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76 Cards in this Set
- Front
- Back
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Aminoglycosides
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1. 30S
2. Bactericidal 3. Results in premature release of aberrant protein |
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Tetracylines
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1. 30S Subunit
2. Bacteriostatic 3. Prevents elongation |
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Oxazolidinone
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1. 50S Subunit
2. Bacteriostatic 3. Inhibits initiation complex |
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Macrolides
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1. 50S Subunit
2. Bacteriostatic 3. Prevents elongation |
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Chloramphenicol
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1. 50S Subunit
2. Bacteriostatic 3. Prevents elongation |
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Daptomycin acts on ____ of gram ____ cells
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Daptomycin acts on CELL MEMBRANE of gram POSITIVE cells
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Polymyxin
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Works on outer membrane of Gram Negative bacteria.
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Mechanism of vancomycin
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Prevents crosslinking by binding 5th a.a., preventing it from getting clipped.
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Beta Lactams
1. Where do they work? 2. Function? 3. Common beta lactam? |
1. Cell wall (peptidoglycan)
2. The cell sees them as D-alanine + D-alanine and irreversibly inserts this segment into peptidoglycan 3. Penicillin is a common lactam |
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Sulfonamides & Trimethoprim
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Block tetrahydrofolate pathway needed for the production of nucleic acids (Thymine)
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Rifampin
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Stops bacterial RNA polymerase
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Do beta lactams work on Gram+ or Gram-
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Both!
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Linezolid is an example of which antibiotic class?
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Oxazoldinones
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Erythromycin is an example of which class?
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Macrolides
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PENICILLINS (PCN)
4 Compounds Function |
Beta Lactams
Disrupt cell wall synthesis Penicillin Oxacillin Ampicillin Piperacillin |
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Penicillin - Drug of choice for (2):
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Strep
syphilis |
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What is the super penicillin? Why is it called this?
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Piperacillin
It's a super penicillin because it is very broad spectrum (even against Gram-) |
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Adverse effects of penicillin
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Allergy (anaphylaxis / immediate& delayed hypersensitivity)
Bone marrow probs nephritis seizures |
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Beta Lactam / lactamase inhibitor (4)
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Amoxicillin/ clavulanic acid
ampicillin/sulbactam ticarcillin/clavulanic acid piperacillin/tazobactam |
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Where do you see the largest activity gain using beta lactam / lactamase inhibitors
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Anaerobic bacteria and Gram negative rods (pseudomonas)
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Problem with lactam/lactamase inhibitors:
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They won't work if resistance is not mediated through Beta lactamase
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Cephalosporins:
Mode of action Resistance Excretion Administered? Side effects? |
Block cell wall synthesis
- Resistance similar to PCN Renal excretion Can be given orally and parenterally Side effects similar to PCN (note cross allergies) |
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Cephalosporins - 5 drugs
For each state generation and any Drug of Choice |
Cefazolin (1st gen.) DOC= Staph, strep. E. coli (mostly Gram+, note E.Coli is Gram-)
Cefuroxime (2nd gen) good for Staph/strep, more Gram- (esp. respiratory) Ceftriaxone, Cefotaximine & Ceftazidime (3rd gen) Gram+&- BACT MENINGITIS Cefepime (4th gen) PSEUDOMONAS AERUGINOSA |
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What is cefepime ineffective against?
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Enterococcus
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Carbapenems (CARBAP)
4 drugs: |
1. Imipenem/cilastatin
2. Meropenem 3. Doripenem 4. Ertapenem (all end in "penem") |
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Carbapenems:
-Mode of action -Resistance -Excretion -Administration |
Action = Stop cell wall
Beta lactamase stable, although bact can aquire resistance via carbapenemase Excretion via kidneys No oral dosage |
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Carbapenems:
Adverse reactions Any cross allergies? |
Similar to PCN (rash/marrow/seizures)
Can have cross allergies with PCN Also see seizures and superinfection |
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What bugs are Carbapenems good at fighting?
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Very broad spectrum
Both Gram+ and Gram- as well as anaerobes However, only used for severe and/or complex infections |
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Ampicillin is the drug of choice for what (2)?
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1.Enterococcus
2.Listeria |
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Monobactam (MONOB)
-Drug (1) -Function -Resistance (2) -Administration -Excretion Side effects? Cross allergy to PCN? |
Aztreonam
Stops cell wall synthesis -Resistance through (1) Altering binding sites & (2) enzyme degredation No oral dosage Excreted through urine. Rxn similar to PCN although they can be given to patients allergic to PCN. There is NO cross allergy to PCN |
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Which bacteria can monobactam (MONOB) treat?
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Only gram negative organisms.
