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TriptanAka: Sumatriptan, Naratriptan, Amerge, Eletriptan, Relpax, Frovatriptan, Frova, Imitrex, Rizatriptan, Maxalt, Zolmitriptan, Zomig
- Class
- Serotonin Agonists
- Indications
- Migraine Abortive Treatment
- Contraindications
- Coronary Artery Disease
- Uncontrolled Hypertension
- Basilar Artery Migraine
- Familial Hemiplegic Migraine
- Ischemic Cerebrovascular Accident
- Prinzmetal's Angina
- Pregnancy
- Concurrent Medication use (absolute contraindications)
- MAO inhibitor use
- Ergotamine use in prior 24 hours
- Controversial cohorts in whom Triptan use is thought safe
- Controlled Diabetes Mellitus
- Controlled Hypertension
- Controlled Hyperlipidemia
- Postmenopausal women
- Men over age 40 years
- Drug Interactions
- See absolute contraindications above
- Ergotamine
- MAO inhibitors
- Lithium
- Selective Serotonin Reuptake Inhibitor (SSRI)
- Risk of Serotonin Syndrome
- Propranolol with Rizatriptan
- Requires reducing Rizatriptan dose
- Dosing: General
- Screen for cardiac disease before use!
- Limit to no more than twice weekly
- Dosing: Sumatriptan (Imitrex)
- Subcutaneous Sumatriptan
- Initial: 6 mg SC
- Repeat in 12 hours prn
- Maximum: 12 mg/day
- Oral Sumatriptan
- Initial: 25 mg PO
- Repeat 25 to 100 mg PO every 2 hours prn
- Maximum: 300 mg/day
- Intranasal Sumatriptan
- Initial: 5, 10 or 20 mg intranasal
- Dose responsive (20 mg more effective)
- Repeat after 2 hours prn
- Maximum: 40 mg/day
- Safety of use in over 4 Headaches per month not known
- Dosing: Rizatriptan (Maxalt, Maxalt MLT)
- Initial: 5 to 10 mg PO (MLT form is lingual)
- Repeat dose in 2 hours
- Maximum: 30 mg in 24 hours
- Dosing: Naratriptan (Amerge)
- Initial: 1 to 2.5 mg PO
- Repeat in 4 hours
- Maximum: 5 mg in 24 hours
- Dosing: Zolmitriptan (Zomig)
- Oral
- Initial: 1.25 to 2.5 mg PO
- Repeat dose every 2 hours
- Maximum: 10 mg in 24 hours
- Intranasal
- Dose: 5 mg spray (single dose unit)
- Onset: 15 minutes (faster than oral preparations)
- Dosing: Eletriptan (Relpax)
- Initial: 20 to 40 mg PO
- May repeat dose in 2 hours
- Maximum: 40 mg/dose or 80 mg/day
- Dosing: Almotriptan (Axert)
- Initial: 6.25 to 12.5 mg PO; may repeat in 2 hours
- Maximum: 2 doses in 24 hours
- Dosing: Frovatriptan (Frova)
- Initial dosing: 2.5 mg PO; may repeat in 2 hours
- Maximum dose: 7.5 mg per day
- Adverse reactions
- Tingling, Flushing or burning sensation at injection
- Heavy chest
- Generally benign in low risk populations
- Risk of Coronary Artery Disease exacerbation
- Terrible taste with intranasal preparations
- Efficacy: Sumatriptan
- Efficacy dependent on mode of drug delivery
- Subcutaneous effective in 80% of patients
- Intranasal effective in 70% of patients
- Oral effective in 60% of patients
- Oral form does not prevent Migraine recurrence
- Rapoport (1995) Neurology 45:1505
- Efficacy
- Most effective oral agents (c/w Imitrex 100 mg PO)
- Rizatriptan (Maxalt) 10 mg PO
- Eletriptan (Relpax) 80 mg PO
- Almotriptan (Axert) 12.5 mg PO (least side effects)
- References
- Ferrari (2001) Lancet 358:1668
- References
- Jamieson (2002) Am J Med 112:138
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| 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. |
| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | Sumatriptan, SUMATRIPTAN PREPARATION, Sumatriptan product |
| Spanish | sumatriptán, sumatriptan, sumatriptano |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | rizatriptan, RIZATRIPTAN PREPARATION, Rizatriptan product |
| Spanish | rizatriptán, rizatriptan, rizatriptano |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| 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)
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| English | zolmitriptan, ZOLMITRIPTAN PREPARATION, Zolmitriptan product |
| Spanish | zolmitriptán, zolmitriptan, zolmitriptano |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | naratriptan, NARATRIPTAN PREPARATION, Naratriptan product |
| Spanish | naratriptán, naratriptan, naratriptano |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | AscoTop, Astra brand of zolmitriptan, AstraZeneca brand of zolmitriptan, Zeneca brand of zolmitriptan, Zomig, Zomigoro |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | Amerge, Glaxo Wellcome brand of naratriptan hydrochloride, GlaxoSmithKline brand of naratriptan hydrochloride, Naramig, Schwarz brand of naratriptan hydrochloride |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | frovatriptan, FROVATRIPTAN PREPARATION, Frovatriptan product |
| Spanish | frovatriptan, producto con frovatriptano |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | eletriptan, ELETRIPTAN PREPARATION |
| Spanish | eletriptán, eletriptan |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | Elan brand of frovatriptan succinate, Frova, UCB brand of frovatriptan succinate |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | Mack brand of eletriptan hydrobromide, Pfizer brand of eletriptan hydrobromide, Relpax |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Definition (MSH) | Derivatives of TRYPTAMINES that are SEROTONIN AGONISTS acting at 5-HT1 RECEPTORS. Some are used to treat MIGRAINE DISORDERS. |
| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | Triptans |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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