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{{Eletriptan}}
{{drugbox
{{drugbox
| IUPAC_name = 3-[(1-methylpyrrolidin-2-yl) methyl]-5- (2-phenylsulfonylethyl)- 1H-indole
| IUPAC_name = 3-[(1-methylpyrrolidin-2-yl) methyl]-5- (2-phenylsulfonylethyl)- 1H-indole
Line 5: Line 6:
| ATC_prefix = N02
| ATC_prefix = N02
| ATC_suffix = CC06
| ATC_suffix = CC06
| ATC_supplemental =  
| ATC_supplemental =
| PubChem = 77993
| PubChem = 77993
| DrugBank = APRD00945
| DrugBank = APRD00945
Line 11: Line 12:
| molecular_weight = 382.52 g/mol
| molecular_weight = 382.52 g/mol
| bioavailability = 50%
| bioavailability = 50%
| protein_bound =  
| protein_bound =
| metabolism = MAO
| metabolism = MAO
| elimination_half-life = 4 hours
| elimination_half-life = 4 hours
| pregnancy_category =  
| pregnancy_category =
| legal_status = prescription
| legal_status = prescription
| routes_of_administration = oral
| routes_of_administration = oral
}}
}}
__NOTOC__
{{CMG}}
'''''For patient information about Eletriptan, click [[Eletriptan (patient information)|here]].'''''
{{SB}} RELPAX
==Overview==
'''Eletriptan Hydrobromide''' is the active metabolite of '''Relpax®,''' the only FDA-approved eletriptan product currently on the market in the U.S. Eletriptan is a second generation [[triptan]] [[medication|drug]] developed by [[Pfizer Inc]] for the treatment of [[migraine]] [[headache]]s.
'''Eletriptan Hydrobromide''' is the active metabolite of '''Relpax®,''' the only FDA-approved eletriptan product currently on the market in the U.S. Eletriptan is a second generation [[triptan]] [[medication|drug]] developed by [[Pfizer Inc]] for the treatment of [[migraine]] [[headache]]s.
==Category==
Antimigraine Drugs, Triptans
==FDA Package Insert==
====RELPAX (eletriptan hydrobromide) tablet, film coated====
'''  [[Eletriptan indications and usage|Indications and Usage]]'''
'''| [[Eletriptan dosage and administration|Dosage and Administration]]'''
'''| [[Eletriptan dosage forms and strengths|Dosage Forms and Strengths]]'''
'''| [[Eletriptan contraindications|Contraindications]]'''
'''| [[Eletriptan warnings and precautions|Warnings and Precautions]]'''
'''| [[Eletriptan adverse reactions|Adverse Reactions]]'''
'''| [[Eletriptan drug interactions|Drug Interactions]]'''
'''| [[Eletriptan use in specific populations|Use in Specific Populations]]'''
'''| [[Eletriptan overdosage|Overdosage]]'''
'''| [[Eletriptan description|Description]]'''
'''| [[Eletriptan clinical pharmacology|Clinical Pharmacology]]'''
'''| [[Eletriptan nonclinical toxicology|Nonclinical Toxicology]]'''
'''| [[Eletriptan clinical studies|Clinical Studies]]'''
'''| [[Eletriptan how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[Eletriptan patient counseling information|Patient Counseling Information]]'''
'''| [[Eletriptan labels and packages|Labels and Packages]]'''


==Approval and availability==
==Approval and availability==
Relpax was approved by the U.S. [[FDA]] on December 26, 2002 for the acute treatment of migraine with or without aura in adults. It is available only by [[Medical prescription|prescription]] in the [[United States]] and [[Canada]]. It is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine.  It is available in 20 mg and 40 mg strengths.
Relpax was approved by the U.S. [[FDA]] on December 26, 2002 for the acute treatment of migraine with or without aura in adults. It is available only by [[Medical prescription|prescription]] in the [[United States]] and [[Canada]]. It is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine.  It is available in 20 mg and 40 mg strengths.


Relpax tablets for oral administration contain 24.2 mg or 48.5 mg of eletriptan hydrobromide equivalent to 20 mg or 40 mg of eletriptan, respectively.  Each tablet also contains the inactive ingredients microcrystalline cellulose NF, lactose NF, croscarmellose sodium NF, magnesium stearate NF, titanium dioxide USP, hydroxypropyl methylcellulose NF, triacetin USP and FD&C Yellow No. 6 aluminum lake.
Relpax tablets for oral administration contain 24.2 mg or 48.5 mg of eletriptan hydrobromide equivalent to 20 mg or 40 mg of eletriptan, respectively.  Each tablet also contains the inactive ingredients microcrystalline cellulose NF, lactose NF, croscarmellose sodium NF, magnesium stearate NF, titanium dioxide USP, hydroxypropyl methylcellulose NF, triacetin USP and FD&C Yellow No. 6 aluminum lake.


==Mode of action==
==Mechanism of Action==
Treatment with Relpax reduces swelling of blood vessels surrounding the brain. This swelling is associated with the headache pain of a migraine attack. Relpax blocks the release of  
 
substances from nerve endings that cause more pain and other symptoms like nausea, and sensitivity to light and sound.  It is thought that these actions contribute to relief of symptoms by Relpax.
Treatment with Relpax reduces swelling of blood vessels surrounding the brain. This swelling is associated with the headache pain of a migraine attack. Relpax blocks the release of substances from nerve endings that cause more pain and other symptoms like nausea, and sensitivity to light and sound.  It is thought that these actions contribute to relief of symptoms by Relpax.


Eletriptan is a serotonin agonist.  Specifically, it is a selective 5-hydroxytryptamine 1B/1D ([[5-HT1B]]/1D) receptor [[agonist]].
Eletriptan is a serotonin agonist.  Specifically, it is a selective 5-hydroxytryptamine 1B/1D ([[5-HT1B]]/1D) receptor [[agonist]].


