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GI
GI drugs
90
Pharmacology
Graduate
02/01/2012

Additional Pharmacology Flashcards

 


 

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Term
Antidiarrheal
opiod agonists
Definition
significant constipating FX. inhibits presynaptic cholinergics -> decrease colonic mvmt
-> increase transit time thus increasing reabsorption of fluid

Diphenoxylate and Loperamide(doesn't cross BBB)
Term
Kaolin
Pectin
Definition
kaolin - hydrated Mg(OH)SiO3
pectin - indigestable carb from apples
Anti-diarrheal
Both appear to act as absorbents of bacteria, toxins, and fluid, thereby decreasing stool liquidity and number.
Term
Bismuth Compounds
Definition
bismuth/salicylates - anitdiarrheal
ulcer coater, inhibit prostaglandin/Cl sectretion
Dark stool
C/I renal pts
Term
bile salt binding resins
Definition
Cholestyramine, cholestipol, cholesevelam(no drug intrxn, binds drugs in lumen)
ANTI-DIARRHEAL - CROHN'S
Term
OCTREOTIDE
Definition
ANTI-DIARRHEAL (high dose)/PROKINETIC (low dose)
effects are dose related
Somatostatin analogue
GI carcinoid tumors
Term
pancreatin
pancrelipase
Definition
pancreatic enzyme replacement
Term
D2 agonists
Definition
ANTI-EMETIC
PROKINETICS/ANTI-EMETIC
disinhibit Ach -> increase LES pressure and esophageal peristalsis, no effect on SI/LI
METOCLOPRAMIDE, Domperidone (central)
Term
CHOLINOMIMETICS
Definition
Prokinetics
bethanechol -> M3
neostigmine -> AChE inhibitor
Term
Canabanoids
Definition
ANTI-EMETIC (unk MOA) - for chemo
Dronabinol - THC
Nabilone - THC analogue
Term
antihistamines, anticholinergics
Definition
ANTI-EMETIC
Diphenhydramine - H1
Meclizine - H1 (little anticholinergic effects)
Scopolamine - M (motion sickness patch)
Term
Metclopramide
Definition
inhibit dopamine R
ANTI-EMETIC
Term
Prochlorperazine
Promethazine
Definition
ANTI-EMETIC
inhibit Dopa/M and H receptors
Term
ODANSETRON
Granisetron
dolasetron
palonosetron
Definition
ANTI-EMETICS (5-HT antagonist)
post-operative and chemo
palonosetron - newer w/ higher affinity
Term
Misoprostil
lanoprostil
prostacyclin
aloprostadil
Definition
Prostaglandins
decrease acid production and increase mucus
misoprostil = PGE1 for NSAID PUD
lanoprostil = PGF2
prostacyclin = PGI2 for portal HTN
alprostadil = PGE1
Term
Celecoxib
Meloxicam
Definition
COX-2 inhibitor
Term
Diflunisol
Etodolac
Ibuprofen
Tolmetin
Acetaminophen
Definition
NSAIDS nonselective
acetaminophen = no anti-inflamm effects
Term
Sulindac
Definition
converted to sulfide metabolite->bile-> enterohepatic circulation -> 12-16hr duration
suppresses FAP inhibits colon cancer
Term
Oxaprozin
Definition
NSAID 60hr T(1/2)
nonselective
Term
Nambumetrone
Definition
NSAID
not an acid - little stomach damage
$$$$$$
Term
ketorlac
ketoprofen
Definition
NSAID
ketorlac - IV/IM for opiod reduction
ketoprofen - COX and LOX
Term
SULFASALAZINE
olsalazine
balsalazide
mesalamine
Definition
AMINOSALICYLATES -> IBD, UC, CROHNS
SULFASALAZINE -> 5ASA-N=N-sulfapyradine
-> sulfapyradine inhibits absorption
bacteria break N=N bond (in regions of IBD) AWESOME!
though to inhibit COX and LOX
Term
Azathioprine
6-mercaptopurine
Definition
PURINE ANALOGUES - used in chronic IBD
azathioprine -> 6-mercaptopurine
LONG time till onset of sx relief (17 wks)
Term
Infliximab
Adalimumab
Certolizumab
Definition
CROHN'S/UC
anti-TNF Ab IgG1
Fc portion = promotes Ab-mediated apoptosis, complement activation
certolizumab = no Fc fragment
Term
Cimetidine
Ranitidine
Famotidine
Nizatidine
Definition
H2 antagonists -> decrease gastric acid
cimetidine - gynecomastia
Term
Omneprazole
esomeprazole
lansoprazole
Rabeprazole
pantoprazole
Definition
irreversibly inhibits(S-S) Proton pump
enteric coat -> duodenal use
omeprazole - inhibit metab of warfarin, diazepam

