Drilldown: Medicines

Bromazolam (1) · Insulin degludec (1) · Insulin glargine (1)

(none, never marketed) (1) · Lantus, Basaglar, Semglee, Toujeo (U-300) (1) · Tresiba (1)

Designer benzodiazepine (1) · Research material (1) · Sedative-Hypnotic (1) · Triazolobenzodiazepine (1) · [[:Category:Basal_insulins|Basal insulin]] (2) · [[:Category:Insulins|Insulin]] (2) · [[:Category:Long-acting_insulins|Long-acting insulin analog]] (1) · [[:Category:Ultra-long-acting_insulins|Ultra-long-acting insulin analog]] (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-00000237-QINU`"' Binds the same insulin receptor as endogenous insulin with comparable mitogenic-to-metabolic ratio; provides basal hepatic glucose suppression and peripheral glucose uptake without prandial peaks'"`UNIQ--ref-00000238-QINU`"'. (1) · '"`UNIQ--vote-00001356-QINU`"' Binds the same insulin receptor as endogenous insulin with comparable mitogenic-to-metabolic ratio'"`UNIQ--ref-00001357-QINU`"'. (1)

No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000239-QINU`"', '"`UNIQ--vote-0000023A-QINU`"' (1) · '"`UNIQ--vote-00001358-QINU`"', '"`UNIQ--vote-00001359-QINU`"' (1)

No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · ~10 units SC at the same time daily, or 0.1-0.2 units/kg/d; titrate by fasting glucose (2)

100 U/mL (FlexTouch pen) and 200 U/mL (FlexTouch pen, higher-dose convenience) (1) · 100 U/mL (Lantus, Basaglar, Semglee) vials and pens; 300 U/mL (Toujeo) pens (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)

None · Indication-specific · 40 mg/d · 10 mg/d · 20 mg/d · 80 mg/d · 10 mg/d (adults) · 100 mg/d · 4 g/d · 400 mg/d · 40 mg/d typical; up to 240 mg/d for Zollinger-Ellison · 5 mg/d · 50 mg/d · 600 mg/d · No fixed ceiling; titrate to clinical effect and tolerability with CDC opioid prescribing guidance constraints on morphine-milligram-equivalent (MME) totals · No fixed maximum; titrated to TSH target · TID per eye · Titrated to glucose; no fixed ceiling · Titrated to glucose; no fixed maximum · '''20 mg/day in adults >60 years''' per FDA's 2011-2012 QT-prolongation warning; 40 mg/day in adults ≤60

Other values:

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intranasal; rectal and IV reported. (1) · Oral (1) · Subcutaneous (never IV; not for use in insulin pumps) (2) · sublingual (1)

1-2 hours (1) · ~1 hour (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

6–10 h subjective; full pharmacologic effect considerably longer. (1) · >42 hours per dose (effectively flat once at steady state) (1) · ~24 hours per dose (peakless profile by design) (1)

Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~12 hours apparent (functional duration ~24 hours due to depot release kinetics)'"`UNIQ--ref-0000023B-QINU`"' (1) · ~25 hours apparent (functional duration well over 42 hours from multi-hexamer depot)'"`UNIQ--ref-0000135A-QINU`"' (1)

Not formally characterized in humans. (1) · ~100% from subcutaneous depot (1) · ~100% from subcutaneous depot (by definition of the route) (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) · Insulin is the preferred glucose-lowering therapy in pregnancy; degludec has reassuring observational data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Insulin is the preferred glucose-lowering therapy in pregnancy; glargine has reassuring observational data, though NPH and detemir remain the traditional choices.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

None (1) · [[USLegal:Prescription only|Rx-only]] in US (2)