Drilldown: Medicines

Bromazolam (1) · Dexmethylphenidate (1) · Linagliptin (1) · Sildenafil (1) · Sitagliptin (1)

(none, never marketed) (1) · Focalin, Focalin XR (1) · Januvia; with metformin Janumet/Janumet XR (1) · Tradjenta; with metformin Jentadueto (1) · Viagra, Revatio (1)

CNS stimulant (1) · Designer benzodiazepine (1) · NDRI (1) · PDE5 Inhibitor (1) · Psychostimulant (1) · Research material (1) · Sedative-Hypnotic (1) · Triazolobenzodiazepine (1) · [[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (2) · [[:Category:DPP-4_inhibitors|DPP-4 inhibitor]] (2) · [[:Category:Incretin_modulators|Incretin pathway modulator]] (2)

None (1) · Norepinephrine–dopamine reuptake inhibition (DAT, NET), d-threo enantiomer of methylphenidate (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) · Selective inhibitor of phosphodiesterase type 5 (PDE5), preventing cGMP breakdown in vascular smooth muscle. In the corpus cavernosum, potentiates the NO/cGMP cascade triggered by sexual stimulation. (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-00000150-QINU`"', '"`UNIQ--vote-00000151-QINU`"' (1) · '"`UNIQ--vote-00000705-QINU`"', '"`UNIQ--vote-00000706-QINU`"' (1) · '"`UNIQ--vote-00000764-QINU`"' (1) · '"`UNIQ--vote-0000117B-QINU`"' (1)

None (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) · 50 mg ~1 h before sexual activity (ED); 20 mg TID (PAH) (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

None (1) · 25, 50, 100 mg tablets; combination tablets with metformin (1) · 25, 50, 100 mg tabs (Viagra); 20 mg tabs and 10 mg/mL oral suspension (Revatio) (1) · 5 mg tablets; combination with metformin (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)

None (1) · 100 mg/d (1) · 100 mg/d (ED); 20 mg TID (PAH) (1) · 5 mg/d (1) · N/A (never approved) (1)

intranasal; rectal and IV reported. (1) · IV (Revatio) (1) · 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 (2) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · IR 4–6 h; XR 8–12 h (1) · ~4 h (1)

2.2 h (IR parent); ~3 h (XR parent) (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) · ~4 h (1)

Not formally characterized in humans. (1) · ~22–25% (1) · ~30% (oral)'"`UNIQ--ref-0000117D-QINU`"' (1) · ~40% (1) · ~87% (oral)'"`UNIQ--ref-00000766-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) · Category B (1) · Category C (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) · Rx-only in US (1) · Schedule II (1) · [[USLegal:Prescription only|Rx-only]] in US (2)