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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/06/25 11:07:02」(JST)
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| Systematic (IUPAC) name | |
|---|---|
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4-Amino-5-chloro-N-(2-(diethylamino)ethyl)-2-methoxybenzamide
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| Clinical data | |
| Pronunciation | /ˌmɛtəˈklɒprəmaɪd/ |
| Trade names | Reglan, Metozolv, others[1] |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a684035 |
| License data |
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| Pregnancy category |
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| Routes of administration |
Oral, intravenous, intramuscular |
| Legal status | |
| Legal status |
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| Pharmacokinetic data | |
| Bioavailability | 80±15% (oral) |
| Metabolism | Hepatic |
| Biological half-life | 5 h to 6 h |
| Excretion | 70–85% renal, 2% faecal |
| Identifiers | |
| CAS Number | 364-62-5 Y |
| ATC code | A03FA01 (WHO) |
| PubChem | CID 4168 |
| IUPHAR/BPS | 241 |
| DrugBank | DB01233 Y |
| ChemSpider | 4024 Y |
| UNII | L4YEB44I46 Y |
| KEGG | D00726 Y |
| ChEBI | CHEBI:107736 Y |
| ChEMBL | CHEMBL86 Y |
| Chemical data | |
| Formula | C14H22ClN3O2 |
| Molar mass | 299.80 g/mol |
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SMILES
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InChI
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| Physical data | |
| Melting point | 147.3 °C (297.1 °F) |
| (verify) | |
Metoclopramide is a medication used mostly for stomach and esophageal problems.[2] It is commonly used to treat nausea and vomiting, to help with emptying of the stomach in people with delayed stomach emptying due to either diabetes or following surgery, and to help with gastroesophageal reflux disease.[3] It is also used to treat migraine headaches.[4][needs update]
Common side effects include: feeling tired, diarrhea, and feeling restless. More serious side effects include: movement disorder like tardive dyskinesia, a condition called neuroleptic malignant syndrome, and depression.[3] It is thus rarely recommended that people take the medication for longer than twelve weeks.[3] It is pregnancy category B in the United States and category A in Australia, meaning no evidence of harm has been found after being taken by many pregnant women.[3][5] It belongs to the group of medications known as dopamine-receptor antagonists.[3]
In 2012, metoclopramide was one of the top 100 most prescribed medications in the United States.[6] It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.[7]
Contents
- 1 Medical uses
- 2 Adverse effects
- 3 Cautions and contraindications
- 3.1 Pregnancy
- 3.2 Infants
- 4 Mechanism of action
- 5 Brand names
- 6 Veterinary use
- 7 See also
- 8 References
- 9 Further reading
Medical uses
Metoclopramide 5-mg tablets (Pliva)
Metoclopramide is commonly used to treat nausea and vomiting associated with conditions such as uremia, radiation sickness, cancer and the effects of chemotherapy, labor, infection, migraine headaches, and emetogenic drugs.[3][8][9][10] In the setting of painful conditions such as migraine headaches, metoclopramide may be used in combination with paracetamol (acetaminophen) or in combination with aspirin. It is also used preventatively by some EMS providers when transporting people who are conscious and spinally immobilized.[11]
Evidence also supports its use for gastroparesis, a condition that causes the stomach to empty poorly, and gastroesophageal reflux disease.[3] It is also used in pregnancy as a second choice for treatment of hyperemesis gravidarum (severe nausea and vomiting of pregnancy).[3] It increases peristalsis of the duodenum and jejunum, increases tone and amplitude of gastric contractions, and relaxes the pyloric sphincter and duodenal bulb, while simultaneously increasing lower esophageal sphincter tone. 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.[12]
Adverse effects
Plastic ampoule of metoclopramide
Common adverse drug reactions (ADRs) associated with metoclopramide therapy include restlessness (akathisia), 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.[9]
Metoclopramide may be the most common cause of drug-induced movement disorders.[13] The risk of extrapyramidal effects is increased in people under 20 years of age, and with high-dose or prolonged therapy.[8][9] 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.[13] Consequently, the US Food and Drug Administration (FDA) recommends that metoclopramide be used for short-term treatment, preferably less than 12 weeks. In 2009, the FDA 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.[13]
Dystonic reactions may be treated with benzatropine, diphenhydramine, trihexyphenidyl, or procyclidine. Symptoms usually subside with diphenhydramine injected intramuscularly.[14] Agents in the benzodiazepine class of drugs may be helpful, but benefits are usually modest and side effects of sedation and weakness can be problematic.[15]
In some cases, the akathisia effects of metoclopramide are directly related to the infusion rate when the drug is administered intravenously. Side effects were usually seen in the first 15 min after the dose of metoclopramide.[16]
Cautions and contraindications
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 one's mental state.[9] It is contraindicated in patients with a suspected bowel obstruction[3] and in epilepsy, if a stomach operation has been performed in the previous three or four days, if the patient has ever had bleeding, perforation or blockage of the stomach, in cases of pheochromocytoma, and in newborn babies.[10]
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 emesis. Patients who take antipsychotics are recommended not to take metoclopramide.