Use where GNR's are isolated "1/2 the molecule with 1/2 the activity" |
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Aminoglycosides (AMINOG):
4 drugs in this family: |
1. Streptomycin
2.Gentamicin 3. Tobramycin 4.Amikacin |
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Aminoglycosides (AMINOG):
Mechanism Resistance Excretion Administration |
Mechanism: Binds to 30s of ribosomes
Resistance via (1) Inactivating enzymes & (2) Decr. Uptake Excretion: Via the kidneys Admin: No oral dosage (Tobramycin can be inhaled) |
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What are aminoglycosides effective against?
How can they be synnergistic? |
Good for fighting gram netative bacilli & some mycobacterial (TB)
Synergy with beta lactams (especially pseudomonus) |
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Adverse effects of aminoglycosides(3):
Which ones are reversible and which are irreversible? |
Nephrotoxicity/Ototoxicity/Neuromuscular blockade
Nephro = reversible Oto = irreversible (both deafness and balance loss) |
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What is the post antibiotic effect? Which classes of drugs does it pertain to?
Why is it beneficial for clinicians? |
Post antibiotic effect means drug will work below min level of antibiotics (MIC) needed to kill bacteria
(Drug lingers) Helpful for dosing Pertains to aminoglycosides & quinupristin/dalfopristin |
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Tetracycline (TET):
3 drugs in family (besides tetracycline): |
1. Doxycycline
2. Minocycline 3.Tigecycline |
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Tetracycline (TET):
Mechanism Resistance Excretion Administration |
Mechanism: Binds to 30S (bacteriostatic)
Resistance through decr. Uptake and EFFLUX Excretion = Renal for TET itself, billiary for other drugs in this class Can be taken IV or orally |
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Which bacteria can tetracyclines treat?
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Tetracycline itself is good for acne
Drugs in this class are good for CHLAMYDIA and bizarro ARTHROPOD BORNE diseases Drugs are generally broad spectrum |
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Adverse effects of Tetracyclines (TET)
Who can these drugs not be perscribed to? |
Upset stomach/Diarrhea
Also photosensitivty, depressed bone growth, discolored teeth (permanent) Pregnant women and children should not take it |
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Chloramphenicol (CHLORO):
-Mechanism -Resistance -Excretion -Administration |
Binds to 50S
-Bacteriostatic/cidal depending on bacteria Resistance by (1) Decr. Permeability & (2) Acetylating enzyme Liver and renal excretion Can be given orally and by IV |
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Which bacteria can chloramphenicol (CHLORO) treat?
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Broad range against both Gram+ and Gram- organisms.
Excellent against anaerobes. Good against rickets, spirochetes, mycoplasma, chlamydia |
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Adverse effects of chloramphenicol:
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Aplastic anemia
Bone marrow toxicity (reversible) Gray Baby syndrome Optic neuritis For these reasons, these drugs are not used in the USA too often |
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Which bacteria can chloramphenicols be used for as an alternative here in the USA (3)?
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1. Meningitis
2.RMSF 3.Typhoid fever |
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MACROLIDES (MACRO):
Name 3 drugs in this family |
Erythromycin
Azithromycin Clarithromycin Note all end in Mycin |
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Macrolides (MACRO):
-Mechanism -Resistance -Administration -Excretion |
Mechanism: Binds to 50S (bacteriostatic)
Resistance: (1) Decr perm. (2) Altering binding sites on ribosomes Can be given orally and through IV Excretion: Biliary |
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Which bacteria are macrolides effective against?
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Mostly gram positive (newer ones are also Gram-)
DRUG OF CHOICE FOR: LEGIONELLA, MYCOPLASMA, DIPTHERIA, PERTUSIS |
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Adverse effects of macrolides:
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Upset stomach, gout exacerbation, rash
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Quinupristin/Dalfopristin:
-Mechanism -Excretion -Resistance -Administration |
Stops 50S protein synthesis
-Biliary excretion -Resistance???? -IV administration only Drug is very similar to Macrolides |
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What is quinupristin/dalfopristin used for?
What is the special exception? |
Selective against Gram+ organisms
Generally restricted to VRE faecium Not active against E faecalis |
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Adverse effects to Quinupristin/Dalfopristin:
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Very expensive!
Causes arthralgias/myalgias Causes hyperbilirubinemia Needs to be infused through central vein Antagonistic to erythromycin |
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Linezolid:
-Mechanism -Excretion -Resistance |
Mechanism: Binds 50s blocks initiation (fMEt-tRNA)
Excretion: Mostly by biliary, some by renal -Resistance: Who knows? |
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Administration of Linezolid:
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Can be taken orally or through IV.
Cleared by dialysis so those patients must be given drug after dialysis In the body it is protein bound |
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Drug/food interactions with linezolid:
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It's an MAO inhibitor so be careful with px on SSRI antidepressants. Also with pseudoephedrine & phenylpropalolamine
Food interactions with high tyramine (Asain ruben sandwich with beer) |
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Which bacteria is linezolid good at treating?
