Drilldown: Medicines

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None (10)

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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 (3) · 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) · Irreversible non-selective MAO inhibitor (3) · Melatonin receptor agonist (2) · Melatonin receptor agonist; 5-HT2C antagonist (1) · Mu-opioid agonist; modulates glutamate AMPA receptors (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) · Potent serotonin reuptake inhibitor; also NRI (1) · Reversible inhibitor of MAO-A (1) · Selective GABAA agonist (extrasynaptic delta subunit) (1) · Selective norepinephrine reuptake inhibitor (3) · Serotonin and norepinephrine reuptake inhibitor (3) · Serotonin reuptake inhibitor and 5-HT2A antagonist (1) · Serotonin–norepinephrine reuptake inhibition (balanced) (1) · Serotonin–norepinephrine reuptake inhibitor (2) · TrkB/BDNF'"`UNIQ--ref-00000084-QINU`"' '"`UNIQ--vote-00000085-QINU`"' (1) · Weak SRI; primarily H1/D2/alpha antagonist (1) · '"`UNIQ--vote-0000001D-QINU`"' '''QT prolongation''' risk at high doses prompted the FDA's 2015 caution against use in patients with prolonged QT or with concurrent QT-prolonging medicines'"`UNIQ--ref-0000001E-QINU`"'. (1)

None (47) · Depression, anxiety, neuropathic pain, fibromyalgia, chronic musculoskeletal pain (1) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (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`"' (1)

None (47) · 15 mg PO at bedtime, titrate to 30-45 mg/day after 1-2 weeks. '''Counterintuitive dose paradox''': lower doses (7.5-15 mg) are more sedating than higher doses because H1 antihistamine effect dominates at low dose (1) · 25 mg (1) · Anxiety: 25-50 mg PO QID. Pruritus: 25 mg PO TID-QID. Insomnia: 25-50 mg PO at bedtime. Pediatric: 50-100 mg/day divided (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

None (47) · 25 mg, 50 mg, 100 mg tablets; oral concentrate 20 mg/mL (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · Tablets 10, 25, 50 mg (HCl); capsules 25, 50, 100 mg (pamoate); oral suspension 25 mg/5 mL; injection 25, 50 mg/mL (IM only, never IV) (1) · Tablets 7.5, 15, 30, 45 mg; orally disintegrating tablets (SolTab) 15, 30, 45 mg (1)

None (47) · 200 mg/d (1) · 400 mg/day theoretical; in practice rarely exceeds 200 mg/day (1) · 45 mg/day (1) · N/A (never approved) (1)

None (46) · intramuscular (1) · intranasal; rectal and IV reported. (1) · Oral (5) · sublingual (1)

None (46) · 15-30 minutes (oral) (1) · Anxiolysis classically 3-4 weeks, continuing improvement to 8-12 weeks (1) · Mood: 2–4 weeks. Pain: often within 1–2 weeks. (1) · Sleep effect from first dose; antidepressant effect over 1-4 weeks (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (46) · 24 hours (HS dosing) (1) · 4-6 hours (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Chronic daily dosing (1) · Long (1)

None (46) · 14-25 hours (longer in elderly and hepatic impairment)'"`UNIQ--ref-00000026-QINU`"' (1) · 20-40 hours'"`UNIQ--ref-00000023-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~12 hours (1) · ~26 h (sertraline; range 13-45 h, longer in females); ~62-104 h (N-desmethylsertraline, weakly active) (1)

None (46) · Absolute bioavailability not precisely characterized; food modestly increases exposure (1) · Not formally characterized in humans. (1) · ~50% (highly variable) (1) · ~50% (oral; substantial first-pass)'"`UNIQ--ref-00000024-QINU`"' (1) · ~80% (oral)'"`UNIQ--ref-00000027-QINU`"' (1)

None (46) · 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) · Category C (1) · Category C'"`UNIQ--ref-0000008F-QINU`"' (1) · Limited human data; older agent with substantial use experience; some signal for first-trimester exposure but not conclusive.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; some observational signals reassuring relative to other antidepressants.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

None (47) · Rx-only (1) · Rx-only in US (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000025-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, which is a meaningful clinical advantage over the benzodiazepine alternatives for short-term anxiety'"`UNIQ--ref-00000028-QINU`"' (1)