GI Drugs Flashcards
Drugs acting on the GI system fall into what 5 categories?
Appetite stimulant Inducer/suppressor of emesis Anti-ulcer Increase/decrease GI motility Pancreas and liver
Where is the appetite and satiety center?
Hypothalamus
What are endogenous inhibitors of appetite?
Serotonin
Cholecystokinin
Glucagon-like peptide
Leptin
What are endogenous stimulants of appetite ?
GABA
Ghrelin
Dopamine
Norepinephrine
How does GABA stimulate appetite
By inhibiting the satiety center
What GABA agonists can be used to simulate appetite?
Benzodiazepine (Diazepam, midazolam)
Propofol
What species are benzodiazepines more useful for stimulating appetite?
Cats
What is the most common side effect of benzodiazepines as a appetite stimulant?
Sedation
How do I administer diazepam and midazolam ?
Diazepam -IV
Midazolam -IV or IM
What benzodiazepine can be given PO to cats?
Oxazepam
NOT diazepam-> hepatotoxicity
What drug is an agonist at the ghrelin receptor?
Capromorelin -> increases appetite
Capormorelin is labeled for _______
Dog
What is the MOA of cyproheptadine and mirtazapine?
Serotonin and histamine antagonist -> inhibit satiety center by blocking 5-HT receptor
What is the most common side effect of cyproheptadine?
Sedation
Cyproheptadine is more effective in __________ and mirtazapine is more effective in _________
Cat;dog
T/F: Cats have more A2 and 5-HT receptors than dogs, but have fewer D2 and H1
True
What peripheral emetic works by directly irritating the oropharynx/GI lining
Hydrogen peroxide 3%
Why can hydrogen peroxide not be used as an emetic in cats?
Hemorrhagic gastritis
What is the MOA of apomorphine ?
stimulates D2 receptors -> emesis
Oops.. i have accidentally overdosed a dog with apomorphine? What should i do?
Overdose can cause respiratory depression -> reverse with naloxone
What is my emetic of choice in the cats? What is the MOA?
Xylazine or Dexmedatomidine
A2-agonist (cats have more A2 receptors than dogs)
What are the 3 most common emetics?
Maroptiant
Metoclopramide
Ondasetron
What is the MOA of maropitant citrate?
NK1 receptor -> block substance P and reduces its contribution to vomiting (central at CRTZ and peripherally at GI tract)
What is the purpose of substance P
Integration of pain, stress, anxiety, and vomiting
What are precautions to using maropitant
Injection stings
Bone marrow suppression with high doses in young dogs
What is the MOA of metoclopramide?
Dopamine antagonist (also 5-HT) -> inhibit vomiting at CRTZ
Higher doses prokinetic
What is the MOA of ondasetron ?
Serotonin (5-HT) antagonist centrally and peripherally -> inhibit vomiting at CRTZ and in GI tract
What two anti-emetics have activity both centrally and peripherally
Maropitant
Ondasetron
How is ondasetron usually administer?
injection
There is an oral formulation available
What drug is labeled for motion sickness in dogs, and acute treatment of vomiting in dogs and cats?
Maropitant
Antihistamines “H2” blockers are used to treat what?
Gastric ulcer
What are the Antihistamine “H2” blockers?
Cimetidine
Famotidine
Ranitidine
What is the MOA of cimetidine, famodtinide, and ranitidine?
Competitively inhibit H2 in the stomach -> gastric acid and pepsin secretion inhibited
What is the most potent and longest acting H2 blocker?
Famodtidine
What H2 blocker may have prokinetic effects?
Ranitidine
What H2 blocker inhibits P450 enzymes?
Cimetidine
Where are the H2 blockers metabolized
Cimetidine and Ranitidine - liver
Famotidine -unchanged excreted in urine
What is the MOA of proton pump inhibitors and what drug is commonly used?
Irreversibly inhibit H/K/ATPase proton pump resulting in decreased HCl production
Omeprazole
How is omeprazole administered?
Oral ONLY
What drug has the greatest effect on increasing grastic pH?
Omeprazole (proton pump inhibitor)
More potent than H2 blockers
What is a precaution of omeprazole?
Can inhibit p450 enzyme
What is mioprostol? What are its main actions?
Prostaglandin E analog
Direct decrease in acid production
Increase mucus and sodium bicarbonate secretion
Stimulate epithelializaiton of the mucosa
Stimulate mucosal blood flow
=> ulcer healing
What is a precaution to misoprostol?
Can stimulate uterine contractions (abortion)
Diarrhea
What drug is most appropriate to react NSAID- induced gastric ulcers?
Misoprostol
What is the MOA of sucralfate?
Bind to ulcer site and protect against damage from acid, pepsin, and bile
->protective coating lasting up to 6 hrs
May also stimulate protective PGs and antioxidants and increase mucosal blood flow
How is sucralfate administered ?
Orally- local action only
Should you administer concurrent oral therapies before or after sucralfate
Before
Can bind/inhibit absorption of other drugs
What are the oral antacids and how do they reduce ulcers?
Aluminum, magnesium, and calcium salts
Chemically neutralize HCl
What will bind phosphorus in the gut and may reduce absorption of other drugs
Oral antacids
For the GI tract, if the motility is decreased, the transit time will be ____________
Increased
What endogenous molecules will cause an increased GI motility
ACh (PSNS)
Serotonin
Peptides
What endogenous molecules will cause decreased GI motility?
Norepi
Dopamine
Endorphins (opioid)
What drugs INCREASE GI motility?
Serotonin agonist
- cisapride
- mosapride
Dopamine antagonist
- metoclopramide
- domperidone
What is the MOA of cisapride ?
Serotonin agonsit -> prokinetic
What do I use to treat megacolon and constipation in cats?
Cisapride
What drugs DECREASE GI motility?
Anticholinergics
- aminopentamide
- atropine/gycopyrrolate
Opioid
-loperamide and diphenoxylate
What are GI protectants/absorbents?
Magnesium/aluminum products
Bismuth subsalicylate
Activated charcoal
What do you call mechanical lubricants line mineral oil or laxatone?
Emollient laxatives
What kind of drug stimulates movement by building up pressure in the intestine by absorbing water from the lumen?
Simple bulk laxatives
What drug will osmotically draw fluid into the GI lumen to improve motility
Osmotic cathartic
What irritates the GI mucosa to stimulate motility and secretions
Irritant Catharine
Who do you not give a phosphate enema to ?
Cats -> toxic
What drug to you used to manage hepatic encephalopathy?
Lactulose
How is lactulose administered?
Orally
Acute situation -> enema
What is the MOA of lactulose?
Ion trap ammonia in the colonic lumen to enhance removal from the body
What drug do I chose for chronic inflammatory over disease in small animals ?
Ursodiol
What is the MOA of ursodiol?
Bile salt-> choleretic (increase bile flow)
When is ursodiol contraindicated
Biliary obstruction
What do I use to treat exocrine pancreatic insufficiency (EPI)?
Pancrelipase (enzyme replacement therapy)
What are the products that can be used to treat exocrine pancreatic insufficiency
Viokase, Pancrezyme, raw pancreas
Viokase has more enzyme and better efficacy than pancrezyme
Raw pancreas is cheap but inconsistent
How is pancreatic enzyme replacement therapy administered?
Orally with meal
What can you give patients concurrently to improve efficacy of pancreatic enzyme replacement therapies ?
Famotidine
-> H2 blocker -> decreased acidity and pepsin in stomach -> less breakdown of the therapy