IBD Overview and Medications
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Questions and Answers

What is the primary mechanism of action of thiopurines?

  • Inhibition of cytokine production
  • Inhibition of purine nucleotide metabolism (correct)
  • Enhancement of DNA synthesis
  • Stimulation of T cell function

    • What side effect is NOT commonly associated with glucocorticoids?

  • Insomnia
  • Increased intraocular pressure
  • Nausea and vomiting (correct)
  • Osteoporosis

    • Which thiopurine metabolite is an active nucleotide involved in the drug's action?

  • 6-TGN (correct)
  • 6-TU
  • Azathioprine
  • 6-MMP

    • When should 6-mercaptopurine be taken?

    <p>On an empty stomach</p> Signup and view all the answers

    What dietary adjustments should patients taking glucocorticoids consider?

    <p>High protein and potassium-rich</p> Signup and view all the answers

    Which of the following is a boxed warning for thiopurines?

    <p>Lymphoma</p> Signup and view all the answers

    What is the mechanism of action of low-dose thiopurines?

    <p>Inhibits AICAR</p> Signup and view all the answers

    Which anti-TNF-alpha agent is coded as a chimeric monoclonal antibody?

    <p>Infliximab</p> Signup and view all the answers

    How should the dose of 6-TGN be adjusted for poor metabolizers?

    <p>Decreased due to risk of suppression</p> Signup and view all the answers

    Which of the following side effects is associated with anti-TNF-alpha agents?

    <p>Increased infections</p> Signup and view all the answers

    Which medication must be monitored for potential interactions with thiopurines?

    <p>Allopurinol</p> Signup and view all the answers

    What is one of the serious side effects of thiopurines?

    <p>Hepatotoxicity</p> Signup and view all the answers

    Why are infliximab and adalimumab more potent than certolizumab?

    <p>They contain an Fc portion that activates the complement pathway.</p> Signup and view all the answers

    Which drug can cause adverse effects related to immunosuppression?

    <p>Both A and C</p> Signup and view all the answers

    What is a common adverse reaction of thiopurines?

    <p>Myelosuppression</p> Signup and view all the answers

    What is the recommended management to prevent renal toxicity during thiopurine therapy?

    <p>Maintain hydration and make urine basic</p> Signup and view all the answers

    Which of the following is not an indication for thiopurines?

    <p>Hypertension</p> Signup and view all the answers

    Which classification of drugs is certolizumab categorized under?

    <p>Anti-TNF-alpha agent</p> Signup and view all the answers

    Which adverse reaction is specifically noted for higher doses of thiopurines?

    <p>Crystalluria</p> Signup and view all the answers

    What is the significance of monitoring liver function tests (LFTs) during thiopurine therapy?

    <p>To monitor for hepatotoxicity</p> Signup and view all the answers

    What type of immunity is primarily activated in ulcerative colitis?

    <p>Humoral mediated immunity</p> Signup and view all the answers

    Which of the following drugs is classified as an aminosalicylate used to treat IBD?

    <p>Mesalamine</p> Signup and view all the answers

    What is the mechanism of action of sulfasalazine in treating IBD?

    <p>Inhibits synthesis of prostaglandins</p> Signup and view all the answers

    Which adverse drug reaction is most commonly associated with sulfasalazine?

    <p>Bone marrow suppression</p> Signup and view all the answers

    Which inflammatory bowel disease can affect any part of the gastrointestinal tract?

    <p>Crohn’s disease</p> Signup and view all the answers

    What is a major side effect of glucocorticoids used in IBD treatment?

    <p>Adrenal suppression</p> Signup and view all the answers

    Which drug class includes azathioprine and 6-mercaptopurine?

    <p>Thiopurines</p> Signup and view all the answers

    What is the active compound of sulfasalazine responsible for its therapeutic effects?

    <p>Mesalamine</p> Signup and view all the answers

    Which janus kinase inhibitor is used in the treatment of IBD?

    <p>Tofacitinib</p> Signup and view all the answers

    Which drug is a glucocorticoid commonly used to treat IBD?

    <p>Budesonide</p> Signup and view all the answers

    What is the primary therapeutic effect of natalizumab?

    <p>Inhibits migration of memory T cells</p> Signup and view all the answers

    Which adverse effect is common to both natalizumab and vedolizumab?

    <p>Brain infection (PML)</p> Signup and view all the answers

    How does tofacitinib exert its therapeutic effects in treating IBD?

    <p>Through inhibition of janus kinase</p> Signup and view all the answers

    What is a side effect associated with vedolizumab?

    <p>Nasopharyngitis</p> Signup and view all the answers

    What is the mechanism of action of integrin receptor antagonists like natalizumab?

    <p>Inhibits interaction with adhesion molecules</p> Signup and view all the answers

    In the case of an allergic reaction during natalizumab treatment, what immediate action should be taken?

