MOAs Flashcards
Tegaserod
Serotonin Agonist (Tx of IBS)
Scopalamine
anti-cholinergic (used to decrease salivation)
-prazoles
IRREVERSIBLE H/K ATPase inhibitor
- abs in SI (enteric coating get it past stomach)
- lipid soluble so it travels to stomach and diffuses into canalculi
- gets ionized in canalculi and is trapped there (where H+ pumps are found)
Bismuth
chelates proteins at base of ulcer to protect them from pepsin and acid = forms protective layer
- -also increase Bicarb and mucous secretions
- -BACTERIOSTATIC to H. pylori
Also used to treat diarrhea, it abs bacteria/toxins/viruses = protective against travelers diarrhea
Clarithromycin
Macroline = 50s inhib
H.pylori eradication
Cevimeline
M3»_space;> M1 agonist (used to increase salivation)
Metoclopramide
D2 antagonist = accelerates gastric emptying!! (inc motility)
and
5-HT4 agonist = increased PSNS tone
amoxcicillin
B lactam **resistant to B lactamases = good for gram - bacterial infection (H. pylori)
Sulfasalazine
5-ASA derivative that decreases inflammation locally
Pilocarpine
Muscarininc agonist (all M receptors) --used to increase salivation
Sucralfate
- *requires acidic pH** to form a protective gel over ulcer
* do not need to alkylate in order to protect = decreased chance of bacterial overgrowth
Metronidazole
taken up by bacteria, protozoans, and ameobas and then reduced to ferrodoxin –> nitro intermediates –> thiolinkages on cysteine bearing enzymes
–> in bacteria, will also disrupt DNA
Methylprednisolone
GCS used to dec inflammation in IBD
Laculose
fecal acidifier = laculose is broken down by bacteria in gut into organic acids. the decreased pH in the colon prevents the diffusion of NH3 into the blood stream. therefore this is a treatment for Hepatic encephalopahy
Gemcitabine
DNA pol inhibitor
oral TKIs
Imatinib
sunitinib
soratinib
Mitomycin
mono or bi alkylating agent
Neomycin
antimicrobial given as an enema to decrease the colonic bacteria = dec NH3 formed = treatment for hepatic encephalopathy
cyclin dept kinase inhibitor
trastuzumab
Cisplatin
DNA crosslinks
erlotinib
EGFR TKI
imatinib
oral KIT TKI
Fidaxomicin
macrolide = 50s inhibitor of bac RNA pol
- *minimal systemization
- tx of C diff
upper or lower GI route of fecal transplant better
lower
Metamucil
hydrophillic mucolipid (fiber) that forms a large gelatinous mass when mixes with water –> more formed stools *treatment for constipation and diarrhea
Docusate Sodium [Colace]
anionic surfactant that allows for more water and fat to be incorporated into stools = stool softener
Biscodyl [Ducolax]
PRODRUG CONVERTED BY ENTERIC BACTERIA
stimulant laxative that activates myenteric plexus –> contractions
also causes tight junctions to become more leaky (NaCl and water into lumen)
Lubiprostone
stimualtes Cl- channel directly to increase Cl- efflux into lumen –> H2O follows
**used in Tx of IBS-D
castor oil
anionic surfactant that allows for more water and fat to be incorporated into stools = stool softener
also cathartic and causes complete evacuation of the intestines
Loperamide [Imodium]
opiate receptor agonist that increases gut transit time (inhibiti Ach) allows more time for things to get abs by gut
Cascara
stimulant laxatives, with the glycosides stimulating peristalsis, and emodin exciting smooth muscle cells in the large intestine.
Senna
Stimulant laxitive, glycosides increase gastric fluid secretion and bowel motility (stimulate peristalsis)
–activate myenteric plexus and increase permeability
Scopalamine
anti-cholinergic = blocks M1 and vagal simulation of CN 8 (vestibular N) = motion sickness
patch preparation that is put on behind the ear 1 hr before getting on boat (or whatever) –only effective if started before!!
Chlorpromazine
centrally acting D2 and muscarinit receptor antagonists for the treatment of N/V
Granisetron
peripherally acting 5-HT3 antagonist (in stomach and small intestine) = blocks vagal afferents going to chemoreceptor trigger zone/area postrema
Cyclizine
H1 antihistamine = vagal and vestibular blockers for the treatment of motion sickness
used to treat intractable hiccough
chlorpromazine
aprepitant
central substance P/neurokinin 1 receptor antagonist
Droperidol
centrally acting D2 blocker
Meclizine
H1 anti-histamine = used to tret vertigo
**depresses hyperstimulation of the labyrinth
used to treat post-opertave N/V
Droperidol
given prior to chemo
lorazepam
Dolesetron
peripherally acting 5-HT3 antagonist (in stomach and small intestine) = blocks vagal afferents going to chemoreceptor trigger zone/area postrema
**longest half life!!!
HBV treatment drugs
HCV drugs
B: lamivudine, adefovir, tenofovir, entacavir, emtricitabine
C: ribavarin, telprevir, boceprevir
Emtricitabine
triphosphate cytosine analog that inhibits viral RNA pol
Entacavir
d-cyclopentane and guanosine analog that inhibits viral RNA pol
Lamivudine
L-nuceloside and cytosine analog that inhibis viral RNA po
Adefovir
acyclic diphosphate adenoside analog that inhibits viral reverse transcriptase and causes chain termination
Tenofovir
acyclic diphosphate adenoside analog that inhbits viral RNA pol and causes chain termination
Used to treat HIV and HBV co infection
emticitabine > tenofovir
transient thryroid disturbance (hashimotos and graves)
interferons
ribavarin
- increases CTLs
- inhibits RdRP
- depletes GTP pool (via inhib IMPDH)
- mutates RNA (as virus replicates)
teleprevir
inhibits NS3/4 serine protease needed to cleave precursor peptide strand into functional polypeptide
**high resistance and must be used with ribavarin
boceprevir
inhibits NS3/4 serine protease needed to cleave precursor peptide strand into functional polypeptide
**high resistance and must be used with ribavarin
Ciprofloxacin
inhibits DNA gyrase and topoisomerases
Chlorpheniramine
H1 antagonist and SSRI (anti-emetic?)
Donepezil
Ach E inhibitor
Methylnaltrexone
μ-opioid antagonists **speed up gut motility = constipation Tx?
Naloxone
Opiate Antagonist *speed up gut motility = constipation Tx?
