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Drilldown: Medicines

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Medicines > classes : Botanical or Research material or [[:Category:Immunosuppressants|Immunosuppressant]]

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generic:
brand:
None (153) · (none, never marketed) (1) · Decadron (historical), Dexpak (taper pack), Hemady, Ozurdex (intravitreal) (1) · Deltasone, Rayos (delayed-release); mostly prescribed generically (1) · Humira; biosimilars Amjevita, Cyltezo, Hadlima, Hulio, Hyrimoz, Idacio, Yusimry, Abrilada (1) · Medrol (oral), Solu-Medrol (IV/IM), Depo-Medrol (depot injection) (1) · O-DSMT (1) · Prelone, Pediapred, Orapred ODT, Millipred, Veripred (1) · Sandimmune, Neoral (modified microemulsion, increased bioavailability), Gengraf, Restasis (ophthalmic) (1) · Trexall, Otrexup, Rasuvo, Xatmep, Rheumatrex (discontinued) (1)
classes: (Click arrow to add another value)
mechanism:
5-HT2A agonist (26) · Monoamine releasing agent (9) · GABAA positive allosteric modulator (8) · CB1/CB2 agonist (7) · Dopamine/norepinephrine reuptake inhibitor (5) · Potent 5-HT2A agonist (5) · None (4) · LSD analogue; 5-HT2A agonist (4) · Prodrug of LSD; 5-HT2A agonist (4) · Serotonin/norepinephrine/dopamine releasing agent (3) · Cathinone analogue; monoamine reuptake inhibitor (2) · Contains LSA (2) · Contains mescaline (2) · Dopamine and norepinephrine reuptake inhibitor (2) · NMDA antagonist (2) · Prodrug of GHB (2)
uses:
None (155) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-0000029D-QINU`"', '"`UNIQ--vote-0000029E-QINU`"', '"`UNIQ--vote-0000029F-QINU`"', '"`UNIQ--vote-000002A0-QINU`"', '"`UNIQ--vote-000002A1-QINU`"', '"`UNIQ--vote-000002A2-QINU`"' (1) · '"`UNIQ--vote-000007C1-QINU`"', '"`UNIQ--vote-000007C2-QINU`"', '"`UNIQ--vote-000007C3-QINU`"', '"`UNIQ--vote-000007C4-QINU`"', '"`UNIQ--vote-000007C5-QINU`"', '"`UNIQ--vote-000007C6-QINU`"', '"`UNIQ--vote-000007C7-QINU`"' (1) · '"`UNIQ--vote-00000862-QINU`"', '"`UNIQ--vote-00000863-QINU`"', '"`UNIQ--vote-00000864-QINU`"', '"`UNIQ--vote-00000865-QINU`"', '"`UNIQ--vote-00000866-QINU`"' (1) · '"`UNIQ--vote-000008C0-QINU`"', '"`UNIQ--vote-000008C1-QINU`"', '"`UNIQ--vote-000008C2-QINU`"', '"`UNIQ--vote-000008C3-QINU`"' (1) · '"`UNIQ--vote-00000A8C-QINU`"', '"`UNIQ--vote-00000A8D-QINU`"', '"`UNIQ--vote-00000A8E-QINU`"', '"`UNIQ--vote-00000A8F-QINU`"', '"`UNIQ--vote-00000A90-QINU`"' (1) · '"`UNIQ--vote-00000E23-QINU`"', '"`UNIQ--vote-00000E24-QINU`"', '"`UNIQ--vote-00000E25-QINU`"', '"`UNIQ--vote-00000E26-QINU`"', '"`UNIQ--vote-00000E27-QINU`"', '"`UNIQ--vote-00000E28-QINU`"', '"`UNIQ--vote-00000E29-QINU`"', '"`UNIQ--vote-00000E2A-QINU`"' (1)
starting dose:
None (154) · 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) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (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)
preparations:
None (154) · 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) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (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)
fda max:
None (154) · 40 mg every week (selected indications); otherwise 40 mg every other week (1) · Indication-specific (3) · N/A (never approved) (1) · No fixed maximum; cumulative-dose toxicity drives all chronic decisions (1) · Rheumatologic ~25 mg/week; oncology indication-specific (1) · Transplant: regimen-specific (1)
routes:
None (154) · IM (3) · intra-articular (2) · intramuscular (1) · intranasal; rectal and IV reported. (1) · intrathecal (1) · intrathecal (rare and controversial) (1) · intrathecal (rare) (1) · intravitreal (1) · IV (4) · IV (prednisolone sodium phosphate) (1) · ophthalmic (2) · Oral (7) · Subcutaneous (2) · sublingual (1)
onset:
None (154) · 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) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (154) · 2 weeks per dose (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (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)
halflife:
None (154) · 3-10 hours (low dose); 8-15 hours (high dose); much longer in third-space accumulation (pleural effusion, ascites)'"`UNIQ--ref-000007C8-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (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)
bioavailability:
None (154) · 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) · Not formally characterized in humans. (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)
pregnancy:
None (155) · '''Contraindicated in pregnancy''' (Category X); abortifacient and teratogenic. Discontinuation 3-6 months before conception is standard.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Avoid. Benzodiazepines are associated with neonatal sedation, floppy-infant syndrome, and withdrawal; teratogenic signal weak but non-zero. Designer benzo with no safety data, assume worst-case. (1) · Use when benefits outweigh; small association with oral clefts debated.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Use when benefits outweigh; small association with oral clefts in first trimester debated.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Used in antenatal lung maturation (24-34 weeks gestation; 6 mg IM q12h × 4 doses); broader use weighs benefits against fetal HPA suppression.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Used in transplant pregnancy when continued immunosuppression is required; reassuring data overall but careful monitoring needed.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Used when benefits outweigh risk; oral cleft signal in first-trimester exposure is debated and small in absolute terms.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (156) · [[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)

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