Antibiotics (Bbd Exam 1)

Front 1

Carbapenems
(common Rx)

Back 1

1. Impinem
2. Meropenem
3. Ertapenam

Front 2

Carbapenems
(spectrum)

Back 2

1. Excellent gram pos, gram neg, anaerobic
2. No coverage against MRSA
3. Need combination therapy with aminoglycosides for enterococcus coverage
4. Ertapenem - not as effective with pseudomonas
5. Watch for emerging carbapenamase

Front 3

Carbapenem
(toxicities)

Back 3

1. Typical (nausea/vomiting)
2. If pt is allergic to penicillin, prob allergic to carbapenem too
3. Seizures (esp in pts with renal failure)

Front 4

Monobactam
(common Rx)

Back 4

1. Aztreonam

Front 5

Monobactam - Aztreonam
(spectrum)

Back 5

1. Only gram neg! (E. coli, K. pneumoniae, Pseudomonas aeruginosa)
2. No gram pos or anaerobes!
3. No cross-reactivity with beta-lactams (can use for pts with severe rxns to penicillins)

Front 6

Beta-Lactam Antibiotics
(classes)

Back 6

1. Penicillins
2. Cephalosporins
3. Carbapenems
4. Monobactams

Front 7

Glycopeptides
(common Rx)

Back 7

1. Vancomycin (IV/po)

Front 8

Glycopeptides - Vancomycin
(mechanism of action)

Back 8

1. binds D-Ala-D-Ala terminus of PG precursor (1 step earlier than beta-lactams) and prevents cross-linking of bacterial cell wall

Front 9

Glycopeptides - Vancomycin
(pharmakinetics)

Back 9

1. Not absorbed; stays in the gut lumen
2. used to treat C. diff

Front 10

Glycopeptides - Vancomycin
(spectrum)

Back 10

1. BROAD gram pos (KILLS MRSA!)
2. NO gram neg
3. watch for VRE
4. new Staph aureus are becoming resistant to vanco (rare though)
5. Still need combo therapy with aminoglycoside to kill enterococci

Front 11

Vancomycin
(Toxicities)

Back 11

1. Red Man Syndrome (red rash on face, chest, and neck with pruritis and hypotension) - if this happened in the past... its ok, just slow IV push and give prophylactic anti-histamines
2. Rxn to IV vanco
3. Leukopenia

Front 12

Folic-acid-synthesis inhibitors
(common Rx)

Back 12

1. Sulfonamides
2. DHF Reductase Inhibitors (Trimethoprim and Pyrimethamine)

Front 13

Folic-acid-synthesis inhibitors
(mechanism of action)

Back 13

1. Inhibit nucleaic acid synthesis
2. some are PABA analogues (sulfonamides)
3. some inhibit DHF reductase (Trimethoprim)

Front 14

Folic-acid-synthesis inhibitors
(spectrum of Bactrim)

Back 14

TMP/Sx
1. Cover gram pos (including MRSA)
2. No GAS coverage or enterococci
3. OK gram neg
4. jirovecii coverage
5. covers nocardia, listeria, stenotrophomonas

Front 15

Bactrim

Back 15

1. Combination of Sulfamide/trimethoprim
2. Covers E. coli, UTIs,
3. Adverse Rxns (toxicities) HYPERKALEMIA and kernicterus in infants, Stevens Johnson Syndrome

Front 16

Penicillins
(mechanism of action)

Back 16

1. Inhibit TRANSPEPTIDATION of PG sheet in bacterial cell wall
2. Penicillin binds to PBP (penicillin binding protein, thus inhibiting synthesis

Front 17

Natural Penicillins
(common Rx)

Back 17

1. Penicillin G (IV)
2. Penicillin V (po)
3. Procaine Penicillin (IM) - anaesthetic, slow absorption, 24 hrs therapeutic levels
4. Benzathine Penicillin (IM) - 1 week therapeutic levels

Front 18

What else is Homocystiene Methyl Transferase needed for?

