What is the mechanism of action of Cephalosporins Quizlet

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What is the mechanism of action of cephalosporin?
What does cephalosporins do to bacteria?
What do cephalosporins inhibit?
What is the target of cephalosporins?

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Medicine
Infectious Disease

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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

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What is the mechanism of action of cephalosporin?

Mechanism of Action Initially derived from the fungus Cephalosporium sp., cephalosporins are a large group of bactericidal antimicrobials that work via their beta-lactam rings. The beta-lactam rings bind to the penicillin-binding protein and inhibit its normal activity.

What does cephalosporins do to bacteria?

Cephalosporins are bactericidal drugs, meaning they kill bacteria directly. They do this by interfering with how bacteria build their cell walls. Cephalosporins are grouped into five generations based on when the drugs were developed. In general, each generation is effective against certain types of bacteria.

What do cephalosporins inhibit?

Cephalosporins are an important class of β-lactam antibacterials that are irreversible inhibitors of penicillin-binding protein (PBPs) involved in bacterial cell wall synthesis.

What is the target of cephalosporins?

Penicillins and cephalosporins are β-lactam antibiotics widely used to treat bacterial infectious diseases. They mainly target the cell wall biosynthesis pathway to inhibit bacterial growth.