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126 Cards in this Set

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What is nitrofurantoin used for?
UTIs that are NOT caused by PP --> Proteus and Pseudomonas.
What is a side effect of nitrofurantoin?
Can cause brownish discoloration of urine --> because it is metabolized and excreted by kidney.

2) allergic pulmonary infiltrates
3) Lupus like syndrome
4) G6PD-deficiency: hemolytic anemia
What is the mechanism of action of TMP?
Inhibits bacterial dihydrofolate reductase, so it is a bacteriostatic!
What is TMP-SMX used for?
Recurrent UTIs and PCP Pneumonia.
What are the side effects of TMP-SMX?
Treats the marrow poorly
1) G6PD deficiency
2) megaloblastic anemia
3) leukopenia
4) granulocytopenia, neutropenia
What are some examples of sulfonamides?
Sulfamethoxazole (SMX), sulfisoxazole, triple sulfas, and sulfadiazine.
What is the mechanism of action of sulfonamides?
Inhibits dihydropteroate synthase, preventing formation of dihydropteroid acid so cant make dihydrofolic acid. It is a bacteriostatic
What are sulfonamides used for?
Treat Nocardia, Chlamydia, simple UTIs.
What are side effects of sulfonamides?
Hypersensitivity reactions, hemolysis if G6PD deficient.
2) Nephrotoxicity (tubulointerstitial)
3) kernicterus in infants
4) Can displace drugs from albumin (warfarin)
5) Steven-Johnson syndrome
What are fluoroquinones?
Antibiotics that inhibit topoisomerae II (DNA gyrase) and topoisomerase IV, causing termination of DNA replication.
What are quinolones?
They are 1st generation and consist of nalidixic acid.
What is nalidixic acid used for?
Used for UTIs caused by gram negative bacteria. It is a quinolone antibiotic (1st generation)
What are the 2nd generation fluoroquinolones?
Norfloxacin, Oflaxacin, and Ciprofloxacin.
What are teh side effects of nalidix acid? (1st generation quinolone)
Seizures, anaphylaxis,
What are the 3rd generation fluoroquinolones?
Levofloxacin, gatifloxacin, and moxifloxacin
What are the 2nd generation fluoroquinolones?
Norfloxacin, oflaxacin, ciprofloxacin
What are the 3rd generation fluoroquinolones?
Levofloxacin, gatifloxacin, and moxifloxacin. used as "respiratory quinolones"
What is the 4th generation fluoroquinolone?
Trovafloxacin
What is the side effect of trovafloxacin?
Hepatotoxicity
What are the general side effects of fluoroquinolones?
1) GI upset
2) Rash, allergy, photosensitivity
3) QT prolongation
4) Chondrocyte toxicity causing impaired cartilage development, so dont give to pregnant women, breast feeding women, or children.
What is the mechanism of action of fluoroquinolones?
Inhibit topoisomerase II (AKA DNA gyrase) and topoisomerase IV (causing termination of DNA replication).
What does topoisomerase II normally do?
Functions in negative supercoiling and elimination of supercoils at the replication fork.
What does topoisomerase IV normally do?
Functions in separation of daughter molecules after replication is complete.
What are some side effects of fluoroquinolones in adults?
Tendonitis and tendon rupture
What are some side effects of fluoroquinolones in children?
Leg cramps and myalgias in kids.
What are fluoroquinolones used for?
Gram-negative rods of urinary and Gi tracts. Used to treat UTIs and sometimes atypical respiratory bugs.
What is the most active fluoroquinolone against Pseudomonas?
Ciprofloxacin.
What is mechanism of Clindamycin?
Inhibits protein synthesis at the level of the 50S ribisome. Remember buy AT 30, CELL at 50. cLindamycin
What is the clinical use of clindamycin?
Used to treat anaerobic infections (Bacteroides, Clostridium).
What is the toxicities of clindamycin?
Pseudomembranous colitis (C. dificile overgrowth), fever, and diarrhea. It is commonly associated with this!
What is the mechanism of action of chloramphenicol?
It inhibits 50 S subunit of ribosome. CELL at 50! It is a bacteriostatic.
What is chloramphenicol used for?
Used to treat meningitis due to haemophilus, neisseria, and strep.
What is the side effect of chloramphenicol?
