Drilldown: Medicines
Use the filters below to narrow your results.
generic:
brand:
classes:
Beta Blocker (1) ·
Cardioselective (β1) (1) ·
Dual orexin receptor antagonist (DORA) (1) ·
Multimodal antidepressant: SERT inhibitor + 5HT1A agonist + 5HT1B partial agonist + 5HT3/5HT7 antagonist (1) ·
PDE5 Inhibitor (1) ·
Selective 5HT2A inverse agonist (with weaker 5HT2C inverse agonism) (1) ·
the first approved (1) ·
[[:Category:Alpha-1_blockers|Alpha-1 adrenergic blocker (non-selective)]] (1) ·
[[:Category:Antiasthmatic_agents|Antiasthmatic]] (1) ·
[[:Category:Antihistamines|Antihistamine]] (2) ·
[[:Category:Antihypertensives|Antihypertensive]] (1) ·
[[:Category:BPH_treatments|Benign prostatic hyperplasia treatment]] (1) ·
[[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist (second-generation)]] (2) ·
[[:Category:Leukotriene_receptor_antagonists|Leukotriene receptor antagonist]] (1)
mechanism:
None (2) ·
Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (1) ·
Highly β1-selective adrenergic antagonist. Greater selectivity than metoprolol or atenolol. (1) ·
Selective inhibitor of PDE5. Slightly higher PDE5/PDE6 selectivity vs sildenafil (less visual side effect) but more PDE1 cross-activity (occasional QT effects at high doses). (1) ·
Selective inverse agonist at 5HT2A receptors with weaker activity at 5HT2C. Has no significant dopamine D2 affinity, unique among approved antipsychotics. Inverse agonism (rather than antagonism) reduces constitutive 5HT2A receptor activity below baseline. (1) ·
'"`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) ·
'"`UNIQ--vote-0000111B-QINU`"' Intraoperative floppy iris syndrome is a recognized class effect. Recently emerging evidence (observational) suggests possible Parkinson's disease risk reduction via PGK1 binding — investigational and not a clinical indication'"`UNIQ--ref-0000111C-QINU`"'. (1)
uses:
Hallucinations and delusions associated with Parkinson's disease psychosis (PDP). Investigational for psychosis in other dementias and as augmentation for depression. (1) ·
Insomnia (sleep onset and/or maintenance) in adults (FDA-approved August 2014). Also studied for insomnia in mild-moderate Alzheimer disease. (1) ·
Major depressive disorder in adults (FDA-approved 2013). Notable for evidence of cognitive benefit (processing speed) that distinguishes it from other antidepressants. (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-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (1) ·
'"`UNIQ--vote-00000669-QINU`"' (1) ·
'"`UNIQ--vote-0000111D-QINU`"', '"`UNIQ--vote-0000111E-QINU`"' (1)
starting dose:
1 mg PO at bedtime to limit first-dose syncope; titrate weekly to 5-10 mg (1) ·
10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (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) ·
10 mg PO once daily; may increase to 20 mg as tolerated, or decrease to 5 mg if needed (1) ·
10 mg ~1 h before sexual activity (1) ·
2.5–5 mg daily (HTN); 1.25 mg daily (HFrEF, slow titration) (1) ·
34 mg PO once daily (1)
preparations:
1, 2, 5, 10 mg capsules and tablets (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) ·
10 mg, 34 mg capsules/tablets (1) ·
2.5, 5, 10, 20 mg tabs (Levitra); 10 mg ODT (Staxyn) (1) ·
5 mg, 10 mg tablets; 5 mg, 10 mg chewables; 1 mg/mL oral syrup; OTC (1) ·
5 mg, 10 mg, 15 mg, 20 mg tablets (1) ·
5 mg, 10 mg, 20 mg tablets (1) ·
5, 10 mg tabs (1)
fda max: (Click arrow to add another value)
routes:
onset:
1-3 hours (slower onset than cetirizine; symptom relief somewhat less) (1) ·
1–2 h (1) ·
30-60 minutes (1) ·
Benefit over weeks of dosing (1) ·
BP and symptomatic LUTS improvement within 1-2 weeks (1) ·
Bronchodilation within 1-2 hours; full controller effect 1-2 weeks (1) ·
Typical antidepressant 4-6 week onset (1) ·
~30 min (2)
duration:
halflife:
2.7-5.5 hours'"`UNIQ--ref-0000015E-QINU`"' (1) ·
4–5 h (1) ·
8-10 hours (longer in elderly and renal impairment)'"`UNIQ--ref-00000396-QINU`"' (1) ·
9–12 h (1) ·
~12 hours (1) ·
~12 hours'"`UNIQ--ref-0000111F-QINU`"' (1) ·
~57 hours (parent), ~200 h (active metabolite) (1) ·
~66 hours (1) ·
~8 hours (parent); ~28 hours (desloratadine, the active metabolite, marketed separately as Clarinex)'"`UNIQ--ref-00000621-QINU`"' (1)
bioavailability:
>90% (oral; not significantly affected by food)'"`UNIQ--ref-00001120-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) ·
Not characterized; oral dosing once daily (1) ·
~15% (extensive hepatic first-pass) (1) ·
~64% (oral; not significantly affected by food)'"`UNIQ--ref-0000015F-QINU`"' (1) ·
~75% (1) ·
~82% (1) ·
~90% (low first-pass) (1)
pregnancy:
Category B (1) ·
Category C (1) ·
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> (1) ·
Limited data; avoid (2) ·
Limited data; weigh benefits/risks (1)
legal:
OTC in US (2) ·
Rx (1) ·
Rx, Schedule IV (US) (1) ·
Rx-only in US (2) ·
Rx. FDA black-box warning for increased mortality in elderly patients with dementia-related psychosis (class warning shared with all antipsychotics) (1) ·
[[USLegal:Prescription only|Rx-only]] in US (1) ·
[[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 9 results in range #1 to #9.