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58 Cards in this Set

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  • Back
How to PPI's get to the parietal cells?
They are absorbed into the intestines and move directly to the site of action
True/False: PPI's block both active and inactive pumps.
When should PPI's be administered? Why is this important? How long do they take to have an effect and how long does their effect last?
An hour before food is consumed--this is because the pumps are turned on by eating..maximal effect is attained by taking 1 hr before
Effect lasts up to 24 hours because new pumps must be made and it may take up to 3 days to take effect because it only affects active pumps
What interaction is a concern with PPI's? Therefore?
Omeprazole inhibits the metabolism of clopidigrel to its active form and the increase in gastric pH might reduce the absorption of clopidigrel
If you have a patient with a high risk for GI bleed--these are high risk patients for whom you would use something OTHER THAN OMEPRAZOLE LIKE ESOMEPRAZOLE OR PANTOPRAZOLE
For other patients--maybe use an H2 receptor antagonist or antacid instead of the PPI
What are some examples of H2 antagonists?
Cimetidine, ranitidine, famotidine, nizatidine
Tagament, Zantac, Pepcid, and Axid
How are H2 antagonists excreted?
Renal excreted so you have to adjust for renal patients
What interactions are of concern with cimetidine? Which drug has fewer relative interactions?
Warfarin and amniodarone
Will increase the amounts of both
Ranitidine has fewer reactions and Nizatidine only inhibits CYP3A4 weakly
Famotidine is the BEST with the LEAST interactions
Which H2 antagonist is known to be the safest with respect to drug interactions?
Famotidine--it has no effect on the CYP450
What is misoprostol's(cytotec) mechanism of action? What is it therefore used for?
Prostaglandin analogue--bind to receptor on parietal cells to stimulate Gi pathway and decrease cAMP which decreases gastric acid secretion
Prevent gastric injury by stimulation of mucin and bicarb secretion and INCREASED MUCOSAL BLOOD FLOW
What are the two mechanisms for NSAID toxicity?
The are absorbed across the gastric mucosa due to not being ionized at the pH found in the stomach
COX-1 is expressed in most tissues including the GI mucosa and NSAID's cause reversible COX-1 inhibition and this decreases PG activity leading to GI mucosal damage
How do 5-HT3 receptor antagonists work?
Blocks the serotonin 5HT3 receptors that are found centrally in the chemoreceptor trigger zone and peripherally at vagal nerve terminals in the intestines
They are used to treat chemo and post-op related vomiting
What is metoclopramide?
Dopamine receptor antagonist that also blocks serotonin receptors in the chemoreceptor trigger zone of the CNS
It is useful with nausea and vomiting associated with decreased gastric motility
Increases lower esophageal sphincter tone, aids gastric emptying
True/False: Fewer side effects are noted with meclizine.
TRUE--this antihistamine does not cross the blood brain barrier and so its ASE's are less
Where are aminosalicylates first absorbed?
In the small intestine and than it is carried in the bile to the colon where it is metabolized by bacteria into the active form
What prevents the sulfasalazine from being absorbed in the stomach?
The azo linkage
What are the two groups of aminosalicylates?
Prodrugs and coated drugs
What are some ASE's of aminosalicylates?
Antacids, H2RA's, and PPI's
How should corticosteroids be administered for GI diseases?
Taper to lowest effective dose--longer taper than other therapies
When should hydrocortisone based products be used in the GI system?
Distal disease/colorectal problems
What is a good drug to use for ileal disease?
Why should 6-TG levels be checked?
For thiopurine metabolism--high levels of 6TG will cause bone marrow suppression
What are some major drug interactions for thiopurines?
allopurinol(inhibits xanthine oxidase)
What are some ASE's associated with Natalizumab?
risk of progressive multifocal leukoencephalopathy and rarely fatal demyelinating disease of the CNS
What are some problematic ASE's of methotrexate?
Leukopenia, renal failure, SJS, pharyngitis, HTN
What are some drug interactions of methotrexate?
Bactrim or drugs interfering with folate metabolism
Nephrotoxic drugs(NSAID's)
What is special about the structure of oral vancomycin?
