ELETRIPTAN HEMISULFATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	2C22H26N2O2S.H2O4S
Molecular Weight	863.117
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OS(O)(=O)=O.CN1CCC[C@@H]1CC2=CNC3=C2C=C(CCS(=O)(=O)C4=CC=CC=C4)C=C3.CN5CCC[C@@H]5CC6=CNC7=C6C=C(CCS(=O)(=O)C8=CC=CC=C8)C=C7

InChI

InChIKey=IYVZCNNIKYUHHM-WXMGBDCWSA-N

InChI=1S/2C22H26N2O2S.H2O4S/c2*1-24-12-5-6-19(24)15-18-16-23-22-10-9-17(14-21(18)22)11-13-27(25,26)20-7-3-2-4-8-20;1-5(2,3)4/h2*2-4,7-10,14,16,19,23H,5-6,11-13,15H2,1H3;(H2,1,2,3,4)/t2*19-;/m11./s1

HIDE SMILES / InChI

Molecular Formula	H2O4S
Molecular Weight	98.078
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C22H26N2O2S
Molecular Weight	382.519
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21016_relpax_lbl.pdf
Curator's Comment: Description was created using several sources including: https://www.ncbi.nlm.nih.gov/pubmed/10193663 | http://www.migraines.org/treatment/pro_rlpx.htm

Eletriptan (eletriptan hydrobromide, trade name Relpax) is a selective 5-hydroxytryptamine (5-HT1B/1D) serotonin receptor agonist (triptan) indicated for the acute treatment of migraine with or without aura in adults. Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, and has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors. The therapeutic activity of eletriptan 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. Eletriptan (Relpax) has been approved for use in the acute treatment of migraine in 51 countries and has been introduced in 17 countries including Mexico, Italy, France and Japan.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
5-hydroxytryptamine receptor 1D 17 Target ID: P28221 Gene ID: 3352.0 Gene Symbol: HTR1D Target Organism: Homo sapiens (Human) Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21016_relpax_lbl.pdf	Agonist 2678	0.92 nM [Kd]
5-hydroxytryptamine receptor 1B 21 Target ID: P28222 Gene ID: 3351.0 Gene Symbol: HTR1B Target Organism: Homo sapiens (Human) Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21016_relpax_lbl.pdf	Agonist 2678	3.14 nM [Kd]
5-hydroxytryptamine receptor 1F 8 Target ID: P30939 Gene ID: 3355.0 Gene Symbol: HTR1F Target Organism: Homo sapiens (Human) Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21016_relpax_lbl.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/11834243	Agonist 2678

Conditions

Condition	Modality	Targets	Highest Phase	Product
Migraine 103 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21016_relpax_lbl.pdf	Primary		Approved 8429	RELPAX Approved Use RELPAX is indicated for the acute treatment of migraine with or without aura in adults. RELPAX is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. Safety and effectiveness of RELPAX Tablets have not been established for cluster headache, which is present in an older, predominantly male population. Launch Date 1.04086077E12

C_max

Value	Dose	Analyte	Population
183.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	40 mg 2 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
200.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
46.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
94.72 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED

AUC

Value	Dose	Analyte	Population
1278 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	40 mg 2 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
1282 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
291.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
575.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED

T_1/2

Value	Dose	Analyte	Population
4.75 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	40 mg 2 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
4.58 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
4.92 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
4.63 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
15% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021016s021s023s024s027lbl.pdf			ELETRIPTAN plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	Disc. AE: Nausea, Dizziness... AEs leading to discontinuation/dose reduction: Nausea (0.4%) Dizziness (0.4%) Asthenia (0.3%) Chest pain (0.3%) Headache (0.2%) Vomiting (0.2%) Hypertonia (0.2%) Paresthesia (0.2%) Somnolence (0.2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102

AEs

AE	Significance	Dose	Population
Headache	0.2% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102
Hypertonia	0.2% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102
Paresthesia	0.2% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102
Somnolence	0.2% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102
Vomiting	0.2% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102
Asthenia	0.3% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102
Chest pain	0.3% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102
Dizziness	0.4% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102
Nausea	0.4% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inhibitor 1587 inducer 781	inhibitor 1767 inducer 389	substrate 1217 inhibitor 1852 inducer 97

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2C19 1478 CYP1A2 1524 CYP2B6 810 CYP2E1 882	CYP1A 22 P-gp 1537	CYP2A6 79 CYP1A2 701 CYP2C19 293 CYP2E1 128

