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79 Cards in this Set

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Natural Penicillins
penicillin G (benzathine, aqueous, procaine)

penicillin V (potassium)
Penicillinase resistant
nafcillin, oxacillin
Aminopenicillin
ampicillin, amoxicillin
Extended spectrum penicillins
pipercillin, pipercillin/tazobactam, ticarcillin, ticarcillin/potassium clavulanate, ampicillin/sulbactam, amoxicillin/potassium clavulanate
Clavulanic acid, sulbactam and tazobactam
B-lactamase inhibitors
What is the MOA of penicillin?
Inhibits the bacterial wall synthesis by binding to the penicillin binding proteins which inhibit transpeptidase leading to cell wall autolysis
Drug Interactions of Penicillins
Decreased effect - tetracylcines, aminoglycosides

Increased effect - neuromuscular blocking agents, aminoglycosides - synergistic activity
1st Generation Cephalosporins
Cefazolin
Cefadroxil
Cephalexin
2nd Generation Cephalosporins
Cefaclor
Cefatetan
Cefoxitin
Cefuroxime
Loracarbef
3rd Generation Cephalosporins
Ceftriaxone
Cefotaxime
Ceftaxidime
Cefixime
Cefdinir
4th Generation Cephalosporins
Cefepime
MOA of cephalosporins
Inhibits bacterial wall synthesis by binding to penicillin binding proteins which inhibits transpeptidase leading to cell wall autolysis (like PCN)
Drug interactions of Cephalosporins
aminoglycosides and furosemide may increase the probability of nephrotoxicity
Macrolides
Erythromycin
Azithromycin
Clarithromycin
Dirithromycin
troleandomycin
MOA of macrolides
bacteriostatic or bactericidal

reversibly bind to the 50S ribosomal subunit of susceptible organisms and may inhibit RNA dependent protein synthesis
Drug Interactions of Macrolides
Antacids
fluconazole
anticoagulants
carbamazepine
cyclosporin & digoxin (macrolides increase levels)
statins (increase with macrolides)
Tetracyclines
tetracycline
doxycline (vibramycin DOC for lymes disease)
minocycline
MOA of tetracyclines
(bacteriostatic)
Inhibits protein synthesis by binding to the 30S ribosomal subunit of susceptible bacteria thus disrupting the cytoplasmic membrane
Drug interactions of Tetracyclines
antacids (dec. bioavail of tetra)
anticoagulants (increase PT)
antiepileptics (phenytoin can dec. doxy)
iron (dec. doxy bioavail)
oral contraceptives
MOA of nitrofurantoin
Inhibits acetyl CoA reductase interfering with cell metabolism and cell wall synthesis
Drug interactions of nitrofurantoin
antacids including Mg
1st generation FQ
nalidixic acid
cinoxacin

(neither available)
2nd generation FQ
ciprofloxacin
ofloxacin
norfloxacin
3rd generation FQ
levofloxacin
moxifloxacin
gatifloxacin (Tequin no longer avail.)
trovafloxacin (Trovan no longer avail)
gemifloxacin
MOA of Fluoroquinolones
bactericidal + conc dependent kill

inhibits DNA-gyrase in susceptible organisms causing unraveling of double-stranded DNA.
3rd generation-inhibits topoisomerase II and IV
Drug interactions of Fluoroquinolones
antacids/heavy metals (Ca, Fe, Zn, Al, Mg dec. bioavail 90%)
anticoagulants/digoxin
theophylline (incres. CNS stim)
antiarrhythmics class 1A (quinidine, procainamide) and class III (amiodarone and sotalol) agents that cause an increase in QT interval

enterofeeding can dec. absorp
Glycopeptides
vancomycin
teicoplanin
MOA of vancomycin
inhibits bacterial cell wall synthesis and alters bacterial cell-membrane permeability
Drug interactions of glycopeptides
agents associated with increased nephrotoxicity (aminoglycosides, cyclosporine, amphotericin B, NSAIDs) and ototoxicity (aminoglycosides, loop diuretics)
Intravenous Aminoglycosides
gentamicin
tobramycin
amikacin

streptomycin
kanamycin
netilmicin
oral aminoglycosides
kanamycin
*neomycin
paromomycin
MOA of aminoglycosides
bactericidal +conc dependent kill

irreversibly binds to 30S subunit of bacterial ribosomes thus inhibiting protein synthesis

