Drilldown: Medicines

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None (26) · (none, never marketed) (1) · Ambien (IR), Ambien CR (biphasic-release), Edluar (sublingual), Intermezzo (low-dose sublingual for middle-of-night awakening), Zolpimist (oral spray) (1) · Ativan (oral, injectable), Loreev XR (1) · Dalmane (1) · Doral (1) · Doriden (1) · DXM (1) · DXO (1) · Halcion (1) · Hetlioz (1) · Imovane (1) · Klonopin (1) · Lunesta (1) · Mogadon (1) · Nembutal (1) · Placidyl (1) · ProSom (1) · Quaalude (1) · Restoril (1) · Rohypnol (1) · Rozerem (1) · Seconal (1) · Sonata (1) · Spravato (1) · THIP (1) · Ultram (IR), Ultram ER, ConZip ER (1) · Valium (oral, IV/IM, rectal), Diastat (rectal gel for breakthrough seizures), Valtoco (nasal spray for breakthrough seizures), Libervant (buccal film) (1) · Versed (1) · Xyrem (1)

Research material · Classic Psychedelic · Stimulant · Opioid · Sedative-Hypnotic · Phenethylamine · Tryptamine · Benzodiazepine · Botanical · [[:Category:Antihypertensives|Antihypertensive]] · Dissociative · Anticonvulsant · Antidepressant · Plant Medicine · Analgesic · Antiparkinsonian · Antipsychotic · Empathogen · Neuroleptic · Cathinone

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None (8) · Active metabolite of DXM; NMDA antagonist (1) · Contains salvinorin A (1) · Extremely potent GABAA positive allosteric modulator (1) · GABAA positive allosteric modulator (15) · GABAA positive allosteric modulator (non-benzodiazepine) (3) · GABAA positive allosteric modulator; very long half-life (1) · GABAA potentiator (1) · GABAA potentiator and direct activator (2) · GABAB agonist; GHB receptor agonist (1) · Kappa-opioid agonist; NMDA antagonist; SERT/DAT/NET inhibitor (1) · Kappa-opioid receptor agonist (1) · Melatonin receptor agonist (2) · NMDA antagonist (3) · NMDA antagonist; endogenous opioid releaser (1) · NMDA antagonist; fluorinated ketamine analogue (1) · NMDA antagonist; kappa-opioid agonist (1) · NMDA antagonist; ketamine analogue (1) · NMDA antagonist; more stimulating than PCP (1) · NMDA antagonist; opioid agonist (1) · NMDA antagonist; potent opioid agonist (1) · NMDA antagonist; SERT inhibitor; sigma-1 agonist (1) · NMDA antagonist; sigma receptor agonist (2) · NMDA antagonist; sigma receptor agonist; dopaminergic (1) · NMDA antagonist; sigma-1 agonist; serotonin reuptake inhibitor (1) · Positive allosteric modulator of the GABA_A receptor at the benzodiazepine binding site; increases frequency of Cl⁻ channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (1) · Selective GABAA agonist (extrasynaptic delta subunit) (1)

None (48) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · Treatment-resistant depression (TRD) in adults, as adjunct to oral antidepressant (FDA-approved March 2019). Depressive symptoms in adults with MDD with acute suicidal ideation or behavior (FDA-approved Aug 2020). (1) · '"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"' (1) · '"`UNIQ--vote-00000019-QINU`"', '"`UNIQ--vote-0000001A-QINU`"', '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"' (1) · '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"' (1) · '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"' (2)

None (48) · '''5 mg PO at bedtime for women, 5-10 mg for men''' (per FDA's 2013 sex-specific dose reduction for women due to slower clearance). Ambien CR 6.25 mg women / 6.25-12.5 mg men. Intermezzo SL 1.75 mg women / 3.5 mg men (1) · Anxiety: 0.25 mg PO BID, titrate by 0.125-0.25 mg every 3 days to target 1-4 mg/day divided. Seizures: 1.5 mg/day divided TID, titrate by 0.5-1 mg every 3 days (1) · Anxiety: 0.5-1 mg PO BID-TID. Insomnia: 1-2 mg PO at bedtime. Status epilepticus: 4 mg IV (adult), repeat after 5-10 minutes if needed. Acute agitation: 1-2 mg IM (1) · Anxiety: 2-10 mg PO 2-4 times daily. Alcohol withdrawal: 10-20 mg PO/IV every 4-6 hours, symptom-triggered. Status epilepticus: 5-10 mg IV. Breakthrough seizures: Diastat rectal 0.2-0.5 mg/kg or Valtoco intranasal 5-20 mg (1) · Induction (TRD): 56 mg intranasal twice weekly × 4 weeks. Maintenance: 56-84 mg once weekly × 4 weeks, then 56-84 mg every 1-2 weeks. For acute suicidality: 84 mg twice weekly × 4 weeks. Administered under medical supervision in REMS-certified site. (1) · IR: 25-50 mg PO every 4-6 hours as needed, titrate as tolerated. ER: 100 mg PO once daily, titrate by 100 mg every 5 days (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