1) Aplastic anemia (dose independent)
2) Bone marrow depression: granulocytopenia, leukopenia
3) Gray baby syndrome (in premature infants because they lack liver UDP-glucuronyl transferase)
What is linezolid?
Antibiotics used to treat resistant bacteria such as MRSA, VISA, and VRE
What is unique about linezolid?
It is a weak monoamine oxidase inhibitor, so patients should avoid tyramine rich foods and drugs with seretonergic and/or adrenergic effects.
What are Streptogramins?
They consist of quinopristin-dalfopristin and used in MRSA, VRE, and pencillin-resistant pneumococci.
What is the mechanism of action of streptogramins?
blocks 50 S ribosomal unit.
What is the toxicity of streptogramins (quinopristin-dalfopristin)?
Potent inhibitor P450 enzyme and increases QT interval.
What are some examples of macrolides?
erythromycin
azithromycin
clarithrymocyin
What is the mechanism of macrolides (erythromycin, azithromycin, clarithromycin)
Block 50 S ribosomal subunit. It is bacterostatic.
What are the clinical uses of erythromycin, azithromycin, and clarithromycin?
URIs, pneumonias, STDs: Mycoplasma, Legionella, Chlamydia, Neisseria.
what are the side effects of macrolides?
Gi discomfort, cholestatic hepatitis, skin rashes. All macrolides can cause ventricular tachycardia, QT prolongation, and torsades de pointes.
What are the macrolides effect on CY P450?
It can inhibit p450 strongly and increase serum concentration of theophyllines and oral anticoagulants.
This class of drug blocks cell wall synthesis by inhibition of peptidoglycan cross-linking
Penicillin, ampicillin, ticarcillin, piperacillin, imipenem, aztreonam, cephalosporins.
These drugs block peptidoglycan synthesis (NOT block peptidoglycan cross-linking)
Bacitracin and vancomycin
This class disrupts bacteria/fungal cell membranes
Polymyxins
Blocks nucleotide synthesis
Sulfonamides, trimethoprim
Blocks DNA topoisomerases
Quinolones
This class of drug blocks mRNA synthesis
Rifampin
These drugs block protein synthesis at 50S ribosomal subunits
Chloramphenicol, erythromycin/macrolides, lincomycin, clindamycin, linezolid, streptogramins (quinupristin, dalfopristin)
Block protein synthesis at 30 S ribosomal subunit
Aminoglycosides and tetracyclines
Bactericidal antibiotics
1) Penicillin
2) Cephalosporins
3) Vancomycin
4) Aminoglycosides (only one of the protein inhibitors)
5) Fluoroquinolones
6) Metronidazole
What is a bacteriocidal?
Antibiotic that kills the bacteria with the host immune system NOT required for bacterial killing.
What is a bacteriostatic?
An antibiotic that stops the growth of the bacteria, allowing the host immune system to fight bacteria more efficiently.
What is a transpeptidase?
It is a penicillin-binding protein that cross links peptidoglycan subunits to the bacterial cell wall.
What do Beta-Lactam drugs do?
They bind to PBPs covalently and prevent its action. They also activate endogenous autolysins that degrade the cell wall.
What is the key side effect of cell wall inhibitors?
Allergic reaction with rash.
What is the IV form of penicillin?
Penicillin G
What is the oral form of penicillin?
Penicillin V
What is the mechanism of penicillin?
1) Binds transpeptidase (PBP)
2) Blocks transpeptidase cross-liking of cell wall
3) Activate endogenous autolysins
What are the indications for penicillin use?
1) Gram +
2) Gram negative cocci
3) Streptococcus
4) Syphilis
5) Neisseria meningitidis
6) Clostridium specieis
What is the toxicity associated with penicillin use?
Hypersensitivity reactions and hemolytic anemia.
What is the action of probenecid?
Inhibits renal tubular excretion of penicillin, thus increases the systemic concentration of antibitioc.
What is the mechanism of action of methicillin, nafcillin, oxacillin?
1) Binds Pencillin binding protein
2) inhibits its cross-linking action
3) activates endogenous autolysis
4) Penicillinase resistant because of bulkier R group.
What is the indication to use methicillin, nafcillin, oxacillin?
Staph aureus. (Except MRSA: MRSA is resistant due to altered transpeptidase target site)
What is the toxicity of methicillin?
interstitial nephritis
What is toxicity of nafcillin, dicloxacillin?
Hypersensitivity reactions!
