ELETRIPTAN SUCCINATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C22H26N2O2S.C4H6O4
Molecular Weight	500.607
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)CCC(O)=O.CN1CCC[C@@H]1CC2=CNC3=C2C=C(CCS(=O)(=O)C4=CC=CC=C4)C=C3

InChI

InChIKey=SYWHMGMNOKNVGL-FSRHSHDFSA-N

InChI=1S/C22H26N2O2S.C4H6O4/c1-24-12-5-6-19(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;5-3(6)1-2-4(7)8/h2-4,7-10,14,16,19,23H,5-6,11-13,15H2,1H3;1-2H2,(H,5,6)(H,7,8)/t19-;/m1./s1

HIDE SMILES / InChI

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

Molecular Formula	C4H6O4
Molecular Weight	118.088
Charge	0
Count

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

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 18 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 2752	0.92 nM [Kd]
5-hydroxytryptamine receptor 1B 22 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 2752	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 2752

Conditions

Condition	Modality	Targets	Highest Phase	Product
Migraine 107 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21016_relpax_lbl.pdf	Primary		Approved 8583	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 2002

C_max

Value	Dose	Analyte	Population
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
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
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

AUC

Value	Dose	Analyte	Population
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
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
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

T_1/2

Value	Dose	Analyte	Population
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
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
4.75 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

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 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	unhealthy, 41.9 Health Status: unhealthy Age Group: 41.9 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf	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

AEs

AE	Significance	Dose	Population
Headache	0.2% Disc. AE	80 mg 1 times / day single, oral 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	unhealthy, 41.9 Health Status: unhealthy Age Group: 41.9 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf
Hypertonia	0.2% Disc. AE	80 mg 1 times / day single, oral 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	unhealthy, 41.9 Health Status: unhealthy Age Group: 41.9 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf
Paresthesia	0.2% Disc. AE	80 mg 1 times / day single, oral 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	unhealthy, 41.9 Health Status: unhealthy Age Group: 41.9 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf
Somnolence	0.2% Disc. AE	80 mg 1 times / day single, oral 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	unhealthy, 41.9 Health Status: unhealthy Age Group: 41.9 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf
Vomiting	0.2% Disc. AE	80 mg 1 times / day single, oral 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	unhealthy, 41.9 Health Status: unhealthy Age Group: 41.9 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf
Asthenia	0.3% Disc. AE	80 mg 1 times / day single, oral 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	unhealthy, 41.9 Health Status: unhealthy Age Group: 41.9 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf
Chest pain	0.3% Disc. AE	80 mg 1 times / day single, oral 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	unhealthy, 41.9 Health Status: unhealthy Age Group: 41.9 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf
Dizziness	0.4% Disc. AE	80 mg 1 times / day single, oral 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	unhealthy, 41.9 Health Status: unhealthy Age Group: 41.9 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf
Nausea	0.4% Disc. AE	80 mg 1 times / day single, oral 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	unhealthy, 41.9 Health Status: unhealthy Age Group: 41.9 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inhibitor 2252 inducer 1087	inhibitor 2438 inducer 440	substrate 1388 inhibitor 2507 inducer 109

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2C19 2057 CYP1A2 2153 CYP2B6 926 CYP2E1 1060	CYP1A 26 P-gp 2052	CYP2A6 86 CYP1A2 832 CYP2C19 329 CYP2E1 131

Drug as perpetrator

Target	Modality	Activity
CYP2A6 911	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	likely
CYP2B6 1160	inhibitor 4027 Sources: https://dmd.aspetjournals.org/content/31/7/861.long Page: 7,8	little
CYP2C19 2141	inhibitor 4027 Sources: https://dmd.aspetjournals.org/content/31/7/861.long Page: 7,8	little
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	no
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	no
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	no
CYP2D6 2546	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	no
CYP2E1 1146	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	no
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	no
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	yes [IC50 41 uM]
CYP3A4 2633	inducer 1966 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 2052	substrate 4014 Sources: https://dmd.aspetjournals.org/content/31/7/861.long Page: 9.0	inconclusive
CYP3A4 1946	substrate 4014 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 26	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=9 Page: 9.0	minor
CYP2D6 1388	substrate 4014 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
eMolecules	30512783	https://www.emolecules.com/cgi-bin/more?vid=30512783
MolPort	MolPort-005-940-717	https://www.molport.com/shop/molecule-link/MolPort-005-940-717
ZINC	ZINC000003823475	http://zinc15.docking.org/substances/ZINC000003823475

