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Medicines > pregnancy : Limited data or Limited data; avoid or Not relevant (geriatric problem)

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generic:
None (14) · Memantine ER / Donepezil (1)
brand:
Aimovig (1) · Ajovy (1) · Auvelity (dextromethorphan/bupropion ER) (1) · Belsomra (1) · Dayvigo (1) · Emgality (1) · Kisunla (1) · Leqembi (1) · Namzaric (1) · Nuplazid (1) · Qelbree (1) · Quviviq (1) · Vraylar (1) · Vyepti (1) · Zavzpret (zavegepant) (1)
classes:
Anti-amyloid beta (Aβ) monoclonal antibody (2) · Anti-CGRP ligand monoclonal antibody (3) · Anti-CGRP receptor monoclonal antibody (1) · Atypical antipsychotic (1) · CGRP receptor antagonist (1) · Combined cholinesterase inhibitor + NMDA antagonist (1) · D2/D3/5HT1A partial agonist (1) · Dual orexin receptor antagonist (DORA) (3) · Gepant (1) · NMDA receptor antagonist + sigma-1 agonist + NDRI (combination) (1) · non-stimulant ADHD agent (1) · Selective 5HT2A inverse agonist (with weaker 5HT2C inverse agonism) (1) · Selective norepinephrine reuptake inhibitor (NRI) with 5HT1A partial agonism (1) · targets protofibrils (1) · targets pyroglutamated Aβ in plaques (1) · the first approved (1)
mechanism:
None (5) · Competitive antagonist at OX1R and OX2R. Faster receptor association/dissociation kinetics than suvorexant (~16 sec dissociation vs ~57 sec) hypothesized to support sleep onset, with sufficient duration for maintenance. (1) · Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (1) · Donepezil: reversible AChE inhibitor, increases synaptic acetylcholine. Memantine: uncompetitive low-affinity NMDA receptor antagonist, dampens pathological glutamate overactivation while preserving normal synaptic signaling. Targets two distinct mechanisms in Alzheimer's. (1) · Humanized IgG1 monoclonal antibody binding CGRP peptide; IV infusion enables fastest onset of any CGRP mAb (1) · Humanized IgG2 monoclonal antibody binding both isoforms of CGRP peptide (1) · Humanized IgG2 monoclonal antibody binding the CGRP receptor (not the peptide); blocks CGRP-mediated vasodilation and nociceptive signaling (1) · Humanized IgG4 monoclonal antibody binding CGRP peptide; prevents CGRP from activating its receptor (1) · 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) · Selective NET inhibitor (no significant DAT activity, distinguishes from amphetamine/methylphenidate). Also: 5HT1A receptor partial agonism, 5HT2B and 5HT7 receptor antagonism. The serotonergic actions may underlie better tolerability and possibly different efficacy spectrum than atomoxetine. (1) · Small-molecule CGRP receptor antagonist; intranasal formulation (1)
uses:
Acute treatment of migraine with or without aura in adults (1) · ADHD in children (6+), adolescents, and adults (FDA-approved 2021 for pediatric, 2022 for adult) (1) · Alzheimer disease (MCI or mild dementia stage), FDA-approved July 2024 (1) · Alzheimer disease (MCI or mild dementia stage); FDA accelerated approval Jan 2023 → traditional approval July 2023 (1) · Hallucinations and delusions associated with Parkinson's disease psychosis (PDP). Investigational for psychosis in other dementias and as augmentation for depression. (1) · Insomnia (sleep onset and/or maintenance) in adults (FDA-approved August 2014). Also studied for insomnia in mild-moderate Alzheimer disease. (1) · Insomnia (sleep onset and/or maintenance) in adults (FDA-approved Dec 2019) (1) · Insomnia (sleep onset and/or sleep maintenance) in adults (FDA-approved Jan 2022) (1) · Major depressive disorder in adults (FDA-approved August 2022) (1) · Preventive treatment of migraine in adults (1) · Preventive treatment of migraine in adults (episodic and chronic) (2) · Preventive treatment of migraine in adults; episodic cluster headache (1) · Schizophrenia (FDA-approved 2015). Acute manic or mixed episodes of bipolar I disorder. Bipolar I depression (FDA-approved 2019). Adjunctive treatment of major depressive disorder (FDA-approved Dec 2022). (1) · '"`UNIQ--vote-00000468-QINU`"' (1)
starting dose:
