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Encyclopedia > Metoclopramide
Metoclopramide
Systematic (IUPAC) name
4-amino-5-chloro-N-(2-(diethylamino)ethyl)-
2-methoxybenzamide
Identifiers
CAS number 364-62-5
ATC code A03FA01
PubChem 4168
DrugBank APRD00665
Chemical data
Formula C14H22ClN3O2 
Mol. mass 299.80 g/mol
Pharmacokinetic data
Bioavailability 80±15% (oral)
Metabolism Hepatic
Half life 5–6 hours
Excretion 70–85% renal, 2% faecal
Therapeutic considerations
Pregnancy cat.

A (Au), B (U.S.) Image File history File links Metoclopramide. ... Image File history File links Size of this preview: 800 × 480 pixelsFull resolution (1000 × 600 pixel, file size: 97 KB, MIME type: image/png) File history Legend: (cur) = this is the current file, (del) = delete this old version, (rev) = revert to this old version. ... IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A division of the Anatomical Therapeutic Chemical Classification System A Alimentary tract and metabolism A03A Drugs for functional bowel disorders A03AA Synthetic anticholinergics, esters with tertiary amino group A03AA01 Oxyphencyclimine A03AA03 Camylofin A03AA04 Mebeverine A03AA05 Trimebutine A03AA06 Rociverine A03AA07 Dicycloverine A03AA08 Dihexyverine A03AA09 Difemerine A03AA30 Piperidolate A03AB Synthetic anticholinergics, quaternary... PubChem is a database of chemical molecules. ... The DrugBank database available at the University of Alberta is a unique bioinformatics and cheminformatics resource that combines detailed drug (i. ... This article or section does not cite any references or sources. ... General Name, Symbol, Number carbon, C, 6 Chemical series nonmetals Group, Period, Block 14, 2, p Appearance black (graphite) colorless (diamond) Standard atomic weight 12. ... General Name, Symbol, Number hydrogen, H, 1 Chemical series nonmetals Group, Period, Block 1, 1, s Appearance colorless Atomic mass 1. ... General Name, Symbol, Number chlorine, Cl, 17 Chemical series halogens Group, Period, Block 17, 3, p Appearance yellowish green Standard atomic weight 35. ... General Name, Symbol, Number nitrogen, N, 7 Chemical series nonmetals Group, Period, Block 15, 2, p Appearance colorless gas Standard atomic weight 14. ... General Name, Symbol, Number oxygen, O, 8 Chemical series nonmetals, chalcogens Group, Period, Block 16, 2, p Appearance colorless (gas) very pale blue (liquid) Standard atomic weight 15. ... The molecular mass (abbreviated Mr) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... The liver is an organ in vertebrates including humans. ... It has been suggested that Effective half-life be merged into this article or section. ... Excretion is the process of eliminating waste products of metabolism and other materials that are of no use. ... Kidneys viewed from behind with spine removed The kidneys are bean-shaped excretory organs in vertebrates. ... Feces, faeces, or fæces (see spelling differences) In humans, defecation may occur (depending on the individual and the circumstances) from once every two or three days to several times a day. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ... Anthem Advance Australia Fair Royal anthem: God Save the Queen Capital Canberra Largest city Sydney Official languages English (de facto 1) Government Federal constitutional monarchy and parliamentary democracy  -  Queen Elizabeth II  -  Governor-General Michael Jeffery  -  Prime Minister John Howard Independence from the United Kingdom   -  Constitution 1 January 1901   -  Statute of... Motto: (Out Of Many, One) (traditional) In God We Trust (1956 to date) Anthem: The Star-Spangled Banner Capital Washington D.C. Largest city New York City None at federal level (English de facto) Government Federal constitutional republic  - President George Walker Bush (R)  - Vice President Dick Cheney (R) Independence from...

Legal status

S3/S4 (Au), POM (UK), ℞-only (U.S.) The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ...

Routes Oral, IV, IM

Metoclopramide (INN) (IPA: [mɛtəˈkloprəmaɪd, -ˈklɒ-]) is a potent dopamine receptor antagonist used for its antiemetic and prokinetic properties. Thus it is primarily used to treat nausea and vomiting, and to facilitate gastric emptying in patients with gastric stasis. In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... An intravenous drip in a hospital Intravenous therapy or IV therapy is the administration of liquid substances directly into a vein. ... Intramuscular injection is an injection of a substance directly into a muscle. ... An International Nonproprietary Name (INN) is the official non-proprietary or generic name given to a pharmaceutical substance, as designated by the World Health Organization. ... Articles with similar titles include the NATO phonetic alphabet, which has also informally been called the “International Phonetic Alphabet”. For information on how to read IPA transcriptions of English words, see IPA chart for English. ... The dopamine receptors are a class of metabotropic G-protein-coupled receptors with the neurotransmitter dopamine as their endogenous ligand. ... Antagonists In medicine and biology, a receptor antagonist is a ligand that inhibits the function of an agonist and inverse agonist for a specific receptor. ... An antiemetic is a drug that is effective against vomiting and nausea. ... This article or section does not adequately cite its references or sources. ... In anatomy, the stomach (in ancient Greek στομάχι) is an organ in the alimentary canal used to digest food. ...


