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Medicines > classes : Research material or Tryptamine or [[:Category:Mast_cell_stabilizers|Mast cell stabilizer]]

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generic:
brand:
None (132) · (none, never marketed) (1) · Astelin, Astepro (intranasal); Optivar (ophthalmic); with fluticasone as Dymista (1) · O-DSMT (1) · Patanol, Pataday (ophthalmic, now OTC), Patanase (intranasal) (1) · Zaditor, Alaway (ophthalmic, OTC); Zaditen (systemic, outside US) (1)
classes: (Click arrow to add another value)
mechanism:
5-HT2A agonist (27) · 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) · Cathinone analogue; monoamine reuptake inhibitor (2) · Dopamine and norepinephrine reuptake inhibitor (2) · NMDA antagonist (2) · Prodrug of GHB (2)
uses:
None (133) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-000011D7-QINU`"', '"`UNIQ--vote-000011D8-QINU`"' (1) · '"`UNIQ--vote-00001286-QINU`"' (1) · '"`UNIQ--vote-000013B3-QINU`"', '"`UNIQ--vote-000013B4-QINU`"', '"`UNIQ--vote-000013B5-QINU`"' (1)
starting dose:
None (133) · Intranasal 0.1% or 0.15%: 1-2 sprays/nostril BID; ophthalmic 0.05%: 1 drop in each eye BID (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · Ophthalmic 1 drop in each eye every 8-12 hours (1) · Ophthalmic Pataday 0.7%: 1 drop in each eye once daily (24-hour formulation); Patanol 0.1% BID; intranasal Patanase 2 sprays/nostril BID (1)
preparations:
None (133) · 0.025%, 0.035% ophthalmic solutions (1) · 0.1% (Patanol), 0.2% (Pataday once-daily original), 0.7% (Pataday 24-hour) ophthalmic solutions; 0.6% nasal spray (1) · 0.1%, 0.15% intranasal spray; 0.05% ophthalmic solution; combination Dymista (azelastine 0.137 mg + fluticasone 50 mcg/spray) (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
None (133) · 1 drop per eye q8-12h (1) · 2 sprays/nostril BID (1) · N/A (never approved) (1) · Once daily (Pataday 0.7%); BID (other ophthalmic) (1)
routes:
None (133) · Intranasal (2) · intranasal; rectal and IV reported. (1) · Oral (1) · sublingual (1) · topical ophthalmic (3)
onset:
None (133) · 15 minutes (1) · Symptom relief within 30-60 minutes (1) · Within minutes (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (133) · 12 hours (1) · 24 hours (0.7% formulation); 8-12 hours (lower-strength) (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · 8-12 hours (1)
halflife:
None (133) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Not meaningfully described for ophthalmic use'"`UNIQ--ref-00001287-QINU`"' (1) · ~22 hours; longer 54 hours (desmethylazelastine, active metabolite)'"`UNIQ--ref-000013B6-QINU`"' (1) · ~3 hours (systemic, when measurable; topical action dominates)'"`UNIQ--ref-000011D9-QINU`"' (1)
bioavailability:
None (133) · Intranasal ~40% systemic; ophthalmic minimal'"`UNIQ--ref-000013B7-QINU`"' (1) · Not formally characterized in humans. (1) · Topical with minimal systemic absorption'"`UNIQ--ref-000011DA-QINU`"' (1) · Topical with minimal systemic absorption'"`UNIQ--ref-00001288-QINU`"' (1)
pregnancy:
None (133) · 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) · Generally considered safe (minimal systemic exposure).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe; minimal systemic exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; second-line to intranasal corticosteroids or PO loratadine/cetirizine.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (134) · OTC (Astepro 0.15%) and [[USLegal:Prescription only|Rx-only]] (other intranasal, ophthalmic, Dymista) in US (1) · OTC (Pataday ophthalmic) and [[USLegal:Prescription only|Rx-only]] (Patanase intranasal) in US (1) · OTC in US (1)

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