| Medication | Dosing | Mechanism of Action | Comments |
|---|
| 5-ASA | | | Not consistently effective for CD |
| Sulfasalazine | 0.5 g bid-1.5 g qid | Metabolized to 5-ASA and a sulfapyridine moiety | Significant side effects from sulfapyridine moiety; especially effective for IBD arthropathy |
| Mesalamine | Varies by brand | Active component of sulfasalazine | Also available in suppository or enema for distal UC
Rarely can cause paradoxical worsening of colitis |
| Asacola | 800–1600 mg PO tid | Released at a pH of 7 in the distal ileum | |
| Pentasaa | 0.5–1.0 g PO qid | Time- and pH-dependent release mechanism distributes in the small bowel and colon | |
| Aprisoa | 1.5 g PO qday | pH-dependent release distributes throughout the colon | |
| Lialdaa (multimatrix delivery system) | 1.2–2.4 g PO qday–bid | Sustained release throughout the colon despite decreased frequency of administration | |
| Balsalazide (Colazal) | 1.5 g bid–2.25 tid | Bacterial cleavage to mesalamine by colonic bacteria | |
| Olsalazine (Dipentum) | 500 mg bid | 5-ASA dimer cleaved by colonic bacteria | |
| Antibiotics | | | Used to treat fistulizing CD and abscesses |
| Metronidazole | 250–500 mg PO tid | | Risk of neuropathy |
| Ciprofloxacin | 500 mg PO bid | | Risk of tendon rupture |
| Corticosteroids | | Multiple immunosuppressing effects | Should NOT be used as maintenance therapy. Topical therapy can be used for distal disease |
| Methylprednisolone | 60 mg IV qday | | |
| Prednisone | 40–60 mg qday | | |
| Budesonide | 9 mg qday | pH-controlled release delivers drug to ileum and ascending colon (Entocortb)
Multimatrix system preferentially acts on colon (Ucerisb)
Topical formulations can be used for distal disease | May reduce side effects due to first-pass metabolism |
| Immunomodulators |
| 6-Mercaptopurine | 1.0–1.5 mg/kg/d PO | Purine analog, causes preferential suppression of T-cell activation and antigen recognition | Checking thiopurine methyltransferase (TPMT) enzyme activity prior to starting therapy identifies patients at risk for dangerous cytopenias
6-Thioguanine (6-TG) metabolite levels assess adequacy of dosing; high 6-methyl mercaptopurine (6-MMP) levels predict hepatotoxicity |
| Azathioprine | 1.5–2.5 mg/kg/d PO | S-imidazole precursor of 6-MP | Risk of hepatosplenic T-cell lymphoma with thiopurines, especially in young men |
| Methotrexate | 15–25 mg IM or PO weekly | Inhibits DNA synthesis | May cause nausea/vomiting, hepatotoxicity |
| Biologics |
| Infliximab (Remicade) | 5 mg/kg IV infusions at weeks 0, 2, and 6, followed by maintenance infusions every 4–8 weeks | Monoclonal antibody against tumor necrosis factor-alpha (anti–TNF-α) | Risk of opportunistic infections, reactivation of TB and HBV with all anti–TNF-α agents |
| Adalimumab (Humira) | 160 mg SC at week 0, then 80 mg SC at week 2, followed by 40 mg SC every 1–2 weeks | Anti–TNF-α | |
| Certolizumab pegol (Cimzia) | 400 mg SC at weeks 0, 2, and 4, followed by maintenance doses every 4 weeks | Anti–TNF-α | |
| Golimumab (Simponi) | 200 mg SC at week 0, then 100 mg SC at week 2 and every 4 weeks thereafter | Anti–TNF-α | Only approved for UC |
| Vedolizumab (Entyvio) | 300-mg infusions at weeks 0 and 2, followed by infusions every 4–8 weeks | Monoclonal antibody against α4β7 integrin, prevents T cell migration to inflammation. α4β7 is specific to GI tract | Good safety profile because of gut specificity |
| Natalizumab (Tysabri) | 300-mg infusions at weeks 0, 4, and 8, followed by monthly infusions thereafter | Monoclonal antibody to α-4 integrin. In contrast to α4β7, α-4 is found in and outside the GI tract | Risk of JC polyomavirus reactivation causing progressive multifocal leukoencephalopathy has limited its use |
| Ustekinumab (Stelara) | Weight-dependent dosing of 260–520-mg infusion at week 1, followed by 90-mg subcutaneous maintenance injections every 8 weeks | Monoclonal antibody to the p40 subunit of interleukin-12 and interleukin-23 | Good safety profile. Also approved for psoriasis, so good option for IBD patients with psoriasis or psoriaform reactions to anti–TNF-α |
| Tofacitinib (Xeljanz) | 5 mg or 10 mg oral twice a day | Janus kinase inhibitor | Risk of thromboembolic events; use with caution in patients with CV risk factors |