Farmakologi Ulcerative

Colitis
Kelompok 1
 Nama Kelompok
• Shaiba amalia (G1A113045)
• Fraya Livia Ulima (G1A113046)
• Sara Ashari (G1A113047)
• Fiona Mazka (G1A113048)
• Putri Rahmadanita (G1A113049)
• Veragita Mayasari (G1A113050)
• Wenny Oktaviani (G1A113052)
• Argius Tumanggor (G1A113053)
• Rabani Mukram, D (G1A113054)
• Febriano Ramadhana (G1A113055)
• Inflammatory bowel disease (IBD) refers to the
idiopathic bowel disorders, ulcerative colitis and
Crohn's disease
• The couses are unidentified
 Distinguishing features of ulcerative
colitis (UC) versus Crohn's disease

Ulcerative colitis Crohn's disease

Mucosal Disease Transmural disease

a patchy distribution
the rectum is virtually always
throughout the entire
involved,
gastrointestinal (GI) tract

a contiguous manner may involve any part of the

extending proximally from GI tract from the mouth to
the rectum the anus.
 Ulcerative Colitis Crohn's Disease

Pain crampy, lower abdominal, relieved Pain constant, often in right lower
by bowel movement quadrant, not relieved by bowel
movement
Bloody stool Stool usually not grossly bloody

No abdominal mass Abdominal mass, often in right lower

quadrant
Affects only colon May affect small and large bowel,
occasionally esophagus and stomach

Mucosal disease (granulomas are not a Transmural disease (granulomas found

feature) in a minority of patients)

Continuous from rectum May be discontinuous (skip areas)

 DRUGS
• Because the etiology of IBD is incompletely
understood, drug treatment is aimed at
alleviating and reducing inflammation.
• Jarang digunakan antibiotik untuk terapi agen
proinflamasi pada C.U
• Amino Salicylic Acid.
• Corticosteroids.
• Immunomodulators.
• Antidiarrheal medications.
 Amino Salicylic Acid
• Sulfasalazine
• aminosalicylates (mesalamines)
 Sulfasalazine
 efficacious in active and remitted UC and inactive
Crohn's disease when the colon is involved.
 consists of sulfapyridine linked to 5-aminosalicylic
acid (5-ASA or mesalamine) via an azo bond
 Intestinal bacteria -> break into 2
 The sulfapyridine moiety is systemically absorbed
and excreted in the urine and the 5-ASA moiety, the
active component, stays in the intestinal lumen in
contact with the mucosa and eventually is excreted
in the feces
 Side effects :
1. Abdominal discomfort -> minimized by
ingestion of the sulfasalazine after eating
2. folate-deficient
3. skin eruptions and bone marrow
suppression (less common)
 Dosage :
1. The initial daily dose is low (1 g) to
minimize GI side effects.
2. A therapeutic dose of 3 to 4 g per day is
appropriate.
3. A CBC and liver chemistry tests should be
obtained before starting therapy
Maintenance treatment
1. to reduce the frequency of
exacerbations of ulcerative colitis.
2. 2 to 3 g per day in divided doses
 The 5-ASA preparations and
sulfasalazine are safe to use in
pregnant women.
B. Other 5-ASA (mesalamine) preparations
• serious side effects of sulfasalazine are related
to the sulfa portion
• Oral 5-ASA preparations : Olsalazine
(Dipentum), Asacol, Pentasa, Balsalazide
disodium (Colazal)
• Topical 5-ASA preparations : Rowasa and
Canasa
 ORAL 5-ASA preparations

1. Olsalazine (Dipentum)
 consists of two 5-ASA molecules joined by
an azo bond such as sulfasalazine,
 Requires bacterial degradation in the
colon.
 effective against active UC and in
maintaining remission
2. Asacol
 controlled-release tablet form of 5-ASA
 dissolves at a pH higher than 6.0.
3. Pentasa
 controlled-release formulation of 5-ASA
 encapsulated in ethylcellulose microgranules.
 Pentasa appears to help in maintaining remission
in both small-bowel and colonic Crohn's disease.
4. Balsalazide disodium (Colazal)
 a newer 5-ASA preparation
primarily effective in treating IBD involving the
colon especially left-sided colitis.
 Topical 5-ASA preparations
• Rowasa enema and Canasa suppositories.
1. effective in active and remitted distal UC and
ulcerative proctitis.
 Drug Name Formulation Dosage
Azulfidine 500-mg tablets 1-2 tablets global p.o. q.i.d
(1-4 g/d)

Dipentum 500-mg tablets 2 capsules p.o. b.i.d.(1 g/d)

Asacol 400-mg tablets 2-4 tablets p.o. t.i.d (2.4-4.8
g/d)

Pentasa 250-mg capsules 4 capsules p.o. t.i.d. (3-4

g/d)
Colazal 750-mg capsules 3 capsules p.o. t.i.d. (1,250
mgRowasa enema)

Rowasa enema 4 g-unit dose/60-mL enema 1-2 daily (preferably at

bedtime)

Canasa suppositories 500-mg rectal suppositories 1-2 times daily

ASA, aminosalicylic acid; p.o. per os; q.i.d., four times daily; t.i.d., three times
daily.
• to induce a remission
• IV : Intravenous (IV) steroids (i.e.
hydrocortisone 100 mg IV q6h or
methylprednisolone 10-20 mg IV every 6 to 8
hours.
• Oral : prednisone at doses of 40 to 60 mg per
day.
• If symptoms improve, the drug is tapered and
withdrawn over a period of several months.
not recommended for
maintenance therapy of
UC or Crohn's disease

steroids do not prevent

relapse of Crohn's disease
or UC

major side effects.

• many patients become steroid dependent and
experience recurrence of symptoms when the
dose of prednisone is reduced to less than 15
mg per day. One strategy is to use
azathioprine,6-mercapopurine (6-MP), or
azathioprine (Imuran) for steroid-dependent
patients to help to taper them off steroids.
• Several corticosteroid enema preparations are
available for the treatment of proctitis and
distal colitis. These are usually administered
once or twice a day.
 immunomodulator
• Azathioprine (Imuran)
• Cyclosporin (Neoral Sandimmune)
• Infliximab (Remicade)
• Nicotine
 Azathioprine (Imuran)
• is effective and safe.
• Indications of UC include, refractory UC, steroid-
dependent UC, UC remission maintenance
recurrence.
• Maximum clinical response takes 2 to 3 months.
• Monthly or bimonthly CBC is recommended to
monitor and prevent neutropenia
• safe for use during pregnancy
 Cyclosporin (Neoral Sandimmune
• 4 mg/kg per day IV; therapeutic range 250-
350 mg/mL
• used successfully in severe steroid refractory
UC as a bridge therapy to either long-term
immunomodulatory therapy (i.e., with Imuran
or 6-MP) or definitive colectomy (e.g. in
pregnant or young patients in whom
immediate surgery is not optimal)
• side-effect profile (hypertension, and nephro-
and bone marrow toxicities) limits its
usefulness.
• Cyclosporin should not be used for remission
maintenance for UC or Crohn's disease.
 Nicotine
• given in enema form has shown some benefit
in patients with distal UC
• not widely used
 Antidiarrheal medications.
• If diarrhea does not improve with the previously
described medical therapy in patients with mild-
to-moderate IBD
• Codeine is most effective
• loperamide (Imodium) or diphenoxylate
(Lomotil) may be preferred because of their
lower addictive potential.
• Opiate derivatives should not be used in patients
with severe IBD because of the possibility of
inducing toxic megacolon.