Neurology Book

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Triptan

Aka: Triptan, Sumatriptan, Imitrex, Rizatriptan, Maxalt, Zolmitriptan, Zomig, Naratriptan, Amerge, Eletriptan, Relpax, Frovatriptan, Frova, Treximet
  1. Class
    1. Serotonin Agonists
  2. Indications
    1. Migraine Abortive Treatment
  3. Contraindications
    1. Coronary Artery Disease
    2. Uncontrolled Hypertension
    3. Basilar ArteryMigraine
    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
    4. Treximet (combination with Naproxen)
      1. Contains Sumatriptan 85 mg with Naproxen 500 mg
      2. Released as Sumatriptan becomes generically available
      3. Cheaper to purchase generic Sumatriptan (when available) and Naproxen separately
  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 45:1505-9
  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 358:1668-75
  17. References
    1. Jamieson (2002) Am J Med 112:138

Triptans (C1567966)

Definition (MSH) Derivatives of TRYPTAMINES that are SEROTONIN RECEPTOR AGONISTS acting at 5-HT1 RECEPTORS. Some are used to treat MIGRAINE DISORDERS.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D014363
French Triptans
English Triptans
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Amerge (C0594660)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C106783
English Naramig, amerge, Amerge, Glaxo Wellcome brand of naratriptan hydrochloride, GlaxoSmithKline brand of naratriptan hydrochloride, Schwarz brand of naratriptan hydrochloride
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Relpax (C1171655)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C115647
English Relpax, relpax, Mack brand of eletriptan hydrobromide, Pfizer brand of eletriptan hydrobromide
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Imitrex (C0721044)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
English Imitrex, imitrex
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Maxalt (C0721599)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C093622
English Maxalt, maxalt
Sources
Derived from the NIH UMLS (Unified Medical Language System)


frovatriptan (C0754647)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C108128
SnomedCT 370215003, 408042004, 411990007
Spanish frovatriptan (producto), frovatriptán (producto), producto con frovatriptano (producto), frovatriptán, producto con frovatriptano, frovatriptan, frovatriptan (sustancia)
English 3-methylamino-6-carboxamido-1,2,3,4-tetrahydrocarbazole, frovatriptan, frovatriptan [Chemical/Ingredient], Frovatriptan product (product), Frovatriptan product, Frovatriptan (product), Frovatriptan, Frovatriptan (substance), FROVATRIPTAN
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Sumatriptan (C0075632)

Definition (CSP) sulfonamide serotonin agonist and vasoconstrictor that acts selectively at 5HT1 receptors; frequently used in treating migraines.
Definition (MSH) A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.
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.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D018170
SnomedCT 350311006, 395892000, 322822007
English Sumatriptan, 3-(2-(Dimethylamino)ethyl)-N-methyl-1H-indole-5-methanesulfonamide, 1H-Indole-5-methanesulfonamide, 3-(2-(dimethylamino)ethyl)-N-methyl-, sumatriptan (medication), selective 5-HT receptor agonists sumatriptan, sumatriptan, SUMATRIPTAN, Sumatriptan [Chemical/Ingredient], sumatriptans, SUMAtriptan, Sumatriptan product, Sumatriptan (substance), Sumatriptan product (product), Sumatriptan product (substance)
Swedish Sumatriptan
Czech sumatriptan
Spanish Sumatriptan product, sumatriptán (producto), sumatriptán, producto (producto), sumatriptán, sumatriptán, producto, sumatriptano (sustancia), sumatriptano, Sumatriptán, Sumatriptan
Finnish Sumatriptaani
Russian SAMATRIPTAN, SUMATRIPTAN, САМАТРИПТАН, СУМАТРИПТАН
Japanese コハク酸スマトリプタン, スマトリプタン, イミグラン
Polish Sumatryptan
French Sumatriptan
German Sumatriptan
Italian Sumatriptan
Portuguese Sumatriptana
Sources
Derived from the NIH UMLS (Unified Medical Language System)


naratriptan (C0540623)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C106783
SnomedCT 363571003, 108408002
English N-methyl-3-(1-methyl-4-piperidinyl)-1H-indole-5-ethanesulfonamide, naratriptan, NARATRIPTAN, Naratriptan product, naratriptan [Chemical/Ingredient], Naratriptan, Naratriptan (product), Naratriptan (substance), Naratriptan product (substance)
Spanish naratriptano, naratriptano (producto), naratriptán (producto), naratriptano (sustancia), naratriptán (sustancia), naratriptán
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Zomig (C0594405)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C089750
English Zomig, zomig, AscoTop, Astra brand of zolmitriptan, AstraZeneca brand of zolmitriptan, Zeneca brand of zolmitriptan, Zomigoro
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Frova (C1099778)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C108128
English Frova, frova, Elan brand of frovatriptan succinate, UCB brand of frovatriptan succinate
Sources
Derived 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.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C089750
SnomedCT 363582006, 108406003
English 4-((3-(2-(dimethylamino)ethyl)-1H-indol-5-yl)methyl)-2-oxazolidinone, 2-Oxazolidinone, 4-((3-(2-(dimethylamino)ethyl)-1H-indol-5-yl)methyl)-,(S)-, zolmitriptan, Zolmitriptan product, zolmitriptan (medication), selective 5-HT receptor agonists zolmitriptan, ZOLMITRIPTAN, zolmitriptan [Chemical/Ingredient], ZOLMitriptan, Zolmitriptan, Zolmitriptan (product), Zolmitriptan (substance), Zolmitriptan product (substance)
Spanish zolmitriptano, zolmitriptano (producto), zolmitriptán (producto), zolmitriptano (sustancia), zolmitriptán (sustancia), zolmitriptán
Sources
Derived from the NIH UMLS (Unified Medical Language System)


rizatriptan (C0297635)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C093622
SnomedCT 363573000, 108411001
English N,N-dimethyl-2-(5-(1,2,4-triazol-1-ylmethyl)-1H-indole-3-yl)ethylamine, rizatriptan, Rizatriptan product, rizatriptan [Chemical/Ingredient], Rizatriptan, Rizatriptan (product), Rizatriptan (substance), Rizatriptan product (substance), RIZATRIPTAN
Spanish rizatriptán (producto), rizatriptano (producto), rizatriptano, rizatriptano (sustancia), rizatriptán (sustancia), rizatriptán
Sources
Derived from the NIH UMLS (Unified Medical Language System)


eletriptan (C0759933)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C115647
SnomedCT 395255007, 410843003
English eletriptan, eletriptan [Chemical/Ingredient], Eletriptan (product), Eletriptan, Eletriptan (substance), ELETRIPTAN
Spanish eletriptán (producto), eletriptán, eletriptán (sustancia)
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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