Back 18

Nucleotide synthesis

Front 19

Penicillin
(spectrum)

Back 19

1. Great coverage of GAS
2. Bad Streptococcus pneumoniae coverage
3. Need combo with aminogoycoside to kill enterococci
4. few gram neg coverage (no gonorrhoeae coverage - too resistant)
5. Pneumococcus (major resistance problems)
6. Used to treat dental abscesses
7. Kills Spirochetes (syphilis)
8. Only RARE Stapholococci are susceptable to Penicillin (usually they produce penicillinase)
9. No coverage for enterococci

Front 20

Anti-Staph Penicillin
(common Rx)

Back 20

1. Methicillin
2. Nafcillin, Oxacillin (IV)
3. Decloxacillin (po)

Front 21

How would you treat uncomplicated cellulitis?

Back 21

1. Rx - Nafcillin, oxacillin, dicloxacillin (b/c - Staph aureus and GAS commonly cause cellulitis... these agents cover both of these

Front 22

Methicillin
(random facts)

Back 22

1. first Anti-Staph antibiotic developed
2. not used anymore b/c of nephrotoxicity

Front 23

Aminopenicillins
(common Rx)

Back 23

1. Ampicillin (IV)
2. Amoxicillin (po)

Front 24

Aminopenicillins
(spectrum)

Back 24

1. Retain coverage of natural penicillins, but gain coverage of LISTERIA **test question**
2. Cover some simple community gram neg (E. coli, Proteus, Haemophilus influenzae

Front 25

Anti-Pseudomonal Ureidopenicillins
(common Rx)

Back 25

1. Ppeeracillin (IV)
2. Ticarcillil (IV)

Front 26

Anti-Pseudomonal Ureidopenicillins - Piperacillin, Ticarcillin
(spectrum)

Back 26

1. Similar to ampicillin with added gram neg coverage (nosocomial coverage) - covers Pseudomonas, Enterobacter, Acinetobacter
2. *Quirk* Ticarcillin NOT useful against enterococcus
3. Both are susceptable to beta-lactamases and have poor staph activity
4. Cover gram neg anaerobes (below the diaphragm

Front 27

Beta-Lactamase Inhibitors
(common Rx)

Back 27

1. Used in combination with Ampicillin, Amoxicillin, Piperacillin, and Ticarcillin
2. Common Rx - sulbactam (IV), clavulanate (po), and tazobactam (IV)

Front 28

Beta-Lactamase Inhibitor combination coverate

Back 28

**increases as you go down**
1. amp/sulb
2. amox/clav
3. piper/tazo
4. ticar/clav

Front 29

Name the 3 types of inhibitors of bacterial protein synthesis (function of antibiotics)

Back 29

1. Inhibitors of amino acid t-RNA synthetase
2. Inhibitors of peptide initiation reactions
3. Inhibitors of peptide bond formation and elongation

Front 30

Rifampin
(mechanism of action)

Back 30

1. Binds to beta chain of bacterial RNA polymerase (not in our eukaryotic cells)
2. Wide spectrum (but resistance happens quickly) - so we rarely use them

Front 31

Rifampin
(pharmacology)

Back 31

1. taken orally (po)
2. Wide tissue distribution
3. t 1/2 - 1.5 to 5. hrs
4. colors body fluids (should warn pt) **gatorade sweat**

Front 32

Rifampin
(toxicities)

Back 32

1. Rash, fever, GI, hepatotoxicity
2. DRUG INTERACTIONS (they induce P450s and effect metabolism of other drugs like digoxin, coumadin, methadone, and oral contraceptives

Front 33

Rifampin
(clinical uses)

Back 33

1. Useful treatment of TB and leporsy
2. Prophylaxis against meningococcal and H. influenzae meningitis (as monotherapy only)
3. can be combined with other agents against "tolerant" organisms

Front 34

Clofazimine
(mechanism of action)

