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Domperidone

Domperidone structure

CAS No:
57808-66-9
Formula:
C22H24ClN5O2
Chemical Name:
Domperidone
Synonyms:
2H-Benzimidazol-2-one,5-chloro-1-[1-[3-(2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)propyl]-4-piperidinyl]-1,3-dihydro-;5-Chloro-1-[1-[3-(2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)propyl]-4-piperidinyl]-1,3-dihydro-2H-benzimidazol-2-one;Domperidone;Motilium;KW 5338;R 33812;Nauzelin;Nauzelin Ds;Mod;Peridys;Gastronorm;Euciton;Peridon;Evoxin;NSC 299589;Motillium;Motinorm costi;Nomit;Domperi 10 DT;Domcolic
Categories:
Active Pharmaceutical Ingredients > Digestive System Drugs

Description

Domperidone is a dopamine blocker and an antidopaminergic reagent.Target: Dopamine ReceptorDomperidone is a useful alternative to metoclopramide for treatment of gastroparesis due to better tolerability. Effectiveness and side-effects from domperidone may be influenced by patient-related factors including polymorphisms in genes encoding drug-metabolizing enzymes, drug transporters, and domperidone targets [1]. Domperidone is a dopamine D(2) receptor antagonist, which has been used as ant

Solid

Domperidone is 1-[3-(Piperidin-1-yl)propyl]-1,3-dihydro-2H-benzimidazol-2-one in which the 4-position of the piperidine ring is substituted by a 5-chloro-1,3-dihydro-2H-benzimidazol-2-on-1-yl group. A dopamine antagonist, it is used as an antiemetic for the short-term treatment of nausea and vomiting, and to control gastrointestinal effects of dopaminergic drugs given in the management of parkinsonism. The free base is used in oral suspensions, while the maleate salt is used in tablet preparations. It has a role as an antiemetic and a dopaminergic antagonist. It is a member of benzimidazoles and a heteroarylpiperidine.|A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.|Domperidone is a peripheral-specific antagonist of the dopamine receptor D2 (D2R), with antiemetic, gastrokinetic and galactagogue activities. Following administration, domperidone binds to D2R expressed by peripheral neurons; this inhibits dopamine binding and D2R-mediated signaling. Inhibition of peripheral D2R signaling prevents or relieves various gastrointestinal (GI) symptoms, such as nausea and vomiting, and may help relief reflux and symptoms of a variety of other upper GI disorders.

Domperidone Basic Attributes

Molecular Weight：

425.91100

Exact Mass：

425.91

EC Number：

260-968-7

UNII：

5587267Z69

NSC Number：

759575|299589

DSSTox ID：

DTXSID1045116

NCI Thesaurus Code：

C454

ATC Code：

A03FA03|A - Alimentary tract and metabolism

HScode：

2933990090

Characteristics

PSA：

78.82000

XLogP3：

3.29110

Appearance：

Solid

Density：

1.341 g/cm3

Melting Point：

242.5 °C

Boiling Point：

723.6±70.0 °C at 760 mmHg

Flash Point：

391.4±35.7 °C

Refractive Index：

1.729

Water Solubility：

Slightly soluble in water.

Storage Conditions：

Keep tightly closed.

PKA：

7.9None

Dissociation Constants：

7.9

Collision Cross Section：

201.8 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

hazard class code：

R62; R63

safety instructions：

S26-S36

RTECS Number：

DE2275900

Marks：

Stability/Shelf Life：

Stable. Incompatible with strong oxidizing agents.

Precautionary statement(s)：

P280

Hazard Statements：

H361

GHS Classification：

|Warning|H361 (91.59%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]|P201, P202, P281, P308+P313, P405, and P501|Aggregated GHS information provided by 108 companies from 6 notifications to the ECHA C&L Inventory.

Toxicity

Toxicity Summary：

Side effects include galactorrhea, gynecomastia, or menstrual irregularities.

Protein Binding：

91%-93%

Drug Information

Drug Indication：

For management of dyspepsia, heartburn, epigastric pain, nausea, and vomiting.

Pharmacology：

Domperidone is a specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.

MeSH：

Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME. (See all compounds classified as Dopamine Antagonists.)|Drugs used to prevent NAUSEA or VOMITING. (See all compounds classified as Antiemetics.)

Metabolism/Metabolites：

Domperidone has known human metabolites that include 1-Propyl-1,3-dihydro-2H-benzimidazol-2-one, 3-[3-[4-(5-Chloro-2-oxo-3H-benzimidazol-1-yl)piperidin-1-yl]propyl]-6-hydroxy-1H-benzimidazol-2-one, and 5-Chloro-1-(piperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one.