It is available under various trade names including: Maxolon (Shire/Valeant), Reglan (Wyeth), Degan (Lek), Maxeran (Sanofi Aventis), Primperan (Sanofi Aventis), and Pylomid (Bosnalijek). It was protected under U.S. patent 3177252 until 6 April 1982. A trade name, also known as a trading name or a business name, is the legal name of a business, or the name which a business trades under for commercial purposes. ... Shire Pharmaceuticals is British manufacturer of pharmaceuticals products including Adderall and Carbatrol. ... Valeant Pharmaceuticals International is a pharmaceutical company with activities spanning the drug discovery pipeline from target identification through clinical trials and commercialization. ... Wyeth, formerly known as American Home Products, is one of the largest pharmaceutical companies in the world. ... Lek has three meanings: The Albanian Lek currency. ... Sanofi-aventis (Euronext: SAN, NYSE: SNY), headquartered in Paris, France, is one of the 3 largest pharmaceutical companies in the world, along with Pfizer,GlaxoSmithKline. ... Sanofi-aventis (Euronext: SAN, NYSE: SNY), headquartered in Paris, France, is one of the 3 largest pharmaceutical companies in the world, along with Pfizer,GlaxoSmithKline. ... Category: ... A patent is a set of exclusive rights granted by a state to a patentee for a fixed period of time in exchange for a disclosure of an invention. ...

Contents

Mode of action

Metoclopramide was first described by Dr. Louis Justin-Besançon and C. Laville in 1964.[1] 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 receptors agonist. 1964 (MCMLXIV) was a leap year starting on Wednesday (the link is to a full 1964 calendar). ... The dopamine receptors are a class of metabotropic G-protein-coupled receptors with the neurotransmitter dopamine as their endogenous ligand. ... Antagonists In medicine and biology, a receptor antagonist is a ligand that inhibits the function of an agonist and inverse agonist for a specific receptor. ... In the field of neurochemistry, 5-HT receptors are receptors for the neurotransmitter and peripheral signal mediator serotonin, also known as 5-hydroxytryptamine or 5-HT. 5-HT receptors are located on the cell membrane of nerve cells and other cell types in animals and mediate the effects of serotonin...


The anti-emetic 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.[2] At higher doses, 5-HT3 antagonist activity may also contribute to the anti-emetic effect. The Chemoreceptor trigger zone (CTZ) is an area of the brain which receives inputs from blood-borne drugs or hormones, and communicates with the Vomit Centre, to initiate vomiting. ... A diagram showing the CNS: 1. ...


The prokinetic activity of metoclopramide is mediated by muscarinic activity, D2 receptor antagonist activity and 5-HT4 receptor agonist activity.[3][4] The prokinetic itself may also contribute to the anti-emetic effect. Muscarinic receptors are those membrane bound acetylcholine receptors that are more sensitive to muscarine than to nicotine. ...


Clinical use

Antiemetic use

Metoclopramide is commonly used to treat nausea and vomiting (emesis) associated with conditions including: emetogenic drugs, uraemia, radiation sickness, malignancy, labour, and infection.[5][6] It is also used by itself or in combination with paracetamol (acetaminophen) for the relief of migraine. For the Beck song, see Nausea (song). ... Vomiting (also throwing up or emesis) is the forceful expulsion of the contents of ones stomach through the mouth and sometimes the nose. ... Vomiting (also throwing up or emesis) is the forceful expulsion of the contents of ones stomach through the mouth and sometimes the nose. ... Uremia is a toxic condition resulting from renal failure, when kidney function is compromised and urea, a waste product normally excreted in the urine, is retained in the blood. ... Radiation poisoning, also called radiation sickness, is a form of damage to organic tissue due to excessive exposure to ionizing radiation. ... When normal cells are damaged or old they undergo apoptosis; cancer cells, however, avoid apoptosis. ... Childbirth (also called labour, birth, partus or parturition) is the culmination of a human pregnancy with the emergence of a newborn infant/s from the mothers uterus. ... An infection is the detrimental colonization of a host organism by a foreign species. ...


