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Metoclopramide (INN) (pron.: /ˌmɛtəˈklɒprəmaɪd/) is an antiemetic and gastroprokinetic agent. It is commonly used to treat nausea and vomiting, to facilitate gastric emptying in people with gastroparesis, and as a treatment for the gastric stasis often associated with migraine headaches.

Medical uses

Clinicians commonly use metoclopramide to treat nausea - including that due to chemotherapy and that occurring post-operatively. Evidence also supports its use for gastroparesis (poor stomach emptying) and gastroesophageal reflux disease.^[1]

Antiemetic

Metoclopramide 5mg tablets (Pliva)

Metoclopramide can treat nausea and vomiting associated with conditions such as uremia, radiation sickness, malignancy, labor, infection, migraine headaches, and emetogenic drugs.^[2]^[3] In the setting of painful conditions such as migraine headaches, metoclopramide may be used in combination with paracetamol (acetaminophen) (available in the UK as Paramax, and in Australia as Metomax), or in combination with aspirin (MigraMax).

Gastroprokinetic

Metoclopramide increases peristalsis of the jejunum and duodenum, increases tone and amplitude of gastric contractions, and relaxes the pyloric sphincter and duodenal bulb. These gastroprokinetic effects make metoclopramide useful in the treatment of gastric stasis (for example: after gastric surgery or diabetic gastroparesis), as an aid in gastrointestinal radiographic studies by accelerating transit through the gastrointestinal system in barium studies, and as an aid in difficult intubation of the small intestine. It is also used in gastroesophageal reflux disease (GERD).

Other indications

By inhibiting the action of dopamine, metoclopramide has sometimes been used to stimulate lactation.^[4] It can also help treat migraines in the setting of allodynia, where it is more effective than triptans.^[5]

Adverse effects

Plastic ampoule of metoclopramide

Common adverse drug reactions (ADRs) associated with metoclopramide therapy include restlessness (akathisia), drowsiness, dizziness, fatigue, and focal dystonia. Infrequent ADRs include hypertension, hypotension, hyperprolactinaemia leading to galactorrhea, constipation, depression, headache, and extrapyramidal effects such as oculogyric crisis. Rare but serious ADRs associated with metoclopramide therapy include agranulocytosis, supraventricular tachycardia, hyperaldosteronism, neuroleptic malignant syndrome, akathisia and tardive dyskinesia.^[3]

Metoclopramide may be the most common cause of drug-induced movement disorders.^[6] The risk of extrapyramidal effects is increased in people under 20 years of age, and with high-dose or prolonged therapy.^[2]^[3] Tardive dyskinesia may be persistent and irreversible in some patients. The majority of reports of tardive dyskinesia occur in people who have used metoclopramide for more than three months.^[6] Consequently, the USFDA recommends that metoclopramide be used for short term treatment, preferably less than 12 weeks. In 2009, the USFDA required all manufacturers of metoclopramide to issue a black box warning regarding the risk of tardive dyskinesia with chronic or high-dose use of the drug.^[6]

Dystonic reactions may be treated with benztropine, diphenhydramine, trihexyphenidyl or procyclidine.

Mechanism of action

Metoclopramide was first described by Dr. Louis Justin-Besançon and C. Laville in 1964.^[7]

It appears to bind to dopamine D₂ receptors where it is a receptor antagonist, and is also a mixed 5-HT₃ receptor antagonist/ 5-HT₄ receptor agonist.

The antiemetic action of metoclopramide is due to its antagonist activity at D₂ receptors in the chemoreceptor trigger zone (CTZ) in the central nervous system (CNS)—this action prevents nausea and vomiting triggered by most stimuli.^[8] At higher doses, 5-HT₃ antagonist activity may also contribute to the antiemetic effect.

The gastroprokinetic activity of metoclopramide is mediated by muscarinic activity, D₂ receptor antagonist activity and 5-HT₄ receptor agonist activity.^[9]^[10] The gastroprokinetic effect itself may also contribute to the antiemetic effect. Metoclopramide also increases the tone of the lower esophageal sphincter.^[11]

Contraindications and precautions

Metoclopramide is contraindicated in pheochromocytoma. It should be used with caution in Parkinson's disease since, as a dopamine antagonist, it may worsen symptoms. Long-term use should be avoided in patients with clinical depression as it may worsen mental state.^[3] Also contraindicated with a suspected bowel obstruction.^[1]

Patients with a history of ADHD, Restless legs syndrome, Hyperprolactinaemia, and Parkinson's disease should be closely monitored when using dopamine antagonists for treatment of emesies. Patients who take antipsychotics are recommended not to take metoclopramide.

