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TriptanAka: Sumatriptan, Naratriptan, Amerge, Eletriptan, Relpax, Frovatriptan, Frova, Imitrex, Rizatriptan, Maxalt, Zolmitriptan, Zomig

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  1. Class
    1. Serotonin Agonists
  2. Indications
    1. Migraine Abortive Treatment
  3. Contraindications
    1. Coronary Artery Disease
    2. Uncontrolled Hypertension
    3. Basilar Artery Migraine
    4. Familial Hemiplegic Migraine
    5. Ischemic Cerebrovascular Accident
    6. Prinzmetal's Angina
    7. Pregnancy
    8. Concurrent Medication use (absolute contraindications)
      1. MAO inhibitor use
      2. Ergotamine use in prior 24 hours
  4. Controversial cohorts in whom Triptan use is thought safe
    1. Controlled Diabetes Mellitus
    2. Controlled Hypertension
    3. Controlled Hyperlipidemia
    4. Postmenopausal women
    5. Men over age 40 years
  5. Drug Interactions
    1. See absolute contraindications above
      1. Ergotamine
      2. MAO inhibitors
    2. Lithium
    3. Selective Serotonin Reuptake Inhibitor (SSRI)
      1. Risk of Serotonin Syndrome
    4. Propranolol with Rizatriptan
      1. Requires reducing Rizatriptan dose
  6. Dosing: General
    1. Screen for cardiac disease before use!
    2. Limit to no more than twice weekly
  7. Dosing: Sumatriptan (Imitrex)
    1. Subcutaneous Sumatriptan
      1. Initial: 6 mg SC
      2. Repeat in 12 hours prn
      3. Maximum: 12 mg/day
    2. Oral Sumatriptan
      1. Initial: 25 mg PO
      2. Repeat 25 to 100 mg PO every 2 hours prn
      3. Maximum: 300 mg/day
    3. Intranasal Sumatriptan
      1. Initial: 5, 10 or 20 mg intranasal
        1. Dose responsive (20 mg more effective)
      2. Repeat after 2 hours prn
      3. Maximum: 40 mg/day
      4. Safety of use in over 4 Headaches per month not known
  8. Dosing: Rizatriptan (Maxalt, Maxalt MLT)
    1. Initial: 5 to 10 mg PO (MLT form is lingual)
    2. Repeat dose in 2 hours
    3. Maximum: 30 mg in 24 hours
  9. Dosing: Naratriptan (Amerge)
    1. Initial: 1 to 2.5 mg PO
    2. Repeat in 4 hours
    3. Maximum: 5 mg in 24 hours
  10. Dosing: Zolmitriptan (Zomig)
    1. Oral
      1. Initial: 1.25 to 2.5 mg PO
      2. Repeat dose every 2 hours
      3. Maximum: 10 mg in 24 hours
    2. Intranasal
      1. Dose: 5 mg spray (single dose unit)
      2. Onset: 15 minutes (faster than oral preparations)
  11. Dosing: Eletriptan (Relpax)
    1. Initial: 20 to 40 mg PO
    2. May repeat dose in 2 hours
    3. Maximum: 40 mg/dose or 80 mg/day
  12. Dosing: Almotriptan (Axert)
    1. Initial: 6.25 to 12.5 mg PO; may repeat in 2 hours
    2. Maximum: 2 doses in 24 hours
  13. Dosing: Frovatriptan (Frova)
    1. Initial dosing: 2.5 mg PO; may repeat in 2 hours
    2. Maximum dose: 7.5 mg per day
  14. Adverse reactions
    1. Tingling, Flushing or burning sensation at injection
    2. Heavy chest
      1. Generally benign in low risk populations
      2. Risk of Coronary Artery Disease exacerbation
    3. Terrible taste with intranasal preparations
  15. Efficacy: Sumatriptan
    1. Efficacy dependent on mode of drug delivery
      1. Subcutaneous effective in 80% of patients
      2. Intranasal effective in 70% of patients
      3. Oral effective in 60% of patients
    2. Oral form does not prevent Migraine recurrence
      1. Rapoport (1995) Neurology 45:1505
  16. Efficacy
    1. Most effective oral agents (c/w Imitrex 100 mg PO)
      1. Rizatriptan (Maxalt) 10 mg PO
      2. Eletriptan (Relpax) 80 mg PO
      3. Almotriptan (Axert) 12.5 mg PO (least side effects)
    2. References
      1. Ferrari (2001) Lancet 358:1668
  17. References
    1. Jamieson (2002) Am J Med 112:138

