II. Indications: General
- Migraine Abortive Treatment
- Cluster Headache
- Controversial cohorts in whom Triptan use is now thought safe (Cardiovascular Risk Factors)
- Controlled Diabetes Mellitus
- Controlled Hypertension
- Controlled Hyperlipidemia
- Postmenopausal women
- Men over age 40 years
III. Contraindications
- Coronary Artery Disease
- Prinzmetal's Angina
- Uncontrolled Hypertension
- Basilar Artery Migraine
- Familial Hemiplegic Migraine
- Ischemic Cerebrovascular Accident
- Pregnancy
- Concurrent Medication use (absolute contraindications)
- MAO Inhibitor use
- Ergotamine use in prior 24 hours
IV. Mechanism
- Serotonergic 5-HT1 receptor Agonists
- Inhibits sensory dural nerve fiber neuropeptide release
- Intracranial extracerebral artery Vasoconstriction
- Mediated by Triptan direct effect on cerebrovascular Smooth Muscle
V. Dosing: General
- Screen for cardiovascular disease before use!
- Limit to no more than twice weekly
VI. Dosing: Sumatriptan (Imitrex)
- Subcutaneous Sumatriptan
- Initial: 6 mg SC
- Repeat in 12 hours prn
- Maximum: 12 mg/day
- Even generic dosing approaches $100/dose
- Oral Sumatriptan
- Dose 25 to 100 mg orally every 2 hours prn
- Start at max single dose, 100 mg orally for best efficacy in young adult without contraindications
- Maximum: 300 mg/day
- Generic dosing may be as low as $3/dose
- Dose 25 to 100 mg orally every 2 hours prn
- 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
- Initial: 5, 10 or 20 mg intranasal
-
Treximet (combination with Naproxen)
- Contains Sumatriptan 85 mg with Naproxen 500 mg
- Released as Sumatriptan becomes generically available
- Cheaper to purchase generic Sumatriptan (when available) and Naproxen separately
- Other Sumatriptan formulations
- Zecurity patch
- Removed from market 2016 due to serious adverse effects including burns
- http://www.fda.gov/Drugs/DrugSafety/ucm504588.htm
- Zecurity patch
VII. Dosing: Rizatriptan (Maxalt, Maxalt MLT)
- Initial: 5 to 10 mg orally (MLT form is lingual)
- Start at max single dose, 10 mg orally for best efficacy in young adult without contraindications
- Repeat dose in 2 hours
- Maximum: 30 mg in 24 hours
VIII. Dosing: Naratriptan (Amerge)
- Initial: 1 to 2.5 mg orally
- Repeat in 4 hours
- Maximum: 5 mg in 24 hours
- Generic options available, but more expensive than Sumatriptan, Rizatriptan
- Consider for longer lasting Migraines (but have delayed onset)
IX. Dosing: Zolmitriptan (Zomig)
- Oral
- Initial: 1.25 to 2.5 mg orally
- 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)
X. Dosing: Eletriptan (Relpax)
- Initial: 20 to 40 mg orally
- May repeat dose in 2 hours
- Maximum: 40 mg/dose or 80 mg/day
XI. Dosing: Almotriptan (Axert)
- Initial: 6.25 to 12.5 mg orally; may repeat in 2 hours
- Maximum: 2 doses in 24 hours
XII. Dosing: Frovatriptan (Frova)
- Initial dosing: 2.5 mg orally; may repeat in 2 hours
- Maximum dose: 7.5 mg per day
- Consider for longer lasting Migraines (but have delayed onset)
XIII. Adverse Effects
- See Triptan Overdose
- Vasospasm
- Generally benign in low risk populations
- Avoid in Coronary Artery Disease, Cerebrovascular Disease, Peripheral Arterial Disease
- Also avoid in hemiplegic Migraine or basilar Migraine
-
Medication Overuse Headaches
- Highest risk with >10 doses per month
- Limit to two doses weekly
- Injection (e.g. Sumatriptan)
- Intranasal preparations
- Dysgeusia (Terrible taste)
XIV. Safety
- Unknown safety in Lactation
- Pregnancy Category C (most Triptans, but generally avoided in pregnancy)
- See Migraine Medications in Pregnancy
- Not recommended for routine use in pregnancy
- Consult obstetrics before use
- May be considered if Migraines are uncontrolled, debilitating