    <p>Stop taking the medication</p> Signup and view all the answers

    Which of the following drugs is primarily used for rheumatoid arthritis but also shows benefits in IBD?

    <p>Tofacitinib</p> Signup and view all the answers

    What is a common management step for infusion reactions when using natalizumab?

    <p>Use Tylenol or Benadryl</p> Signup and view all the answers

    Which of these is NOT a side effect of tofacitinib?

    <p>Nausea and vomiting</p> Signup and view all the answers

    If there is no therapeutic benefit from natalizumab treatment after 12 weeks, what should be done?

    <p>Discontinue treatment</p> Signup and view all the answers

    Match the following brand names with their generic equivalents:

    <p>Asacol HD = Mesalamine Azulfidine = Sulfasalazine Lialda = Mesalamine Pentasa = Mesalamine</p> Signup and view all the answers

    Match the following generic names with their categories:

    <p>Mesalamine = Aminosalicylate Sulfasalazine = Aminosalicylate Olsalazine = Aminosalicylate Balsalazide = Aminosalicylate</p> Signup and view all the answers

    Match the following mechanisms of action with their corresponding drug:

    <p>Inhibits leukotriene production = Sulfasalazine Acts topically on colonic mucosa = Mesalamine Prodrug that breaks down into sulfapyridine = Sulfasalazine Exerts anti-inflammatory effects in the GI tract = Mesalamine</p> Signup and view all the answers

    Match the common side effects with their occurrence:

    <p>Nausea = Common Blood dyscrasias = Less common but serious Diarrhea = Common Hepatic dysfunction = Less common but serious</p> Signup and view all the answers

    Match the therapeutic uses with their respective conditions:

    <p>Ulcerative colitis = Treatment of inflammatory bowel diseases Crohn's disease = Limited efficacy Maintenance of remission = Ulcerative colitis Induction of remission = Exacerbations of ulcerative colitis</p> Signup and view all the answers

    Match the side effects to the appropriate classification:

    <p>Headache = Common Skin rashes = Less common but serious Abdominal pain = Common Pneumonitis = Less common but serious</p> Signup and view all the answers

    Match the following drugs to their side effects:

    <p>Sulfasalazine = Hypersensitivity reactions Mesalamine = Fatigue Azulfidine = Headache Pentasa = Diarrhea</p> Signup and view all the answers

    Match the generic names with their potential off-label uses:

    <p>Mesalamine = Other inflammatory conditions Sulfasalazine = Adjunctive therapy in intestinal diseases Balsalazide = Not specifically indicated Olsalazine = Adjunctive therapy in intestinal diseases</p> Signup and view all the answers

    Match the following brand names with their generic equivalents:

    <p>Asacol = Mesalamine Pentasa = Olsalazine Lialda = Balsalazide Rowasa = Sulfasalazine</p> Signup and view all the answers

    Match the following generic names with their primary function:

    <p>Mesalamine = Anti-inflammatory for IBD Sulfasalazine = Combination of sulfapyridine and 5-ASA Olsalazine = Prodrug converting to mesalamine Balsalazide = Prodrug releasing mesalamine</p> Signup and view all the answers

    Match the following brand names with their administration forms:

    <p>Asacol = Oral tablets Canasa = Suppositories Rowasa = Enemas Pentasa = Oral tablets</p> Signup and view all the answers

    Match the following generic names with their brand counterparts:

    <p>Mesalamine = Lialda Sulfasalazine = Apriso Balsalazide = Colazal Olsalazine = Dipentum</p> Signup and view all the answers

    Match the following brands with their formulations:

    <p>Pentasa = Oral and rectal formulations Canasa = Suppositories Rowasa = Enemas Asacol = Oral tablets</p> Signup and view all the answers

    What are the primary uses of aminosalicylates?

    <p>Managing inflammatory bowel diseases</p> Signup and view all the answers

    Which metabolite of mesalamine is known for its anti-inflammatory effects?

    <p>Acetyl-mesalamine</p> Signup and view all the answers

    What is a common side effect associated with sulfasalazine?

    <p>Hypersensitivity reactions</p> Signup and view all the answers

    Where is mesalamine primarily absorbed in the body?

    <p>Small intestine</p> Signup and view all the answers

    What is a significant consideration for patients taking aminosalicylates?

