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Esomeprazole magnesium

Esomeprazole magnesium structure

CAS No:
161973-10-0
Formula:
C34H36MgN6O6S2
Chemical Name:
Esomeprazole magnesium
Synonyms:
Magnesium,bis[6-methoxy-2-[(S)-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl-κO]-1H-benzimidazolato-κN3]-,(T-4)-;Magnesium,bis[5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazolato]-,[T-4-(S),(S)]-;(T-4)-Bis[6-methoxy-2-[(S)-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl-κO]-1H-benzimidazolato-κN3]magnesium;Esomeprazole magnesium;H 199/18;Nexium;(-)-Omeprazole magnesium;(S)-Omeprazole magnesium;Perprazole;Raciper;302841-07-2;320416-93-1;371759-50-1;372519-57-8;376628-34-1;502497-87-2;870780-01-1;202742-32-3;922731-05-3
Categories:
Active Pharmaceutical Ingredients > Digestive System Drugs

Description

ChEBI: A magnesium salt resulting from the formal reaction of magnesium hydroxide with 2 mol eq. of esomeprazole. An inhibitor of gastric acid secretion, it is used for the treatment of gastro-oesophageal reflux disease, dyspepsia, peptic ulcer disease, and Zolli ger-Ellison syndrome.Esomeprazole magnesium,S-bis(5-rnethoxy-2-[(S)-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole-l-yl) magnesiumtrihydrate (Nexium), is the S-enantiomer ofomeprazole. The benzimidazole PPIs co

Magnesium 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methylsulfinyl]benzimidazol-1-ide is a member of benzimidazoles and a sulfoxide.|The S-isomer of omeprazole.

Esomeprazole magnesium Basic Attributes

Molecular Weight：

713.12

Exact Mass：

712.198792

EC Number：

2017-001-1

DSSTox ID：

DTXSID5044231

Characteristics

PSA：

163

Boiling Point：

600°C at 760 mmHg

Flash Point：

316.7ºC

Specific rotation：

D20 -128.2° (c = 1 in methanol)

Safety Information

Precautionary statement(s)：

P261, P264, P270, P272, P273, P280, P301+P312, P302+P352, P321, P330, P333+P313, P363, P501

Hazard Statements：

H302

GHS Classification：

|Warning|H302 (33.33%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P272, P273, P280, P301+P312, P302+P352, P304+P340, P305+P351+P338, P312, P321, P330, P332+P313, P333+P313, P337+P313, P362, P363, P403+P233, P405, and P501|Aggregated GHS information provided by 6 companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.|H302 (53.03%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P272, P273, P280, P301+P312, P302+P352, P321, P330, P333+P313, P363, and P501|Aggregated GHS information provided by 66 companies from 5 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.|H302 (98.85%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P272, P273, P280, P301+P312, P302+P352, P305+P351+P338, P321, P330, P333+P313, P337+P313, P363, P391, and P501|Aggregated GHS information provided by 87 companies from 5 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

Duodenal ulcer, Gastric ulcer, Gastro-oesophageal reflux disease, Peptic ulcer, site unspecified, Zollinger-Ellison syndrome|Ankylosing spondylitis, Primary generalised osteoarthritis, Rheumatoid arthritis|Duodenal ulcer, Gastric ulcer

MeSH：

Various agents with different action mechanisms used to treat or ameliorate PEPTIC ULCER or irritation of the gastrointestinal tract. This has included ANTIBIOTICS to treat HELICOBACTER INFECTIONS; HISTAMINE H2 ANTAGONISTS to reduce GASTRIC ACID secretion; and ANTACIDS for symptomatic relief. (See all compounds classified as Anti-Ulcer Agents.)|Compounds that inhibit H(+)-K(+)-EXCHANGING ATPASE. They are used as ANTI-ULCER AGENTS and sometimes in place of HISTAMINE H2 ANTAGONISTS for GASTROESOPHAGEAL REFLUX. (See all compounds classified as Proton Pump Inhibitors.)

MeSH Entry Terms：

Esomeprazole

Esomeprazole magnesium Use and Manufacturing

Uses

Antiulcerative

Use Classification：

Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:713.1
Hydrogen Bond Acceptor Count:14
Rotatable Bond Count:10
Exact Mass:712.1988169
Monoisotopic Mass:712.1988169
Topological Polar Surface Area:163
Heavy Atom Count:49
Complexity:453
Undefined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:3
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Esomeprazole is the S-isomer of omeprazole. It reduces gastric acid secretion through a specific targeted mechanism of action and is a specific inhibitor of the proton pump in parietal cells. As a weak base, it is concentrated and converted into an active form in the high acid environment of the acid-secreting microtubules of the parietal cells, thereby inhibiting the H/K-ATPase (proton pump) at this site, inhibiting both basal and stimulated gastric acid secretion. It takes effect within one hour after oral administration, significantly reducing the peak acid secretion caused by pentagastrin stimulation and maintaining an elevated intragastric pH. In addition, the use of antacids may lead to an increase in serum gastrin during treatment, and long-term use may cause an increase in the number of ECL cells and an increased incidence of gastric glandular cysts, but these reactions are benign and reversible.

