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Medicines > classes : Antidepressant or Research material or [[:Category:Nitrates|Organic nitrate]]

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generic:
brand:
None (131) · (none, never marketed) (1) · Anafranil (1) · Aurorix (1) · Cymbalta, Drizalma Sprinkle, Irenka, Yentreve (1) · Edronax (1) · Fetzima (1) · Imdur (mononitrate ER), Isordil (dinitrate); generics; with hydralazine as BiDil for HFrEF in self-identified Black patients (1) · Ludiomil (1) · Marplan (1) · Nardil (1) · Nitrostat, Nitrolingual, NitroMist, Nitro-Bid, Nitro-Dur, Minitran, Rectiv (1) · Norpramin (1) · O-DSMT (1) · Parnate (1) · Savella (1) · Serzone (1) · Stablon (1) · Surmontil (1) · Tofranil (1) · Valdoxan (1) · Vivactil (1) · Zoloft (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) · Irreversible non-selective MAO inhibitor (3) · Selective norepinephrine reuptake inhibitor (3) · Serotonin and norepinephrine reuptake inhibitor (3) · Serotonin/norepinephrine/dopamine releasing agent (3) · None (2) · Cathinone analogue; monoamine reuptake inhibitor (2) · Dopamine and norepinephrine reuptake inhibitor (2) · NMDA antagonist (2) · Prodrug of GHB (2) · Serotonin–norepinephrine reuptake inhibitor (2)
uses:
None (149) · Depression, anxiety, neuropathic pain, fibromyalgia, chronic musculoskeletal pain (1) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000C0A-QINU`"', '"`UNIQ--vote-00000C0B-QINU`"', '"`UNIQ--vote-00000C0C-QINU`"', '"`UNIQ--vote-00000C0D-QINU`"', '"`UNIQ--vote-00000C0E-QINU`"' (1) · '"`UNIQ--vote-0000145E-QINU`"', '"`UNIQ--vote-0000145F-QINU`"', '"`UNIQ--vote-00001460-QINU`"' (1)
starting dose:
None (149) · 25 mg (1) · Isosorbide mononitrate ER: 30-60 mg PO once daily in the morning, titrate to 120-240 mg/d; isosorbide dinitrate IR: 5-20 mg PO TID with a 12-14 hour nitrate-free interval to prevent tolerance (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · SL 0.3-0.6 mg every 5 minutes up to 3 doses for acute angina (call EMS if not resolved after the third); IV infusion 5-10 mcg/min titrated; transdermal patch 0.2-0.4 mg/hr for 12-14 hours daily (nitrate-free interval prevents tolerance) (1)
preparations:
None (149) · 25 mg, 50 mg, 100 mg tablets; oral concentrate 20 mg/mL (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · Mononitrate 10, 20 mg IR; 30, 60, 120 mg ER; dinitrate 5, 10, 20, 30, 40 mg IR and ER (1) · SL 0.3, 0.4, 0.6 mg tablets; lingual spray 0.4 mg/spray; ER 2.5-9 mg capsules; transdermal patch 0.1-0.8 mg/hr; 2% ointment; 0.4% rectal ointment; 5 mg/mL IV (1)
fda max:
None (149) · 200 mg/d (1) · 240 mg/d (mononitrate ER); 160 mg/d (dinitrate) (1) · Indication-specific; titrated to effect (1) · N/A (never approved) (1)
routes:
None (148) · intranasal; rectal and IV reported. (1) · IV (1) · lingual spray (1) · Oral (4) · oral ER (1) · rectal (1) · sublingual (2) · sublingual (dinitrate) (1) · topical (1) · transdermal (1)
onset:
None (148) · Anxiolysis classically 3-4 weeks, continuing improvement to 8-12 weeks (1) · Mood: 2–4 weeks. Pain: often within 1–2 weeks. (1) · SL/spray: 1-3 minutes; IV: minutes; patch: 30-60 minutes (1) · SL: 2-5 minutes; PO mononitrate: 30-60 minutes (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (148) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Chronic daily dosing (1) · Long (1) · Mononitrate ER: 12-24 hours; dinitrate IR: 4-6 hours (1) · SL: 30 minutes; patch: 12-14 hours; IV continuous (1)
halflife:
None (148) · 1-3 minutes (very short)'"`UNIQ--ref-00000C0F-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Mononitrate ~5 hours; dinitrate ~1 hour'"`UNIQ--ref-00001461-QINU`"' (1) · ~12 hours (1) · ~26 h (sertraline; range 13-45 h, longer in females); ~62-104 h (N-desmethylsertraline, weakly active) (1)
bioavailability:
None (148) · Absolute bioavailability not precisely characterized; food modestly increases exposure (1) · Highly route-dependent: SL bypasses first-pass; oral has extensive first-pass (used only for chronic ER preparations); transdermal predictable'"`UNIQ--ref-00000C10-QINU`"' (1) · Mononitrate ~100% (no first-pass; the principal advantage over dinitrate); dinitrate ~20%'"`UNIQ--ref-00001462-QINU`"' (1) · Not formally characterized in humans. (1) · ~50% (highly variable) (1)
pregnancy:
None (148) · 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 C (1) · Category C'"`UNIQ--ref-0000008F-QINU`"' (1) · Limited data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Used in obstetric emergencies (uterine relaxation, severe hypertension) when needed; otherwise limited routine use.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (149) · Rx-only (1) · Rx-only in US (1) · [[USLegal:Prescription only|Rx-only]] in US (2)

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