Pharm - Rami Flashcards
penicillin MOA
binds PBPs thereby blocking peptidoglycan cross linking
what 3 penicillins are more susceptible to beta lactamases?
penicillin, ampicillin, piperacillin
general side effect of penicillins
allergic reaction
side effect of penicillin
drug induced coombs positive hemolytic anemia
drugs that cause drug induced coombs positive hemolytic anemia
penicillin, alpha methyldopa, and cephalosporins
side effect of ampicillin/amoxicillin
non-allergenic skin rash
side effect of methicillin
interstitial nephritis
drugs that cause interstitial nephritis
methicillin, NSAIDs, furosemide (“buy meth in dollars instead of euros”)
what form is pen V given
oral
what form is pen G given
IV
aztreonam structure
monocyclic beta lactam ring
blocks peptidoglycan cross-linking as well
why give aztreonam
renally insufficient patient;
allergic to penicillin
side effect of aztreonam
elevated LFTs
imipenem side effect
seizures in renally impaired patients
what do you give with imipenem
cilastin - inhibits renal dihydropeptidase I (enzyme that inactivates drug in renal tubules)
antibiotic you do not want to give to renally insufficient patient that aztreonam might be great for
aminoglycosides
gen 1 cephalosporins
gram positive
CEFAZOLIN, CEPHALEXIN
gen 2 cephalosporins
gram positive, anaerobes, H flu
CEFACLOR, CEFUROXIME
gen 3 cephalosporins
gram negative
CEFTRIAXONE
gen 4 cephalosporins
gram positive and negative
pseudomonas, CEFEPIME
gen 5 cephalosporins
MRSA,
CEFTAROLINE
cephalosporin side effects
hypersensitivity reaction (10% of patients with penicillin allergy with be allergic),
disulfiram-like reaction,
nephrotoxicity
drugs that cause disulfiram like reactions
“Sorry pals, can’t go mingle”
1st gen sulfonylureas, procarbazine, cephalosporins, griseofulvin. metronidazole
50S inhibitors
"50 cent - I'm a CMLC" chloramphenicol, macrolides, linezolid, clindamycin,
30S inhibitors
aminoglycosides,
tetracyclines
chloramphenicol MOA
reversibly binds 50S to inhibit peptidyl transferase
clindamycin MOA
inhibits formation of initiation complex
aminoglycosides MOA
inhibits formation of initiation complex and causes mRNA misreading
tetracyclines MOA
blocks AMINOACYL tRNA from binding to the ribosome
chloramphenicol side effects
aplastic anemia,
gray baby syndrome (vomiting, flaccidity, gray skin hue, shock in newborns due to lack of UDP-glucuronyl transferase in liver)
drugs that cause aplastic anemia
"Cant Make New Blood Cells Properly" (carbamazepine, methimazole, NSAIDs, benzene, chloramphenicol, PTU)
side effects of macrolides
erythromycin, clarithromycin, azithromycin
acute cholestatic hepatitis (jaundice)
uses of clindamycin
anaerobic infections above the diaphragm
side effects of clindamycin
pseudomembranous colitis (c. diff)
linezolid treats…
VRE, MRSA
VRE: vancomycin resistant enterococcus
uses of metronidazole
anaerobic infections below the diaphragm
side effects of aminoglycosides
nephrotoxicity (especially with cephalosporin),
ototoxicity (especially with loop diuretic),
teratogenicity
aminoglycosides are ineffective against…
anaerobes because they require oxygen to be taken up into bacterial cells
tetracycline side effects
teeth discoloration, bone deformity in kids, fanconi syndrome (aminoaciduria, phosphaturia, acidosis, glycosuria), photosensitivity
how is doxycycline eliminated
fecally –>
so it can be used in renally insufficient patients
uses of demeclocycline
treats SIADH (competitive antagonist at V2 receptor)
name all of the anti mycobacterial agents
rifampin, isoniazid pyrazinamide ethambutol dapsone
rifampin MOA
inhibits bacterial DNA-dependent RNA polymerase
side effects of rifampin
orange urine, hepatitis
isoniazid MOA
inhibits synthesis of mycolic acids
side effects of isoniazid
peripheral neuropathy (due to Vitamin B6 depletion),
G6PD-hemolytic anemia,
drug induced lupus,
hepatitis
dapsone MOA
PABA antagonist, inhibits folic acid synthesis
dapsone side effects
G6PD hemolytic anemia
ethambutol MOA
inhibits mycobacterial arabinosyl transferase
ethambutol side effects
retrobulbar neuritis (decreased visual acuity and red green color blindness)
pyrazinamide side effects
hepatotoxicity,
hyperuricemia (gout)
drugs that are hepatotoxic
“Patron is FIRSt fun, then hepatotoxic”