Use in pregnancy

Metoclopramide has long been used in all stages of pregnancy with no evidence of harm to the mother or unborn baby.^[12] A large cohort study of babies born to Israeli women exposed to metoclopramide during pregnancy found no evidence that the drug increases the risk of congenital malformations, low birth weight, preterm birth, or perinatal mortality. ^[13] Metoclopramide is excreted into milk.^[12]

Brand names

It is available under various trade names including Maxolon in Australia and the UK (Shire/Valeant), Reglan in the USA (Schwarz Pharma), Degan (Lek), Maxeran (Sanofi Aventis), Primperan (Sanofi Aventis), Pylomid (Bosnalijek), Plazilin (Iran), "'Tomit'" (Indonesia), Cerucal (AWD Pharma), Pramin (Rafa, Israel)), Plasil (Brazil - Italy)), Pulin(Malaysia).

Veterinary use

Metoclopramide is also used in animals. It is commonly used to prevent vomiting in cats and dogs. It is also used as a gut stimulant in rabbits.^[14]

References

^ ^a ^b "Metoclopramide hydrochloride". Monograph. The American Society of Health-System Pharmacists. http://www.drugs.com/monograph/metoclopramide-hydrochloride.html. Retrieved 2011-04-03.
^ ^a ^b "Maxolon (Australian Approved Product Information)". Valeant Pharmaceuticals. 2000. http://www.mydr.com.au/medicines/cmis/maxolon-tablets.
^ ^a ^b ^c ^d Rossi S., ed. (2006). Australian Medicines Handbook. Adelaide: Australian Medicines Handbook. ISBN 0-9757919-2-3.
^ "Metoclopramide". lowmilksupply.org. http://www.lowmilksupply.org/metoclopramide.shtml.
^ Snow, V.; Weiss, K.; Wall, E. M.; Mottur-Pilson, C.; American Academy of Family Physicians; American College of Physicians-American Society of Internal Medicine (2002). "Pharmacologic Management of Acute Attacks of Migraine and Prevention of Migraine Headache" (pdf). Annals of Internal Medicine 137 (10): 840–849. PMID 12435222. http://www.annals.org/content/137/10/840.full.pdf. edit
^ ^a ^b ^c "FDA requires boxed warning and risk mitigation strategy for metoclopramide-containing drugs" (Press release). U.S. Food and Drug Administration. 2009-02-26. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm149533.htm. Retrieved 2009-06-11. "Lay Summary – WebMD". http://www.webmd.com/digestive-disorders/news/20090227/metoclopramide-drugs-get-black-box-warning.
^ Justin-Besancon, L.; Laville, C. (1964). "Antiemetic Action of Metoclopramide with Respect to Apomorphine and Hydergine" (in French). Comptes Rendus des Séances de la Société de Biologie et de ses Filiales 158: 723–727. PMID 14186927. edit
^ Rang, H. P.; Dale, M. M.; Ritter, J. M.; Moore, P. K. (2003). Pharmacology (5th ed.). Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.
^ Sweetman S., ed. (2004). Martindale: The Complete Drug Reference (34th ed.). London: Pharmaceutical Press. ISBN 0-85369-550-4.
^ Tonini, M.; Candura, S. M.; Messori, E.; Rizzi, C. A. (1995). "Therapeutic Potential of Drugs with Mixed 5-HT4 Agonist/5-HT3 Antagonist Action in the Control of Emesis". Pharmacological Research 31 (5): 257–260. ISSN 1043-6618. PMID 7479521. edit
^ Feldman, M.; Friedman, L. S.; Brandt, L. J., eds. (2010). "Ch. 43: Gastroesophageal Reflux Disease". Sleisenger and Fordtran's Gastrointestinal and Liver Disease (9th ed.). Philadelphia: Saunders. ISBN 978-1-4160-6189-2.
^ ^a ^b Briggs, G. G.; Freeman, R. K.; Yaffe, S. J. (2008). Drugs in Pregnancy and Lactation (8th ed.). Philadelphia: Lippincott Williams & Wilkins. pp. 1197–1200. ISBN 0-7817-7876-X. http://books.google.com/books?id=YOEV2w3XTxsC&pg=PA1197. Retrieved 2009-06-11.
^ Matok, I.; Gorodischer, R.; Koren, G.; Sheiner, E.; Wiznitzer, A.; Levy, A. (2009). "The Safety of Metoclopramide Use in the First Trimester of Pregnancy" (pdf). New England Journal of Medicine 360 (24): 2528–2535. doi:10.1056/NEJMoa0807154. PMID 19516033. http://www.nejm.org/doi/pdf/10.1056/NEJMoa0807154. edit
^ Mikota, S. K.; Plumb, D. C. (2003-06). "Metoclopramide HCl". The Elephant Formulary. Elephant Care International. http://www.elephantcare.org/Drugs/metoclop.htm.

