M.

10B DRUGS USED IN GASTROINTESTINAL DISORDERS

Dr. W. Antonio | March 26, 2018

DRUGS FOR ACID PEPTIC DISEASE

General MOA Pharmacokinetics (PK)
Weak bases that react with 1-3 hrs pc + bedtime
gastric HCL to form salt and severe/uncontrolled: q30min-1hr
ANTACIDS water
Reduce drug absorption
Alter drug solubility
MOA ADR
Reacts with HCl to produce bloatedness, belching, metabolic alkalosis
Sodium Bicarbonate carbon dioxide and sodium
chloride.
React slowly with HCl to Bloatedness, belching, abdominal distention (due to CO2) and hypercalcemia (due to
Calcium Carbonate form carbon dioxide and CaCl2), Milk-alkali syndrome
calcium chloride
React slowly with HCl to Diarrhea - Unabsorbed magnesium salts may cause osmotic diarrhea. MAGtatae
Magnesium Hydroxide or form magnesium chloride Constipation - aluminium salts may cause constipation. ALa tae
Aluminum hydroxide or aluminium chloride and
water
MOA PK Clinical uses ADR
Block histamine release Given TID Acute duodenal ulcers Diarrhea, HA, fatigue, myalgias,
from ECL cells Metabolized in the liver, Prev’n of stress- constipation(<3%)
H2-RECEPTOR
Blocks the stimulation of Excreted renally related bleeding Increased risk of nosocomial
ANTAGONISTS
the H+ K+ ATPase or your IV H2RA > IV PPI Non-ulcer dyspepsia pneumonia in critically ill patients;
(Cimetidine, Ranitidine,
proton pump. Compete with GERD Blockade of cardiac H2Receptor;
Nizatidine, Famotidine)
Decrease nocturnal release Creatinine & other PUD bradycardia, hypotension
of acid drugs for renal tubular
secretion
Inhibits CYP 450 Confusion, hallucinations, agitations.
Inhibit gastric FPE of Reversible Gynecomastia/impotence
***Cimetidine Alcohol ! Inc ROH Galactorrhea
levels (also Ranitidine
& Nizatidine)
PROTON PUMP MOA PK Clinical Use ADR
INHIBITORS Covalently bind and Bioavailability is 1. GERD Diarrhea, headache and abdominal
(Omeprazole, Esomeprazole, irreversibly inhibit decreased - Empiric treatment or pain(1-5%)
Lansoprazole, Pantoprazole, H+K+ATPase system / approximately 50% by therapeutic trial Acute Interstitial Nephritis
Rabeprazole, Proton Pump food A. Non-erosive reflux Safety during pregnancy not
Dexlansoprazole) disease established
PPIs will not act on -intermittent or “on Vitamin B12 deficiency
proton pumps that are demand” treatment Hypocalcemia( Inc. Risk of hip
not active(1 hour B. Erosive reflux fracture)
before meals. Usually disease Hypomagnesia
breakfast) - Long term daily Inc. Risk of both community aquired
maintenance(6 respiratory infections and nosocomial
Serum t1/2: 1.5 hours weeks) pneumonia
B1. Esophageal(Peptic 2 to 3 fold increased risk for hospital
Acid Inhibition: up to Stricture or Barrett’s and community acquired C. dificile
24 hours(May be given esophagus) infection
OD) -Long term daily Increased risk of other enteric
maintence infections: Salmonella, Shigella,
rapid first-pass and B2. EXTRAesophageal E.coli, Campylobacter
systemic hepatic - Sustained acid
metabolism suppression(BID for DRUG INTRXN
at least 3 months) Alter absorption of drugs for which
Negligible renal intragastric acidity affects drug
clearance 2. Peptic Ulcer bioavailability:
Disease 1. Ketoconazole
Only give IV - Duodenal Ulcers: 2. Itraconazole
preparation if the oral PPIs for 4 weeks 3. Digoxin
route is -Gastric Ulcers: PPIs 4. Atazanavir
CONTRAINDICATED for 6-8 weeks

Cheap: Oral>IV PPI

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IDEAL DRUGS 3. H.pylori-associated Esomeprazole: decreases diazepam