Sumatriptan (C0075632)

Definition (MSH)A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.
Definition (CSP)sulfonamide serotonin agonist and vasoconstrictor that acts selectively at 5HT1 receptors; frequently used in treating migraines.
Definition (NCI)A sulfonamide triptan with vasoconstrictor activity. Sumatriptan selectively binds to and activates serotonin 5-HT1D receptors in the central nervous system (CNS), thereby constricting cerebral blood vessels. This may lead to a relief in pain from vascular headaches. Sumatriptan may also relieve vascular headaches by decreasing the release of vasoactive neuropeptides from perivascular trigeminal axons in the dura mater during a migraine, by reducing extravasation of plasma proteins, and by decreasing the release of other mediators of inflammation from the trigeminal nerve.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishSumatriptan, SUMATRIPTAN PREPARATION, Sumatriptan product
Spanishsumatriptán, sumatriptan, sumatriptano
CreditsDerived from the NIH UMLS (Unified Medical Language System)


rizatriptan (C0297635)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
Englishrizatriptan, RIZATRIPTAN PREPARATION, Rizatriptan product
Spanishrizatriptán, rizatriptan, rizatriptano
CreditsDerived from the NIH UMLS (Unified Medical Language System)


zolmitriptan (C0528166)

Definition (NCI)A member of the triptan class agents with anti-migraine property. Zolmitriptan selectively binds to and activates serotonin (5-HT) 1B expressed in intracranial arteries and 5_HT 1D receptors located on peripheral trigeminal sensory nerve terminals in the meninges and central terminals in brain stem sensory nuclei. Receptor binding results in constriction of cranial vessels, reduction of the vessel pulsation and inhibition of nociceptive transmission, thereby providing relief of migraine headaches. Zolmitriptan may also relief migraine headaches by inhibition pro-inflammatory neuropeptide release.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
Englishzolmitriptan, ZOLMITRIPTAN PREPARATION, Zolmitriptan product
Spanishzolmitriptán, zolmitriptan, zolmitriptano
CreditsDerived from the NIH UMLS (Unified Medical Language System)


naratriptan (C0540623)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
Englishnaratriptan, NARATRIPTAN PREPARATION, Naratriptan product
Spanishnaratriptán, naratriptan, naratriptano
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Zomig (C0594405)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishAscoTop, Astra brand of zolmitriptan, AstraZeneca brand of zolmitriptan, Zeneca brand of zolmitriptan, Zomig, Zomigoro
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Amerge (C0594660)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishAmerge, Glaxo Wellcome brand of naratriptan hydrochloride, GlaxoSmithKline brand of naratriptan hydrochloride, Naramig, Schwarz brand of naratriptan hydrochloride
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Imitrex (C0721044)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishImitrex
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Maxalt (C0721599)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishMaxalt
CreditsDerived from the NIH UMLS (Unified Medical Language System)


frovatriptan (C0754647)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
Englishfrovatriptan, FROVATRIPTAN PREPARATION, Frovatriptan product
Spanishfrovatriptan, producto con frovatriptano
CreditsDerived from the NIH UMLS (Unified Medical Language System)


eletriptan (C0759933)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
Englisheletriptan, ELETRIPTAN PREPARATION
Spanisheletriptán, eletriptan
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Frova (C1099778)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishElan brand of frovatriptan succinate, Frova, UCB brand of frovatriptan succinate
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Relpax (C1171655)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishMack brand of eletriptan hydrobromide, Pfizer brand of eletriptan hydrobromide, Relpax
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Triptans (C1567966)

Definition (MSH)Derivatives of TRYPTAMINES that are SEROTONIN AGONISTS acting at 5-HT1 RECEPTORS. Some are used to treat MIGRAINE DISORDERS.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishTriptans
CreditsDerived from the NIH UMLS (Unified Medical Language System)



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