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 |
|||
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 |
|||
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 |
|||
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 |
|||
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 |
---|---|---|
[Evaluation of the effect of proton pump inhibitors on stomal ulcer]. | 1992 Jan |
|
Prostacyclin analog prevents stress-induced expression of immediate early genes and gastric mucosal lesions in the rat stomach. | 1999 |
|
Measurement of cytochrome P450 gene induction in human hepatocytes using quantitative real-time reverse transcriptase-polymerase chain reaction. | 2000 Jul |
|
Fluorometric screening for metabolism-based drug--drug interactions. | 2000 Jul-Aug |
|
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 |
|
[The effectiveness of 7-day combined Helicobacter eradication therapy in patients with peptic ulcer and chronic gastritis]. | 2001 |
|
[Administration of proton pump inhibitor caused esophageal stenosis in two patients with severe reflux esophagitis]. | 2001 Aug |
|
High-dose proton-pump inhibitors as a diagnostic test of gastro-oesophageal reflux disease in endoscopic-negative patients. | 2001 Aug |
|
Role of CYP3A4 and CYP2C19 in the stereoselective metabolism of lansoprazole by human liver microsomes. | 2001 Dec |
|
Gastroesophageal reflux in infants and children. | 2001 Dec 1 |
|
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 |
|
Inhibition of hyphal growth of Candida albicans by activated lansoprazole, a novel benzimidazole proton pump inhibitor. | 2001 Jun |
|
High-performance liquid chromatographic assay for the simultaneous determination of lansoprazole enantiomers and metabolites in human liver microsomes. | 2001 Jun 5 |
|
Review article: tackling the "dyspeptic problem". | 2001 Sep |
|
Bedtime H2 blockers improve nocturnal gastric acid control in GERD patients on proton pump inhibitors. | 2001 Sep |
|
Clinical and ethical concerns about switching patient treatment to "therapeutically interchangeable" medications. | 2001 Sep 24 |
|
Gastroesophageal reflux disease presenting as xerophthalmia. | 2001 Sep-Oct |
|
Potential role of endocrine gastrin in the colonic adenoma carcinoma sequence. | 2002 Aug 27 |
|
Lansoprazole induces mucosal protection through gastrin receptor-dependent up-regulation of cyclooxygenase-2 in rats. | 2002 Dec |
|
Acute manic psychosis induced by triple therapy for H. pylori. | 2002 Jan-Feb |
|
A comparative study on the activity of lansoprazole, omeprazole and PD-136450 on acidified ethanol- and indomethacin-induced gastric lesions in the rat. | 2002 Mar |
|
Anaphylaxis to proton pump inhibitors. | 2002 Nov-Dec |
|
ATPase inhibitors suppress actinomycin D-induced apoptosis in leukemia cells. | 2002 Sep-Oct |
|
Formulation study for lansoprazole fast-disintegrating tablet. I. Effect of compression on dissolution behavior. | 2003 Aug |
|
[New triple therapy for Helicobacter pylori infection in Japan]. | 2003 Jan |
|
Safety and pharmacokinetics of oral lansoprazole in preadolescent rats exposed from weaning through sexual maturity. | 2003 Jan-Feb |
|
Structural and functional characterization of gastric mucosa and central nervous system in histamine H2 receptor-null mice. | 2003 May 2 |
|
Lansoprazole increases testosterone metabolism and clearance in male Sprague-Dawley rats: implications for Leydig cell carcinogenesis. | 2003 Oct 15 |
|
Flavor and taste of lansoprazole strawberry-flavored delayed-release oral suspension preferred over ranitidine peppermint-flavored oral syrup: in children aged between 5-11 years. | 2004 |
|
Enhanced expression of interleukin-8 and activation of nuclear factor kappa-B in endoscopy-negative gastroesophageal reflux disease. | 2004 Apr |
|
Drug-induced tubulo-interstitial nephritis secondary to proton pump inhibitors: experience from a single UK renal unit. | 2004 Jun |
|
[Eradication effect of lansoprazole-based triple therapy against H. pylori]. | 2004 Mar |
|
[Myoclonic encephalopathy associated with proton pump inhibitors]. | 2004 Mar |
|
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 May |
|
Lansoprazole-tacrolimus interaction in Japanese transplant recipient with CYP2C19 polymorphism. | 2004 May |
|
An extensive metabolizer with recurrent ulcer responding to high dose of lansoprazole. | 2004 May-Jun |
|
Management of acid-related disorders in patients with dysphagia. | 2004 Sep 6 |
|
Management of symptoms in step-down therapy of gastroesophageal reflux disease. | 2005 Sep |
|
Lansoprazole, a proton pump inhibitor, reduces the severity of indomethacin-induced rat enteritis. | 2006 Jan |
|
