pharma sgl 1

• Drugs used to induce remission in IBD


  • Rectal and oral 5-aminosalicylates (5-ASAs)
  • Corticosteroids (rectal, oral locally delivered and systemic)
  • Biologic agents (TNF-α inhibitors, α-4 integrin inhibitors, and the IL-12/23 inhibitor ustekinumab)
• Drugs used to maintain remission in IBD


  • Immunomodulators (azathioprine, 6-mercaptopurine, and methotrexate)
• Sulfasalazine


  Prodrug consisting of 5-ASA linked to sulfapyridine
• Mesalamine


  Single 5-ASA molecules enclosed within an enteric coat or a semipermeable membrane
• 1. ASA pharmacokinetics


  • Variable and dependent on route of administration, type of oral formulation, and disease activity
  • Absorption increases with more severe disease and decreases with decreasing pH
• Adverse effects of 5-ASAs

  Mainly due to sulfapyridine (sulfonamide) → drug allergy, bone marrow depression and megaloblastic anemia
• Corticosteroids


  Used in IBD for their anti-inflammatory effects, but long-term maintenance should be avoided due to deleterious effects of chronic use
• Biologic agents


  • Associated with increased risk for infection, patients should be evaluated for tuberculosis and treated for latent TB prior to use
• TNF-α inhibitors


  • Infliximab
  • Adalimumab
  • Certolizumab
  • Golimumab
• α-4 integrin inhibitors


  Reduce lymphocyte migration into the intestinal mucosa and inflammation, used for disease refractory to TNF-α inhibitors
• IL-12/23 inhibitor


  Ustekinumab, inhibits the cytokines IL-12 and IL-23 involved in lymphocyte activation
• Methotrexate


  Structural analogue of folic acid that inhibits the production of folinic acid, mechanism of action in CD unknown
• Thiopurines


  Azathioprine and 6-mercaptopurine, oral medications with concerns of toxicity including bone marrow suppression and hepatotoxicity
• Treatments for IBS


  • Reassurance, increased fluid and fiber intake, antimotility drugs( codeine phosphate(sedation) and loperimide), low-dose tricyclic antidepressants, antispasmodics
• Antimuscarinic drugs


  Block cholinergic transmission and cause smooth muscle relaxation, contraindicated in glaucoma and prostatism, should be avoided in gastro-oesophageal reflux (dicyclomine and propanthilin)
• Direct smooth muscle relaxants


  Mebeverine( used for colonic hypermotility), alverine, peppermint oil, do not have antimuscarinic effects
• Antibiotics


  Neomycin and rifaximin(ideal antibiotic) can be used to treat IBS, as they are nonabsorbable and have limited side effects
• Vedolizumab exhibits specific binding to α-4/β-7 integrin and is indicated for refractory UC and CD.