Antibiotic Agents Interfering with DNA and Protein Synthesis

Question 1

Aminoglycosides (streptomycin, gentamicin, tobramicin, amikacin, neomycin, kanamycin)
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 1

Target and job: inhibits 30s ribosomal subunit
Static vs. Cidal: Bacterialcidal
Spectrum of action: Gram neg
Predominant Uses: Only class with post antibiotic effect
Problems:
1. None can be used orally due to its structure (has an amino part and a glycoside (sugar) part. stupid soluble, positively charges and physiological pH and absorbed, and super polar. so will not cross membranes from the gut. Will be excreted entirely).
2. Nephrotoxicity: They all can barely be metabolised through the kidney. They build up and toxicate the kidney if taken for more than 5 days. Neomycin and tobramycin are the most toxic…neomycin is so troxic it isn’t used systemically. Luckily all the renal damage done by these drugs can be reversed if you stop using these drugs.
3. Ototoxicity (ear): they cause ear damage. Most prominant if taken more than 5 days. can result in loss of hearing to high frequency sounds and tinnitus (ringing)…which may not go away. Can also cause vestibular damage (ability to keep balance)…leading to ataxia and vertigo. Neomycin, kanamycin, and amikacin cause most auditory damage. Streptomycin and gentamicin cause most vestibular damage. Ototoxicity = nerve cell damage. as a result, the damage done by these drugs is irreversible. Never cells can never be replaced.

Question 2

Tetracyclines (tetracycline, demeclocycline, minocycline, doxycycline, oxytetracycline, tigecycline, eracacycline
Half life:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 2

Half life: The only differentiating factor between all these tetracyclines, as they all have the same amount of effect. Reason for concern with half-life is the amount of dosing since compliance is an issue (if patient does not comply, the drug’s effects will be weak…you need drugs that last longer so that you only need to take it once a day). Doxycycline and minocycline are the prescribed choice for this reason.
Target and job: inhibits 30s ribosomal subunit.
Static vs. Cidal Bacteriostatic
Spectrum of action: Prevents the aminoacyl-tRNA that carries the AA from reaching the ribosome, so new AA cannot be added to the chain (elongation blocker). Have broader spectrum (gram neg, gram pos, aerobic, and anaerobic.)
Note: All these drugs can be taken orally or via IV (stupid quick). Also, take these before you eat since food makes the amount of the drug you can get into the blood stream LESS. reason: cations with charges grater than +1 (metals such as Fe…Ca (dairy)). CUT DAIRY FROM YOUR DIET WHEN USING THESE DRUGS. Antacids also are a no go with these drugs for the same reason.

Question 3

Macrolides (erythromycin, clarithomycin, azithromycin, telithromycin)

Answer 3

Target and job: inhibits 50s ribosomal subunit.
Static vs. Cidal:
Spectrum of action:

Question 4

Lincosamide (clindamycin)

Answer 4

Target and job: inhibits 50s ribosomal subunit.
Static vs. Cidal:
Spectrum of action:

Question 5

Stretogramins (Quinupristin/dalfopristin)

Answer 5

Target and job: inhibits 50s ribosomal subunit.
Static vs. Cidal:
Spectrum of action:

Question 6

Oxazolidinone (Linezolid)

Answer 6

Target and job: inhibits 50s ribosomal subunit.
Static vs. Cidal:
Spectrum of action:

Question 7

streptomycin
Class of drug:
Target and job:
Static vs. Cidal: 
Spectrum of action:
Predominant Uses:

Answer 7

Class of drug: Aminoglycoside
Target and job: inhibits 30s
ribosomal subunit
Static vs. Cidal: Bacterialcidal
Spectrum of action: Gram neg. Drug is old, resistance to it is pretty high, BUT it is used in combination regimines for resistance strains. Still only for Tb.
Predominant Uses: second line agent for tuberculosis treatment

Question 8

gentamicin, tobramicin
Class of drug:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:

Answer 8

gentamicin, tobramicin
Class of drug: Aminoglycoside
Target and job: inhibits 30s
ribosomal subunit
Static vs. Cidal: Bacterialcidal
Spectrum of action: Gram neg. Used in combo with beta lactams to end cell wells. The two drugs are synergistic.
Predominant Uses: Life threatening cases of sepsis (systemic infection) or gram negative bacteria infections. Gentamycin is use more frequently since it its cheaper