Back 34

1. Inhibits RNA polymerase

Front 35

Clofazimine
(pharmacology)

Back 35

1. only 50% oral absorption
2. slowly excreted in feces
3. LONGEST T 1/2 OF ANY DRUG (70 days)
4. very slow to act - can take 2 years to life

Front 36

Clofazimine
(toxicities)

Back 36

1. GI, stains skin red (don't confuse with "Red Man Syndrome"

Front 37

Quinolone
(mechanism of action)

Back 37

1. Inhibits DNA synthesis by inhibiting DNA GYRASE (TOPOISOMERASE II OR IV)
2. induce negative supercoils

Front 38

Quinolones - Naldixic acid

Back 38

1. First developed
2. Poor tissue penetration
3. Rarely used
4. Prob not on test... so why did I make this flashcard?

Front 39

Fluoroquinolones
(common Rx)

Back 39

1. Ciprofloxacin (prototype)
2. norfloxacin
3. Ofloxacin
4. Levofloxacin

Front 40

Fluoroquinolones
(pharmacology)

Back 40

1. t 1/2 - 5 to 8 hrs
2. Well absorbed orally
3. High tissue and intracellular levels

Front 41

Fluoroquinolones
(clinical uses)

Back 41

Useful in treatment of...
1. UTI's
2. Chronic suppurative infections
3. CF
4. Mycobacterium
5. bacterial gastroenteritis
6. common pneumonia
7. RESISTENT GRAM NEGATIVE **KNOW THIS FOR EXAM** - Fluoroquinolones are only used for SERIOUS infections

Front 42

Fluoroquinolones
(toxicities)

Back 42

1. GI, may interfere with cartilage formation, prolonged QT interval
2. Resistance develops
3. Use with caution in children

Front 43

Metronidazole (Flagyl)
(mechanism of action)

Back 43

1. Forms a highly reactive O2 species that binds to DNA and destroys it

Front 44

Metronidazole
(pharmacology/toxicities)

Back 44

1. t 1/2 - 8 hrs
2. Diffuses well into all tissues
3. Rare Toxicities (GI, siezures, peripheral neuropathy,
4. NO ALCOHOL USE WITH THIS

Front 45

Metronidazole
(clinical uses)

Back 45

Useful for treatment of
1. Trichomonal infections
2. amebiasis
3. giardiasis
4. C. diff
5. anaerobic bacterial infections
6. H. pylori
7. rosacea (with topical gel)

Front 46

Linezolid (zyvox)
(mechanism of action)

Back 46

1. Binds the 50S subunit
2. Inhibits formation of f-Met-tRNA

Front 47

Linezolid (zyvox)
(pharmacology)

Back 47

1. 100% oral absorption
2. t 1/2 - 4 to 6 hrs

Front 48

Linezolid (zyvox)
(clinical uses, tox)

Back 48

1. covers gram pos cocci (even bacteria that are normally resistant, such as E. fecium, VRE, MRSA
2. Seratonin syndrome in those taking SSRIs

Front 49

Mupirocin
(mechanism of action)

Back 49

1. inhibits isoleucyl tRNA synthetase

Front 50

Mupirocin
(clinical uses)

Back 50

1. Used topically for skin infections (pyoderma or impetago
2. covers S. aureus and S. pyogenes (Beta-hemolytic strep)

Front 51

What antibiotics inhibit the initiation complex?

Back 51

1. Aminoglycosides
2. Tetracyclines

Front 52

Aminoglycosides
(mechanism of action)

Back 52

1. inhibits the binding of aminoacyl tRNA to the 30S subunit to form the initiation complex

Front 53

Aminoglycosides
(pharmacology)

Back 53

1. Polar drug (only absorbed in ECF - only penetrates that CSF in neonates)
2. Renal elimination
3. t 1/2 - 2 to 3 hrs (prolonged by renal insufficiency

Front 54

Aminoglycosides
(clinical uses)

