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: Anticonvulsant

or Sedative-Hypnotic

or [[:Category:Antihistamines|Antihistamine]]

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None (9)

None (2) · AMPA receptor antagonist (1) · Extremely potent GABAA positive allosteric modulator (1) · GABA enhancer; sodium channel blocker; histone deacetylase inhibitor (1) · GABA reuptake inhibitor (GAT-1 blocker) (1) · GABAA positive allosteric modulator (16) · GABAA positive allosteric modulator (non-benzodiazepine) (3) · GABAA positive allosteric modulator; lactate dehydrogenase inhibitor (1) · GABAA positive allosteric modulator; very long half-life (1) · GABAA potentiator (1) · GABAA potentiator and direct activator (3) · GABAB agonist; GHB receptor agonist (1) · Irreversible GABA-T inhibitor (1) · Melatonin receptor agonist (2) · Multiple mechanisms; GPR55 antagonist; TRPV1 agonist (1) · NMDA antagonist; GABAA potentiator (1) · Positive allosteric modulator of the GABAA receptor at the benzodiazepine binding site; increases frequency of Cl− channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (1) · Prodrug of phenytoin; sodium channel blocker (1) · Selective GABAA agonist (extrasynaptic delta subunit) (1) · Serotonin releaser; sigma-1 agonist (1) · Slow-inactivation sodium channel enhancer; CRMP-2 ligand (1) · Sodium channel blocker (2) · Sodium channel blocker; GABAA positive allosteric modulator (1) · Sodium channel modulator (1) · Sodium/T-type calcium channel blocker; carbonic anhydrase inhibitor (1) · SV2A ligand (higher affinity than levetiracetam) (1) · T-type calcium channel blocker (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-00000950-QINU`"' Mostly renally cleared unchanged; dose-reduce in renal impairment. Like cetirizine, retains slightly more sedation than fexofenadine in some users'"`UNIQ--ref-00000951-QINU`"'. (1) · '"`UNIQ--vote-00000CC9-QINU`"' Mostly excreted unchanged in feces and urine; P-glycoprotein substrate (the basis of the fruit-juice interaction). (1)

None (48) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (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-00000952-QINU`"', '"`UNIQ--vote-00000953-QINU`"' (1) · '"`UNIQ--vote-00000CCA-QINU`"', '"`UNIQ--vote-00000CCB-QINU`"' (1)

None (48) · 10 mg PO once daily (1) · 10 mg PO once daily (5 mg in older adults or if sedation occurs) (1) · 5 mg PO once daily in the evening (1) · 60 mg PO BID or 180 mg PO once daily (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

None (48) · 10 mg tablets; 5 mg ODT and chewables; 1 mg/mL oral syrup; combo Claritin-D (with pseudoephedrine, behind-counter) (1) · 30, 60, 180 mg tablets; 30 mg ODT; 6 mg/mL oral suspension; all OTC (1) · 5 mg tablets; 2.5 mg/5 mL oral solution; OTC (1) · 5 mg, 10 mg tablets; 5 mg, 10 mg chewables; 1 mg/mL oral syrup; OTC (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)

None (48) · 10 mg/d (adults) (2) · 180 mg/d (adults) (1) · 5 mg/d (adults) (1) · N/A (never approved) (1)

None (48) · intranasal; rectal and IV reported. (1) · Oral (5) · sublingual (1)

None (48) · 1-2 hours (1) · 1-3 hours (slower onset than cetirizine; symptom relief somewhat less) (1) · 30-60 minutes (2) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (48) · 12-24 hours (1) · 24 hours (3) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)

None (48) · 8-10 hours (longer in elderly and renal impairment)'"`UNIQ--ref-00000396-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~14 hours'"`UNIQ--ref-00000CCC-QINU`"' (1) · ~8 hours (longer in elderly and renal impairment)'"`UNIQ--ref-00000954-QINU`"' (1) · ~8 hours (parent); ~28 hours (desloratadine, the active metabolite, marketed separately as Clarinex)'"`UNIQ--ref-00000621-QINU`"' (1)

None (48) · High (oral); not significantly affected by food'"`UNIQ--ref-00000397-QINU`"' (1) · High (oral; food prolongs absorption modestly)'"`UNIQ--ref-00000622-QINU`"' (1) · Not formally characterized in humans. (1) · ~33% (oral; fruit juices including grapefruit, orange, and apple reduce absorption substantially via OATP1A2 inhibition — distinctive interaction not seen with most other H1s)'"`UNIQ--ref-00000CCD-QINU`"' (1) · ~85-90% (oral; not significantly affected by food)'"`UNIQ--ref-00000955-QINU`"' (1)

None (48) · Avoid. Benzodiazepines are associated with neonatal sedation, floppy-infant syndrome, and withdrawal; teratogenic signal weak but non-zero. Designer benzo with no safety data, assume worst-case. (1) · Generally considered safe; loratadine and cetirizine have more pregnancy data and are typically preferred.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Generally considered safe; widely used. Cetirizine and loratadine remain the more-studied alternatives.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Generally considered safe; widely used. Levocetirizine (the R-enantiomer) is an alternative with similar safety.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Generally considered safe; widely used. Loratadine and cetirizine are the most-recommended 2nd-gen H1s in pregnancy and lactation.[[[Pharmacopedia:Citation needed|citation needed]]] (1)

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