pyrazinamide, fibrates, isoniazid, rifampin, statins,
drugs that cause SLE like syndrome
“Having lupus is Mega SHIPP-E”
methyldopa, sulfa, hydralazine, isoniazid, procainamide, phenytoin, etanercept
drugs that cause hyperuricemia/gout
“Painful Tophi in Feet Need Care”
pyrazinamide, thiazide, furosemide, niacin, cyclosporine
drugs that cause G6PD hemolytic anemia
“Hemolysis IS D PAIN”
isoniazid, sulfonamides, dapsone, primaquine, aspirin, ibuprofen, nitrofurantoin
isoniazid causes peripheral neuropathy because…
it depletes the body of vitamin B6
trimethoprim- sulfamethoxazole MOA
DNA synthesis disruption
trimeth - blocks dihydrofolate reductase
sulfameth - blocks dihydropteroate synthase
bactrim (TMP-SMX) side effects
stevens johnson syndrome,
hemolytic anemia,
kernicterus in newborns,
(BAK)
sulfa drugs
“Popular FACTSSS”
probenecid, furosemide, acetazolamide, celecoxib, thiazides, sulfonamide antibiotics, sulfasalazine, sulfonylureas
fluoroquinolones MOA
inhibits bacterial DNA topoisomerase II –>
DNA strand breaks –> cell death
fluoroquinolones side effects
tendonitis,
tendon rupture,
contraindicated in pregnant women and kids (damages cartilage)
fluoroquinolones coverage
gram negative
vancomycin MOA
binds D-ala D-ala, inhibits transglycosylase, weakens cell wall and causes cell lysis
vancomycin uses
MRSA, C. diff pseudomembranous colitis orally
side effects of vancomycin
“NOT” + red man
nephrotoxicity,
ototoxicity,
thrombophlebitis,
and red man syndrome
side effects of metronidazole
metallic taste,
disulfiram-like rxn
nucleoside reverse transcriptase inhibitors
zidovudine,
didanosine,
lamivudine,
abacavir
non nucleoside reverse transcriptase inhibitors
nevirapine,
efavirenz,
delavirdine
NRTI side effects
zidovudine - megaloblastic anemia
didanosine - pancreatitis
NNRTI side effects
efavirenz - CNS disturbances
nevirapine - stevens johnson syndrome, hepatitis
what NRTI is used on pregnant women?
zidovudine
what is the suffix of the protease inhibitors
-navir
MOA of protease inhibitors
inhibit HIV protease enzyme
side effects of protease inhibitors
altered distribution of fat (buffalo hump, increased truncal obesity), insulin resistance = hyperlipidemia, neuropathy
what disease causes buffalo hump
cushing syndrome (increased cortisol)
what drug besides protease inhibitors leads to fat redistribution
glucocorticoids (fat PIG)
acyclovir MOA
phosphorylated by viral thymidine kinase into analog of dGTP (inhibits DNA synthesis)
acyclovir side effects
neurotoxicity (tremor, delirium),
nephrotoxicity
ganciclovir MOA
inhibit CMV DNA polymerase,
especially useful for CMV retinitis
“I Gan Ci”
amantidine MOA
binds M2 surface protein on influenza A, blocking uncoating of viral RNA,
can also stimulate release of dopamine from neurons of nigra striatum
amantidine side effect
CNS symptoms
zanamivir MOA
inhibits neuraminidase,
treats influenza A and B
ribavirin MOA
inhibits viral RNA polymerase –> inhibits viral replication
ribavirin side effect
teratogenicity
Contraindicated in pregnancy, and in renally insufficient patients
amphotericin MOA
tears holes,
binds ergosterol,
alters permeability of fungal cell membrane,
leads to cell death
amphotericin side effects
“Ampho-Terrible”
infusion related reaction,
nephrotoxicity
does amphotericin cross the BBB
no
flucytosine MOA
inhibits thymidylate synthease - inhibits fungal DNA and RNA synthesis
flucytosine side effect
bone marrow suppression
caspofungin MOA
inhibits B(1,3)-D-glucan synthase
β(1,3)-d-glucan is an essential component of the fungal cell wall
griseofulvin MOA
interferes with microtubule formation and inhibits fungal cell replication
name an allylamine and the enzyme it blocks
terbinafine,
blocks squalene epoxidase,
tx: onychomycosis
what enzyme do azoles block
lanosterol 14 alpha demethylase
ketoconazole, miconazole, clotrimazole side effect
gynecomastia (because they disrupt gonadal and adrenal steroid synthesis)
can be used to treat cushing syndrome because of this
quinine side effects
cinchonism (tinnitus, headache, dizziness, nausea)
coombs positive hemolytic anemia
fetal toxicity
mefloquine side effect
mental status change
primaquine side effects
G6PD hemolytic anemia,
fetal toxicity
alpha 1 receptor secondary messenger
