Pharm Exam 2 Overview Flashcards
What are the four factors that are unique to chemotherapy
- Selective toxicity
- Selects for resistant strains
- Hypersensitivity and toxicity are potential problems
- Lowers the microorganism load so that the hosts defense mechanism can rid the body of foreign organisms
What type of resistance transmission uses a bacteriophage?
Transduction
What type of resistance transmission uses genetic information from the environment?
Transformation
What type of resistance transmission uses direct contact through a sex pilus?
Conjugation
What is the mechanism of action of all bactericidal agents?
Inhibit cell wall/DNA synthesis
What is the mechanism of action of most bacteriostatic agents?
Inhibit protein synthesis
What is the clinical importance of post antibiotic effect?
Less frequent doses and therefore less potential for side effects
What are the 2 most used natural penicillins?
Penicillin G (IV) Penicillin V (oral)
Natural Penicillins
What is the spectrum of coverage?
What are they DOC for?
G+++
G+ infections
Strep pneumonia
Meningitis
What are the penicillin resistant penicillins?
Nafcillin (IV)
Dicloxacin (oral)
Oxacillin (oral)
Penicillin Resistant Penicillins
What is the spectrum of coverage?
What are they DOC for?
G++/G- (resistant to penicillinase)
MSSA
What are the extended spectrum penicillins?
Ampicillin (oral)
Amoxicillin (oral)
Extended Spectrum Penicillins
What is the spectrum of coverage?
What are they DOC for?
G+/G—
Listeria
H. pylori (or Metronidazole)
Amoxocillin: EARLY stage Borrelia burgdorferi (or doxycycline)
What is a possible side effect of the Extended Spectrum Penicillins? Does it preclude future use?
Ampicillin rash, NOT a hypersensitivity rash and does not preclude future use
What are the antipseudomonal penicillins?
Pipercillin (IV)
Ticarcillin (IV)
Antipseudomonal Penicillins
What is the spectrum of coverage?
What are they DOC for?
G+/G—
P. aeruginosa (in combo with an aminoglycoside), Acinetobacter
Which agents can be combined with b-lactamase inhibitors to extend their spectrum?
Ampicillin, Amoxicillin, Pipercillin, and Ticarcillin
What are the b-lactamase inhibitors that Ampicillin, Amoxicillin, Pipercillin, and Ticarcillin can be combined with to extend their spectrum?
Clavulanic acid, Sulbactam, and Tazobactam
What is the main adverse reaction for all penicillins?
Hypersensitivity
Are penicillins bactericidal or bacteriostatic? What is their MOA?
Bactericidal
B-lactam ring binds to the active site of penicillin binding proteins (PBPs) preventing transpeptidation reaction. Bacteria produces remodeling enzymes called autolysins, which allows their synthesis to proceed without cell-wall repair; eventually leading to lysis
MUST HAVE ACTIVELY GROWING CELLS
Are cephalosporins bactericidal or bacteriostatic? What is their MOA?
Bactericidal
B-Lactam (same as penicillin)
What is an advantage that cephalosporins have over penicillins?
Increased resistance to b-lactamase
What are the 1st generation cephalosporins?
Cafazolin (IV)
Cephalexin (oral)
1st Generation Cephalosporins
What is the spectrum of coverage?
What are they DOC for?
G++/G- (narrow spectrum)
Cafazolin- surgical prophylaxis
Proteus, E. coli, Klebsiella
*PEK
What is the most common 2nd generation cephalosporin?
Cefaclor (oral)
2nd Generation Cephalosporins
What is the spectrum of coverage?
What are they DOC for?
G+/G– (intermediate spectrum)
Proteus, E. coli, Klebsiella (PEK)
Moraxella
What are the 3rd generation cephalosporins?
Ceftriaxone (IV, IM)
Ceftotaximine sodium (IV, IM)
Cefazidime (IV, IM)
Cefixime (oral)
3nd Generation Cephalosporins
What is the spectrum of coverage?
What are they DOC for?
G+/G— (broad spectrum)
Ceftriaxione- CNS penetration, N. gonorrhoeae, LATE stage Borrelia burgdorferi, Salmonella
Ceftotaxime- CNS penetration
Cefazidime- Antipseudomonal with aminoglycosides (IF penicillin allergy)
Moraxella
What are the contraindications of 3rd generation cephalosporins?
