drugs gi Flashcards
buspirone
5HT1A receptor agonist - inhibits 5HT release and increases NO release
improves fundic and pyloric accomodation
metroclopramide (reglan)
5 HT4 agonist & dopamine antagonist
improves gastric emptying and is antiemetic
dicyclomine & hyoscyamine
anticholinergics that slow gastric empyting
octretoide
somatostatin analog that inhibits 5HT & motilin release
lubriprostone
laxactive (for constipation) that activates Cl- channelf or increased Cl- secretion & water follows
tagaserod
relieves constipation as 5HT4 partial agonist
ondanstron (zofran)
antiemetic - 5HT3 antagonist
dronabinol
antiemetic that has effects of pot
5PDE antagonist
reduce strength of esophageal contractions
cimetidine
competitive antagonist of H2 receptor
rapidly absorbed and quick onset of action
hepatic metab by p450
renal excretion
continuous dosing - keeps gastic pH > 4 –> inactivates pepsin
used for PUD
*most important one to know - GERD!!
potently binds p450 sytem –> can cause significant drug interactions (warfarin, phenytoin, thephylline and diazepam –> levels are increased)
ranitidine
competitive antagonist of H2 receptor
rapidly absorbed and quick onset of action
hepatic metab by p450
renal excretion
continuous dosing - keeps gastic pH > 4 –> inactivates pepsin
**Most important for GERD
used for PUD
nizatidine
competitive antagonist of H2 receptor
rapidly absorbed and quick onset of action
hepatic metab by p450
renal excretion
continuous dosing - keeps gastic pH > 4 –> inactivates pepsin
used for PUD
famotidine
competitive antagonist of H2 receptor
rapidly absorbed and quick onset of action
hepatic metab by p450
renal excretion
continuous dosing - keeps gastic pH > 4 –> inactivates pepsin
used for PUD
omeprazole, lansoprazole, rebprazole, pantoprazole, esomeprazole
PPIs –> irrrevesibly block the H+/K+/ ATPase final common pathway –> reduces secretion by parietal cells into the lumen
intentionally delivered as prodrugs
when delivered to parietal cell –> protonated, concentrated and sulphonated
tums & oscal
calcium carbonate that neutralize stomach acid
may cause rebound acid secretion, nephrocalcinosis or milk alkali syndrome
regimes used to get rid of H. pylori
clarithromycin, amoxicillin & PPI
clarithromycin, metronidazole, PPI
levofloxin, metronidazole and PPI
misoprostol
PGE2 anaology – prevention of GUI in pt taking NSAIDs
use limited by bloating.diarrhea
abortifacient
sucralfate
complex salt of sucrose sulfate and ALOH3–> binds to mucosa and acts within lumen
stimulates mucus and bicarb and PGE2 production
binds to areas of health mucosa and ulceration
has no effect on acid production and is NOT absorbed
metoclopramide & domperidone (w/drawn b/c SE)
dopamine antagonist used as prokinetics for gastroparesis
D2 antagonist
also antiemetic
erythromycin
motilin agoinst used for gastroparesis
interacts with CYP-3A inhibitors
5-aminoasalicylates
tx of UC
inhibit T cell proliferation, Ag presentation & adhesion & descrease TNF production
SE: diarrhead, interstitial nephritis
busedonide
non systemic glucocorticoid - ileal release - used for CD
inhibit pro-inflammatory cytokines, adhesion molecules, leuktrienes
inhibit protease
regulated NF-kapa beta
decreased phagocytosis for neutrophiles
apoptosis of lympoctes
high degree of first pass metab in liver –> lessened systemic efects
induces remission in CD
thiopurines - AZA & 6-MP (AZA must be converted to 6MP)
inhibits DNA synthesis, induction of apoptosis & inhibition of purine synthesis - immunomodulator used for CD–> Induction & maintenance of remission
must monitor if someone has TPMT mutation –> bone marrow suppresion
take months to begin to work
methotrexate
folate antagonist, inhibits interleukins
induction and maintenance of remission in CD (being evaluated for UC)
increases risk for pneumonitis - if SOB/cough –> STOP DRUG
anti-TNF therapy
inflizimab, adalimumab, certolizumab
bind solube and cell bound TNF-alpha –> induce T cell/lymphocyte apoptosis
an ddecrease IL-1,6,18 and INF gamma
all three for CD, certolizumab not for UC
natalizumab
anti-alpha 4 integrin inhibitor –> used in CD
blocks integrins and thus adhesion of leukocytes
increases risk for PML via reactivation of JC virus
tenofovir
tx hep B - polymerase inhibitor
entecavir
tx hep B - polymerase inhibitor