PubMed

Title	Date	PubMed
[A case of the usefulness of MR angiography and diffusion weighted image to evaluate migraine].	2004-10	15529793
[Spanish contribution to the clinical development of eletriptan: an analysis of controlled studies].	2004-10	15470580
No effect of eletriptan administration during the aura phase of migraine.	2004-10	15469451
Gateways to clinical trials.	2004-09-07	15349141
[Meta-analysis of triptan treatment in migraine].	2004-09	15552863
[Triptans in migraine: from clinical view].	2004-09	15552862
[Triptans in migraine: a comparative review of pharmacology, pharmacokinetics].	2004-09	15552861
Gateways to clinical trials.	2004-09	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).	2004-09	15531016
TRIPSTAR: prioritizing oral triptan treatment attributes in migraine management.	2004-09	15285768
Meta-analysis of oral triptans.	2004-08	15265060
Effect of high-dose intravenous eletriptan on coronary artery diameter.	2004-07	15196292
Cardiovascular safety of triptans.	2004-07	15196291
Involvement of 5-HT1B receptors in triptan-induced contractile responses in guinea-pig isolated iliac artery.	2004-07	15185063
Nitrergic and glutamatergic neuronal mechanisms at the trigeminovascular first-order synapse.	2004-07	15165837
Triptans and CNS side-effects: pharmacokinetic and metabolic mechanisms.	2004-06	15154851
Cost effectiveness of oral triptan therapy: a trans-national comparison based on a meta-analysis of randomised controlled trials.	2004-05	15140331
Double-blind clinical trials of oral triptans vs other classes of acute migraine medication - a review.	2004-05	15096220
Eletriptan for the short-term prophylaxis of cluster headache.	2004-04	15109360
Gateways to clinical trials.	2004-03	15071612
Eletriptan for the acute treatment of migraine: results of bridging a Japanese study to Western clinical trials.	2004-03	15025836
Cost considerations of acute migraine treatment.	2004-03	15012668
Effectiveness of eletriptan in acute migraine: primary care for Excedrin nonresponders.	2004-03	15012657
Gateways to clinical trials.	2004-02-28	14988742
The 5-hydroxytryptamine1B/1D/1F receptor agonists eletriptan and naratriptan inhibit trigeminovascular input to the nucleus tractus solitarius in the cat.	2004-02-13	14725972
[Use of triptanes according to indications. Risk of infarct is not increased].	2004-02-12	15347059
[Recent progress in therapy for migraine headache].	2004-02-10	15007953
New drugs 04, part 1.	2004-02	14758333
The 40-mg dose of eletriptan: comparative efficacy and tolerability versus sumatriptan 100 mg.	2004-02	14748774
Neuronal expression and regulation of CGRP promoter activity following viral gene transfer into cultured trigeminal ganglia neurons.	2004-01-30	14715155
Comparative efficacy of eletriptan and zolmitriptan in the acute treatment of migraine.	2003-12	14984226
Comparative efficacy of eletriptan vs. naratriptan in the acute treatment of migraine.	2003-11	14616928
Efficacy of eletriptan in migraineurs with persistent poor response to nonsteroidal anti-inflammatory drugs.	2003-10	14511275
Tolerability and safety of eletriptan in the treatment of migraine: a comprehensive review.	2003-10	14511273
Migraine: diagnosis and management.	2003-09-27	14511196
Musing on Mathew et al.	2003-09	14562838
Encapsulated sumatriptan is not bioequivalent to commercial sumatriptan.	2003-09	14562837
Unilateral time-delayed encapsulation does not make for a fair race.	2003-09	12940818
Eletriptan issues.	2003-08-30	12945540
[Strong and sustained-acting triptan. Therewith migraine does not return soon].	2003-08-07	14524078
A cost-effectiveness analysis of eletriptan 40 and 80 mg versus sumatriptan 50 and 100 mg in the acute treatment of migraine.	2003-07-16	12859585
Cost-effectiveness of migraine treatment: a commentary.	2003-07-16	12859584
The evolving management of migraine.	2003-06	12858071
[Highly selective beginning. Associated symptoms and side effects in retrospect].	2003-05-26	14579499
[Improved pharmacokinetics. Fast tryptan with sustained response].	2003-05-26	14579498
Safety profile of the triptans.	2003-03	12904112
[Treatment of migraine: an update].	2003-01	15095723
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
Sumatriptan versus eletriptan: which is best?	2002-12	12849329

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 `Tue Apr 01 18:41:43 GMT 2025` Edited by `admin` on `Tue Apr 01 18:41:43 GMT 2025`
Record UNII	92AD31CQ59
Record Status	`Validated (UNII)`
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Name

Type

Language

ELETRIPTAN SUCCINATE

Common Name

English

1H-INDOLE, 3-((1-METHYL-2-PYRROLIDINYL)METHYL)-5-(2-(PHENYLSULFONYL)ETHYL)-, (R)-, BUTANEDIOATE (2:1)

Preferred Name

English

BUTANEDIOIC ACID, COMPD. WITH (R)-3-((1-METHYL-2-PYRROLIDINYL)METHYL)-5-(2-(PHENYLSULFONYL)ETHYL)-1H-INDOLE (1:2)

Systematic Name

English

BUTANEDIOIC ACID, COMPD. WITH 3-(((2R)-1-METHYL-2-PYRROLIDINYL)METHYL)-5-(2-(PHENYLSULFONYL)ETHYL)-1H-INDOLE (1:2)

Systematic Name

English

Code System Code Type Description

PUBCHEM

68966951

Created by admin on Tue Apr 01 18:41:43 GMT 2025 , Edited by admin on Tue Apr 01 18:41:43 GMT 2025

PRIMARY

CAS

143577-61-1

Created by admin on Tue Apr 01 18:41:43 GMT 2025 , Edited by admin on Tue Apr 01 18:41:43 GMT 2025

PRIMARY

FDA UNII

92AD31CQ59

Created by admin on Tue Apr 01 18:41:43 GMT 2025 , Edited by admin on Tue Apr 01 18:41:43 GMT 2025

PRIMARY

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					22QOO9B8KI

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