How should Beta-lactam antibiotics be dosed in patients with renal failure?
Almost all the Beta-lactam antibiotics are excreted by kidneys, so in patients with renal failure, the doses need to be lowered.
What are some mechanisms of resistance to Beta-lactam?
1) Beta-lactamase enzyme cleaving the beta-lactam ring
2) Decreases permeability of cell wall or outer membrane
3) Increased production of penicillin binding proteins.
4) Mutation of penicillin binding proteins to decrease affinity for beta-lactam ring.
What is the mechanism of action of ampicillin, amoxicillin?
Same as penicillin, but also penicillinase sensitive. Must combine with clavulanic acid (penicillinase inhibitor) to enhance action
Which has greater bioavailability ampicillin or amoxicillin?
amOxicillin.
When is amoxicillin used?
Used before dental procedures for patients at risk for bacterial endocarditis.
What is the clinical use of amoxicillin and ampicillin?
HELPS kill enterococci
1) Haemophilus influenzae
2) E. coli
3) Listeria monocytogenes
4) Proteus mirabilis
5) Salmonella
6) Enterococci
Side effects of ampicillin and amoxicillin?
Hypersensitivity reactions; ampicillin rash, and pseudomembranous colitis. Rashes and diarrhea are more common with ampicillin/amoxicillin than with other penicillins especially if given to patient with mononucleosis.
What is the action of ticarcillin, carbenicillin, and piperacillin?
Same as penicillin. TCP: Take care of pseudomonas?
What is piperacillin used to treat?
Pseudomonas
What is carbenicillin used to treat?
Pseudomonas
What is tarcacillin used to treat?
Pseudomonas
What are the side effects of anti-pseudomonals?
Ticarcillin, carbenicillin, and piperacillin can cause hypersensitivity, metabolic alkalosis, and platelet dysfunciton.
What are some examples of beta-lactamase inhibitors?
Clavulanic acid, sulbactan, tazobactam
What is mechanism of action of clavulanic acid, sulbactam, tazobactam?
Binds to Beta-lactamase catalytic site preventing degradation of beta-lactam antibiotics. It can also bind to PBP enhancing its action. **Note, these drugs are NOT antibacterial if used alone.
What are cephalosporins?
Beta-lactam drugs that inhibit cell wall synthesis but are less susceptibile to penicillinases. Bactericidal.
What are the first generation cephalosporins?
Cefazolin, Cephalexin
What are the 2nd generation cephalosporins?
Cefoxitin, Cefaclor, Cefuroxime
What are 3rd generation cephalosporins?
Ceftriaxone, Cefotaxime, Ceftazidime; TRI TAX TAZ
What are some 4th generation cephalosporins?
Cefepime, Cefpiramide
What is indication for 1st generation cephalosporins (cefazolin, cephalexin)?
Gram positive cocci: PEcK
1) Proteus mirabilis
2) E. coli
3) Klebsiella
What is indication for 2nd generation (cefoxitin, cefaclor, cefuroxime)?
FAC that FOX has FUR
HEN PEcKs
1) Haemophilus
2) Enterobacter
3) Neisseria
4) Proteus
5) E. coli
6) Klebsiella
7) Serratia
Which class is th eonly active ones against Bacteroides?
2nd generation cephalosporins (Cefoxitin, Cefotetan)
What are the cephalosporins of choice to treat gonorrhea?
Ceftriaxone and Cefixime
Which of the cephalosporins can cause a disulfuram like reaction?
Cefotetan (2nd generation)
Which are the only cephalosporins effective against P. aeruginosa?
Ceftazidime and cefepime
What are some side effects of ceftriaxone?
Gallstones and increase in PT time due to inhibition of Vitamin K-dependent clotting factor synthesis.
What are the fourth generation drugs like cefepime and cefpiramide used for?
Increased activity against Pseudomonas and gram-positive organisms
What do 3rd generation cephalosporins cover?
HEN PEcKs
1) Haemophilus influenzae
2) Enterobacter
3) Neisseria
4) Proteus
5) E.coli
6) Klebsiella
7)Serratia

Can treat meningitis because most penetrate the blood-brain barrier.
What are the 3rd generation cephalosporins?
Ceftriaxone, Ceftazidime, Cefotaxime.
What is the toxicity of cephalosporins?
