PUD & GERD

MOA Uses Side Effects/Contraindications Other

ANTACIDS Neutralizes H+ in stomach lumen GERD, PUD AlOH, MgOH → Renal function Absorption of:
Aluminum OH MgOH → Diarrhea Azoles
Magnesium OH AlOH, CaCO3 → Constipation Tetracyclines
Calcium carbonate All → Metabolic Alkalosis, Fluoroquinolones (flox)
Hypokalemia
H2 BLOCKERS
Cimetidine:
Cimetidine
Reversibly inhibit H2 receptor on PUD, GERD, esophagitis, P450 inhibitor → Drug interactions
Famotidine 24 hr secretion by 70%
parietal cells → H+ secretion GI bleeds, stress ulcers, ZES Anti-androgenic effect in men
Ranitidine
Nizatidine
PPIs
Omeprazole 24 hr action
Esomeprazole Irreversibly inhibit H+/K+ pump PUD, GERD, gastritis, ZES Serum Mg 48 hr secretion by 95%
Rabeprazole in parietal cells → H+ secretion (Fa e e ef/ ea g a H2 ) ↑C. difficile, pneumonia, hip fractures 4-8 wk course of Rx to
Lansoprazole heal ulcer
Pantoprazole
Activated PG receptors on Mostly prescribed for
PGE1 ANALOG Diarrhea, pain & cramps
parietal cells → Gi pathway → NSAID-induced PUD/GERD elderly on long-term
Misoprostol Birth defects, premature birth
H+ secretion, ↑HCO3- secretion NSAIDs for arthritis
ANTI-CHOLINERGIC Atropine-like = Anorexia, blurry vision,
Inhibits M1 AChR → H+ secretion Rare, only as adjunct Rx As effective as H2s
Pirenzepine constipation, dry mouth, sedation
Sucralfate req. acid pH to activate
PROTECTIVE BARRIERS Prevent & Rx PUD Sucralfate - interferes with absorption Bismuth should not be
Coats ulcer base providing
Sucralfate Bismuth damages H. pylori of other drugs (take 2 hours apart) used repeatedly or >2
protective barrier from stomach
Bismuth cell wall Bismuth → black stool, constipation months
acid
ANTI-MICROBIALS H. Pylori-induced PUD
Moderate Abx: Kills H. Pylori → Gastric damage (85% of cases) Metronidazole = used
Amoxicillin Amox - cell wall synthesis
Triple Rx: 7 d, 85% effective in bacterial resistance
Tetracycline Tetra - protein synthesis (30S)
PPI + Mod. Abx + Strong Abx or antibiotic intolerance
Strong Abx: Clarith - protein synthesis (50S)
Quadruple Rx: 3 d, 85% eff. to Amox, Tetra
Clarithromycin Metro - DNA synthesis
Metronidazole Triple Rx + Bismuth