In 2011, the country of France restricted use of the drug in children and adolescents, and issued concerns about usage in certain populations.[17]
Pregnancy
Metoclopramide has long been used in all stages of pregnancy with no evidence of harm to the mother or unborn baby.[18] In the USA, it has been assigned to pregnancy category B by the US FDA.[19] 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. [20] A large cohort study in Denmark found, in addition, no association between metoclopramide exposure and miscarriage.[21] Metoclopramide is excreted into milk.[18]
Infants
A systematic review found a wide range of reported outcomes for treatment of gastroesophageal reflux disease (GERD) in infants and concluded a "poor" rating of evidence and "inconclusive" rating of safety and efficacy for the treatment of GERD in infants.[22]
Mechanism of action
Metoclopramide was first described by Dr. Louis Justin-Besançon and C. Laville in 1964.[23]
It appears to bind to dopamine D2 receptors with nanomolar affinity (Ki 28.8 nM),[24] 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 in the central nervous system — this action prevents nausea and vomiting triggered by most stimuli.[25] 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.[26][27] The gastroprokinetic effect itself may also contribute to the antiemetic effect. Metoclopramide also increases the tone of the lower esophageal sphincter.[28]
Brand names
Metoclopramide is available world-wide under various trade names.[1]
Veterinary use
Metoclopramide is also commonly used to prevent vomiting in cats and dogs. It is also used as a gut stimulant in rabbits.[29]
See also
- Benzamide, the chemical class to which metoclopramide belongs
- Bromopride, the bromo- analogue of metoclopramide
- Cisapride, a benzamide with a different mechanism of action
- Itopride, a newer benzamide with effects similar to those of metoclopramide
- Domperidone, another drug with antiemetic and prokinetic properties
References
- ^ a b Drugs.com International names for metoclopramide Page accessed March 28, 2016
- ^ "Metoclopramide". nlm.nih.gov. Retrieved 28 September 2014.
- ^ a b c d e f g h i "Metoclopramide hydrochloride". Monograph. The American Society of Health-System Pharmacists. Retrieved 2014-09-27.
- ^ Derry, S; Moore, RA; McQuay, HJ (Nov 10, 2010). "Paracetamol (acetaminophen) with or without an antiemetic for acute migraine headaches in adults.". The Cochrane database of systematic reviews (11): CD008040. doi:10.1002/14651858.CD008040.pub2. PMID 21069700.
- ^ "Prescribing medicines in pregnancy database". Australian Government. 3 March 2014. Retrieved 22 April 2014.
- ^ Bartholow, Michael. "Top 200 Drugs of 2012". Pharmacy Times. Retrieved 22 April 2014.
- ^ "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.
- ^ a b "Maxolon (Australian Approved Product Information)". Valeant Pharmaceuticals. 2000.
- ^ a b c d Rossi S., ed. (2006). Australian Medicines Handbook. Adelaide: Australian Medicines Handbook. ISBN 0-9757919-2-3.
- ^ a b http://xpil.medicines.org.uk/ViewPil.aspx?DocID=8068
- ^ "Ambulance Victoria Clinical Guideline A0701"http://www.ambulance.vic.gov.au/media/docs/Adult%20CPG%20wm-a01f0e1e-4fc0-405c-bc83-3136adf4a723-0.pdf
- ^ "METOCLOPRAMIDE (metoclopramide hydrochloride) injection, solution [Hospira, Inc.]" http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=373ba08b-33ad-49fc-28a7-928e89a65314#nlm34089-3
- ^ 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. Retrieved 2009-06-11. "Lay Summary – WebMD".
- ^ "Metoclopramide (metoclopramide hydrochloride) injection, solution [Hospira, Inc.]" http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=373ba08b-33ad-49fc-28a7-928e89a65314#nlm34089-3
- ^ Olanow C, Schapira AV. Chapter 372. Parkinson's Disease and Other Movement Disorders. In: Longo DL, Fauci AS, Kasper DL, Hauser SL, Jameson J, Loscalzo J. eds. Harrison's Principles of Internal Medicine, 18e. New York, NY: McGraw-Hill; 2012.
- ^ Parlak, I; Atilla, R; Cicek, M; Parlak, M; Erdur, B; Guryay, M; Sever, M; Karaduman, S (Sep 2005). "Rate of metoclopramide infusion affects the severity and incidence of akathisia.". Emergency medicine journal : EMJ 22 (9): 621–4. doi:10.1136/emj.2004.014712. PMC 1726928. PMID 16113179.