UpToDate Contents

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2. 成人におけるレストレスレッグ症候群の治療 treatment of restless legs syndrome in adults
3. Palliative care: Assessment and management of nausea and vomiting
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5. 傍神経節腫：限局性疾患の治療 paragangliomas treatment of locoregional disease

English Journal

Metoclopramide-induced hyperprolactinemia effects on the pituitary and uterine prolactin receptor expression.

Amaral VC, Maciel GA, Carvalho KC, Marcondes RR, Soares JM Jr, Baracat EC.SourceLaboratorio de Ginecologia Estrutural e Molecular (LIM-58), Disciplina de Ginecologia, Faculdade de Medicina da Universidade de São Paulo, SP, Brazil. Electronic address: vcdoamaral@gmail.com.
General and comparative endocrinology.Gen Comp Endocrinol.2013 Aug 1;189:105-10. doi: 10.1016/j.ygcen.2013.04.037. Epub 2013 May 14.
In this work we have evaluated the gene expression profile of prolactin and prolactin receptor in the pituitary and the uterus of female mice with metoclopramide-induced hyperprolactinemia treated with estrogen and/or progesterone. For this purpose, 49 Swiss female mice were allocated to seven group
PMID 23684968

Dysarthria induced by irinotecan in a patient with colorectal cancer.

Lee KA, Kang HW, Ahn JH, Suk HJ, Kim H.SourceKyung A. Lee, B.S., is Pharmacist; Hee Won Kang, B.S., is Pharmacist; Ji Hyune Ahn, M.S., is Pharmacist; and Hyoun Ju Suk, B.S., is Director, Department of Pharmacy, Yonsei University Healthcare System, Seoul, South Korea. Hyunah Kim, Pharm.D., is Assistant Professor, College of Pharmacy, Ajou University, Suwon, South Korea.
American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists.Am J Health Syst Pharm.2013 Jul 1;70(13):1140-3. doi: 10.2146/ajhp120542.
PURPOSE: Successful management and subsequent prevention of a rare adverse drug reaction (ADR) associated with irinotecan chemotherapy are reported.SUMMARY: A 49-year-old man with meta-static colon cancer undergoing treatment with i.v. irinotecan (180 mg/m(2) to be infused over 120 minutes) as part
PMID 23784161

BET 1: Metoclopramide or prochlorperazine for headache in acute migraine?

[No authors listed]AbstractA short-cut review was carried out to determine whether metoclopramide or prochlorperazine was better at relieving headache in patients attending the emergency department with acute migraine. Eighty-one papers were found using the reported searches, of which three presented the best evidence to answer the clinical question. The author, date and country of publication, patient group studied, study type, relevant outcomes, results and study weaknesses of those best papers are shown in table 1. It is concluded that in adult patients presenting to the emergency department with acute migraine, prochlorperazine 10 mg is better than metoclopramide 10 mg at relieving headache.
Emergency medicine journal : EMJ.Emerg Med J.2013 Jul;30(7):595-6. doi: 10.1136/emermed-2013-202853.1.
A short-cut review was carried out to determine whether metoclopramide or prochlorperazine was better at relieving headache in patients attending the emergency department with acute migraine. Eighty-one papers were found using the reported searches, of which three presented the best evidence to answ
PMID 23765765

Japanese Journal

Dopamine D2–Receptor Antagonists Ameliorate Indomethacin-Induced Small Intestinal Ulceration in Mice by Activating α7 Nicotinic Acetylcholine Receptors

Yasuda Masashi,Kawahara Ryoji,Hashimura Hiroshi,Yamanaka Naoki,Iimori Maho,Amagase Kikuko,Kato Shinichi,Takeuchi Koji
Journal of Pharmacological Sciences 116(3), 274-282, 2011
… Dopamine D2–receptor antagonists, such as domperidone and metoclopramide, enhance the release of ACh from vagal efferent nerves. … The present study examined the effects of domperidone and metoclopramide on indomethacin-induced small intestinal ulceration in mice, focusing on the α7AChR. … 10 mg/kg) and metoclopramide (0.03 – … Similar effects were also observed by metoclopramide. …
NAID 130001014458

