Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | 2C16H14F3N3O2S.3H2O |
| Molecular Weight | 792.769 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O.O.O.CC1=C(C[S@@+]([O-])C2=NC3=C(N2)C=CC=C3)N=CC=C1OCC(F)(F)F.CC4=C(C[S@@+]([O-])C5=NC6=C(N5)C=CC=C6)N=CC=C4OCC(F)(F)F
InChI
InChIKey=XTQWZVSRVXCIGB-BBBDYAHLSA-N
InChI=1S/2C16H14F3N3O2S.3H2O/c2*1-10-13(20-7-6-14(10)24-9-16(17,18)19)8-25(23)15-21-11-4-2-3-5-12(11)22-15;;;/h2*2-7H,8-9H2,1H3,(H,21,22);3*1H2/t2*25-;;;/m11.../s1
| Molecular Formula | H2O |
| Molecular Weight | 18.0153 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C16H14F3N3O2S |
| Molecular Weight | 369.361 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionSources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208056lbl.pdfhttp://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21-428lbl.pdfCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/22950496
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208056lbl.pdfhttp://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21-428lbl.pdf
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/22950496
Lansoprazole is a proton pump inhibitor, which prevents the stomach from producing acid. Lansoprazole has been marketed for many years and is one of several proton-pump inhibitors (PPI's). It was used for the treatment of acid-reflux disorders (GERD), peptic ulcer disease, H. pylori eradication, and prevention of gastrointestinal bleeds with NSAID use. Lansoprazole belongs to a class of ant secretory compounds, the substituted benzimidazoles, that do not exhibit anticholinergic or histamine H2-receptor antagonist properties, but that suppress gastric acid secretion by specific inhibition of the (H+, K+ )-ATPase enzyme system at the secretory surface of the gastric parietal cell. Because this enzyme system is regarded as the acid (proton) pump within the parietal cell, lansoprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production. This effect is dose-related and leads to inhibition of both basal and stimulated gastric acid secretion irrespective of the stimulus. Lansoprazole is extensively metabolized in the liver. Two metabolites have been identified in measurable quantities in plasma (the hydroxylated sulfinyl and sulfone derivatives of lansoprazole). These metabolites have very little or no antisecretory activity. Lansoprazole is thought to be transformed into two active species which inhibit acid secretion by (H+, K+ )-ATPase within the parietal cell canaliculus, but are not present in the systemic circulation. The plasma elimination half-life of lansoprazole does not reflect its duration of suppression of gastric acid secretion. Thus, the plasma elimination half-life is less than two hours, while the acid inhibitory effect lasts more than 24 hours.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2095173 |
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Target ID: CHEMBL2095173 |
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Target ID: CHEMBL2095173 |
5.2 µM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | PREVACID Approved UseUse •treats frequent heartburn (occurs 2 or more days a week) •not intended for immediate relief of heartburn; this drug may take 1 to 4 days for full effect Launch Date1.0306656E12 |
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| Primary | PREVACID Approved UseUse •treats frequent heartburn (occurs 2 or more days a week) •not intended for immediate relief of heartburn; this drug may take 1 to 4 days for full effect Launch Date1.0306656E12 |
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| Primary | PREVACID Approved UseUse •treats frequent heartburn (occurs 2 or more days a week) •not intended for immediate relief of heartburn; this drug may take 1 to 4 days for full effect Launch Date1.0306656E12 |
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| Primary | DEXILANT Approved UseDEXILANT is a proton pump inhibitor (PPI) indicated for: •Healing of all grades of erosive esophagitis (EE). (1.1) •Maintaining healing of EE and relief of heartburn. (1.2) •Treating heartburn associated with symptomatic non-erosive gastroesophageal reflux disease (GERD). (1.3) 1.1 Healing of Erosive Esophagitis DEXILANT is indicated for healing of all grades of erosive esophagitis (EE) for up to eight weeks. 1.2 Maintenance of Healed Erosive Esophagitis DEXILANT is indicated to maintain healing of EE and relief of heartburn for up to six months. 1.3 Symptomatic Non-Erosive Gastroesophageal Reflux Disease DEXILANT is indicated for the treatment of heartburn associated with symptomatic non-erosive gastroesophageal reflux disease (GERD) for four weeks. Launch Date1.23327362E12 |
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| Curative | DEXILANT Approved UseDEXILANT is a proton pump inhibitor (PPI) indicated for: •Healing of all grades of erosive esophagitis (EE). (1.1) •Maintaining healing of EE and relief of heartburn. (1.2) •Treating heartburn associated with symptomatic non-erosive gastroesophageal reflux disease (GERD). (1.3) 1.1 Healing of Erosive Esophagitis DEXILANT is indicated for healing of all grades of erosive esophagitis (EE) for up to eight weeks. 1.2 Maintenance of Healed Erosive Esophagitis DEXILANT is indicated to maintain healing of EE and relief of heartburn for up to six months. 1.3 Symptomatic Non-Erosive Gastroesophageal Reflux Disease DEXILANT is indicated for the treatment of heartburn associated with symptomatic non-erosive gastroesophageal reflux disease (GERD) for four weeks. Launch Date1.23327362E12 |
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| Primary | PREVACID Approved UseINDICATIONS AND USAGE. Short-Term Treatment of Active Duodenal Ulcer PREVACID is indicated for short-term treatment (up to 4 weeks) for healing and symptom relief of active duodenal ulcer.
H. pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence.
Triple Therapy: PREVACID/amoxicillin/clarithromycin. PREVACID in combination with amoxicillin plus clarithromycin as triple therapy, is indicated for the treatment of patients with H. pylori infection and duodenal ulcer disease (active or one-year history of a duodenal ulcer) to eradicate H. pylori. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.
Dual Therapy: PREVACID/amoxicillin. PREVACID in combination with amoxicillin as dual therapy, is indicated for the treatment of patients with H. pylori infection and duodenal ulcer disease (active or one-year history of a duodenal ulcer) who are either allergic or intolerant to clarithromycin or in whom resistance to clarithromycin is known or suspected. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.
Maintenance of Healed Duodenal Ulcers PREVACID is indicated to maintain healing of duodenal ulcers. Controlled studies do not extend beyond 12 months.
Short-Term Treatment of Active Benign Gastric Ulcer PREVACID is indicated for short-term treatment (up to 8 weeks) for healing and symptom relief of active benign gastric ulcer
Healing of NSAID-Associated Gastric Ulcer PREVACID IS INDICATED FOR THE TREATMENT OF NSAID-ASSOCIATED GASTRIC ULCER IN PATIENTS WHO CONTINUE NSAID USE. CONTROLLED STUDIES DID NOT EXTEND BEYOND 8 WEEKS.
Risk Reduction of NSAID-Associated Gastric Ulcer PREVACID is indicated for reducing the risk of NSAID-associated gastric ulcers in patients with a history of a documented gastric ulcer who require the use of an NSAID. Controlled studies did not extend beyond 12 weeks.
Gastroesophageal Reflux Disease (GERD) Short-Term Treatment of Symptomatic GERD PREVACID is indicated for the treatment of heartburn and other symptoms associated with GERD. Short-Term Treatment of Erosive Esophagitis PREVACID is indicated for short-term treatment (up to 8 weeks) for healing and symptom relief of all grades of erosive esophagitis. For patients who do not heal with PREVACID for 8 weeks (5-10%), it may be helpful to give an additional 8 weeks of treatment. If there is a recurrence of erosive esophagitis an additional 8-week course of PREVACID may be considered.
Maintenance of Healing of Erosive Esophagitis PREVACID is indicated to maintain healing of erosive esophagitis. Controlled studies did not extend beyond 12 months.
Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome PREVACID is indicated for the long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome. Launch Date1.03057922E12 |
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| Primary | PREVACID Approved UseINDICATIONS AND USAGE. Short-Term Treatment of Active Duodenal Ulcer PREVACID is indicated for short-term treatment (up to 4 weeks) for healing and symptom relief of active duodenal ulcer.
H. pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence.
Triple Therapy: PREVACID/amoxicillin/clarithromycin. PREVACID in combination with amoxicillin plus clarithromycin as triple therapy, is indicated for the treatment of patients with H. pylori infection and duodenal ulcer disease (active or one-year history of a duodenal ulcer) to eradicate H. pylori. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.
