What are effective oral medications for Rheumatoid Arthritis (RA)?

From the Guidelines

Methotrexate is the most effective oral medication for Rheumatoid Arthritis (RA) and should be started at a dose of 10-15 mg/week, with escalation of 5 mg every 2-4 weeks up to 20-25 mg/week, depending on clinical response and tolerability, as recommended by the most recent and highest quality study 1.

Key Points

• Methotrexate is the first-line treatment for most patients with RA, due to its efficacy, acceptable toxicity profile, and low costs 1.
• The optimal dosage and route of administration of methotrexate in RA is to start with 10-15 mg/week orally, escalating with 5 mg every 2-4 weeks up to 20-25 mg/week, depending on clinical response and tolerability 1.
• Other effective oral medications for RA include hydroxychloroquine, leflunomide, and sulfasalazine, which can be used in combination with methotrexate or as alternative treatments 1.
• For symptom management, NSAIDs like naproxen or celecoxib can be used alongside disease-modifying drugs, and oral JAK inhibitors such as tofacitinib, baricitinib, or upadacitinib may be prescribed in more severe cases or when traditional DMARDs are ineffective 1.

Monitoring and Safety

• Regular monitoring of blood counts, liver function, and kidney function is essential with these medications to ensure safety and effectiveness 1.
• Patients should take folic acid supplements (1 mg daily) to reduce side effects associated with methotrexate therapy 1.

Treatment Goals

• The main goal of DMARD treatment is to achieve clinical remission, and regular monitoring of disease activity, adverse events, and comorbidities should guide decisions on choice and changes in treatment strategies to reach this target 1.

From the FDA Drug Label

Leflunomide is indicated in adults for the treatment of active rheumatoid arthritis (RA): to reduce signs and symptoms to inhibit structural damage as evidenced by X-ray erosions and joint space narrowing to improve physical function Single oral doses of 7.5 mg once weekly.† Divided oral dosages of 2.5 mg at 12 hour intervals for 3 doses given as a course once weekly.

The effective oral medications for Rheumatoid Arthritis (RA) are:

• Methotrexate: 7.5 mg once weekly or 2.5 mg at 12 hour intervals for 3 doses given as a course once weekly 2
• Leflunomide: 20 mg per day after an initial loading dose of 100 mg per day for three days 3, 3

From the Research

Effective Oral Medications for Rheumatoid Arthritis (RA)

• Methotrexate (MTX) is considered the drug of choice for the treatment of RA due to its favorable risk/benefit ratio, good safety profile, and low costs 4, 5, 6, 7.
• The optimal dosage of MTX is a starting dose of 15 mg/week orally, escalating to 25 to 30 mg/week or the highest tolerable dose 4, 8.
• Oral MTX is widely preferred due to its low costs and patient preferences, but parenteral MTX has higher bioavailability 4.
• MTX treatment can be initiated with oral administration, but parenteral administration is indicated in patients with poor compliance toward the oral form 4.
• The subcutaneous route of MTX administration may be more effective than the oral route due to better usability and absence of pain at the infusion site 4, 8.
• Methotrexate is generally well-tolerated, but has important potential side-effects including a risk of liver toxicity and cytopenias, and requires diligent monitoring 6, 7.