Used in synergy always, never alone
Drug interactions of aminoglycosides
Agents associated with increased nephrotoxicity and ototoxicity. May enhance neuromuscular blockade if administered with neuromuscular blocking agents
Sulfonamides
sulfadiazine
sulfamethoxazole
sulfisoxazole
MOA of sulfonamides and trimethoprim
MOA sulf (bacteriostatic)
inhibits bacterial growth by competitive antagonism of para-aminobenzoic acid (PABA) required for folic acid production

MOA (trimethoprim)
inhibits dihydrofolic acid reduction to tetrahydrofolate resulting in inhibition of enzymes for the folic acid pathway
Drug interactions of sulfonamides
CYP2C9 enzyme inhibitor
anticoagulants
methotrexate (increase toxicities)
sulfonylureas
cyclosporine
What is a severe adverse reaction to sulfonamides?
Steven Johnson Syndrome

also other skin reactions such as allergy and photosensitivity
Lincosamides
clindamycin
lincomycin
MOA of lincosamides
(bacteriostatic)
Binds to the 50S subunit of susceptible bacteria to suppress protein synthesis
Drug interactions of lincosamides
may enhance neuromuscular blockade if administered with NMBA
MOA of metronidazole
interacts with DNA of susceptible organisms resulting in inhibition of protein synthesis and cell death
Drug interactions of metronidazole
CYP2C9 enzyme substrate, CYP2C9, 3A3/4 and 3A5-7 enzyme inhibitor
phenytoin/phenobarbital may decrease metronidazole efficacy
may increase lithium levels!
Codename: Gorillamycin because of broad and strong coverage
Carbapenems
Carbapenems
imipenem/cilastatin
meropenem
ertapenem
What is the MOA of carbapenems?
[bactericidal]
inhibits bacterial cell wall synthesis by binding to 1 or more penicillin binding proteins (which inhibits the final trans-peptidase step of peptidoglycan-synthesis) resulting in cell wall lysis.
Drug interactions of imipenems.
cyclosporin and ganciclovir my enhance CNS activity (seizure)
Adverse effects of imipenims
rash, pancytopenia, increased LFTs, diarrhea, seizures have occurred in patients with compromised renal function/renal failure and dialysis patients - agent should be avoided. risk vs benefit.
What is the MOA of chloramphenicol?
[bacteriostatic]
binds to the 50S ribosomal subunit of susceptible bacteria interfering with protein synthesis resulting in cell death
what are some drug interactions of chlorampenicol?
CYP2C9 inhibitor
barbiturates (dec effec of barbs)
hydantoins (phenytoin can dec. conc of chloro)
rifampin (can dec conc. of chlor)
anticoagulants (incr. anticoagulant effect)
What are some adverse reactions of chloramphenical?
serious blood dyscrasis, severly toxic to bone marrow, CNS effects - confusino, delirium
What is the MOA of rifampin?
It inhibits RNA synthesis by binding to the beta subunit of RNA polymerase, blocking RNA transcription.
What are some drug interactions with Rifampin?
Rifampin is a substrate of CYP2A6, 2C8/9, 3A4
Rifampin is an inducer of CYP1A2, 2A6, 2B6, 3A4
Rifampin + pyrazainamide = hepatoxic reactions
rifampin decreases the plasma conc. of many agents.
anticoagulants, contraceptives, FQ, digoxin, cyclosporine, levothyroxine, protease inhibitors
What are some adverse effects of rifampin?
drowsiness, confusion, pruritis, urticaria, leucopenia, hemolytic anemia, thrombocytopenia, increase LFTs
May discolor body fluids - urine, tears, sweat to red-orange color
rifampin
What are the streptogramins?
quinupristin/dalfopristin (Syncercid)
What is the MOA of quinupristin/dalfopristin?
Two drugs work synergistically
quinupristin inhibits the late phase of protein synthesis at the bacterial ribosome
dalfopristin inhibits the early phase of protein synthesis at the bacterial ribosome
What are some drug interactions of streptogramins?
CYP450 3A4 inhibitor, cyclosporin, nifedipine, midazolam, protease inhibitors, carbamazepine
What are some adverse effects of quinupristin/dalfupristin?
arthralgias, myalgias (increas. dosing interval has shown some benefit), venous irritation, LFTs, bilirubin, CPK and LDH
what are some adverse reactions of quinupristin/dalfupristin?
arthralgias, myalgias (increa dosing interval), venous irritation, LFTs, bilirubin, CPK, and LDH
What are the oxalodinones?
linezolid (Zyvox)
What is the MOA of oxalodinones?
[bacteriostatic - enterococci adn staphylococci]
[bactericidal - streptococci]
binds to the 23S ribosomal RNA of the 50S subunit of susceptible organisms and prevents the formation of the 70S subunit needed for bacterial replication.
What are some drug interactions of oxalodinones?
no CYP450 metabolism
adrenergic agents (dopamine, epinephrine) incrase in blood pressure, serotonin syndrome with other serotonergic drugs
What are some adverse reactions to linezolid?
myelosupression, diarrhea, HTN with adrenergic agents, LFTs, lactic acidosis, peripheral neuropathy. Monitor CBC, platelets, avoid tyramine
What are the monobactams?
aztreonam
What is the MOA of monobactams?
Inhibition of bacterial cell wall synthesis by binding to one or more of the PBP
What are the drug interactions for monobactams?
potential nephrotoxic and ototoxicity if used with aminoglycosides. Must adjust for renal failure
What are some adverse reactions of monobactams?
rash, TENS, diarrhea, thromobocytopenia, pancytopenia, elevation of LFTs
What are the lipopeptides?
daptomycin
What is the MOA of daptomycin?
binding to gram positive bacterial cell wall membrane resulting in depolarization and dysfunction of protein, DNA, and RNA synthesis resulting in bacterial cell death (cyclin lipo-peptide antibiotic)
What are some drug interactions of lipopeptides?
possible interaction with warfarin
HMG-CoA may potentiate myopathy and CPK elevations (CPK > 1000, discontinue drug)
What are some adverse effects of lipopeptides?
fever, rash, injection site reaction, abnormal liver function tests, elevated CPK
What are the Ketolides?
telithromycin (Ketek)
What is the MOA of telithromycin?
bactericidal
blocks the protein synthesis of 23S rRNA of the 50S subunit resulting in cell death
What are some drug interactions of telithromycin?
telithromycin is a strong inhibitor and inducer of CYP P450 3A4 system

