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)

None (48) · 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)

None (48) · 25 mg (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) · Oral tablets 50 mg (ReVia, Depade, generics); Vivitrol extended-release IM suspension 380 mg single-dose vial; Contrave (naltrexone 8 mg + bupropion 90 mg ER tablets); compounded 1, 2, 3, 4.5 mg tablets/capsules for LDN (1)

None (47) · 200 mg/d (1) · 50 mg/day oral; 380 mg/4 weeks IM (Vivitrol); 32 mg + 360 mg naltrexone/bupropion daily (Contrave maximum after titration) (1) · N/A (never approved) (1)

None (46) · intramuscular (depot) (1) · intranasal; rectal and IV reported. (1) · Oral (4) · sublingual (1)

None (46) · Anxiolysis classically 3-4 weeks, continuing improvement to 8-12 weeks (1) · Mood: 2–4 weeks. Pain: often within 1–2 weeks. (1) · Oral peak plasma 1 hour; therapeutic opioid blockade within hours of first dose. IM Vivitrol: peak plasma 2-3 days; therapeutic blockade through the dosing interval. (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (46) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Chronic daily dosing (1) · Long (1) · Oral mu-blockade clinically meaningful for 24-72 hours; IM Vivitrol blockade through 4 weeks. (1)

None (46) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Naltrexone parent ~4 hours (oral); 6-beta-naltrexol (active metabolite) ~13 hours. Vivitrol depot terminal half-life 5-10 days with sustained release from microspheres maintaining blockade for the 4-week dosing interval.'"`UNIQ--ref-0000004F-QINU`"' (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) · ~5-40% (oral, highly variable due to extensive first-pass metabolism; mean ~5-10% for parent naltrexone with the majority of pharmacologic effect coming from 6-beta-naltrexol). IM Vivitrol bypasses first-pass entirely.'"`UNIQ--ref-00000050-QINU`"' (1) · ~50% (highly variable) (1)

None (47) · 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)

None (48) · Rx-only (1) · Rx-only in US (1)