It is considered ineffective in postoperative nausea and vomiting (PONV) at standard doses, and ineffective for motion sickness.[5][6] In nausea and vomiting associated with cancer chemotherapy, it has been superseded by the more effective 5-HT3 antagonists (e.g. ondansetron). Postoperative nausea and vomiting is an unpleasant complication affecting about a third of the 10% of the population undergoing general anaesthesia each year. ... It has been suggested that airsickness, seasickness be merged into this article or section. ... Chemotherapy is the use of chemical substances to treat disease. ... Skeletal formula of ondansetron, the prototypical 5-HT3 antagonist The 5-HT3 antagonists are a class of medications which act as receptor antagonists at the 5-hydroxytryptamine-3 receptor (5-HT3 receptor), a subtype of serotonin receptor found in terminals of the vagus nerve and certain areas of the brain. ... Ondansetron (INN) (IPA: ) is a serotonin 5-HT3 receptor antagonist used mainly to treat nausea and vomiting following chemotherapy. ...


Prokinetic use

Metoclopramide increases peristalsis of the jejunum and duodenum, increases tone and amplitude of gastric contractions, and relaxes the pyloric sphincter and duodenal bulb. These prokinetic effects make metoclopramide useful in the treamtent of gastric stasis (e.g. after gastric surgery or diabetic gastroparesis), as an aid in gastrointestinal radiology by increasing transit in barium studies, and as an aid in difficult small intestinal intubation. It is also used in gastroesophageal reflux disease (GERD/GORD). In much of the digestive tract, muscles contract in sequence to produce a peristaltic wave which forces food (called bolus while in the esophagus and chyme below the esophagus) along the alimentary canal. ... Diagram of the Human Intestine In anatomy of the digestive system, the jejunum is the central of the three divisions of the small intestine and lies between the duodenum and the ileum. ... In anatomy of the digestive system, the duodenum is a hollow jointed tube connecting the stomach to the jejunum. ... From Greek pylorus; pyl- = gate, -orus = guard. ... The Duodenal bulb is the portion of the duodenum which is closest to the stomach. ... Gastroparesis, also called delayed gastric emptying, is a disorder in which the stomach takes too long to empty its contents. ... Image A: A normal chest X-ray. ... Gastroesophageal Reflux Disease (GERD, or GORD when -oesophageal, the BE form, is substituted) is injury to the esophagus that develops from chronic exposure of the esophagus to acid coming up from the stomach (reflux). ...


Other indications

By inhibiting the action of prolactin inhibiting hormone (i.e. dopamine), metoclopramide has sometimes been used to stimulate lactation. Prolactin (PRL) is a peptide hormone primarily associated with lactation. ... Kittens nursing Lactation describes the secretion of milk from the mammary glands, the process of providing that milk to the young, and the period of time that a mother lactates to feed her young. ...


Contraindications/precautions

Metoclopramide is contraindicated in phaeochromocytoma. 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.[6] Also contraindicated with a suspected bowel obstruction. A pheochromocytoma (also phaeochromocytoma, English spelling) is a tumor in the medulla of the adrenal glands (or, rarely, the ganglia of the sympathetic nervous system) which secretes excessive amounts of catecholamines, usually epinephrine and norepinephrine. ... Clinical depression (also called major depressive disorder, or unipolar depression when compared to bipolar disorder) is a state of intense sadness, melancholia or despair that has advanced to the point of being disruptive to an individuals social functioning and/or activities of daily living. ...


Adverse effects

Plastic ampoule of metoclopramide
Plastic ampoule of metoclopramide

Common adverse drug reactions (ADRs) associated with metoclopramide therapy include: restlessness, drowsiness, dizziness, and/or headache. Infrequent ADRs include: extrapyramidal effects (EPSE) such as oculogyric crisis (and other acute dystonic reactions), hypertension, hypotension, hyperprolactinaemia leading to galactorrhoea, diarrhoea, constipation, and/or depression. Rare but serious ADRs associated with metoclopramide therapy include: agranulocytosis, supraventricular tachycardia, hyperaldosteronism, neuroleptic malignant syndrome and/or tardive dyskinesia.[6] plastic 10mg metoclopramide ampule This image has been released into the public domain by the copyright holder, its copyright has expired, or it is ineligible for copyright. ... plastic 10mg metoclopramide ampule This image has been released into the public domain by the copyright holder, its copyright has expired, or it is ineligible for copyright. ... An adverse drug reaction (abbreviated ADR) is a term to describe the unwanted, negative consequences sometimes associated with the use of medications. ... In human anatomy, the extrapyramidal system is a neural network located in the brain that is part of the motor system involved in the coordination of movement. ... Oculogyric crisis (OGC) is the name of a severe reaction to certain drugs and/or medical conditions including neuroleptics, amantadine, benzodiazepines, carbamazepine, chloroquine, cisplatin, diazoxide, influenza vaccine, levodopa, lithium, metoclopramide, nifedipine, pemoline, phencyclidine, reserpine, tricyclics, postencephalitic Parkinsons, Tourettes syndrome, multiple sclerosis, neurosyphilis, head trauma, bilateral thalamic infarction, lesions... This article or section does not cite any references or sources. ... In physiology and medicine, hypotension refers to an abnormally low blood pressure. ... Prolactin is a hormone secreted by lactotropes in the adenohypophysis (anterior pituitary gland) which is made up of 199 amino acids with a molecular weight of about 23,000 daltons. ... Galactorrhea or galactorrhoea is the spontaneous flow of milk from the breast, unassociated with childbirth or nursing. ... This article or section does not cite any references or sources. ... Neuroleptic malignant syndrome (NMS) is a life-threatening, neurological disorder most often caused by an adverse reaction to neuroleptic or antipsychotic drugs. ... Tardive dyskinesia is a serious neurological disorder caused by the long-term and/or high-dose use of dopamine antagonists, usually antipsychotics and among them especially the typical antipsychotics. ...


