GastroIntestinal Flashcards
Idiopathic disease involving an immune reaction of the body to its own intestinal tract
Inflammatory Bowel Disease (IBS)
IBS major types?
UC
Crohns
UC is limited to the ?
colon
Crohns disease can involve ________ of the gastrointestinal tract
any part
IBS: goal of therapy?
Goal of therapy: Reduce inflammation and control flare-ups
IBS tx step wide approach ?
Benign drugs first
5-ASA’s first
Crohns, peri-anal disease and inflammatory mass
Corticosteroids 2nd
Immune modifying agents 3rd
______ oral aminosalicylate agents in the United States
Six
Two most common 5-ASAs?
Sulfasalazine (Azulfidine)
Mesalamine ( Asacol, Pentasa, Lialda)
_________ was originally proposed as a treatment for rheumatoid arthritis.
Sulfasalazine
It was subsequently discovered that sulfasalazine was also efficacious in treating ?
inflammatory bowel disease, particularly ulcerative colitis.
The 5-aminosalicylic acid (5-ASA) medications were developed because many patients were intolerant of or allergic to _________.
sulfasalazine
____________ is a prodrug composed of 5-aminosalicylic acid (5-ASA) linked to __________.
Sulfasalazine
sulfapyridine
___________ accounts for many of its side effects
Sulfapyridine
5-ASA MOA?
exact mechanism of action unknown
blocks cyclooxygenase and inhibits prostaglandin
production
producing anti-inflammatory effects
ASA also black cyclooxygenase
Also known as “DMARDS” (disease-modifying antirheumatic drugs)?
5-ASA
Compounds are broken up by ____________ releasing active compound 5-ASA
colonic bactreria
Indications for Sulfasalazine (Azulfidine)?
Ulcerative Colitis
Crohn’s Disease
Rheumatoid Arthritis
Sulfasalazine trade?
Azulfidine
Side effects can occur with both sulfasalazine and 5-ASA, but are more common with ____________
sulfasalazine
Approximately ______ percent of patients discontinue sulfasalazine due to side effects.
20 to 25
Adverse reactions and interactions to Sulfasalazine (Azulfidine)?
Pruritus
abnormal LFTs
leukopenia
urticaria, anemia
hemolytic anemia
TTP
cyanosis
anorexia
N/V, HA and dizziness
Sulfasalazine (Azulfidine) monitoring?
CBC w/ diff, LFTs at baseline, then q2wk x3mo, then
BUN/Cr, urinalysis w/ microscopic exam
Sulfasalazine (Azulfidine) decreases?
Decreases the effects of
Iron supplement, Digoxin and Folic Acid
Sulfasalazine (Azulfidine) increases the effects of?
oral anticoagulants,
hypoglycemic agents
methotrexate
**check INR and glucose*
Contraindications to Sulfasalazine (Azulfidine)?
Hypersensitivities to sulfonamides and salicylates (ASA, Bactrim)
GI obstruction
caution if renal impairment
caution if hepatic impairment
**it will slow motility so you get GI obstruction *
Sulfasalazine (Azulfidine) is Preg. Cat?
Pregnancy Cat B (trimester specific due to folate metabolism)
** cause what it does to the folic acid synthesis *
Sulfasalazine (Azulfidine) dosing?
Dosing
Crohns: Dz 500 mg PO q 6hr - give with food
RA: 1 Gm PO q 12 hr
UC: 500 mg q 6 hr
mesalamine three trade name?
Asacol
Pentasa
Lialda
Mesalamine indications?
Indicated for Crohns Disease and Ulcerative Colitis
Mesalamine is a derivative of?
derivative of salicylic acid (anti-inflammatory effects)
The release of 5-ASA is ____________
pH-dependent
** pH dependent is the key to the drug especially when it comes to prescribing it *
Oesophagus pH?
7.0
Stomach pH?
1-2.5 (5 when fed)
Proximal small intestine pH?
6.16-7.35
Distal small intestine pH?
6.8-7.88
Ascending colon pH?
5.26-6.72
Descending colon pH?
5.02-7.02
Mesalamine targets location depending on ?
pH
_______- drug released at a pH of 7 (typically at the terminal ileum)
Asacol
**more for UC*
_______ – time release coating begins at pylorus (pH 4), used proximal colonic disease ( more acidic)
Pentasa
**more for crohns*
______ indicated to induce remission of active UC
Lialida
_________ of release mechanism of Asacol and Pentasa
Combination
Mesalamine has a ____ relapse
high
__________ high concentration of mesalamine to descending colon (enema or suppository for proctitis)
Rectal dosage
Mesalamine: UC tx?
