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: Sedative-hypnotic

or [[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]]

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Bromazolam (1) · Clonazolam (1) · Dapagliflozin (1) · Deschloroetizolam (1) · Diclazepam (1) · Empagliflozin (1) · Estazolam (1) · Eszopiclone (1) · Ethchlorvynol (1) · Flualprazolam (1) · Flubromazepam (1) · Flubromazolam (1) · Flunitrazepam (1) · Flunitrazolam (1) · Flurazepam (1) · Gaboxadol (1) · GHB (1) · Glimepiride (1) · Glipizide (1) · Glutethimide (1) · Linagliptin (1) · Lormetazepam (1) · Metformin (1) · Methaqualone (1) · Midazolam (1) · Nifoxipam (1) · Nitrazepam (1) · Pentobarbital (1) · Pioglitazone (1) · Quazepam (1) · Ramelteon (1) · Secobarbital (1) · Sitagliptin (1) · Tasimelteon (1) · Temazepam (1) · Triazolam (1) · Zaleplon (1) · Zopiclone (1)

None (7) · 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) · Melatonin receptor agonist (2) · Positive allosteric modulator of the GABAA receptor at the benzodiazepine binding site; increases frequency of Cl− channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (1) · Selective GABAA agonist (extrasynaptic delta subunit) (1) · '"`UNIQ--vote-00000013-QINU`"' Does not stimulate insulin secretion; minimal hypoglycemia risk as monotherapy. Cleared renally unchanged; dose-adjust by eGFR'"`UNIQ--ref-00000014-QINU`"'. Rare lactic acidosis primarily in renal failure or acute illness. (1) · '"`UNIQ--vote-000002D7-QINU`"' Hypoglycemia is the central risk, especially in elderly and renally impaired patients (glipizide has shorter half-life than glyburide, which is one reason it is preferred in older adults). CYP2C9 substrate; weight gain typical. (1) · '"`UNIQ--vote-00000762-QINU`"' Largely renally cleared, hence the eGFR-tiered dosing. Rare but well-documented signals: acute pancreatitis (uncertain causal contribution), severe joint pain, and bullous pemphigoid (class effect, especially in older Asian patients)'"`UNIQ--ref-00000763-QINU`"'. (1)

None (29) · 1-2 mg PO once daily with breakfast; titrate by glycemic response (1) · 10 mg PO once daily in the morning; 5 mg starting in heart failure (1) · 10 mg PO once daily in the morning; may titrate to 25 mg for additional glycemic effect (1) · 100 mg PO once daily (50 mg if CrCl 30-44; 25 mg if <30 or dialysis) (1) · 15-30 mg PO once daily; titrate to 45 mg (1) · 5 mg PO once daily (no renal dose adjustment, unlike sitagliptin) (1) · 5 mg PO once daily, 30 minutes before breakfast; XL: 5 mg with breakfast (1) · 500 mg PO once or twice daily with meals; titrate weekly to limit GI effects (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

None (29) · 1 mg, 2 mg, 4 mg tablets (1) · 10 mg, 25 mg tablets (1) · 15, 30, 45 mg tablets (1) · 25, 50, 100 mg tablets; combination tablets with metformin (1) · 5 mg tablets; combination with metformin (1) · 5 mg, 10 mg immediate-release tablets; 2.5 mg, 5 mg, 10 mg extended-release tablets (1) · 5 mg, 10 mg tablets (1) · 500 mg, 850 mg, 1000 mg IR tablets; 500 mg, 750 mg, 1000 mg ER tablets; 500 mg/5 mL oral solution (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)

None (29) · 10 mg/d (1) · 100 mg/d (1) · 25 mg/d (1) · 2550 mg/d (IR); 2000 mg/d (ER) (1) · 40 mg/d (IR; doses >15 mg given as divided BID); 20 mg/d (XL) (1) · 45 mg/d (1) · 5 mg/d (1) · 8 mg/d (1) · N/A (never approved) (1)

None (29) · intranasal; rectal and IV reported. (1) · Oral (9) · sublingual (1)

None (29) · 1-2 hours (1) · Glucose lowering within days; HbA1c effect at 8-12 weeks (1) · Glycosuria within hours; HbA1c effect at 12 weeks; cardiovascular and renal benefits over months (1) · Glycosuria within hours; HbA1c effect at 12 weeks; CV/renal benefits over months (1) · HbA1c effect at 12-16 weeks (slower than other classes) (1) · Postprandial glucose effect within days; HbA1c by 12 weeks (2) · Within 30 minutes (IR) (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (29) · 24 hours (6) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · ~12 hours (IR); 24 hours (ER) (1) · ~12-24 hours (1)

None (29) · 2-5 hours'"`UNIQ--ref-000002D9-QINU`"' (1) · 6.2 hours (plasma); ~17 hours in erythrocytes'"`UNIQ--ref-00000018-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~12 hours (effective); terminal much longer'"`UNIQ--ref-0000117C-QINU`"' (1) · ~12.4 hours'"`UNIQ--ref-0000027C-QINU`"' (1) · ~12.4 hours'"`UNIQ--ref-00000765-QINU`"' (1) · ~12.9 hours'"`UNIQ--ref-00000552-QINU`"' (1) · ~3-7 hours (parent); 16-24 hours including active metabolites'"`UNIQ--ref-00000824-QINU`"' (1) · ~5-9 hours (parent and active metabolites combined)'"`UNIQ--ref-00000492-QINU`"' (1)

None (29) · 50-60% (oral; decreased with food, but food given anyway for GI tolerance)'"`UNIQ--ref-00000019-QINU`"' (1) · High (oral; absorption not affected by food)'"`UNIQ--ref-00000825-QINU`"' (1) · High (oral; not affected by food, but typically given with the morning meal)'"`UNIQ--ref-0000027D-QINU`"' (1) · Not formally characterized in humans. (1) · ~100% (oral; food delays absorption, hence pre-meal dosing for IR)'"`UNIQ--ref-000002DA-QINU`"' (1) · ~100% (oral; not significantly affected by food)'"`UNIQ--ref-00000493-QINU`"' (1) · ~30% (oral)'"`UNIQ--ref-0000117D-QINU`"' (1) · ~78% (oral; high-fat meal modestly reduces but is not clinically significant)'"`UNIQ--ref-00000553-QINU`"' (1) · ~87% (oral)'"`UNIQ--ref-00000766-QINU`"' (1)

None (29) · Avoid in second and third trimesters; fetal SGLT2 inhibition disrupts kidney development.[[[Pharmacopedia:Citation needed|citation needed]]] (2) · 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) · Avoid; switch to insulin. Hypoglycemia in newborn reported.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Avoid; switch to insulin. Neonatal hypoglycemia reported.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Generally considered safe; widely used in PCOS and gestational diabetes; placental transfer occurs.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Limited data; switch to insulin where feasible.[[[Pharmacopedia:Citation needed|citation needed]]] (3)

None (30) · [[USLegal:Prescription only|Rx-only]] in US (7) · [[USLegal:Prescription only|Rx-only]] in US. Carries a '''Boxed Warning''' for heart failure (do not initiate in NYHA III/IV; can precipitate or worsen HF in any patient)'"`UNIQ--ref-00000826-QINU`"' (1)