Dual Therapy: PREVACID/amoxicillin. PREVACID in combination with amoxicillin as dual therapy, is indicated for the treatment of patients with H. pylori infection and duodenal ulcer disease (active or one-year history of a duodenal ulcer) who are either allergic or intolerant to clarithromycin or in whom resistance to clarithromycin is known or suspected. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.
Maintenance of Healed Duodenal Ulcers PREVACID is indicated to maintain healing of duodenal ulcers. Controlled studies do not extend beyond 12 months.
Short-Term Treatment of Active Benign Gastric Ulcer PREVACID is indicated for short-term treatment (up to 8 weeks) for healing and symptom relief of active benign gastric ulcer
Healing of NSAID-Associated Gastric Ulcer PREVACID IS INDICATED FOR THE TREATMENT OF NSAID-ASSOCIATED GASTRIC ULCER IN PATIENTS WHO CONTINUE NSAID USE. CONTROLLED STUDIES DID NOT EXTEND BEYOND 8 WEEKS.
Risk Reduction of NSAID-Associated Gastric Ulcer PREVACID is indicated for reducing the risk of NSAID-associated gastric ulcers in patients with a history of a documented gastric ulcer who require the use of an NSAID. Controlled studies did not extend beyond 12 weeks.
Gastroesophageal Reflux Disease (GERD) Short-Term Treatment of Symptomatic GERD PREVACID is indicated for the treatment of heartburn and other symptoms associated with GERD. Short-Term Treatment of Erosive Esophagitis PREVACID is indicated for short-term treatment (up to 8 weeks) for healing and symptom relief of all grades of erosive esophagitis. For patients who do not heal with PREVACID for 8 weeks (5-10%), it may be helpful to give an additional 8 weeks of treatment. If there is a recurrence of erosive esophagitis an additional 8-week course of PREVACID may be considered.
Maintenance of Healing of Erosive Esophagitis PREVACID is indicated to maintain healing of erosive esophagitis. Controlled studies did not extend beyond 12 months.
Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome PREVACID is indicated for the long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome. Launch Date1.03057922E12 |
|||
| Primary | PREVACID Approved UseINDICATIONS AND USAGE. Short-Term Treatment of Active Duodenal Ulcer PREVACID is indicated for short-term treatment (up to 4 weeks) for healing and symptom relief of active duodenal ulcer.
H. pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence.
Triple Therapy: PREVACID/amoxicillin/clarithromycin. PREVACID in combination with amoxicillin plus clarithromycin as triple therapy, is indicated for the treatment of patients with H. pylori infection and duodenal ulcer disease (active or one-year history of a duodenal ulcer) to eradicate H. pylori. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.
Dual Therapy: PREVACID/amoxicillin. PREVACID in combination with amoxicillin as dual therapy, is indicated for the treatment of patients with H. pylori infection and duodenal ulcer disease (active or one-year history of a duodenal ulcer) who are either allergic or intolerant to clarithromycin or in whom resistance to clarithromycin is known or suspected. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.
Maintenance of Healed Duodenal Ulcers PREVACID is indicated to maintain healing of duodenal ulcers. Controlled studies do not extend beyond 12 months.
Short-Term Treatment of Active Benign Gastric Ulcer PREVACID is indicated for short-term treatment (up to 8 weeks) for healing and symptom relief of active benign gastric ulcer
Healing of NSAID-Associated Gastric Ulcer PREVACID IS INDICATED FOR THE TREATMENT OF NSAID-ASSOCIATED GASTRIC ULCER IN PATIENTS WHO CONTINUE NSAID USE. CONTROLLED STUDIES DID NOT EXTEND BEYOND 8 WEEKS.
Risk Reduction of NSAID-Associated Gastric Ulcer PREVACID is indicated for reducing the risk of NSAID-associated gastric ulcers in patients with a history of a documented gastric ulcer who require the use of an NSAID. Controlled studies did not extend beyond 12 weeks.
Gastroesophageal Reflux Disease (GERD) Short-Term Treatment of Symptomatic GERD PREVACID is indicated for the treatment of heartburn and other symptoms associated with GERD. Short-Term Treatment of Erosive Esophagitis PREVACID is indicated for short-term treatment (up to 8 weeks) for healing and symptom relief of all grades of erosive esophagitis. For patients who do not heal with PREVACID for 8 weeks (5-10%), it may be helpful to give an additional 8 weeks of treatment. If there is a recurrence of erosive esophagitis an additional 8-week course of PREVACID may be considered.