It is not absorbed systemically and can therefore selectively battle against C. diff
What is the first line therapy for non-severe C. diff? Severe?
Oral vancomycin
Headache and B12 deficiency
Hip factures
C. diff because altering pH
How can tolerance develop with H2 blockers?
Effect of secondary hypergastrinemia to stimulate histamine release from ECL cells via alternative pathways
True/False: PPI's are technically prodrugs
TRUE--designed to get past gastric lumen and be absorbed in the SI
True/False: PPI bioavailability is increased by food in the stomach
FALSE--it is decreased by 50% so administer 1 hr before eating
True/False: H2 receptor antagonists work like PPI's in that they are irreversible
As a drug class, what drugs interactions are generally seen with H2 antagonists?
Altering the pH of the stomach alters the absorption of drugs that require a low pH to become activated
What are the three acid neutralizing agents?
Sodium bicarb, calcium carbonate, and magnesium hydroxide
Sodium bicarb
Antacid that isn't used much because of its alkali and sodium load risk for heart/renal failure patients and its affect on systemic acid-base balance
Calcium carbonate
Antacid that may induce more acid rebound secretion and so requires more frequent administration--CO2 may cause gas
Magnesium/Aluminum Hydroxide
Antacid--use CAUTION with renal insufficiency patients
Poorly absorbed so extended action
Antacids cause ________ absorption of weakly acidic drugs.
Antacids cause decreased absorption of weakly acidic drugs and vice versa for weakly basic dugs
What are antacids notorious for binding and preventing effectivity?
TETRACYCLINES AND FLOUROQUINOLONES--give antacids separate from antibiotics
Misoprostol ASE's and Interactions
ASE's--diarrhea, abdominal pain
Interactions--should not be given with anything that causes uterine contraction DON'T GIVE TO PREGNANT WOMEN CAUSE IT CAUSES ABORTION
What drug should never be given to pregnant women?
Sucralfate MOA
Reacts with HCl in the stomach to mach an acid buffer paste that adheres to active ulcers
Sucralfate ASE's
Constipation and aluminum absorption
Sucralfate Interactions
ALUMINUM--binds to other drugs so give separate
Also aluminum can cause severe renal impairment
True/False: Selective COX-2 inhibitors eliminate ulcer risk
FALSE--try to use selectives and non-selectives with increased Cox2 effect but they don't eliminate risk entirely
What is standard 1st line therapy for H. pylori infection?
A PPI AND Clarithromycin and amoxicillin OR metronidazole
Onandsetron, Granisetron, Palonosetron, and Dolasetron are all what?
5-HT3 receptor antagonists
What are some ASE's for 5-HT3 receptor antagonists?
Heacache, constripation, and QT PROLONGATION
Who get metoclopramide?
Patients with gastric emptying issues like diabetics
Chronic use of metoclopramide has been associated with what?
tardive dyskinesia
Antidopaminergics: Phenotheazines
Useful in patients with nausea and vomiting
Can induce sedation--limits their use
SEVERE TISSUE INJURY AND GANGRENE WITH IV ADMINISTRATION--give IM due to risk of tissue injury(subQ and intra-arterial have high risks)
What are prochlorperazine and promethazine?
Phenotheazines/Antidopaminergics/Anti-Nausea agents
What are some common antihistamines?
Cyclizine, hydroxyzine, diphenhydramine, and meclizine
Antihistamine ASE's
Antihistamine MOA
Act on vestibular afferents of the brain stem
H1 antagonists--good for motion sickness of inner ear
Work on NTS
Prevention and treatment of motion sickness
Antagonizes ACh at anti-muscarinic receptors
As an antiemetic, scopolamine probably blocks neural pathways from the vestibular nuclei in the inner ear to the brain stem and from the reticular formation to the vomiting center
Aprepitant and Fosaprepitant(EMENT)
Substance P receptor antagonists(NK1 receptor antagonists)
Used to increase efficacy of standard anti-emetics with chemo
Interactions: Metabolized by CYP3A4 so may inhibit metabolism of other drugs; levels increased with clarithromycin or ritonavir
Makes you kinda crazy