Drugs used in inflammatory bowel disease in detail

1. Drug acting on
Inflammatory Bowel
Disease
Ms Alisha Talwar

2. Inflammatory Bowel Disease
 Inflammatory bowel disease (IBD) is an umbrella term
used to describe disorders that involve chronic
inflammation of the digestive tract.
 Types of IBD include:
 Ulcerative colitis
 Crohn's disease

5. Pharmacological Management
 5-Aminosalicylic Acid (5-ASA, Mesalamine)
 Corticosteroids
 Immunomodulating Drugs
 Biologic Agents
 Antibiotics
 Probiotics

6. 5-Aminosalicylic
Acid (Mesalamine)

7. 5-Aminosalicylic Acid
 Mesalamine is an anti-inflammatory agent
 It is an Aminosalicylate
 Generic Name- SULPHASALAZINE
 Trade Names -Azulfidine, PMS
Sulfasalazine , PMS Sulfasalazine

8. Contd…
 Classifications: Gastrointestinal agent; mucous
membrane agent; anti-inflammatory; sulphonamide
 Availability- 500 mg tablets; 500 mg sustained release
tablets

9. Mechanism of Action
 Locally acting sulfonamide.
 Believed to be converted by intestinal microflora to
sulfapyridine (provides antibacterial action)
 Also has an anti-inflammatory effect.
 It also helps in inhibition of prostaglandins known to cause
diarrhea and affect mucosal transport, and interference with
absorption of fluids and electrolytes from colon.

10. Indications
 Ulcerative colitis
 Regional enteritis
 Rheumatoid arthritis.

11. Contraindications
 Sensitivity to sulfasalazine
 Agranulocytosis
 Children <2 y
 Intestinal and urinary tract obstruction
 porphyria

12. Route & Dosage
 Ulcerative Colitis
Adult: PO 1–2 g/d in 4 divided doses, may increase up
to 8 g/d if needed
Child: PO 40–50 mg/kg/d in 4 divided doses (max: 75
mg/kg/d)

13. Pharmacokinetics
 Absorption: 10–15% absorbed from GI tract
unchanged; remaining drug is hydrolyzed in colon
 Peak: 1.5–6 h
 Distribution: Crosses placenta; distributed into breast
milk.
 Metabolism: Metabolized in intestines and liver.
 Elimination: All metabolites are excreted in urine.
 Half-Life: 5–10 h.

14. Nursing Implications
 Monitor for GI distress
 Measure RBC folate in patients on high doses (more
than 2 g/d
 Drug may cause alkaline urine and skin orange-yellow in
colour
 Remain under close medical supervision. Relapses occur
in about 40% of patients after initial satisfactory
response.

15. Corticosteroids

16. Corticosteroids
 Used to reduce inflammation and suppress the immune
system.
 Drugs used are hydrocortisone, methylprednisolone,
Budesonide
 Mechanism of Action -It reduces inflammation in the
digestive tract and relieve symptoms and suppresses the
immune system

17. Corticosteroids

18. Hydrocortisone Methylprednisolone Budesonide
Trade Name Alphaderm, Cetacort,
Cortaid, Cort-
Dome, Cortenema, Cor
tril
Medrol Entocort EC
Classification Skin and mucous
membrane
agent; anti-
inflammatory; synthetic
hormone; adrenal
corticosteroids;
glucocorticoid;
mineralocorticoid
Hormones and
synthetic
substitutes; adrenal
corticosteroid;
glucocorticoid; anti-
inflammatory
Hormone and synthetic
substitute; adrenal
corticosteroid;
glucocorticoid;
mineralocorticoid
Availability Hydrocortisone Sodium
Phosphate 50 mg/mL
injection
Hydrocortisone Sodium
Succinate 100 mg/2
mL, 250 mg/2 mL, 500
mg/4 mL, 1000 mg/8
mL vials
Methylprednisolone 2
mg, 4 mg, 8 mg, 16
mg, 24 mg, 32 mg
tablets
Methylprednisolone
Acetate 20 mg/mL, 40
mg/mL, 80 mg/mL
injection
32 mcg/inhalation; 3
mg capsule

