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Medicines > halflife : 11-15 hours'"`UNIQ--ref-00000842-QINU`"' or ~27 days or ~9 hours (terminal)

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generic:
None (3) · Irbesartan (1)
brand:
Avapro (1) · Emgality (1) · Vyepti (1) · Zulresso (1)
classes:
Anti-CGRP ligand monoclonal antibody (2) · GABA-A positive allosteric modulator (1) · Neuroactive steroid (1) · [[:Category:Angiotensin_receptor_blockers|Angiotensin receptor blocker (ARB)]] (1) · [[:Category:Antihypertensives|Antihypertensive]] (1)
mechanism:
None (1) · Humanized IgG1 monoclonal antibody binding CGRP peptide; IV infusion enables fastest onset of any CGRP mAb (1) · Humanized IgG4 monoclonal antibody binding CGRP peptide; prevents CGRP from activating its receptor (1) · '"`UNIQ--vote-0000083E-QINU`"' CYP2C9 substrate; no clinically active metabolites. The IDNT trial established renoprotection in diabetic nephropathy independent of BP lowering, contributing to the ARB class indication in T2DM with proteinuria'"`UNIQ--ref-0000083F-QINU`"'. (1)
uses:
Postpartum depression (PPD) in adults (1) · Preventive treatment of migraine in adults (1) · Preventive treatment of migraine in adults; episodic cluster headache (1) · '"`UNIQ--vote-00000840-QINU`"', '"`UNIQ--vote-00000841-QINU`"' (1)
starting dose:
100 mg IV every 3 months; may increase to 300 mg IV every 3 months (1) · 150 mg PO once daily; titrate to 300 mg if needed (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) · 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)
preparations:
100 mg/20 mL vial, single-use (1) · 100 mg/mL vial for IV infusion (1) · 120 mg/mL prefilled syringe or autoinjector (1) · 75, 150, 300 mg tablets (1)
fda max:
240 mg loading + 120 mg/month for migraine; 300 mg/month for cluster (1) · 300 mg/d (1) · 300 mg/quarter (1) · Single 60-hour course (1)
routes:
Intravenous (continuous infusion in a REMS-certified facility) (1) · Intravenous infusion (1) · Oral (1) · Subcutaneous (1)
onset:
Antidepressant effect within hours of infusion start; sustained at 30 days (1) · BP effect within 1-2 weeks (1) · Effect demonstrated within 24 hours in some patients (1) · Over weeks (1)
duration:
24 hours (1) · 3-month dosing interval (1) · Monthly dosing (1) · Single infusion course (1)
halflife: (Click arrow to add another value)
bioavailability:
100% (IV) (2) · 60-80% (oral; not significantly affected by food)'"`UNIQ--ref-00000843-QINU`"' (1) · Not formally established (high SC) (1)
pregnancy:
'''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-00000844-QINU`"' (1) · Limited data; avoid (2) · Medicine is structurally identical to endogenous allopregnanolone; pregnancy considerations relate to breastfeeding during/after infusion. Limited data; brief interruption of breastfeeding considered (1)
legal:
Rx (2) · Rx; REMS program required (excessive sedation/loss of consciousness during infusion) (1) · [[USLegal:Prescription only|Rx-only]] in US (1)
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