AWESOME - low T.5, concentrated/activated in stomach, and Long duration of action.
Term
H. pylori therapies
Definition
triple(14d)- PPI + Clarithromycin + Amoxicillin or metronidazole

Consecutive-
1-5d - PPI + Amoxicillin
6-10d - PPI + Clarithromycin + Tinidazole
Term
Amoxicillin
Metronidazole
Clarithromycin
Tinidazole
Definition
H. pylori Rx
Amoxicillin - inhibit cell wall
Metronidazole/tinidazole - inhibit protein/DNA
Clarithromycin - inhibit 50S
Term
Aluminium hydroxide
magnesium hydroxide
calcium carbonate
Sodium Carbonate
Definition
ANTACID
Mg - osmotic diarrhea
Al - constipating
use Al and Mg together no issues
carbonates produce gas, alkalosis
sodium = fast reacting
Term
Sucralfate
Definition
Sucrose + Aluminum hydroxide
- coats ulcer
increase PGI, HCO3

decrease other drug absorb
Term
Pirenzepine
Telenzepine
Definition
Antimuscarinics - decrease gastric acid, little salivary effect
Telenzepine is more potent
Term
Disulfram
Definition
inhibits ALDH
Term
Psyllium
Methylcellulose
Polycarbophil
Definition
BULK FORMING LAXATIVES
large indigestable(bacteria->gas), hydrophillic fibers
swell->gel->distend colon->promote peristalsis
polycarbophil = synthetic fibers
Term
DOCUSATE
mineral oil
Definition
STOOL SOFTNER
don't aspirate mineral oil
oil for fecal impaction
Term
Magnesium hydroxide
LACTULOSE
polyethylene Glycol
Definition
OSMOTIC LAXATIVES
Mg/lactulose - cramps, gas - chronic constipation
polyethylene - B4 endoscopic procedures, no cramps or gas
Term
Aloe
senna
Cascara
Definition
STIMULANT LAXATIVES
low absorption, hydrolyzed in colon->BM, chronic use = melanosis coli
Term
LUBIPROSTONE
Definition
CHLORIDE CHANNEL ACTIVATOR (IBS)
activates type 2 Cl channels -> increase intralumenal Cl-> increase motility
Term
METHYLNALTREXONE
Alvimopan
Definition
OPIOD R ANTAGONISTS
don't cross BBB
methylnatrexone -> subQ. good for opiod induced constipation
alvimopan -> short term due to cardiac toxic, shorten post-op ileus
Term
5-FU and Leucovoran
capecitabine
Definition
GI cancer rx
leucovoran = co-factor for 5-FU, rescue for MTX
capecitabine = oral version of 5-FU
Term
Gefitinib
Erlotinib
Definition
inhibits EGFR (Tyrosine Kinase)
reversible
resistance = poor penetration
Term
CETUXIMAB
Definition
MAB against EGFR in colon cancer
infusion reaction prevented with dexamethasone
Term
Bevacizumab
Definition
MAB against VEGF for colon cancer (not breast)
tox: perforation, HTN, proteinuria
Term
Cisplatin
Oxaliplatin
Definition
DNA CROSS LINKERS
oxaliplatin is a better drug, peripheral neuropathy
cisplatin = nausea
Term
Gemcitabine
mitomycin
Definition
PANCREATIC CANCER
mitomycin - alkylator, stomach/colon too
gemcitabine - antimetabolite(don't use with rad therapy), 1st choice pancreas, can use esophagus, for dividing and resting tumors
Term
streptozocin
Definition
NITROSOUREA
alkylator
no carbamoylated protein toxicity (like in carmustine)
Term
Pacitaxel
Definition
ESOPHAGEAL CANCER
Binds beta-tubulin polymers and blocks disassembly
Term
Chloramphenicol
tetracyclins
Definition
doxycycline - oral, fecal elim
chloramphenicol - use in early pregnancy (unlike tetracyclines), but not late = grey baby
Term
SULFONAMIDES
Definition
SULFAMETHOXAZOLE
sulfasalazine (bowel), sulfisoxazole (used alone), sulfadiazine, sulfacetamide, sulfadoxine
inhibit folate synthesis
Term
Salmonella Rx
Definition
Ciprofloxacin, levofloxacin, or in children azithromycin
Term
Shigella Rx
Definition
Ciprofloxacin, sulfa
Term
Campylobacter jujenii
Definition
Azithromycin
Term
E. coli
Definition
Ciprofloxacin
no treatment for enterohemorrhagic
Term
Vibrio Cholera
Definition
Ciprofloxacin or doxy
Term
Yersinia enterocolitica
Definition
Doxycyclin plus gentamicin
Term
C. Difficile
Definition
Metronidazole
Term
Trimethoprim-sulfamethoxazole
Definition
inhibition of multiple steps in folate synthesis
Term
Ciprofloxacin
levofloxacin
Definition
inhibits Gyrase
don't use in kids
Term
Erythromycin
Telithromycin
Definition
increase GI mobility
inhibits 50S
enteric coated
telithromycin has lower toxicity
Term
Clindamycin
Definition
NOT A MACROLIDE
binds 50S
Term
Giardia lambdia
Definition
metronidazole/tinidazole
Term
Enteroamoeba histolytica
Definition
metronidazole
Term
Metronidazole
Tinidazole
Definition
degrades DNA in anaerobic bacteria.
S/E: inhibits ALDH
Tinidazole has less tox
Term
paromomycin
Definition
LUMENAL AMINOGLYCOSIDE
used to clear residual giardia
Term
Iodoquil
Definition
LUMENAL AGENT
CLEAR e. HISTOLYTICA
Term
NITAZOXANIDE
Definition
interferes with ferredoxin oxidoreductase enzyme dependent electron transfer reaction in anaerobic metabolism
Term
mebendazole,
albendazole
ivermectin
Definition
ANTI ROUND/HOOKWORMS
benzimidazoles- bind beta-tubulin monomers