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MOA
SALICYLATES (ASAs) COX suppression → PGs →
Sulfasalazine inflammation (5-ASA product)
Mesalazine
Balsalazide
Olsalazine
Inflammation by:
CORTICOSTEROIDS IL, cytokine transcription
Prednisone AA metabolism (PLA2 inhibitor)
↑Lymphocyte apoptosis
Converted to active form 6-
THIOPURINES
mercaptopurine (purine analog):
Azathioprine
De novo purine synthesis
Mercaptopurine
↑T cell apoptosis
FOLIC ACID ANALOG Inhibits DHFR → dTMP →
Methotrexate DNA synthesis
Inhibits calcineurin →
Cyclosporin
T cell clonal expansion
Anti-TNFα antibody →
Infliximab
Potent Inflammation
INFLAMMATORY BOWEL DISEASE
U ce a e C &C D ea e
Uses
Mild symptoms (Active Outbreaks)
Maintain remission
Risk of Colorectal cancer
Moderate to severe symptoms &
relapses
Severe symptoms
(Active & Chronic)
Steroid sparing
Severe symptoms (relapsing/active)
Secondary use to ASAs, thiopurine
Severe symptoms (Active & Chronic)
Steroid sparing
Bridging (Temporary) therapy
Fistulizing, severe active symptoms
refractory to steroids/others
Side Effects/Contraindications Other
Nausea, headache Oral or Rectal prep
Epigastric pain, diarrhea
Hypersensitivity (Sulfa drug) Sulfasalazine contains
Caution renal impairment, sulfapyridine (anti-bacterial),
pregnancy, breast feeding activated by colonic flora
C g -like effects:
Acne, moon-face, sleep/mood
disturbance, indigestion,
hyperglycemia, cataracts,
osteoporosis, myopathy
Leukopenia monitor for infection Toxicity increased by
Myelosuppression allopurinol (xanthine oxidase
metabolized 6-MP)
GI side effects
Hepatotoxicity
Pneumonitis
Tremor, parasthesia
Malaise, headache
Abnormal LFT, aplastic anemia
Very powerful drug
Gingival hyperplasia, hirsutism
Nephrotoxicity, infections,
neurotoxicity (major)
Infusion reaction
Sepsis IV infusion every 4-6 weeks
TB reactivation
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 CONSTIPATION
MOA Uses Side Effects/Contraindications Other
BULK AGENTS (FIBER) Insoluble
↑Bowel volume content → activates
Psyllium, Bran Must take with lots of water Non-absorbable
stretch receptors → reflex peristalsis
Methylcellulose Non-digestible
OSMOTIC LAXATIVES Effective in 1-3 hrs
Draws fluid into bowel lumen→ ↑Bowel
Magnesium hydroxide Lactulose broken down into
volume → activates stretch receptors
Magnesium sulfate Purge intestines (surgery, acetic & lactic acid by gut
→ reflex peristalsis
Polyethylene glycol colonoscopy, poisoning) ↑Constipation (#1 cause) flora (can treat hepatic
Lactulose Hypokalemia encephalopathy by ↑NH4
Enemas = Sodium PO4/citrate
Sorbitol (Prunes) Diarrhea secretion)
STOOL SOFTENERS Dehydration
Aka Emollients
Docusate sodium
Lubricates stool Docusate = surfactant &
Liquid paraffin (oral)
stimulates
Glycerin (suppository)
IRRITANT/STIMULANT Irritate GI mucosa → draws water out
Castor oil, Senna into bowel lumen → Severe constipation
Effective in 6-8 hrs
Bisacodyl Lubiprostone (PGE1 analog) → opens (more rapid effects needed)
Lubiprostone Cl- channels → Cl- rich secretions
DIARRHEA
MOA Uses Side Effects/Contraindications Other
Contraindications:
Diarrhea >2-3 days Toxic material induced diarrhea
OPIOIDS Simulate opiate receptors in bowel →
Severe diarrhea in elderly/kids Microorganisms (Salmonella, E.coli) Loperamide 40-50x
Loperamide opens K+ channels, closes Ca2+
-Risk of dehydration Antibiotic assoc. diarrhea stronger than morphine but
Diphenoxylate channels → ACh release →
Chronic inflammatory disease Overdose: does not cross BBB
Morphine peristalsis → ↑time for water
Secretory diarrhea (Cholera, Paralytic ileus T ½ =11 hrs (long)
Codeine absorption
E.coli toxin mediated) CNS depression
Toxic megacolon (IBD)
ANTI-MICROBIALS Contraindications:
Stop offending Abx → Start new Abx Antibiotic associated diarrhea
Metronidazole Metro liver or renal impairment
→ kills C. difficile (C. difficile induced)
Vancomycin Vanco renal impairment
FLATULENCE
MOA Uses Side Effects/Contraindications Other
Detergent alters elasticity of mucus- Gas Limited data on effectiveness
ANTI-FLATULANTS
coated bubbles → size of gas bubbles In combo with loperamide for
Simethicone
→ bloating/pain diarrhea-induced gas

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 EMESIS
MOA Uses Side Effects/Contraindications Other
Emergent use only (>1 hr Drowsiness
Irritates gastric mucosa Vagus nerve
Syrup of Ipecac delay to the ER) with poison Diarrhea
stimulates CTZ
ingestion Stomach ache
Side Effects: Dry mouth, dizziness,
restlessness, dilated pupils,
M1 ANTAGONIST Inhibits mAChR in vestibular apparatus delirium, allergic reaction
Motion sickness
Scopolamine & CTZ Contraindications: kidney/liver dx,
enlarged prostate/bladder
problems, heart disease, glaucoma
H1/D2 ANTAGONISTS Side Effects: Blurred vision, dry
PHENOTHIAZINES mouth, dizziness, restlessness, Long-term Rx can cause
Promethazine (H1, D2) Inhibit both histamine & dopamine seizures extrapyramidal effects (low
Short-term (<2 months)
Metoclopramide (D2) receptors in the CTZ Contraindications: Allergy to D2 in substantia nigra):
Prochlorperazine (D2) (neuroleptic drugs) phenothiazines, glaucoma, liver dx, tardive dyskinesia
prostate/bladder problems
Side Effects: (Few) headache, Very safe & effective
5-HT3 ANTAGONISTS
Inhibits serotonin receptors in Chemo-induced nausea & constipation Oral or IV administration
Ondansetron
Brain (CTZ) & GIT (stomach) vomiting Rare: hiccups, itchiness, transient Antidote to cisplatin
Granisetron
blindness (chemo drug)