1. Short serum half-life ulcers metabolism
2. Concentrated and - PPI BID +
activated near their site Clarithromycin 500mg Lansoprazole: enhances theophylline
of action BID and Amoxicillin clearance
3. Long duration of 1g BID or
action Metronidazole 500mg
BD
PPI vs H2 antagonist:
PPIs inhibit 90-98% of 4. NSAID-associated
24 hour acid secretion. ulcers
Most potent drug that -Tx of Ulcers: H2RAs
inhibits acid production. or PPI

Clopidogrel + PPI = Clopidogrel+PPI

cardiovascular events. • can use: Pantoprazole,
Better PPI options: rabeprazole, lansoprazole.
Pantoprazole and • except: Omeprazole and
Lameprazole Esomeprazole
• increased risk of GI Bleeding
5. Prevention of re- • Chronic gastroesophageal reflux
bleeding from peptic or PUD
ulcers • Increased incidence of MI
-Initial: 80mg bolus
administration
esomeprazole or
pantoprazole then
maintain constant
infusion (8mg/h)

6. Prevention of
Stress-related
mucosal bleeding
-Omeprazole+
naHCO3: BID initially
then OD thru NG
tube; patients w/o NG
tube or with
significant ileus: IV
H2RAs>PPI
-Gastrinoma: High
dose omeprazole
60mg or 120mg/day

Delayed release
formulation of
Lansoprazole

Longer T max and

greater area under the
Dexlansoprazole
curve

Comparable to other
agents in the ability to
supppress acid
secretion
SUCRALFATE MOA Dosage Indications Adverse Effects
Unclear 1g QID on an empty 1. prevention of Constipation(2%)
stomach at least 1 hour stress-related May impair absorption of
Coats gastric mucoa; forms before meals bleeding medications
a physical barrier; it acts as
mucous bicarbonate layer 2. Reason for choice
over H2RAs/PPIs:
Prevents further ulceration Because of fear for
or hasten healing of ulcers the devlopment of
nosocomial infections
Stimulates mucosal when using H2RAs
prostaglandin and and PPIs
bicarbonate secretion

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MISOPROSTOL MOA Adverse effects Uses

BISMUTH COMPOUNDS
Bismuth Subsalicylate
Stimulates mucus and Diarrhea and cramping Approved for prevention of NSAID-induced ulcers in high risk
bicarbonate secretion abdominal pain patients
Enhances mucosal blood
flow No signigicant Induce uterine contraction
interactions reported
MOA
Unkown
Coat ulcers and erosions, creating a protective layer against acid and pepsin
Stimulate prostaglandin, mucus, and bicarbonate secretion
Reduces stool frequency and liquidity in acute infectious diarrhea
Direct antimicrobial effects and binds enterotoxins
Direct antimicrobial activity against H.pylori
LAXATIVES

TYPES MOA EXAMPLES

Fibers increase the bulk of stool by absorbing water thereby, causing distension & stimulate Methyl cellulose,
Bulk forming proximal contraction and distal relaxation of the bowel wall. Psyllium(C-lium),
Increases peristalsis Polycarbophil
Advice patient to drink lots of water, also to prevent obstruction.
Prevents reabsorption of water ! water goes to stool, mas malambot Docusate,
Stool softeners
glycerin,
mineral oil
Forms a non-absorbable solution ! increases fluid in intestines ! increase fluidity of stools ! Lactulose,
watery stools Magnesium oxide,
sorbitol,
Osmotic
Fluids will not be absorbed kaya “liquidy” ung stools mo. lactulose,
magnesium citrate,
sodium phosphate,
polyethylene glycol
Stimulates the enteric nervous system ! increase contraction of intestines Aloe,
SE: Abdominal cramps senna,
Stimulant cascara,
Can be carcinogenic, causes melanosis coli (darkening of intestines) castor oil,
bisacodyl
Chloride channel Stimulates type 2 Cl- channel in the small intestines 4 increase fluid secretion ! increases fluidity Lubiprostone
activator of stool

Opioid receptor Opioids may cause constipation Methylnaltrexone,

agonists Alvimopan (for Post-op
ileus)

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