Hypersensitivity reactions. Cross-hypersensitivity with penicillins in 5-10% of patients. Have increased nephrotoxicity of aminoglycosides; disulfuram-like reaction with ethanol.
What is aztreonam?
It is an alternative to aminoglycosides and can be used in patients with penicillin allergy. Its a synergistic effect with aminoglycosides.
What is aztreonam used for?
Limited to gram negative aerobes! Has no activity vs gram positive or anaerobes.
What is the mechanism of action of aztreonam?
Gram negative aerobes ONLY
Inhibits cell wall synthesis by binding to PBP
It is resistant to B-lactamases
When can aztreonam be used?
Gram negative aerobes! Can be used in patients with renal failure who cannot tolerate aminoglycosides or in patients with penicillin allergy.
What is imipinem?
Broad specturem, Beta-lactamase resistant carbapenem. Always administered with cilastatin to decrease inactivation in renal tubules.
Why is cilastatin used with imipinem?
Cilastin is an inhibitor of renal dihydropeptidase I to decrease imipinems inactivation in renal tubules.
What is the drug of choice for Enterobacter?
Imipinem
What is action of imipinem?
Broad spectrum and drug of choice for enterobacter. Reserved for serious mixed polymicrobial infections in with aerobes and anaerobes are involved.
Toxicity of imipinem?
Skin rash. CNS toxicity (seizures) at high plasma levels.

Remember: they are Beta-lactamase resistant!
What is vancomycin mechanism of action?
Blocks peptidoglycan synthesis. It binds D-ala D-ala portion of cell wall precursors preventing peptidoglycan formation.
How do bacteria become resistant to vancomycin?
They change their D-ala D-ala to D-ala D-lac to prevent vancomycin binding. (i.e. Vancomycin resistant enterococci)
What is vancomycin used for?
Reserved for serious infections by MRSA and C. dificile. It is 2nd choice for pseudomembranous colitis.
What is vancomycin toxicity?
nephrotoxicity, ototoxicity, thrombophlebitis, diffuse flushing "red man syndrome"
Red man syndrome can be prevented by pretreatment with antihistamines and slow infusion rate.
What are the 30 S Protein inhibitors?
Aminoglycosides (streptomycin, gentamicin, tobramycin, amikacin)

Tetracyclines (bacteriostatic)
Are aminoglycosides bacteriostatic or bactericidal?
Bactericidal. Only one of the protein synthesis inhibitors that are bactericidal. --> streptomycin, gentamicin, tobramycin, amikacin.
What are the 50 S protein synthesis inhibitors?
Chloramphenicol,
Erythromycin (macrolides)
Lincolmycin
Clindamycin
What are some examples of aminoglycosides?
Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin "Mean GNATS canNOT kill anaerobes"
What is mechanism of action of aminoglycosides?
Bind to 30 s subunits and interfere with protein synthesis
What is unique to aminoglycosides?
They require oxygen for uptake, so Can NOT be used for anerobic infection. They are synergistic with Beta-lactams and Aztreonam.
2) Also has a post-antibiotic effect: antibacterial killing can continue after serum drug concentration declines below minimum inhibitory concentration.
what is neomycin used for?
Bowel surgery
What agents are used for plague and tularemia?
Streptomycin
What is the aminoglycoside toxicity?
Nephrotoxicity with Cephalosporins
Ototoxicity with loop diuretics
Teratogen.
What are the tetracycline classes?
Tetracycline, doxycycline, demeclocycline, and minocycline.
What is action of tetracyclines?
It binds to 30S and prevents protein synthesis. Has limited CNS penetration.
Which tetracycline can be used in renal failure?
Doxycycline because it is excreted in feces.
What are some contraindications with taking doxycyline?
Can NOT take with milk, antacids, or iron-containing preparations because divalent cations inhibits its absorption in the gut.
What are the clinical uses of tetracyclines?
VACUUM THe BedRooom
1) Vibrio
2) Acne
3) Chlamydia
4) Ureplasma Urealyticum
5) Mycoplasma pneumoniae
6) Tularemia/H.pylori
7) Borrelia
8) Ricketssia
What is the toxicity of tetracyclines?
Gi distress, discoloration of teeth, growth inhibition in children, and photosensitivity. ABOSLUTELY CONTRAINDICATED IN PREGNANCY.
What is special about the tetracycline demeclocycline?
It is an ADH antagonist, so can act as a diuretic in SIADH.