Twenty nonsteroidal immunosuppressive agents are reviewed and classified into the following medication categories: anti-tumor necrosis factor-α agents, calcineurin inhibitors, antilymphocyte antibodies, IL-2 receptor antagonists, cytotoxic agents, mammalian target of rapamycin inhibitors, and others (hydroxychloroquine, chloroquine, imatinib). For each individual medication, the toxicity profile, monitoring profile, pregnancy classification, and unique recommendations are summarized in text subsections. Specific considerations for clinicians regarding assessing the risks for TB and hepatitis; monitoring blood work, drug clearance, and drug-drug interactions; and providing prophylaxis against infections are also included. Finally, a summary of monitoring for each agent is found in an easy-to-read table. Other tables include summaries of adverse reactions by specific agents, infection prophylaxis considerations for intense immunosuppression, and a summary of drug-drug interactions. Given that these medications have significant potential to cause harm, it is hoped that providing clinicians with this concise, yet comprehensive review of medication monitoring will improve the benefit/risk ratio for the patients receiving them.