Back 54

Useful in treatment of...
1. GRAM NEG INFECTIONS
2. Endocarditis
3. combination therapy with serious infections
4. Topical forms available
5. Oral forms used to "sterilize the gut" before surgery
6. Spectinomycin only used for gonorrhea
7. Gentamycin drops used for eye inffections

Front 55

Aminoglycosides
(toxicities)

Back 55

1. Ear (cochlear and vestibular damage IRREVERSABLE
2. Renal - reversable
3. Neuromuscular blockage - reversed by calcium

Front 56

Tetracyclines
(mechanism of action)

Back 56

1. Binds the 30S subunit and prevents tRNA attachment to the A site

Front 57

Tetracyclines
(pharmacology)

Back 57

1. used both (po) and (IV)
2. Oral absorption lessened by food (binds calcium)
3. Wide distribution
4. Wide range of t 1/2 (2-4 for tetracycline and 16-18 for oxycycline or minocycline)

Front 58

Tetracyclines
(clinical use)

Back 58

1. Wide spectrum (covers gram pos, gram neg, mycoplasma, rickettsia
2. recently replaced with safer antibiotics
3. NOW COMMONLY USED FOR LYME DISEASE AND ACNE **know this for exam**

Front 59

Tetracyclines
(toxicity)

Back 59

1. uptake into growing bone
2. Phototoxicity
3. Renal disease
4. Liver disease
5. increases IC pressure in infants

Front 60

What antibiotics inhibit peptide bond formation and elongation?

Back 60

1. Chloramphenicol
2. Clindamycin
3. Macrolides

Front 61

Chloramphenicol
(mechanism of action)

Back 61

1. Binds 50S subunit and inhibits peptidyl synthetase (thing that binds the AAs together)
2. Toxicities - Grey baby syndrome (Chloramphinicol, if not bound to an inactive monoglucuronide is cardiotoxic and causes a weak, thready pulse)

Front 62

Clindamycin
(mechanism, pharmocology, and toxicity)

Back 62

1. Causes dissociation of the peptidyl-tRNA from the ribosome - stops protein synthesis
2. GREAT po absorption, widely distributed
3. t 1/2 - colitis, diarrhea (if this happens... d/c right away)

Front 63

Clindamycin
(clinical uses)

Back 63

Useful in treatment of...
1. gram pos, and ANAEROBES
2. Gram pos (ok for beta lactam allergic pts.)
3. combo therapy for streptococcal infections
4. Bacteriodes

Front 64

Clindamycin
(toxicities)

Back 64

1. skin rashes, psuedomembranous colitis with C. diff infection (can be deadly)

Front 65

Macrolides
(common Rx)

Back 65

1. Erythromycin
2. Clarithromycin
3. Azithromycin
4. Ketolides

*these all have lactone rings*

Front 66

Erythromycin
(mechanism of action)

Back 66

1. Inhibits translocase (the movement of the aminoacyl-tRNA from the A site to the P site)

Front 67

Erythromycin
(spectrum)

Back 67

Useful in treatment of...
1. gram pos cocci
2. mycoplasma
3. Legionnaires bacillus
4. pertussis
5. tetanus
6. Campylobacter

Front 68

Erythromycin
(pharmocology)

Back 68

1. given (po)
2. t 1/2 - 1.6 hrs
3. unstable in stomach pH
4. Diffusion to TBW, poor CSF penetratoin
5. Excreted through biliary tract

Front 69

Erythromycin
(clinical use)

Back 69

Useful for treating...
1. Gram pos infections (for those allergic to Penicillins)
2. Mycoplasma
3. Impetigo (staph and strep)
4. Legionnaire's bacillus
5. Pertussis (especially carriers

Front 70

Erythromycin
(toxicity)

Back 70

1. GI, hepatitis, INHIBITS P450s (affecting cyclosporing, warfarin, cyclosporine, carbamazepine)
2. These toxicities may lead to DEATH

Front 71

pick up at...