PLC,
increased IP3 and DAG –>
increased intracellular calcium
alpha 2 and D2 secondary messenger
Gi - inhibition of AC leads to decreased cAMP
beta 1 and 2 and D1 secondary messenger
Gs - AC activation leading to increased cAMP
direct sympathomimetics - uses
emergency shock,
anaphylaxis
(fast decrease in BP)
epinephrine - receptors
alpha agonist at high doses,
beta agonist at low doses
uses of epinephrine
anaphylaxis,
bronchospasm
epinephrine SE
hypertension,
pulmonary edema
norepinephrine - receptors
alpha 1, alpha 2, beta 1 (increased contractility)
dopamine - receptors
alpha agonist at high doses
beta agonist at low doses
D1 agonist at even lower doses
dobutamine - receptors
beta 1 agonist
selective = B for BRAT
uses of dobutamine
cardiac stress test,
cardiogenic shock
side effect of dobutamine
hypotension (via rebound)
direct sympathomimetics
“Duplicate sympathetic END point”
dobutamine,
epinephrine,
norepinephrine,
dopamine
indirect sympathomimetics - stimulate the release of…
direct sympathomimetics
ephedrine stimulates release of…
norepinephrine,
also stimulates beta 2 receptors and the CNS
effect of ephedrine
increased contractility (same as NE), bronchodilation (beta 2)
uses of ephedrine
nasal decongestant (pseudoephedrine),
athletic enhancement drug
(since it is a CNS stimulant)
cocaine MOA
blocks Na/K ATPase pump responsible for reuptake of NE, serotonin, and dopamine
results in euphoria, vasoconstriction
also blocks voltage-gated Na channels
results in anesthesia
cocaine side effects
hypertension,
cardiac ischemia,
cardiac arrhythmias
indirect sympathomimetics
amphetamines,
cocaine,
ephedrine
use of phenylephrine
mydriasis (eye exam)
“would you like me to dilate your Pupils?”
phenylephrine MOA
alpha 1 agonist
midodrine MOA
alpha 1 agonist
midodrine uses
used in patients with advanced hepatic disease,
orthostatic hypotension
Think: Me go faint & M1dodr1ne
side effect of midodrine
supine hypertension
clonidine uses
treats hypertension by inhibiting release of sympathetic neurotransmitters
clonidine side effect
rebound hypertension if withdrawn quickly
Think: “Clonidine clones itself” - goes from treating HTN to causing it!
clonidine MOA
alpha 2 agonist
isoproterenol uses
treats torsades de pointes (long QT) - given with magnesium for this,
can also treat cardiac arrest/heart block
isoproterenol MOA
beta 1 and 2 agonist
fenoldopam use
produces renal vasodilation for severe hypertension
albuterol uses
produces bronchodilation (treats asthma), treats hyperkalemia by causing transcellular shift of K into the cell
beta 2 agonists
“Beta 2 agonist needed for SAT-induced asthma!”
salmeterol,
albuterol,
terbutaline,
salmeterol uses
long acting treatment for COPD and asthma;
used with inhaled corticosteroids
analogue of albuterol
terbutaline MOA
beta 2 agonist;
relaxes smooth muscle in lungs and uterus
by directly-acting on the receptor
terbutaline use
delay preterm labor by reducing uterine contractions
Think: “TERM-butaline”
side effects of terbutaline
tachycardia,
tremor
methyldopa MOA
alpha 2 agonist
methyldopa uses
treats moderate hypertension
using adrenergic neurotransmitters
methyldopa side effects
positive coombs test,
orthostatic hypotension
phenoxybenzamine MOA
irreversible alpha receptor antagonist
phenoxybenzamine side effect
inhibition of ejaculation
phenoxybenzamine use
treats pheochromocytoma
both are 16 letters
phentolamine MOA
SHORT-ACTING
reversible alpha receptor antagonist
phentolamine use
diagnose pheochromocytoma
prazosin (-zosin) and tamulosin MOA
selective alpha 1 antagonist
prazosin (-zosin) and tamulosin uses
decrease prostatic and bladder neck contraction,
decrease blood pressure,
treatment for hypertension and BPH
prazosin (-zosin) and tamulosin side effect
first dose syncope (severe orthostatic hypotension –> syncope)
timolol MOA
beta 1 and 2 antagonist
timolol uses
ophthalmic solution - decreases aqueous humor secretion;
used to treat glaucoma
pindolol MOA
weak beta receptor agonist,
beta receptor antagonist,
intrinsic sympathomimetic properties
pindolol uses
treats: HTN, bradycardia
propranolol MOA
beta 1 and 2 antagonist
propranolol uses
tachycardia associated with hyperthyroidism and chronic migraines
side effects of propranolol