Question 9

amikacin
Class of drug:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:

Answer 9

Class of drug: Aminoglycoside
Target and job: inhibits 30s
ribosomal subunit
Static vs. Cidal: Bacteriocidal
Spectrum of action: Gram neg. Not as effective as gentamicin, tobramicin, but still hit everything that gentamicin and tobramicin cannot hit due to the bacteria having resistant enzymes against those two drugs.
Predominant Uses: Used when gentamicin or tobramicin fails to work

Question 10

neomycin, kanamycin
Class of drug:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:

Answer 10

neomycin, kanamycin
Class of drug: Aminoglycosides
Target and job: 30s subunit of bacterial ribosome
Static vs. Cidal: Bacteriocidal
Spectrum of action: Gram neg
Predominant Uses: Barely used since they are toxic. Kanamycin is prefered only when the others fail. Neomycin is not used at all. Both systemically. these guys are only used topically. Used as topical use (eye drops, and skin) (neosporin). All the drugs are super toxic…hence why only used topically, not systemically. Number one use for rickettesia infections, chlamydiae infections, and mycoplasmas. works against protozoa (eukaryotes). All these tetracyclines are just as effective, but they change in pharmakokinatics (how long drugs act when you take them). This is measured in half-lives.

Question 11

oxytetracycline
Half life:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 11

Half life: short (6-8 hours)
Class: Tetracycline
Target and job: inhibits 30s ribosomal subunit.
Static vs. Cidal Bacteriostatic
Spectrum of action: Prevents the aminoacyl-tRNA that carries the AA from reaching the ribosome, so new AA cannot be added to the chain (elongation blocker). Have broader spectrum (gram neg, gram pos, aerobic, and anaerobic.). Really good for STI’s (chlamydia…) and rickettsial infections, respiratory tract infections (pnemonia), skin and soft tissue infections (community staph, moderate to severe acne).
Note: GI disturbance and bony structures/teeth take the L. As in, DO NOT GIVE TO PEDIATRIC PATIENT. Can cause bone inhibition and the teeth become forever discolored. In addition, you have to stay out of the sun…tetracycline causes photosensitization. Can even cause liver disturbances.

Question 12

tetracycline
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 12

Half life: short (6-8 hours)
Class: Tetracycline
Target and job: inhibits 30s ribosomal subunit.
Static vs. Cidal Bacteriostatic
Spectrum of action: Prevents the aminoacyl-tRNA that carries the AA from reaching the ribosome, so new AA cannot be added to the chain (elongation blocker). Have broader spectrum (gram neg, gram pos, aerobic, and anaerobic.). Really good for STI’s (chlamydia…) and rickettsial infections, respiratory tract infections (pnemonia), skin and soft tissue infections (community staph, moderate to severe acne)
Note: GI disturbance and bony structures/teeth take the L. As in, DO NOT GIVE TO PEDIATRIC PATIENT. Can cause bone inhibition and the teeth become forever discolored. In addition, you have to stay out of the sun…tetracycline causes photosensitization. Can even cause liver disturbances..

Question 13

demeclocycline
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 13

Half life: intermediate (12 hours)
Class: Tetracycline
Target and job: inhibits 30s ribosomal subunit.
Static vs. Cidal Bacteriostatic
Spectrum of action: Prevents the aminoacyl-tRNA that carries the AA from reaching the ribosome, so new AA cannot be added to the chain (elongation blocker). Have broader spectrum (gram neg, gram pos, aerobic, and anaerobic.). Really good for STI’s (chlamydia…) and rickettsial infections, respiratory tract infections (pnemonia), skin and soft tissue infections (community staph, moderate to severe acne.
Note: GI disturbance and bony structures/teeth take the L. As in, DO NOT GIVE TO PEDIATRIC PATIENT. Can cause bone inhibition and the teeth become forever discolored. In addition, you have to stay out of the sun…tetracycline causes photosensitization. Can even cause liver disturbances.