    <p>Regular monitoring of renal function</p> Signup and view all the answers

    Match the following mechanisms of action with their corresponding effects of glucocorticoids:

    <p>Inhibiting cytokines = Reduces inflammation Suppressing immune cells = Decreases edema Activating anti-inflammatory pathways = Prevents fluid retention Reducing blood vessel permeability = Minimizes immune response</p> Signup and view all the answers

    Match the following side effects of glucocorticoids with their description:

    <p>Cushing's syndrome = Facial swelling and hypertension Osteoporosis = Increased risk of bone fractures Mood changes = Anxiety or depression symptoms Weight gain = Fluid retention and increased appetite</p> Signup and view all the answers

    Match the following classes of drugs with their characteristics in comparison to glucocorticoids:

    <p>Immunosuppressants = Long-term management, slower acting Biologics = Target specific inflammation pathways 5-ASA compounds = Favorable safety profile Glucocorticoids = Short-term management due to side effects</p> Signup and view all the answers

    Match the following long-term management strategies with their descriptions:

    <p>Regular monitoring = Adjust treatment based on disease activity Lifestyle modifications = Support nutritional and exercise needs Transition therapy = Switch to biologics after flare-ups Education = Teach recognition of flare-up symptoms</p> Signup and view all the answers

    Match the common short-term side effects of glucocorticoids to their potential impact:

    <p>Increased appetite = Can lead to weight gain Fluid retention = May cause swelling in the body Mood changes = Affects emotional well-being Insomnia = Disrupts sleep patterns</p> Signup and view all the answers

    Match the following glucocorticoid effects with their specific outcomes:

    <p>Reduced permeability of blood vessels = Decreases edema Inhibition of pro-inflammatory cytokines = Lowers inflammation Suppressed lymphocyte activity = Diminished immune response Activated anti-inflammatory pathways = Promotes healing</p> Signup and view all the answers

    Match the following long-term treatment options with their benefits:

    <p>Immunosuppressants = Lower incidence of short-term side effects Biologics = Effective for moderate to severe cases 5-ASA compounds = Good safety profile in long-term use Glucocorticoids = Effective for acute flare-ups</p> Signup and view all the answers

    Match the common risks associated with long-term use of glucocorticoids:

    <p>Cataracts = Visual impairment over time Increased risk of infections = Due to immune suppression Osteoporosis = Brittle bones and increased fracture risk Cushing's syndrome = Metabolic and physical changes</p> Signup and view all the answers

    Match the following side effects of glucocorticoids with their long-term implications:

    <p>Osteoporosis = Fractures Cataracts = Vision loss Cushing's syndrome = Chronic health issues Increased infection risk = Risk of severe illnesses</p> Signup and view all the answers

    Match the following treatment strategies with their goals:

    <p>Transition to maintenance therapy = Use immunosuppressants after flare-ups Lifestyle modifications = Encourage healthy living Patient education = Promote adherence to therapy Regular monitoring = Adapt treatment as needed</p> Signup and view all the answers

    Match the following glucocorticoids with their brand names:

    <p>Prednisone = Deltasone Budesonide = Entocort Hydrocortisone = Cortef Methylprednisolone = Medrol</p> Signup and view all the answers

    Match the following brand names with their generic equivalents:

    <p>Entocort = Budesonide Cortef = Hydrocortisone Medrol = Methylprednisolone Deltasone = Prednisone</p> Signup and view all the answers

    Match the following thiopurines with their primary therapeutic use:

    <p>Azathioprine = Treatment of Crohn's disease 6-Mercaptopurine = Treatment of Ulcerative Colitis 6-Thioguanine = Short-term remission of IBD 6-TGN = Not used for therapeutic purposes</p> Signup and view all the answers

    Match the following generic glucocorticoids with their dosage forms:

    <p>Prednisone = Oral tablet Budesonide = Capsule Hydrocortisone = Topical cream Methylprednisolone = Injection</p> Signup and view all the answers

    Match the following glucocorticoids with their indication in IBD:

    <p>Prednisone = Moderate to severe flare-ups Budesonide = Mild to moderate IBD Hydrocortisone = Acute exacerbation Methylprednisolone = Severe cases requiring hospitalization</p> Signup and view all the answers

    Match the following thiopurine medications with their brand names:

    <p>Azathioprine = Imuran 6-Mercaptopurine = Purinethol 6-Thioguanine = Tabloid 6-TGN = Not applicable</p> Signup and view all the answers

    Match the following brand names with their thiopurine generic equivalents:

    <p>Imuran = Azathioprine Purinethol = 6-Mercaptopurine Tabloid = 6-Thioguanine Not applicable = 6-TGN</p> Signup and view all the answers

    Match the following glucocorticoid generics with their primary action:

    <p>Prednisone = Anti-inflammatory Budesonide = Localized action in intestines Hydrocortisone = Systemic inflammation reduction Methylprednisolone = Immunosuppressive action</p> Signup and view all the answers

    Match the thiopurines with their commonly known side effects:

    <p>Azathioprine = Myelosuppression 6-Mercaptopurine = Hepatotoxicity 6-Thioguanine = Nausea 6-TGN = Not applicable</p> Signup and view all the answers

    Match the thiopurines with their routes of administration:

    <p>Azathioprine = Oral 6-Mercaptopurine = Oral 6-Thioguanine = Oral 6-TGN = Not applicable</p> Signup and view all the answers

    Which of the following is a brand name for azathioprine?

