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: Anticonvulsant

or [[:Category:Immunosuppressants|Immunosuppressant]]

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Aptiom (1) · Banzel (1) · Briviact (1) · Cerebyx (1) · Decadron (historical), Dexpak (taper pack), Hemady, Ozurdex (intravitreal) (1) · Deltasone, Rayos (delayed-release); mostly prescribed generically (1) · Depakote (1) · Diacomit (1) · Dilantin (1) · Epidiolex (1) · Felbatol (1) · Fintepla (1) · Fycompa (1) · Gabitril (1) · Humira; biosimilars Amjevita, Cyltezo, Hadlima, Hulio, Hyrimoz, Idacio, Yusimry, Abrilada (1) · Luminal (1) · Medrol (oral), Solu-Medrol (IV/IM), Depo-Medrol (depot injection) (1) · Onfi (1) · Prelone, Pediapred, Orapred ODT, Millipred, Veripred (1) · Sabril (1) · Sandimmune, Neoral (modified microemulsion, increased bioavailability), Gengraf, Restasis (ophthalmic) (1) · Trexall, Otrexup, Rasuvo, Xatmep, Rheumatrex (discontinued) (1) · Vimpat (1) · Xcopri (1) · Zarontin (1) · Zonegran (1)

None (4) · AMPA receptor antagonist (1) · GABA enhancer; sodium channel blocker; histone deacetylase inhibitor (1) · GABA reuptake inhibitor (GAT-1 blocker) (1) · GABAA positive allosteric modulator (1) · GABAA positive allosteric modulator; lactate dehydrogenase inhibitor (1) · GABAA potentiator and direct activator (1) · Irreversible GABA-T inhibitor (1) · Multiple mechanisms; GPR55 antagonist; TRPV1 agonist (1) · NMDA antagonist; GABAA potentiator (1) · Prodrug of phenytoin; sodium channel blocker (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-00000860-QINU`"' Activates the glucocorticoid receptor to broadly remodel inflammatory, immune, and metabolic transcription. Unlike prednisone, it does not require hepatic activation, making it the preferred oral choice in severe hepatic dysfunction'"`UNIQ--ref-00000861-QINU`"'. (1) · '"`UNIQ--vote-000008BE-QINU`"' Preferred over prednisone in advanced hepatic dysfunction where hepatic 11β-HSD1 activation is impaired. Liquid formulations are the workhorse pediatric oral corticosteroid for asthma and croup'"`UNIQ--ref-000008BF-QINU`"'. (1) · '"`UNIQ--vote-000010F8-QINU`"' Pre-treatment screening for latent TB (PPD or IGRA) and chronic hepatitis B is standard. Anti-drug antibody formation is a recognized cause of secondary loss of response'"`UNIQ--ref-000010F9-QINU`"'. (1)

None (19) · 0.5-2 mg/kg/d divided or single morning dose for acute conditions; lowest effective dose for chronic conditions, with planned taper (1) · 40 mg SC every other week (most adult indications); IBD induction 160 mg week 0, 80 mg week 2, then 40 mg every other week (1) · Indication-specific: 0.5-9 mg PO/IV daily for inflammation; 4 mg IV q6h for cerebral edema; 40 mg PO once weekly in MM; 6 mg PO/IV daily ×10 days for severe COVID-19; 0.6 mg/kg PO single dose for croup (max 16 mg) (1) · Pediatric 1-2 mg/kg/d (max 60 mg) PO for asthma exacerbation; adult dosing similar to prednisone milligram-for-milligram (~1:1 potency) (1) · PO Medrol Dosepak (5-day taper from 24 mg to 4 mg) is the prototypic short-course outpatient regimen; IV pulse 1 g daily for 3-5 days for MS relapse; intra-articular 4-80 mg per joint q1-5 weeks (1) · Rheumatologic: 7.5-15 mg PO or SC '''once weekly''' (not daily — daily dosing is a recognized fatal error); folic acid 1 mg PO daily on non-MTX days; oncology dosing is far higher and indication-specific (1) · Transplant: 5-10 mg/kg/d divided BID, titrated to trough levels (typically 100-300 ng/mL depending on regimen and post-transplant interval); ophthalmic Restasis 0.05% one drop BID (1)