Question 14

doxycycline
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 14

Half life: long (16-18 hours)
Class: Tetracycline
Target and job: inhibits 30s ribosomal subunit.
Static vs. Cidal Bacteriostatic
Spectrum of action: Prevents the aminoacyl-tRNA that carries the AA from reaching the ribosome, so new AA cannot be added to the chain (elongation blocker). Have broader spectrum (gram neg, gram pos, aerobic, and anaerobic.). Really good for STI’s (chlamydia…) and rickettsial infections, respiratory tract infections (pnemonia), skin and soft tissue infections (community staph, moderate to severe acne). Specifically used to treat lyme disease. Note: GI disturbance and bony structures/teeth take the L. As in, DO NOT GIVE TO PEDIATRIC PATIENT. Can cause bone inhibition and the teeth become forever discolored. In addition, you have to stay out of the sun…tetracycline causes photosensitization. Can even cause liver disturbances.

Question 15

minocycline
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 15

Half life: long (16-18 hours)
Class: Tetracycline
Target and job: inhibits 30s ribosomal subunit.
Static vs. Cidal Bacteriostatic
Spectrum of action: Prevents the aminoacyl-tRNA that carries the AA from reaching the ribosome, so new AA cannot be added to the chain (elongation blocker). Have broader spectrum (gram neg, gram pos, aerobic, and anaerobic.). Really good for STI’s (chlamydia…) and rickettsial infections, respiratory tract infections (pnemonia), skin and soft tissue infections (community staph, moderate to severe acne). Note: GI disturbance and bony structures/teeth take the L. As in, DO NOT GIVE TO PEDIATRIC PATIENT. Can cause bone inhibition and the teeth become forever discolored. In addition, you have to stay out of the sun…tetracycline causes photosensitization. Can even cause liver disturbances.

Question 16

Tigecycline
Half life:
Class:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 16

Half life: 36 hours
Class: Glycylcycline (glycine amino acid attachement to tetracycline)
Target and job: inhibits 30s ribosomal subunit.
Static vs. Cidal Bacteriostatic
Spectrum of action: Prevents the aminoacyl-tRNA that carries the AA from reaching the ribosome, so new AA cannot be added to the chain (elongation blocker). Have broader spectrum (gram neg, gram pos, aerobic, and anaerobic.)
Note: NO MORE ORAL VIABILITY DUE TO GLYCINE. IV only. Also, take these before you eat since food makes the amount of the drug you can get into the blood stream LESS. reason: cations with charges grater than +1 (metals such as Fe…Ca (dairy)). CUT DAIRY FROM YOUR DIET WHEN USING THESE DRUGS. Antacids also are a no go with these drugs for the same reason. Used for MRSA (refractory infections), gram neg beta lactam bugs, strep.

Question 17

Eravacycline
Half life:
Class:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 17

Half life: 20 hours
Class: Glycylcycline (Glycine added to tetracycline…kills oral viability)
Target and job: inhibits 30s ribosomal subunit.
Static vs. Cidal Bacteriostatic
Spectrum of action: Prevents the aminoacyl-tRNA that carries the AA from reaching the ribosome, so new AA cannot be added to the chain (elongation blocker). Have broader spectrum (gram neg, gram pos, aerobic, and anaerobic.)
Note: NO MORE ORAL VIABILITY DUE TO GLYCINE. IV only. Also, take these before you eat since food makes the amount of the drug you can get into the blood stream LESS. reason: cations with charges grater than +1 (metals such as Fe…Ca (dairy)). CUT DAIRY FROM YOUR DIET WHEN USING THESE DRUGS. Antacids also are a no go with these drugs for the same reason. Used for MRSA (refractory infections), gram neg beta lactam bugs, strep.

Question 18

Macrolides (erythomycin, clarithromycine, azithromycine, and telithromycin (use when previous 2 don't work))
Half life:
Class:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 18

Macrolides
Half life: Again, the only real difference between these drugs.
Class: Macrolide
Target and job: Inhibits 50 s (large subunit) of bacterial ribosome
Static vs. Cidal: Bacterioalstatic
Spectrum of action: Poor with anaerobes, really good with aerobes, great with gram pos, but some gram neg. Not as broad as tetracyclines.
Predominant Uses: Respiratory tract infections (pneumonia, bronchitis…problem is that most of the time the source of these illnesses is viral, not bacterial, so there isn’t an effect…so you tend not to prescribe unless it is persistent for over a weak), skin and soft tissue infections. Can’t treat MRSA. Acute otitis media, streptococcal pharyngitis, chlamydia, diptheria, pertssis (whooping cough),
Problems:
1. Gi: With oral stimulation (cramps, increases diarrheas)
2. Hepatitis: can produce acute cholestatic hepatitis (more so with telithromycin…also can lead to that hepatitis)