Back 71

Other macrolides

Front 72

Clindamycin
(toxicities)

Back 72

1. skin rashes, psuedomembranous colitis with C. diff infection (can be deadly)

Front 73

Macrolides
(common Rx)

Back 73

1. Erythromycin
2. Clarithromycin
3. Azithromycin
4. Ketolides

*these all have lactone rings*

Front 74

Erythromycin
(mechanism of action)

Back 74

1. Inhibits translocase (the movement of the aminoacyl-tRNA from the A site to the P site)

Front 75

Erythromycin
(spectrum)

Back 75

Useful in treatment of...
1. gram pos cocci
2. mycoplasma
3. Legionnaires bacillus
4. pertussis
5. tetanus
6. Campylobacter

Front 76

Erythromycin
(pharmocology)

Back 76

1. given (po)
2. t 1/2 - 1.6 hrs
3. unstable in stomach pH
4. Diffusion to TBW, poor CSF penetratoin
5. Excreted through biliary tract

Front 77

Erythromycin
(clinical use)

Back 77

Useful for treating...
1. Gram pos infections (for those allergic to Penicillins)
2. Mycoplasma
3. Impetigo (staph and strep)
4. Legionnaire's bacillus
5. Pertussis (especially carriers

Front 78

Erythromycin
(toxicity)

Back 78

1. GI, hepatitis, INHIBITS P450s (affecting cyclosporing, warfarin, cyclosporine, carbamazepine)
2. These toxicities may lead to DEATH

Front 80

Other Macrolides
(common Rx)
**from other substitutions on the lactone ring**

Back 80

1. clarithromycin
2. azithromycin
3. Telithromycin (Ketek)

Front 81

Azithromycin
(pharmacology)

Back 81

1. t 1/2 - 70 hrs
2. accumulates in WBCs and tissues
3. dosing prevents noncompliance (by dosing less frequently) *this also helps with fighting resistance*
4. great absorption... resists degredation in low pH of the stomach

Front 82

Telithromycin (Ketek)
(mechanism of actoin)

Back 82

1. Binds to 2 regions of the ribosome (making it very difficult for bacteria to overcome this - or become resistant

Front 83

Telithromycin
(pharmacology, clinical use, toxicities)

Back 83

1. Once daily dosing, inhibits P450s (watch drug interactions)
2. Used to treat respiratory pathogens
3. Hepatotoxicity issues

Front 84

Macrolides
(other clinical uses)

Back 84

...Just have an idea for these
1. community acquired pneumonia
2. ear/sinus infections
3. pharyngitis
4. chlamydia/gonorrhea
5. Mycobacterium avium in HIV pts
6. skin and soft tissue infections

Front 85

D/Q (Synercid)
What is it?

Back 85

1. a 30:70 ratio of Dalfopristin/Quinupristin

Front 86

D/Q
(mechanism of action)

Back 86

1. Dalfopristin - binds nearby and deforms 50S subunit (enhances Quinupristin binding)
2. Quinupristin - binds at the same site as macrolides

Front 87

D/Q
(pharmacology, clinical uses)

Back 87

1. IV only!
2. t 1/2 - 1 hour for both
3. biliary excretion
4. inhibits P450 enzymes
5. Treats VRE and staph and strep skin infections

Front 88

Which antibiotics would you you use to treat Tuberculosis?
(top 4 first line drugs)

Back 88

1. isoniazid*** (not MDR or XDR)
2. rifampin*** (not MDR or XDR)
3. ethambutol
4. pyrazinamide

Front 89

Isoniazid (INH)
(mechanism of action)

Back 89

1. inhibits the biosynthesis of mycolic acids (that are unique to mycobacterium cell wall)
2. Vit B6 analogue

Front 90

Isoniazid (INH)
(pharmacology)

Back 90

1. **only drug that you have to consider genetics of drug metabolism to prescribe the correct dose**
2. Given (po)
3. Saturates CSF

Front 91

Isoniazid
(toxicity)