Oral: Usual course of therapy is 6 to 8 weeks:
Asacol HD: 1.6 g 3 times daily for 6 weeks
Delzicol: 800 mg 3 times daily for 6 weeks
Lialda: 2.4 or 4.8 g once daily
Pentasa: 1 g 4 times daily
Mesalamine: UC remission maintenance?
Oral:
Apriso: 1.5 g once daily in the morning
Delzicol: 1.6 g in 2 to 4 divided doses
Lialda: 2.4 g once daily
Pentasa: 1 g 4 times daily
**GOUT people get an additional high dose and then a maintenance dose *
Anti-diarrhea Meds: Absorbent preparations
?
Bismuth subsalicylate (Pepto-Bismal, Kaopectate)
Anti-diarrhea Meds: Opiates?
Diphenoxylate with atropine (Lomotil)
Anti-diarrhea Meds: Anticholinergics (IBS)?
Belladonna
Scopalamine
remember glaucoma effects of anticholenigerics - closed canal of schlemm which would increase IOP.
Biological Therapies are ?
Immune Modifying Agents or Biologicals
When are Biological Therapies indicated?
When corticosteroids fail or require long term therapy
Biologicals not used in acute flare-ups - cause onset of action is not until 2-3 months
BT: Class: Tumor Necrosis Factor (TNF) Inhibitors
examples?
Infliximab (Remicade)
Etanercept (Embrel)
Adalimumab (Humira)
TNF Inhibitors BBW?
Chronic or recurrent infection
Pulmonary and extrapulmonary tuberculosis (TB)
Invasive fungal infections and other opportunistic infections incl. Legionella and Listeria ( especially w/ PNA)
**these really suppress immune system and open you up for opportunistic infections, CXR and basic lab work for monitoring and before you give them treatment with these guys *
TNF Inhibitors indications?
Crohns Ulcerative Colitis Rheumatoid Arthritis Ankylosing Spondylitis Psoriasis
TNF inhibitors contrindications?
Contraindicated in co-morbid active infections and disease:
DM
hepatitis
restrictive lung disease
TNF Inhibitor facts?
Peds under >6 yo
Many drug-drug interactions
TNF inhibitor reactions?
serum sickness
anaphylactoid rxn
hypersensitivity rxn ( rashes preload with prednisone and benadryl ( premedicate))
Opportunistic infections, sepsis, pneumonia, opportunistic infection, tuberculosis, malignancy, lymphoma, hepatosplenic T-cell lymphoma (peds pts), leukemia, HBV reactivation, hepatotoxicity, CHF
TNFI are administered _________ and repeated at _ week and _ week intervals
Administered IV infusion and repeated at 2 week and 6 week intervals
How long do you observe for post infusion signs of infections when taking TNFI?
Observed for post infusion signs of infections (3-12 days)
Lipase Inhibitor?
Orlistat
Orlistat is the only drug in class?
Lipase Inhibitors
FDA approval in 1999
What is commonly used for obesity management?
Orlistat:
Commonly used for obesity management
Weight loss
Weight maintenance
Reduce the risk of weight gain following weight loss
**reduces absorbing of fat , potato chip*
What is Orlistat used with ?
calorie diet
Orlistat trade name?
Orlistat (Alli, Xenical)
Orlistat indications Obesity?
BMI greater than 30
BMI greater than 27 with co-morbidities (HTN, DM, HLP)
Orlistat MOA?
reversible inhibitor of gastric and pancreatic lipases, thus inhibiting absorption of dietary fats by 30%
Binds sites stomach and small intestines
Does not break down dietary fat
Undigested triglycerides not absorbed causing reduced caloric intake
Orlistat availability?
OTC 60 mg capsule PO tid
Reduced calorie diet and exercise
Orlistat adverse reactions?
Fatty / oily stools
Fecal urgency, flatulence, increased stools
Contraindications to Orlistat?
Malabsorption disorders, vitamin deficiency and cholestasis
**short gut sycnrome or gastroparesis or GB disease - avoid this medication in these people *
Zofran is Preg. Cat ?
C
it used to be B
What is a Reverse Lipase Inhibitor?
Binds sites stomach and small intestines
Does not break down dietary fat
Undigested triglycerides not absorbed causing reduced caloric intake