    <p>Imuran</p> Signup and view all the answers

    What is the generic name for the drug marketed under the brand name Purixan?

    <p>6-mercaptopurine</p> Signup and view all the answers

    Which of the following is NOT a thiopurine used for inflammatory bowel disease?

    <p>Methotrexate</p> Signup and view all the answers

    Which of the following brand names corresponds to thioguanine?

    <p>Tabloid</p> Signup and view all the answers

    Which thiopurine is available as an oral medication for inflammatory bowel disease?

    <p>Azathioprine</p> Signup and view all the answers

    Match the following immunosuppressive drugs with their generic names:

    <p>Methotrexate = Immunosuppressive Cyclosporine = Immunosuppressive Tofacitinib = Janus Kinase Inhibitor Ustekinumab = Interleukin Receptor Antagonist</p> Signup and view all the answers

    Match the following classes of drugs with their examples:

    <p>Anti-TNF alpha = Infliximab Adhesion Molecule Antagonist = Natalizumab Interleukin Receptor Antagonist = Ustekinumab Janus Kinase Inhibitors = Tofacitinib</p> Signup and view all the answers

    Match the following anti-TNF alpha drugs with their characteristics:

    <p>Infliximab = Chimeric monoclonal antibody Adalimumab = Fully human monoclonal antibody Certolizumab pegol = Pegylated antibody fragment Natalizumab = Integrin inhibitor</p> Signup and view all the answers

    Match the following biological therapies to their mechanisms:

    <p>Infliximab = Neutralizes TNF alpha Vedolizumab = Blocks integrin adhesion Adalimumab = Inhibits TNF alpha Ustekinumab = Targets interleukin pathways</p> Signup and view all the answers

    Match the following drug classes used for IBD with their actions:

    <p>Immunosuppressives = Reduce immune response Anti-TNF alpha = Inhibit tumor necrosis factor Adhesion Molecule Antagonist = Prevent white blood cell migration Janus Kinase Inhibitors = Block intracellular signaling pathways</p> Signup and view all the answers

    Match the following immunosuppressive drugs with their descriptions:

    <p>Methotrexate = Used in various autoimmune conditions, including IBD Cyclosporine = Inhibits T-cell activation Tofacitinib = Janus Kinase inhibitor used in IBD Ustekinumab = Interleukin receptor antagonist</p> Signup and view all the answers

    Match the following anti-TNF alpha drugs with their brand names:

    <p>Infliximab = Remicade Adalimumab = Humira Certolizumab pegol = Cimzia Golimumab = Simponi</p> Signup and view all the answers

    Match the following classes of drugs to their corresponding examples:

    <p>Immunosuppressives = Methotrexate Anti-TNF alpha = Adalimumab Adhesion Molecule Antagonist = Vedolizumab Janus Kinase Inhibitors = Tofacitinib</p> Signup and view all the answers

    Match the following drug classes with their therapeutic targets:

    <p>Adhesion Molecule Antagonists = Prevent leukocyte migration Interleukin Receptor Antagonists = Block inflammatory cytokines Janus Kinase Inhibitors = Inhibit intracellular signaling pathways Anti-TNF alpha = Inhibit tumor necrosis factor alpha</p> Signup and view all the answers

    Match the following adhesion molecule antagonists with their brand names:

    <p>Natalizumab = Tysabri Vedolizumab = Entyvio Adalimumab = Humira Infliximab = Remicade</p> Signup and view all the answers

    What is the mechanism of action of sulfasalazine in the treatment of IBD?

    <p>Modulation of immune response and inhibition of inflammatory mediators</p> Signup and view all the answers

    What is a common adverse drug reaction associated with sulfasalazine?

    <p>Gastrointestinal disturbances such as nausea and sore throat</p> Signup and view all the answers

    Which active compound of sulfasalazine is responsible for its therapeutic effects?

    <p>Mesalamine</p> Signup and view all the answers

    What supplementation is commonly needed for patients taking sulfasalazine?

    <p>Vitamin B12</p> Signup and view all the answers

    Which of the following is NOT a side effect associated with sulfasalazine therapy?

    <p>Weight gain</p> Signup and view all the answers

    What is a common adverse drug reaction associated with thiopurines like azathioprine and 6-mercaptopurine?

    <p>Cytopenia</p> Signup and view all the answers

    Which metabolite of thiopurines is crucial for their pharmacological activity?

    <p>6-thioguanine nucleotide (6-TGN)</p> Signup and view all the answers

    How do slow metabolizers typically respond to thiopurine therapy?

