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Medicines > classes : Research material or [[:Category:Beta-lactam_antibiotics|β-lactam antibiotic]]

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generic:
brand:
None (130) · (none, never marketed) (1) · Amoxil, Trimox, Moxatag; mostly prescribed generically (1) · Bicillin L-A (benzathine), Bicillin C-R (combination procaine + benzathine), Pfizerpen (potassium IV) (1) · Ceftin (oral), Zinacef (IV) (1) · Keflex, Daxbia, Panixine; mostly prescribed generically (1) · O-DSMT (1) · Omnicef (discontinued in US under brand); mostly generic (1) · Pen-V, Veetids (mostly generic) (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) · None (5) · 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-0000019B-QINU`"', '"`UNIQ--vote-0000019C-QINU`"', '"`UNIQ--vote-0000019D-QINU`"', '"`UNIQ--vote-0000019E-QINU`"', '"`UNIQ--vote-0000019F-QINU`"', '"`UNIQ--vote-000001A0-QINU`"' (1) · '"`UNIQ--vote-000004ED-QINU`"', '"`UNIQ--vote-000004EE-QINU`"', '"`UNIQ--vote-000004EF-QINU`"', '"`UNIQ--vote-000004F0-QINU`"', '"`UNIQ--vote-000004F1-QINU`"' (1) · '"`UNIQ--vote-000009DF-QINU`"', '"`UNIQ--vote-000009E0-QINU`"', '"`UNIQ--vote-000009E1-QINU`"', '"`UNIQ--vote-000009E2-QINU`"', '"`UNIQ--vote-000009E3-QINU`"' (1) · '"`UNIQ--vote-00000E71-QINU`"', '"`UNIQ--vote-00000E72-QINU`"', '"`UNIQ--vote-00000E73-QINU`"', '"`UNIQ--vote-00000E74-QINU`"', '"`UNIQ--vote-00000E75-QINU`"' (1) · '"`UNIQ--vote-00000FF3-QINU`"', '"`UNIQ--vote-00000FF4-QINU`"', '"`UNIQ--vote-00000FF5-QINU`"', '"`UNIQ--vote-00000FF6-QINU`"', '"`UNIQ--vote-00000FF7-QINU`"', '"`UNIQ--vote-00000FF8-QINU`"' (1) · '"`UNIQ--vote-00001414-QINU`"', '"`UNIQ--vote-00001415-QINU`"', '"`UNIQ--vote-00001416-QINU`"', '"`UNIQ--vote-00001417-QINU`"', '"`UNIQ--vote-00001418-QINU`"' (1)
starting dose:
None (132) · 250-500 mg PO BID × 7-14 days; IV 1.5 g q8h for serious infections (1) · 250-500 mg PO every 6-8 hours (1) · 300 mg PO BID, or 600 mg PO once daily, ×5-10 days; pediatric 14 mg/kg/d (1) · 500 mg PO every 6 hours, or 250 mg every 6 hours for mild infections (1) · 500 mg PO TID or 875 mg PO BID for most indications; 80-90 mg/kg/d divided BID in pediatric otitis media (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
None (131) · 125, 250, 500 mg tablets; 125 mg/5 mL, 250 mg/5 mL suspension; 750 mg, 1.5 g IV vials (1) · 250 mg, 500 mg capsules; 500 mg, 875 mg tablets; 125, 200, 250, 400 mg/5 mL oral suspension; 775 mg ER; 50 mg/mL drops (1) · 250 mg, 500 mg tablets; 125 mg/5 mL, 250 mg/5 mL suspension (1) · 250 mg, 500 mg, 750 mg capsules; 250 mg/5 mL, 125 mg/5 mL suspension; tablets (1) · 300 mg capsules; 125, 250 mg/5 mL suspension (1) · Bicillin L-A 600,000; 1.2M; 2.4M U IM; aqueous crystalline (Pfizerpen) 5M, 20M U IV; procaine 600,000 U/mL IM (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
None (131) · 1 g/d (oral); 6 g/d (IV) (1) · 2 g/d typical (1) · 3 g/d typical; higher in severe infections under specialist guidance (1) · 4 g/d (1) · 600 mg/d (1) · Indication-specific (1) · N/A (never approved) (1)
routes:
None (131) · IM (1) · IM (benzathine (1) · intranasal; rectal and IV reported. (1) · IV (1) · IV (aqueous crystalline); '''NEVER IV for benzathine — fatal cardiopulmonary events reported''' (1) · Oral (6) · procaine) (1) · sublingual (1)
onset:
None (131) · Hours (4) · IV: minutes; IM benzathine: depot levels last weeks (1) · Peak plasma at 1-2 hours; clinical effect within 24-72 hours (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (131) · 12-24 hours (1) · 6-8 hours (2) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · 8-12 hours (1) · IM benzathine: 3-4 weeks of detectable levels (1) · ~8 hours per dose (1)
halflife:
None (131) · 1-1.3 hours'"`UNIQ--ref-000001A1-QINU`"' (1) · Aqueous crystalline ~30 minutes; benzathine effective ~3 weeks via depot release'"`UNIQ--ref-00001419-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~1 hour'"`UNIQ--ref-000004F2-QINU`"' (1) · ~1.5 hours'"`UNIQ--ref-00000FF9-QINU`"' (1) · ~1.7 hours'"`UNIQ--ref-000009E4-QINU`"' (1) · ~30-60 minutes'"`UNIQ--ref-00000E76-QINU`"' (1)
bioavailability:
None (131) · 16-21% capsule, 25% suspension (oral; iron and antacids reduce absorption substantially)'"`UNIQ--ref-000009E5-QINU`"' (1) · 75-90% (oral; minimally affected by food)'"`UNIQ--ref-000001A2-QINU`"' (1) · 90% (oral; food delays but does not reduce absorption)'"`UNIQ--ref-000004F3-QINU`"' (1) · Acid-labile; not effective orally (oral form available outside US as penicillin G salts but penicillin V is preferred for oral use)'"`UNIQ--ref-0000141A-QINU`"' (1) · Not formally characterized in humans. (1) · ~37% (oral, as axetil prodrug; food modestly improves absorption)'"`UNIQ--ref-00000FFA-QINU`"' (1) · ~60% (oral; phenoxymethyl modification makes it acid-stable, unlike penicillin G which is destroyed by gastric acid)'"`UNIQ--ref-00000E77-QINU`"' (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) · Generally considered safe in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2) · Generally considered safe; widely used in pregnancy and lactation.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe; widely used.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2) · Penicillin G is the only fully effective syphilis treatment in pregnancy; penicillin-allergic pregnant patients require desensitization.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (132) · [[USLegal:Prescription only|Rx-only]] in US (6)

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