Medications in Rheumatology

Mariana Gonzalez Trevino


Background

  • "-cept" refers to fusion of a receptor to the Fc part of human immunoglobulin G1 (IgG1).
  • "-mab" indicates a monoclonal antibody (mAb).
  • "-ximab" indicates a chimeric mAb.
  • "-zumab" indicates a humanized mAb.
  • "-umab" indicates a fully human mAb.
  • “-tinib” indicates a tyrosine kinase inhibitor (small molecule inhibitors, not true biologics).
Drug NameIndicationsMechanism of ActionCommon ToxicitiesHold or Continue on Admission/Clinic?
NSAIDsPain, inflammation in RA, SpA, goutCOX-1/COX-2 inhibition → decreased prostaglandin synthesisGI bleeding, AKI, hypertension, cardiovascular events, platelet dysfunction. CV risk lower with naproxen. GI risk lower with celecoxib.HOLD for: severe infection, AKI, GI bleeding, volume depletion, TBI/ICH, perioperative bleeding risk. Continue for: mild infections if renal function stable
ColchicineGout, CPPD, pericarditis, FMFMicrotubule inhibition → decreased neutrophil migration and inflammasome assemblyGI intolerance (5-8%), myelosuppression (rare), neuromuscular toxicity, rhabdomyolysisHOLD for: severe infection, CrCl <30, severe hepatic dysfunction (Child-Pugh C), concurrent strong CYP3A4/P-gp inhibitors (clarithromycin, azoles, cyclosporine). Continue for: mild infections, stable disease
AllopurinolGout (first line ULT), hyperuricemia with cancer therapy, recurrent calcium oxalate stonesXanthine oxidase inhibitor → blocks conversion of hypoxanthine to xanthine and xanthine to uric acidRash (most common), allopurinol hypersensitivity syndrome (AHS) (rare but potentially fatal: SJS/TEN, DRESS), hepatotoxicity, myelosuppression, AKIHOLD for: new rash (evaluate for hypersensitivity), severe AKI (dose adjust or hold), severe hepatic dysfunction. HLA-B58:01 screening recommended in high-risk populations (Black Americans, Han Chinese, Thai, Korean) before starting. Avoid with azathioprine/6-mercaptopurine (increased toxicity)
FebuxostatGout (second-line ULT: inadequate response/intolerance of allopurinol)Non-purine xanthine oxidase inhibitor → more potent than allopurinol; no dose adjustment needed in mild-moderate CKDHepatotoxicity, GI upset, rash, arthralgia, FDA black box warning: increased CV mortalityCONTINUE for: most admissions (stopping may trigger flare). HOLD for: ALT/AST >3× ULN (investigate cause), serious skin reactions, acute CV event. Avoid with azathioprine/6-mercaptopurine (increased toxicity)
MethotrexateRA, PsA, SLE, vasculitisIncreases extracellular adenosine at low doses used for rheumatologic indicationsHepatotoxicity, cytopenias, pneumonitis (rare in RA), mucositis, nauseaContinue for: stable patients, perioperatively. HOLD for: active infection (especially respiratory), severe cytopenias, transaminases >3× ULN, AKI. Supplement with folic acid to reduce toxicity. Monitor CBC, LFTs, Cr q3-4 months
LeflunomideRA, PsAPyrimidine synthesis inhibitorHepatotoxicity, diarrhea, alopecia, hypertension, cytopeniasContinue for: stable patients. HOLD for: active infection, severe hepatic dysfunction, cytopenias. Monitor CBC, LFTs, Cr. Cholestyramine washout if toxicity/unexpected pregnancy.
SulfasalazineRA, SpA, IBD5-ASA + sulfapyridine → anti-inflammatoryGI upset, rash, hepatotoxicity, cytopenias, oligospermiaContinue for: most admissions including perioperatively. HOLD for: severe infection, severe cytopenias. Monitor CBC, LFTs, Cr q3-4 months
HydroxychloroquineRA, SLELysosomal pH alteration → immune modulationRetinopathy (rare 1%), cardiomyopathy, QT prolongation, GI upsetContinue for: most admissions including perioperatively, even with infections. No infection risk. Caution with CKD → higher risk of toxicity. Monitor: baseline and annual eye exams, periodic CBC
AzathioprineSLE, vasculitis, myositisPurine analog → inhibits DNA synthesisMyelosuppression, hepatotoxicity, pancreatitis, increased malignancy riskHOLD for: active infection, severe cytopenias, perioperatively. Continue for: stable patients without infection. Check TPMT before starting. Monitor CBC, LFTs q3-4 months
MycophenolateSLE, LN, ILD, vasculitis, myositisInhibits inosine monophosphate dehydrogenase → lymphocyte proliferationGI upset, myelosuppression, increased infection riskHOLD for: active infection, perioperatively. Continue for: stable patients without infection. Monitor CBC q3-4 months
Calcineurin inhibitors (cyclosporine, tacrolimus, voclosporin)LN, myositisInhibit calcineurin → suppress IL-2 and T-cell activation; stabilize podocytesNephrotoxicity, HTN, hyperkalemia, hypomagnesemia, tremor. Cyclosporine: gingival hyperplasia, hirsutism, hyperlipidemia. Tacrolimus: hyperglycemia/DM. Voclosporin: QT prolongationCONTINUE for: stable patients, perioperatively (case-by-case). HOLD for: active serious infection, AKI (Cr↑>25-30%), severe HTN, neurotoxicity. Monitor: Trough levels (cyclosporine/tacrolimus; voclosporin does NOT require monitoring), Cr, BP, K+, Mg2+, glucose, LFTs. Drug interactions: Avoid grapefruit; caution with CYP3A4 inhibitors