Ivermectin - paralyse worms by activating glutamate sensitive Cl channels
Both are well tolerated.
Term
Praziquantel
Definition
ANTIFLUKE/TAPEWORMS
cause influx of Ca to produce paralysis of the musculature.
can treat flukes with metrifonate too
Term
PEGylated IFN alpha
Definition
HEPATITIS RX
inhibits viral replication, and the translation steps of viral protein synthesis.
HEP C, synergistic with ribavirin
Term
pentazocine
Definition
opiod analgesic
Term
propantheline bromide
Definition
antimuscarinic reduces cramping
Term
meperidine
Definition
opiod with some antimuscarinic
Term
cisapride
Definition
interacts with erythromycin to cause QT prolongation.
Term
diclofenac
Definition
NSAID
w/ omeprazole = stops recurrent bleed
w/ misoprostil = reduce GI ulcer
Term
tegaserod
Definition
PROKINETIC, 5-HT4 agonist
these are presynaptic receptors and enhances release of NT to promote peristaltic reflex; no effect on esophagus, induces Cl secretion in colon
removed from market, CV toxic
Term
flurbiprofen
Definition
NSAID
also effects TNF-alpha and NOS
Term
indomethacin
Definition
NSAID
may inhibit PLA,PLC,reduce PMN movement, decrease T/B cell proliferation
SE = pancreatitis
Term
naproxen
Definition
NSAID
free fraction higher in F than M
Term
piroxicam
Definition
NSAID
high dose stops PMN migraiton, decrease ROS production, but PUD/bleeding risk
Term
phenacitin
Definition
precursor of acetaminophen
Term
hydrocortisone
budesonide
Definition
glucocorticoids for IBD
hydrocortisone = enemas, suppositories for topical IBD tx
budesonide - analog of prednisone with controlled release for ileum/colon
Term
methotrexate
Definition
antimetabolite for Crohn's
may inhibit IL-1
Term
naltrexone
Definition
opioid antagonist for EtOH W/D
do NOT give with disulfiram b.c both hepatotoxic
Term
acamprosate
Definition
NMDA-R antagonist, GABAa activator for EtOH W/D
Term
odansetron
topiramate
Definition
maintains abstinence and reduces cravings in alcoholism
odansetron = 5-HT3 antagonist
Term
fomepizole
Definition
inhibits ADH - prevents conversion of methanol and ethylene glycol to toxic metabolites
expensive
Term
bisacodyl
Definition
Stimulant laxative
used with polyethylene glycol for colon cleansing before procedures
Term
irinotecan
Definition
topi I inhibitor
used in combo for colon cancer
Term
3 drugs never given orally
Definition
vancomycin = IV only
teicoplanin = IM
bacitracin = topical
Term
cryptosporidium treatment
Definition
nitazoxanide
Term
metrifonate
Definition
organophosphate - ACHE inhibitor
Term
Adefovir
Lamivudine
Definition
Hep B treatment
Adefovir - inhibitor of viral polymerase/reverse transcriptase enzyme, chain terminator
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