None (48) · 28 mg/device (each dose uses 2 devices) (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · IR tablets 5, 10 mg; CR tablets 6.25, 12.5 mg; SL tablets 1.75, 3.5, 5, 10 mg; oral spray (1) · IR tablets 50 mg; ER tablets 100, 200, 300 mg (Ultram ER, ConZip); oral solution 5 mg/mL; combination products with acetaminophen (Ultracet) (1) · Tablets 0.5, 1, 2 mg; oral concentrate 2 mg/mL; injection 2 mg/mL and 4 mg/mL; Loreev XR capsules 1, 2, 3 mg (1) · Tablets 0.5, 1, 2 mg; orally disintegrating tablets 0.125, 0.25, 0.5, 1, 2 mg (1) · Tablets 2, 5, 10 mg; oral solution 1, 5 mg/mL; injection 5 mg/mL; Diastat rectal gel 2.5, 5, 10, 20 mg; Valtoco nasal spray 5, 7.5, 10 mg/dose; Libervant buccal film (1)

None (48) · 10 mg/day (anxiety, oral) (1) · 10 mg/day (IR); 12.5 mg/day (CR) (1) · 20 mg/day (seizures); commonly limited to 4 mg/day for anxiety in current practice (1) · 40 mg/day (oral, anxiety) (1) · 400 mg/day (IR, adult); 300 mg/day (ER); 300 mg/day in elderly >75 years (1) · 84 mg per session (1) · N/A (never approved) (1)

None (48) · buccal (1) · IM (1) · intramuscular (1) · intranasal (1) · Intranasal (under direct medical supervision) (1) · intranasal; rectal and IV reported. (1) · intravenous (1) · IV (1) · Oral (6) · oromucosal spray (1) · rectal (1) · sublingual (2)

None (48) · 15-30 minutes (1) · 15-60 minutes (oral); 1-5 minutes (IV); 4-10 minutes (rectal or intranasal) (1) · 20-60 minutes (1) · 30-60 minutes (IR) (1) · 30-60 minutes (oral); 5 minutes (IV); 15-30 minutes (IM) (1) · Within hours of first administration (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (48) · 4-6 hours (IR); 24 hours (ER) (1) · 6-12 hours (long-acting among benzodiazepines) (1) · 6-24 hours (parent); much longer when accounting for the long-lived active metabolites (1) · 6-8 hours (1) · 6-8 hours (IR); 8 hours (CR via biphasic release) (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (1)

None (48) · 12-15 hours (intermediate); '''no active metabolites''' (key clinical feature)'"`UNIQ--ref-00000023-QINU`"' (1) · 30-40 hours (long; accumulates with chronic dosing)'"`UNIQ--ref-00000026-QINU`"' (1) · Diazepam 20-50 hours; '''N-desmethyldiazepam (nordazepam) 30-200 hours''' is the major active metabolite and accumulates substantially with chronic dosing'"`UNIQ--ref-00000026-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Tramadol 6-7 hours; M1 active metabolite 7-9 hours'"`UNIQ--ref-0000001D-QINU`"' (1) · ~2.5 hours'"`UNIQ--ref-0000001A-QINU`"' (1) · ~7-12 hours (1)

None (48) · Not formally characterized in humans. (1) · ~48% intranasal (1) · ~70% (oral)'"`UNIQ--ref-0000001B-QINU`"' (1) · ~75% (IR, rises with multi-dose administration due to saturable first-pass)'"`UNIQ--ref-0000001E-QINU`"' (1) · ~90% (oral)'"`UNIQ--ref-00000024-QINU`"' (1) · ~90% (oral)'"`UNIQ--ref-00000027-QINU`"' (1) · ~93% (oral); ~90% (rectal)'"`UNIQ--ref-00000027-QINU`"' (1)

None (48) · 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; may cause fetal harm (1) · Chronic third-trimester exposure produces neonatal opioid withdrawal syndrome and respiratory depression at delivery.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; case reports of neonatal sedation with late-pregnancy exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; some signal for cleft palate with first-trimester exposure (debated); neonatal sedation and withdrawal with third-trimester exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Some signal for cleft lip/palate with first-trimester exposure (debated); neonatal sedation and withdrawal with third-trimester exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Some signal for cleft palate with first-trimester exposure (debated); neonatal sedation and withdrawal with third-trimester exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

None (49) · Rx, Schedule III (US). REMS program required. (1) · [[USLegal:Schedule IV|Schedule IV controlled substance]] in US (federally scheduled 2014); some states schedule higher'"`UNIQ--ref-0000001F-QINU`"' (1) · [[USLegal:Schedule IV|Schedule IV controlled substance]] in US. Carries the benzodiazepine class '''Boxed Warning''' for risk of fatal respiratory depression, coma, and death when combined with opioids'"`UNIQ--ref-00000025-QINU`"' (1) · [[USLegal:Schedule IV|Schedule IV controlled substance]] in US. Carries the benzodiazepine class '''Boxed Warning''' for risk of fatal respiratory depression, coma, and death when combined with opioids'"`UNIQ--ref-00000028-QINU`"' (2) · [[USLegal:Schedule IV|Schedule IV controlled substance]] in US. Carries the FDA '''Boxed Warning''' for '''complex sleep behaviors''' (sleep-driving, sleep-walking, sleep-eating, other parasomnias) added in 2019'"`UNIQ--ref-0000001C-QINU`"' (1)