- If used, Sumatriptan has the longest safety data
- Adverse effects in pregnancy
- Avoid in first trimester (fetal malformations and adverse pregnancy outcomes)
- Risk of uterine atony and peripartum Hemorrhage (but may be considered in debilitating Headache)
- Associated with hyperactivity and emotionality at age 3 in exposed children (AHRQ)
- References
XV. Drug Interactions
- See absolute contraindications above
- Lithium
-
Selective Serotonin Reuptake Inhibitor (SSRI)
- Risk of Serotonin Syndrome when combined with SSRI, SNRI or MAO Inhibitors
-
Propranolol with Rizatriptan
- Requires reducing Rizatriptan dose
XVI. Efficacy: General
- Most effective oral agents (compared with Imitrex 100 mg PO)
- Rizatriptan (Maxalt) 10 mg orally
- Eletriptan (Relpax) 80 mg orally
- Almotriptan (Axert) 12.5 mg orally (least side effects)
- References
XVII. 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
XVIII. Management: Overdose or Toxicity
- See Triptan Overdose
XIX. Resources
- Triptans (StatPearls)
- Where do Triptans act in the treatment of Migraine? (PMC)
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Definition (MSH) | Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT1 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT1 receptor subtypes. |
Concepts | Pharmacologic Substance (T121) |
MSH | D058825 |
SnomedCT | 108405004, 363560004 |
English | Serotonin 5-HT1 receptor agonist (substance), Serotonin 5-HT1 receptor agonist product (product), Serotonin 5-HT1 receptor agonist product (substance), Serotonin 5-HT1 receptor agonist product, Serotonin 5-HT1 receptor agonist, Serotonin 5-HT<sub>1</sub> receptor agonist (substance), Serotonin 5-HT<sub>1</sub> receptor agonist product (product), Serotonin 5-HT<sub>1</sub> receptor agonist product (substance), Serotonin 5-HT<sub>1</sub> receptor agonist product, Serotonin 5-HT<sub>1</sub> receptor agonist, Serotonin 5 HT1 Receptor Agonists, 5 HT1 Agonist, Agonists, 5-HT1, 5 HT1 AGON, 5 HT1 AG, 5-HT1 Agonists, 5-HT1 Agonist, Agonist, 5-HT1, Serotonin 5-HT1 Receptor Agonists, 5 HT1 Agonists, Serotonin 5-HT>1< receptor agonist (substance), Serotonin 5-HT>1< receptor agonist product (product), Serotonin 5-HT>1< receptor agonist product, Serotonin 5-HT>1< receptor agonist, Serotonin 5-HT>1< receptor agonist product (substance) |
Spanish | agonista del receptor de serotonina 5-HT<sub>1</sub> (sustancia), agonista del receptor de serotonina 5-HT<sub>1</sub>, agonista del receptor de serotonina 5-HT1 (sustancia), agonista del receptor de serotonina 5-HT1, Agonistas del Receptor de Serotonina 5-HT1, Agonistas de 5-HT1, agonista del receptor de serotonina 5-HT>1< (sustancia), agonista del receptor de serotonina 5-HT>1<, agonista del receptor serotoninérgico 5 - HT1, producto (producto), agonista del receptor serotoninérgico 5 - HT1, producto |
French | Agonistes 5-HT1, Agonistes des récepteurs 5-HT1 de la sérotonine |
German | 5-HT1-Agonisten, Serotonin-5-HT1-Rezeptor-Agonisten, Serotonin-5-HT1-Rezeptoragonisten, 5-HT1-Agonist |
Czech | 5-HT1 agonisté, serotoninové receptory 5-HT1 - agonisté |
Italian | Agonisti 5-HT1, Agonisti della serotonina 5-HT1, Agonista 5-HT1 |
Russian | СЕРОТОНИНА 5-HT1 РЕЦЕПТОРОВ АГОНИСТЫ, SEROTONINA 5-HT1 RETSEPTOROV AGONISTY |
Portuguese | Agonistas do Receptor 5-HT1 de Serotonina, Agonista de 5-HT1, Agonista 5-HT1 |
Polish | Agoniści receptora serotoninowego 5-HT1 |
Ontology: 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 |
Czech | triptany |
Norwegian | Triptaner |
English | Triptans |
Ontology: selective 5-HT receptor agonists (C2224138)
Concepts | Pharmacologic Substance (T121) |
English | selective 5-HT receptor agonists, selective 5-HT receptor agonists (medication) |