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: Tryptamine

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None (26) · Altace (1) · Apresoline (historical); mostly generic; combination with isosorbide dinitrate marketed as BiDil for self-identified Black patients with HFrEF (1) · Avapro (1) · Benicar (1) · Calan, Calan SR, Verelan, Verelan PM, Isoptin SR (1) · Cardizem, Tiazac, Cartia XT, Dilacor XR, Taztia XT, Matzim LA (1) · Cardura, Cardura XL (1) · Coreg, Coreg CR (1) · Cozaar (1) · Diovan; Entresto (in fixed-dose combination with sacubitril) (1) · Folvite; mostly generic (1) · Generic; huge OTC presence (1) · Generic; many OTC formulations (1) · Hytrin (US brand discontinued); mostly generic (1) · Kapvay (ER, ADHD), Catapres (IR, antihypertensive), Catapres-TTS (transdermal patch), Duraclon (epidural injection) (1) · Lotensin (1) · Many generics/OTC (1) · Many OTC and Rx; Nascobal (intranasal); generic injection (1) · Micardis (1) · Microzide; mostly prescribed generically (1) · Niaspan (ER, Rx), Niacor (IR, Rx); huge OTC presence (1) · Norvasc, Katerzia (1) · Procardia, Procardia XL, Adalat CC, Afeditab CR (1) · Tenormin (1) · Thalitone; mostly prescribed generically (1) · Timoptic (ophthalmic), Timoptic-XE (gel-forming once-daily), Istalol (once-daily 0.5%), Betimol; Blocadren (oral, discontinued in many markets); combination eye drops Combigan (with brimonidine), Cosopt (with dorzolamide) (1) · Trandate, Normodyne (discontinued in US) (1) · Vasotec, Vasotec IV, Epaned (1) · Zestril, Prinivil, Qbrelis (1)

None (26) · 0.4 mg PO daily (general prevention); 0.8-1 mg/d in pregnancy; 4 mg/d for women with prior NTD-affected pregnancy; 1 mg/d during methotrexate therapy (1) · 1 mg PO at bedtime to limit first-dose syncope; titrate weekly to 5-10 mg (1) · 10 mg PO once daily (5 mg if on a diuretic); titrate to 40 mg (1) · 12.5-25 mg PO once daily (1) · 12.5-25 mg PO once daily; titrate to 50 mg (1) · 150 mg PO once daily; titrate to 300 mg if needed (1) · 2.5 mg PO once daily (1.25 mg in CHF or volume depletion); titrate to 5-10 mg/d (1) · 2.5-5 mg PO once daily; titrate to 10 mg/d (1) · 20 mg PO once daily; titrate to 40 mg/d after 2 weeks if needed (1) · 25-50 mg PO once daily; titrate to 100 mg/day (1) · 40 mg PO once daily; titrate to 80 mg (1) · 5-10 mg PO once daily (2.5 mg if on diuretic or in heart failure); titrate to 10-20 mg BID for HFrEF (1) · 5-10 mg PO once daily (2.5 mg in heart failure, hyponatremia, or volume depletion) (1) · 50 mg PO daily (25 mg in volume depletion or hepatic impairment) (1) · 80-160 mg PO once daily (40 mg BID in HFrEF, titrating up to 160 mg BID) (1) · ADHD (Kapvay ER): 0.1 mg PO at bedtime, titrate weekly to 0.4 mg/day divided BID. HTN (IR): 0.1 mg PO BID, titrate by 0.1 mg increments (1) · ER 180-240 mg PO once daily; IR 30 mg PO QID; IV 0.25 mg/kg over 2 min for acute rate control, then 5-15 mg/h infusion (1) · ER 30-60 mg PO once daily; immediate-release 10 mg PO TID (now rarely used for hypertension due to reflex tachycardia) (1) · General supplementation 75-90 mg/d (RDA); scurvy treatment 100-1000 mg/d for several weeks; megadose claims unsupported (1) · Heart failure: 3.125 mg PO BID, doubling every 2 weeks as tolerated to target 25 mg BID (50 mg BID if >85 kg). Hypertension: 6.25 mg PO BID, titrate to 25 mg BID (1) · IR 1 mg PO at bedtime, titrate weekly; XL 4-8 mg PO daily (1) · IR 80-120 mg PO TID; ER 180-240 mg PO daily; IV 2.5-5 mg over 2 min for SVT termination (under monitoring); cluster prophylaxis up to 480-960 mg/d in divided doses (1) · Migraine prophylaxis: 400 mg PO daily; deficiency replacement 5-30 mg/d (1) · Niaspan ER 500 mg PO at bedtime, titrate weekly to 1-2 g/d; flushing-protective aspirin 30-60 minutes before dose; pellagra replacement 100-500 mg/d (1) · Ophthalmic: 1 drop 0.5% in affected eye(s) BID (or once daily for XE / Istalol). Oral hypertension: 10 mg PO BID, titrate to 60 mg/day. Migraine prophylaxis: 10 mg BID, titrate to 30 mg/day (1) · Oral: 100 mg PO BID, titrate to 400 mg BID. IV: 20 mg over 2 minutes, repeat 40-80 mg every 10 minutes as needed (maximum cumulative 300 mg); continuous infusion 2 mg/minute (1) · PO 10 mg QID; IV 5-10 mg every 20-30 minutes for hypertensive emergency (1) · Replacement: 1000 mcg IM daily for 1 week, then weekly for 4 weeks, then monthly; or 1000-2000 mcg PO daily (effective even in pernicious anemia via passive diffusion); intranasal 500 mcg weekly (1) · Replacement: 15-30 mg (22.5-45 IU) daily; NASH: 800 IU daily; AREDS-2: 400 IU daily (in combination formula) (1)

