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Medicines > bioavailability

: 100% (IV)

or ~80% (oral)'"`UNIQ--ref-00000027-QINU`"'

or ~95%

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None (7) · Citalopram (1) · Escitalopram (1) · Hydroxyzine (hydrochloride; pamoate salt) (1) · Lactated Ringer's solution (1)

Aduhelm (1) · Celexa (1) · Kisunla (1) · Lactated Ringer's Injection (Baxter, B. Braun, ICU Medical); Hartmann's solution (intl.) (1) · Leqembi (1) · Lexapro (1) · Rexulti (1) · Sunosi (1) · Vistaril (pamoate), Atarax (HCl, discontinued in US as brand) (1) · Vyepti (1) · Zulresso (1)

5HT1A activity than aripiprazole (1) · 5HT2A (1) · Anti-amyloid beta (Aβ) monoclonal antibody (3) · Anti-CGRP ligand monoclonal antibody (1) · Atypical antipsychotic (1) · D2/5HT1A partial agonist with stronger α1A (1) · GABA-A positive allosteric modulator (1) · Neuroactive steroid (1) · Norepinephrine-dopamine reuptake inhibitor (NDRI) (1) · targets protofibrils (1) · targets pyroglutamated Aβ in plaques (1) · wake-promoting agent (1) · [[:Category:Antidepressants|Antidepressant]] (2) · [[:Category:Antihistamines|First-generation antihistamine]] (1) · [[:Category:Antipruritics|Antipruritic]] (1) · [[:Category:Anxiolytics|Anxiolytic]] (2) · [[:Category:Crystalloid_IV_fluids|Crystalloid IV fluid]] (1) · [[:Category:Electrolyte_replacements|Electrolyte replacement]] (1) · [[:Category:Sleep aids|Sleep aid (off-label)]] (1) · [[:Category:SSRIs|Selective serotonin reuptake inhibitor (SSRI)]] (2)

None (3) · Human IgG1 monoclonal antibody targeting aggregated forms of amyloid-β (Aβ), soluble oligomers and insoluble fibrils. Reduces Aβ plaque burden on PET imaging via Fc-mediated microglial clearance. Whether plaque reduction translates to clinical benefit is the core controversy. (1) · Humanized IgG1 monoclonal antibody binding CGRP peptide; IV infusion enables fastest onset of any CGRP mAb (1) · Partial agonist at D2 and 5HT1A. Antagonist at 5HT2A, α1A, α1B, α2C. More potent 5HT2A antagonism, 5HT1A partial agonism, and α1 antagonism (relative to D2 partial agonism) than aripiprazole, proposed to reduce akathisia and enhance affective/cognitive effects. (1) · Selective dopamine and norepinephrine reuptake inhibitor (DAT and NET inhibition). Unlike amphetamine, does not significantly release monoamines, pure reuptake inhibition. (1) · '"`UNIQ--vote-0000001D-QINU`"' '''QT prolongation''' risk at high doses prompted the FDA's 2015 caution against use in patients with prolonged QT or with concurrent QT-prolonging medicines'"`UNIQ--ref-0000001E-QINU`"'. (1) · '"`UNIQ--vote-0000001D-QINU`"' CYP2C19 + CYP3A4 metabolism, with CPIC PGx guidance: poor CYP2C19 metabolizers have ~3-fold higher exposure and benefit from a lower starting dose; ultrarapid metabolizers may have inadequate response'"`UNIQ--ref-0000001E-QINU`"'. (2) · '"`UNIQ--vote-00000086-QINU`"' Calcium content is a relative contraindication for co-administration with citrated blood products through the same line'"`UNIQ--ref-00000087-QINU`"'. (1)

10 mg PO once daily; titrate to 20 mg/day after 1-2 weeks if needed (1) · 10 mg/kg IV every 2 weeks (1) · 100 mg IV every 3 months; may increase to 300 mg IV every 3 months (1) · 20 mg PO once daily; titrate to 40 mg/day after 1 week if tolerated. Elderly (>60) and hepatic impairment: 20 mg/day ceiling (1) · 700 mg IV q4w × 3 doses, then 1400 mg IV q4w; may discontinue when amyloid PET shows clearance (1) · Anxiety: 25-50 mg PO QID. Pruritus: 25 mg PO TID-QID. Insomnia: 25-50 mg PO at bedtime. Pediatric: 50-100 mg/day divided (1) · Narcolepsy: 75 mg PO once daily upon awakening, titrate every 3 days. OSA: 37.5 mg PO once daily, titrate. (1) · Schizophrenia: 1 mg PO daily × 4 days, then 2 mg daily × 3 days, then 4 mg daily. MDD adjunct: 0.5-1 mg daily, increase to 2 mg max. AD agitation: 0.5 mg daily, titrate to 2-3 mg daily. (1) · Single 60-hour continuous IV infusion: 30 mcg/kg/h × 4h → 60 mcg/kg/h × 20h → 90 mcg/kg/h × 28h → 60 mcg/kg/h × 4h → 30 mcg/kg/h × 4h (1) · Volume titrated to clinical status; typical adult bolus 500-1000 mL, then reassess (1) · Was 1 mg/kg IV q4w × 2, then 3 mg/kg × 2, then 6 mg/kg × 2, then 10 mg/kg q4w (1)