A proton pump inhibitor, lansoprazole, ameliorates asthma symptoms in asthmatic patients with gastroesophageal reflux disease. | 2006 Jul |
|
Myopathy including polymyositis: a likely class adverse effect of proton pump inhibitors? | 2006 Jun |
|
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 Mar 7 |
|
Suppression of proinflammatory cytokine production in macrophages by lansoprazole. | 2006 Nov |
|
Lack of pharmacokinetic interaction between omeprazole or lansoprazole and ivabradine in healthy volunteers: an open-label, randomized, crossover, pharmacokinetic interaction clinical trial. | 2006 Oct |
|
Stimulation programs for pediatric drug research--do children really benefit? | 2007 Aug |
|
Influence of H pylori on plasma ghrelin in patients without atrophic gastritis. | 2007 Mar 14 |
|
Gastroprotective and antioxidant effects of amiodarone on indomethacin-induced gastric ulcers in rats. | 2007 Nov |
|
Immune and Inflammatory Responses in GERD and Lansoprazole. | 2007 Sep |
|
Gastroprotective and antioxidant effects of montelukast on indomethacin-induced gastric ulcer in rats. | 2007 Sep |
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
Mon Mar 31 18:03:12 GMT 2025
by
admin
on
Mon Mar 31 18:03:12 GMT 2025
|
Record UNII |
0K5C5T2QPG
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Preferred Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Brand Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Code | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Brand Name | English | ||
|
Brand Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
WHO-ATC |
A02BC03
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
||
|
WHO-VATC |
QA02BD07
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
||
|
LIVERTOX |
NBK548452
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
||
|
WHO-VATC |
QA02BD03
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
||
|
WHO-ATC |
A02BD03
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
||
|
WHO-VATC |
QA02BD02
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
||
|
WHO-ATC |
A02BD02
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
||
|
WHO-ATC |
A02BD10
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
||
|
WHO-ATC |
A02BD07
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
||
|
NCI_THESAURUS |
C29723
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
||
|
WHO-VATC |
QA02BC03
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
||
|
FDA ORPHAN DRUG |
446014
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
||
|
WHO-ATC |
A02BC53
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
||
|
NDF-RT |
N0000000147
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
||
|
NDF-RT |
N0000175525
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
||
|
FDA ORPHAN DRUG |
264508
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
||
|
WHO-ATC |
A02BD09
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
m6683
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | Merck Index | ||
|
0K5C5T2QPG
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
100000089867
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
17128
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | RxNorm | ||
|
1356916
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
N0000009724
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | Inhibition Gastric Acid Secretion [PE] | ||
|
3883
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
1547
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
103577-45-3
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
6397
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
7208
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
DB00448
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
C29150
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
LANSOPRAZOLE
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
C058687
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
758638
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
7204
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
Lansoprazole
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
DTXSID4023200
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
0K5C5T2QPG
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
SUB08403MIG
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
CHEMBL480
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
AA-78
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY | |||
|
6375
Created by
admin on Mon Mar 31 18:03:12 GMT 2025 , Edited by admin on Mon Mar 31 18:03:12 GMT 2025
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
ENANTIOMER -> RACEMATE | |||
|
BASIS OF STRENGTH->SUBSTANCE |
ASSAY (TITRATION)
EP
|
||
|
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 |
|
||