contraindicated - cisapride, pimozide (increase QT interval)
HMG-CoAs - avoid simva, atorva, and lova others ok
cyclosporin, carbamazepine, felodipine, verapamil, venlafaxine, digoxin, moxifloxacin, gatifloxacin, itraconazole, ketoconazole
Adverse reactions of telithromycin
visual disturbances, loss of conciousness, increase QT, avoid in brady, hypokalemia and hypomagnesemia and patients using class Ia (quinidine, procainamide) and class III (dofetilide) antiarrhythmic agents, visual disturbances, increase LFTs, diarrhea

****hepatic necrosis/failure in US and Canada. Monitor AST/ALT, bilirubin, hepatomegaly, jaundice*******
Glycylcyclines
tigecycline
(newer drug, a little different than tetracycline)
What is the MOA of tigecycline?
structurally similiar to tetracycline. binds to the 30S ribosomal subunit in prokaryotic cells, blocking the entry of amino-acyl tRNA molecules into the A site of the ribosome thus inhibiting protein synthesis
What are some drug interactions of tegecycline?
tigecycline decreases the clearance of warfarin
oral contraceptives my be less effective
no interaction with drugs that effect the CYP450 isoenzyme system
photosensitivity
What are the adverse reactions of tigecycline?
nausea, vomiting and diarrhea, photosensitivy reactions