Drilldown: Medicines

Azithromycin (1) · Bromazolam (1) · Fluconazole (1) · Linagliptin (1) · Sitagliptin (1)

(none, never marketed) (1) · Diflucan (1) · Januvia; with metformin Janumet/Janumet XR (1) · Tradjenta; with metformin Jentadueto (1) · Zithromax, Z-Pak, Zmax (1)

Designer benzodiazepine (1) · Research material (1) · Sedative-Hypnotic (1) · Triazolobenzodiazepine (1) · [[:Category:Antifungals|Antifungal (triazole)]] (1) · [[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (2) · [[:Category:Azalides|Azalide]] (1) · [[:Category:DPP-4_inhibitors|DPP-4 inhibitor]] (2) · [[:Category:Incretin_modulators|Incretin pathway modulator]] (2) · [[:Category:Macrolide_antibiotics|Macrolide antibiotic]] (1) · [[:Category:Triazoles|Triazole]] (1)

None (3) · 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-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)

No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-000003F6-QINU`"', '"`UNIQ--vote-000003F7-QINU`"', '"`UNIQ--vote-000003F8-QINU`"', '"`UNIQ--vote-000003F9-QINU`"', '"`UNIQ--vote-000003FA-QINU`"', '"`UNIQ--vote-000003FB-QINU`"' (1) · '"`UNIQ--vote-00000764-QINU`"' (1) · '"`UNIQ--vote-00000A42-QINU`"', '"`UNIQ--vote-00000A43-QINU`"', '"`UNIQ--vote-00000A44-QINU`"', '"`UNIQ--vote-00000A45-QINU`"', '"`UNIQ--vote-00000A46-QINU`"' (1) · '"`UNIQ--vote-0000117B-QINU`"' (1)

100 mg PO once daily (50 mg if CrCl 30-44; 25 mg if <30 or dialysis) (1) · 5 mg PO once daily (no renal dose adjustment, unlike sitagliptin) (1) · 500 mg PO day 1, then 250 mg PO daily days 2-5 (Z-Pak); 1 g PO single dose for chlamydia; pediatric dosing 10 mg/kg day 1, 5 mg/kg days 2-5 (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · Vulvovaginal: 150 mg PO single dose; oropharyngeal: 200 mg PO day 1, then 100 mg daily ×14 days; invasive candidiasis: 800 mg load, then 400 mg PO/IV daily; cryptococcal meningitis: 400-800 mg/d (1)

25, 50, 100 mg tablets; combination tablets with metformin (1) · 250 mg, 500 mg, 600 mg tablets; 100, 200 mg/5 mL suspension; 2 g ER suspension (Zmax); 500 mg IV (1) · 5 mg tablets; combination with metformin (1) · 50, 100, 150, 200 mg tablets; 10, 40 mg/mL oral suspension; 2 mg/mL IV (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)

100 mg/d (1) · 5 mg/d (1) · 500 mg/d (typical regimen); single 2 g for Zmax; 2 g for select STIs (1) · 800 mg/d (severe invasive disease) (1) · N/A (never approved) (1)

intranasal; rectal and IV reported. (1) · IV (2) · Oral (5) · sublingual (1)

None · Hours · 30-60 minutes · 1-2 hours · ~30 min · LDL lowering at 2 weeks, max by 4 weeks · ~1 hour · 15-30 minutes · 15–30 min · 1–2 h · 30–60 min · Antidepressant effect emerges over 1-2 weeks · BP and symptomatic LUTS improvement within 1-2 weeks · BP effect within 1-2 weeks · Clinical improvement within 24-72 hours · Days · Motor improvement over days at therapeutic dose · Over weeks · Postprandial glucose effect within days; HbA1c by 12 weeks · Sleep effect from first dose; antidepressant effect over 1-4 weeks

Other values:

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24 hours (3) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Tissue half-life supports once-daily and post-treatment effect (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-00000765-QINU`"' (1) · ~30 hours (long, supports once-daily dosing and substantial drug-interaction window after discontinuation)'"`UNIQ--ref-00000A47-QINU`"' (1) · ~68 hours (terminal; reflects deep tissue accumulation, much longer than plasma)'"`UNIQ--ref-000003FC-QINU`"' (1)

>90% (oral; not affected by food or gastric pH — a major practical advantage over itraconazole)'"`UNIQ--ref-00000A48-QINU`"' (1) · Not formally characterized in humans. (1) · ~30% (oral)'"`UNIQ--ref-0000117D-QINU`"' (1) · ~37% (oral; food reduces absorption modestly)'"`UNIQ--ref-000003FD-QINU`"' (1) · ~87% (oral)'"`UNIQ--ref-00000766-QINU`"' (1)

None (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) · Generally considered safe; commonly used in pregnancy when macrolide indicated.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; switch to insulin where feasible.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2)

None (1) · [[USLegal:Prescription only|Rx-only]] in US (4)