Back 91

1. hepatitis
2. peripheral neuropathy (because when you give a B6 analogue, bacteria will "steal" the readily available B6 that our tissues would normally use... so we supplement with B6 when using isoniazid to prevent this complication)
3. optic nerritis

Front 92

Rifampin
(clinical uses)

Back 92

1. Treats all classes of Leprosy (Tuberculiod, Borderline, Lepromatous, Indeterminate)

*like dapsone*

Front 93

Dapsone
(clinical uses)

Back 93

1. Treats all classes of Leprosy (Tuberculiod, Borderline, Lepromatous, Indeterminate)

*like rifampin*

Front 94

Dapsone
(mechanism of action, pharmacology)

Back 94

1. similar to sulfonamides - PABA analogue
2. Rapidly and completely absorbed in the GI, t 1/2 - 20 to 30 hrs
3. Metabolized by acetylation by the same enzyme that acetylates isoniazid

Front 95

Name the 1st through 4 generations of cephalosporins...

Back 95

1st - (cefazolin, cephalexin)
2nd - (cefuroxime, cefoxitin)
3rd - ceftriaxone, cefotaxime, ceftazidime)
4th - (cefepime)

Front 96

Discuss the general trend of cephalosporins with regard to their coverage...

Back 96

1st generation of cephalosporins covers minimal gram neg, but great gram positive... 2nd through 4th generation covers gram neg progressively better, but progressively less coverage for gram pos (cefepime has no gram pos coverage)

Front 97

1st generation cephalosporins
(spectrum)

Back 97

1. covers gram positives (including MSSA, GAS
2. covers community acquired gram neg rods (aerobic only)

**NO MRSA or enterococcus**

Front 98

1st generation cephalosporins
(clinical uses)

Back 98

**cefazolin, cephalexin**
1. used to treat uncomplicated cellulitis (S. aureus, GAS)
2. Open heart surgery prophylaxis

Front 99

2nd generation cephalosporins
(common Rx)

Back 99

1. cefuroxime (IV/po)
2. cefoxitin (IV)

Front 100

2nd generation cephalosporins
(spectrum)

Back 100

1. ***unique feature*** - decent ANAEROBIC coverage in addition to expected spectrum

**NO MRSA or enterococci**

Front 101

3rd generation cephalosporins
(common Rx)

Back 101

1. Cefatriaxone (IV)
2. cefotaxime (IV)

Front 102

3rd generation cephalosporins
(spectrum)

Back 102

1. ***unique feature*** - cefatriaxone can cross the BBB! So they can be used to treat CNS infections such as meningitis
2. this is in addition to the expected spectrum trends
3. ceftazidime (not really discussed at length) has broader gram neg coverate (pseudomonas), but there are major resistance problems

Front 103

Clinical corrleate...

An adult pt's CSF is infected with bacterial meningitis (S. pneumoniae or N. meningitides)... what drug would you prescribe?

Back 103

Answer
Ceftriaxone - because it crosses the BBB and has good gram neg coverage

Front 104

4th generation cephalosporins
(common Rx)

Back 104

1. Cefipime

Front 105

4th generation cephalosporins
(spectrum)

Back 105

1. **also crosses BBB, but use is limited b/c a narrower spectrum agent is also useful
2. NO MRSA or enterococci still
3. VERY broad gram neg, including PSEUDOMONAS and other nosocomial infections

Front 106

Clinical correlate...

Nosocomial aspiration pneumonia can be caused by Pseudomonas, Enterobacter, Klebsiella, Acinetobacter and other drug-resistant gram negatives... What agent would you select for antibiotic therapy?

Back 106

1. Cefepime

Front 107

Cephalosporins
(toxicities)

Back 107

1. **5-10% cross-allergenicity between penicillins and cephalosporins (if pt had severe rxn to penicillins... don't use, otherwise it is probably OK)**
2. other typical antibiotic toxicities (Nausea, GI upset, biliary sludging), but generally well tolerated