Strategy and principles of treatment
Therapy for rheumatoid arthritis and other autoimmune pathologies requires a systemic and balanced approach. The clinician's primary objective is to achieve sustained remission and protect the patient's joints from irreversible destruction.
The key rule of rheumatology: treatment with disease-modifying antirheumatic drugs must be started immediately upon establishing a precise diagnosis.
To achieve maximum efficacy, a combination regimen is used:
- A DMARD (acts as the foundation of treatment by influencing pathogenesis).
- Nonsteroidal anti-inflammatory drugs (NSAIDs) to control active inflammation and pain.
- Glucocorticoids (GCs) in low doses.
The minimum continuous course of DMARD therapy is 3 months. This is because they are slow-acting drugs: their therapeutic effect develops gradually.
Classification of DMARDs
DMARDs are divided into several classes based on their chemical structure and sites of action within the immune system:
- Gold compounds: the classical representative is auranofin.
- 4-Aminoquinoline derivatives: originally developed as synthetic antimalarial agents (chloroquine, hydroxychloroquine, known as Plaquenil).
- Targeted therapy (proinflammatory cytokine inhibitors): selectively block inflammatory mediators. These include:
- Interleukin-1 (IL-1) receptor antagonists: anakinra.
- Tumor necrosis factor (TNF-alpha) inhibitors: etanercept, infliximab.
- Cytostatics and immunosuppressants: a broad group including methotrexate, leflunomide, azathioprine, sulfasalazine, and penicillamine.
Characteristics of key immunosuppressants
Let us examine several important drugs from the synthetic DMARD group, their mechanisms, and application features in more detail.
Azathioprine Pharmacologically, this is a prodrug. Upon entering the body, it is metabolized in the liver into active 6-mercaptopurine. This substance inhibits nucleic acid synthesis, thereby suppressing the proliferation of immune cells. It is used for rheumatoid arthritis (in combination with NSAIDs and low-dose GCs) and systemic lupus erythematosus. It is strictly contraindicated during pregnancy and lactation.
Penicillamine It is a structural analogue of the amino acid cysteine. The drug effectively slows down bone tissue destruction in rheumatoid arthritis. Interestingly, in addition to rheumatology, it acts as a potent antidote for heavy metal poisoning and is also prescribed for cystinuria.
Sulfasalazine Often used for mild forms of rheumatoid arthritis. In complex cases, a combination therapy regimen is used: sulfasalazine is prescribed together with chloroquine and methotrexate.
Toxicity and adverse effects
Interference with the immune system and the cell cycle inevitably entails serious risks that require constant monitoring.
| Drug / Group | Specific risks and side effects |
|---|---|
| 4-Aminoquinoline derivatives (chloroquine) | Ocular toxicity. They accumulate in ocular tissues, causing retinopathy, corneal opacity, and decreased visual acuity. |
| Penicillamine | Prolonged use causes nephrotoxicity ( nephritis) and hematotoxicity (aplastic anemia). |
| Sulfasalazine | Development of leukopenia is possible. |
Important tactic: Regular ophthalmological monitoring is mandatory during treatment with chloroquine or hydroxychloroquine. At the very first visual complaints, the drug must be discontinued immediately.
Briefly: answers to topical questions
Which drugs belong to tumor necrosis factor (TNF-alpha) inhibitors?
Tumor necrosis factor (TNF-alpha) inhibitors include:
- Etanercept.
- Infliximab.
- Adalimumab.
- Golimumab.
- Certolizumab pegol.
Which drugs are included in the group of cytostatics and immunosuppressants in the treatment of rheumatoid arthritis?
The group of cytostatics and immunosuppressants in the treatment of rheumatoid arthritis includes:
- Methotrexate.
- Leflunomide.
- Penicillamine.
- Azathioprine.
- Sulfasalazine.
What side effects are characteristic of penicillamine?
Side effects of prolonged penicillamine use:
- Nephrotoxicity — nephritis.
- Hematotoxicity — aplastic anemia.
For what pathologies is the use of penicillamine indicated?
Penicillamine is used for:
- Rheumatoid arthritis.
- Wilson's disease.
- Heavy metal poisoning — as an antidote.
- Cystinuria.
What drug classes belong to targeted therapy for rheumatoid arthritis?
Drug classes of targeted therapy for rheumatoid arthritis include:
- Tumor necrosis factor (TNF-alpha) inhibitors.
- Interleukin-1 (IL-1) receptor antagonists.
- Janus kinase (JAK) inhibitors.
- Interleukin-6 (IL-6) inhibitors.
What are the contraindications for prescribing azathioprine?
Contraindications for prescribing azathioprine:
- Pregnancy.
- Lactation period.
To memorize the triad of combination therapy for rheumatoid arthritis, use the «D-NSAID-G» rule: Disease-modifying antirheumatic drug + NSAID + Glucocorticoids (in low doses).
Class and exam questions
How quickly does the effect of sulfasalazine appear?
The drug belongs to slow-acting agents. Its therapeutic effect is delayed in time and only begins to manifest clinically after 1–3 months of regular intake.
Why is a regular ophthalmological examination mandatory during chloroquine treatment?
Chloroquine has pronounced ophthalmotoxicity. It can accumulate in ocular tissues, causing dangerous complications: retinopathy, corneal opacity, and decreased visual acuity.
What is the specific mechanism of action of azathioprine?
Azathioprine is a prodrug. In the liver, it is converted into an active metabolite (6-mercaptopurine), which blocks nucleic acid synthesis and halts cell division.
Can azathioprine be prescribed to pregnant patients?
No, this drug is strictly contraindicated during pregnancy, as well as during breastfeeding.
What else to study on this topic
- Mechanism of action and pharmacokinetics of gold preparations (auranofin).
- Specifics of targeted therapy use: TNF-alpha inhibitors (etanercept, infliximab) and IL-1 receptor antagonists (anakinra).
- The role of cytostatics methotrexate and leflunomide in treatment regimens for autoimmune diseases.
- Use of penicillamine as an antidote in heavy metal poisoning and in the therapy of cystinuria.
Master the entire topic in the «Pharmacology» course
This is a summary. The course covers everything tested in classes and exams.
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