GI Flashcards
esomeprazole, omeprazole, inasoprazole, dexlansoprazole, pantoprazole, rabeprazole
PPI
- Benzimidazole compounds irreversibly inhibit parietal cell proton pump (H/K ATPase)
- The inhibition persists after stoping the drug (because its an irreversible inhibitor) - have to wait for new pumps to be made
- They are pro drugs that are inactive at neutral pH (need acid to be active)
- Take with meals = food -> more gastric secretion
- These drugs are unstable at low pH - enteric coating (only disolves in alkaline pH) to get past stomach - absorbed in intestines -> carried in circulation to parietal cells where it acts
- The drug acts at the intracellular canaliculi which is upstream from the proton pump (this is how it stays chornically active even when it shuts down gastric acid secretion ) (it still needs acidic envionrment to work)
- Drugs
- Esomeprazole, omeprazole, lansoprazole, dexlansoprazole, pantroprazole, rabeprazole
- Curretnly the most effective drugs for suppressing gastric acid secretion because gastric response to all stimuli is inhibited\
- Can give a single daily dose
- AE
- GI effects (nausea, colic, flatulence, constipation, diarrhea)
- CNS effects (headaches, dizziness, somnolence)
- Skin rashes
- With prolonged use diarrhea often occurs due to GIT bacterial overgrowth from removal of natural acid barrier
- Hypergastrinemia can happen
- Hepatic metabolism with negligible renal clearance
- Uses
- Promote peptic ulcer healing and prevent recurrence
- Effective in patienst unresponsive to H2 antagonists
- More effective than H2 antagonists for GERD or NSAID induced peptic ulcers
cimetidine, famotidine, nizatidine, ranitidine
H2 receptor antagonists
- All are over the counter structural histamine analogs -> block H2 receptors selectivlty to reduce gastric acid and pepsin secretion
- Doesn’t affect H/K ATPase, H1 or any other receptors
- Best at inhibiting nocturnal secretion (largely driven by histamine)
- AE
- Diarrhea, headaches, fatigue, myalgias, constipation, bradycardia
- Don’t give to pregannt women or nursing women - they can cross placenta and get into milk
- Mental changes: confusion, hallucinations and agitation may occur with IV administration in patents who are old or have renal or hepatic dysfunction
- Cimetidine can cuase gynecomastia or impotence in men
- Cimetidine inhibits dihydrotestosterone to androgen receptors
- Can also interfere with CYP 450 pathways for other drugs
- They stop formation of protons at the canaliculi of parietal cells = less activation of PPDs
- Uses
- All equally effective for healing and preventing recurrence of PUD
- Given once a day at bed time
- We have better drugs so they are used less now
- Can be combined with antibiotics and bismuth for treatment of H pylori
aluminum hydroxide
antacid
- Aluminum hydroxide, calcium carbonate, combination aluminum hydroxide and magnesium hydroxide
- AE
- Aluminum hydroxide - produces constipation
*
- Aluminum hydroxide - produces constipation
magnesium hydroxide
antacid
produces diarrhea
calcium carbonate
tums and others - antacids
doesnt really cuase constipation or diarrhea
combination aluminum hydroxide and magnesium hydroxide
antacid
aluminum cuases constipation and the magnesium cuases diarrhea - put them together - they cancel eachother out
sucralfate
mucosal protective agent
- Binds selectively to necrotic ulcer tissue and acts as a barier
- Polymerizes to produce a viscous gel that adheres to the epi cells
- Effective in healing duodenal ulcers
- AE
- Constipation = most common
- Requires acidic pH for activation - don’t give with antacids, H2 antagonists or PPIs
misoprostol
mucosal protective agent
- Misoprostol - Methyl analog of PGE1
- Binds to PG receptors on parietal cells to inhibit acid secretion
- NSAIDs inhibit production of PG - but you can replace the PG in the stomach to stop the ulcers from forming
- Use
- Prevent NSAIDs ulcers from forming
- AE
- Diarrhea and abdominal pain
- May cause abortion by stimulating uterine contractions
- Binds to PG receptors on parietal cells to inhibit acid secretion
bismuth subsalicylate
peto-bismol
- Bismuth subsalicylate (pepto bismol) - colloidal bismuth
- Protective coating of ulcers - precipitates out in the stomach forming a lining on the stomach
- The precipitate is black - can turn your tongue black
- Antibacteiral agaisnt H pylori
- Protective coating of ulcers - precipitates out in the stomach forming a lining on the stomach
how to treat H pylori
clarithromycin
amoxicillin
PPI
glycerin
osmotic laxatives - saline laxatives - nondigestible sugars and alcohols
- Glycerin -
- Trihydroxy alcohol that acts as a lubricant and osmotic agent
- Lactulose, sorbitol, mannitol - non absorbable sugars
- Saline laxatives - non absorbable salts containing magnesium cations (mag citrate) or phosphate anions (sodium phosphate)
- Have a very bitter taste - people commonly add to fuit juices
- Avoid in patients with
- Renal insufficiency - theses patients already have issues with water balance
- Heart disease
- Electrolyte imbalance
- Diuretic drug co treatment
lactulose
osmotic laxatives - saline laxatives - nondigestible sugars and alcohols
sorbitol
osmotic laxatives - saline laxatives - nondigestible sugars and alcohols
minnitol-polyethylene glycol
osmotic laxatives - saline laxatives - nondigestible sugars and alcohols
(PEG) - electrolyte solutions
- Poorly absorbed and retain added water by osmotic pressure
- Mixtures of: sodium sulfate, sodium bicarbonate, sodium chloride, potassium chloride in isotonic solution
- Used in colonoscopy preparation - drink 3-4 liters over 3-4 hours to produce watery diarrhea and remove solid wastes
bisacodyl
stimulant or irritant laxatives
- Bisacodyl
- Enteric coated tablets taken at bedtime to take effect next morning
- Don’t chew = break the capsule
- Enteric coated tablets taken at bedtime to take effect next morning
cascara sagrada
stimulant or irritant laxatives
- Anthraquinones like: aloe, cascara sagrada, or senna
- Poorly absorbed in small intestine and require activation in the colon (laxative effects 6-12 hours later)
- Long term use can cuase melanomic pigmentation of colonic mucosa and cathartic colon (colon dilated and ahaustral)
senna
stimulant or irritant laxatives
- Anthraquinones like: aloe, cascara sagrada, or senna
- Poorly absorbed in small intestine and require activation in the colon (laxative effects 6-12 hours later)
- Long term use can cuase melanomic pigmentation of colonic mucosa and cathartic colon (colon dilated and ahaustral)
ricinoleic acid
stimulant or irritant laxatives (castor oil)
- Local irritant -> increases intestinal secretion and motility
- Now seldom used due to unpleasant taste and toxic potential
methylcellulose
bulk forming laxatives
contain lots of soluble fiber and other stuff to give you more material in feces
Methylcellulose, lactulose and polycarbophil
Still have to keep hydrated - need water to move everything along
lactulose
bulk forming laxatives
contain lots of soluble fiber and other stuff to give you more material in feces
Methylcellulose, lactulose and polycarbophil
Still have to keep hydrated - need water to move everything along
polycarbophil
bulk forming laxatives
contain lots of soluble fiber and other stuff to give you more material in feces
Methylcellulose, lactulose and polycarbophil
Still have to keep hydrated - need water to move everything along