Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C16H14F3N3O2S |
| Molecular Weight | 369.361 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(OCC(F)(F)F)C=CN=C1C[S+]([O-])C2=NC3=C(N2)C=CC=C3
InChI
InChIKey=MJIHNNLFOKEZEW-UHFFFAOYSA-N
InChI=1S/C16H14F3N3O2S/c1-10-13(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/h2-7H,8-9H2,1H3,(H,21,22)
| 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: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21-428lbl.pdfhttps://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208056lbl.pdfCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/24773330 | https://www.ncbi.nlm.nih.gov/pubmed/25881966 | http://www.sciencedirect.com/science/article/pii/000629529190584R?via%3Dihub
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21-428lbl.pdfhttps://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208056lbl.pdf
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/24773330 | https://www.ncbi.nlm.nih.gov/pubmed/25881966 | http://www.sciencedirect.com/science/article/pii/000629529190584R?via%3Dihub
Dexlansoprazole (trade names Kapidex, Dexilant) is a proton pump inhibitor (PPI) that is marketed by Takeda Pharmaceuticals for the treatment of erosive esophagitis and gastro-oesophageal reflux disease. Dexlansoprazole is used to heal and maintain healing of erosive esophagitis and to treat heartburn associated with gastroesophageal reflux disease (GERD). It lasts longer than lansoprazole, to which it is chemically related, and needs to be taken less often. Dexlansoprazole is supplied for oral administration as a dual delayed-release formulation in capsules and orally disintegrating tablets. The capsules and tablets contain dexlansoprazole in a mixture of two types of enteric-coated granules with different pH-dependent dissolution profiles. The most significant adverse reactions (≥2%) reported in clinical trials were diarrhea, abdominal pain, nausea, upper respiratory tract infection, vomiting, and flatulence.
CNS Activity
Originator
Sources: http://www.takeda.com/company/history/1985.htmlhttp://www.sciencedirect.com/science/article/pii/000629529190584R?via%3Dihub
Curator's Comment: # Takeda
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2095173 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11693467 |
|||
Target ID: CHEMBL2095173 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20974316 |
|||
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 Date2002 |
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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 Date2002 |
|||
| 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 Date2002 |
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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 Date2009 |
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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 Date2009 |
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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 Date2002 |
|||
| 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 Date2002 |
|||
| 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 Date2002 |
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 |
|
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: |
|
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: |
|
37.3 ng/mL/(mg dose) 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: UNKNOWN food status: UNKNOWN |
|
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: UNKNOWN food status: UNKNOWN |
|
33.5 ng/mL/(mg dose) 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: |
|
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: |
|
16.1 ng/mL/(mg dose) 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: |
|
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 |
|
0.36 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8710755/ |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
LEVOLANSOPRAZOLE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
337 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/ |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
528 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/ |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1156 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/ |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
167 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/ |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
848.13 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31338800/ |
30 mg 2 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
811.63 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31338800/ |
30 mg 2 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
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 |
|
128 μg × h/L/(mg dose) 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: UNKNOWN food status: UNKNOWN |
|
143.2 μg × h/L/(mg dose) 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: UNKNOWN food status: UNKNOWN |
|
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: |
|
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: |
|
96 μg × h/L/(mg dose) 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: |
|
87.6 μg × h/L/(mg dose) 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: |
|
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: |