0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets (1) · 100 mg/20 mL vial, single-use (1) · 100 mg/mL vial for IV infusion (1) · 200 mg/2 mL, 500 mg/5 mL vials for IV infusion (1) · 250, 500, 1000 mL IV bags. Composition per liter: Na+ 130 mEq, K+ 4 mEq, Ca2+ 3 mEq, Cl- 109 mEq, lactate 28 mEq (1) · 350 mg/20 mL vial for IV infusion (1) · 75 mg, 150 mg tablets (1) · Tablets 10, 20, 40 mg; oral solution 10 mg/5 mL (1) · Tablets 10, 25, 50 mg (HCl); capsules 25, 50, 100 mg (pamoate); oral suspension 25 mg/5 mL; injection 25, 50 mg/mL (IM only, never IV) (1) · Tablets 5, 10, 20 mg; oral solution 1 mg/mL (1) · Was: 170 mg/1.7 mL, 300 mg/3 mL vials for IV infusion (1)

'''20 mg/day in adults >60 years''' per FDA's 2011-2012 QT-prolongation warning; 40 mg/day in adults ≤60 (1) · 10 mg/kg q2w (1) · 1400 mg q4w (1) · 150 mg/d (1) · 20 mg/day (adult); 10 mg/day in elderly and in hepatic impairment (1) · 300 mg/quarter (1) · 4 mg/d (schizophrenia); 3 mg/d (AD agitation); 3 mg/d (MDD adjunct) (1) · 400 mg/day theoretical; in practice rarely exceeds 200 mg/day (1) · No fixed maximum; titrated to clinical endpoints (1) · Single 60-hour course (1) · Withdrawn 2024 (1)

intramuscular (1) · Intravenous (continuous infusion in a REMS-certified facility) (1) · Intravenous infusion (1) · IV (1) · IV infusion (60 min) every 2 weeks; outpatient or infusion-center setting (1) · IV infusion every 4 weeks (2) · Oral (5)

15-30 minutes (oral) (1) · Amyloid PET clearance within months; cognitive benefit over 18 months (1) · Antidepressant effect emerges over 1-2 weeks; full clinical effect 4-6 weeks (1) · Antidepressant effect over 1-2 weeks; full clinical effect 4-6 weeks (1) · Antidepressant effect within hours of infusion start; sustained at 30 days (1) · Effect demonstrated within 24 hours in some patients (1) · Immediate intravascular expansion (1) · PET Aβ reduction over months (1) · Slowing of cognitive decline over 18 months (modest effect, ~27% relative slowing) (1) · Weeks for psychosis/depression; AD agitation benefit emerges over weeks (1) · ~30-60 min (1)

24 hours (once-daily dosing) (2) · 3-month dosing interval (1) · 4-6 hours (1) · Daily dosing (1) · Ongoing dosing (1) · Roughly 20-30% remains intravascular at 1 hour (1) · Single infusion course (1) · Treatment can be discontinued upon achieving amyloid clearance (1) · Withdrawn (1) · ~9 hours (1)

14-25 hours (longer in elderly and hepatic impairment)'"`UNIQ--ref-00000026-QINU`"' (1) · 27-32 hours'"`UNIQ--ref-00000026-QINU`"' (1) · Not applicable (electrolyte solution) (1) · ~12.1 days (1) · ~25 days (1) · ~27 days (1) · ~35 hours'"`UNIQ--ref-00000026-QINU`"' (1) · ~5-7 days (1) · ~7.1 hours (1) · ~9 hours (terminal) (1) · ~91 hours (1)

None (1) · Discontinued/withdrawn (1) · Limited data (2) · Limited data; avoid (1) · Limited data; National Pregnancy Registry available (1) · Limited data; pregnancy exposure registry available (1) · Limited human data; older agent with substantial use experience; some signal for first-trimester exposure but not conclusive.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) · Medicine is structurally identical to endogenous allopregnanolone; pregnancy considerations relate to breastfeeding during/after infusion. Limited data; brief interruption of breastfeeding considered (1) · Observational signal for persistent pulmonary hypertension of the newborn (small absolute risk) and neonatal adaptation syndrome with third-trimester exposure.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) · Standard resuscitation fluid in pregnancy (1)

Rx (2) · Rx, Schedule IV (US) (1) · Rx; ARIA monitoring required (1) · Rx; REMS program required (excessive sedation/loss of consciousness during infusion) (1) · Rx; REMS-like program for ARIA monitoring (1) · Withdrawn from US market January 2024 (1) · [[USLegal:Prescription only|Rx-only]] in US (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000028-QINU`"' (2) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, which is a meaningful clinical advantage over the benzodiazepine alternatives for short-term anxiety'"`UNIQ--ref-00000028-QINU`"' (1)

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