Maintenance of Healing of Erosive Esophagitis PREVACID is indicated to maintain healing of erosive esophagitis. Controlled studies did not extend beyond 12 months.
Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome PREVACID is indicated for the long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome. Launch Date1.03057922E12 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1705 ng/mL |
30 mg single, intravenous dose: 30 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
LANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1136 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00847210 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Adolescents sex: food status: |
|
691 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00847210 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Adolescents sex: food status: |
|
16.1 (ng/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
33.5 (ng/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
37.3 (ng/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
15 mg 1 times / day multiple, oral dose: 15 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
1005 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
559 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
15 mg 1 times / day multiple, oral dose: 15 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
964 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
658 ng/mL |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
1397 ng/mL |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
3192 ng × h/mL |
30 mg single, intravenous dose: 30 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
LANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
143.2 (ng*h/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
15 mg 1 times / day multiple, oral dose: 15 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
55.5 (ng*h/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
87.6 (ng*h/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
2149 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
15 mg 1 times / day multiple, oral dose: 15 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
2628 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
3330 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
128 (ng*h/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
15 mg 1 times / day multiple, oral dose: 15 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
62 (ng*h/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
96 (ng*h/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
1914 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
15 mg 1 times / day multiple, oral dose: 15 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
2892 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
3747 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
3275 ng × h/mL |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
6529 ng × h/mL |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1.3 h |
30 mg single, intravenous dose: 30 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
LANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2.59 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00847210 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Adolescents sex: food status: |
|
1.66 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00847210 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Adolescents sex: food status: |
Doses
| Dose | Population | Adverse events |
|---|---|---|
30 mg 2 times / day multiple, intravenous Dose: 30 mg, 2 times / day Route: intravenous Route: multiple Dose: 30 mg, 2 times / day Sources: |
healthy, 18-29 years n = 18 Health Status: healthy Age Group: 18-29 years Sex: M+F Population Size: 18 Sources: |
|
90 mg single, intravenous Dose: 90 mg Route: intravenous Route: single Dose: 90 mg Sources: |
healthy, 18-29 years n = 8 Health Status: healthy Age Group: 18-29 years Sex: M+F Population Size: 8 Sources: |
|
300 mg single, oral Highest studied dose |
healthy, 35 years (range: 18 - 50 years) n = 36 Health Status: healthy Age Group: 35 years (range: 18 - 50 years) Sex: M+F Population Size: 36 Sources: |
|
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy, 48 years (range: 18-90 years) n = 2218 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 2218 Sources: |
Disc. AE: Diarrhea... AEs leading to discontinuation/dose reduction: Diarrhea (0.7%) Sources: |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: Page: p. 35 |
unhealthy, 48 years (range: 18-90 years) n = 2218 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 2218 Sources: Page: p. 35 |
Disc. AE: Abdominal pain... AEs leading to discontinuation/dose reduction: Abdominal pain (0.5%) Sources: Page: p. 35 |