    <p>They may experience increased toxicity</p> Signup and view all the answers

    What is a significant drug-drug interaction (DDI) effect that can impact thiopurine metabolism?

    <p>Co-administration with allopurinol</p> Signup and view all the answers

    Which condition is primarily treated with thiopurines such as azathioprine and 6-mercaptopurine?

    <p>Inflammatory bowel disease (IBD)</p> Signup and view all the answers

    What is the primary therapeutic use of methotrexate in the treatment of IBD?

    <p>To induce remission</p> Signup and view all the answers

    Which of the following is a common adverse drug reaction (ADR) associated with methotrexate?

    <p>Liver toxicity</p> Signup and view all the answers

    What is the mechanism of action (MOA) of methotrexate?

    <p>Interference with folate metabolism</p> Signup and view all the answers

    What is the antidote used in cases of methotrexate overdose?

    <p>Leucovorin</p> Signup and view all the answers

    At high doses, methotrexate is primarily associated with which of the following risks?

    <p>Increased risk of infection</p> Signup and view all the answers

    What is the primary mechanism of action of methotrexate in the treatment of IBD?

    <p>Antagonism of folate metabolism</p> Signup and view all the answers

    Which of the following is a common adverse drug reaction (ADR) associated with methotrexate?

    <p>Nausea and vomiting</p> Signup and view all the answers

    What is the primary use of low-dose methotrexate?

    <p>Treatment of rheumatoid arthritis</p> Signup and view all the answers

    What is the antidote for a methotrexate overdose?

    <p>Leucovorin</p> Signup and view all the answers

    At high doses, what serious adverse reaction can methotrexate cause?

    <p>Renal toxicity</p> Signup and view all the answers

    Which anti-TNF α agent is classified as a chimeric monoclonal antibody?

    <p>Infliximab (Remicade)</p> Signup and view all the answers

    Which drug among the anti-TNF α agents is known for its higher potency?

    <p>Infliximab (Remicade)</p> Signup and view all the answers

    What is a common adverse drug reaction (ADR) associated with anti-TNF α agents?

    <p>Increased risk of infections</p> Signup and view all the answers

    Which of the following anti-TNF α agents is pegylated?

    <p>Certolizumab Pegol (Cimzia)</p> Signup and view all the answers

    Which of the following statements is true regarding the mechanism of action (MOA) of anti-TNF α agents?

    <p>They neutralize TNF α activity.</p> Signup and view all the answers

    Which anti-TNF α agent is a chimeric monoclonal antibody?

    <p>Infliximab</p> Signup and view all the answers

    Which anti-TNF α agent has the highest potency in treating inflammatory bowel disease?

    <p>Infliximab</p> Signup and view all the answers

    What common adverse effect is associated with the use of anti-TNF α agents?

    <p>Increased infection risk</p> Signup and view all the answers

    Which of the following best describes Certolizumab Pegol?

    <p>PEGylated Fab fragment</p> Signup and view all the answers

    If a drug is shown to have more potency, what characteristic can contribute to this potency?

    <p>Higher affinity for receptors</p> Signup and view all the answers

    Which drug is classified as an integrin receptor antagonist?

    <p>Natalizumab</p> Signup and view all the answers

    What is the primary drug name for the Janus kinase inhibitor used in IBD treatment?

    <p>Xeljanz</p> Signup and view all the answers

    Which formulation of cyclosporine has better bioavailability?

    <p>Neoral</p> Signup and view all the answers

    Ustekinumab is categorized as an antagonist of which interleukins?

    <p>IL-12/IL-23</p> Signup and view all the answers

    What is the main issue regarding the bioavailability of the oral formulation of cyclosporine?

    <p>Low bioavailability affects efficacy</p> Signup and view all the answers

    Which type of inflammatory bowel disease primarily involves humoral mediated immunity?

    <p>Ulcerative colitis</p> Signup and view all the answers

    Which drug class is NOT considered an anti-inflammatory treatment for IBD?

    <p>Antibiotics</p> Signup and view all the answers

    What is a common adverse reaction associated with the use of sulfasalazine?

    <p>Yellow-orange discoloration of skin/urine</p> Signup and view all the answers

    What type of immunity is primarily activated in Crohn's disease?

    <p>Cell mediated immunity</p> Signup and view all the answers

    Which of the following drugs is an example of a Janus kinase inhibitor used for treating IBD?

    <p>Tofacitinib</p> Signup and view all the answers

    What is the primary mechanism of action of thiopurines?

    <p>Suppress purine nucleotide metabolism and DNA synthesis</p> Signup and view all the answers

    Which side effect is specifically linked to long-term use of glucocorticoids?

    <p>Osteoporosis</p> Signup and view all the answers

    How should the dose of azathioprine be adjusted for patients taking allopurinol for gout?

