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IBD Drugs
| Generic | Brand | Route | Drug Class | Indication | Mechanism of Action | Adverse Effects |
|---|---|---|---|---|---|---|
| Mesalamine (5-ASA) PO | Pentasa/Apriso/Asacol/Delzicol/Lialda | PO | Aminosalicylate | Ulcerative Colitis | Activates PPAR-γ and nuclear transcription factor to decrease proinflmmatory cytokines (eg. IL-1/TNF-α) | Bone marrow suppression, skin rashes, headaches |
| Mesalamine (5-ASA) Suppository | Canasa | Suppository | Aminosalicylate | Ulcerative Colitis | Activates PPAR-γ and nuclear transcription factor to decrease proinflmmatory cytokines (eg. IL-1/TNF-α) | Bone marrow suppression, skin rashes, headaches |
| Mesalamine (5-ASA) Enema | Rowasa | Enema | Aminosalicylate | Ulcerative Colitis | Activates PPAR-γ and nuclear transcription factor to decrease proinflmmatory cytokines (eg. IL-1/TNF-α) | Bone marrow suppression, skin rashes, headaches |
| Sulfasalazine | Azulfidine | PO | Aminosalicylate | Ulcerative Colitis | Activates PPAR-γ and nuclear transcription factor to decrease proinflmmatory cytokines (eg. IL-1/TNF-α) | Bone marrow suppression, skin rashes, headaches |
| Prednisone | Deltasone/Rayos | PO | Corticosteroid | IBD (UC, CD) | Activates glucocorticoid receptors/nuclear receptors; inhibits pro-inflammatory (interleukins/ cytokines; TNF-a) and expression of adhesion molecules (NF-κB) | Hypertension, insomnia, peptic ulcer, pituitary/adrenal suppression (ACTH inhibition) |
| Budesonide | Entocort EC/Uceris | PO | Corticosteroid | IBD (UC, CD) | Activates glucocorticoid receptors/nuclear receptors; inhibits pro-inflammatory (interleukins/ cytokines; TNF-a) and expression of adhesion molecules (NF-κB) | Hypertension, insomnia, peptic ulcer, pituitary/adrenal suppression (ACTH inhibition) |
| Azathioprine | Imuran | PO | Thiopurine (Immunosuppressive) | IBD (UC, CD) | Suppresses T-cell proliferation and DNA/RNA replication through inhibiting de novo purine synthesis | Bone marrow suppression, infections, pancreatitis, hepatitis, lymphoma risk |
| Mercaptopurine | Purinethol | PO | Thiopurine (Immunosuppressive) | IBD (UC, CD) | Suppresses T-cell proliferation and DNA/RNA replication through inhibiting de novo purine synthesis | Bone marrow suppression, infections, pancreatitis, hepatitis, lymphoma risk |
| Methotrexate | Trexall | IM/SQ | Antimetabolite (Immunosuppressive) | Crohn's Disease | competitively and reversibly inhibits dihydrofolate reductase and B-cell proliferation; ↓ thymidine and purine production to block DNA/RNA synthesis; stimulates adenosine release | Bone marrow suppression, hepatotoxicity, alopecia, infections, malignancies, stomatitis; BW: Teratogenicity |
| Cyclosporine | Neoral | PO | Caclineurin Inhibitor (Immunosupressive) | Ulcerative Colitis | binds to cyclophilin, forming a complex that inhibits calcineurin ∴ prevents activation of NFAT leading to decreased transcription of IL-2 (primarily), IL-3, and IFN-γ in T cells | Nephrotoxicity, electrolyte imbalances, neurotoxicity, hepatotoxicity, hypertension, hyperglycemia, hyperkalemia, altered mental status |
| Infliximab | Remicade | IV | TNF-α Inhibitor | IBD (UC, CD) | Prevents TNF-α stimulation of TNFR on immune cells (macrophages/T-helper cells) ∴ decrease release of proinflammatory cytokines, T-cell proliferation, and endothelial adhesion molecules | Infusion reactions, antibodies to the antibodies BW: Infections, malignancy (lymphoma), TB risk |
| Adalimumab | Humira | SQ | TNF-α Inhibitor | IBD (UC, CD) | Prevents TNF-α stimulation of TNFR on immune cells (macrophages/T-helper cells) ∴ decrease release of proinflammatory cytokines, T-cell proliferation, and endothelial adhesion molecules | Antibodies to the antibodies BW: Infections, malignancy (lymphoma), TB risk |
| Certolizumab | Cimzia | SQ | TNF-α Inhibitor | Crohn's Disease | Prevents TNF-α stimulation of TNFR on immune cells (macrophages/T-helper cells) ∴ decrease release of proinflammatory cytokines, T-cell proliferation, and endothelial adhesion molecules | Antibodies to the antibodies BW: Infections, malignancy (lymphoma), TB risk |
