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Medicines > classes : Research material or [[:Category:Antifolates|Antifolate]] & routes: Oral

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generic:
Bromazolam (1) · Methotrexate (1)
brand:
(none, never marketed) (1) · Trexall, Otrexup, Rasuvo, Xatmep, Rheumatrex (discontinued) (1)
classes: (Click arrow to add another value)
mechanism:
None (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)
uses:
No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-000007C1-QINU`"', '"`UNIQ--vote-000007C2-QINU`"', '"`UNIQ--vote-000007C3-QINU`"', '"`UNIQ--vote-000007C4-QINU`"', '"`UNIQ--vote-000007C5-QINU`"', '"`UNIQ--vote-000007C6-QINU`"', '"`UNIQ--vote-000007C7-QINU`"' (1)
starting dose:
No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · Rheumatologic: 7.5-15 mg PO or SC '''once weekly''' (not daily — daily dosing is a recognized fatal error); folic acid 1 mg PO daily on non-MTX days; oncology dosing is far higher and indication-specific (1)
preparations:
2.5 mg tablets; 10-50 mg/mL injection; pre-filled subcutaneous autoinjectors (Otrexup, Rasuvo); 2.5 mg/mL oral solution (Xatmep) (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
N/A (never approved) (1) · Rheumatologic ~25 mg/week; oncology indication-specific (1)
routes: (Click arrow to add another value)
onset:
Rheumatologic effect at 4-8 weeks; ectopic resolution over 2-3 weeks (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
6–10 h subjective; full pharmacologic effect considerably longer. (1) · Once-weekly dosing in rheumatology (1)
halflife:
3-10 hours (low dose); 8-15 hours (high dose); much longer in third-space accumulation (pleural effusion, ascites)'"`UNIQ--ref-000007C8-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1)
bioavailability:
60-70% PO at low doses; saturable at high doses (parenteral routes preferred above 15-25 mg/week)'"`UNIQ--ref-000007C9-QINU`"' (1) · Not formally characterized in humans. (1)
pregnancy:
'''Contraindicated in pregnancy''' (Category X); abortifacient and teratogenic. Discontinuation 3-6 months before conception is standard.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · 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)
legal:
None (1) · [[USLegal:Prescription only|Rx-only]] in US (1)

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