Multivariate Optimization Strategies in the Development of an Electro-analytical Method for the Assay of Metoclopramide Using Mercury-Film-Modified Carbon Nanotube Paste Electrode

MENDES Camila Bitencourt,ANDRADE Felipe Nascimento,SEGATELLI Mariana Gava,PEREIRA Arnaldo Cesar,DRAGUNSKI Douglas Cardoso,TARLEY Cesar Ricardo Teixeira
Bulletin of the Chemical Society of Japan 83(11), 1364-1366, 2010-11-15
NAID 10027652711

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★リンクテーブル★

リンク元	「メトクロプラミド」「ベンズアミド」
拡張検索	「metoclopramide hydrochloride」「metoclopramide test」

「メトクロプラミド」

Metoclopramide
Systematic (IUPAC) name
	4-amino-5-chloro-N-(2-(diethylamino)ethyl)-; 2-methoxybenzamide
Clinical data
Trade names	Reglan
AHFS/Drugs.com	monograph
MedlinePlus	a684035
Pregnancy cat.	A (Au), B (U.S.)
Legal status	S3/S4 (Au), POM (UK), ℞-only (U.S.)
Routes	Oral, intravenous, intramuscular
Pharmacokinetic data
Bioavailability	80±15% (oral)
Metabolism	Hepatic
Half-life	5–6 hours
Excretion	70–85% renal, 2% faecal
Identifiers
CAS number	364-62-5
ATC code	A03FA01
PubChem	CID 4168
IUPHAR ligand	241
DrugBank	DB01233
ChemSpider	4024
UNII	L4YEB44I46
KEGG	D00726
ChEBI	CHEBI:107736
ChEMBL	CHEMBL86
Chemical data
Formula	C14H22ClN3O2
Mol. mass	299.80 g/mol
	SMILES Clc1cc(c(OC)cc1N)C(=O)NCCN(CC)CC;
	InChI InChI=1S/C14H22ClN3O2/c1-4-18(5-2)7-6-17-14(19)10-8-11(15)12(16)9-13(10)20-3/h8-9H,4-7,16H2,1-3H3,(H,17,19) ; Key:TTWJBBZEZQICBI-UHFFFAOYSA-N ;
Physical data
Melt. point	147.3 °C (297 °F)
(what is this?) (verify);

　　[★]

英: metoclopramide
関: ベンズアミド
商: Reglan、プリンペラン、エリーテン、テルペラン、プロメチン、アノレキシノン、ネオプラミール、フォリクロン、プラミール、ペラプリン、プリンパール

健胃薬

胃腸機能調整薬

特徴

ベンズアミド系

構造

ベンズアミド骨格を有する

薬理作用

消化器機能をつかさどる脳幹部に作用し、食道から近位小腸までの平滑筋の運動を増強し、胃内容物の排出、腸管内での移動を促進する
中枢性のみならず末梢性の嘔吐を抑制する。

適応

プリンペラン錠

次の場合における消化器機能異常（悪心・嘔吐・食欲不振・腹部膨満感）

胃炎、胃・十二指腸潰瘍、胆嚢・胆道疾患、腎炎、尿毒症、乳幼児嘔吐、薬剤（制癌剤・抗生物質・抗結核剤・麻酔剤）投与時、胃内・気管内挿管時、放射線照射時、開腹術後

X線検査時のバリウムの通過促進

禁忌

プリンペラン錠

1. 本剤の成分に対し過敏症の既往歴のある患者
2. 褐色細胞腫の疑いのある患者［急激な昇圧発作を起こすおそれがある。］
3. 消化管に出血、穿孔又は器質的閉塞のある患者［本剤には消化管運動の亢進作用があるため、症状を悪化させるおそれがある。］

副作用

遅発性ジスキネジア　←　D2受容体拮抗作用を有するため。

長期投与により、口周部等の不随意運動があらわれ、投与中止後も持続することがあるので、観察を十分に行い、異常が認められた場合には適切な処置を行うこと。(プリンペラン錠)

添付文書

プリンペラン

http://www.info.pmda.go.jp/go/pack/2399004F1200_1_02/

「ベンズアミド」

　　[★]