|
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: |
|
62 μg × h/L/(mg dose) 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: |
|
55.5 μg × h/L/(mg dose) 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: |
|
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: |
|
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: |
|
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 |
|
1.56 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8710755/ |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
LEVOLANSOPRAZOLE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
524 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/ |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
967 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/ |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
3892 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/ |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
451 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/ |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1161.07 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31338800/ |
30 mg 2 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1180.29 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31338800/ |
30 mg 2 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
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 |
|
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: |
|
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: |
|
0.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/ |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
0.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/ |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/ |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/ |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1.02 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31338800/ |
30 mg 2 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
0.87 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31338800/ |
30 mg 2 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
LEVOLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
5.8% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8710755/ |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
LEVOLANSOPRAZOLE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
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 Health Status: healthy Age Group: 18-29 years Sex: M+F Sources: |
|
90 mg single, intravenous Dose: 90 mg Route: intravenous Route: single Dose: 90 mg Sources: |
healthy, 18-29 years Health Status: healthy Age Group: 18-29 years Sex: M+F Sources: |
|
300 mg single, oral Highest studied dose |
healthy, 35 years (range: 18 - 50 years) Health Status: healthy Age Group: 35 years (range: 18 - 50 years) Sex: M+F 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) Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F 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: |
unhealthy, 48 years (range: 18-90 years) Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Sources: |
Disc. AE: Abdominal pain... AEs leading to discontinuation/dose reduction: Abdominal pain (0.5%) Sources: |
30 mg 1 times / day steady, oral Dose: 30 mg, 1 times / day Route: oral Route: steady Dose: 30 mg, 1 times / day Sources: |
unhealthy, 48 years (range: 18-90 years) Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Sources: |
Disc. AE: Diarrhea... AEs leading to discontinuation/dose reduction: Diarrhea (0.2%) Sources: |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: |
unhealthy, 48 years (range: 18-90 years) Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Sources: |
Disc. AE: Diarrhea, Abdominal pain... AEs leading to discontinuation/dose reduction: Diarrhea (0.7%) Sources: Abdominal 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: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Disc. AE: Dyspepsia, Eructation... AEs leading to discontinuation/dose reduction: Dyspepsia (3 patients) Sources: Eructation (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: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Disc. AE: Dyspepsia, Eructation... AEs leading to discontinuation/dose reduction: Dyspepsia (1 patient) Sources: Eructation (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) Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F 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: |
unhealthy, 48 years (range: 18-90 years) Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Sources: |
| 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: |
unhealthy, 48 years (range: 18-90 years) Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Sources: |
| 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: |
unhealthy, 48 years (range: 18-90 years) Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Sources: |
| 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: |
unhealthy, 48 years (range: 18-90 years) Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Sources: |
