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Drilldown: Medicines

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Medicines > classes : Antidepressant or Sedative-Hypnotic or [[:Category:Trace_elements|Trace element]]

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generic:
brand:
None (10)
classes: (Click arrow to add another value)
mechanism:
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<sub>A</sub> receptor at the benzodiazepine binding site; increases frequency of Cl<sup>−</sup> 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)
uses:
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-0000131A-QINU`"', '"`UNIQ--vote-0000131B-QINU`"' (1)
starting dose:
None (47) · 25 mg (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · OTC dentifrice/rinse 0.05-0.5% fluoride daily; Rx 1.1% sodium fluoride toothpaste/gel daily; supplements (where local water non-fluoridated) age-titrated 0.25-1 mg/d (1)
preparations:
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) · Toothpaste, rinse, gel, varnish (topical); 0.25, 0.5, 1 mg tablets and drops (Rx supplements where appropriate) (1)
fda max:
None (47) · 200 mg/d (1) · N/A (never approved) (1) · Topical: per formulation; oral supplement age-dependent (1)
routes:
None (46) · intranasal; rectal and IV reported. (1) · Oral (4) · sublingual (1) · Topical (1)
onset:
None (46) · Anxiolysis classically 3-4 weeks, continuing improvement to 8-12 weeks (1) · Caries reduction over months to years of consistent use (1) · Mood: 2–4 weeks. Pain: often within 1–2 weeks. (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (46) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Chronic daily dosing (1) · Hours per topical application (1) · Long (1)
halflife:
None (46) · 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) · ~6 hours plasma; long bone retention (1)
bioavailability:
None (46) · Absolute bioavailability not precisely characterized; food modestly increases exposure (1) · Not formally characterized in humans. (1) · Topical: local effect on enamel; systemic supplementation has high oral bioavailability with skeletal accumulation (1) · ~50% (highly variable) (1)
pregnancy:
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) · Safe at routine fluoride levels.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (47) · OTC (most dentifrice and rinse) and [[USLegal:Prescription only|Rx-only]] (high-concentration paste/gel, supplements) in US (1) · Rx-only (1) · Rx-only in US (1)

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