30 mg 1 times / day steady, oral Dose: 30 mg, 1 times / day Route: oral Route: steady Dose: 30 mg, 1 times / day Sources: Page: p. 35 |
unhealthy, 48 years (range: 18-90 years) n = 455 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 455 Sources: Page: p. 35 |
Disc. AE: Diarrhea... AEs leading to discontinuation/dose reduction: Diarrhea (0.2%) Sources: Page: p. 35 |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: Page: p. 35 |
unhealthy, 48 years (range: 18-90 years) n = 1754 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 1754 Sources: Page: p. 35 |
Disc. AE: Diarrhea, Abdominal pain... AEs leading to discontinuation/dose reduction: Diarrhea (0.7%) Sources: Page: p. 35Abdominal pain (0.6%) |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2311 Health Status: unhealthy Age Group: adult Population Size: 2311 Sources: Page: p. 36 |
Disc. AE: Dyspepsia, Eructation... AEs leading to discontinuation/dose reduction: Dyspepsia (3 patients) Sources: Page: p. 36Eructation (2 patients) Nausea (6 patients) Vomiting (6 patients) Erosive esophagitis (1 patient) |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2142 Health Status: unhealthy Age Group: adult Population Size: 2142 Sources: Page: p. 36 |
Disc. AE: Dyspepsia, Eructation... AEs leading to discontinuation/dose reduction: Dyspepsia (1 patient) Sources: Page: p. 36Eructation (1 patient) Nausea (9 patients) Vomiting (6 patients) |
60 mg 2 times / day steady, oral Overdose Dose: 60 mg, 2 times / day Route: oral Route: steady Dose: 60 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Other AEs: Hypertension... Other AEs: Hypertension (serious) Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Diarrhea | 0.7% Disc. AE |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy, 48 years (range: 18-90 years) n = 2218 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 2218 Sources: |
| Abdominal pain | 0.5% Disc. AE |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: Page: p. 35 |
unhealthy, 48 years (range: 18-90 years) n = 2218 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 2218 Sources: Page: p. 35 |
| Diarrhea | 0.2% Disc. AE |
30 mg 1 times / day steady, oral Dose: 30 mg, 1 times / day Route: oral Route: steady Dose: 30 mg, 1 times / day Sources: Page: p. 35 |
unhealthy, 48 years (range: 18-90 years) n = 455 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 455 Sources: Page: p. 35 |
| Abdominal pain | 0.6% Disc. AE |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: Page: p. 35 |
unhealthy, 48 years (range: 18-90 years) n = 1754 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 1754 Sources: Page: p. 35 |
| Diarrhea | 0.7% Disc. AE |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: Page: p. 35 |
unhealthy, 48 years (range: 18-90 years) n = 1754 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 1754 Sources: Page: p. 35 |
| Erosive esophagitis | 1 patient Disc. AE |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2311 Health Status: unhealthy Age Group: adult Population Size: 2311 Sources: Page: p. 36 |
| Eructation | 2 patients Disc. AE |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2311 Health Status: unhealthy Age Group: adult Population Size: 2311 Sources: Page: p. 36 |
| Dyspepsia | 3 patients Disc. AE |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2311 Health Status: unhealthy Age Group: adult Population Size: 2311 Sources: Page: p. 36 |
| Nausea | 6 patients Disc. AE |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2311 Health Status: unhealthy Age Group: adult Population Size: 2311 Sources: Page: p. 36 |
| Vomiting | 6 patients Disc. AE |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2311 Health Status: unhealthy Age Group: adult Population Size: 2311 Sources: Page: p. 36 |
| Dyspepsia | 1 patient Disc. AE |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2142 Health Status: unhealthy Age Group: adult Population Size: 2142 Sources: Page: p. 36 |
| Eructation | 1 patient Disc. AE |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2142 Health Status: unhealthy Age Group: adult Population Size: 2142 Sources: Page: p. 36 |
| Vomiting | 6 patients Disc. AE |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2142 Health Status: unhealthy Age Group: adult Population Size: 2142 Sources: Page: p. 36 |
| Nausea | 9 patients Disc. AE |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2142 Health Status: unhealthy Age Group: adult Population Size: 2142 Sources: Page: p. 36 |
| Hypertension | serious | 60 mg 2 times / day steady, oral Overdose Dose: 60 mg, 2 times / day Route: oral Route: steady Dose: 60 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| unlikely | ||||
