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Drilldown: Medicines

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Medicines > classes : Research material or SSRI)]] & routes: Oral

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generic:
Bromazolam (1) · Olanzapine / Fluoxetine (1)
brand:
(none, never marketed) (1) · Symbyax (1)
classes: (Click arrow to add another value)
mechanism:
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) · '"`UNIQ--vote-00001549-QINU`"' Metabolic effects (weight gain, dyslipidemia, glucose dysregulation) dominate the long-term tolerability profile; routine metabolic monitoring is standard'"`UNIQ--ref-0000154A-QINU`"'. (1)
uses:
No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-0000154B-QINU`"', '"`UNIQ--vote-0000154C-QINU`"' (1)
starting dose:
6/25 mg PO once daily in the evening; titrate within range 3/25 to 18/75 mg by clinical response and tolerability (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
Capsules: 3/25, 6/25, 6/50, 12/25, 12/50 mg olanzapine/fluoxetine (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
18 mg olanzapine / 75 mg fluoxetine per day (1) · N/A (never approved) (1)
routes: (Click arrow to add another value)
onset:
Mood improvement at 1-3 weeks; full effect 4-6 weeks (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
24 hours (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)
halflife:
Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Olanzapine ~30 hours; fluoxetine 1-4 days (norfluoxetine 7-15 days)'"`UNIQ--ref-0000154D-QINU`"' (1)
bioavailability:
Not formally characterized in humans. (1) · Olanzapine 60% (oral); fluoxetine high (oral)'"`UNIQ--ref-0000154E-QINU`"' (1)
pregnancy:
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; fluoxetine has reassuring data but olanzapine carries metabolic-syndrome and gestational diabetes signals.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the '''antidepressant Boxed Warning''' for suicidality in children/adolescents/young adults and the atypical-neuroleptic '''Boxed Warning''' for increased mortality in elderly dementia patients'"`UNIQ--ref-0000154F-QINU`"' (1)

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