3. Triptans Flashcards
MOA of triptans
selective agonists for the 5-HT1 receptor; causes vasoconstriction of cranial blood vessels, inhibit neuropeptide release and decrease pain transmission
naratriptan (brand, dosing)
available as a tablet
Amerge
Initial: 1-2.5 mg, can repeat x1 after 4 hrs (max 5 mg/day)
almotriptan (brand, dosing)
available as a tablet
Axert
Initial: 6.25-12.5 mg, can repeat x1 after 2 hrs (max 25 mg/day)
frovatriptan (brand, dosing)
available as a tablet
Frova
Initial: 2.5 mg, can repeat x1 after 2 hrs (max 7.5 mg/day)
SUMAtriptan (brand names, formulations)
available as a tablet, SC injection, needle-free SC delivery, nasal spray, transdermal patch
Imitrex: tablet, nasal spray
Imitrex STATdose: SC injection
Alsuma: SC injection
Sumavel DosePro: needle-free SC delivery
Zecuity: iontophoretic transdermal patch
Imitrex dosing for tablet
25, 50, 100 mg, can repeat x1 after 2 hrs (max 200 mg/day)
Imitrex dosing for nasal spray
5, 10, 20 mg in one nostril, can repeat x1 after 2 hrs (max 40 mg/day)
Imitrex and Alsuma dosing for SC injection
4, 6 mg, can repeat x1 after 1 hr (max 12 mg/day)
inject on thigh or arm; hold against skin and press blue button, hold for 5 seconds
Zecuity dosing for iontophoretic transdermal patch
apply 1 patch, may apply 2nd patch after 2 hrs
runs on lithium batteries, will need to pull tabs to expose batteries and push button to activate drug release
rizatriptan (brand, dosing)
available as a tablet, ODT
Maxalt, Maxalt MLT
Initial 5-10 mg, can repeat x1 after 2 hrs
ODT: 5 mg, no water needed
(max 30 mg/day)
eletriptan (brand, dosing)
available as a tablet
Relpax
initial: 20-40 mg, can repeat x1 after 2 hrs (max 80 mg/day)
ZOLMItriptan (brand, dosing)
available as a tablet, ODT, nasal spray
Zomig, Zomig-ZMT
PO: 1.25-5 mg, can repeat x1 after 2 hrs
Intranasal: 5 mg, can repeat x1 after 2 hrs
(max 10 mg/day)
Triptan CI: CV related (4)
–cerebrovascular disease (stroke/TIA)
–uncontrolled HTN
–ischemic heart disease
–peripheral vascular disease
Triptan CI: hx of _____ or ______ migraine
hemiplegic
basilar
Triptan CI: severe _______ impairment
hepatic
Triptan CI: which 3 are CI with MAO-Is?
–sumatriptan
–rizatriptan
–zolmitriptan
Triptan CI: which one is CI with strong CYP3A4 inhibitors?
eletriptan
Triptan SEs
somnolence, nausea, paresthesias (tingling/numbness), throat/neck pressure, dizziness, hot/cold sensations, chest pain/tightness
triptan sensations (pressure in the chest or heaviness or pressure in the neck region) that usually dissipate after administration - may feel like a heart attack
What dosage forms are useful if nausea present?
ODT, nasal spray, injections
Which dosage forms work faster?
nasal sprays, injections
Imitrex and Zomig nasal sprays contain _____ dose(s) and [should/should not] be primed
one
should not
Triptans approved for children and adolescents ≥12 yo (2)
–almotriptan tablets
–zolmitriptan nasal spray
Triptan approved for children and adolescents 6-17 yo
rizatriptan
SUMAtriptan + naproxen (brand, dosing)
Treximet
85-500 mg
1 tab, may repeat x1 after 2 hrs (max 2 tab/day)
Treximet needs to be kept in original container (contains _______)
dessicant
The longest-acting triptan is _______ and ______. Longer acting = ______ _______. Choose if HA recurs after dosing or lasts a long time.
–frovatriptan (t1/2=26hrs)
–naratriptan
–slower onset
Triptans with a shorter half-life have a faster onset. (5)
–almotriptan –eletriptan –rizatriptan –sumatriptan –zolmitriptan
Triptan DDI: with SSRIs and SNRIs
some risk for serotonin syndrome, however keep in mind triptans are PRN and risk is low if taken sporadically
(SS sx: restlessness, sweating, poor coordination, confusion, hallucinations)
Migraine prophylaxis should be considered if… (4)
–pt requests it
–acute tx is used ≥2 days/wk or ≥3 times/month
–migraines decrease quality of life
–acute tx is ineffective or contraindicated