Drug as perpetrator

Target	Modality	Activity
CYP2A6 739	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	likely
CYP2B6 1001	inhibitor 3277 Sources: https://dmd.aspetjournals.org/content/31/7/861.long Page: 7,8	little
CYP2C19 1553	inhibitor 3277 Sources: https://dmd.aspetjournals.org/content/31/7/861.long Page: 7,8	little
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	no
CYP2C19 1553	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	no
CYP2C9 1819	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	no
CYP2D6 1891	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	no
CYP2E1 970	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	no
CYP2E1 970	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	no
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	yes [IC50 41 uM]
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
P-gp 1537	substrate 3367 Sources: https://dmd.aspetjournals.org/content/31/7/861.long Page: 9.0	inconclusive
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=9 Page: 9.0	major	yes (co-administration study) Comment: when administered with ketoconazole, Cmax and AUC increased by 2.7-fold and 5.9-fold, respectively; when administered with verapamil, Cmax and AUC increased by 2.2-fold and 2.7-fold, respectively; when administered with fluconazole, Cmax and AUC increased by 1.4-fold and 2-fold, respectively; Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=9 Page: 9.0
CYP1A 22	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=9 Page: 9.0	minor
CYP2D6 1217	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=9 Page: 9.0	minor

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:50922	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:50922
ChemicalBook	CB1404591	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB1404591
MolPort	MolPort-005-940-717	https://www.molport.com/shop/molecule-link/MolPort-005-940-717
ZINC	ZINC000003823475	http://zinc15.docking.org/substances/ZINC000003823475
eMolecules	30512783	https://www.emolecules.com/cgi-bin/more?vid=30512783

PubMed

Title	Date	PubMed
Eletriptan: pharmacological differences and clinical results.	2001	12463280
Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain.	2001 Aug 17	11513839
Pharmacokinetics and safety of oral eletriptan during different phases of the menstrual cycle in healthy volunteers.	2001 Dec	11762561
Safety and rational use of the triptans.	2001 Jul	11480267
Oral triptans (serotonin 5-HT(1B/1D) agonists) in acute migraine treatment: a meta-analysis of 53 trials.	2001 Nov 17	11728541
Spotlight on rizatriptan in migraine.	2002	12269863
Gateways to Clinical Trials.	2002 Apr	12087878
Sumatriptan versus eletriptan: which is best?	2002 Dec	12849329
Efficacy, safety and tolerability of oral eletriptan in the acute treatment of migraine: results of a phase III, multicentre, placebo-controlled study across three attacks.	2002 Feb	11993610
[Migraine has to be treated. Otherwise a stroke threatens].	2002 Feb 14	11887744
Tripstar: a comprehensive patient-based approach to compare triptans.	2002 Jan	11966860
[New triptanes in control of migraine attacks. More rapid onset of action--more efficient reduction of pain].	2002 Jan 24	11862794
Mechanisms of action of the 5-HT1B/1D receptor agonists.	2002 Jul	12117355
Pharmacological treatments for acute migraine: quantitative systematic review.	2002 Jun	12044621
Pharmacokinetics, pharmacodynamics, and safety of the 5-HT(1B/1D) agonist eletriptan following intravenous and oral administration.	2002 May	12017347
The pharmacokinetics and safety of single escalating oral doses of eletriptan.	2002 May	12017346
Agonist-directed trafficking explaining the difference between response pattern of naratriptan and sumatriptan in rabbit common carotid artery.	2002 May	12010764
Gateways to clinical trials.	2002 Oct	12500432
Triptans (serotonin, 5-HT1B/1D agonists) in migraine: detailed results and methods of a meta-analysis of 53 trials.	2002 Oct	12383060
Suppression by eletriptan of the activation of trigeminovascular sensory neurons by glyceryl trinitrate.	2002 Oct 25	12384251
Eletriptan Pfizer.	2002 Sep	12498013
Gateways to Clinical Trials.	2002 Sep	12428432
Current perspectives on effective migraine treatments: are small clinical differences important for patients?	2003	15071619
Newer formulations of the triptans: advances in migraine management.	2003	14524731
Eletriptan (relpax) for migraine.	2003 Apr 28	12719695
[Treatment of migraine: an update].	2003 Jan	15095723
[Pharmacological, pharmacokinetic and clinical profile of eletriptan (Relpax), a new triptan for migraine].	2003 Jul	12843576
Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoprotein.	2003 Jul	12814962
The evolving management of migraine.	2003 Jun	12858071
Efficacy, safety, and tolerability of oral eletriptan for treatment of acute migraine: a multicenter, double-blind, placebo-controlled study conducted in the United States.	2003 Mar	12603638
[Highly selective beginning. Associated symptoms and side effects in retrospect].	2003 May 26	14579499
[Improved pharmacokinetics. Fast tryptan with sustained response].	2003 May 26	14579498
Comparative efficacy of eletriptan vs. naratriptan in the acute treatment of migraine.	2003 Nov	14616928
Tolerability and safety of eletriptan in the treatment of migraine: a comprehensive review.	2003 Oct	14511273
Encapsulated sumatriptan is not bioequivalent to commercial sumatriptan.	2003 Sep	14562837
The 40-mg dose of eletriptan: comparative efficacy and tolerability versus sumatriptan 100 mg.	2004 Feb	14748774
[Recent progress in therapy for migraine headache].	2004 Feb 10	15007953
Neuronal expression and regulation of CGRP promoter activity following viral gene transfer into cultured trigeminal ganglia neurons.	2004 Jan 30	14715155
Gateways to clinical trials.	2004 Jan-Feb	14988742
Effect of high-dose intravenous eletriptan on coronary artery diameter.	2004 Jul	15196292
Triptans and CNS side-effects: pharmacokinetic and metabolic mechanisms.	2004 Jun	15154851
Gateways to clinical trials.	2004 Mar	15071612
Cost considerations of acute migraine treatment.	2004 Mar	15012668
Cost effectiveness of oral triptan therapy: a trans-national comparison based on a meta-analysis of randomised controlled trials.	2004 May	15140331
Double-blind clinical trials of oral triptans vs other classes of acute migraine medication - a review.	2004 May	15096220
[Spanish contribution to the clinical development of eletriptan: an analysis of controlled studies].	2004 Oct	15470580
No effect of eletriptan administration during the aura phase of migraine.	2004 Oct	15469451
[Triptans in migraine: from clinical view].	2004 Sep	15552862
Gateways to clinical trials.	2004 Sep	15538546
Priorities for triptan treatment attributes and the implications for selecting an oral triptan for acute migraine: a study of US primary care physicians (the TRIPSTAR Project).	2004 Sep	15531016

