Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C16H21N3O2 |
Molecular Weight | 287.3568 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)CCC1=CNC2=C1C=C(C[C@H]3COC(=O)N3)C=C2
InChI
InChIKey=ULSDMUVEXKOYBU-ZDUSSCGKSA-N
InChI=1S/C16H21N3O2/c1-19(2)6-5-12-9-17-15-4-3-11(8-14(12)15)7-13-10-21-16(20)18-13/h3-4,8-9,13,17H,5-7,10H2,1-2H3,(H,18,20)/t13-/m0/s1
Molecular Formula | C16H21N3O2 |
Molecular Weight | 287.3568 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020768s019s021,021231s010s011lbl.pdfCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/9154322
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020768s019s021,021231s010s011lbl.pdf
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/9154322
Zolmitriptan (Zomig; formerly 311C90) is a novel 5-hydroxytryptamine (5HT)1B/1D receptor agonist with proven efficacy in the acute treatment of migraine with or without preceding aura. The N-desmethyl metabolite also has high affinity for 5-HT1B/1D and moderate affinity for 5-HT1A receptors. Migraines are likely due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system. The therapeutic activity of Zomig for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system, which result in cranial vessel constriction, and inhibition of pro-inflammatory neuropeptide release.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1983 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9154322 |
|||
Target ID: CHEMBL1898 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9154322 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Palliative | ZOMIG Approved UseINDICATIONS & USAGE Zolmitriptan is indicated for the acute treatment of migraine with or without aura in adults. Limitations of Use Only use zolmitriptan if a clear diagnosis of migraine has been established. If a patient has no response to zolmitriptan treatment for the first migraine attack, reconsider the diagnosis of migraine before zolmitriptan are administered to treat any subsequent attacks. Zolmitriptan is not indicated for the prevention of migraine attacks. Safety and effectiveness of zolmitriptan have not been established for cluster headache. Zolmitriptan is a serotonin(5-HT)1B/1D receptor agonist (triptan) indicated for the acute treatment of migraine with or without aura in adults (1) Limitations of Use: Use only after a clear diagnosis of migraine has been established (1) Not indicated for the prophylactic therapy of migraine (1) Not indicated for the treatment of cluster headache (1) Launch Date1997 |
|||
Palliative | ZOMIG Approved UseINDICATIONS & USAGE Zolmitriptan is indicated for the acute treatment of migraine with or without aura in adults. Limitations of Use Only use zolmitriptan if a clear diagnosis of migraine has been established. If a patient has no response to zolmitriptan treatment for the first migraine attack, reconsider the diagnosis of migraine before zolmitriptan are administered to treat any subsequent attacks. Zolmitriptan is not indicated for the prevention of migraine attacks. Safety and effectiveness of zolmitriptan have not been established for cluster headache. Zolmitriptan is a serotonin(5-HT)1B/1D receptor agonist (triptan) indicated for the acute treatment of migraine with or without aura in adults (1) Limitations of Use: Use only after a clear diagnosis of migraine has been established (1) Not indicated for the prophylactic therapy of migraine (1) Not indicated for the treatment of cluster headache (1) Launch Date1997 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
0.925 mg single, intravenous dose: 0.925 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
4.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
5.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
10 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
1.475 mg single, intravenous dose: 1.475 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
10.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
1.85 mg single, intravenous dose: 1.85 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
9.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
22.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
2.95 mg single, intravenous dose: 2.95 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
16.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
0.925 mg single, intravenous dose: 0.925 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
17.7 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
21.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
23.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
30.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
32.4 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
1.475 mg single, intravenous dose: 1.475 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
32.5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
1.85 mg single, intravenous dose: 1.85 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
54.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
55.7 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
71.2 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
2.95 mg single, intravenous dose: 2.95 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
0.925 mg single, intravenous dose: 0.925 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.29 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.56 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
2.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
1.475 mg single, intravenous dose: 1.475 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
2.32 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
1.85 mg single, intravenous dose: 1.85 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.82 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
2.66 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9833595 |
2.95 mg single, intravenous dose: 2.95 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
ZOLMITRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
75% |
unknown, unknown |
ZOLMITRIPTAN plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
5 mg single, intranasal Highest studied dose Dose: 5 mg Route: intranasal Route: single Dose: 5 mg Sources: Page: p.845 |
unhealthy, 41.7 ± 10.4 n = 783 Health Status: unhealthy Condition: Migraine Age Group: 41.7 ± 10.4 Sex: M+F Population Size: 783 Sources: Page: p.845 |
