Drilldown: Medicines
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generic:
brand:
classes:
Dual orexin receptor antagonist (DORA) (1) ·
[[:Category:Alpha-2_agonists|Alpha-2 adrenergic agonist]] (1) ·
[[:Category:Antiasthmatic_agents|Antiasthmatic]] (1) ·
[[:Category:Antihistamines|Antihistamine]] (2) ·
[[:Category:Beta-3_agonists|β3 adrenergic agonist]] (1) ·
[[:Category:Carbonic_anhydrase_inhibitors|Carbonic anhydrase inhibitor (topical)]] (1) ·
[[:Category:Glaucoma_medications|Glaucoma medication]] (2) ·
[[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist (second-generation)]] (2) ·
[[:Category:Leukotriene_receptor_antagonists|Leukotriene receptor antagonist]] (1) ·
[[:Category:Ocular_hypotensive_agents|Ocular hypotensive agent]] (2) ·
[[:Category:Overactive_bladder_medications|Overactive bladder medication]] (1)
mechanism:
None (5) ·
'"`UNIQ--vote-00000391-QINU`"' Minimal CYP metabolism; mostly renally cleared unchanged. Cetirizine is the active racemate; levocetirizine is the active R-enantiomer marketed separately'"`UNIQ--ref-00000392-QINU`"'. (1) ·
'"`UNIQ--vote-0000061E-QINU`"' Less reliably anticholinergic than first-generation H1s; minimal antiemetic effect. Desloratadine (Clarinex) is the active enantiomer-of-metabolite version marketed as a Rx alternative. (1)
uses:
Insomnia (sleep onset and/or sleep maintenance) in adults (FDA-approved Jan 2022) (1) ·
'"`UNIQ--vote-0000015B-QINU`"', '"`UNIQ--vote-0000015C-QINU`"', '"`UNIQ--vote-0000015D-QINU`"' (1) ·
'"`UNIQ--vote-00000393-QINU`"', '"`UNIQ--vote-00000394-QINU`"', '"`UNIQ--vote-00000395-QINU`"' (1) ·
'"`UNIQ--vote-0000061F-QINU`"', '"`UNIQ--vote-00000620-QINU`"' (1) ·
'"`UNIQ--vote-00000B08-QINU`"', '"`UNIQ--vote-00000B09-QINU`"' (1) ·
'"`UNIQ--vote-00000C4C-QINU`"', '"`UNIQ--vote-00000C4D-QINU`"' (1) ·
'"`UNIQ--vote-000010CE-QINU`"', '"`UNIQ--vote-000010CF-QINU`"', '"`UNIQ--vote-000010D0-QINU`"' (1)
starting dose:
1 drop in affected eye(s) TID (monotherapy); BID with timolol (Cosopt) (1) ·
10 mg PO once daily (1) ·
10 mg PO once daily (5 mg in older adults or if sedation occurs) (1) ·
10 mg PO once daily in the evening (adults); 4-5 mg in children (1) ·
25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) ·
25 mg PO once daily; titrate to 50 mg after 4-8 weeks if needed (1) ·
Ophthalmic 1 drop in affected eye(s) TID; topical Mirvaso 0.33% gel applied to face daily (1)
preparations:
0.1%, 0.15%, 0.2% ophthalmic solutions; 0.33% topical gel; combinations with timolol (Combigan) and brinzolamide (Simbrinza) (1) ·
10 mg tablets; 4 mg, 5 mg chewables; 4 mg granules (1) ·
10 mg tablets; 5 mg ODT and chewables; 1 mg/mL oral syrup; combo Claritin-D (with pseudoephedrine, behind-counter) (1) ·
2% ophthalmic solution (Trusopt); 2%/0.5% fixed combination with timolol (Cosopt, Cosopt PF) (1) ·
25 mg, 50 mg tablets (1) ·
25, 50 mg ER tablets; 8 mg/mL granules for oral suspension (Myrbetriq Granules, pediatric) (1) ·
5 mg, 10 mg tablets; 5 mg, 10 mg chewables; 1 mg/mL oral syrup; OTC (1)
fda max: (Click arrow to add another value)
routes:
onset:
1-3 hours (slower onset than cetirizine; symptom relief somewhat less) (1) ·
30-60 minutes (1) ·
Bronchodilation within 1-2 hours; full controller effect 1-2 weeks (1) ·
IOP lowering at 1 hour; max at 2-3 hours (1) ·
IOP lowering at 2 hours; max at 4 hours (1) ·
Symptom improvement within weeks (1) ·
~30 min (1)
duration:
halflife:
2.7-5.5 hours'"`UNIQ--ref-0000015E-QINU`"' (1) ·
8-10 hours (longer in elderly and renal impairment)'"`UNIQ--ref-00000396-QINU`"' (1) ·
~3 hours'"`UNIQ--ref-000010D1-QINU`"' (1) ·
~4 months in erythrocytes (carbonic anhydrase binding in red cells; not relevant to topical IOP duration)'"`UNIQ--ref-00000B0A-QINU`"' (1) ·
~50 hours'"`UNIQ--ref-00000C4E-QINU`"' (1) ·
~8 hours (parent); ~28 hours (desloratadine, the active metabolite, marketed separately as Clarinex)'"`UNIQ--ref-00000621-QINU`"' (1) ·
~8 hours (shorter than suvorexant and lemborexant) (1)
bioavailability:
25 mg: ~29%; 50 mg: ~35%; food reduces absorption'"`UNIQ--ref-00000C4F-QINU`"' (1) ·
High (oral); not significantly affected by food'"`UNIQ--ref-00000397-QINU`"' (1) ·
High (oral; food prolongs absorption modestly)'"`UNIQ--ref-00000622-QINU`"' (1) ·
Topical with measurable systemic absorption (small CA inhibition observed clinically with chronic use)'"`UNIQ--ref-00000B0B-QINU`"' (1) ·
Topical; clinically meaningful systemic absorption can produce systemic α2 effects (somnolence, hypotension), especially in children'"`UNIQ--ref-000010D2-QINU`"' (1) ·
~62% (1) ·
~64% (oral; not significantly affected by food)'"`UNIQ--ref-0000015F-QINU`"' (1)
pregnancy:
Generally considered safe; pregnancy registries do not show increased major malformation risk.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Generally considered safe; widely used. Levocetirizine (the R-enantiomer) is an alternative with similar safety.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Generally considered safe; widely used. Loratadine and cetirizine are the most-recommended 2nd-gen H1s in pregnancy and lactation.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Limited data.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (2) ·
Limited data; avoid (1) ·
Limited data; weigh against alternatives.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1)
legal:
OTC in US (2) ·
Rx, Schedule IV (US) (1) ·
[[USLegal:Prescription only|Rx-only]] in US (3) ·
[[USLegal:Prescription only|Rx-only]] in US. '''FDA Boxed Warning (2020):''' neuropsychiatric events including agitation, depression, sleep disturbance, and suicidal thoughts; benefit-risk should be reassessed regularly'"`UNIQ--ref-00000160-QINU`"'. (1)
Showing below up to 7 results in range #1 to #7.