Antiinflammatory Drugs: Disease-Modifying Antirheumatic Drugs

Golimumab

Route and Dosage:
Rheumatoid arthritis:A: Subcut: 50 mg every month
A: IV: 2 mg/kg over 30 min, repeat after 4 wk, then q8wk

Uses and Considerations:
For RA, psoriatic arthritis, ankylosing spondylitis, and ulcerative colitis. May cause injection site reaction, antibody development, hypertension, elevated hepatic enzymes, influenza, and infection. PB: UK; t½: 2 wk

Anakinra

Route and Dosage:
Rheumatoid arthritis:A: Subcut: 100 mg/d; max: 100 mg/d

Uses and Considerations:
For RA and COVID-19. May cause injection-site reaction, headache, fever, nausea, vomiting, diarrhea, abdominal pain, arthralgia, pharyngitis, sinusitis, antibody formation, and infection. PB: UK; t½: 4–6 h

Etanercept

Route and Dosage:
Psoriasis:
A: Subcut: 50 mg twice weekly for 3 months, then 50 mg/wk; max: 100 mg/wk

Uses and Considerations:
For RA, psoriatic arthritis, psoriasis, and ankylosing spondylitis. May cause injection site reaction, antibody formation, diarrhea, pharyngitis, rash, sinusitis, influenza, and infection. PB: UK; t½: 72–132 h

Infliximab

Route and Dosage:
Rheumatoid arthritis:
A: IV: Initially 3 mg/kg over 2 h on wk 0, 2, and 6; maint: 3 mg/kg q8wk; max: 10 mg/kg/dose q4wk
Crohn disease:
A: IV: Initially 5 mg/kg over 2 h on wk 0, 2, and 6; maint: 5–10 mg/kg q8wk; max: 10 mg/kg/dose

Uses and Considerations:
To treat psoriasis, rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, ulcerative colitis, and Crohn disease

Rituximab

Route and Dosage:
Rheumatoid arthritis:
A: IV: 1000 mg on day 1 and day 15, then q24wk

Uses and Considerations:
For RA, lymphocytic leukemia, and non-Hodgkin lymphoma. May cause antibody formation, headache, depression, fever, chills, peripheral edema, anemia, nausea, diarrhea, abdominal pain, alopecia, dizziness, angioedema, peripheral neuropathy, infection, and weakness. PB: UK; t½: 5.17–77.5 d

Adalimumab

Route and Dosage:
Rheumatoid arthritis:
A: Subcut: 40 mg q2wk; max: 40 mg/wk or 80 mg q2wk

Uses and Considerations:
For RA, psoriatic arthritis, Crohn disease, ulcerative colitis, psoriasis, and ankylosing spondylitis. May cause injection site reaction, headache, nausea, abdominal pain, infection, rash, sinusitis, and antibody formation. PB: UK; t½: 10–20 d

Leflunomide

Route and Dosage:
A: PO: LD:100 mg/d for 3 d; maint: 10–20 mg/d

Uses and Considerations:
For RA. May cause hypertension, dizziness, headache, alopecia, rash, abdominal pain, weakness, back pain, elevated hepatic enzymes, dyspepsia, nausea, diarrhea and infection. PB: 99%; t½: 18–19 d

Abatacept

Route and Dosage:
Rheumatoid arthritis:
A >100 kg: IV: 1 g over 30 min q2wk for 3 doses, then 1 g q4wk
A 60–100 kg: IV: 750 mg over 30 min q2wk for 3 doses, then q4wk
A <60 kg: IV: 500 mg over 30 min q2wk for 3 doses, then q4wk
A: Subcut: 125 mg/wk

Uses and Considerations:
For RA and psoriatic arthritis. May cause dizziness, headache, diarrhea, pharyngitis, sinusitis, antibody formation, infection, hypo/hypertension, influenza, and infusion-related reaction. PB: UK; t½: 14.3 d

Tofacitinib

Route and Dosage:
Immediate release:
A: PO: 5 mg bid; max: 10 mg bid
Extended release:
A: PO: 11 mg/d; max: 11 mg/d