None (26) · 0.4, 0.8, 1 mg OTC; 1 mg Rx; 5 mg/mL injection (1) · 1, 2, 4, 8 mg IR tablets; 4, 8 mg XL tablets (1) · 1, 2, 5, 10 mg capsules and tablets (1) · 1.25, 2.5, 5, 10 mg capsules (1) · 10, 20 mg IR capsules; 30, 60, 90 mg ER tablets (1) · 10, 25, 50, 100 mg tablets; 20 mg/mL IV (1) · 100, 200, 400 IU softgels and capsules; many proprietary OTC blends; combined formulations (AREDS-2) (1) · 100, 250, 500, 1000 mg tablets, chewables, gummies, effervescent; IV (specialty) (1) · 100, 250, 500, 1000, 5000 mcg tablets (OTC and Rx); 1000 mcg/mL injection; intranasal spray; sublingual (1) · 12.5 mg capsules; 12.5, 25, 50 mg tablets (1) · 15 mg, 25 mg, 50 mg tablets (1) · 2.5, 5, 10 mg tablets; 1 mg/mL oral suspension (1) · 2.5, 5, 10, 20 mg tablets; 1 mg/mL oral solution (Epaned); 1.25 mg/mL IV (enalaprilat) (1) · 2.5, 5, 10, 20, 30, 40 mg tablets; 1 mg/mL oral solution (1) · 20, 40, 80 mg tablets (1) · 25 mg, 50 mg, 100 mg tablets (1) · 25, 50, 100, 250, 400 mg tablets; OTC (1) · 40, 80, 160, 320 mg tablets; oral suspension (1) · 5, 10, 20, 40 mg tablets (1) · 5, 20, 40 mg tablets (1) · 75, 150, 300 mg tablets (1) · IR 30, 60, 90, 120 mg tablets; multiple ER capsules and tablets 60-420 mg; IV 5 mg/mL (1) · IR 40, 80, 120 mg tablets; SR/ER 100-360 mg; IV 2.5 mg/mL (1) · IR tablets 0.1, 0.2, 0.3 mg; ER tablets 0.1, 0.2 mg (Kapvay); transdermal patches 0.1, 0.2, 0.3 mg/24h (TTS-1/2/3, weekly); epidural injection (Duraclon) (1) · IR tablets 3.125, 6.25, 12.5, 25 mg; Coreg CR capsules 10, 20, 40, 80 mg (once-daily) (1) · OTC IR niacin 50-500 mg tablets; Niaspan ER 500, 750, 1000 mg tablets; "no-flush" niacin (inositol hexaniacinate, lacks evidence) (1) · Tablets 100, 200, 300 mg; injection 5 mg/mL (1) · Tablets 25, 50, 100 mg (1) · Tablets 5, 10, 20 mg; ophthalmic solution 0.25%, 0.5%; ophthalmic gel-forming solution 0.25%, 0.5% (Timoptic-XE) (1)

