cyclizine lactate

• 乳酸シクリジン

関

cyclizine、cyclizine hydrochloride

WordNet

1. a salt or ester of lactic acid

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/06/29 16:49:12」(JST)

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Cyclizine

Systematic (IUPAC) name
1-benzhydryl-4-methyl-piperazine
Clinical data
Trade names	Marezine, Valoid, Nausicalm
AHFS/Drugs.com	Consumer Drug Information
Pregnancy cat.	A (AU)
Legal status	Pharmacist Only (S3) (AU) POM (UK) OTC (Netherlands)
Routes	Oral, IM, IV
Pharmacokinetic data
Metabolism	N-demethylated to inactive norcyclizine[citation needed]
Half-life	20 hours
Identifiers
CAS number	82-92-8 Y
ATC code	R06AE03
PubChem	CID 6726
DrugBank	DB01176
ChemSpider	6470 Y
UNII	QRW9FCR9P2 Y
KEGG	D03621 Y
ChEBI	CHEBI:3994 Y
ChEMBL	CHEMBL648 Y
Chemical data
Formula	C18H22N2
Mol. mass	266.381 g/mol
SMILES CN(CC1)CCN1C(C2=CC=CC=C2)C3=CC=CC=C3
InChI InChI=1S/C18H22N2/c1-19-12-14-20(15-13-19)18(16-8-4-2-5-9-16)17-10-6-3-7-11-17/h2-11,18H,12-15H2,1H3 Y Key:UVKZSORBKUEBAZ-UHFFFAOYSA-N Y
Y (what is this?)  (verify)

Cyclizine is an antihistamine drug used to treat nausea, vomiting and dizziness associated with motion sickness, vertigo and post-operatively following administration of general anaesthesia and opioids.

Indications

Nausea, vomiting and dizziness associated with motion sickness, vertigo and post-operatively following administration of general anaesthesia and opioids. It is sometimes given in hyperemesis gravidarum, although the manufacturer advises that it be avoided in pregnancy. Off-licence use often occurs with specialists in hospitals to treat inpatients who have become severely dehydrated in pregnancy. An off-label use is as an opioid/opiate potentiator.

The drug Diconal is a combination of cyclizine with the opioid dipipanone. Dipipanone is a schedule I controlled substance in the US, due to its high abuse potential.

Contraindications

Its antimuscarinic action warrants caution in patients with prostatic hypertrophy, urinary retention, or glaucoma. Liver disease exacerbates its sedative effects.

Adverse effects

Common (over 10%) – Drowsiness, xerostomia (dry mouth)

Uncommon (1% to 10%) – Headache, psychomotor impairment, and antimuscarinic effects such as urinary retention, diplopia (blurred vision), dermatitis, and gastro-intestinal disturbances.

Rare – Hypersensitivity reactions (bronchospasm, angioedema, anaphylaxis, rashes and photosensitivity reactions), extrapyramidal effects, dizziness, confusion, depression, sleep disturbances, tremor, liver dysfunction and hallucinations

Formulations

As cyclizine hydrochloride 50 mg tablets and cyclizine lactate solution for intramuscular or intravenous injection (brand names: Valoid in UK and Marezine, Marzine and Emoquil in US). Cyclizine HCl 25 mg is marketed as Bonine for Kids in the US.

Pharmacology

Cyclizine is a piperazine derivative with histamine H₁-receptor antagonist (antihistamine) activity. The precise mechanism of action in inhibiting the symptoms of motion sickness is not well understood. It may have effects directly on the labyrinthine apparatus and on the chemoreceptor trigger zone. Cyclizine exerts a central anticholinergic (antimuscarinic) action.

History

Cyclizine was developed in the American division of pharmacy company Burroughs Wellcome (today GlaxoSmithKline) during a research involving many drugs of the antihistamine group. Cyclizine was quickly clinically found as a potent and long-acting antiemetic. Company named the substance – or more precisely cyclizine's hydrochloride form which it usually appears in – "marezine hydrochloride" and started to sell it in the United States under trade name Marezine. Selling was begun in France under trade name Marzine in 1965.

The substance received more credit when NASA chose it as a space antiemetic for the first occupied moon flight. Cyclizine was introduced to many countries as a common antiemetic. It is an over-the-counter drug in many countries because it has been well tolerated, although it has not been very much studied.

Recreational use

Some people using methadone recreationally combine cyclizine with their methadone dose, a combination that is known to produce strong psychoactive effects. It has also been used recreationally for its anticholinergic effects to induce hallucinations.

See also

• Chlorcyclizine

References

UpToDate Contents

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• 1. 乗物酔い motion sickness
• 2. 麻酔後ケア病棟における合併症発生の概要 overview of complications occurring in the post anesthesia care unit
• 3. 制吐剤の特性 characteristics of antiemetic drugs
• 4. 患者情報：妊娠による悪心および嘔吐（詳細） nausea and vomiting of pregnancy beyond the basics
• 5. 患者情報：緊急避妊（モーニングアフターピル）（詳細） emergency contraception morning after pill beyond the basics

English Journal

• Drug combinations in syringe drivers: the compatibility and stability of diamorphine with cyclizine and haloperidol.

• Grassby PF1, Hutchings L.
• Palliative medicine.Palliat Med.1997 May;11(3):217-24.
• The compatibility and stability of 2B combinations of diamorphine hydrochloride (5-100 mg/ml) with cyclizine lactate (5-50 mg/ml), eight combinations of diamorphine (10-100 mg/ml) with haloperidol (2-4 mg/ml) and eight combinations of all three drugs was assessed after storage in 1 ml polypropylene
• PMID 9205655

• Compatibility of cyclizine lactate and haloperidol lactate.

• Fawcett JP, Woods DJ, Munasiri B, Becket G.
• American journal of hospital pharmacy.Am J Hosp Pharm.1994 Sep 15;51(18):2292.
• PMID 7801994

• N(+)-glucuronidation of aliphatic tertiary amines, a general phenomenon in the metabolism of H1-antihistamines in humans.

• Luo H1, Hawes EM, McKay G, Korchinski ED, Midha KK.
• Xenobiotica; the fate of foreign compounds in biological systems.Xenobiotica.1991 Oct;21(10):1281-8.
• 1. Representative drugs of the various structural classes of H1 antihistamines were chosen for study. The drugs chosen (class name in parentheses) were chlorpheniramine maleate and pheniramine maleate (alkylamines), diphenhydramine hydrochloride and doxylamine succinate (ethanolamines), pyrilamine m
• PMID 1686692

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★リンクテーブル★

リンク元	「シクリジン」「cyclizine hydrochloride」「乳酸シクリジン」
関連記事	「cyclizine」「lactating」

「シクリジン」

　　[★]

英

cyclizine、cyclizine hydrochloride、cyclizine lactate

関

サイクリジン、塩酸シクリジン、乳酸シクリジン

-cyclizine

「cyclizine hydrochloride」

　　[★]

• 塩酸シクリジン

関

cyclizine、cyclizine lactate

「乳酸シクリジン」

　　[★]

英

cyclizine lactate

関

シクリジン

「cyclizine」

　　[★]

シクリジン、サイクリジン

関

cyclizine hydrochloride、cyclizine lactate

同

Marezine

「lactating」

　　[★]

• n.

• 授乳中、泌乳

関

lactation