Patents

Sample Use Guides

In Vivo Use Guide

The maximum recommended single dose of Relpax (eletriptan hydrobromide) is 40 mg. If after the initial dose, headache improves but then returns, a repeat dose may be beneficial. If a second dose is required, it should be taken at least 2 hours after the initial dose. If the initial dose is ineffective, controlled clinical trials have not shown a benefit of a second dose to treat the same attack. The maximum daily dose should not exceed 80 mg.

Route of Administration: Oral

In Vitro Use Guide

The 5-hydroxytryptamine (5-HT) receptor mediation of the contraction in guinea-pig iliac arteries moderately precontracted by prostaglandin F2alpha (PGF2alpha) was characterized in vitro using eletriptan. Eletriptan contracted guinea-pig iliac arteries and the concentration-response curve for eletriptan was biphasic (first phase: 0.01-3 uM, pD2 approximately 6.6; second phase: greater or equal 10 uM).

Substance Class	Chemical Created by `admin` on `Fri Dec 15 16:24:33 UTC 2023` Edited by `admin` on `Fri Dec 15 16:24:33 UTC 2023`
Record UNII	AMM8PSU28B
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ELETRIPTAN HEMISULFATE

Common Name

English

Code System Code Type Description

PUBCHEM

9832589

Created by admin on Fri Dec 15 16:24:33 UTC 2023 , Edited by admin on Fri Dec 15 16:24:33 UTC 2023

PRIMARY

CAS

219790-71-3

Created by admin on Fri Dec 15 16:24:33 UTC 2023 , Edited by admin on Fri Dec 15 16:24:33 UTC 2023

PRIMARY

FDA UNII

AMM8PSU28B

Created by admin on Fri Dec 15 16:24:33 UTC 2023 , Edited by admin on Fri Dec 15 16:24:33 UTC 2023

PRIMARY

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ELETRIPTAN

ACTIVE MOIETY

Details

SMILES

InChI

DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21016_relpax_lbl.pdfCurator's Comment: Description was created using several sources including: https://www.ncbi.nlm.nih.gov/pubmed/10193663 | http://www.migraines.org/treatment/pro_rlpx.htm

CNS Activity

Originator

Approval Year

Targets

Conditions

Approved Use

Launch Date

Cmax

AUC

T1/2

Funbound

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Sourcing

PubMed

Patents

Sample Use Guides

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21016_relpax_lbl.pdf
Curator's Comment: Description was created using several sources including: https://www.ncbi.nlm.nih.gov/pubmed/10193663 | http://www.migraines.org/treatment/pro_rlpx.htm

C_max

T_1/2

F_unbound

Drug as perpetrator