| 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: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| 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: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| 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: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| 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: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| 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: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| 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: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| 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: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| 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: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| 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: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| 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 |
|---|---|---|---|---|
Page: 11.0 |
unlikely | |||
Page: 11.0 |
unlikely | |||
Page: 11.0 |
unlikely | |||
Page: 11.0 |
unlikely | |||
Page: 11.0 |
unlikely | |||
Page: 11.0 |
unlikely | |||
Page: 11.0 |
unlikely | |||
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 theophylline (CYP1A2 substrate) Page: 11.0 |
||
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 |
|---|---|---|---|---|
Page: 10.0 |
yes | |||
Page: 10,12 |
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 |
|---|---|---|
| Hypersensitivity to proton pump inhibitors: lansoprazole-induced Kounis syndrome. | 2009-05-29 |
|
| Lansoprazole protects and heals gastric mucosa from non-steroidal anti-inflammatory drug (NSAID)-induced gastropathy by inhibiting mitochondrial as well as Fas-mediated death pathways with concurrent induction of mucosal cell renewal. | 2008-05-23 |
|
| Gastroprotective and antioxidant effects of amiodarone on indomethacin-induced gastric ulcers in rats. | 2007-11 |
|
| Gastroprotective effect of mangiferin, a xanthonoid from Mangifera indica, against gastric injury induced by ethanol and indomethacin in rodents. | 2007-10 |
|
| Immune and Inflammatory Responses in GERD and Lansoprazole. | 2007-09 |
|
| Gastroprotective and antioxidant effects of montelukast on indomethacin-induced gastric ulcer in rats. | 2007-09 |
|
| Stimulation programs for pediatric drug research--do children really benefit? | 2007-08 |
|
| Antiulcerogenic effect and acute toxicity of a hydroethanolic extract from the cashew (Anacardium occidentale L.) leaves. | 2007-06-13 |
|
| Long-term management of gastroesophageal reflux disease with pantoprazole. | 2007-06 |
|
| Influence of rabeprazole and lansoprazole on the pharmacokinetics of tacrolimus in relation to CYP2C19, CYP3A5 and MDR1 polymorphisms in renal transplant recipients. | 2007-05 |
|
| Functional involvement of PHOSPHO1 in matrix vesicle-mediated skeletal mineralization. | 2007-04 |
|
| Influence of H pylori on plasma ghrelin in patients without atrophic gastritis. | 2007-03-14 |
|
| Prevalence and clinical manifestations of gastro-oesophageal reflux-associated chronic cough in the Japanese population. | 2007-01-08 |
|
| Protective effects of proton pump inhibitors against indomethacin-induced lesions in the rat small intestine. | 2007-01 |
|
| Laryngopharyngeal reflux disease with nocturnal gastric acid breakthrough while on proton pump inhibitor therapy. | 2006-12 |
|
| Suppression of proinflammatory cytokine production in macrophages by lansoprazole. | 2006-11 |
|
| Helicobacter pylori infection with a duodenal ulcer in a 6-year-old boy. | 2006-10 |
|
| Lack of pharmacokinetic interaction between omeprazole or lansoprazole and ivabradine in healthy volunteers: an open-label, randomized, crossover, pharmacokinetic interaction clinical trial. | 2006-10 |
|
| Beyond gastric acid reduction: proton pump inhibitors induce heme oxygenase-1 in gastric and endothelial cells. | 2006-07-07 |
|
| A proton pump inhibitor, lansoprazole, ameliorates asthma symptoms in asthmatic patients with gastroesophageal reflux disease. | 2006-07 |
|
| Myopathy including polymyositis: a likely class adverse effect of proton pump inhibitors? | 2006-06 |
|
| Comparison of the effects of proton pump inhibitors on human plasma adrenocorticotropic hormone and cortisol levels under the starved condition. | 2006-04 |
|
| Sensitive determination of omeprazole and its two main metabolites in human plasma by column-switching high-performance liquid chromatography: application to pharmacokinetic study in relation to CYP2C19 genotypes. | 2006-03-07 |
|
| Inlet patch of gastric mucosa in upper esophagus causing chronic cough and vocal cord dysfunction. | 2006-01 |
|
| Lansoprazole, a proton pump inhibitor, reduces the severity of indomethacin-induced rat enteritis. | 2006-01 |
|
| "Proton-pump inhibitor-first" strategy versus "step-up" strategy for the acute treatment of reflux esophagitis: a cost-effectiveness analysis in Japan. | 2005-11 |
|
| Management of symptoms in step-down therapy of gastroesophageal reflux disease. | 2005-09 |
|
| Mechanisms of action of leptin in preventing gastric ulcer. | 2005-07-21 |
|
| Lansoprazole prevents experimental gastric injury induced by non-steroidal anti-inflammatory drugs through a reduction of mucosal oxidative damage. | 2005-07-14 |
|
| Effect of concomitant dosing of famotidine with lansoprazole on gastric acid secretion in relation to CYP2C19 genotype status. | 2005-07-01 |
|
| Lansoprazole-associated collagenous colitis: a case report. | 2005-07 |
|
