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Considerations (4)
- Prophylaxis (epidemic, prosthetics, transplants, surgery)
- Empiric
- Pathogen Directed (Identified)
- Susceptibility Guided Therapy
Types of Antibiotics (5)
- Nucleic Acid Synthesis
- DNA Damaging Agents
- Cell Wall Synthesis
- Cell Membrane Damage
- Protein Synthesis
Nucleic Acid Synthesis Inhibitors (2 categories)
- anti-folate (sulfonamides, trimethoprim) - Bacteristatic

- anti-RNA polymerase (rifampin) - Bactericidal
Sulfonamides
- mechanism
- potency
- spectrum
- clinical uses
- pharmacokinetics
- misc.
- Nucleic Acid Synthesis (Antifolate): competes with p-aminobenzoic acid and inhibits dihydropteroate synthase
- bacteriSTATIC 
- gram (-) and gram (+) - lots of resistant strains
- UTIs, Toxoplasmosis (parasitic disease), topical burns, Pneumocystis jarovecii
- Oral Absorption
- Renal Clearance - Take w/ Plenty of water (Crystalluria)
- Wide Distribution (inc. CSF)
- Kernicterus - Bilirubin in newborns -> encephalopathy
- Stevens-Johnson - hypersensitivity reaction
- Photosensitivity
Trimethoprim
- mechanism
- potency
- spectrum
- clinical uses
- pharmacokinetics
- misc.
- Nucleic Acid Synthesis (Antifolate): Inhibits Dihydrofolate Reductase (DHFR)
- BacteriSTATIC alone
- Gram (-) and Gram (+)
- Used with Sulfamethoxazole. (Bacteriocidal)
- Treat UTI, intestinal infections, Prostatitis, Pneumocystis jarovecii, MRSA
- Oral
- Wide (CNS)
- Renal
- Anemia (Special human DHFR)
Rifampin
- Mechanism
- Potency
- Spectrum
- Clinical Uses
- Pharmacokinetics
- misc
- Nucleic Acid Synthesis (anti-RNA polymerase)
- BacteriCIDAL
- Mycobacteria tuberculosis ("Atypical"), Staphylococci
- TB, prosthetic valve endocarditis, staph infections; prophylaxis for meningococcal + meningitis
- Oral
- Widely Distributed (CSF)
- Renal Excretion
- P450 Deacetylation (Jaudice. Liver Damage)
- Induces Liver Metabolism + decrease HIV anti-retroviral drugs
- RIPE = Treatment of TB
- Isoniazid + pyrazinamide (cell envelope), ethambutol
DNA Damaging Agents (4)
- Quinolones (Bactericidal)
- Nitrofurans
- Methenamine
- Metronidazole (Bactericidal)
Quinolones
- mechanism
- potency
- spectrum
- clinical uses 
- pharmacokinetics
- DNA Damaging Agents: DNA Gyrase (uncoiling) and DNA topoisomerase (separation)
- BacteriCIDAL 
- Gram (-) and Gram (+)
- UTI (Cipro), RTI, anti-TB, pseudomonas (not @ UPMC)
- Oral (Ca++ Chelator. Limits)
- Renal (High Urine)
- Prostatic Fluid
- Cipro - tendon rupture in children + insomnia
- 3rd + 4th gen better for (+)

- Nalidixic Acid (1), Cirpofloxacin, Ofloxacin, Norfloxacin (2), Levofloxacin (3), Moxifloxacin (4)
Nitrofurans
- mechanism
- spectrum
- clinical uses
- pharmacokinetics
- misc
- DNA Damaging Agents: O2 Free Radical Formation
- Gram (+) and Gram (-)
- ONLY UTIs
- Oral
- Renal
- Pulmonary Fibrosis
Methenamine
- mechanism
- clinical use
- pharmacokinetics
- DNA Damaging Agents: Hydrolyzed to form formaldehyde. Acidify Urine
- Gram (-) except Psudomonas
- Prophylactic - Lower UTI
- Oral
- Gastric Distress (Stomach Hydrolysis), Crystalluria
Metronidazole
- mechanism
- spectrum
- clinical uses
- pharmacokinetics
- DNA Damaging Agents: Reductive activation of nitro group (pro-drug)
- BacteriCIDAL
- Anaerobic Gram (+) and Gram (-)
- Anaerobic + protozoal infections
- Oral
- Renal
- Wide (CNS)
- Disulfiram-like effects (alcoholism prevention) = nausea, vomiting, GI distress.
Cell Wall Synthesis Inhibitors (3)
- Mechanism
- Resistance
Bacitracin
Vancomycin
B-Lactam - Penicillins
- Cephalosporins
- Monobactams
- Carbapenems