    <p>Decrease the dose of azathioprine</p> Signup and view all the answers

    Which of the following dietary recommendations is crucial for patients on glucocorticoids?

    <p>High protein and potassium-rich diet</p> Signup and view all the answers

    What must be monitored in patients on thiopurines to prevent serious side effects?

    <p>Complete blood count (CBC) and liver function tests (LFTs)</p> Signup and view all the answers

    Study Notes

    Thiopurine Mechanism of Action

    • Thiopurines like azathioprine and 6-mercaptopurine act by inhibiting purine synthesis, a critical step in DNA and RNA production.
    • This slows down the rate of cell division, particularly in inflammatory cells, helping to reduce inflammation in conditions like Inflammatory Bowel Disease (IBD).
    • 6-thioguanine (6-TGN) is the active metabolite of thiopurines, directly interfering with DNA synthesis.

    Thiopurine Administration & Dosage

    • 6-mercaptopurine should be taken on an empty stomach, ideally at bedtime, for optimal absorption.
    • Dosage adjustments are necessary for poor metabolizers of 6-TGN, requiring lower amounts.

    Thiopurine Side Effects & Monitoring

    • Common side effects of thiopurines include bone marrow suppression leading to decreased white blood cell count, nausea, vomiting, and diarrhea.
    • Serious adverse effects of thiopurines include hepatotoxicity (liver damage) and pancreatitis.
    • Monitoring liver function tests (LFTs) is essential during thiopurine therapy to detect early signs of potential liver complications.
    • Renal toxicity is another concern, so prophylactic measures like hydration and monitoring of renal function are crucial.

    Glucocorticoids in IBD

    • Glucocorticoids like prednisone are often used to manage IBD due to their potent anti-inflammatory properties.
    • A common side effect of glucocorticoids is weight gain, NOT associated with them is hypoglycemia.
    • Patients on glucocorticoids should adjust their diet to control weight gain and maintain blood sugar balance.

    Anti-TNF-alpha Agents in IBD

    • Infliximab, adalimumab, and certolizumab are anti-TNF-alpha agents commonly used in IBD.
    • Infliximab and adalimumab are more potent than certolizumab because they are fully human monoclonal antibodies, while certolizumab is a chimeric antibody.
    • Common adverse effects of anti-TNF-alpha agents include infusion reactions, infections, and reactivation of latent tuberculosis.
    • Anti-TNF-alpha agents are associated with increased risk of lymphoma, a serious side effect.
    • Monitoring for interactions with thiopurines is crucial when using anti-TNF-alpha agents.

    Other IBD Medications

    • Sulfasalazine, an aminosalicylate, is used in treating IBD.
    • It works by inhibiting the synthesis of prostaglandins, inflammatory mediators, and also acts as an antimicrobial agent against specific gut bacteria.
    • The most common side effect associated with sulfasalazine is nausea and vomiting.
    • Mesalamine, a metabolite of sulfasalazine, is particularly effective in its anti-inflammatory action.
    • Aminosalicylates are typically absorbed in the ileum (last part of the small intestine).
    • Tofacitinib, a janus kinase inhibitor, is used to treat IBD by blocking specific enzymes involved in inflammation.
    • Natalizumab and vedolizumab are integrin receptor antagonists that target adhesion molecules involved in leukocyte migration, reducing inflammation.

    IBD Treatment Strategies & Considerations

    • The most common type of immunity activated in ulcerative colitis is cell-mediated immunity, involving T lymphocytes.
    • Ulcerative colitis can affect any part of the gastrointestinal (GI) tract, unlike Crohn's disease which can affect any part of the GI tract from the mouth to the anus.
    • Treatment of IBD aims to achieve remission (control inflammation), maintain remission, and improve patient quality of life.
    • Long-term treatment with glucocorticoids can lead to osteoporosis, cataracts, and Cushing's syndrome, serious implications.
    • Infusion reactions during natalizumab treatment require immediate action. The infusion should be stopped and appropriate medical assistance sought.
    • Methotrexate, primarily used for rheumatoid arthritis, can also be beneficial in treating IBD.
    • If no therapeutic benefit is observed from natalizumab treatment within 12 weeks, alternative therapies should be considered.

    Drug Groups & Classifications

    • Thiopurines include azathioprine and 6-mercaptopurine, and their main use is for IBD.
    • Glucocorticoids include prednisone, methylprednisolone, and hydrocortisone, which are commonly used for IBD treatment.
    • Aminosalicylates include sulfasalazine and mesalamine, used for their anti-inflammatory actions in IBD.
    • Anti-TNF-alpha agents include infliximab, adalimumab, and certolizumab, used for their ability to block TNF-alpha, a key inflammatory mediator.
    • Integrin receptor antagonists include natalizumab and vedolizumab, used for their ability to block adhesion molecules, preventing leukocyte migration.
    • Janus kinase inhibitors include tofacitinib, which blocks specific enzymes involved in inflammation.

