Table 2. DMARDs approved for the treatment of rheumatoid arthritis (cDMARD white, bDMARD olive).
| Active substance | Dosage | Strength of recommendation (S1 guideline [40]) | When? | Frequent adverse effects (>1/100; recorded using the treatment monitoring form of the DGRh [http://dgrh.de/therapieueberwachen.html] unless otherwise specified) |
|---|---|---|---|---|
| Abatacept | 10 mg/kg BW/ 4 weeks after induction phase | ↑ ↑ | As 1st or 2nd bDMARD following inadequate response to 2 cDMARDs | Hyperlipidemia, headache, dizziness, drowsiness, bronchitis, coughing, upper airway infections (including tracheitis, nasopharyngitis), rhinitis, abdominal pain, nausea, diarrhea, dyspepsia, skin rash, herpes simplex, urinary tract infection, tiredness, weight loss, hypertension, flushing |
| Adalimumab | 40 mg/2 weeks | ↑ ↑ | As 1st or 2nd bDMARD following inadequate response to 2 cDMARDs | Decreased hemoglobin concentration, hypertension, headache, dizziness, drowsiness, upper airway infections, rhinitis, sinusitis, bronchitis, increased coughing, pneumonia, nausea, diarrhea, sore throat, elevated transaminases, reactions at injection site, skin rash, pruritus, herpes simplex, urinary tract infection, weight loss, influenza syndrome |
| Anakinra | 100 mg/day | ↑ | As alternative to 1st or 2nd bDMARD | Reactions at injection site, headache |
| Antimalarial drugs | 4 mg chloroquine/kg or >6.5 mg hydroxychloroquine/kg BW/day | ↑ | As alternative to 2nd cDMARD or in combination with cDMARDs | Nausea, lack of appetite, diarrhea |
| Azathioprine | 2–3 mg/kg BW/day | – | As alternative to 2nd cDMARD | Nausea, vomiting, diarrhea, leukopenia, anemia, infection, drug fever |
| Certolizumab | 200 mg/ 2 weeks after induction phase | ↑ ↑ | As 1st or 2nd bDMARD following inadequate response to 2 cDMARDs | Urinary tract infection, herpes simplex, upper airway infections, headache, dizziness, skin rash, pruritus, exhaustion, pyrexia, pain and reddening at site of administration (product information 04/2009) |
| Cyclosporine | 2.5–3.5 mg/kg BW/day | ↑ | As alternative to 2nd cDMARD or in combination with cDMARDs | Lack of appetite, nausea and occasional vomiting, diarrhea, muscle twitching and cramp may indicate magnesium deficiency, slight trembling of hands, slight increase in body hair, swelling and inflammation of gums, hypertension, tiredness |
| Etanercept | 50 mg/week | ↑ ↑ | As 1st or 2nd bDMARD following inadequate response to 2 cDMARDs | Irritation at injection site, infections |
| Golimumab | 50 mg/month | ↑ ↑ | As 1st or 2nd bDMARD following inadequate response to 2 cDMARDs | Upper airway infections (nasopharyngitis, pharyngitis, laryngitis, rhinitis), bacterial infections (e.g., inflammation of subcutaneous tissue), viral infections (e.g., influenza and herpes), bronchitis, sinusitis, superficial fungal infections, anemia, allergic reactions (bronchospasm, hypersensitivity, urticaria), autoantibody positive, depression, sleeplessness, dizziness, paresthesias, headache, hypertension, obstipation, dyspepsia, gastrointestinal and abdominal pain, nausea, elevated ALT/GPT levels, elevated AST/GOT levels, alopecia, dermatitis, itching, skin rash, fever, asthenia, reaction at injection site (e.g., erythema, urticaria, induration, pain, bruising, itching, irritation und paresthesias), delayed wound healing, thoracic symptoms (product information 11/2012) |
| Infliximab | 3–5 mg/kg BW every 8 weeks after induction phase | ↑ ↑ | As 1st or 2nd bDMARD following inadequate response to 2 cDMARDs | Headache, dizziness, drowsiness, infections of upper and lower respiratory tract (e.g., sinusitis, pneumonia), nausea, diarrhea, elevated transaminases, urticaria, skin rash, pruritus, reactions to infusion |
| Leflunomide | 10–20 mg/day | ↑ ↑ | As alternative to 1st or 2nd cDMARD or in combination with cDMARDs | Diarrhea, nausea, vomiting, abdominal pain, mouth ulcers, elevated liver parameters, leukocytopenia, headache, dizziness, asthenia, hypertension, eczema, hair loss, skin rash, itching, weight loss, mutagenicity, teratogenicity (both in animal experiments) |
| Methotrexate | 10–25 mg/week | ↑ ↑ | As 1st cDMARD or in combination with cDMARDs and especially bDMARDs | Stomatitis, hair loss, nausea, vomiting, elevated transaminases |
| Parenteral gold | 50 mg/ 2 weeks after initial phase | ↑ | As alternative to 2nd cDMARD | Dermatitis, stomatitis, pruritus, eosinophilia, proteinuria, deposits on cornea/lens if gold dose >1500 mg (harmless), metallic taste |
| Rituximab | Two doses of 1000 mg at a 2-week interval every 6–12 months | ↑ ↑ | As 2nd bDMARD following inadequate response to 2 cDMARDs | Airway infections, reactions to infusion, influenza-like symptoms, infections, transitory hyperuricemia (15%) |
| Sulfasalazine | 2 g/day after initial phase | ↑ | As alternative to 1st or 2nd cDMARD or in combination treatment with cDMARDs | Exanthema, pruritus, nausea, abdominal pain, lack of appetite, hyperchromasia, oligospermia, reversible loss of fertility in men, headache, feeling of weakness, tiredness |
| Tocilizumab | 8 mg/kg BW every 28 days | ↑ ↑ | As 1st or 2nd bDMARD following inadequate response to 2 cDMARDs | Skin and subcutaneous infections, pneumonia, oral herpes simplex, herpes zoster, mouth ulcers, gastritis, exanthema, pruritus, headache, dizziness, elevated transaminases, hypertension, leukopenia, neutropenia, conjunctivitis |
↑, These recommendations are based on studies in which the certainty of the findings is limited and/or the benefits only slightly outweigh the risks. ↑ ↑, These recommendations are based on studies with a high level of certainty in which the benefits are shown to clearly outweigh the risks. DMARD, disease-modifying antirheumatic drug; bDMARD, biological DMARD; cDMARD, classic synthetic DMARD; DGRh, Deutsche Gesellschaft für Rheumatologie (German Society for Rheumatology)