| unlikely | ||||
| unlikely | ||||
| unlikely | ||||
| unlikely | ||||
| unlikely | ||||
| unlikely | ||||
| unlikely | no (co-administration study) Comment: in vivo studies showed that DEXILANT did not have an impact on the pharmacokinetics of coadministered theophylline (CYP1A2 substrate) Page: 11.0 |
|||
| unlikely | no (co-administration study) Comment: in vivo studies showed that DEXILANT did not have an impact on the pharmacokinetics of coadministered phenytoin (CYP2C9 substrate) Page: 11.0 |
|||
| weak | unknown (co-administration study) Comment: The mean AUC of the active metabolite of clopidogrel was reduced by approximately 9% (mean AUC ratio was 91%, with 90% CI of 86- 97%) |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| yes | ||||
| yes | yes (pharmacogenomic study) Comment: mean dexlansoprazole Cmax and AUC values were up to 2 times higher in intermediate compared to extensive metabolizers; in poor metabolizers, mean Cmax was up to 4 times higher and mean AUC was up to 12 times higher compared to extensive metabolizers Page: 10,12 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| The treatment of gastroesophageal reflux disease with proton-pump inhibitors and its implications on managed care--pharmacoeconomics and its application to antisecretory drugs: a case study. | 2001 |
|
| Advantage of expressing the variations in some digestive parameters as a function of gastric emptying instead of time. | 2001 |
|
| [The effectiveness of 7-day combined Helicobacter eradication therapy in patients with peptic ulcer and chronic gastritis]. | 2001 |
|
| Lansoprazole treatment of patients with chronic idiopathic laryngitis: a placebo-controlled trial. | 2001 Apr |
|
| [H2 receptor antagonists and proton pump inhibitors: principles and rules of use]. | 2001 Apr 15 |
|
| Helicobacter pylori eradication treatment does not benefit patients with nonulcer dyspepsia. | 2001 Aug |
|
| High-dose proton-pump inhibitors as a diagnostic test of gastro-oesophageal reflux disease in endoscopic-negative patients. | 2001 Aug |
|
| Comparative pharmacokinetics and pharmacodynamics of lansoprazole oral capsules and suspension in healthy subjects. | 2001 Aug 15 |
|
| Do some patients with Helicobacter pylori infection benefit from an extension to 2 weeks of a proton pump inhibitor-based triple eradication therapy? | 2001 Feb |
|
| Early stage gastric MALT lymphoma with high-grade component cured by Helicobacter pylori eradication. | 2001 Feb |
|
| Allergic contact dermatitis due to lansoprazole, a proton pump inhibitor. | 2001 Jan |
|
| Long-term follow-up and serologic assessment after triple therapy with omeprazole or lansoprazole of Helicobacter-associated duodenal ulcer. | 2001 Jan |
|
| Factors affecting Helicobacter pylori eradication using a seven-day triple therapy with a proton pump inhibitor, tinidazole and clarithromycin, in Brazilian patients with peptic ulcer. | 2001 Jan-Feb |
|
| Healing and relapse rates in gastroesophageal reflux disease treated with the newer proton-pump inhibitors lansoprazole, rabeprazole, and pantoprazole compared with omeprazole, ranitidine, and placebo: evidence from randomized clinical trials. | 2001 Jul |
|
| Proton pump inhibitors versus H2-antagonists: a meta-analysis of their efficacy in treating bleeding peptic ulcer. | 2001 Jul |
|
| Factors associated with non-response in proton pump inhibitor users: a study of lansoprazole therapy. | 2001 Jun |
|
| Strategy for retreatment of therapeutic failure of eradication of Helicobacter pylori infection. | 2001 Jun |
|
| Discoloured tongue: a new cause? | 2001 Jun |
|
| Laryngopharyngeal reflux symptoms improve before changes in physical findings. | 2001 Jun |
|
| Pharmacological and pharmacodynamic essentials of H(2)-receptor antagonists and proton pump inhibitors for the practising physician. | 2001 Jun |
|
| Three-day lansoprazole quadruple therapy for Helicobacter pylori-positive duodenal ulcers: a randomized controlled study. | 2001 Jun |
|
| Pharmacodynamic effects and kinetic disposition of rabeprazole in relation to CYP2C19 genotypes. | 2001 Jun |
|
| Effect of Helicobacter pylori eradication on cyclooxygenase 2 (COX-2) and inducible nitric oxide synthase (iNOS) expression during gastric adaptation to aspirin (ASA) in humans. | 2001 Jun 1 |
|
| High-performance liquid chromatographic assay for the simultaneous determination of lansoprazole enantiomers and metabolites in human liver microsomes. | 2001 Jun 5 |
|
| Pantoprazole versus lansoprazole in French patients with reflux esophagitis. | 2001 Mar |
|
| Gastroprotective effect of aparisthman, a diterpene isolated from Aparisthmium cordatum, on experimental gastric ulcer models in rats and mice. | 2001 Mar |