Biological Half-Life：

7 hours

Mechanism of Action：

Domperidone acts as a gastrointestinal emptying (delayed) adjunct and peristaltic stimulant. The gastroprokinetic properties of domperidone are related to its peripheral dopamine receptor blocking properties. Domperidone facilitates gastric emptying and decreases small bowel transit time by increasing esophageal and gastric peristalsis and by lowering esophageal sphincter pressure. Antiemetic: The antiemetic properties of domperidone are related to its dopamine receptor blocking activity at both the chemoreceptor trigger zone and at the gastric level. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which - among others - regulates nausea and vomiting

MeSH Entry Terms：

Apo Domperidone

Domperidone Use and Manufacturing

Uses

Peripheral dopamine receptor antagonist that does not cross the blood-brain barrier; anti-emetic.

Use Classification：

Animal Drugs -> FDA Approved Animal Drug Products (Green Book) -> Active Ingredients

Computed Properties

Molecular Weight:425.9
XLogP3:3.9
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:5
Exact Mass:425.1618527
Monoisotopic Mass:425.1618527
Topological Polar Surface Area:67.9
Heavy Atom Count:30
Complexity:655
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Material

Methyl isobutyl ketone

Benzimidazole

Dimethylformamide

Potassium iodide

Drug Function and Efficacy

This product is a peripheral dopamine receptor blocker that acts directly on the gastrointestinal wall, can increase the tension of the lower esophageal sphincter, prevent gastroesophageal reflux, enhance gastric motility, promote gastric emptying, coordinate gastric and duodenal motility, inhibit nausea and vomiting, and effectively prevent bile reflux without affecting gastric juice secretion. This product is not easy to pass through the blood-cerebrospinal fluid barrier and has an inhibitory effect on dopamine receptors in the brain. Therefore, there are no extrapyramidal and other neurological and psychiatric adverse reactions.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Vitamin C effervescent tablets
Ingredients	Each tablet of this product contains 10 mg of domperidone. Excipients are: starch, microcrystalline cellulose, lactose, and magnesium stearate.
Indication	1. Anticholinergic drugs such as acetaminophen, propantheline bromide, scopolamine, belladonna tablets, etc. will weaken the effect of this product and should not be taken together; 2. When this product is used together with acetaminophen, ampicillin, levodopa, tetracycline, etc., the absorption rate of these drugs will increase; 3. When this product is used together with digoxin, the absorption of the latter will be reduced; 4. If you are taking other medicines, please consult a doctor or pharmacist before using this product.
Specifications	0.5 g
Manufacturer	Qingdao Guoxin Pharmaceutical Co., Ltd.

Domperidone Capsules
Ingredients	Domperidone.
Indication	1. Anticholinergic drugs, such as Tongjingping, propantheline bromide, scopolamine, belladonna tablets, etc., will weaken the effect of this product and should not be taken at the same time. 2. When this product is used together with acetaminophen, ampicillin, levodopa, tetracycline, etc., the absorption rate of these drugs will increase. 3. Antacids and anti-secretory drugs will reduce the oral bioavailability of domperidone and should not be taken with this product at the same time. 4. Domperidone is mainly metabolized by the liver microsomal CYP3A4 enzyme. In vitro tests have shown that co-use with CYP3A4 enzyme inhibitors (such as imidazole antifungal drugs, macrolide antibiotics, HIV protease inhibitors, nefazodone) will lead to an increase in the blood concentration of domperidone. 5. Because domperidone has the effect of promoting gastric motility, it will theoretically affect the oral drugs used in combination.
Specifications	10mg
Manufacturer	Beijing Saier Biological Pharmaceutical Co., Ltd.

Domperidone Tablets
Ingredients	Each tablet of this product contains the main ingredient domperidone 10 mg, and the auxiliary ingredients are: starch, hydrogenated cottonseed oil, lactose, magnesium stearate, microcrystalline cellulose, povidone K90, pregelatinized starch, and sodium lauryl sulfate.
Indication	1. It should not be used together with azole antifungal drugs such as ketoconazole and itraconazole, macrolide antibiotics such as erythromycin, HIV protease inhibitors and nefazodone. 2. Anticholinergic drugs such as tamoxifen, propantheline bromide, anisodamine, belladonna tablets, etc. will weaken the effect of this product and should not be taken with this product. 3. Antacids and drugs that inhibit gastric acid secretion can reduce the bioavailability of this product and should not be taken with this product. 4. If used with other drugs at the same time, drug interactions may occur. Please consult a doctor or pharmacist for details.
Specifications	10mg
Manufacturer	Dandong Hongye Pharmaceutical Co., Ltd.

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Registered Holders

Shandong Gowmo Pharma Ltd

China
Active
Tianjin J&K Limited

China
Active
Zhao QING City Dingkang Pharmaceutical Co., Ltd.

China
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