19. Hydrocortisone Methylprednisolone Budesonide
Indications • Replacement therapy
in adrenocortical
insufficiency
• Hypercalcemia
• Ulcerative colitis
• Inflammatory
conditions
• acute & chronic
inflammatory
diseases
• palliative
management of
neoplastic
diseases
• Treatment of allergic
and perennial
rhinitis,
• mild to moderate
Crohn's disease;
• prophylaxis for
asthma.
Contraindications • Hypersensitivity to
glucocorticoids
• acute
glomerulonephritis,
• hypercorticism
(Cushing's syndrome)
• Hypersensitivity
• Systemic fungal
infections
• Hypersensitivity
• Lactation
Route and Dosage Anti-inflammatory Agent
Adult: Topical Apply to
the affected area 1–4
times/d PR Insert 1%
cream, 10% foam, 10–25
mg suppository
Inflammation
Adult: PO 2–60
mg/d IM (Acetate)
4–80 mg/wk for 1–4
wk; (Succinate) 10–
250 mg q6h IV 10–
250 mg q6h
Crohn's Disease
Adult: PO 9 mg once/d
in a.m. for up to 8 wk,
may taper to 6 mg q.d.
for 2 wk

20. Hydrocortisone Methylprednisolone Budesonide
Adverse Effects • Hypertension
• Hyperglycemia
• Weakened bones
• Thinning of the skin
• Weight gain
• Acne or stretch marks
• Rounding of the face
• Increased facial hair
• Insomnia
• Mood swings
• Nausea & Vomiting
• Euphoria
• Insomnia
• Edema
• Nausea Vomiting
• Muscle weakness
• Leucocytosis
• Hypokalemia
• CHO intolerance
• Hyperglycemia
• Arthralgia
• Fatigue
• Fever
• hyperkinesis,
• Myalgia
• Asthenia
• Headache
• Nausea Vomiting
• Infection
• Alopecia
Pharmacokinetics Absorption: Readily GI
tract Onset: 1–2 h PO;
immediately IV
Peak: 1 h PO
Metabolism: Hepatically
metabolized.
Elimination: excreted in
urine
Half-Life: 1.5–2 h
Absorption: Readily
GI tract Peak: 1–2 h
PO; 4–8 d
IM. Duration: 1.25–
1.5 d PO; 1–5 wk
IM. Metabolism: Met
abolized in
liver. Half-Life: >3.5 h
Absorption: Readily GI
tract Peak: 8 wk oral
Metabolism: in liver
Elimination: 60%
excreted in urine, 40%
in feces. Half-Life: 2–
3.6 h

22. Nursing Implications
 Monitor BP, weight, fluid and electrolyte balance, and blood
glucose levels
 Observe for periodic serum electrolytes blood glucose, Hct
and Hgb, platelet count, and WBC with differential.
 Monitor for adverse effects. Older adults and patients with
low serum albumin are especially susceptible to adverse
effects.
 Be alert to signs of hypocalcemia, cushing syndrome and
thyroid

23. Contd….
 Expect a slight weight gain with improved appetite.
 Avoid alcohol and caffeine
 Do not ignore dyspepsia with hyperacidity, Report physician
 Do not breast feed while taking this drug
 Compliance to treatment, Don’t miss or stop abruptly
 Report immediately if Fatigue, nausea, anorexia, joint pain,
muscular weakness, dizziness, fever occur

24. Immunomodulating
Drugs

25. Immunomodulating agents
 The antimetabolites azathioprine, 6-mercaptopurine,
and methotrexate are also used in combination therapy
with biologic agents.

26. Azathioprine
 Generic Name- Azathioprine
 Trade Name-Azasan, Imuran
 Classifications: IMMUNOSUPPRESSANT
 Availability- 50 mg, 75 mg, 100 mg
tablets; 100 mg vial

27. Contd….
 Action- inhibits DNA, RNA, and normal protein synthesis in
rapidly growing cells
 Indications
 Adjunctive agent to prevent rejection of kidney allografts,
 Active rheumatoid arthritis
 Ulcerative colitis
 Other inflammatory and immunologic diseases

28. Contraindications
 Hypersensitivity to azathioprine or mercaptopurine;
 clinically active infection
 Anuria
 Pancreatitis
 concurrent radiation therapy
 pregnancy & lactation

29. Route & Dosage
 Adult: PO 1 mg/kg/d initially, may be increased by 0.5
mg/kg/d at 4–6 wk intervals

30. Adverse Effects
 Hypersensitivity (skin eruptions, rash, arthralgia)
 GI: Nausea, vomiting, anorexia, esophagitis, diarrhea,
steatorrhea
 Hematologic: Bone marrow depression,
pancytopenia.
 Other: dysarthria, alopecia;

31. Pharmacokinetics
 Absorption: Readily absorbed from GI tract.
 Distribution: Crosses placenta.
 Metabolism: Extensively metabolized in liver to active
metabolite mercaptopurine.
 Elimination: Eliminated in urine.
 Half-Life: 3 h

32. Nursing Implications
 Monitor CBC, kidney function, vitals and liver function
 Report for easy bruising, bleeding gums, petechiae,
purpura, melena, epistaxis, dark urine (hematuria),
hemoptysis, hematemesis- signs of bleeding
 Avoid contact with infected person
 Avoid breastfeed while taking this drug.