Eletriptan binds with high affinity to 5-HT1B, [[5-HT1D]] and [[5-HT1F]] receptors, has modest affinity for [[5-HT1A]], [[5-HT1E]], [[5-HT2B]] and [[5-HT7]] receptors, and little or no affinity for [[5-HT2A]], [[5-HT2C]], [[5-HT3]], [[5-HT4]], [[5-HT5A]] and [[5-HT6]] receptors.  Eletriptan has no significant affinity or pharmacological activity at adrenergic alpha1, alpha2, or beta; dopaminergic D1 or D2; muscarinic; or opioid receptors.  
Eletriptan binds with high affinity to 5-HT1B, [[5-HT1D]] and [[5-HT1F]] receptors, has modest affinity for [[5-HT1A]], [[5-HT1E]], [[5-HT2B]] and [[5-HT7]] receptors, and little or no affinity for [[5-HT2A]], [[5-HT2C]], [[5-HT3]], [[5-HT4]], [[5-HT5A]] and [[5-HT6]] receptors.  Eletriptan has no significant affinity or pharmacological activity at adrenergic alpha1, alpha2, or beta; dopaminergic D1 or D2; muscarinic; or opioid receptors.


Two theories have been proposed to explain the efficacy of 5-HT receptor agonists in migraine.  One theory suggests that activation of 5-HT1 receptors located on intracranial blood vessels, including those on the arteriovenous anastomoses, leads to vasoconstriction, which is correlated with the relief of migraine headache.  The other hypothesis suggests that activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.  
Two theories have been proposed to explain the efficacy of 5-HT receptor agonists in migraine.  One theory suggests that activation of 5-HT1 receptors located on intracranial blood vessels, including those on the arteriovenous anastomoses, leads to vasoconstriction, which is correlated with the relief of migraine headache.  The other hypothesis suggests that activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.


Chemical name: (R)-5-[2-(Fenylsulfonyl)etyl]-3-[(1-metyl-2-pyrrolidinyl)metyl]-1H-indol
==References==


==External links==
{{Reflist|2}}
*[http://www.relpax.com Relpax] Official homepage by Pfizer
*[http://www.duchs.com/information/Relpax Relpax Information] Fact Sheet
*[http://www.fda.gov/cder/foi/label/2002/21016_relpax_lbl.pdf] FDA Approved Label (Full Prescribing Information)
{{triptans}}


{{Triptans}}
[[Category:Cardiovascular Drugs]]
[[Category:Drugs]]
[[Category:Triptans]]
[[Category:Triptans]]
[[de:Eletriptan]]
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Revision as of 07:32, 10 February 2014

Eletriptan
RELPAX® FDA Package Insert
Indications and Usage
Dosage and Administration
Dosage Forms and Strengths
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
Nonclinical Toxicology
Clinical Studies
How Supplied/Storage and Handling
Patient Counseling Information
Labels and Packages
Clinical Trials on Eletriptan
ClinicalTrials.gov
Eletriptan
File:Eletriptan structure.svg
Clinical data
Routes of
administration		oral
ATC code
Legal status
Legal status
  • prescription
Pharmacokinetic data
Bioavailability50%
MetabolismMAO
Elimination half-life4 hours
Identifiers
CAS Number
PubChem CID
DrugBank
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC22H26N2O2S
Molar mass382.52 g/mol

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

For patient information about Eletriptan, click here.

Synonyms / Brand Names: RELPAX

Overview

Eletriptan Hydrobromide is the active metabolite of Relpax®, the only FDA-approved eletriptan product currently on the market in the U.S. Eletriptan is a second generation triptan drug developed by Pfizer Inc for the treatment of migraine headaches.

Category

Antimigraine Drugs, Triptans

FDA Package Insert

RELPAX (eletriptan hydrobromide) tablet, film coated

Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

Approval and availability

Relpax was approved by the U.S. FDA on December 26, 2002 for the acute treatment of migraine with or without aura in adults. It is available only by prescription in the United States and Canada. It is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. It is available in 20 mg and 40 mg strengths.

Relpax tablets for oral administration contain 24.2 mg or 48.5 mg of eletriptan hydrobromide equivalent to 20 mg or 40 mg of eletriptan, respectively. Each tablet also contains the inactive ingredients microcrystalline cellulose NF, lactose NF, croscarmellose sodium NF, magnesium stearate NF, titanium dioxide USP, hydroxypropyl methylcellulose NF, triacetin USP and FD&C Yellow No. 6 aluminum lake.

Mechanism of Action

Treatment with Relpax reduces swelling of blood vessels surrounding the brain. This swelling is associated with the headache pain of a migraine attack. Relpax blocks the release of substances from nerve endings that cause more pain and other symptoms like nausea, and sensitivity to light and sound. It is thought that these actions contribute to relief of symptoms by Relpax.

Eletriptan is a serotonin agonist. Specifically, it is a selective 5-hydroxytryptamine 1B/1D (5-HT1B/1D) receptor agonist.

Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors, and little or no affinity for 5-HT2A, 5-HT2C, 5-HT3, 5-HT4, 5-HT5A and 5-HT6 receptors. Eletriptan has no significant affinity or pharmacological activity at adrenergic alpha1, alpha2, or beta; dopaminergic D1 or D2; muscarinic; or opioid receptors.

Two theories have been proposed to explain the efficacy of 5-HT receptor agonists in migraine. One theory suggests that activation of 5-HT1 receptors located on intracranial blood vessels, including those on the arteriovenous anastomoses, leads to vasoconstriction, which is correlated with the relief of migraine headache. The other hypothesis suggests that activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.

References

Template:Triptans

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