None (19) · 0.5, 0.75, 1, 1.5, 2, 4, 6 mg tablets; oral solution; 4, 10, 20, 100 mg/mL IV; intravitreal implant (Ozurdex) (1) · 1, 2.5, 5, 10, 20, 50 mg tablets; 5 mg/5 mL syrup; 5 mg/mL concentrate (1) · 2, 4, 8, 16, 32 mg oral tablets; 40, 125, 500, 1000 mg IV vials; Depo-Medrol 20, 40, 80 mg/mL IM depot (1) · 2.5 mg tablets; 10-50 mg/mL injection; pre-filled subcutaneous autoinjectors (Otrexup, Rasuvo); 2.5 mg/mL oral solution (Xatmep) (1) · 40 mg/0.4 mL or 40 mg/0.8 mL prefilled syringe and autoinjector pen; 10, 20, 80 mg pediatric/induction strengths (1) · 5 mg tablets; 5 mg/5 mL, 10 mg/5 mL, 15 mg/5 mL oral solutions (sweetened pediatric); 5 mg/5 mL syrup; ophthalmic 0.12%, 1% suspensions and 1% solution (1) · Sandimmune 25, 100 mg capsules; Neoral 25, 100 mg modified soft gel; 100 mg/mL oral solution; 50 mg/mL IV; Restasis 0.05% ophthalmic emulsion (1)

None (19) · 40 mg every week (selected indications); otherwise 40 mg every other week (1) · Indication-specific (3) · No fixed maximum; cumulative-dose toxicity drives all chronic decisions (1) · Rheumatologic ~25 mg/week; oncology indication-specific (1) · Transplant: regimen-specific (1)

None (19) · IM (3) · intra-articular (2) · intramuscular (1) · intrathecal (1) · intrathecal (rare and controversial) (1) · intrathecal (rare) (1) · intravitreal (1) · IV (4) · IV (prednisolone sodium phosphate) (1) · ophthalmic (2) · Oral (6) · Subcutaneous (2)

None (19) · Days for immunosuppressive effect (1) · Hours (3) · IV pulse: hours; PO: hours; intra-articular: days (1) · Rheumatologic effect at 4-8 weeks; ectopic resolution over 2-3 weeks (1) · Symptomatic effect within weeks; full response by 12-24 weeks (1)

None (19) · 2 weeks per dose (1) · Biologic 12-36 hours (intermediate-acting) (1) · Biologic 12-36 hours (intermediate-acting); Depo-Medrol depot weeks (1) · Biologic 36-72 hours (long-acting) (1) · Biologic half-life ~12-36 hours (intermediate-acting); plasma half-life shorter (1) · Dosing-frequency dependent (1) · Once-weekly dosing in rheumatology (1)

None (19) · 3-10 hours (low dose); 8-15 hours (high dose); much longer in third-space accumulation (pleural effusion, ascites)'"`UNIQ--ref-000007C8-QINU`"' (1) · Plasma 2-3 hours; biologic ~18-36 hours'"`UNIQ--ref-00000867-QINU`"' (1) · Plasma 2-3 hours; biologic ~18-36 hours'"`UNIQ--ref-000008C4-QINU`"' (1) · Plasma 3-4 hours; biologic ~12-36 hours'"`UNIQ--ref-000002A3-QINU`"' (1) · Plasma ~3-4.5 hours; biologic ~36-72 hours'"`UNIQ--ref-00000E2B-QINU`"' (1) · ~14 days'"`UNIQ--ref-00001103-QINU`"' (1) · ~8-27 hours (highly variable across the population)'"`UNIQ--ref-00000A91-QINU`"' (1)

None (19) · 60-70% PO at low doses; saturable at high doses (parenteral routes preferred above 15-25 mg/week)'"`UNIQ--ref-000007C9-QINU`"' (1) · 70-80% (oral)'"`UNIQ--ref-000002A4-QINU`"' (1) · Sandimmune: highly variable (~30%); Neoral microemulsion: ~50%, less variable; '''Sandimmune and Neoral are NOT bioequivalent and not interchangeable''''"`UNIQ--ref-00000A92-QINU`"' (1) · ~64% from SC depot'"`UNIQ--ref-00001104-QINU`"' (1) · ~70% (oral)'"`UNIQ--ref-000008C5-QINU`"' (1) · ~80% (oral)'"`UNIQ--ref-00000E2C-QINU`"' (1) · ~80-99% (oral)'"`UNIQ--ref-00000868-QINU`"' (1)

None (20) · '''Contraindicated in pregnancy''' (Category X); abortifacient and teratogenic. Discontinuation 3-6 months before conception is standard.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Use when benefits outweigh; small association with oral clefts debated.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Use when benefits outweigh; small association with oral clefts in first trimester debated.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Used in antenatal lung maturation (24-34 weeks gestation; 6 mg IM q12h × 4 doses); broader use weighs benefits against fetal HPA suppression.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Used in transplant pregnancy when continued immunosuppression is required; reassuring data overall but careful monitoring needed.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Used when benefits outweigh risk; oral cleft signal in first-trimester exposure is debated and small in absolute terms.[[[Pharmacopedia:Citation needed|citation needed]]] (1)

None (20) · [[USLegal:Prescription only|Rx-only]] in US (5) · [[USLegal:Prescription only|Rx-only]] in US. Carries '''Boxed Warning''' for risk of malignancy and serious infection; nephrotoxicity, hypertension, and immunosuppression-associated complications'"`UNIQ--ref-00000A93-QINU`"' (1)