Disc. AE: Taste abnormality, Migraine aggravated... AEs leading to discontinuation/dose reduction: Taste abnormality (0.4%) Sources: Page: p.845Migraine aggravated (0.4%) |
50 mg single, oral Overdose Dose: 50 mg Route: oral Route: single Dose: 50 mg Sources: Page: p.13 |
unhealthy Health Status: unhealthy Condition: Migraine Sources: Page: p.13 |
Other AEs: Sedation... Other AEs: Sedation Sources: Page: p.13 |
5 mg single, oral (max) Recommended Dose: 5 mg Route: oral Route: single Dose: 5 mg Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Migraine Sources: Page: p.1 |
Disc. AE: Arrhythmia, Cerebral hemorrhage... AEs leading to discontinuation/dose reduction: Arrhythmia Sources: Page: p.1Cerebral hemorrhage Subarachnoid hemorrhage Stroke Gastrointestinal ischemia Peripheral vasoconstriction Serotonin syndrome |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Migraine aggravated | 0.4% Disc. AE |
5 mg single, intranasal Highest studied dose Dose: 5 mg Route: intranasal Route: single Dose: 5 mg Sources: Page: p.845 |
unhealthy, 41.7 ± 10.4 n = 783 Health Status: unhealthy Condition: Migraine Age Group: 41.7 ± 10.4 Sex: M+F Population Size: 783 Sources: Page: p.845 |
Taste abnormality | 0.4% Disc. AE |
5 mg single, intranasal Highest studied dose Dose: 5 mg Route: intranasal Route: single Dose: 5 mg Sources: Page: p.845 |
unhealthy, 41.7 ± 10.4 n = 783 Health Status: unhealthy Condition: Migraine Age Group: 41.7 ± 10.4 Sex: M+F Population Size: 783 Sources: Page: p.845 |
Sedation | 50 mg single, oral Overdose Dose: 50 mg Route: oral Route: single Dose: 50 mg Sources: Page: p.13 |
unhealthy Health Status: unhealthy Condition: Migraine Sources: Page: p.13 |
|
Arrhythmia | Disc. AE | 5 mg single, oral (max) Recommended Dose: 5 mg Route: oral Route: single Dose: 5 mg Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Migraine Sources: Page: p.1 |
Cerebral hemorrhage | Disc. AE | 5 mg single, oral (max) Recommended Dose: 5 mg Route: oral Route: single Dose: 5 mg Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Migraine Sources: Page: p.1 |
Gastrointestinal ischemia | Disc. AE | 5 mg single, oral (max) Recommended Dose: 5 mg Route: oral Route: single Dose: 5 mg Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Migraine Sources: Page: p.1 |
Peripheral vasoconstriction | Disc. AE | 5 mg single, oral (max) Recommended Dose: 5 mg Route: oral Route: single Dose: 5 mg Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Migraine Sources: Page: p.1 |
Serotonin syndrome | Disc. AE | 5 mg single, oral (max) Recommended Dose: 5 mg Route: oral Route: single Dose: 5 mg Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Migraine Sources: Page: p.1 |
Stroke | Disc. AE | 5 mg single, oral (max) Recommended Dose: 5 mg Route: oral Route: single Dose: 5 mg Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Migraine Sources: Page: p.1 |
Subarachnoid hemorrhage | Disc. AE | 5 mg single, oral (max) Recommended Dose: 5 mg Route: oral Route: single Dose: 5 mg Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Migraine Sources: Page: p.1 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020768ap_zomig_phrmrp1.pdf#page=26 Page: 26.0 |
weak | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020768ap_zomig_phrmrp1.pdf#page=26 Page: 26.0 |
yes | yes (co-administration study) Comment: The increased exposure to zolmitriptan and 183C91 by cimetidine indicated that a reduction in the total daily recommended dose of zolmitriptan may be necessary when treating migraine patients who are taking nonspecific cytochrome P450 inhibitors or specific cytochrome 1A2 inhibitors. (https://pubmed.ncbi.nlm.nih.gov/18370509/) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020768ap_zomig_phrmrp1.pdf#page=26 Page: 26.0 |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/10553725/ Page: - |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/10553725/ Page: - |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/10553725/ Page: - |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/10553725/ Page: - |
weak | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/10553725/ Page: - |
weak | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/10553725/ Page: - |
weak | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/10553725/ Page: - |
weak | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020768ap_zomig_phrmrp1.pdf#page=25 Page: 25.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020768ap_zomig_phrmrp1.pdf#page=25 Page: 25.0 |
yes | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/22509823/ Page: - |
yes | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/17524230/ Page: - |
yes |
PubMed
Title | Date | PubMed |
---|---|---|
Pre-clinical pharmacology of zolmitriptan (Zomig; formerly 311C90), a centrally and peripherally acting 5HT1B/1D agonist for migraine. | 1997 Oct |
|
Pharmacological analysis of the haemodynamic effects of 5-HT1B/D receptor agonists in the normotensive rat. | 1998 Jan |
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Zolmitriptan (311C90) does not interact with fluoxetine in healthy volunteers. | 1998 Jun |
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[Mechanism of action of zolmitriptan]. | 1998 Oct |
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Profiles of 5-HT 1B/1D agonists in acute migraine with special reference to second generation agents. | 1999 Jun |
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Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. | 1999 Mar 5 |
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Are triptans with enhanced lipophilicity used for the acute treatment of migraine associated with an increased consulting rate for depressive illness? | 2000 Oct |
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Zolmitriptan versus a combination of acetylsalicylic acid and metoclopramide in the acute oral treatment of migraine: a double-blind, randomised, three-attack study. | 2002 |
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Cost considerations of acute migraine treatment. | 2004 Mar |
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Prediction of genotoxicity of chemical compounds by statistical learning methods. | 2005 Jun |
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[3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties. | 2005 Mar |