None (26) · 1 mg/d typical Rx; higher in specific indications (1) · 10 mg/d (1) · 100 mg/d (1) · 100 mg/d (rarely used) (1) · 100-200 mg/day depending on indication (1) · 120 mg/d (ER); IR not for chronic hypertension (1) · 16 mg/d (IR); 8 mg/d (XL) (1) · 2 g/d (Niaspan); higher off-label use historical (1) · 2.4 mg/day (HTN, IR); 0.4 mg/day (ADHD, Kapvay) (1) · 20 mg/d (1) · 20 mg/d (hypertension); 10 mg/d (other indications typical) (1) · 2400 mg/day (oral); 300 mg total per IV bolus dosing series (1) · 300 mg/d (1) · 300 mg/d typical practical limit (toxicity rises sharply above) (1) · 320 mg/d (hypertension); 320 mg/d (HF) (1) · 40 mg/d (2) · 50 mg BID in heart failure (or once-daily equivalent CR); 25 mg BID in hypertension (1) · 50 mg/d (hypertension); up to 200 mg/d (edema) (1) · 60 mg/day (oral, hypertension); 0.5% BID (ophthalmic) (1) · 80 mg/d (3) · No strict ceiling for water-soluble vitamin; UL not set (1) · No strict ceiling; water-soluble vitamin, low toxicity (1) · UL 1000 mg (~1500 IU natural)/d in adults; routinely exceeded in older AREDS-1 trials (1) · UL 2000 mg/d in adults (1) · ~480 mg/d (oral) for cardiovascular indications; higher off-label for cluster (1) · ~480 mg/d (oral); IV per protocol (1)

None (26) · epidural injection (1) · IM (3) · intranasal (1) · intravenous (1) · IV (7) · IV (rare) (1) · MI reports) (1) · multiple ER formulations) (1) · ophthalmic (1) · Oral (26) · Oral (IR (1) · Oral (IR and multiple ER) (1) · Oral; sublingual IR is discouraged (uncontrolled BP drops (1) · SC (2) · sublingual (1) · transdermal (1)

None (26) · 30-60 min (IR oral); 2-3 days to steady state (transdermal patch) (1) · Antihypertensive effect within 1 week; heart-failure mortality benefit accrues over months of titration (1) · BP and symptomatic LUTS improvement within 1-2 weeks (2) · BP effect 1 hour; max at 4-6 hours (1) · BP effect 1-2 hours; max at 6 hours (1) · BP effect 1-2 weeks; antihypertensive peak 3-6 weeks (1) · BP effect 1-2 weeks; max at 2-3 weeks (1) · BP effect 2 hours; max at 4-6 weeks (1) · BP effect within 1-2 weeks (2) · BP effect within 24 hours; full effect at 1-2 weeks (long half-life) (1) · BP effect within hours (oral); 5-10 minutes (IV) (1) · BP effect within hours (oral); IOP reduction within 30 minutes, full effect 1-2 weeks (ophthalmic) (1) · BP effect within hours; full effect over 1-2 weeks (1) · BP lowering within 1 hour; max at 6 hours (1) · BP lowering within 1 hour; max effect at 6 hours (1) · Days for symptom improvement in scurvy (1) · Days to weeks for tissue saturation (1) · Diuresis at 2 hours; antihypertensive effect within days, max at 3-4 weeks (1) · Diuresis at 2-3 hours; BP effect over weeks (1) · Hematologic response within days (1) · IR 20 minutes; ER ~6 hours (1) · IV: 1-3 minutes (SVT termination); PO IR: 30-60 minutes; ER: hours (1) · IV: 3-7 minutes (rate control); PO IR: 30-60 minutes; ER: hours (1) · IV: 5-20 minutes; PO: 30-60 minutes (1) · Lipid changes 4-8 weeks (1) · Migraine effect after 1-3 months of daily use (1) · Reticulocyte response at 3-5 days; neurologic recovery weeks to months (and may be incomplete if longstanding) (1)