33. Mercaptopurine
 Generic name-Mercaptopurine (6-mp, 6-
mercaptopurine)
 Trade Name-Purinethol
 Classifications: ANTINEOPLASTIC; ANTIMETABOLITE,
PURINE ANTAGONIST; IMMUNOSUPPRESSANT
 Availability- 50 mg tablets

34. Mechanism of Action
 Blocks conversion of inosinic acid to adenine and
xanthine ribotides within sensitive tumor cells. Also
inhibits adenine-containing coenzymes, suggesting an
influence over multiple cellular reactions

35. Indication
 Primarily for acute lymphocytic and myelogenous
leukemia
 Prevention of transplant graft rejection
 SLE
 Rheumatoid arthritis
 Crohn's disease.

36. Contd….
 Contraindications- Hypersenstivity to
mercaptopurine, pregnancy, lactation
 Route & Dosage- PO Loading Dose 2.5 mg/kg/d,
may increase up to 5 mg/kg/d after 4wk

37. Adverse Effects
 GI: Stomatitis, esophagitis, anorexia, nausea, vomiting,
diarrhea, intestinal ulcerations, impaired liver
function, hepatic necrosis.
 Hematologic: Leukopenia, anemia, eosinophilia,
pancytopenia, thrombocytopenia, abnormal bleeding.
 Urogenital: Hyperuricemia, oliguria, renal impairment.

38. Pharmacokinetics
 Absorption: Approximately 50% absorbed from GI
tract.
 Peak: 2 h.
 Distribution: Distributes into total body water.
 Metabolism: Rapidly metabolized by xanthine oxidase
in liver.
 Elimination:11% excreted in urine within 6 h.
 Half-Life: 20–50 min.

39. Nursing Implications
 Monitor CBC with differential, platelet count, Hgb, Hct,
and liver functions
 Record baseline data related to I&O ratio and pattern
and body weight.
 Check vital signs daily. Report febrile states promptly.
 Report nausea, vomiting, or diarrhea
 Watch for signs of abnormal bleeding

40. Methotrexate
 Generic Name-Methotrexate
 Trade name-amethopterin, mexate, mtx
 Classifications: ANTINEOPLASTIC
AGENT; ANTIMETABOLITE,
ANTIFOLATE; IMMUNOSUPPRESSANT
 Availability- 2.5 mg tablets; 20 mg, 1 g powder for
injection; 2.5 mg/mL, 25 mg/mL injection

41. Mechanism of Action
 Action-Antimetabolite and folic acid antagonist. Blocks
folic acid participation in nucleic acid synthesis, thereby
interfering with mitotic process

42. Indications
 Gestational choriocarcinoma
 hydatidiform mole
 kidney transplantation
 leukemias
 Rheumatoid arthritis
 SLE
 Crohn’s Disease

43. Contraindications
 Pregnancy
 men and women in childbearing age
 Lactation
 Hepatic and renal insufficiency
 Alcohol

44. Route & Dosage
 Adult: PO 15–30 mg/d for 5 d, repeat q12wk for 3–5
courses IM/IV 15–30 mg/d for 5 d, repeat q12wk for
3–5 courses

45. Adverse Effects
 Headache
 drowsiness
 blurred vision
 Confusion
 Glossitis & Gingivitis
 Leucopenia
 Rashes
 Myelosuppression

46. Nursing Implications
 Monitor CBC, LFT, KFT
 Monitor for and report ulcerative stomatitis with glossitis and
gingivitis, often the first signs of toxicity. Inspect mouth daily; report
patchy necrotic areas, bleeding and discomfort, or overgrowth (black,
furry tongue).
 Avoid or moderate alcohol ingestion, which increases the incidence
and severity of methotrexate hepatotoxicity.
 Do not self-medicate with vitamins. Some OTC compounds may
include folic acid (or its derivatives), which alters methotrexate
response.

48.  http://www.crohnscolitisfoundation.org/resources/immu
nomodulators.html

49. Biologic agents

50. Anti TNF agents
 Infliximab, certolizumab, adalimumab,
and golimumab are antibodies to tumor necrosis factor
(TNF).

51. Infliximab
 Generic Name-Infliximab
 Trade Name-Remicade
 Classifications: BIOLOGIC RESPONSE
MODIFIER; TUMOR NECROSIS FACTOR MODIFIER
 Availability- 100 mg powder for injection

52. Mechanism of Action
 IgG1-K monoclonal antibody that binds specifically to
tumor necrosis factor-alpha (TNF-alpha), a cytokine.
Thus, it prevents TNF-alpha from binding to its
receptors. TNF-alpha induces proinflammatory cytokines
such as interleukin-1 (IL-1) and IL-6.