Question 19

erythomycin
Half life:
Class:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 19

Half life: 1.5 hours
Class: Macrolide
Target and job: Inhibits 50 s (large subunit) of bacterial ribosome
Static vs. Cidal: Bacterioalstatic
Spectrum of action: Poor with anaerobes, really good with aerobes, great with gram pos, but some gram neg. Not as broad as tetracyclines.
Predominant Uses: Respiratory tract infections (pneumonia, bronchitis…problem is that most of the time the source of these illnesses is viral, not bacterial, so there isn’t an effect…so you tend not to prescribe unless it is persistent for over a weak), skin and soft tissue infections. Can’t treat MRSA. Acute otitis media, streptococcal pharyngitis, chlamydia, diptheria, pertssis (whooping cough),
Problems:
1. Gi: With oral stimulation (cramps, increases diarrheas)
2. Hepatitis: can produce acute cholestatic hepatitis (more so with telithromycin…also can lead to that hepatitis)

Question 20

clarithromycine
Half life:
Class:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 20

Half life: 6 hours
Class: Macrolide
Target and job: Inhibits 50 s (large subunit) of bacterial ribosome
Static vs. Cidal: Bacterioalstatic
Spectrum of action: Poor with anaerobes, really good with aerobes, great with gram pos, but some gram neg. Not as broad as tetracyclines.
Predominant Uses: Respiratory tract infections (pneumonia, bronchitis…problem is that most of the time the source of these illnesses is viral, not bacterial, so there isn’t an effect…so you tend not to prescribe unless it is persistent for over a weak), skin and soft tissue infections. Can’t treat MRSA. Acute otitis media, streptococcal pharyngitis, chlamydia, diptheria, pertssis (whooping cough),
Problems:
1. Gi: With oral stimulation (cramps, increases diarrheas)
2. Hepatitis: can produce acute cholestatic hepatitis (more so with telithromycin…also can lead to that hepatitis)

Question 21

telithromycin
Half life:
Class:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 21

Half life: 10 hours
Class: Macrolide
Target and job: Inhibits 50 s (large subunit) of bacterial ribosome
Static vs. Cidal: Bacterioalstatic
Spectrum of action: Poor with anaerobes, really good with aerobes, great with gram pos, but some gram neg. Not as broad as tetracyclines.
Predominant Uses: Respiratory tract infections (pneumonia, bronchitis…problem is that most of the time the source of these illnesses is viral, not bacterial, so there isn’t an effect…so you tend not to prescribe unless it is persistent for over a weak), skin and soft tissue infections. Can’t treat MRSA. Acute otitis media, streptococcal pharyngitis, chlamydia, diptheria, pertssis (whooping cough),
Problems:
1. Gi: With oral stimulation (cramps, increases diarrheas)
2. Hepatitis: can produce acute cholestatic hepatitis (more so with telithromycin…also can lead to that hepatitis)

Question 22

azithromycine
Half life:
Class:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 22

Half life: 3 days (hence most prescribed)
Class: Macrolide
Target and job: Inhibits 50 s (large subunit) of bacterial ribosome
Static vs. Cidal: Bacterioalstatic
Spectrum of action: Poor with anaerobes, really good with aerobes, great with gram pos, but some gram neg. Not as broad as tetracyclines.
Predominant Uses: Respiratory tract infections (pneumonia, bronchitis…problem is that most of the time the source of these illnesses is viral, not bacterial, so there isn’t an effect…so you tend not to prescribe unless it is persistent for over a weak), skin and soft tissue infections. Can’t treat MRSA. Acute otitis media, streptococcal pharyngitis, chlamydia, diptheria, pertssis (whooping cough),
Problems:
1. Gi: With oral stimulation (cramps, increases diarrheas)
2. Hepatitis: can produce acute cholestatic hepatitis (more so with telithromycin…also can lead to that hepatitis)

Question 23

Lincosamides (Clindamycin)
Half life:
Class:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 23

Half life:
Class: Lincosamide
Target and job: Treats skin and soft tissue inections caused by aerobic and anerobic gram-pos bacteria
Static vs. Cidal: Bacteriostatic
Spectrum of action: aerobic and anerobic gram-pos bacteria ONLY
Predominant Uses: skin and soft tissue infections
Problems:

Question 24

Streptogramins (Quinupristin/dalfopristin)
Half life:
Class:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 24