| Golilumab | Simponi | SQ | TNF-α Inhibitor | Ulcerative Colitis | Prevents TNF-α stimulation of TNFR on immune cells (macrophages/T-helper cells) ∴ decrease release of proinflammatory cytokines, T-cell proliferation, and endothelial adhesion molecules | Antibodies to the antibodies BW: Infections, malignancy (lymphoma), TB risk |
| Vedolizumab | Entyvio | IV | Integrin receptor antagonist | IBD (UC, CD) | Inhibits lymphocyte migration to inflamed endothelial tissue via blocking integrin adhesion molecules | Hepatotoxicity, progressive multifocal leukoencephalopathy (PML) risk, hypersensitivy reaction, infections, rash, headache, arthralgias, nasopharyngitis, antibody development |
| Ustekinumab | Stelara | IV/SQ | IL-12 + IL-23 Inhibitor | IBD (UC, CD) | Inhibits specific interleukins ∴ ↓ activation of NK cells & TH1 cells; ↓ TNF-α expression and T-cell differentiation & maturation | Infections, nasopharyngitis, TB, malignancy, neutralizing antibodies risk |
| Guselkumab | Tremfya | IV/SQ | IL-23 Inhibitor | IBD (UC, CD) | Inhibits specific interleukins ∴ ↓ activation of NK cells & TH1 cells; ↓ TNF-α expression and T-cell differentiation & maturation | Infections, nasopharyngitis, TB, malignancy, neutralizing antibodies risk |
| Risankizumab | Skyrizi | IV/SQ | IL-23 Inhibitor | IBD (UC, CD) | Inhibits specific interleukins ∴ ↓ activation of NK cells & TH1 cells; ↓ TNF-α expression and T-cell differentiation & maturation | Infections, nasopharyngitis, TB, malignancy, neutralizing antibodies risk |
| Mirkizumab | Omvoh | IV/SQ | IL-23 Inhibitor | IBD (UC, CD) | Inhibits specific interleukins ∴ ↓ activation of NK cells & TH1 cells; ↓ TNF-α expression and T-cell differentiation & maturation | Infections, nasopharyngitis, TB, malignancy, neutralizing antibodies risk |
| Ozanimod | Zeposia | PO | Sphingosine 1-Phosphate (S1P) Receptor Modulator | Ulcerative Colitis | Down regulates S1P₁ receptors on lymphocytes, blocking lymphocyte egress from lymph nodes and reducing immune cell migration to inflamed tissues | Hepatotoxicity, dyspnea, infections, macular edema/vision changes, PML, PRES, bradycardia/AV block, orthostatic hypotension, hypertension, skin malignancies, lymphocytopenia |
| Etrasimod | Velspity | PO | Sphingosine 1-Phosphate (S1P) Receptor Modulator | Ulcerative Colitis | Down regulates S1P₁ receptors on lymphocytes, blocking lymphocyte egress from lymph nodes and reducing immune cell migration to inflamed tissues | Hepatotoxicity, dyspnea, infections, macular edema/vision changes, PML, PRES, bradycardia/AV block, orthostatic hypotension, hypertension, skin malignancies, lymphocytopenia |
| Tofacitinib | Xeljanz | PO | Janus Kinase (JAK) Enzyme Inhibitor | Crohn's Disease | Selective JAK inhibitors that prevent further downstream effects to phosphorylate the STAT molecule ∴ no phosphorylated STAT (transcription factor); ↓ proinflammatory cytokines | ↑Cholesterol; infections, nasopharyngitis, malignancy, CV events, thrombosis, treatment-related mortality |
| Upadacitinib | Rinvoq | PO | Janus Kinase (JAK) Enzyme Inhibitor | IBD (UC, CD) | Selective JAK inhibitors that prevent further downstream effects to phosphorylate the STAT molecule ∴ no phosphorylated STAT (transcription factor); ↓ proinflammatory cytokines | ↑Cholesterol; infections, nasopharyngitis, malignancy, CV events, thrombosis, treatment-related mortality |
| Metronidazole | Flagyl | PO/IV | Anaerobic Antibiotic | IBD (UC, CD) | bactericidal activity of anaerobic bacteria | Neurotoxicity; metallic tase; Abx resistance; disulfiram-reactions; peripheral neuropathy; stomatitis |
| Ciprofloxacin | Cipro | PO/IV | Fluoroquinolone Antibiotic | IBD (UC, CD) | inhibits DNA gyrase and topoisomerase | CV, CNS,Liver toxicity; poor glucose regulation; QTc prolongation BW: tendon rupture; myasthenia gravis |