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Myocardial infarction after taking zolmitriptan. | 2005 May |
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Anti-migraine action of triptans is preceded by transient aggravation of headache caused by activation of meningeal nociceptors. | 2005 May |
|
Myalgia and cramps associated with zolmitriptan. | 2005 Sep-Oct |
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Improved migraine management in primary care: results of a patient treatment experience study using zolmitriptan orally disintegrating tablet. | 2006 Dec |
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Molecular drug targets and structure based drug design: A holistic approach. | 2006 Dec 23 |
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Acute renal failure in a 17-year-old female with ALL receiving escalating intravenous methotrexate without leukovorin. | 2007 Aug |
|
The 1:1 inclusion compounds zolmitriptan-benzene and zolmitriptan-phenol. | 2007 Jul |
|
Triptans and troponin: a case report. | 2009 Jun 18 |
|
Takotsubo syndrome (or apical ballooning syndrome) secondary to Zolmitriptan. | 2015 Mar-Apr |
Patents
Sample Use Guides
The recommended starting dose of ZOMIG (zolmitriptan) is 1.25 mg or
2.5 mg. The 1.25 mg dose can be achieved by manually breaking the functionally-scored 2.5 mg tablet in half. The maximum recommended single dose of ZOMIG is 5 mg.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10844127
Stimulation of a Ca(2+)-dependent K(+) current by zolmitriptan was investigated in C6 glioma cells stably expressing recombinant human 5-HT(1B) receptors. Outward K(+) currents (I(K)) were examined in non-transfected C6 glioma cells and in cells expressing cloned human 5-HT(1B) receptors using the patch-clamp technique in the whole-cell configuration. In C6 glioma cells expressing recombinant human 5-HT 1B) receptor, zolmitriptan increased I(K) in a concentration-dependent manner (maximum increase 16.3+/-7.8%, n=5, p<0.001) with a pD(2) value (geometric mean with 95% confidence intervals) of 7.03 (7.90-6.10). Zolmitriptan failed to elicit increases in I(K) in non-transfected C6 cells.
Substance Class |
Chemical
Created
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admin
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Record UNII |
2FS66TH3YW
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Record Status |
Validated (UNII)
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Record Version |
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WHO-VATC |
QN02CC03
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NCI_THESAURUS |
C47794
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NDF-RT |
N0000175763
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NDF-RT |
N0000175765
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WHO-ATC |
N02CC03
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LIVERTOX |
1052
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NDF-RT |
N0000175764
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7408
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JJ-2
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admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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Zolmitriptan
Created by
admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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60
Created by
admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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760383
Created by
admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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2869
Created by
admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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ZOLMITRIPTAN
Created by
admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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DB00315
Created by
admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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10124
Created by
admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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C47789
Created by
admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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C089750
Created by
admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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DTXSID8045933
Created by
admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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135775
Created by
admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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PRIMARY | RxNorm | ||
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SUB00181MIG
Created by
admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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1727009
Created by
admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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2FS66TH3YW
Created by
admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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m11660
Created by
admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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CHEMBL1185
Created by
admin on Fri Dec 15 15:53:18 GMT 2023 , Edited by admin on Fri Dec 15 15:53:18 GMT 2023
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Related Record | Type | Details | ||
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TARGET -> AGONIST |
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BINDER->LIGAND |
BINDING
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TARGET -> AGONIST | |||
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TARGET -> AGONIST |
Related Record | Type | Details | ||
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METABOLITE INACTIVE -> PARENT | |||
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METABOLITE ACTIVE -> PARENT | |||
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METABOLITE INACTIVE -> PARENT |
Related Record | Type | Details | ||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT | |||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT |
Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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