    Drug-Specific Information:

    • Purixan is the brand name for azathioprine.
    • Thioguanine is marketed under the brand name Thioguanine.
    • Azathioprine and 6-mercaptopurine are available as oral medications for IBD.
    • Sulfasalazine is commonly used by patients suffering from both Crohn's disease and ulcerative colitis, the two primary forms of IBD.
    • The mechanism of action of sulfasalazine is based on both its anti-inflammatory properties and its antibacterial effects.
    • 6-Mercaptopurine can cause serious side effects such as myelosuppression, leading to low blood cell counts, including anemia, leukopenia, and thrombocytopenia.
    • The active metabolite of thiopurines responsible for their therapeutic effect is 6-thioguanine (6-TGN).
    • Folic acid supplementation is often necessary for patients taking sulfasalazine to prevent potential deficiencies.
    • Sulfasalazine can cause hepatotoxicity (liver damage), a serious side effect.
    • Sulfasalazine is often not recommended for patients with sulfa allergies.

    Thiopurines: Key Facts

    • Azathioprine is an immunosuppressant that blocks purine synthesis.
    • 6-Mercaptopurine is a purine analog that disrupts DNA synthesis.
    • 6-Thioguanine is a thiopurine used for IBD.
    • Thiopurines can cause adverse effects like myelosuppression, hepatotoxicity, and pancreatitis.

    Glucocorticoids: Essential Information

    • Glucocorticoids are anti-inflammatory medications commonly used for IBD.
    • They modulate the immune system by suppressing the production of inflammatory mediators.
    • Glucocorticoids can have significant side effects, including osteoporosis, cataracts, Cushing's syndrome, and weight gain.
    • Long-term use of glucocorticoids can increase the risk of infections and other complications.

    Ulcerative Colitis vs. Crohn's Disease

    • Ulcerative colitis (UC): Mucosal inflammation affecting the rectum and colon. Humoral mediated immunity (B cells) are involved.
    • Crohn's disease (CD): Transmucosal inflammation affecting any part of the body, from mouth to anus. Cell mediated immunity (T cells) are involved.
    • Common symptom: Bloody diarrhea

    Drug Classes for Treating IBD

    • Anti-inflammatory drugs: Aminosalicylates, such as 5-ASA (5-aminosalicyclic acid), are commonly used.
      • Azo-containing 5-ASA drugs: Azulfidine, Dipentum, Colazal
      • Mesalamine (5-ASA) drugs: Pentasa, Azacol, Rowasa, Canasa, Lialda
    • Other drugs:
      • Glucocorticoids: Prednisone, prednisolone, budesonide, methylprednisone
      • Thiopurines: Azathioprine, 6-mercaptopurine
      • Immunosuppressives: Methotrexate, cyclosporine
      • Anti-TNF-alpha agents: Infliximab, adalimumab, certolizumab pegol, natalizumab
      • IL-receptor antagonist: Ustekinumab
      • Janus kinase inhibitors: Tofacitinib

    Sulfasalazine: MOA, ADRs, Active Compounds, Supplementation

    • Mechanism of action (MOA): Inhibits prostaglandin synthesis (anti-inflammatory). Azo component is broken down to 5-ASA, the active compound.
    • Side effects: Sulfa allergy, headache, rash, nausea, vomiting, diarrhea, bone marrow suppression, yellow-orange discoloration of skin and urine.
    • Active compounds: Mesalamine = 5-ASA
    • Drug-drug interactions (DDIs): Folic acid deficiency may occur, requiring supplementation (1 mg/day).
    • Important note: Sulfasalazine has the most side effects but is also the least expensive.

    Glucocorticoids: MOA and ADRs

    • MOA: Inhibit production of cytokines.
    • Side effects: Cushing's syndrome, adrenal suppression, insomnia, behavioral changes, peptic ulcers, hyperglycemia, impaired wound healing, immunosuppression, osteoporosis, increased intraocular pressure, hypertension, hypokalemia.
    • Pregnancy considerations: All are pregnancy category C, EXCEPT budesonide (pregnancy category B).
    • Important notes: Patients should follow high protein and potassium-rich diets due to hypokalemia. Abrupt discontinuation should be avoided. Patients unresponsive to glucocorticoids cannot take them, and patients dependent on glucocorticoids must take a small dose for life.

    Thiopurines: MOA, ADRs, and DDI Effects

    • MOA: 6-TG (active compound) suppresses purine nucleotide metabolism and DNA synthesis, thereby inhibiting cell division and proliferation, and it inhibits B and T cell function.
    • Side effects: Nausea, vomiting, hepatotoxicity, lymphoma, leukopenia, thrombocytopenia.
    • Boxed warning: Lymphoma, leukopenia, thrombocytopenia.
    • DDIs: Allopurinol is a xanthine oxidase inhibitor, which can increase thiopurine levels. Careful monitoring of CBC and LFTs is essential. In patients with both gout and IBD, high-dose allopurinol is still needed, requiring a decrease in the dose of 6-TGN (azathioprine).