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Only gram positive (especially strep)
DOC for VRE, MRSA, PNEUMONIA |
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Adverse effects of linezolid:
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It's an MAO inhibitor.
It enhances adrenergic and serotenergic meds Also GI distress & thromocytopenia |
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Daptomycin:
-Mechanism -Excretion -Administration -Resistance |
Mechanism: Lipophilic & protein bound. Depolarizes PM of Gram positive bacteria (bactericidal).
Excretion: Mostly renal Administered by IV only Very little resistance |
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What is daptomycin good at treating?
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Gram Positives-
DOC for MRSA & VRE & SOFT TISSUE/SKIN INFECTIONS Also good for both E faecalis and E faecium unlike Quinupristin |
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What is daptomycin approved for? What disease can daptomycin NOT be used for?
Why? |
Approved for complicated skin and soft tissue infections.
Cannot be used for Pneumonia -Binds to lung surfactant |
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Adverse effects of daptomyin:
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Mild & self-limiting
-Muscle discomfort & weakness Elevation of CPK (asymptomatic) |
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Trimethoprim-Sulfamethoxazole (TMP-SMX)
-Mechanism Resistance Excretion Administered? |
Mechanism: Stops folic acid synthesis (bacteriostatic)
Resistance: (1) decr permeability or (2) enzyme affinity Excreted: Via urine Administered: Can be given orally or by IV |
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Which bacteria are sulfamethoxazoles good at treating?
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What aren't they good at?
Can treat pretty much everything except (1) anaerobes (2) Enterococcus (3) P. aeruginosa. DOC FOR PNEUMOCYSTIS CARINII, STENOTOPHOMONAS MALTOPHILIA, NOCARDIA |
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Adverse effects of sulfamethoxazoles:
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Stevens-Johnson Syndrome (dermatologic hypersensitivity)
Renal and liver dysfunction Bone marrow suppression Crystalluria |
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Quinolones (Q)
Name 3 drugs in this class: |
Ciprofloxacin (Gen 2)
Levofloxacin (Gen 2) Moxifloxacin (gen 3) "Note floxacins" |
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Quinolones (Q):
-Mechanism -Resistance -Excretion Administration |
Mechanism: Inhibits DNA gyrase
Resistance: Via (1) Altered binding site & (2) Active efflux -Excretion varies by compound -Admin: Can be given orally or by IV |
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Quinolones (Q) are good for treating which bacteria?
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In general, excellent Gram Negative activity, Good gram positive activity
3rd Generation (Moxifloxacin) is good at anaerobes as well Also, second line of defense against TB |
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Adverse effects of Quinolones (Q)
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Rash, GI distress
Also problems with CNS toxicity Alters glucose metabolism Bound by cations and metals (interacts with antacids) Interferes with developing cartilage (so you can't give to children or pregnant women) |
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Vancomycin (VANCO)
-Mechanism -Resistance Excretion Administration |
Mechanism: Inhibits cell wall synthesis (works on Gram+ only!)
Resistance: Via alteration of end molecule binding site -Note resistance from overuse. Excretion: Renal Administered: Parenteral (oral only for c. dif colitis) |
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Vancomycin (VANCO) is good for treating which bacteria?
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Used for gram positive bacteria only!
DOC for PENICILLIN RESISTANT MENINGITIS (PRSP), MRSA |
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Clindamycin:
-Mechanism -Resistance -Excretion -Administered |
Mechanism: Binds to 50 S subunits
Resistance: From altered binding site Excretion: Biliary Administered: Orally or by IV (the oral form is miserable for patients) |
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What is Clindamycin good at fighting?
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Good for anaerobic activity
Good for Gram+ (although not enterococcus or MSA) Microaerophilic organisms Also good for head and neck infections, aspiration pneumonia, intraabdominal infxn, pelvic infxn |
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Adverse effects of clindamycin
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Rash & GI distress
Greatest association with pseudomembranous colitis |
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Metronidazole:
-Mechanism -Resistance -Excretion -Administration |
Mechanism: Interrupt DNA synthesis
Resistance: Who knows? Excreted: Biliary Admin: Can be taken orally or through IV |
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What is metronidazole (METRO) good at fighting?
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Gold standard for anaerobes (DOC) - Includes Bacteroides and clostridium
-Some antiparasitic action (Giardia, Entamoeba, Trichomona, Gardnerella vaginais) -NO aerobic action |
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Adverse effects of metronidazole (METRO):
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Bad metallic taste
Neuropathy (peripheral) Disulfiram-like rxn Pancreatitis Patients will vomit if they take it with alcohol |
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Adverse effects of Vancomycin
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Ototoxicity (like aminogycosides)
Nephrotoxicity Vein sclerosis Rash/Redman syndrome |
