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Drilldown: Medicines

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Medicines > classes : Research material or [[:Category:Antiarrhythmics|Antiarrhythmic (class IV)]]

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generic:
brand:
None (130) · (none, never marketed) (1) · Calan, Calan SR, Verelan, Verelan PM, Isoptin SR (1) · Cardizem, Tiazac, Cartia XT, Dilacor XR, Taztia XT, Matzim LA (1) · O-DSMT (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) · 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-0000063E-QINU`"', '"`UNIQ--vote-0000063F-QINU`"', '"`UNIQ--vote-00000640-QINU`"', '"`UNIQ--vote-00000641-QINU`"' (1) · '"`UNIQ--vote-00000A66-QINU`"', '"`UNIQ--vote-00000A67-QINU`"', '"`UNIQ--vote-00000A68-QINU`"', '"`UNIQ--vote-00000A69-QINU`"', '"`UNIQ--vote-00000A6A-QINU`"' (1)
starting dose:
None (131) · ER 180-240 mg PO once daily; IR 30 mg PO QID; IV 0.25 mg/kg over 2 min for acute rate control, then 5-15 mg/h infusion (1) · IR 80-120 mg PO TID; ER 180-240 mg PO daily; IV 2.5-5 mg over 2 min for SVT termination (under monitoring); cluster prophylaxis up to 480-960 mg/d in divided doses (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
None (131) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · IR 30, 60, 90, 120 mg tablets; multiple ER capsules and tablets 60-420 mg; IV 5 mg/mL (1) · IR 40, 80, 120 mg tablets; SR/ER 100-360 mg; IV 2.5 mg/mL (1)
fda max:
None (131) · N/A (never approved) (1) · ~480 mg/d (oral) for cardiovascular indications; higher off-label for cluster (1) · ~480 mg/d (oral); IV per protocol (1)
routes:
None (131) · intranasal; rectal and IV reported. (1) · IV (2) · multiple ER formulations) (1) · Oral (1) · Oral (IR (1) · Oral (IR and multiple ER) (1) · sublingual (1)
onset:
None (131) · IV: 1-3 minutes (SVT termination); PO IR: 30-60 minutes; ER: hours (1) · IV: 3-7 minutes (rate control); PO IR: 30-60 minutes; ER: hours (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (131) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · IR: 4-8 hours; ER: 24 hours (1) · IR: 6-8 hours; ER: 24 hours (1)
halflife:
None (131) · 3-4.5 hours (IR); 5-7 hours (ER; effective duration 24 hours via formulation)'"`UNIQ--ref-00000642-QINU`"' (1) · 3-7 hours (IR); functional 24 hours (ER)'"`UNIQ--ref-00000A6B-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1)
bioavailability:
None (131) · Not formally characterized in humans. (1) · ~20-35% (oral; extensive first-pass via CYP3A4 with R/S enantiomer differences)'"`UNIQ--ref-00000A6C-QINU`"' (1) · ~40% (oral; extensive first-pass via CYP3A4)'"`UNIQ--ref-00000643-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) · Limited data; alternative antihypertensives generally preferred. Crosses placenta.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; labetalol/nifedipine generally preferred. Crosses placenta.<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)

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