- ^ "Contre-indication des spécialités à base de métoclopramide (Primpéran® et génériques) chez l’enfant et l’adolescent et renforcement des informations sur les risques neurologiques et cardiovasculaires - Lettre aux professionnels de santé".
- ^ 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. Retrieved 2009-06-11.
- ^ http://www.drugs.com/metoclopramide.html
- ^ 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.
- ^ Pasternak, B. R.; Svanström, H.; Mølgaard-Nielsen, D.; Melbye, M.; Hviid, A. (2013). "Metoclopramide in Pregnancy and Risk of Major Congenital Malformations and Fetal Death". JAMA 310 (15): 1601–1611. doi:10.1001/jama.2013.278343. PMID 24129464.
- ^ Hibbs, AM; Lorch, SA (Aug 2006). "Metoclopramide for the treatment of gastroesophageal reflux disease in infants: a systematic review.". Pediatrics 118 (2): 746–52. doi:10.1542/peds.2005-2664. PMID 16882832.
- ^ Justin-Besancon, L.; Laville, C. (1964). "Antiemetic Action of Metoclopramide with Respect to Apomorphine and Hydergine". Comptes Rendus des Séances de la Société de Biologie et de ses Filiales (in French) 158: 723–727. PMID 14186927.
- ^ Prediction of Catalepsies Induced by Amiodarone, Aprindine and Procaine: Similarity in Conformation of Diethylaminoethyl Side Chain http://jpet.aspetjournals.org/content/287/2/725.full.pdf
- ^ 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. doi:10.1016/1043-6618(95)80029-8. ISSN 1043-6618. PMID 7479521.
- ^ 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.
- ^ Mikota, S. K.; Plumb, D. C. (June 2003). "Metoclopramide HCl". The Elephant Formulary. Elephant Care International.
Further reading
- Brenner, G. M. (2000). Pharmacology. London: Saunders. ISBN 0-7216-7757-6.
- Compendium of Pharmaceuticals and Specialties 2011. Toronto: Canadian Pharmacists Association. 2011. ISBN 978-1-894402-54-5.
- Anderson, E. P.; Freeman, E. B. (May 2004). "Recognition of Movement Disorders and Extrapyramidal side effects - would you recognize them if you see them?" (pdf). Practical Gastroenterology: 14.
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UpToDate Contents
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- 1. 吃逆の概要 overview of hiccups
- 2. 胃不全麻痺の治療 treatment of gastroparesis
- 3. 成人における片頭痛の急性期治療 acute treatment of migraine in adults
- 4. 遅発性ジスキネジア：病因および疫学 tardive dyskinesia etiology and epidemiology
- 5. 遅発性ジスキネジア：予防および治療 tardive dyskinesia prevention and treatment
English Journal
- Medication use in the neonatal intensive care unit.
- Hsieh EM1, Hornik CP2, Clark RH3, Laughon MM4, Benjamin DK Jr2, Smith PB2; Best Pharmaceuticals for Children Act—Pediatric Trials Network.
- American journal of perinatology.Am J Perinatol.2014 Oct;31(9):811-22. doi: 10.1055/s-0033-1361933. Epub 2013 Dec 17.
- Objective The aim of the article is to provide an update on medication use in infants admitted to the neonatal intensive care unit (NICU) in the United States and examine how use has changed over time. Study Design We performed a retrospective review (2005-2010) of a large prospectively collecte
- PMID 24347262
- Poly(N-isopropylacrylamide-co-methacrylic acid) pH/thermo-responsive porous hydrogels as self-regulated drug delivery system.
- Constantin M1, Bucatariu S1, Harabagiu V1, Popescu I1, Ascenzi P2, Fundueanu G3.
- European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.Eur J Pharm Sci.2014 Oct 1;62:86-95. doi: 10.1016/j.ejps.2014.05.005. Epub 2014 May 15.
- A dual drug delivery system based on a "biosensor" (pH-sensitive unit) and a delivery component (thermosensitive hydrogel) was developed. The pH/thermosensitive hydrogel is able to restore the thermosensitive characteristics after electrostatic interaction of the pH-sensitive units with selected bio
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- Understanding Variability in Posaconazole Exposure Using an Integrated Population Pharmacokinetic Analysis.
- Dolton MJ1, Brüggemann RJ2, Burger DM2, McLachlan AJ3.
- Antimicrobial agents and chemotherapy.Antimicrob Agents Chemother.2014 Sep 8. pii: AAC.03777-14. [Epub ahead of print]
- Posaconazole oral suspension is widely used for antifungal prophylaxis and treatment in immunocompromised patients, with highly variable pharmacokinetics reported in patients due to inconsistent oral absorption. This study aimed to characterise the pharmacokinetics of posaconazole in adults and inve
- PMID 25199779
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★リンクテーブル★
| リンク元 | 「メトクロプラミド」 |
| 関連記事 | 「reglan」 |
「メトクロプラミド」
- 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/
「reglan」
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