The risk of EPSEs are increased in young adults (<20 years) and children.[6] Such dystonic reactions are usually treated with benztropine or procyclidine. The risk of tardive dyskinesia and EPSE is increased with high dose therapy and with prolonged use. Tardive dyskinesias may be persistent and irreversible in some patients.[5] Benztropine (Cogentin®) is an anticholinergic drug principally used for the treatment of: Drug-induced parkinsonism, akathisia and acute dystonia; Parkinson disease; and Idiopathic or secondary dystonia. ... Procyclidine hydrochloride is an anticholinergic drug principally used for the treatment of: Drug-induced parkinsonism, akathisia and acute dystonia; Parkinson disease; and Idiopathic or secondary dystonia. ...


References

  1. ^ Justin-Besançon L, Laville C. Action antiémétique du métoclopramide vis-à-vis de l'apomorphine et de l'hydergine [Antiemetic action of metoclopramide with respect to apomorphine and hydergine]. C R Seances Soc Biol Fil 1964;158:723–7. PMID 14186927.
  2. ^ Rang HP, Dale MM, Ritter JM, Moore PK. Pharmacology. 5th ed. Edinburgh: Churchill Livingstone; 2003. ISBN 0-443-07145-4
  3. ^ Sweetman S, editor. Martindale: The complete drug reference. 34th ed. London: Pharmaceutical Press; 2004. ISBN 0-85369-550-4
  4. ^ Tonini M, Candura SM, Messori E, Rizzi CA. Therapeutic potential of drugs with mixed 5-HT4 agonist/5-HT3 antagonist action in the control of emesis. Pharmacol Res 1995;31(5):257-60. PMID 7479521
  5. ^ a b c Valeant Pharmaceuticals. Maxolon (Australian Approved Product Information). Auburn (NSW): Valeant Pharmaceuticals Australasia; 2000.
  6. ^ a b c d e Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006. ISBN 0-9757919-2-3

The Australian Medicines Handbook or AMH is a medical reference text commonly used in practice by health professionals (particularly general practitioners and pharmacists) in Australia. ...

Further reading

  • Brenner GM. Pharmacology. London: W B Saunders; 2000 ISBN 0-7216-7757-6
  • Canadian Pharmacists Association. Compendium of Pharmaceuticals and Specialties. 25th ed. Toronto: Webcom; 2000. ISBN 0-919115-76-4
  • Practical Gastroenterology May 2004 Recognition of Movement Disorders and Extrapyramidal side effects - would you recognize them if you see them?. Available on practicalgastro.com

  Results from FactBites:
 
metoclopramide (Reglan) - drug class, medical uses, medication side effects, and drug interactions by MedicineNet.com (583 words)
Metoclopramide decreases stomach acid reflux by strengthening the lower esophagus sphincter.
Metoclopramide interferes with dopamine receptors in the brain.
Metoclopramide is also used in the treatment of nausea related to postoperative state and cancer chemotherapy.
Metoclopramide - Wikipedia, the free encyclopedia (527 words)
Metoclopramide (INN) (IPA: [mɛtəˈkloprəmaɪd, -ˈklɒ-]) is a potent dopamine receptor antagonist used for its antiemetic and prokinetic properties.
Metoclopramide is commonly used to treat nausea and vomiting (emesis) associated with conditions including: emetogenic drugs, uraemia, radiation sickness, malignancy, labour, and infection (Valeant Pharmaceuticals, 2000; Rossi, 2006).
Metoclopramide increases peristalsis of the jejunum and duodenum, increases tone and amplitude of gastric contractions, and relaxes the pyloric sphincter and duodenal bulb.
  More results at FactBites »

 
 

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