Drilldown: Medicines
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generic:
brand:
classes:
Multimodal serotonergic; HSDD treatment (1) ·
[[:Category:Angiotensin_receptor_blockers|Angiotensin receptor blocker (ARB)]] (1) ·
[[:Category:Antiasthmatic_agents|Antiasthmatic]] (1) ·
[[:Category:Antihistamines|Antihistamine]] (2) ·
[[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (1) ·
[[:Category:Antihypertensives|Antihypertensive]] (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 (1) ·
5-HT1A agonist, 5-HT2A antagonist, with weaker activity at D4 and other receptors. Net effect involves enhanced prefrontal dopaminergic/noradrenergic tone with decreased serotonergic inhibition of sexual desire. (1) ·
'"`UNIQ--vote-000000B6-QINU`"' Active metabolite EXP3174 is ~10-40-fold more potent than the parent and accounts for most of the antihypertensive effect; CYP2C9 polymorphism affects conversion'"`UNIQ--ref-000000B7-QINU`"'. (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-00000762-QINU`"' Largely renally cleared, hence the eGFR-tiered dosing. Rare but well-documented signals: acute pancreatitis (uncertain causal contribution), severe joint pain, and bullous pemphigoid (class effect, especially in older Asian patients)'"`UNIQ--ref-00000763-QINU`"'. (1)
uses:
'"`UNIQ--vote-000000B8-QINU`"', '"`UNIQ--vote-000000B9-QINU`"', '"`UNIQ--vote-000000BA-QINU`"', '"`UNIQ--vote-000000BB-QINU`"' (1) ·
'"`UNIQ--vote-0000015B-QINU`"', '"`UNIQ--vote-0000015C-QINU`"', '"`UNIQ--vote-0000015D-QINU`"' (1) ·
'"`UNIQ--vote-000002C1-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-00000764-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) ·
100 mg at bedtime daily (1) ·
100 mg PO once daily (50 mg if CrCl 30-44; 25 mg if <30 or dialysis) (1) ·
50 mg PO daily (25 mg in volume depletion or hepatic impairment) (1)
preparations:
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) ·
100 mg tabs (1) ·
25 mg, 50 mg, 100 mg tablets (1) ·
25, 50, 100 mg tablets; combination tablets 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) ·
BP effect 1-2 weeks; antihypertensive peak 3-6 weeks (1) ·
Bronchodilation within 1-2 hours; full controller effect 1-2 weeks (1) ·
Effects accumulate over weeks; assess at 8 weeks (1) ·
Postprandial glucose effect within days; HbA1c by 12 weeks (1)
duration:
halflife:
2 hours (parent); 6-9 hours for active carboxylic acid metabolite EXP3174'"`UNIQ--ref-000000BC-QINU`"' (1) ·
2.7-5.5 hours'"`UNIQ--ref-0000015E-QINU`"' (1) ·
8-10 hours (longer in elderly and renal impairment)'"`UNIQ--ref-00000396-QINU`"' (1) ·
~11 h (1) ·
~12.4 hours'"`UNIQ--ref-00000765-QINU`"' (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) ·
~33% (1) ·
~33% (extensive first-pass via CYP2C9 and CYP3A4)'"`UNIQ--ref-000000BD-QINU`"' (1) ·
~64% (oral; not significantly affected by food)'"`UNIQ--ref-0000015F-QINU`"' (1) ·
~87% (oral)'"`UNIQ--ref-00000766-QINU`"' (1)
pregnancy:
'''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-000000BE-QINU`"' (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; switch to insulin where feasible.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Not indicated; pregnancy effects unknown (1)
legal:
OTC in US (2) ·
Rx-only in US (REMS program) (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.