| Laryngopharyngeal reflux: prospective cohort study evaluating optimal dose of proton-pump inhibitor therapy and pretherapy predictors of response. | 2005-07 |
|
| Enhanced ghrelin secretion in rats with cysteamine-induced duodenal ulcers. | 2005-07 |
|
| CYP35: xenobiotically induced gene expression in the nematode Caenorhabditis elegans. | 2005-06-01 |
|
| Prediction of genotoxicity of chemical compounds by statistical learning methods. | 2005-06 |
|
| Preventive therapy for non-steroidal anti-inflammatory drug-induced ulcers in Japanese patients with rheumatoid arthritis: the current situation and a prospective controlled-study of the preventive effects of lansoprazole or famotidine. | 2005-06 |
|
| Hyponatremia with consciousness disturbance associated with esomeprazole. | 2005-04 |
|
| Neuropathy associated with lansoprazole treatment. | 2005-01 |
|
| Lansoprazole ameliorates intestinal mucosal damage induced by ischemia-reperfusion in rats. | 2004-10-01 |
|
| Management of acid-related disorders in patients with dysphagia. | 2004-09-06 |
|
| Interleukin-8 expression in the esophageal mucosa of patients with gastroesophageal reflux disease. | 2004-09 |
|
| Effect of lansoprazole and rabeprazole on tacrolimus pharmacokinetics in healthy volunteers with CYP2C19 mutations. | 2004-08 |
|
| Comparison of inhibitory effects of the proton pump-inhibiting drugs omeprazole, esomeprazole, lansoprazole, pantoprazole, and rabeprazole on human cytochrome P450 activities. | 2004-08 |
|
| Aplastic anemia associated with initiation of nizatidine therapy in a hemodialysis patient. | 2004-06 |
|
| An extensive metabolizer with recurrent ulcer responding to high dose of lansoprazole. | 2004-05-18 |
|
| Identification and relative contributions of human cytochrome P450 isoforms involved in the metabolism of glibenclamide and lansoprazole: evaluation of an approach based on the in vitro substrate disappearance rate. | 2004-05 |
|
| Enhanced expression of interleukin-8 and activation of nuclear factor kappa-B in endoscopy-negative gastroesophageal reflux disease. | 2004-04 |
|
| [Eradication effect of lansoprazole-based triple therapy against H. pylori]. | 2004-03 |
|
| [Myoclonic encephalopathy associated with proton pump inhibitors]. | 2004-03 |
|
| H2-receptor antagonist-refractory ulcer: its pathophysiology and treatment. | 1991 |
Patents
Sample Use Guides
Duodenal Ulcers: 15 mg Once daily for 4 weeks
Gastroesophageal Reflux: 30 mg Once daily for up to 8 weeks
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9184356
Lansoprazole is a gastric parietal cell proton pump inhibitor that is also active against Helicobacter pylori in vitro. The antimicrobial activity of lansoprazole and of its sulfenamide, a rearrangement product occurring spontaneously in acid environments, was studied by determining the MICs and MBCs for 11 cytotoxic and eight non-cytotoxic H. pylori strains and by measuring the rapidity of bacterial killing. The MIC90 and MBC90 were 2.5 mg/L and 10 mg/L, respectively, both for lansoprazole and for its sulfenamide.
| Substance Class |
Chemical
Created
by
admin
on
Edited
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0K5C5T2QPG
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Validated (UNII)
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WHO-ATC |
A02BC03
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QA02BD07
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NBK548452
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QA02BD03
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A02BD03
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A02BD02
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A02BD10
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A02BD07
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NCI_THESAURUS |
C29723
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WHO-VATC |
QA02BC03
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FDA ORPHAN DRUG |
446014
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A02BC53
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NDF-RT |
N0000000147
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N0000175525
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WHO-ATC |
A02BD09
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m6683
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ASSAY (TITRATION)
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||
|
DEGRADENT -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
|
||
|
|
SALT/SOLVATE -> PARENT | |||
|
|
ENANTIOMER -> RACEMATE | |||
|
BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
USP
|
||
|
BINDER->LIGAND |
BINDING
|
||
|
|
TARGET -> INHIBITOR |
|
||
|
METABOLIC ENZYME -> INDUCER | |||
|
DEGRADENT -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
METABOLIC ENZYME -> SUBSTRATE |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
METABOLITE ACTIVE -> PRODRUG |
|
||
|
|
METABOLITE ACTIVE -> PRODRUG | |||
|
METABOLITE ACTIVE -> PRODRUG | |||
|
METABOLITE -> PARENT |
These metabolites have very little or no antisecretory activity.
|
||
|
METABOLITE -> PARENT |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Biological Half-life | PHARMACOKINETIC |
|
|
|||
| Volume of Distribution | PHARMACOKINETIC |
|
|
|||
| Biological Half-life | PHARMACOKINETIC |
|
With Hepatic impairment PHARMACOKINETIC PHARMACOKINETIC |
|
||