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Medicines > classes : PDE5 Inhibitor or Research material

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generic:
brand:
None (130) · (none, never marketed) (1) · Cialis, Adcirca (1) · Levitra, Staxyn (1) · O-DSMT (1) · Stendra (1) · Viagra, Revatio (1)
classes: (Click arrow to add another value)
mechanism:
5-HT2A agonist (26) · Monoamine releasing agent (9) · GABAA positive allosteric modulator (8) · CB1/CB2 agonist (7) · Dopamine/norepinephrine reuptake inhibitor (5) · Potent 5-HT2A agonist (5) · LSD analogue; 5-HT2A agonist (4) · Prodrug of LSD; 5-HT2A agonist (4) · Serotonin/norepinephrine/dopamine releasing agent (3) · Cathinone analogue; monoamine reuptake inhibitor (2) · Dopamine and norepinephrine reuptake inhibitor (2) · NMDA antagonist (2) · Prodrug of GHB (2)
uses:
None (131) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000040-QINU`"' (1) · '"`UNIQ--vote-00000669-QINU`"' (1) · '"`UNIQ--vote-00000705-QINU`"', '"`UNIQ--vote-00000706-QINU`"' (1) · '"`UNIQ--vote-00000738-QINU`"', '"`UNIQ--vote-00000739-QINU`"', '"`UNIQ--vote-0000073A-QINU`"' (1)
starting dose:
None (131) · 10 mg PRN; 2.5–5 mg daily for continuous coverage / BPH (1) · 10 mg ~1 h before sexual activity (1) · 100 mg ~15 min before sexual activity (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)
preparations:
None (131) · 2.5, 5, 10, 20 mg tabs (1) · 2.5, 5, 10, 20 mg tabs (Levitra); 10 mg ODT (Staxyn) (1) · 25, 50, 100 mg tabs (Viagra); 20 mg tabs and 10 mg/mL oral suspension (Revatio) (1) · 50, 100, 200 mg tabs (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
None (131) · 100 mg/d (ED); 20 mg TID (PAH) (1) · 20 mg/d (1) · 20 mg/d (ED, PRN); 5 mg/d (daily / BPH); 40 mg/d (PAH) (1) · 200 mg/d (100 mg/d if on CYP3A4 inhibitors) (1) · N/A (never approved) (1)
routes:
None (131) · intranasal; rectal and IV reported. (1) · IV (Revatio) (1) · Oral (5) · sublingual (1)
onset:
None (131) · 30 min (1) · 30–60 min (1) · ~15 min (fastest of the PDE5 inhibitors) (1) · ~20–40 min PO; faster sublingual/intranasal. (1) · ~30 min (1)
duration:
None (131) · 4–5 h (1) · 4–6 h (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Up to 36 h ("the weekend pill") (1) · ~4 h (1)
halflife:
None (131) · 4–5 h (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~17.5 h (1) · ~4 h (1) · ~5 h (1)
bioavailability:
None (131) · Not formally characterized in humans. (1) · Rapid absorption; absolute bioavailability not formally established (1) · Reasonable (not formally established as a percentage) (1) · ~15% (extensive hepatic first-pass) (1) · ~40% (1)
pregnancy:
None (131) · 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 (3) · Category C (not relevant; not used in women) (1)
legal:
None (132) · Rx-only in US (4)

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