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Medicines > classes : Research material or Tryptamine or [[:Category:Antimuscarinics|Antimuscarinic]]

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generic:
brand:
None (132) · (none, never marketed) (1) · Atrovent (inhaler, intranasal); also generic (1) · Bentyl (1) · Ditropan, Ditropan XL, Oxytrol (transdermal), Gelnique (gel) (1) · O-DSMT (1) · Spiriva, Spiriva Respimat (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) · None (4) · 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-000006DE-QINU`"', '"`UNIQ--vote-000006DF-QINU`"', '"`UNIQ--vote-000006E0-QINU`"' (1) · '"`UNIQ--vote-000009BE-QINU`"', '"`UNIQ--vote-000009BF-QINU`"' (1) · '"`UNIQ--vote-00000B23-QINU`"', '"`UNIQ--vote-00000B24-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) · 20 mg PO QID (start 10 mg and titrate); IM 20 mg q6h short-term (1) · IR 5 mg PO BID-TID; ER 5-10 mg PO daily, titrate; transdermal patch 3.9 mg/d twice weekly (OTC) (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) · 10, 20 mg tablets/capsules; 10 mg/5 mL syrup; 10 mg/mL IM injection (1) · 18 mcg HandiHaler capsules; 2.5 mcg/actuation Respimat solution inhaler (1.25 mcg/actuation for asthma indication) (1) · 5 mg IR tablets; 5, 10, 15 mg ER tablets; 5 mg/5 mL syrup; 3.9 mg/24 h transdermal patch (Oxytrol); 10% topical gel (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)
fda max:
None (133) · 12 puffs MDI/d typical; nebulized 2000 mcg/d (1) · 160 mg/d (rarely tolerated due to anticholinergic effects) (1) · 30 mg/d (XL) typical (1) · N/A (never approved) (1) · One dose per day (1)
routes:
None (133) · IM (not for IV) (1) · Inhaled (DPI (1) · Inhaled (MDI (1) · intranasal (1) · intranasal; rectal and IV reported. (1) · intravesical (1) · nebulized) (1) · Oral (3) · soft-mist inhaler) (1) · sublingual (1) · topical gel (1) · transdermal (1)
onset:
None (133) · 1-2 hours PO (1) · 30-60 minutes (PO) (1) · Bronchodilation 15-30 minutes (1) · Bronchodilation 30 minutes; steady-state at 1-2 weeks (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (133) · 24 hours (long receptor dissociation half-life from M3) (1) · 4 hours (1) · 4-6 hours (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · IR: 6-10 hours; ER: 24 hours (1)
halflife:
None (133) · 2-3 hours (parent and active N-desethyl metabolite)'"`UNIQ--ref-000006E1-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~1.8 hours (initial); ~10 hours (terminal)'"`UNIQ--ref-00000B25-QINU`"' (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) · ~6% IR oral (substantial first-pass to active N-desethyl metabolite, which contributes most of the antimuscarinic adverse effects); transdermal bypasses first-pass and is better tolerated'"`UNIQ--ref-000006E2-QINU`"' (1) · ~67% (oral)'"`UNIQ--ref-00000B26-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 avoided; not first-line.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (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)
legal:
None (134) · OTC (transdermal patch in women) and [[USLegal:Prescription only|Rx-only]] (other forms) in US (1) · [[USLegal:Prescription only|Rx-only]] in US (3)

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