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Medicines > classes : Research material or [[:Category:Triptans|Triptan (5-HT1B/1D agonist)]]

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generic:
brand:
None (130) · (none, never marketed) (1) · Imitrex (oral, injectable, nasal), Tosymra (nasal spray), Onzetra Xsail (nasal powder), Zembrace SymTouch (low-dose autoinjector), Sumavel DosePro (needle-free SC) (1) · Maxalt (tablet), Maxalt-MLT (orally disintegrating tablet) (1) · O-DSMT (1) · Treximet (1)
classes: (Click arrow to add another value)
mechanism:
5-HT2A agonist (26) · Monoamine releasing agent (9) · GABAA positive allosteric modulator (8) · CB1/CB2 agonist (7) · Dopamine/norepinephrine reuptake inhibitor (5) · Potent 5-HT2A agonist (5) · LSD analogue; 5-HT2A agonist (4) · Prodrug of LSD; 5-HT2A agonist (4) · Serotonin/norepinephrine/dopamine releasing agent (3) · None (2) · Cathinone analogue; monoamine reuptake inhibitor (2) · Dopamine and norepinephrine reuptake inhibitor (2) · NMDA antagonist (2) · Prodrug of GHB (2)
uses:
None (131) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000011-QINU`"' (1) · '"`UNIQ--vote-00000013-QINU`"', '"`UNIQ--vote-00000014-QINU`"' (1) · '"`UNIQ--vote-000015D0-QINU`"' (1)
starting dose:
None (131) · 1 tablet (85/500 mg sumatriptan/naproxen) PO at migraine onset; may repeat after 2 hours if needed; maximum 2 tablets per 24 hours (1) · 5-10 mg PO at migraine onset; may repeat after 2 hours, maximum 30 mg/24 hours (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · Oral: 50-100 mg at migraine onset, may repeat in 2 hours if needed. SC: 6 mg, may repeat in 1 hour. Nasal: 5-20 mg per nostril, may repeat in 2 hours (1)
preparations:
None (131) · 85 mg sumatriptan / 500 mg naproxen sodium tablets; lower-dose 10/60 mg pediatric (Treximet pediatric) (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · Oral tablets 25, 50, 100 mg; SC injection 4, 6 mg autoinjector; needle-free SC 6 mg (Sumavel); nasal spray 5, 20 mg; nasal powder 22 mg (Onzetra Xsail); low-dose autoinjector 3 mg (Zembrace SymTouch) (1) · Tablets 5, 10 mg; ODT (Maxalt-MLT) 5, 10 mg (1)
fda max:
None (131) · 2 tablets per 24 hours; ≤4 days per month to avoid medicine-overuse headache (1) · 200 mg/day (oral); 12 mg/day (SC); 40 mg/day (nasal spray); 44 mg/day (Onzetra) (1) · 30 mg/24 hours (1) · N/A (never approved) (1)
routes:
None (131) · intranasal (1) · intranasal; rectal and IV reported. (1) · Oral (4) · subcutaneous (1) · sublingual (1)
onset:
None (131) · 10 minutes (SC); 15-30 minutes (nasal); 30-60 minutes (oral) (1) · 30 minutes for migraine relief (1) · Headache relief at 30-60 minutes (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (131) · 2-4 hours; headache recurrence rate ~20-30% within 24 hours (1) · 4-6 hours; headache recurrence is common (1) · 4-8 hours (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)
halflife:
None (131) · 2 hours'"`UNIQ--ref-00000015-QINU`"' (1) · 2-3 hours'"`UNIQ--ref-00000012-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Sumatriptan ~2.5 hours; naproxen 12-15 hours'"`UNIQ--ref-000015D1-QINU`"' (1)
bioavailability:
None (131) · Not formally characterized in humans. (1) · Sumatriptan ~15% (oral; substantial first-pass); naproxen ~95%'"`UNIQ--ref-000015D2-QINU`"' (1) · ~14% (oral; substantial first-pass); ~97% (subcutaneous); ~17% (nasal)'"`UNIQ--ref-00000016-QINU`"' (1) · ~45% (oral; substantially higher than sumatriptan's ~14%)'"`UNIQ--ref-00000013-QINU`"' (1)
pregnancy:
None (131) · Avoid. Benzodiazepines are associated with neonatal sedation, floppy-infant syndrome, and withdrawal; teratogenic signal weak but non-zero. Designer benzo with no safety data, assume worst-case. (1) · Avoid; NSAID-class restriction after 20 weeks (FDA 2020) and limited triptan pregnancy data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; pregnancy registry data have been broadly reassuring across the triptan class.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; pregnancy registry data have been broadly reassuring relative to baseline malformation rates.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (132) · [[USLegal:Prescription only|Rx-only]] in US (2) · [[USLegal:Prescription only|Rx-only]] in US. NSAID-class '''Boxed Warning''' for CV thrombotic events and GI bleeding; triptans contraindicated in coronary artery disease, peripheral vascular disease, uncontrolled hypertension, and recent ergot or MAOI use'"`UNIQ--ref-000015D3-QINU`"' (1)

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