1 tablet (dextromethorphan 45 mg / bupropion 105 mg) PO daily × 3 days, then increase to 1 tablet BID (1) · 10 mg (one spray) intranasally in one nostril (1) · 10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (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) · 225 mg SC monthly, or 675 mg SC every 3 months (quarterly) (1) · 25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) · 34 mg PO once daily (1) · 5 mg PO at bedtime; may increase to 10 mg if inadequate (1) · 70 mg SC monthly; may increase to 140 mg monthly (1) · 700 mg IV q4w × 3 doses, then 1400 mg IV q4w; may discontinue when amyloid PET shows clearance (1) · For patients already stable on memantine 28 mg/d + donepezil 10 mg/d, switch to one capsule daily of equivalent strength (1) · Migraine: 240 mg SC loading dose, then 120 mg SC monthly. Cluster: 300 mg SC at onset of cluster period, then monthly during cluster. (1) · Pediatric 6-11: 100 mg PO daily, titrate weekly to max 400 mg. Adolescent 12-17: 200 mg, max 400 mg. Adult: 200 mg, max 600 mg. (1) · Schizophrenia: 1.5 mg PO daily, increase to 1.5-6 mg as tolerated. Bipolar mania: 1.5 mg, may increase to 3-6 mg. Bipolar depression: 1.5 mg daily for 14 days, then 3 mg. MDD adjunct: 1.5 mg, may increase to 3 mg. (1)
preparations:
1.5 mg, 3 mg, 4.5 mg, 6 mg capsules (1) · 10 mg, 34 mg capsules/tablets (1) · 10 mg/spray nasal solution (1) · 100 mg, 150 mg, 200 mg extended-release capsules (can be sprinkled on food) (1) · 100 mg/mL vial for IV infusion (1) · 120 mg/mL prefilled syringe or autoinjector (1) · 200 mg/2 mL, 500 mg/5 mL vials for IV infusion (1) · 225 mg/1.5 mL prefilled syringe or autoinjector (1) · 25 mg, 50 mg tablets (1) · 350 mg/20 mL vial for IV infusion (1) · 5 mg, 10 mg tablets (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1) · 7/10, 14/10, 21/10, 28/10 mg ER capsules (memantine ER / donepezil) (1) · 70 mg/mL or 140 mg/mL prefilled autoinjector (1) · Dextromethorphan 45 mg + bupropion 105 mg ER tablets (1)
fda max:
10 mg per 24 h (1) · 10 mg/d (1) · 10 mg/kg q2w (1) · 140 mg/month (1) · 1400 mg q4w (1) · 2 tablets/day (dextromethorphan 90 mg / bupropion 210 mg) (1) · 20 mg/d (1) · 240 mg loading + 120 mg/month for migraine; 300 mg/month for cluster (1) · 28/10 mg/d (1) · 300 mg/quarter (1) · 34 mg/d (1) · 400 mg/d (pediatric); 600 mg/d (adult) (1) · 50 mg/d (1) · 6 mg/d (psychosis/mania); 3 mg/d (depression adjunct) (1) · 675 mg/quarter (1)
routes:
Intranasal (1) · Intravenous infusion (1) · IV infusion (60 min) every 2 weeks; outpatient or infusion-center setting (1) · IV infusion every 4 weeks (1) · Oral (7) · Oral (capsule whole or opened/sprinkled on applesauce) (1) · Subcutaneous (3)
onset:
ADHD symptom improvement reported within 1-2 weeks (faster than atomoxetine which takes 4-6 weeks) (1) · Amyloid PET clearance within months; cognitive benefit over 18 months (1) · Benefit over weeks of dosing (1) · Component effects accumulate over weeks (1) · Effect demonstrated within 24 hours in some patients (1) · Onset of preventive effect over weeks; some patients respond after first dose (1) · Over weeks (2) · Pain relief reported within 15 min in trials (1) · Significant antidepressant response by week 1 in trials (faster than monoaminergic antidepressants which take 4-6 weeks) (1) · Slowing of cognitive decline over 18 months (modest effect, ~27% relative slowing) (1) · Weeks for psychosis/mood efficacy (1) · ~30 min (3)
duration:
24 h (1) · 3-month dosing interval (1) · Daily dosing (2) · Daily dosing; active metabolites with very long half-lives (up to 1-3 weeks) (1) · Monthly dosing (2) · Monthly or quarterly dosing (1) · Ongoing dosing (1) · Sustained with twice-daily dosing (1) · Treatment can be discontinued upon achieving amyloid clearance (1) · ~48 h sustained pain freedom in responders (1) · ~7-8 hours (3)
halflife:
Cariprazine ~2-4 d; major active metabolites desmethyl-cariprazine (DCAR) ~1-3 weeks → 'oral depot' effect with delayed steady-state and reduced effect of missed doses (1) · Dextromethorphan ~22 h (when CYP2D6 inhibited); bupropion ~21 h (1) · ~12 hours (1) · ~12.1 days (1) · ~17-19 hours (longer than daridorexant) (1) · ~27 days (2) · ~28 days (1) · ~31 days (1) · ~5-7 days (1) · ~57 hours (parent), ~200 h (active metabolite) (1) · ~6.6 h (1) · ~60–80 h (memantine); ~70 h (donepezil) (1) · ~7 hours (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)
bioavailability:
100% (IV) (3) · Adequate oral bioavailability (1) · Adequate oral bioavailability with extended-release formulation (1) · Not characterized; oral dosing once daily (1) · Not formally characterized for the combination (1) · Not formally established (1) · Not formally established (high SC) (1) · ~100% both components (1) · ~44% (1) · ~5% intranasal (1) · ~62% (1) · ~82% (1) · ~82% SC (1)
pregnancy: (Click arrow to add another value)
legal:
Rx (7) · Rx, '''not a controlled substance''' (no DEA scheduling) (1) · Rx, Schedule IV (US) (3) · Rx-only in US (1) · Rx. FDA black-box warning for increased mortality in elderly patients with dementia-related psychosis (class warning shared with all antipsychotics) (1) · Rx; ARIA monitoring required (1) · Rx; REMS-like program for ARIA monitoring (1)

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