Uses and Considerations:
For RA, psoriatic arthritis, and ulcerative colitis. May cause headache, nausea, diarrhea, gastritis, pharyngitis, infection, anemia, and rash. PB: 40%; t½: 3 h immediate release, 6–8 h extended release

Tocilizumab

Route and Dosage:
A: IV: Initially 4 mg/kg over 1 h q4wk; max: 800 mg/dose
A <100 kg: Subcut: 162 mg q2wk
A >100 kg: Subcut: 162 mg/wk

Uses and Considerations:
For RA and juvenile idiopathic arthritis. May cause infusion/injection-related reaction, headache, hyperlipidemia, elevated hepatic enzymes, neutropenia, infection, pharyngitis, constipation, and hypertension. PB: UK; t½: subcut 5–13 d; IV, 11–13 d

Secukinumab

Route and Dosage:
Psoriasis:
A: Subcut: 300 mg wk 0–4, followed by 300 mg q4wk; max: 300 mg/dose

Uses and Considerations:
For psoriasis, psoriatic arthritis, and ankylosing spondylitis. May cause oral ulceration, neutropenia, infection, pharyngitis, rhinitis, and antibody formation. PB: UK; t½: 22–31 d

Apremilast

Route and Dosage:
Psoriatic arthritis:
A: PO: Initially 10 mg in the morning; day 2, 10 mg bid; day 3, 10 mg in morning and 20 mg in evening; day 4, 20 mg bid; day 5, 20 mg in morning and 30 mg in evening; maint: 30 mg bid starting on day 6; max: 60 mg/d

Uses and Considerations:
For psoriatic arthritis and psoriasis. May cause headache, abdominal pain, nausea, vomiting, diarrhea, weight loss, and infection. PB: 68%; t½: 6–9 h

Canakinumab

Route and Dosage:
Adol/C >2 y >7.5 kg: Subcut: 4 mg/kg q4wk; max: 300 mg/dose
A: Subcut: 4 mg/kg q4wk; max: 300 mg/dose

Uses and Considerations:
For systemic juvenile idiopathic arthritis. May cause headache, injection-site reaction, nausea, abdominal pain, diarrhea, weight gain, musculoskeletal pain, pharyngitis, rhinitis, influenza, and infection. PB: UK; t½: 26 d

Sarilumab

Route and Dosage:
A: Subcut: 200 mg q2wk; reduce dose to 150 mg q2wk to manage elevated hepatic enzymes, neutropenia, and thrombocytopenia

Uses and Considerations:
For moderate to severe rheumatoid arthritis and COVID-19. May cause elevated hepatic enzymes, antibody formation, erythema, infection, pruritus, neutropenia, thrombocytopenia, injection site reaction, and hypercholesterolemia. PB: UK; t½: 8–43 d depending upon concentration

Ixekizumab

Route and Dosage:
Psoriatic arthritis:
A: Subcut: LD: 160 mg/wk, then 80 mg q4wk

Uses and Considerations:
For psoriatic arthritis and plaque psoriasis. May cause antibody formation, infection, injection site reaction, neutropenia, influenza, ocular infection, conjunctivitis, and nausea. PB: UK; t½: 13 d

Certolizumab pegol

Route and Dosage:
Rheumatoid arthritis:A: Subcut: Two 200 mg on wk 0, 2, 4; then 200 mg q2wk or 400 mg q4wk

Uses and Considerations:
For Crohn disease, rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, and plaque psoriasis. Should be given as monotherapy or concomitantly with nonbiological disease-modifying antirheumatic drugs. May cause antibody formation, infection, arthralgia, back pain, headache, hypertension, rash, pharyngitis, fatigue, and cough. PB: UK; t½: 14 d

Baricitinib

Route and Dosage:
Rheumatoid arthritis:A: PO: 2 mg/d

Uses and Considerations:
For RA and COVID-19. May cause infection, nausea, and elevated hepatic enzymes. PB: 45%; t½: 12 h

Upadacitinib

Route and Dosage:
A: PO: 15 mg/d

Uses and Considerations:
For RA. May cause infection, cough, nausea, lymphopenia, neutropenia, and elevated hepatic enzymes. PB: 52%; t½: 8–14 h