Drilldown: Medicines
Use the filters below to narrow your results.
generic:
brand:
classes:
Selective 5HT2A inverse agonist (with weaker 5HT2C inverse agonism) (1) ·
[[:Category:5-alpha-reductase_inhibitors|5α-reductase inhibitor]] (1) ·
[[:Category:Androgen_modulators|Androgen modulator]] (1) ·
[[:Category:Antiasthmatic_agents|Antiasthmatic]] (1) ·
[[:Category:Antihistamines|Antihistamine]] (2) ·
[[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (1) ·
[[:Category:BPH_treatments|Benign prostatic hyperplasia treatment]] (1) ·
[[:Category:DPP-4_inhibitors|DPP-4 inhibitor]] (1) ·
[[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist (second-generation)]] (2) ·
[[:Category:Incretin_modulators|Incretin pathway modulator]] (1) ·
[[:Category:Leukotriene_receptor_antagonists|Leukotriene receptor antagonist]] (1)
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-0000052E-QINU`"', '"`UNIQ--vote-0000052F-QINU`"', '"`UNIQ--vote-00000530-QINU`"' (1) ·
'"`UNIQ--vote-0000061F-QINU`"', '"`UNIQ--vote-00000620-QINU`"' (1) ·
'"`UNIQ--vote-0000117B-QINU`"' (1)
starting dose:
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) ·
5 mg PO daily for BPH; 1 mg PO daily for androgenetic alopecia (1) ·
5 mg PO once daily (no renal dose adjustment, unlike sitagliptin) (1)
preparations:
1 mg, 5 mg 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) ·
5 mg tablets; combination with metformin (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) ·
Benefit over weeks of dosing (1) ·
BPH symptom improvement at 3-6 months; prostate volume reduction over 6-12 months; hair regrowth at 6-12 months (1) ·
Bronchodilation within 1-2 hours; full controller effect 1-2 weeks (1) ·
Postprandial glucose effect within days; HbA1c by 12 weeks (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) ·
~12 hours (effective); terminal much longer'"`UNIQ--ref-0000117C-QINU`"' (1) ·
~5-6 hours in young men, ~8 hours in elderly'"`UNIQ--ref-00000531-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) ·
~30% (oral)'"`UNIQ--ref-0000117D-QINU`"' (1) ·
~63% (oral)'"`UNIQ--ref-00000532-QINU`"' (1) ·
~64% (oral; not significantly affected by food)'"`UNIQ--ref-0000015F-QINU`"' (1)
pregnancy:
'''Pregnant individuals should not handle crushed/broken tablets''' (skin absorption risk); can cause hypospadias in male fetus. Not used in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (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; avoid (1) ·
Limited data; switch to insulin where feasible.<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.