Neonates, bilirubin displacement, pseudolithiasis
What is the 4th generation cephalosporin?
Cefepime (IV)
4th Generation Cephalosporin
What is the spectrum of coverage?
What are the DOC for?
G+/G— (Broad spectrum- MOST normal flora changes)
Antipseudomonal
Only used for serious infections
Empirical therapy when B-lactamases are anticipated
What is the 5th generation cephalosporin?
Ceftaroline fosamil (IV)
5th Generation Cephalosporin
What is the spectrum of coverage?
What are the DOC for?
Binds to mutated PBP that other b-lactams cannot bind to; MRSA and VRSA
What are the main adverse reactions for all cephhalosporins (3)?
- Dilsulfiram-like reaction with alcohol consumption (Metronidazole)
- Allergy: 10% cross sensitivity with penicillins
- Does-dependent renal tubular necrosis; do not give to patients with decreased kidney function
What are the four groups of B-lactam agents?
- Penicillins
- Cefalosporins
- Monobactams
- Carbapenems
What class is aztreonam in?
Monobactam
What is the coverage of aztreonam?
ONLY Aerobic G-, including pseudomonas
What is important about the cross sensitivity of aztreonam?
No cross sensitivity with other b-lactam agents (good option for pts with penicillin allergy)
What type of agents are Imipenem + Cilastin and Meropenem?
Carbapenems
What is the coverage of Imipenem + Cilastin and Meropenem?
Anaerobes, G+, G- (broad spectrum)
What are carbapenems DOC for?
Enterobacter
What are contraindications/ possible adverse reactions of carbapenems?
Seizures: do not give to pts with head trauma (meropenem less likely)
Do not give Imipenem to pts with decreased kidney function
Why is imipenem always given with cilastin?
Imipenem is inactivated by renal dihydropepdidases and must be given with cilastatin, a dihydropeptidase inhibitor.
How are monobactams and carbapenems given?
IV
What is MOA of vancomycin?
Binds to D-ala-D-ala (NOT PBPs); cell wall inhibitor= CIDAL
What is the coverage of vancomycin?
ONLY G+
What is IV vancomycin DOC for?
What is oral vancomycin DOC for?
IV: MRSA
Oral: C. diff
Drug of last resort for everything else because of vancomycin resistant enterocooi
What are the main adverse reactions of vancomycin?
Ototoxicity
Nephrotoxicity
Redman syndrome
What is the MOA for Fosfomycin? What is the coverage?
Prevents NAG to NAM reduction; cell wall inhibitor=CIDAL
G+, G-
What is the MOA for Bacitracin?
Interferes with dephosphorylation; prevents NAG-NAM transport; cell wall inhibitor=CIDAL
What is the coverage of Bactracin?
G+
What is Bactracin DOC for?
Combined with polymyxin and neomycin to treat superficial skin infections
What classes of protein synthesis inhibitors bind to the 50S subunit?
Macrolides Ketolides Clindamycin Streptogramins Oxazolidinones Chloramphenicol "50 Men Kiss Cute Strippers On Couches"
How do protein synthesis inhibitor resistant microbes form?
Efflux pumps
Methylation of ribosome binding site
What abx are in the macrolide class?
Erythromycin
Clarithromycin
Azithromycin
What are the macrolides DOC for?
Mycoplasma pneumoniae, Chlamydia
What are the most common adverse reactions of macrolides?
Diarrhea
QT prolongation
Drug interactions
Which macrolide does not inhibit CYP3A4? What advantage does this provide?
Azithromycin
Least drug interactions
Which macrolide has the most GI effects?
Which macrolide has the least GI effects?
Most = Erythromycin Least = Clarithromycin
What abx is in the ketolide class?
Telithromycin (oral)
How do ketolides differ from macrolides?
Ketolides bind to two sites on ribosomal RNA
macrolides are used before ketolides because ketolides can cause hepatoxicity
What is clindamycin the DOC for?
Clostridia, streptococcus, staphylococcus, toxic shock syndrome, and osteomyelitis
“Catherine clearly should stop taking opiods”