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Encyclopedia > Domperidone
Domperidone
Systematic (IUPAC) name
1,3-dihydro-5-chloro-1-(1-(3-(2,3-dihydro-
2-oxo-1H-benzimidazol-1-yl)propyl)-
4-piperidinyl)-2H-benzimidazol-2-one
Identifiers
CAS number 57808-66-9
ATC code A03FA03
PubChem 3151
DrugBank APRD00418
Chemical data
Formula C22H24ClN5O2 
Mol. mass 425.911 g/mol
Pharmacokinetic data
Bioavailability High
Protein binding 91–93%
Metabolism Hepatic and intestinal (first-pass)
Half life 7 hours
Excretion Breast milk, renal
Therapeutic considerations
Pregnancy cat.

Not classified (US) Image File history File links Size of this preview: 800 × 306 pixelsFull resolution (957 × 366 pixel, file size: 11 KB, MIME type: image/png) File historyClick on a date/time to view the file as it appeared at that time. ... Image File history File links Size of this preview: 800 × 567 pixelsFull resolution (1276 × 904 pixel, file size: 686 KB, MIME type: image/png) 3D structure of Domperidone Benchware 3D Explorer Tripos I, the copyright holder of this work, hereby release it into the public domain. ... 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. ... A drugs efficacy may be affected by the degree to which it binds to the proteins within blood plasma. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... The liver is an organ present in vertebrates and some other animals. ... In anatomy, the intestine is the segment of the alimentary canal extending from the stomach to the anus and, in humans and other mammals, consists of two segments, the small intestine and the large intestine (or colon). ... The first pass effect (or first pass metabolism) is a phenomenon of drug metabolism. ... 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. ... 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. ...

Legal status

Not approved for use or sale: US; prescription medicine: Australia, Canada; Over the Counter (OTC): UK, Belgium, Ireland, Italy, Japan, Netherlands, South Africa, Switzerland, China, Russia, Slovakia, Malta, South Korea, and Romania[1] The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ...

Routes Oral, intravenous, rectal

Domperidone (trade name Motilium or Motillium) is an antidopaminergic drug, developed by Janssen Pharmaceutica, and used orally, rectally or intravenously, generally to suppress nausea and vomiting. It has also been used to stimulate lactation. 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. ... Intravenous therapy or IV therapy is the giving of liquid substances directly into a vein. ... This page is a candidate to be moved to Wiktionary. ... This article does not cite any references or sources. ... Johnson & Johnson NYSE: JNJ is an international pharmaceutical, medical devices and consumer packaged goods manufacturer founded in 1885. ... The posterior aspect of the rectum exposed by removing the lower part of the sacrum and the coccyx. ... An intravenous drip in a hospital Intravenous therapy or IV therapy is the administration of liquid substances directly into a vein. ... For other uses, see Nausea (disambiguation). ... Vomiting (also throwing up or emesis) is the forceful expulsion of the contents of ones stomach through the mouth and sometimes the nose. ... 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. ...

Contents

Uses

Gastrointestinal problems

Domperidone is used, together with metoclopramide, cyclizine, and 5HT3 receptor antagonists (such as granisetron) in the treatment of nausea and vomiting. It is useful in patients with Parkinson's disease because, unlike metoclopramide, domperidone does not cross the blood-brain barrier. Metoclopramide (INN) (IPA: ) is a potent dopamine receptor antagonist used for its antiemetic and prokinetic properties. ... Cyclizine is an antihistamine drug used to treat nausea, vomiting and dizziness associated with motion sickness, vertigo and post-operative following administration of general anaesthesia and opioids. ... 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. ... Granisetron is used to prevent nausea and vomiting caused by cancer chemotherapy and radiation therapy. ... Metoclopramide (INN) (IPA: ) is a potent dopamine receptor antagonist used for its antiemetic and prokinetic properties. ... The blood-brain barrier (BBB) is a membranic structure that acts primarily to protect the brain from chemicals in the blood, while still allowing essential metabolic function. ...


Domperidone has also been found effective in the treatment of gastroparesis,[2] a stomach motility condition, and for paediatric Gastroesophageal reflux (infant vomiting). Gastroparesis, also called delayed gastric emptying, is a disorder in which the stomach takes too long to empty its contents. ... Pediatrics (also spelled paediatrics or pædiatrics) is the branch of medicine that deals with the medical care of infants and children. ... 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). ...


Lactation

The hormone prolactin stimulates lactation in humans, and its release is inhibited by the dopamine secreted by the hypothalamus. Domperidone, by acting as an anti-dopaminergic, results in increased prolactin secretion, and thus promotes lactation. Prolactin (PRL) is a peptide hormone primarily associated with lactation. ... Dopamine is a phenethylamine naturally produced by the human body. ... The hypothalamus links the nervous system to the endocrine system via the pituitary gland (hypophysis). ... Prolactin (PRL) is a peptide hormone primarily associated with lactation. ...


