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Terms in this set (56)
Mechanism of Action of Cephalosporins
Interfere with synthesis of the peptidoglycan component of the bacterial cell wall
Binds to enzymes called penicillin binding proteins (PBPs)
Causes progressive bacterial lysis
Usually bactericidal
1st Generation Cephalosporins
Cefazolin IV
Cephalexin PO
Cefadroxil PO
Narrow spectrum of activity
Gram positive cocci (S. aureus)
Moderate gram negative rod activity (E. coli, Klebsiella, Proteus)
2nd Generation Cephalosporins
Cefuroxime IV, Cefuroxime PO, Cefaclor PO, Cefprozil PO, Loracarbef PO
Cephamycins (Cefoxitin IV, Cefotetan IV)
variable activity
against gram positive cocci and increased activity against gram negative bacteria
Cephamycins-potent against gram negative aerobic and anaerobic organisms
3rd Generaton Cephalosporins
Cfoaxime IV, Ceftriaxone IV, Ceftazidime IV. Cefixime PO, Cefpodoxime PO, Cef[pdoxime PO, Ceftibuten PO, Cefdinir PO
Limited activity against gram positive cocci with very marked actiity against gram negative bacteria
(Pseudomonas)
4th Generation Cephalosporins
Cefipime IV
Activity against gram positive cocci (methicillin resistant S. aureus), many gram negative bacteria (Pseudomonas), and Enterobacter species that produce Blactamases
5th Generation Cephalosporins
advanced generation cepoalosporin
Ceftaroline, Fosamil IV
Works
against MRSA, many gram - bacteria, not Pseudomonas
Resistance of Cephalosporins
alteration of PBP target
Production of B-lactamases(enzymes that destroy antibiotic)
Decreased ability of antibiotic to reach its PBP target
Adverse effects of Cephalosporins
Injecion site reactions
hypersensitivity reactions
GI
reactions
Indications of 1st generation cephalosporins
UTI
Skin and soft tissue infections
Indications of 2nd generation cephalosporins
otitis media
community acquired pneumonia
sinusitis
intra-abdominal infections
pelvic and gynecologic infections
Indications of 3rd generation cephalosporins
gonorrhea
community acquired pneumonia
lyme disease
meningitis
hospital acquired pneumonia
Indications of 4th generation Cephalosporins
hospital acquired pneumonia
febrile neutropenia
complicated gram negative infections
Indications of 5th generation Cephalosporins
community acquired bacterial pneumonia
acute bacterial skin and skin structure infections
Contraindications of Cephalosporins
avoid in patients that have had an allergic reaction to a cephalosporin
Mechanism of action for Aminoglycosides
bactericidal
concentration dependent
inhibit protein snthesis by
irreversible binding to 30s subunit of bacterial ribosomes causing cell death
Resistance in Aminoglycosides
Failure to permeate
low affinity for the bacterial ribosome
inactivation by microbial enzymes
Adverse effects of Aminoglycosides
hearing and balance
kidney toxicity
Indications of aminoglycosides
Serious gram negative infections (Pseudomonas)
In combination with PCN or Vancomycin for Enterococcus, Staph or Streptococcal endocarditis
Complicated UTIs and respirator tract infections
can be in form of opthalmic and topical preparations
Contraidicatons of Aminoglycosides
hypersensitivity
Mechanism of Action for Tetracyclines
Bacteriostatic
inhibit bacterial protein snthesis by binding to the 30s bacterial ribosome
Resistance in Tetracyclines
Decreased accumulation of tetracycline
Drecreased access of tetracycilne to the ribosome
Enzymatic inactivation of tetracycline
Adverse effects of Tetracyclines
GI
Photosensitivity
Discoloration of teeth in children
Fanconi syndrome
Indications of Tetracyclines
Rickettsial Infections (Rocky Mountan Spotted Fever, Lyme Disease)
Pneumonia (Mycoplasma & Chlamydia)
Sexyally transmitted diseases (Gonorrhea)
Brucella
Tularemia
Cholera
Indications of Tigecycline
MRSA, Vancomycin Resistant Endococci (VRE), Extended Spectrum B-lactymases (ESBL)
Complicated SSSI
Complicated intra-abdominal infection
Bacteremia
Pneumonia
Not active agains Pseudomonas aeruginosa and poorly active against Proteus, Morganella or Providencia species
Adverse effects of Tigecycline
up to 20% of patients experience nausea and
