Drilldown: Medicines
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generic:
brand:
classes:
Dual orexin receptor antagonist (DORA) (3) ·
the first approved (1) ·
[[:Category:Anti-inflammatories|Anti-inflammatory]] (1) ·
[[:Category:Antigout_agents|Antigout agent]] (1) ·
[[:Category:B-vitamins|B-vitamin]] (2) ·
[[:Category:Hematinics|Hematinic]] (3) ·
[[:Category:Iron_supplements|Iron supplement]] (1) ·
[[:Category:Microtubule_inhibitors|Microtubule inhibitor]] (1) ·
[[:Category:Vitamins|Vitamin]] (2)
mechanism:
None (5) ·
Competitive antagonist at OX1R and OX2R. Faster receptor association/dissociation kinetics than suvorexant (~16 sec dissociation vs ~57 sec) hypothesized to support sleep onset, with sufficient duration for maintenance. (1) ·
Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (1)
uses:
Insomnia (sleep onset and/or maintenance) in adults (FDA-approved August 2014). Also studied for insomnia in mild-moderate Alzheimer disease. (1) ·
Insomnia (sleep onset and/or maintenance) in adults (FDA-approved Dec 2019) (1) ·
Insomnia (sleep onset and/or sleep maintenance) in adults (FDA-approved Jan 2022) (1) ·
'"`UNIQ--vote-0000059A-QINU`"', '"`UNIQ--vote-0000059B-QINU`"' (1) ·
'"`UNIQ--vote-000005B3-QINU`"', '"`UNIQ--vote-000005B4-QINU`"', '"`UNIQ--vote-000005B5-QINU`"', '"`UNIQ--vote-000005B6-QINU`"' (1) ·
'"`UNIQ--vote-00000607-QINU`"', '"`UNIQ--vote-00000608-QINU`"', '"`UNIQ--vote-00000609-QINU`"', '"`UNIQ--vote-0000060A-QINU`"' (1) ·
'"`UNIQ--vote-00000C6D-QINU`"', '"`UNIQ--vote-00000C6E-QINU`"', '"`UNIQ--vote-00000C6F-QINU`"', '"`UNIQ--vote-00000C70-QINU`"', '"`UNIQ--vote-00000C71-QINU`"' (1)
starting dose:
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) ·
10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) ·
25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) ·
325 mg PO daily to TID (=65 mg elemental iron/tablet); alternate-day dosing is now favored by hepcidin physiology for better absorption with less GI burden (1) ·
5 mg PO at bedtime; may increase to 10 mg if inadequate (1) ·
Acute gout: 1.2 mg PO at first symptom, then 0.6 mg 1 hour later (total 1.8 mg in 1 hour, the FDA-revised regimen); prophylaxis 0.6 mg PO daily or BID; FMF 1-2 mg/d; pericarditis 0.5-0.6 mg BID for 3 months; Lodoco 0.5 mg PO daily for CV risk reduction (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)
preparations:
0.4, 0.8, 1 mg OTC; 1 mg Rx; 5 mg/mL injection (1) ·
0.6 mg tablets; 0.6 mg/5 mL solution; 0.5 mg tablets (Lodoco) (1) ·
100, 250, 500, 1000, 5000 mcg tablets (OTC and Rx); 1000 mcg/mL injection; intranasal spray; sublingual (1) ·
25 mg, 50 mg tablets (1) ·
325 mg tablets (65 mg elemental Fe); 220 mg/5 mL liquid (44 mg elemental Fe/5 mL); 142 mg/mL drops; OTC and Rx (1) ·
5 mg, 10 mg tablets (1) ·
5 mg, 10 mg, 15 mg, 20 mg tablets (1)
fda max:
1 mg/d typical Rx; higher in specific indications (1) ·
1.8 mg in any 1-hour period (acute gout); 1.2 mg/d (prophylaxis with renal/hepatic impairment); much lower with strong CYP3A4 or P-gp inhibitors (1) ·
10 mg/d (1) ·
20 mg/d (1) ·
50 mg/d (1) ·
No strict ceiling; water-soluble vitamin, low toxicity (1) ·
~200 mg elemental iron/d typical practical limit (1)
routes:
onset:
Anti-inflammatory effect within 24 hours of gout flare onset; loses effectiveness if delayed (1) ·
Hematologic response within days (1) ·
Reticulocyte response at 3-5 days; neurologic recovery weeks to months (and may be incomplete if longstanding) (1) ·
Reticulocyte response at 7-10 days; hemoglobin rise of ~1 g/dL per 3 weeks (1) ·
~30 min (3)
duration: (Click arrow to add another value)
halflife:
N/A (incorporated into hemoglobin and tissue stores) (1) ·
~0.5 hours plasma; tissue retention longer (1) ·
~12 hours (1) ·
~17-19 hours (longer than daridorexant) (1) ·
~27-31 hours; markedly prolonged in renal/hepatic impairment and with CYP3A4 or P-gp inhibitors'"`UNIQ--ref-00000C72-QINU`"' (1) ·
~6 days (plasma); hepatic stores last 3-5 years (1) ·
~8 hours (shorter than suvorexant and lemborexant) (1)
bioavailability:
pregnancy:
Limited data; avoid (3) ·
Routinely supplemented in pregnancy and preconception to prevent neural tube defects.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Routinely supplemented in vegan pregnancies and pernicious anemia.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Routinely used; iron requirements rise substantially in pregnancy and lactation.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Used in FMF in pregnancy; otherwise weigh against alternatives.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1)
Showing below up to 7 results in range #1 to #7.