Although it has never been officially approved for use in the United States, domperidone is widely purchased from pharmacies in other countries for this purpose. Since, according to the FDA, domperidone is not approved for enhanced lactation in any country,[3] it is still prescribed "off-label" for this use in countries besides the United States.[4] For other uses, see Pharmacy (disambiguation). ... Off-label use is the practice of prescribing drugs for a purpose outside the scope of the drugs approved label, most often concerning the drugs indication. ...


Controversy

Janssen Pharmaceutical has brought Domperidone before the FDA several times in the last two decades, with the most recent effort in the 1990s. Numerous U.S. clinical drug trials have demonstrated its safety and efficacy in dealing with gastroparesis symptoms, but the FDA turned down Janssen's application for Domperidone, even though the FDA's division of gastrointestinal drugs had approved Domperidone.[5]


In June 2004, the United States' main regulation agency, the Food and Drug Administration (FDA), issued a letter warning women not to take domperidone, citing unknown risks to parents and infants, and warned pharmacies that domestic sale was illegal, and that import shipments from other countries would be searched and seized. Domperidone is excreted in breast milk, and no studies on its effects on breastfeeding infants have been reported in the literature. Individual incidents of problems with the drug include cardiac arrest and arrhythmia, complications with other medications, as well as complications with improper intravenous use[4] hi “FDA” redirects here. ... A cardiac arrhythmia, also called cardiac dysrhythmia, is a disturbance in the regular rhythm of the heartbeat. ...


It has been widely speculated that this action by the FDA is related to increasing drug importation from countries such as Canada.[citation needed]


Yet prominent doctors and pharmacists have rejected the FDA's reasoning and still promote domperidone's use in increasing milk supply. Such doctors and pharmacists are confident the drug is safe in the doses given for this purpose.[6] The American Academy of Pediatrics considers domperidone "usually compatible with breastfeeding".[7]


There is a new controversy in Britain regarding lethal levels of sodium found in children who are administered this drug. It is now subject to a medical review following a number of criminal trials.[8]


Brand

Domperidone is marketed in India by Ion healthcare under the brand name MELDOM-DT.


Also conjuction with Pantoprazole as Dompan Tablets mktg by MEDLEY Pharma. Ltd.


References

  1. ^ Domperidone MedSafe NZ Government
  2. ^ Silvers D, Kipnes M, Broadstone V, et al (1998). "Domperidone in the management of symptoms of diabetic gastroparesis: efficacy, tolerability, and quality-of-life outcomes in a multicenter controlled trial. DOM-USA-5 Study Group". Clinical therapeutics 20 (3): 438-53. PMID 9663360. 
  3. ^ Domperidone for lactating women, Canadian Medical Association Journal, Orlando P. da Silva and David C. Knoppert. 2004 Sep 28;171(7):725-6.
  4. ^ a b FDA Warns Against Women Using Unapproved Drug, Domperidone, to Increase Milk Production FDA
  5. ^ Letter to Consumer Safety Office, FDA Gastroparesis and Dysmotilities Association
  6. ^ Official Statements From Prominent Physicians breastfeedingonline.com
  7. ^ Maternal Medication Usually Compatible With Breastfeeding American Academy of Pediatrics
  8. ^ Current news coverage of latest trial The Scotsman

hi “FDA” redirects here. ...

External links

  • Domperidone Issue Brief International Academy of Compounding Pharmacists.
  • GPDA letter to the FDA about Domperidone for gastroparesis

  Results from FactBites:
 
Breastfeeding: Domperidone to increase milk production (1132 words)
Domperidone (Motilium) is a drug that has, as a side effect, the increased production of the hormone prolactin.
Domperidone is generally used for disorders of the gastrointestinal tract (gut) and has not been released for use as a stimulant for milk production.
Domperidone has many fewer side effects because it does not enter the brain tissue in significant amounts (does not pass the blood-brain barrier).
FDA Warns Against Women Using Unapproved Drug, Domperidone, to Increase Milk Production (461 words)
Domperidone may increase the secretion of prolactin, a hormone that is needed for lactation.
Although domperidone is approved in several countries outside the U.S. to treat certain gastric disorders, it is not approved in any country, including the U.S., for enhancing breast milk production in lactating women and is also not approved in the U.S. for any indication.
In several countries where the oral form of domperidone continues to be marketed, labels for the product contain specific warnings against use of domperidone by breastfeeding women and note that the drug is excreted in breast milk that could expose a breastfeeding infant to unknown risks.
  More results at FactBites »


 

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