TNF Inhibitors (adalimumab, etanercept, infliximab, golimumab, certolizumab)RA, PsA, SpA, IBDTNF-α blockade → decreased inflammationSerious infections (TB, fungal), malignancy, demyelination, CHF exacerbation, lupus-like syndromeHOLD for: active infection (restart 7-14 days after symptom resolution). Continue perioperatively (hold 1 dosing interval before surgery). Screen for TB, hepatitis B/C at baseline
IL-17 Inhibitors (secukinumab, ixekizumab, brodalumab, bimekizumab)PsA, SpA, psoriasisIL-17 blockade → inhibits Th17-mediated inflammation at entheses, skin, jointsMucocutaneous candidiasis, upper respiratory infections, injection site reactions, new-onset or exacerbation of IBD (avoid in active IBD), neutropenia (rare), hepatotoxicity (rare).CONTINUE for: low-risk procedures, mild infections, perioperatively (case-by-case). HOLD for: active serious infection, active IBD or new GI symptoms (bloody diarrhea), severe neutropenia. Absolute contraindications: Active IBD, active TB, bacterial infection, hepatitis B. Restart 7-14 days after infection resolution. Monitor: Periodic assessment for infections, IBD symptoms, suicidal ideation (brodalumab)
IL-6 Inhibitors (tocilizumab, sarilumab)RA, GCA, SJIA/AOSD, PMRIL-6 receptor blockadeSerious infections, GI perforation, diverticulitis, hepatotoxicity, cytopenias, hyperlipidemiaHOLD for: active infection, diverticulitis. CRP not a reliable inflammatory marker while on IL-6 inhibitors (suppressed). Monitor CBC, LFTs at 4-8 weeks then q3 months; lipids at weeks 4, 8 then q6 months
IL-1 Inhibitors (anakinra, canakinumab)SJIA/AOSD, autoinflammatory syndromes, gout, HLHIL-1 blockadeInjection site reactions (anakinra), neutropenia, increased infection riskMay continue for: autoinflammatory conditions even with mild infection (case-by-case). HOLD for: severe infection. Monitor CBC monthly x3 months then q3 months
Anti-CD20 (rituximab, obinutuzumab)RA, vasculitis, SLE, LNB-cell depletionInfusion reactions, hypogammaglobulinemia, cytopeniasHOLD for: active infection. Dosed q6 months; plan surgery in month 7. Monitor CBC q2-4 months. Screen for hepatitis B. Vaccination prior to initiation.
BelimumabSLE, LNBLyS (B-lymphocyte stimulator)-inhibitor → inhibits B-cell survivalInfusion/injection reactions, infections, depression/psychiatric events, hypersensitivity.CONTINUE for: most admissions, perioperatively. HOLD for: active serious infection, severe hypersensitivity reaction. Restart after infection resolution.
JAK Inhibitors (tofacitinib, baricitinib, upadacitinib)RA, PsA, SpA, UC, GCAJAK-STAT pathway inhibitionHerpes zoster, serious infections, MACE (age >50 with CV risk), VTE, malignancy, hyperlipidemiaHOLD for: active infection (restart 7-14 days after resolution). Hold 3-7 days preoperatively. Monitor CBC, LFTs at 4-8 weeks then q3 months; lipids at 4-8 weeks then q6 months
Complement Inhibitors (avacopan, eculizumab, ravulizumab)Avacopan: ANCA-associated vasculitis. Eculizumab/Ravulizumab: PNH, aHUS, AChR+ myasthenia gravis, NMOSD (AQP4+)Avacopan: C5a receptor antagonist (does not block MAC). Eculizumab/Ravulizumab: Anti-C5 monoclonal antibodies blocking terminal complement (MAC formation)Avacopan: Hepatotoxicity, nausea, headache. Eculizumab/Ravulizumab: BLACK BOX—meningococcal infection; headache, URI, nauseaContinue during hospitalization (flare risk if held). Eculizumab/Ravulizumab: Maintain meningococcal prophylaxis (penicillin or ciprofloxacin); requires MenACWY + MenB vaccination; if febrile → urgent meningococcal evaluation

Key Pearls for Inpatient Management (Always Confirm with Rheumatology)

  • General approach to infections: For most DMARDs and biologics, hold during active infection and restart 7-14 days after symptom resolution for uncomplicated infections.
    Hydroxychloroquine and sulfasalazine have relatively low infection risk and can often be continued.
  • Disease flare risk: Discontinuing DMARDs/biologics increases flare risk (31-61% in studies), which may necessitate rescue glucocorticoids and increase infection risk. Balance infection risk against disease control on a case-by-case basis.
  • Drug interactions: Colchicine requires dose reduction or temporary hold with strong CYP3A4/Pgp inhibitors (clarithromycin, azoles, cyclosporine, ritonavir/Paxlovid).
  • Renal/hepatic dysfunction: Adjust or hold methotrexate (CrCl <30), leflunomide (severe hepatic disease), colchicine (CrCl <30), and azathioprine (severe hepatic disease).
  • Screening prior to initiation varies based on specific agent. Consider latent TB (via IGRA), Hepatitis B/C, HIV, age-appropriate cancer screening, pregnancy counseling. Discuss with rheumatology required vaccinations prior to treatment initiation.

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