英: benzamide
関

向精神薬

抗精神病薬

消化性潰瘍治療薬
消化性潰瘍治療薬から見いだされた

構造

ベンズアミド骨格を有する

作用

D2受容体阻害作用

ベンズアミド系代表薬物

「metoclopramide hydrochloride」

　　[★]

塩酸メトクロプラミド

関: metoclopramide

「metoclopramide test」

　　[★] メトクロプラミド試験

[AHFS-1] "Metoclopramide hydrochloride". Monograph. The American Society of Health-System Pharmacists. http://www.drugs.com/monograph/metoclopramide-hydrochloride.html. Retrieved 2011-04-03.

[Maxolon-2] "Maxolon (Australian Approved Product Information)". Valeant Pharmaceuticals. 2000. http://www.mydr.com.au/medicines/cmis/maxolon-tablets.

[AMH2006-3] Rossi S., ed. (2006). Australian Medicines Handbook. Adelaide: Australian Medicines Handbook. ISBN 0-9757919-2-3.

[4] "Metoclopramide". lowmilksupply.org. http://www.lowmilksupply.org/metoclopramide.shtml.

[Snow2002-5] Snow, V.; Weiss, K.; Wall, E. M.; Mottur-Pilson, C.; American Academy of Family Physicians; American College of Physicians-American Society of Internal Medicine (2002). "Pharmacologic Management of Acute Attacks of Migraine and Prevention of Migraine Headache" (pdf). Annals of Internal Medicine 137 (10): 840–849. PMID 12435222. http://www.annals.org/content/137/10/840.full.pdf. edit

[FDA2009-6] "FDA requires boxed warning and risk mitigation strategy for metoclopramide-containing drugs" (Press release). U.S. Food and Drug Administration. 2009-02-26. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm149533.htm. Retrieved 2009-06-11. "Lay Summary – WebMD". http://www.webmd.com/digestive-disorders/news/20090227/metoclopramide-drugs-get-black-box-warning.

[Justin1964-7] Justin-Besancon, L.; Laville, C. (1964). "Antiemetic Action of Metoclopramide with Respect to Apomorphine and Hydergine" (in French). Comptes Rendus des Séances de la Société de Biologie et de ses Filiales 158: 723–727. PMID 14186927. edit

[Rang2003-8] Rang, H. P.; Dale, M. M.; Ritter, J. M.; Moore, P. K. (2003). Pharmacology (5th ed.). Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.

[Sweetman2004-9] Sweetman S., ed. (2004). Martindale: The Complete Drug Reference (34th ed.). London: Pharmaceutical Press. ISBN 0-85369-550-4.

[Tonini1995-10] Tonini, M.; Candura, S. M.; Messori, E.; Rizzi, C. A. (1995). "Therapeutic Potential of Drugs with Mixed 5-HT4 Agonist/5-HT3 Antagonist Action in the Control of Emesis". Pharmacological Research 31 (5): 257–260. ISSN 1043-6618. PMID 7479521. edit

[Feldman2010-11] Feldman, M.; Friedman, L. S.; Brandt, L. J., eds. (2010). "Ch. 43: Gastroesophageal Reflux Disease". Sleisenger and Fordtran's Gastrointestinal and Liver Disease (9th ed.). Philadelphia: Saunders. ISBN 978-1-4160-6189-2.

[Briggs2008-12] Briggs, G. G.; Freeman, R. K.; Yaffe, S. J. (2008). Drugs in Pregnancy and Lactation (8th ed.). Philadelphia: Lippincott Williams & Wilkins. pp. 1197–1200. ISBN 0-7817-7876-X. http://books.google.com/books?id=YOEV2w3XTxsC&pg=PA1197. Retrieved 2009-06-11.

[Matok2009-13] Matok, I.; Gorodischer, R.; Koren, G.; Sheiner, E.; Wiznitzer, A.; Levy, A. (2009). "The Safety of Metoclopramide Use in the First Trimester of Pregnancy" (pdf). New England Journal of Medicine 360 (24): 2528–2535. doi:10.1056/NEJMoa0807154. PMID 19516033. http://www.nejm.org/doi/pdf/10.1056/NEJMoa0807154. edit

[14] Mikota, S. K.; Plumb, D. C. (2003-06). "Metoclopramide HCl". The Elephant Formulary. Elephant Care International. http://www.elephantcare.org/Drugs/metoclop.htm.

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metoclopramide