treatment approaches of PUD
eradicating H.P reducing gastric acid mucosal protective agents
quadruple therapy for PUD H.P
bismuth, metronidazole, tetracycline, PPi
triple therapy for PUD H.P
PPi, amoxicillin, clarithromycin
while quadruple therapy is first line, when is triple therapy preferred for PUD
low resistance/exposure to atb
endings of H2-r antagonists
"tidine"
______ was the first H2-r antagonist but use is limited due to SE + DD interactions
cimetidine
moa of H2-r antagonists
act selectively on H2 r in stomach, competitive antagonists + reversible
cli of h2-r antagonists
PUD, acute stress ulcers (IV), GERD
what drugs are preferred to h2-r antagonists
ppis
pharmacokinetics of H2-r antagonists
distribute widely (milk + placenta), excreted in urine
which h2-r antagonists are available iv and require dosage adjustments in renal dysfxn
cimetidine, ranitidine, famotidine
SE h2-r antagonists
only cimetidine -> endocrine (gynecomastia + galactorrhea), CNS (confusion)
_______ inhibits cytochrome p450 and can interfere w/ warfarin, phenytoin and clopidogrel
cimetidine
PPis bind to __________ and suppresses secretion of _______ into gastric lumen
H+/k+-ATPase enzyme system acids
ending of ppis
"prazole"
moa ppi
prodrugs w/ acid-resistant enteric coat -> removed in duodenum -> covalent bond w/ proton pump -> inhibits 90% acid secretion
an oral product containing ______ combined w/ _______ for faster absorption is available to decrease gastric acid secretion
omeprazole sodium bicarb
cli ppi
GERD, erosive esophagitis, active duodenal ulcers, Zollinger-Ellison, prevention NSAID + stress ulcers
pharmacokinetics of ppis
orally -> taken 30-60m before breakfast or largest meal of day, excreted in urine and feces
which ppis are available iv
esomeprazole, lansoprazole, pantoprazole
se ppis
omeprazole + esomeprazole decreases clopidogrel fractures, b12 + ca + mg deficiency, diarrhea + c. difficile colitis, pneumonia
cli prostaglandins
NSAID gastric ulcers
prostaglandins ending
"prostol"
CO misoprostol
pregnancy (uterine contractions)
SE PGs
diarrhea
_____ reduce gastric acidity + pepsin activity
antacids
when should antacids be taken
full stomach
2 antacids used
aluminum OH magnesium OH
cli antacids
symptoms of PUD, heartburn, GERD
SE antacids
aluminum OH - constipation magnesium OH - diarrhea
sucralfate
mucosal protective agent, aluminum OH + sucrose -> physical gel barrier
cli sucralfate
duodenal ulcers, prevention stress ulcers
why is sucralfate not used much
multiple daily dosing, DD interactions w/ PPis, H2 antagonists and antacids (needs acidic pH)
bismuth
mucosal protective agent w/ antimicrobial action + coats ulcer
which brainstem vomiting site is outside bbb
CTZ
_____ functions mainly in motion sickness
vestibular system
moa phenothiazines
block dopa r in CTZ
phenothiazines cli
emetogenic chemo drugs
__________ is a phenothiazine
prochlorperazine
ending 5-H53-r blockers
"setron"
moa 5-ht3-r blockers
block 5-ht3 r in periphery + CTZ
cli 5-ht3-r blockers
for CINV, administered as single dose before chemo
5-ht3 antagonists are metabolized by liver but only ________ need dosage requirements in hepatic insufficiency
ondansetron
SE 5-ht3-r blockers
only ondansetron + dolasetron = qt prolongation
the substituted benzamide, _______ is effective at high doses against chemo
metoclopramide
metoclopramide moa + SE
inhibition of dopa in CTZ -> extrapyramidal symptoms
metoclopramide cli
gastroparesis + CINV
moa butyrophenones
blocking dopa r
butyrophenones ending
"peridol" (droperidol + haloperidol)
cli droperidol
sedation in interventions (antiemetic)
why is droperidol last resort antiemetic
qt prolongation
benzodiazepines ending
"zepam" (lorazepam + alprazolam)
cli benzos
anticipatory vomiting
corticosteroids such as _______ are used alone for CINV
dexamethasone, methylprednisolone
substance p/neurokinin-1-r antagonists endings
"pitant"
substance P antagonists are used for _____ in combo w/ ______
delayed phase CINV dexamethasone + 5-ht3 antagonist
substance P antagonists undergo hepatic metabolism by
CYP4A4 (many DD interactions)
SE substance P antagonists
hiccups
antiemetic combo: corticosteroids are given with
metoclopramide, phenothiazine and butyrophenone/benzo
antiemetic combo: metoclopramides are given in combo with
antihistamines (reduced extrapyramidal) or corticosteroids (reduced diarrhea)
best antiemetic combo for delayed CINV
substance P antagonist + 5-HT3 antagonist + dexamethasone
classes of antidiarrheal drugs
antimotility agents, adsorbents, drugs modifying fluid and electrolyte transport
2 antimotility agents
diphenoxylate + loperamide
moa of antimotility agents (diphenoxylate, loperamide)
opioid-like actions, activated presynaptic opioid receptors in enteric n system -> Ach inhibited -> less peristalsis
loperamide cli
acute + traveler's diarrhea
CO antimotility agent (diphenoxylate + loperamide)
children or colitis
adsorbents for diarrhea
aluminum hydroxide + methylcellulose
moa adsorbents
adsorb toxins/organisms + coat mucosa
bismuth cli for diarrhea
traveler's diarhea
SE bismuth
black tongue + stool
stimulant laxatives
senna and bisacodyl
opioid-induced constipation drug combo
senna + docusate
bisacodyl pharmokinetics
suppository or enteric-coated tablet, acts directly on n
irritant laxative
castor oil
CO castor oil
pregnancy (uterine contractions)
bulk laxatives
methylcellulose
psyllium adverse efect
reduce drug absorption (for 2h)
saline laxatives
magnesium citrate + OH
saline laxatives (magnesium citrate + OH) moa
hold water in intestines
PEG cli
colonic lavage for interventions
lactulose
osmotic laxative
cli lactulose
hepatic encephalopathy + constipation
stool softeners
docusate (Na + Ca)
cli docusate
prophylactic constipation
CO stool softeners
mineral oil
lubricant laxatives
mineral oil + glycerin suppositories
how should mineral oil be taken
upright position
Cl- channel activator
lubiprostone
moa lubiprostone
activates Cl- channels to increase fluid secretion in lumen
cli lubiprostone
chronic constipation + IBS-C
IBD mild/moderation symptoms treatment
aminosalicylates/corticosteroids
IBD chronic symptoms treatment
thiopurines, methotrexate, cyclosporin
_______ is an atb infusion for IBD
infliximab