MedChem Final (small molecule DMARDs)

What is the class of methotrexate?

Antimetabolite

What is the mechanism of methotrexate?

inhibits dihydrofolate reductase, leading to decreased nucleotide synthesis, which in turn impairs cellular proliferation and modulates immune response.

What are the ADR of methotrexate?

Bone marrow suppression, GI toxicity, hepatotoxicity, teratogenic, alopecia

What is the class of azathioprine?

Purine antimetabolite

What is the mechanism of azathioprine?

It is converted to 6-MP then to 6-TG and then it is incorporated into DNA where it decreases B/T cell proliferation and decreases IL-2

What are some ADRs of azathioprine?

Bone marrow suppression, infections, carcinogenicity, GI/liver toxicity, alopecia

What is the class of hydroxychloroquine/chloroquine?

Antimalarial

What is the mechanism of hydroxychloroquine/chloroquine?

decreases T-cell response, chemotaxis, lysosomal stabilization, IFN interference

What are some ADRs of hydroxychloroquine/chloroquine?

Retinopathy, GI upset, cardiomyopathy

What is the class of Leflunomide?

Pyrimidine synthesis inhibitor

What is the mechanism of Leflunomide?

Inhibits dihydroorotate dehydrogenase, reducing pyrimidine synthesis, leading to decreased lymphocyte proliferation.

What are some ADRs of Leflunomide?

Hepatotoxicity

What is the class of cyclophosphamide?

Cytotoxic alkylating agent

What is the mechanism of cyclophosphamide?

Cross links DNA which leads to cell death

What are some ADRs of cyclophosphamide?

Bone marrow suppression, mucosal toxicity, teratogenic

What is the class of Cyclosporine/Tacrolimus?

Calcineurin inhibitors

What is the mechanism of Cyclosporine/Tacrolimus?

Inhibits T-cell activation by blocking IL-2 production, leading to immunosuppression.

What are some ADRs of Cyclosporine/Tacrolimus?

Nephrotoxicity, HTN, tremors, hirsutism, CYP3A DDIs

What class are Tofcitinib, Bancitinib and Updacitinib?

JAK inhibitors

What is the mechanism of Tofcitinib, Bancitinib and Updacitinib?

Inhibits Janus kinase enzymes, which leads to decreased cytokine signaling and immunomodulation.

What are some ADRs of Tofcitinib, Bancitinib and Updacitinib?

Infections, malignancy, CV events, cytopenias