|
| Acetaldehyde production and other ADH-related characteristics of aerobic bacteria isolated from hypochlorhydric human stomach. | 2001 Mar |
|
| Electrochemical studies and differential pulse polarographic analysis of lansoprazole in pharmaceuticals. | 2001 Mar |
|
| Pharmacodynamic modeling of lansoprazole using an indirect irreversible response model. | 2001 Mar |
|
| Haloperidol-stomach lesions attenuation by pentadecapeptide BPC 157, omeprazole, bromocriptine, but not atropine, lansoprazole, pantoprazole, ranitidine, cimetidine and misoprostol in mice. | 2001 Mar 9 |
|
| New-generation proton pump inhibitors: overcoming the limitations of early-generation agents. | 2001 May |
|
| Shortcomings of the first-generation proton pump inhibitors. | 2001 May |
|
| Lansoprazole triple therapy for Turkish children with Helicobacter pylori infections. | 2001 May |
|
| Proton pump inhibitors and their drug interactions: an evidence-based approach. | 2001 May |
|
| Lansoprazole-based triple therapy versus ranitidine bismuth citrate-based dual therapy in the eradication of Helicobacter pylori in patients with duodenal ulcer: a multicenter, randomized, double-dummy study. | 2001 May |
|
| Insulinoma with subsequent association of Zollinger-Ellison syndrome. | 2001 May |
|
| Impact of different therapeutic regimens on the outcome of patients with Crohn's disease of the upper gastrointestinal tract. | 2001 May |
|
| Control of intragastric pH with omeprazole 20 mg, omeprazole 40 mg and lansoprazole 30 mg. | 2001 May |
|
| Review article: long-term use of proton pump inhibitors in GORD--help or hindrance? | 2001 Sep |
|
| Lansoprazole in children: pharmacokinetics and efficacy in reflux oesophagitis. | 2001 Sep |
|
| Drug treatments in upper gastrointestinal bleeding: value of endoscopic findings as surrogate end points. | 2001 Sep |
|
| Does short-term treatment with proton pump inhibitors cause rebound aggravation of symptoms? | 2001 Sep |
|
| Gastroesophageal reflux disease presenting as xerophthalmia. | 2001 Sep-Oct |
|
| Pharmacokinetic differences between the enantiomers of lansoprazole and its metabolite, 5-hydroxylansoprazole, in relation to CYP2C19 genotypes. | 2004 Nov |
|
| Lansoprazole enantiomer activates human liver microsomal CYP2C9 catalytic activity in a stereospecific and substrate-specific manner. | 2005 Feb |
|
| Enantioselective disposition of lansoprazole and rabeprazole in human plasma. | 2006 Jun |
|
| Long-term management of gastroesophageal reflux disease with pantoprazole. | 2007 Jun |
|
| Estimation of the area under the concentration-time curve of racemic lansoprazole by using limited plasma concentration of lansoprazole enantiomers. | 2008 May |
|
| Delayed release dexlansoprazole in the treatment of GERD and erosive esophagitis. | 2009 |
Patents
Sample Use Guides
For erosive esophagitis: One 60 mg capsule once daily for up to 8 weeks
Relief of Heartburn: One 30 mg capsule once daily
Route of Administration:
Oral
A stably transfected gene reporter cell line AZ-AHR, derived from human hepatoma HepG2 cells transfected with a construct containing several AhR binding sites upstream of a luciferase reporter gene, was used for assessment of AhR transcriptional activity. Cells were incubated for 24 h with DEXLANSOPRAZOLE and/or vehicle (DMSO; 0.1% v/v), in the presence or absence of TCDD (10 nM; AZ-AHR cells) or DEX (100 nM; AZ-GR cells). After the treatments, cells were lysed and luciferase activity was measured. In parallel, cell viability was determined by conventional MTT test.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Thu Jul 06 00:04:51 UTC 2023
by
admin
on
Thu Jul 06 00:04:51 UTC 2023
|
| Record UNII |
HS2S9VK3NH
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| Record Status |
Validated (UNII)
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| Record Version |
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71587692
Created by
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PRIMARY | |||
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HS2S9VK3NH
Created by
admin on Thu Jul 06 00:04:51 UTC 2023 , Edited by admin on Thu Jul 06 00:04:51 UTC 2023
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DTXSID50185290
Created by
admin on Thu Jul 06 00:04:51 UTC 2023 , Edited by admin on Thu Jul 06 00:04:51 UTC 2023
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313640-86-7
Created by
admin on Thu Jul 06 00:04:51 UTC 2023 , Edited by admin on Thu Jul 06 00:04:51 UTC 2023
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ANHYDROUS->SOLVATE |
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ACTIVE MOIETY |