None (26) · 12 hours (oral BID); 24 hours (Timoptic-XE) (1) · 12-24 hours (1) · 24 hours (12) · 24 hours (once-daily dosing supported by long elimination) (1) · 48-72 hours per dose (much longer than hydrochlorothiazide) (1) · 6-12 hours (1) · 8-12 hours (IR); ~7 days (transdermal patch) (1) · 8-12 hours (oral); 4-6 hours (IV) (1) · Hours (1) · IR 4-8 hours; ER 24 hours (1) · IR: 4-8 hours; ER: 24 hours (1) · IR: 6-8 hours; ER: 24 hours (1) · IV: 1-4 hours; PO: 3-8 hours (1) · N/A (1) · N/A (replacement) (2) · Weeks (fat-soluble) (1) · ~12 hours (IR); 24 hours (CR) (1)

None (26) · 42-58% (oral; dose-dependent)'"`UNIQ--ref-00000AEF-QINU`"' (1) · 60-80% (oral; not significantly affected by food)'"`UNIQ--ref-00000843-QINU`"' (1) · 64-90% (oral; not affected by food)'"`UNIQ--ref-00000079-QINU`"' (1) · 65-75% (oral)'"`UNIQ--ref-0000013F-QINU`"' (1) · >90% (oral; not significantly affected by food)'"`UNIQ--ref-00001120-QINU`"' (1) · High (oral) (1) · High (oral; food enhances)'"`UNIQ--ref-00001039-QINU`"' (1) · High with fat-containing meal; reduced in malabsorption (1) · Oral ~1-3% via passive diffusion at high doses (independent of intrinsic factor); IM/SC ~100% (1) · ~20-35% (oral; extensive first-pass via CYP3A4 with R/S enantiomer differences)'"`UNIQ--ref-00000A6C-QINU`"' (1) · ~25% (oral; extensive first-pass)'"`UNIQ--ref-0000001B-QINU`"' (1) · ~25% (oral; food does not affect absorption)'"`UNIQ--ref-0000005A-QINU`"' (1) · ~25% (oral; food reduces absorption ~40%)'"`UNIQ--ref-000004CE-QINU`"' (1) · ~25-35% (extensive first-pass), increased by food which slows absorption and reduces orthostatic risk'"`UNIQ--ref-0000001C-QINU`"' (1) · ~25-50% (oral; substantial first-pass via NAT2 acetylation, phenotype-dependent)'"`UNIQ--ref-00000688-QINU`"' (1) · ~26% (oral; prodrug hydrolyzed by intestinal esterases to active olmesartan; not affected by food)'"`UNIQ--ref-0000056D-QINU`"' (1) · ~28% (oral; food slows but does not reduce absorption)'"`UNIQ--ref-00000C33-QINU`"' (1) · ~33% (extensive first-pass via CYP2C9 and CYP3A4)'"`UNIQ--ref-000000BD-QINU`"' (1) · ~37% (oral; food does not affect)'"`UNIQ--ref-00000A23-QINU`"' (1) · ~40% (oral; extensive first-pass via CYP3A4)'"`UNIQ--ref-00000643-QINU`"' (1) · ~50% (oral); systemic absorption from ophthalmic application is clinically meaningful via nasolacrimal drainage'"`UNIQ--ref-0000001C-QINU`"' (1) · ~50% (oral)'"`UNIQ--ref-00000021-QINU`"' (1) · ~50% IR (extensive first-pass via CYP3A4); ER products release-rate-limited'"`UNIQ--ref-0000074E-QINU`"' (1) · ~50-60% (oral; food enhances) (1) · ~60% (oral; food does not affect absorption)'"`UNIQ--ref-00000B85-QINU`"' (1) · ~65% (oral)'"`UNIQ--ref-00000784-QINU`"' (1) · ~65% (oral)'"`UNIQ--ref-00000AB1-QINU`"' (1) · ~70-90% at typical doses; saturable at high doses (>500 mg) (1) · ~75-85% (oral); ~60% (transdermal at steady state)'"`UNIQ--ref-00000027-QINU`"' (1)

None (26) · OTC (low-dose) and [[USLegal:Prescription only|Rx-only]] (1 mg, injectable) in US (1) · OTC (low-dose, dietary supplement) and [[USLegal:Prescription only|Rx-only]] (Niaspan ER) in US (1) · OTC (low/mid-dose oral) and [[USLegal:Prescription only|Rx-only]] (injection, intranasal) in US (1) · OTC in US (3) · [[USLegal:Prescription only|Rx-only]] in US (22) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, like guanfacine and unlike the psychostimulant alternatives for ADHD'"`UNIQ--ref-00000028-QINU`"' (1)