bronchoconstriction, fasting hypoglycemia (decreased glycogenolysis)
esmolol MOA
short acting beta 1 antagonist
“es small” = short acting
esmolol uses
treats critically ill patients with arrhythmias, hypertension, and MI
carvedilol MOA
alpha 1 and beta receptor blocker
carvedilol uses
decreases HR and contractility;
bronchoconstriction,
treats CHF (given with ACEi and diuretics),
treats hypertension
metoprolol MOA
selective beta 1 antagonist
metoprolol uses
decreases HR and contractility,
treats hypertension, tachycardias, CAD, especially in patients with diabetes
M1 and M3 receptors
Gq (increased IP3 and DAG –> increased intracellular calcium)
(same mechanism as alpha1 from adrenergics)
M2 receptor
Gi (AC is inhibited –> decreased cAMP),
also an increase in K+ conductance
same mechanism as alpha2 from adrenergics
Nm and Nn
activation of Na/K channels
pilocarpine and carbachol uses
applied topically to eye (ophthalmic solution);
treats glaucoma;
Think: piloCRYpine and CRYbachol
pilocarpine/carbachol MOA
M3 muscarinic agonist
methacholine uses
bronchial challenge test (inhalation);
diagnoses asthma
methacholine MOA
smooth muscle contraction of bronchi,
M1, M2, M3 muscarinic agonist (*use targets M3)
methacholine side effects
bradycardia, hypotension;
minimally seen because it is inhaled
bethanechol MOA
M2, M3 agonist (use related to M3)
bethanechol uses
promotes urination,
treats neurogenic ileus (urinary retention), especially postpartum or postop
bethanechol side effect
diarrhea
M3 agonists (3 of them)
pilocarpine,
methacholine,
bethanechol
atropine MOA
competitive M1-M3 antagonist
atropine use
antidote for cholinesterase inhibitor poisoning (nerve gas, insecticide)
treatment for atropine poisoning
physostigmine
cholinesterase inhibitor
atropine side effects
characteristic of muscarinic block:
hyperthermia (flushing), decreased salivation, cycloplegia (blurred vision), psychosis, tachycardia
tropicamide and homatropine uses
ophthalmic solutions,
retinal examinations,
temporary cycloplegia and mydriasis
tropicamide and homatropine MOA
atropine analogs,
antimuscarinic M1-M3
benztropine MOA
M1-M3 antagonist, M1 receptors (brain) in corpus striatum (PD)
benztropine use
treats parkinson’s by improving tremor and rigidity;
no effect on bradykinesia
benztropine contraindication
patients with glaucoma
scopolamine MOA
competitive M1-M3 antagonist;
action at MI for usage
scopolamine use
treats motion sickness,
crosses BBB to interact between vestibular ear and vomiting center of brain
think: “scopukeamine”
ipratropium MOA
M3 receptor antagonist
ipratropium uses
inhaled form causes bronchodilation;
treats COPD and asthma
(especially in those who are unable to take adrenergic agents)
think: “i pray to breathe”
oxybutynin MOA
M1-M3 receptor antagonist (action at M3)
oxybutynin uses
treats urinary incontinence and hyperhidrosis
cholinesterase inhibitors (anticholinesterases) have what effects
parasympathetic/muscarinic,
increased ACh
neostigmine MOA
reversibly inhibits acetylcholinesterase,
increased stimulation of nicotinic and muscarinic receptors
does neostigmine cross the BBB
no
neostigmine uses
treats myasthenia gravis,
overcomes nondepolarizing neuromuscular blockade (caused by pancuronium or vecuronium)
physostigmine MOA
reversibly inhibits Acetylcholinesterase
does physostigmine cross BBB
yes - used as antidote for atropine overdose
uses of physostigmine
antidote for atropine overdose,
ophthalmic solution - treats glaucoma
edrophonium and pyridostigmine MOA
reversibly inhibit Acetycholinesterase –>
increased stimulation of both nicotinic and muscarinic receptors
edrophonium use
diagnosis of myasthenia gravis (short acting)
think: “a drop lasts a moment, but a stigma lasts forever”
pyridostigmine use
treats myasthenia gravis (long acting)
tacrine MOA
reversibly inhibits AChE –>
increased stimulation of both nicotinic and muscarinic receptors
tacrine use
treats alzheimers
Think: “Tacrine (taking) care of Alzheimer’s patients”
tacrine side effect
hepatotoxicity
drugs similar to tacrine
Think: “Tacrine RDG”
rivastigmine,
donezepil,
galantamine,
echothiophate MOA
inhibits AChE by covalently binding to the enzyme –>
increased stimulation of both nicotinic and muscarinic receptors