Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C16H14F3N3O2S |
Molecular Weight | 369.361 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 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-RUZDIDTESA-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)/t25-/m1/s1
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 |
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Target ID: CHEMBL2095173 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20974316 |
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Target ID: CHEMBL2095173 |
5.2 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | PREVACID Approved UseUse •treats frequent heartburn (occurs 2 or more days a week) •not intended for immediate relief of heartburn; this drug may take 1 to 4 days for full effect Launch 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 |
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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 |
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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 |
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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 |
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 |
|
[Proton pump inhibitors in the treatment of peptic ulcers resistant to H2-receptor antagonists]. | 1992 Jan |
|
[Submicroscopic aspects of the mechanism of inhibitors of H+/K+-ATPase in gastric parietal cells]. | 2002 |
|
Lansoprazole induces mucosal protection through gastrin receptor-dependent up-regulation of cyclooxygenase-2 in rats. | 2002 Dec |
|
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 |
|
Time-dependent transcriptional induction of CYP1A1, CYP1A2 and CYP1B1 mRNAs by H+/K+ -ATPase inhibitors and other xenobiotics. | 2003 Feb |
|
[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 |
|
Does eradication of Helicobacter pylori reduce hypergastrinaemia during long term therapy with proton pump inhibitors? | 2003 Mar |
|
Structural and functional characterization of gastric mucosa and central nervous system in histamine H2 receptor-null mice. | 2003 May 2 |
|
Formulation study for lansoprazole fast-disintegrating tablet. III. Design of rapidly disintegrating tablets. | 2003 Oct |
|
Stereoselective metabolism of lansoprazole by human liver cytochrome P450 enzymes. | 2003 Oct |
|
Lansoprazole increases testosterone metabolism and clearance in male Sprague-Dawley rats: implications for Leydig cell carcinogenesis. | 2003 Oct 15 |
|
Formulation study for lansoprazole fast-disintegrating tablet. II. Effect of triethyl citrate on the quality of the products. | 2003 Sep |
|
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 |
|
Comparison of inhibitory effects of the proton pump-inhibiting drugs omeprazole, esomeprazole, lansoprazole, pantoprazole, and rabeprazole on human cytochrome P450 activities. | 2004 Aug |
|
Drug-induced tubulo-interstitial nephritis secondary to proton pump inhibitors: experience from a single UK renal unit. | 2004 Jun |
|
Lansoprazole-tacrolimus interaction in Japanese transplant recipient with CYP2C19 polymorphism. | 2004 May |
|
Interleukin-8 expression in the esophageal mucosa of patients with gastroesophageal reflux disease. | 2004 Sep |
|
Lansoprazole-associated collagenous colitis: a case report. | 2005 Jul |
|
Laryngopharyngeal reflux: prospective cohort study evaluating optimal dose of proton-pump inhibitor therapy and pretherapy predictors of response. | 2005 Jul |
|
Enhanced ghrelin secretion in rats with cysteamine-induced duodenal ulcers. | 2005 Jul |
|
Effect of concomitant dosing of famotidine with lansoprazole on gastric acid secretion in relation to CYP2C19 genotype status. | 2005 Jul 1 |
|
Lansoprazole prevents experimental gastric injury induced by non-steroidal anti-inflammatory drugs through a reduction of mucosal oxidative damage. | 2005 Jul 14 |
|
Mechanisms of action of leptin in preventing gastric ulcer. | 2005 Jul 21 |
|
Prediction of genotoxicity of chemical compounds by statistical learning methods. | 2005 Jun |
|
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 Jun |
|
CYP35: xenobiotically induced gene expression in the nematode Caenorhabditis elegans. | 2005 Jun 1 |
|
"Proton-pump inhibitor-first" strategy versus "step-up" strategy for the acute treatment of reflux esophagitis: a cost-effectiveness analysis in Japan. | 2005 Nov |
|
Management of symptoms in step-down therapy of gastroesophageal reflux disease. | 2005 Sep |
|
Comparison of the effects of proton pump inhibitors on human plasma adrenocorticotropic hormone and cortisol levels under the starved condition. | 2006 Apr |
|
Laryngopharyngeal reflux disease with nocturnal gastric acid breakthrough while on proton pump inhibitor therapy. | 2006 Dec |
|
Inlet patch of gastric mucosa in upper esophagus causing chronic cough and vocal cord dysfunction. | 2006 Jan |
|
Lansoprazole, a proton pump inhibitor, reduces the severity of indomethacin-induced rat enteritis. | 2006 Jan |
|
Beyond gastric acid reduction: proton pump inhibitors induce heme oxygenase-1 in gastric and endothelial cells. | 2006 Jul 7 |
|
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 |
|
Lack of pharmacokinetic interaction between omeprazole or lansoprazole and ivabradine in healthy volunteers: an open-label, randomized, crossover, pharmacokinetic interaction clinical trial. | 2006 Oct |
|
Long-term management of gastroesophageal reflux disease with pantoprazole. | 2007 Jun |
|
Antiulcerogenic effect and acute toxicity of a hydroethanolic extract from the cashew (Anacardium occidentale L.) leaves. | 2007 Jun 13 |
|
Influence of H pylori on plasma ghrelin in patients without atrophic gastritis. | 2007 Mar 14 |
|
Influence of rabeprazole and lansoprazole on the pharmacokinetics of tacrolimus in relation to CYP2C19, CYP3A5 and MDR1 polymorphisms in renal transplant recipients. | 2007 May |
|
Gastroprotective and antioxidant effects of amiodarone on indomethacin-induced gastric ulcers in rats. | 2007 Nov |
|
Gastroprotective effect of mangiferin, a xanthonoid from Mangifera indica, against gastric injury induced by ethanol and indomethacin in rodents. | 2007 Oct |
|
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 |
|
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 May 23 |
|
Hypersensitivity to proton pump inhibitors: lansoprazole-induced Kounis syndrome. | 2009 May 29 |
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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by
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Record UNII |
UYE4T5I70X
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Validated (UNII)
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NDF-RT |
N0000000147
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WHO-VATC |
QA02BC06
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NCI_THESAURUS |
C29723
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WHO-ATC | A02BC06 | ||
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N0000175525
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DEXLANSOPRAZOLE
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Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
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BINDER->LIGAND |
BINDING
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RACEMATE -> ENANTIOMER |
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SOLVATE->ANHYDROUS |
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SALT/SOLVATE -> PARENT |
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE -> PARENT |
MINOR
FECAL
|
||
|
METABOLITE ACTIVE -> PRODRUG |
|
||
|
METABOLITE -> PARENT |
MINOR
FECAL
|
||
|
METABOLITE -> PARENT |
In poor metabolizer; mediator: CYP3A
MAJOR
PLASMA
|
||
|
METABOLITE -> PARENT |
Minor in plasma
MAJOR
FECAL
|
||
|
METABOLITE -> PARENT |
EM sujects
MAJOR
PLASMA; URINE
|
||
|
METABOLITE -> PARENT |
EM Subjects
MAJOR
PLASMA; URINE
|
||
|
METABOLITE -> PARENT |
PM sujects
MAJOR
URINE
|
||
|
METABOLITE -> PARENT |
Extensive metabolizers
MINOR
URINE
|
||
|
METABOLITE -> PARENT |
EM Subjects
MAJOR
PLASMA
|
||
|
METABOLITE ACTIVE -> PRODRUG |
|
||
|
METABOLITE -> PARENT |
MINOR
FECAL; PLASMA
|
||
|
METABOLITE -> PARENT |
MINOR
PLASMA; URINE
|
Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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