Drilldown: Medicines
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generic:
brand:
classes:
5HT1A activity than aripiprazole (1) ·
5HT2A (1) ·
5HT2A/D2 antagonist with proposed differential pre/post-synaptic D2 activity (1) ·
Anti-amyloid beta (Aβ) monoclonal antibody (1) ·
Anti-CGRP ligand monoclonal antibody (3) ·
Anti-CGRP receptor monoclonal antibody (1) ·
Atypical antipsychotic (3) ·
CGRP receptor antagonist (1) ·
D2/5HT1A partial agonist with stronger α1A (1) ·
D2/D3/5HT1A partial agonist (1) ·
Gepant (1) ·
Multimodal antidepressant: SERT inhibitor + 5HT1A agonist + 5HT1B partial agonist + 5HT3/5HT7 antagonist (1) ·
NMDA receptor antagonist + sigma-1 agonist + NDRI (combination) (1) ·
Serotonin partial agonist reuptake inhibitor (SPARI) (1) ·
targets pyroglutamated Aβ in plaques (1)
mechanism:
None (6) ·
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) ·
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) ·
Small-molecule CGRP receptor antagonist; intranasal formulation (1)
uses:
Acute treatment of migraine with or without aura in adults (1) ·
Alzheimer disease (MCI or mild dementia stage), FDA-approved July 2024 (1) ·
Major depressive disorder in adults (FDA-approved 2011) (1) ·
Major depressive disorder in adults (FDA-approved 2013). Notable for evidence of cognitive benefit (processing speed) that distinguishes it from other antidepressants. (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) ·
Schizophrenia (FDA-approved 2015). Adjunctive treatment of major depressive disorder (2015). '''Agitation associated with dementia due to Alzheimer disease''' (FDA-approved May 2023, first agent specifically approved for this problem). Investigational for PTSD (combined with sertraline). (1) ·
Schizophrenia (FDA-approved Dec 2019). Bipolar depression as monotherapy or adjunct to lithium/valproate (FDA-approved Dec 2021). (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 once daily × 7 days, then 20 mg × 7 days, then 40 mg as target dose (take with food) (1) ·
10 mg PO once daily; may increase to 20 mg as tolerated, or decrease to 5 mg if needed (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) ·
42 mg PO once daily with food (no titration) (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) ·
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) ·
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) ·
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:
0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets (1) ·
1.5 mg, 3 mg, 4.5 mg, 6 mg capsules (1) ·
10 mg, 20 mg, 40 mg tablets (1) ·
10 mg/spray nasal solution (1) ·
100 mg/mL vial for IV infusion (1) ·
120 mg/mL prefilled syringe or autoinjector (1) ·
225 mg/1.5 mL prefilled syringe or autoinjector (1) ·
350 mg/20 mL vial for IV infusion (1) ·
42 mg capsules (1) ·
5 mg, 10 mg, 20 mg tablets (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) ·
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) ·
300 mg/quarter (1) ·
4 mg/d (schizophrenia); 3 mg/d (AD agitation); 3 mg/d (MDD adjunct) (1) ·
40 mg/d (1) ·
42 mg/d (1) ·
6 mg/d (psychosis/mania); 3 mg/d (depression adjunct) (1) ·
675 mg/quarter (1)
routes:
onset:
4-6 weeks for full antidepressant effect (claimed earlier onset for some patients due to 5HT1A partial agonism) (1) ·
Amyloid PET clearance within months; cognitive benefit over 18 months (1) ·
Antipsychotic effect 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) ·
Typical antidepressant 4-6 week onset (1) ·
Weeks for psychosis/depression; AD agitation benefit emerges over weeks (1) ·
Weeks for psychosis/mood efficacy (1)
duration:
3-month dosing interval (1) ·
Daily dosing (4) ·
Daily dosing; active metabolites with very long half-lives (up to 1-3 weeks) (1) ·
Monthly dosing (2) ·
Monthly or quarterly 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)
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) ·
~12.1 days (1) ·
~18 hours (terminal) (1) ·
~25 hours (1) ·
~27 days (2) ·
~28 days (1) ·
~31 days (1) ·
~6.6 h (1) ·
~66 hours (1) ·
~91 hours (1)
bioavailability:
100% (IV) (2) ·
Adequate oral bioavailability (1) ·
Limited but adequate; take with food (1) ·
Not formally characterized for the combination (1) ·
Not formally established (1) ·
Not formally established (high SC) (1) ·
~5% intranasal (1) ·
~72% (with food); much lower fasting (~36%) (1) ·
~75% (1) ·
~82% SC (1) ·
~95% (1)
pregnancy:
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Showing below up to 12 results in range #1 to #12.