- Osmotic Rupture
- L-form Bacteria (no cell wall), Kidneys (high osmotic pressure)
Beta Lactams (4)
- Penicillin
- Cephalosporins
- Monobactams
- Carbapenems
Penicillin
- mechanism
- potency
- clinical uses
- pharmacokinetics
- Cell Wall Synthesis Inhibitor: B-lactam - mimic D-ala-D-ala. Inhibits transpeptidase (PBP) - peptidoglycan crosslinking.
- Bactericidal, time dependent
- strep pneumoniae, haemophilus influenzae, STD, UTI
- poor oral absorption
- poor distribution (lipid insoluble)
- renal excretion
Penicillin (1st Gen)
- Penicillin G + V
- gram (+) - narrow
- effective against strep
- B-lactamase senstive (staph aureus)

Penicillin (2nd Gen)
- Methicillin, Cloxacillin
- gram (+) - narrow
- B-lactamase resistant
- MRSA (methicillin resistant s. aureus) - low binding PBP.
Penicillin (3rd + 4th Gen)
3rd - Ampicillin ("Broad Spectrum")
- gram (+) and some gram (-)
- enterobacteriaceae

4th - Piperacillin
- gram (+) and gram (-)
- enterobacteriaceae + pseudomonas
Cephalosporins
- mechanism
- potency
- spectrum
- pharmacokinetics
- misc.
- Cell Wall Synthesis Inhibitor: B-Lactam - mimic D-ala-D-ala. Inhibits transpeptidase (PBP) - peptidoglycan crosslinking.
- BacteriCIDAL
- broad: gram (+) and gram (-).
- oral, parenteral (IM), IV (3rd + 4th gen)
- wide (CSF)
- Renal + Biliary
- non-toxic. cross sensitivity allergies w/ penicillin.
- cefepime (4th gen) - effective against pseudomonas.
- sacrifice gram (+) for gram(-) potency. (esp. staph)
Carbapenems
- mechanism
- spectrum
- pharmacokinetics
- misc.
- Cell Wall Synthesis Inhibitor: B-Lactam - mimic D-ala-D-ala. Inhibits transpeptidase (PBP) - peptidoglycan crosslinking.
- gram (+) and gram (-) inc. pseudomonas
- IV
- Renal
- CNS toxicity (Seizures)
- Given w/ Cilastatin (block renal hydrolysis)
- binds PBP, esp in gram (-)
- Saved for Nosocomial Infections (B-lactamase resistant)

Monobactam
- mechanism
- spectrum
- pharmacokinetics
- Aztreonam
- Cell Wall Synthesis Inhibitor: B-Lactam - mimic D-ala-D-ala. Inhibits transpeptidase (PBP) - peptidoglycan crosslinking.
- Narrow - Gram (-)
- IV or IM.
- Renal
- B-lactamase resistant
- penicillin hypersensitivity
Beta-Lactamase Inhibitors
- names
- mechanism
- clinical combinations
- clavulanic acid, sulbactam, tazobactam
- suicide inhibitors. binds serine irreversibly
- Amoxacillin (3rd gen) + Clavulnate (oral + IV) - synergistic
- Ticarcillin + Clavulanic (IV)
- Ampicillin + Sulbactam (IV)
- Pipercillin + Tazobactam (IV)
Vancomycin
- mechanism
- spectrum
- pharmacokinetics
- misc
- Cell Wall Synthesis Inhibitor: Inhibits Peptidoglycan Synthase (polymerization of peptidoglycan by blocking D-ala-D-ala)
- gram (+) - staph, strep, e. faecalis
- IV
- Renal (not metabolized)
- hearing loss.
- Resistance: Changes to D-ala-D-lac, or D-ala-D-Ser
- does not penetrate gram (-) porin
- treat MRSA (methacillin (2nd gen) resistant staph aureus)
Bacitracin
- mechanism
- spectrum
- clinical
- pharmacokinetics
- Cell Wall Synthesis Inhibitor: Binds isoprenyl-phosphate lipid carrier.
- gram (+), some gram (-)
- topical (creams and ointments) for superficial skin infections.
Cell Membrane Damaging Agents
(2)
- Polimixins - Gram (-) - Bactericidal
- Daptomycin - Bactericidal
Polimixin
- mechanism
- potency
- spectrum
- clinical uses
- pharmacokinetics
- misc.