vomiting
photosensitivity
Mechanism of Action for Chloramphenicol
inhibits protein synthesis by binding to 0 s ribosome
bacteriostatic
Resistance in Chloramphenicol
Acetyltransferase inactivates the drug
Adverse effects of chloramphenicol
bone
marrow (aplastic anemia)
GI (unpleasant taste)
Gray baby syndrome
Indications of Chloramphenicol
typhoid fever
bacterial meningitis
rickettsial diseases
brucellosis
Contraindications of Choamphenicol
hyersensitivity
Mechanism of Action for Erythromycin, Clarithromycin & Azithomycin
*macrolide class
bacteriostatic
inhibit protein synthesis by binding reversibly to 50s ribosomal subunits
may be bactericidal in high concentrations (but not used that way because adverse effects are too bad)
Resistance in Erythromycin, Clarithromycin & Azithromycin
Efflux pump
enzyme modifies the ribosome-leads to decreased
drug binding
enzymes destoy macrolides
Alteration of 50S ribosome in ceratin bacteria
Adverse effects of Erythromycin
GI (nausea, vomiting, abdominal crampint)
Indications of Erythromycin
Pneumonia (Mycoplasma and Legionnaire's Disease)
Chlamydia
Diptheria
Pertussis
Contraindications of Erythromycin, Clarithromycin & Azithromycin
Hypersensitivity to any macrolide
re-existing liver disease
drug interactions
Adverse effects of Clarithromycin
allergic (fever, skin eruptions, eosinophilia)
GI
Indications of Clarithroycin
More than erythromycin
Otitis
media
Sinusitis
Acute bronchitis
Pneumonia
H. pylori
Prophylaxis and treatment of MAC in AIDS/HIV infected patients
Adverse Effects of Azithromycin
GI (not as bad as other macrolydes
less drug interactions
Indications of Azithromycin
Community Acquired Pneumonia
Pharyngitis
Skin and Skin structure
infections
Treatment of prophylaxis of MAC infection in AIDS/HIV
Uncomplicated nongonococcal urethritis
Acute otitis media
Mechanism of Action of Ketolides
designed to circumvent resistance
Inhibit bacterial protein synthesis and ribosome assembly
Indication of Ketolides
CN and erythromycin resistant S. pneumoniae, H. influenzae, M. catarrhalis, Chlamydia, Legionella, Mycoplasma
Adverse effects and dosage of Ketolides
Diarrhea
Fewer drug interactions that erythromycin
800 mg daily for 5-10 days
Mechanism of Action for Linezolid
Ribosomal
inhibits ribosome assemly step of protein synthesis
Resistance of Linezolid
mutation of ribosome binding site
Indications of Liezolid
VRE
nosocomial pneumonia
complicated skin and skin structure infections
MSSA and MRSA
Mechanism of Action for Clindamycin
Baceriosatic or Bacericidal
Binds to 50S subunit of bacterial ribosomes and suppresses
protein synthesis
Adverse effects of Clindamycin
Diarrhea
Pseudomembranous colitis (C. diff)
skin rashes
Indications of Clindamycin
Anaerobic infections in respiratory tract
Skin and soft tissue
Female pelvis and genital tract
Gram positive infections in respiratory tract
osteomyelitis
sepsis
Mchanism of action of Fluoroquinolones
Bactericidal
binds to and inhibits bacterial topisomerase II and IV which prevents supercoiling of bacterial DNA
Resistance in Fluoroquinolones
mutations in bacterial topisomerase II or IV
efflux pump
Adverse effects of Fluoropuinolones
GI
Photosensitivity
Confusion/delirium (elderly)
joint swelling/tendon rupture (avoid in children)
Indications of Fluoroquinolones
UTIs
Prostatitis
STDs
Respiratory Tract Infections (bronchitis, sinusitis, pneumonia)
Multi-drug resistant TB
Mycobacterium infection in HIV/AIDs patients
Mechanism of Action of Sulfonamides
Bacteriostatic
competitive antagonists of para-aminobenzoic acid (PABA)
prevents bacteria using PABA to synthesize folic acid
Reisistance with Sulfonamides
Decreasedbinding affinity of sulfonamides
decreased permeability of active efflux of sulfonamide
alternate metabolic pathway
increased production of drug antagonist
Adverse effects of Sulfonamides
Crysalluria
aganulocytosis
aplastic anemia
hypersensitiity reactions (rashes, photosensitivity, drug fever)
GI (nausea/vomiting)
Indications of Sulfonamides
UTIs
Nocardiosis
Toxoplasmosis
Antimicrobials
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