Drilldown: Medicines
Use the filters below to narrow your results.
generic:
brand:
classes:
Selective 5HT2A inverse agonist (with weaker 5HT2C inverse agonism) (1) ·
[[:Category:Alpha-2_agonists|Alpha-2 adrenergic agonist]] (1) ·
[[:Category:Antiasthmatic_agents|Antiasthmatic]] (1) ·
[[:Category:Antihistamines|Antihistamine]] (2) ·
[[: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)
mechanism:
None (3) ·
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)
uses:
Hallucinations and delusions associated with Parkinson's disease psychosis (PDP). Investigational for psychosis in other dementias and as augmentation for depression. (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-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) ·
34 mg PO once daily (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) ·
10 mg, 34 mg capsules/tablets (1) ·
2% ophthalmic solution (Trusopt); 2%/0.5% fixed combination with timolol (Cosopt, Cosopt PF) (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:
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) ·
~57 hours (parent), ~200 h (active metabolite) (1) ·
~8 hours (parent); ~28 hours (desloratadine, the active metabolite, marketed separately as Clarinex)'"`UNIQ--ref-00000621-QINU`"' (1)
bioavailability:
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) ·
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) ·
~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> (1) ·
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. 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 (2) ·
[[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 6 results in range #1 to #6.