- Collistin E + B - Cell Membrane Damaging Agent: cationic detergent
- BacteriCIDAL
- gram (-) only
- pseudomonal infections + pan-resistant gram (-)
- topical + bacterial diarrhea
- poor oral absorption + nephrotoxicity.
Daptomycin
- mechanism
- potency
- spectrum
- clinical uses
- pharmacokinetics
- Cell Membrane Damaging Agent: Lipophilic tail insertion -> membrane depolarization (k+ efflux). DNA, RNA, protein synthesis disruption.
- BacteriCIDAL
- gram (+), esp vancomycin resistant enterococci + methicillin resistant staph aureus.
- skin infections.
- IV, once a day (Concentration Dependent) w/ post-antibiotic effect. 
- narrow: plasma + vascular tissue
Inhibitors of Protein Synthesis (7)
- Aminoglycosides
- Tetracyclines
- Chloramphenicol
- Clindamycin
- Erythromycin (Macrolides)
- Quinupristin + Dalfopristin
- Linezolid
Aminoglycosides
- mechanism
- potency
- spectrum
- clinical uses
- pharmacokinetics
- misc.
- Inhibitor of Protein Synthesis: Binds 30s, 50s rRNA subunit. tRNA attachment (initiation) -> mRNA distortion + polysome breakdown.
- BacteriCIDAL, concentration dependent w/ post-antibiotic effect.
- gram (-), esp pseudomonal and some gram (+)
- streptomycin - TB (IM = hurts), endocarditis
- gentamicin, tobramycin, amikacin - combination w/ ampicillin (B-lactam)
- neomycin + bacitracin - neosporin
- IM + IV
- poor distribution
- poor renal clearance (no metabolism)
- oto + nephrotoxicity
- Resistance: acetylation, adenylylation, phosphorylation
- Cationic
- Single large dose = stays above toxicity level shorter.
Tetracyclines
- mechanism
- spectrum
- distribution
- misc
- Protein Synthesis Inhibition: binds 30s on rRNA.
- BacteriSTATIC
- Broad-spectrum - Rickettsaie, mycoplasma, chlamydia, Gram (+) and Gram (-)
- Oral (partial absorption. Ca++ chelater)
- Renal + Feces
- CNS, placenta, Bone
- Don't give to pregnant / children.
- Fanconi - renal dysfunction from outdated tetracyclines.
- Photosensitive.
Tigecycline
- type
- misc.
- Tetracycline Analogue (Protein Synthesis Inhibitor)
- broad spectrum - gram (+) and (-) and anaerobes
- Not affected by (1) efflux pump, (2) ribosome alteration,
- multiple organisms + resistance to tetracyclines, B lactams, vancomycin.
- skin infections + intra-abdominal
- poor serum levels.
Chloramphenicol
- mechanism
- spectrum
- pharmacokinetics
- misc (toxicity)
- Protein Synthesis Inhibitor: 50s rRNA subunit.
- Broad: Gram (+) and (-)
- oral
- CNS
- Renal (glucuronide metabolism)
- Aplastic Anemia - rare but fatal
- Grey's Syndrome - inhibition of mito protein synthesis due to inability to liver immaturity (glucuronie).
Macrolides
- mechanism
- spectrum
- pharmacokinetics
- misc

- Erythromysin, Azithromysin, Clarithromysin - Protein Synthesis Inhibitor: binds 50s rRNA,
- BacteriSTATIC, BacteriCIDAL (some gram +)
- legionnaires, mycoplasma pneumonia, chlamydial infection
- oral
- wide, CNS
- liver metabolism, renal
- Azithromysin + clarithromysin = longer half-life w/ less side effects.
- methylation of 50s + efflux pump = resistance
Clindamycin
- Protein synthesis inhibitor, bacteriSTATIC.
- gram (+) bacteria + anaerobes

- Side Effect: Pseudomembranous Colitis caused by C. difficile = clindamycin resistance.
Quinopristin/Dalforpristin
- Protein Synthesis Inhibitor
- BacteriCIDAL together
- VRE + MRSA
- IV only
- Vein necrosis
Linezolid
- Protein Synthesis Inhibitor
- broad. gram (+)
- VRE, MRSA
- myelosuppression.
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