications

Most side effects of beta-2 agonists result from their concurrent beta-1 activity, and include increase in heart rate, rise in systolic pressure, decrease in diastolic pressure, chest pain secondary to MI, and arrhythmia. Beta agonists may also cause fluid retention secondary to decrease in water clearance, which when added to the tachycardia and increased myocardial work, may result in cardiac failure. In addition, they increase gluconeogenesis in the liver and muscle resulting in hyperglycemia, which increases insulin requirements in diabetic patients. The passage of beta-agonists through the placenta does occur and may be responsible for fetal tachycardia, as well as hypoglycemia or hyperglycemia at birth.

Patients with type 2 diabetes, high blood pressure or migraines should bring this to their doctor's attention before receiving care.

It has also been associated with post-partum hemorrhage.^{[citation needed]}

References

^ Li X, Zhang Y, Shi Z (February 2005). "Ritodrine in the treatment of preterm labour: a meta-analysis" (PDF). The Indian journal of medical research 121 (2): 120–7. PMID 15756046.
^ Medicinal Chemistry of Adrenergics and Cholinergics

UpToDate Contents

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1. 切迫早産の予防 inhibition of acute preterm labor
2. 外回転術 external cephalic version
3. 胎盤早期剥離：管理 placental abruption management
4. 臍帯脱出 umbilical cord prolapse
5. 低カリウム血症の原因 causes of hypokalemia

English Journal

Short- and long-term outcomes in babies born after antenatal magnesium treatment.

Mitani M, Matsuda Y, Shimada E; Perinatal Research Network Group in Japan.SourceDepartment of Obstetrics and Gynecology Perinatal Medical Center, Tokyo Women's Medical University Hospital, Tokyo, Japan.
The journal of obstetrics and gynaecology research.J Obstet Gynaecol Res.2011 Jul 6. doi: 10.1111/j.1447-0756.2011.01583.x. [Epub ahead of print]
Aim:? To identify the prenatal events associated with adverse outcome in babies born at less than 32?weeks' gestation, including antenatal magnesium sulfate treatment. Methods:? A case-control study was performed to examine the effect of long-term tocolysis with MgSO(4) . Long-term neonatal an
PMID 21733038

The influence of tocolytic drugs on cardiac function, large arteries, and resistance vessels.

Fabry IG, De Paepe P, Kips JG, Van Bortel LM.SourceHeymans Institute of Pharmacology, Department of Clinical Pharmacology, Ghent University Hospital, De Pintelaan 185, 9000 Ghent, Belgium. isabelle.fabry@ugent.be
European journal of clinical pharmacology.Eur J Clin Pharmacol.2011 Jun;67(6):573-80. Epub 2011 Apr 15.
PURPOSE: Beta-2 adrenoceptor agonistic drugs like ritodrine have been the reference tocolytic drugs, but are associated with cardiovascular side-effects. Atosiban, a newer drug, is a competitive antagonist of oxytocin and has been claimed to have fewer cardiovascular side effects. Until now, there h
PMID 21494767

Japanese Journal

帝王切開後に肺水腫による急性呼吸不全を来たした1例

卜部奏子,迎寛,坂本憲穂,中島章太,泉川公一,石松祐二,池田聡司,河野茂
日本呼吸器学会雑誌 = The journal of the Japanese Respiratory Society 48(7), 520-523, 2010-07-10
NAID 10026599196

未分画ヘパリンによる塩酸リトドリン長期投与による輸液針留置困難改善の試み

依藤崇志,牧野真太郎,手島薫,岡部瞳,稲垣徹訓,斉藤知見,輿石太郎,田中利隆,杉村基,竹田省
日本産婦人科・新生児血液学会誌 = The Japanese journal of obstetrical, gynecological & neonatal hematology 20(1), 65, 2010-06-01
NAID 10026710552

「リトドリン」

Ritodrine
Systematic (IUPAC) name
	4-(2-((1R,2S)-1-hydroxy-1-(4-hydroxyphenyl)propan-2-ylamino)ethyl)phenol
Clinical data
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Routes of; administration	Oral, parenteral
Pharmacokinetic data
Protein binding	~56%
Biological half-life	1.7-2.6 hours
Identifiers
CAS Registry Number	26652-09-5
ATC code	G02CA01
PubChem	CID: 33572
IUPHAR/BPS	7294
DrugBank	DB00867
ChemSpider	30971
UNII	I0Q6O6740J
KEGG	D02359
ChEMBL	CHEMBL785
Chemical data
Formula	C17H21NO3
Molecular mass	287.354 g/mol
	SMILES O[C@H](c1ccc(O)cc1)[C@@H](NCCc2ccc(O)cc2)C ;
	InChI InChI=1S/C17H21NO3/c1-12(17(21)14-4-8-16(20)9-5-14)18-11-10-13-2-6-15(19)7-3-13/h2-9,12,17-21H,10-11H2,1H3/t12-,17-/m0/s1 ; Key:IOVGROKTTNBUGK-SJCJKPOMSA-N ;
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　　[★]

英: ritodrine
化: 塩酸リトドリン ritodrine hydrochloride、リトドリン塩酸塩
商: ウテメック、ウテメナール、ウテメリン(キッセイ)、ウテロトップ、ウテロン、ウルペティック、ピロスデン、リトドール、リトメリン、リメトラーク、リンドルフ、ルテオニン、レキサビン
関: アドレナリン受容体

作用機序

βアドレナリン受容体作動薬

β₂受容体刺激薬

薬理作用

子宮収縮抑制

動態

適応

切迫流産、切迫早産

注意

禁忌

ウルペティック錠５mg

強度の子宮出血、子かん、前期破水例のうち子宮内感染を合併する症例、常位胎盤早期剥離、子宮内胎児死亡、その他妊娠の継続が危険と判断される患者［妊娠継続が危険と判断される。］
重篤な甲状腺機能亢進症の患者［症状が増悪するおそれがある。］
重篤な高血圧症の患者［過度の昇圧が起こるおそれがある。］
重篤な心疾患の患者［心拍数増加等により症状が増悪するおそれがある。］
重篤な糖尿病の患者［過度の血糖上昇が起こるおそれがある。また、糖尿病性ケトアシドーシスがあらわれることもある。］
重篤な肺高血圧症の患者［肺水腫が起こるおそれがある。］
妊娠16週未満の妊婦（「重要な基本的注意」の項参照）
本剤の成分に対し重篤な過敏症の既往歴のある患者

副作用

頻脈:β1受容体にも若干agonistとして作用する　→　禁忌も見る
高アミラーゼ血症、顆粒球減少、横紋筋融解症(筋肉痛、脱力感、CPK上昇、血中ミオグロビン上昇、尿中ミオグロビン上昇)
高血糖(β2受容体アゴニストとして作用するため、グリコーゲンが分解される　←　インスリンについてはどうなの？

参考

1. ウルペティック錠５mg - 添付文書

http://www.info.pmda.go.jp/go/pack/2590004F1265_1_02/2590004F1265_1_02

「hydrochloride」

　　[★] 塩酸塩、ハイドロクロライド　

[pmid15756046-1] Li X, Zhang Y, Shi Z (February 2005). "Ritodrine in the treatment of preterm labour: a meta-analysis" (PDF). The Indian journal of medical research 121 (2): 120–7. PMID 15756046.

[2] Medicinal Chemistry of Adrenergics and Cholinergics

匿名

検索

案内

案内

ritodrine hydrochloride