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

Esomeprazole magnesium enteric-coated tablets
Ingredients	The active ingredient of this product is esomeprazole magnesium.
Indication	1. Effect of esomeprazole on the pharmacokinetics of other drugs For drugs whose absorption process is affected by gastric acid, the absorption of these drugs may be increased or decreased during esomeprazole treatment due to the decrease in gastric acid. As with other acid secretion inhibitors or antacids, the absorption of ketoconazole and itraconazole will decrease during esomeprazole treatment. Esomeprazole inhibits CYP2C19, which is the main metabolizing enzyme of esomeprazole. Therefore, when esomeprazole is co-administered with drugs metabolized by CYP2C19 (such as diazepam, citalopram, imipramine, clomipramine, phenytoin, etc.), the plasma concentration of these drugs may be increased and the dose may need to be reduced. This should be considered especially when esomeprazole is used for on-demand treatment. The co-administration of 30 mg of esomeprazole can reduce the clearance of diazepam metabolized by CYP2C19 by 45%. The co-administration of 40 mg of esomeprazole can increase the trough concentration of plasma phenytoin in patients with epilepsy by 13%. Therefore, during phenytoin treatment, when esomeprazole is used in combination or discontinued, it is recommended to monitor the blood concentration of phenytoin. Clinical trials have shown that patients receiving warfarin treatment, combined with esomeprazole 40mg, coagulation time is within an acceptable range. However, after marketing, it has been reported that when the two are used together, individual cases have a clinically significant increase in the international normalized ratio (INR). Therefore, when starting to use or discontinue esomeprazole, it is recommended to monitor the blood concentration of warfarin. In healthy volunteers, the co-administration of esomeprazole 40mg can increase the area under the blood concentration-time curve (AUC) of cisapride by 32% and extend the elimination half-life (t1/2) by 31%, but does not significantly increase the plasma concentration of cisapride. The co-administration of esomeprazole does not aggravate the slight prolongation of the QTc interval caused by cisapride alone. (See [Precautions]). Studies have shown that esomeprazole has no clinically relevant effect on the pharmacokinetics of amoxicillin or quinidine. 2. Effects of other drugs on the pharmacokinetics of esomeprazole Esomeprazole is metabolized by CYP2C19 and CYP3A4. The combined use of esomeprazole and CYP3A4 inhibitor clarithromycin (500 mg twice daily) can double the area under the blood concentration-time curve (AUC) of esomeprazole, but the dose of esomeprazole does not need to be adjusted. 3. Incompatibility None
Specifications	40mg (calculated as C17H19N3O3S)
Manufacturer	AstraZeneca Pharmaceutical Co., Ltd.

Esomeprazole magnesium enteric-coated tablets
Ingredients	The active ingredient of this product is esomeprazole magnesium
Indication	The absorption of ketoconazole and itraconazole will be reduced during esomeprazole treatment. When used in combination with diazepam, citalopram, imipramine, clomipramine, phenytoin, etc., these drugs may need to be reduced in dose. Therefore, during phenytoin treatment, when esomeprazole is used in combination or discontinued, it is recommended to monitor the blood concentration of phenytoin. There is no incompatibility.
Specifications	20mg

Esomeprazole magnesium enteric-coated tablets
Ingredients	The active ingredient of this product is esomeprazole magnesium
Indication	The absorption of ketoconazole and itraconazole will be reduced during esomeprazole treatment. When used in combination with diazepam, citalopram, imipramine, clomipramine, phenytoin, etc., these drugs may need to be reduced in dose. Therefore, during phenytoin treatment, when esomeprazole is used in combination or discontinued, it is recommended to monitor the blood concentration of phenytoin. There is no incompatibility.
Specifications	20mg (calculated as C17H19N3O3S)
Manufacturer	AstraZeneca Pharmaceutical Co., Ltd.

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Registered Holders

HEC PHARM CO LTD

United States
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MATRIX PHARMACORP PRIVATE LTD

United States
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JUBILANT PHARMOVA LTD

United States
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