    Thiopurine Metabolism: Slow and Fast Metabolizers

    • Metabolism pathways: Azathioprine and 6-MP are metabolized through three pathways:
      • Oxidative pathway: XO to 6-TU (inactive)
      • S-methylation: TPMT to 6-MMP (inactive)
      • HGPRT: Active nucleotide 6-TGN
    • Slow metabolizers: Patients lacking TPMT are at increased risk of bone marrow suppression. Reduce the dose of thiopurines.
    • Fast metabolizers: Increased dose may be required.

    Methotrexate: MOA, ADRs, Uses, and Antidote

    • MOA: Low dose inhibits AICAR, inhibiting IL-2 and decreasing inflammation. High dose inhibits cell-mediated immunity, decreasing inflammation in cancer.
    • Uses: Crohn's disease, autoimmune diseases (rheumatoid arthritis, psoriasis, lupus, dermatomyositis), cancers, immunosuppressant.
    • Side effects: Myelosuppression, oral ulceration/stomatitis, renal effects, nausea, vomiting, increased LFTs, pneumonitis, photosensitivity, alopecia, crystalluria (high dose).
    • Antidote: Leucovorin.
    • Important notes: Monitor LFTs and stay hydrated to prevent renal toxicity. Make urine basic using bicarbonate.

    Anti-TNF-alfa Agents: MOA, Drug Names, and ADRs

    • MOA: Inhibit TNF-alpha, decreasing cytokine release.
    • Drug names: Infliximab, adalimumab, certolizumab, golimumab.
    • Side effects: Increased infections, reactivation of latent TB, hepatitis B, lymphoma.
    • Important notes: Avoid use in immunocompromised patients.
      • Monoclonal antibody nomenclature:
        • "-mab" or "-monab" indicates monoclonal antibody.
        • The letter before "mab" indicates antibody source: "o" = mouse, "u" = human, "xi" = chimeric.
        • The internal letter indicates therapeutic use: "tu" = tumor, "vi" = virus, "ci" = circulation.
        • Example: Rituximab is a chimeric human-murine monoclonal antibody.

    Potency of Anti-TNF-alpha Agents

    • Infliximab and Adalimumab: More potent due to the presence of an Fc portion that activates the complement pathway. The Fc portion binds to membrane-bound TNF, activating the complement pathway and increasing potency.
    • Certolizumab: Less potent due to the lack of the Fc portion.

    Integrin Receptor Antagonist, Janus Kinase Inhibitor, Cyclosporine, and IL-12/23 Inhibitors

    • Integrin receptor antagonists: Humanized monoclonal antibodies that block lymphocyte migration.
      • Natalizumab: Blocks the interaction of alpha-4-beta-7 integrin with MadCAM-1, inhibiting migration of memory T cells into inflamed GI tissue.
        • Side effects: Infusion reactions, headache, fatigue, brain infection (PML).
      • Vedolizumab: Similar MOA to natalizumab.
        • Side effects: Nasopharyngitis, headache, arthralgia, brain infection (PML).
      • Important notes: For infusion reactions, take Tylenol or Benadryl. If an allergic reaction occurs, stop treatment. Discontinue natalizumab if no therapeutic benefit is seen after 12 weeks.
    • Janus kinase inhibitor: Inhibits Janus kinase, inhibiting immune cell functions.
      • Tofacitinib (Xeljanz):
        • Side effects: Increased LFTs, increased lipids, infusion reactions, infections.
      • Important notes: Not a monoclonal antibody, but a small molecule taken orally. Primarily used for rheumatoid arthritis but demonstrates benefits in IBD.
    • Cyclosporin: Immunosuppressive agent that inhibits calcineurin, a key enzyme in T cell activation.
      • Adverse effects: Increased risk of infections, kidney dysfunction, hypertension, hair growth, tremor.
    • Inhibitors of IL-12/23: Block the production of IL-12 and IL-23, cytokines that contribute to inflammation in IBD.
      • Ustekinumab:
        • Side effects: Headache, nausea, injection site reactions, infections.
        • Important notes: This drug is approved for the treatment of moderate to severe Crohn's disease and plaque psoriasis.

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    Description

    This quiz covers the basics of Inflammatory Bowel Disease (IBD), focusing on the two major types: Ulcerative Colitis and Crohn's Disease. It also explores various medications used to treat IBD, including anti-inflammatory drugs and immunosuppressives. Test your knowledge on symptoms, treatments, and the pathophysiology of these conditions.

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