To review the toxicity issues of commonly used antirheumatic drugs in pregnancy and lactation.A review of the medical literature using Medline database via Ovid was performed to identify the toxicities of antirheumatic drugs in pregnancy and lactation.Many rheumatologic diseases in women often first present during the childbearing years. In most cases, antirheumatic therapy is required for their disease control. Glucocorticoids may be used during pregnancy; however, first-trimester use should be avoided if possible and breastfeeding should occur 4 hours after the last dosing. Nonsteroidal antiinflammatory drugs (NSAIDs) and cyclooxygenase-2 (COX-2) inhibitors should be discontinued 6 to 8 weeks before delivery. NSAIDs are compatible with lactation, although there is potential risk of jaundice and kernicterus. There is insufficient data on COX-2 inhibitors and lactation. Hydroxychloroquine and sulfasalazine may be continued throughout pregnancy and lactation. Methotrexate and leflunomide are contraindicated during pregnancy and lactation. Cyclophosphamide and mycophenolate mofetil should be avoided during pregnancy and lactation. Azathioprine and cyclosporine A could be used with caution during pregnancy if felt there is a need to suppress disease activity. They are not compatible with breastfeeding. There are insufficient data regarding tumor necrosis factor-antagonists, anakinra, and rituximab in relation to pregnancy and lactation. Male patients should be made aware of the effects methotrexate, leflunomide, sulfasalazine, and cyclophosphamide may have on their fertility.Health care providers should discuss the risks and benefits of antirheumatic therapy during conception, pregnancy, and lactation with their patients. Better maternal and fetal outcomes can be expected if the pregnancy is planned, the rheumatic disease is stable, and if appropriate medication adjustments can be made ahead of time.