Half life:
Class: Streptogramins 
Target and job: IV only. targets only infections caused by vancomycin-resistant enterococcus faecium and complicated methicillin-sensitive S. aureus
Spectrum of action:
Predominant Uses:
Problems:

Question 25

Oxazolidinone (Linezolid)
Half life:
Class:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 25

Half life:
Class:
Target and job: Oral or IV
Static vs. Cidal: Bacteriostatic
Spectrum of action MDR gram pos bacteria ONLY, including MRSA, vancomycin resistant enterococcus faecium (VRE), and penicillin resistant streptococci
Predominant Uses:
Problems:

Question 26

Anti-folate drugs (Sulfonamides: sulfisoxazole, sulfamethoxazole, sulfasalazine...which is specifically used for inflammatory bowel disease)
Half life:
Class:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 26

Anti-folate drugs
Half life:
Class:
Target and job: Screws up purine (A, G) synth by specifically inhibiting PABA conversion to dihydrofolic acid via blocking dihydropteroate synthase.
Static vs. Cidal: Bacteriostatic
Spectrum of action:
Predominant Uses: Used fro UTI’s. Sulfasalazine…which is specifically used for inflammatory bowel disease (Chrons and ulcerative colitis)
Problems: HYPER-allergenic. they are the strongest allergy producing drugs, period. Any drug with an S first letter will do this. can lead to hives, and other acute reactions. Also, super insoluble…they precipitate in urine (crystals in urine causing obstruction)

Question 27

Trimethoprim
Half life:
Class:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 27

Anti-folate drugs
Half life:
Class: Anti-Folate
Target and job: Screws up purine (A, G) synth by specifically inhibiting conversion of dihydrofolic acid to tetrahydrofolic acid via dihydrofolate reductase
Static vs. Cidal: Bacteriostatic
Spectrum of action:
Predominant Uses: Used for UTI’s. Sulfasalazine…which is specifically used for inflammatory bowel disease (Chrons disease and ulcerative colitis)
Problems: HYPER-allergenic. they are the strongest allergy producing drugs, period. Any drug with an S first letter will do this. can lead to hives, and other acute reactions. Also, super insoluble…they precipitate in urine (crystals in urine causing obstruction).
NOTE: take with sulfonamide, work synergistically (TMP-SMX) and will KILL the bacteria.

Question 28

TMP-SMX (Trimethoprim + sulfonamide)
Half life:
Class:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 28

Anti-folate drugs
Half life:
Class: Anti-Folate
Target and job: Screws up purine (A, G) synth by specifically inhibiting both dihydropteratesynthase and dihydrofolate reductase
Static vs. Cidal: Bacteriocidal
Spectrum of action:
Predominant Uses: Used for UTI’s, systemic salmonella infections, and pneumonia
Problems: Aim to use for less than 5 days, otherwise can still lead to rashes (hives) since it still has sulfonamides. If oyu go longer than 5 days, you will notice megaloblastic anemia and leukopenia since it can still target your own purine synth pathway.

Question 29

DNA Gyrase / Topoisomerases  IV Inhibitors (Fluoroquinolones (FQ)): Ciprofloxin, lomefloxacin, levofloxacin, ofloxacin
Half life:
Class:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 29

Half life:
Class:
Target and job:
Static vs. Cidal: Bacteriocidal
Spectrum of action: Gram neg it hits the gyrase). In gram pos, it attacks (topoisomerase). Best wtih gram neg
Predominant Uses: Use ciprofolxacin specifically to treat anthrax caused by bacillus anthaxis. All else can treat intrabdominaal infection, soft tissues, bones.. Can also treat pseudomonal lung infection cystic fibrosis patients.
Problems: Actually well tolerated. All effects are reversible.

Question 30

DNA Gyrase / Topoisomerases  IV Inhibitors (Fluoroquinolones (FQ)): Gemifloxacin and moxifloxicin
Half life:
Class:
Target and job:
Static vs. Cidal:
Spectrum of action:
Predominant Uses:
Problems:

Answer 30

DNA Gyrase / Topoisomerases IV Inhibitors
Half life:
Class:
Target and job:
Static vs. Cidal:
Spectrum of action: Better with gram pos (topoisomerase target), but still great with gram neg
Predominant Uses: UTI’s, salmonella, shiegella,
Problems: