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Medicines > classes : Research material or Tryptamine or [[:Category:Bronchodilators|Bronchodilator]]

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generic:
brand:
None (132) · (none, never marketed) (1) · Atrovent (inhaler, intranasal); also generic (1) · O-DSMT (1) · Spiriva, Spiriva Respimat (1) · Ventolin, ProAir, Proventil, AccuNeb (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) · None (2) · 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-00000095-QINU`"', '"`UNIQ--vote-00000096-QINU`"', '"`UNIQ--vote-00000097-QINU`"', '"`UNIQ--vote-00000098-QINU`"' (1) · '"`UNIQ--vote-000009BE-QINU`"', '"`UNIQ--vote-000009BF-QINU`"' (1) · '"`UNIQ--vote-00000F78-QINU`"', '"`UNIQ--vote-00000F79-QINU`"', '"`UNIQ--vote-00000F7A-QINU`"' (1)
starting dose:
None (133) · 18 mcg DPI once daily (HandiHaler); 2.5 mcg per actuation × 2 inhalations once daily (Respimat) (1) · MDI 90 mcg/puff, 2 puffs q4-6h prn; nebulized 2.5 mg in 3 mL saline q4-6h (1) · Nebulized 500 mcg q6-8h (or with albuterol as DuoNeb); MDI 17 mcg/puff, 2 puffs QID; nasal 0.03% or 0.06% spray BID-TID (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
None (133) · 18 mcg HandiHaler capsules; 2.5 mcg/actuation Respimat solution inhaler (1.25 mcg/actuation for asthma indication) (1) · Atrovent HFA 17 mcg/actuation MDI; 500 mcg/2.5 mL nebulizer solution; 0.03% and 0.06% intranasal sprays; with albuterol as DuoNeb / Combivent Respimat (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · MDI 90 mcg/puff; nebulizer solution 0.083% (2.5 mg/3 mL), 0.5%, 0.021%, 0.042%; syrup 2 mg/5 mL; 2 mg, 4 mg tablets; 4 mg, 8 mg ER (1)
fda max:
None (133) · 12 inhalations/d (rescue); higher for severe exacerbation under monitoring (1) · 12 puffs MDI/d typical; nebulized 2000 mcg/d (1) · N/A (never approved) (1) · One dose per day (1)
routes:
None (133) · Inhaled (DPI (1) · Inhaled (MDI (2) · intranasal (1) · intranasal; rectal and IV reported. (1) · nebulized) (2) · Oral (2) · soft-mist inhaler) (1) · sublingual (1)
onset:
None (133) · Bronchodilation 15-30 minutes (1) · Bronchodilation 30 minutes; steady-state at 1-2 weeks (1) · Inhaled: 5-15 minutes; PO: 30 minutes (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (133) · 24 hours (long receptor dissociation half-life from M3) (1) · 4-6 hours (2) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)
halflife:
None (133) · 4-6 hours (inhaled and PO)'"`UNIQ--ref-00000099-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~2 hours (plasma; minimal relevance — local-action drug)'"`UNIQ--ref-00000F7B-QINU`"' (1) · ~25-44 hours plasma; receptor kinetics drive the once-daily duration'"`UNIQ--ref-000009C0-QINU`"' (1)
bioavailability:
None (133) · Inhaled lung deposition with minimal systemic absorption (the basis of the favorable safety profile vs systemic antimuscarinics)'"`UNIQ--ref-00000F7C-QINU`"' (1) · Inhaled lung deposition ~20%; systemic absorption from lung ~33%; oral component negligible'"`UNIQ--ref-000009C1-QINU`"' (1) · Not formally characterized in humans. (1) · ~10% inhaled reaches systemic circulation; ~50% PO'"`UNIQ--ref-0000009A-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) · Limited data; generally considered acceptable when needed.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; LABA/LAMA strategies in pregnancy generally favor agents with the most reassuring data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Preferred SABA in pregnancy; benefits of asthma control outweigh limited risks.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (134) · [[USLegal:Prescription only|Rx-only]] in US (3)

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