Pharmacology Flashcards
List the H2 blockers you need to know
The DINEs:
Cimeti
Famoti
Nizati
Raniti
Why are H2 receptor blockers commonly taken w/ an NSAIDs?
NSAIDs decrease activity of the pathways involved in protecting the GI wall from digestion
which H2RB also exhibits antiandrogen effects?
cimetidine
Composite a list of drugs you need to know that have have a AE of gynecomastia.
spironolactone
digitalis
cimetidine
ketoconazole
chronic abuse of what substance can cause a long-term complication of gynecomastia?
alcohol
What OTC substances are CYP P450 inhibitors?
alcohol (acute toxic effects)
grapefruit juice
what H2RB is a CYP450 inhibitor?
cimetidine
what class of antifungals are CYP inhibitors
azoles
what antibiotics are CYP inhibitors
erythromycin; sulfonamides; quinidine; isoniazid
what anti-seizure drug is a potent CYP inhibitor
valproate
what OTC substances are CYP inducrers
alcohol (chronic toxic effects)
St. John’s Wort
what anti-seizure drugs are potent CYP inducers
phenytoin
phenobarbital
carbamazepine
griseofulvin
what antibiotic is a CYP inducer
rifampin
PPIs are what kind of inhibitor & what is their MOA
suicide inhibitors of the H+/K+ ATPase
list the PPIs you need to know
The PRAZOLEs
omeprazole
esomeprazole
lansoprazole
dexlansoprazole
pantoprazole
raberprazole
what is a unique AE of omeprazole
potentially dangerous DD rxn. b/t omeprazole & clopidogrel
omeprazole inhibits CYP2C19-
All PPIs have these AEs.
rebound acid secretion (elderly pts. more susceptable)
C. diff & Comm. acquired infections
decreased levels of Vit. B12
what specific PPIs should be used w/ caution for pts. w/ liver diseases
esomeprazole & lansoprazole
Mnemoinc: Primary Function of LIVER is EEEEmulsification regulation & LLLLLipid metabolism
what is the MOA of Vonoprazan
non-competitive allosteric modulator: blocks K+ binding site which keeps HKATPases in their inactive form
Compared to other PPIs, what AEs are not seen w/ vonoprazan
CYP2C19 inhibition
vonoprazan also has a longer duration of action
what antacid is also used for the management of osteoporosis and can therefore cause hypercalcemia
Calcium Carbonate
use of what antacid is assoc. w/ constipation
aluminum hydroxide
use of what antacid is assoc. w/ diarrhea
magnesium hydroxide
sodium bicarbonate has what unique AEs?
flatulence, CV effects, & metabolic alkalosis
If you prescribe these drugs to your pts., you should inform them of this drug-drug interaction.
Antacids are ionic compounds which gives them the ability to increases gastric pH; therefore, certain drugs that rely on gastric pH for their metabolism will not be able to diffuse across the gastric epithelium to be absorbed into the blood stream; these drugs are the following:
tetracyclines, fluoroquinolones, & digoxin
what is the effect of COX2
pro-inflammatory, pain, & fever inducer
what is the effect of COX1
GI mucosal integrity; platelet function; & renal function
why do selective COX2 inhibitors increase the risk of CVD?
COX1-COX2 negative feedback loop:
COX1 is constitutively active in the absence of COX2 agonists; If you only inhbit COX2, this leaves downstrem effects of COX1 unregulated; therefore, there will be an increase in platelet aggregation which will subsequently decrease production of prostacyclin (a potent vaso-dilator)
what is the MOA of SucrALfate?
viscous polymer of sucrose and therefore not absorbed; it adheres to ulcer craters to serve as a band-aid; DOES NOT DECREASES ACID SECRETION
what is the main AE of sucrALfate
AL: ALLUMMINUM INDUCED CONSTIPATION
What is the MOA of misoprostol?
prostaglandin E1 analog
what is the role of PGE1 in the GI tract?
secretion of mucus & bicarbonate
Misoprostol is commonly indicated for chronic use of this drug class to prevent formation of ulcers.
NSAIDs
Why does Misoprostol cause GI crampin & diarrhea
this drug increases motility in the GI tract
why is misoprostol a CI for pregnancy?
this drug also induces uterine contractions leading to preterm, spontaneous delivery
what is a unique AE of Bismuth subsalicylate and describe the mechanism?
black stool & tongue
contents in the GI lumen undergo a chemical rxn. w/ the sulphur group on bismuth that turns the lumen black
Why does Bismuth Subsalicylate also have a salicylate toxicity
anti-inflammatory effect
salicylate toxicity symptoms: tinnitus & acidosis
bismuch subsalicylate is assoc. w/ what pediatric syndrome?
reye’s syndrome: Jaundice, Mental Confusion, Delirium, Dark Urine, Emesis
what ABxs are commonly used for treatment of H. Pylori infections?
amoxicillin, metronidazole, tetracylcline, & clarithromycin
Describe the toxic mechanism of H. Pylori
H. pylori produces and secretes urease to raise gastric pH; an increase in gastric pH activates proinflammatory mediators which increases risk for PUD
what is the MOA of macrolide?
binds 50S: inhibits elongation of growing peptide chains
bacteriostatic effect
why is azithromycin increasingly becoming the preferred macrolide for pts. taking several different medications
no CYP inhibition
macrolides are effective against what pathogens?
chlamydia (alternative for pregies, though doxycycline is 1st lin); mycoplasma; legionella; corynebacterium diptheria; syphilis (penicillin G is 1st line)
Penicllins, cephalosporins, monobactams, & carbapemems inhibit which step of cell wall synthesi?
polymerization of D-ala-D-ala polymers
vancomycin inhibits what step of cell wall synthesis
polymerization of D-alanine polymers
what is the MOA of beta lactams?
inhibit transpeptidases
what are mech. of resistance for macrolides?
methylation of 23S rRNA; enzymatic inactivation of phosphotransferases
what are mech. of resistance for beta lactams?
PBPs; beta-lactamases
what is the MOA of metronidazole?
metronidazole’s nitro group is reduced by pyruvate-ferredoxin oxidoreductases to promote formation of free radicals which damage proteins & nucleic acids (bacterialcidal effect)
what are AEs of metronidazole?
dry mouth; metallic taste; peripheral neuropathy; neutropenia; disulfiram effect
what are the presentations of the disulfiram effect?
N/V; sweating; hyperventilation; tachycardia, vetigo
metronidazole is effective against what microbes?
H. pylori, amebiasis, trichomoniasis, C. diff, rosacea
what is the MOA of tetracyclines?
block t-RNA binding site on 30S which inhabits elongation
what AE of tetracylines is a teratogen?
permanent staining of teeth
what are mech. of ressitance against tetracylcines
decreased uptake; drug efflux
which tetracycline is assoc. w/ vertigo
minocycline
what renal toxicty is assoc. w/ all tetracyclines
PT dysfunction leading to Fanconi Syndrome
