Disease-modifying anti-rheumatic drugs

Disease-modifying anti-rheumatic drugs – There is currently a trend toward earlier use of the disease-modifying drugs, especially methotrexate.

Gold – Retards or prevents progression of bone and articular erosion in some patients. Gold salts are highly protein bound. Renal tubular epithelial cells have a very high affinity for gold. Gold cannot be given with penicillamine, since penicillamine will chelate and remove the gold. The most common side effects are stomatitis, rash, and proteinuria. Gold treatments must be stopped with development of nephrosis, thrombocytopenia, leukopenia, or exfoliative dermatitis.

Penicillamine – Sulfur-containing AA analog useful as a heavy metal chelator (Wilson’s disease). Penicillamine can retard progression of bone and articular destruction, but usefulness is limited by serious toxicity. Most deaths are due to aplastic anemia. Teratogenic.

Methotrexate – Approved for treatment of RA. Immunosuppressant/antimetabolite (folate antagonist).Side effects include hepatic fibrosis, pneumonitis, bone marrow depression, GI ulceration and bleeding. Aspirin and NSAIDs may increase toxicity by slowing excretion.

COX-2 Inhibitor

Celecoxib – Less effective as an analgesic; adverse effects include abdominal pain, diarrhea, dyspepsia, renal toxicity, and GI toxicity; celcoxib inhibits p450 CYP2D6, thereby increasing concentration of -blockers, antidepressants, and antipsychotics.

Category: Pharmacology Notes