Drilldown: Medicines

Benazepril (1) · Bromazolam (1)

(none, never marketed) (1) · Lotensin (1)

Designer benzodiazepine (1) · Research material (1) · Sedative-Hypnotic (1) · Triazolobenzodiazepine (1) · [[:Category:ACE_inhibitors|ACE inhibitor]] (1) · [[:Category:Antihypertensives|Antihypertensive]] (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) · '"`UNIQ--vote-00000A1D-QINU`"' Like other ACE inhibitors, it raises bradykinin (driving the dry cough and rare angioedema). Renally cleared; dose-adjust in renal impairment'"`UNIQ--ref-00000A1E-QINU`"'. (1)

No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000A1F-QINU`"', '"`UNIQ--vote-00000A20-QINU`"', '"`UNIQ--vote-00000A21-QINU`"' (1)

10 mg PO once daily (5 mg if on a diuretic); titrate to 40 mg (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

5, 10, 20, 40 mg tablets (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)

80 mg/d (1) · N/A (never approved) (1)

intranasal; rectal and IV reported. (1) · Oral (2) · sublingual (1)

BP lowering within 1 hour; max at 6 hours (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

24 hours (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)

None · ~12 hours · ~27 days · ~5 h (caffeine) · '''Autoinduction''': 25-65 hours initially, falling to 12-17 hours after 2-3 weeks of dosing as carbamazepine induces its own CYP3A4 metabolism. Major clinical implication: doses require re-titration after the autoinduction period'"`UNIQ--ref-0000001D-QINU`"' · 0.5-1.5 hours (plasma); pharmacodynamic effect persists 24+ hours'"`UNIQ--ref-000000DE-QINU`"' · 1-1.3 hours'"`UNIQ--ref-000001A1-QINU`"' · 1-1.5 hours'"`UNIQ--ref-00000DE3-QINU`"' · 1-2 hours (parent compound)'"`UNIQ--ref-00000029-QINU`"' · 1-2 hours (parent); 18-30 hours for active metabolite oxypurinol'"`UNIQ--ref-0000030F-QINU`"' · 1-2 hours'"`UNIQ--ref-00000017-QINU`"' · 1-3 days acute, 4-6 days chronic; 4-16 days for norfluoxetine'"`UNIQ--ref-0000004C-QINU`"' · 1-3 hours (normal liver); markedly prolonged in overdose with glutathione depletion'"`UNIQ--ref-00000022-QINU`"' · 1-3 minutes (very short)'"`UNIQ--ref-00000C0F-QINU`"' · 1.4 hours (parent); 13-24 hours for active metabolite canrenone'"`UNIQ--ref-00000354-QINU`"' · 1.5-2 hours (longer in renal failure)'"`UNIQ--ref-00000222-QINU`"' · 1.5-2 hours'"`UNIQ--ref-00000020-QINU`"' · 10-11 hours (benazeprilat, the active metabolite)'"`UNIQ--ref-00000A22-QINU`"' · 11-13 h (immediate-release); 11-16 h (extended-release) · 11-15 hours'"`UNIQ--ref-00000842-QINU`"'

Other values:

Search

Not formally characterized in humans. (1) · ~37% (oral; food does not affect)'"`UNIQ--ref-00000A23-QINU`"' (1)

'''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, skull hypoplasia, hypotension. Stop on detection'"`UNIQ--ref-00000A24-QINU`"' (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)

None (1) · [[USLegal:Prescription only|Rx-only]] in US (1)