53. Indications
 Moderately to severely active Crohn's disease
 Rheumatoid arthritis
 Ankylosing spondylitis.

54. Contraindications
 Hypersensitivity to infliximab
 CHF
 Infection
 sepsis
 murine protein hypersensitivity
 lactation.

55. Route & Dosage
 Crohn's Disease
Adult: IV 5 mg/kg infused over at least 2 h, may repeat
at 2 and 6 wk for fistulizing disease

56. Adverse effects
 Fatigue
 Fever
 Back pain
 Dizziness
 Insomnia
 Nausea/vomiting
 Pancytopenia
 urticaria

57. Pharmacokinetics
 Distribution: Distributed primarily to the vascular
compartment.
 Half-Life: 9.5 d.

58. Nursing Implications
 Discontinue IV infusion and notify physician for fever,
chills, pruritus, urticaria, chest pain, dyspnea,
hypo/hypertension.
 Monitor for and immediately report S&S of local IV site
or more generalized infection.

59. Antibiotics

60. Metronidazole
 Generic Name- Metronidazole
 Trade Name-Metrogyl, Flagyl ER, Flagyl IV
RTU, Flagyl 375, Metizol, Metric 21
 Classifications: Antiinfective; antitrichomonal; amebicide;
antibiotic
 Availability- 250 mg, 500 mg tablets; 375 mg capsules;
750 mg sustained release tablets; 500 mg vials; 0.75%
lotion, emulsion; 0.75%, 1% cream; 0.75%, 1% gel

61. Mechanism of Action
 Synthetic compound with direct trichomonacidal and
amebicidal activity as well as antibacterial activity
against anaerobic bacteria and some gram-negative
bacteria.

62. Indications
 Acute intestinal amoebiasis
 Amoebic liver abscess
 Preoperative prophylaxis in colorectal surgery
 Infections
 Treatment of pseudomembranous colitis
 Crohn's disease
 H. pylori eradication.

63. Contraindications
 Hypersensitivity
 Blood dyscrasias
 active CNS disease
 Pregnancy
 Lactation

64. Route & Dosage
 Adult: PO 500–750 mg t.i.d.
Child: PO 35–50 mg/kg/d in 3 divided doses

65. Adverse effects
 Insomnia
 Headache
 Nausea/ vomiting
 dry mouth
 metallic or bitter taste
 Dyspareunia
 Dryness of vagina
 Polyuria
 ECG changes- flattening of
T wave
 Parasthesia

66. Pharmacokinetics
 Absorption: 80% of dose absorbed from GI tract.
 Peak: 1–3 h.
 Distribution: Widely distributed to most body tissues,
including CSF, bone
 Metabolism: 30–60% metabolized in liver.
 Elimination: 77% excreted in urine; 14% excreted in feces
within 24 h.
 Half-Life: 6–8 h.

67. Nursing Implications
 Discontinue therapy immediately if symptoms of CNS toxicity
develop.
 Monitor especially for seizures and peripheral neuropathy
(e.g., numbness and paresthesia of extremities).
 Monitor for S&S of sodium retention, especially in patients
on corticosteroid therapy or with a history of CHF.
 Avoid alcohol
 Urine may appear dark or reddish brown

68. Probiotics

69. Probiotics
 Live bacteria and yeasts that are called "the good"
microorganisms because they benefit the body,
specifically the digestive system.
 Probiotics, available in some foods and dietary
supplements, are similar to probiotics that exist
naturally in the gut.

70. Mechanism of Action
 Probiotics may help to keep healthy by:
 Decreasing the number of "bad" bacteria in the gut
that can cause infections or inflammation
 Replacing the body's "good" bacteria
 Restoring the body's "good" versus "bad" bacterial
balance, which then helps to keep the body
functioning properly

71. Examples
 Probiotics that are naturally found in the intestines
include: Saccharomyces boulardii (a yeast) and bacteria in the
Lactobacillus and Bifobacterium families of microorganisms.
 Foods that contain probiotics include: some juices and soy
drinks, fermented and unfermented milk, buttermilk, some soft
cheeses
 Supplements: dietary probiotic supplements -- which are
available in capsules, tablets, powders and liquid extracts -- each
contain a specific type of probiotic.

72. Indications
 Pouchitis
 Inflammatory bowel diseases
 Irritable bowel syndrome
 Acid reflux
 Spastic colon

73. Adverse effects
 Probiotics may trigger allergic reactions.
 They may also cause mild stomach upset, diarrhea, or
flatulence (passing gas) and bloating for the first few
days after starting to take them

74.  https://www.youtube.com/watch?v=U1p4YMU3vWk&fe
ature=youtu.be

75. Summary