Antibiotics Flashcards
What are beta-lactams?
a group of antibiotics that include a beta-lactam ring.
What are the 4 groups of beta-lactams?
- penicillins
- cephalosporins
- Carbapenems
- Monobactams
What is the mechanism of action of beta-lactams?
They bind to PBPs (penicillin binding proteins) which are the final step of petidoglycan synthesis in bacterial cell walls so lysis occurs leading to death of the bacterial cell (bactericidal)
What are the subclasses of penicillins?
Natural penicillins, penicillinase-resistant penicillins, aminopenicillins and penicillin + beta-lactamase inhibitor
Natural penicillins include
Aqueous Crystalline penicillin G (IV) Penicillin VK (PO)
Natrual penicillin spectrum
Gram-pos
anaerobes
treponema pallidum (causes syphilis)
Penicillinase-resistant penicillins include
Nafcillin (IV) - for MSSA
Dicloxacilin (PO)
Penicillinase-resistant penicillin spectrum
staphylococcus (MSSA)
streptococcus
Aminopenicillins include
Ampicillin (IV and PO)
Amoxicillin (PO)
Aminopenicillin spectrum
gram-pos
anaerobes
Penicillin + Beta-lactamase ibhibitor includes ?
amoxicillin + clavulanic acid (Augmentin) (PO)
Penicillin + beta lactamase inhibitor spectrum
gram-pos, enterococcus
gram-neg, pseudomonas earuginosa
anaerobes
Adverse effects of penicillins
allergic or hypersensitivity reaction - ocurrs in 3-10%
Adverse effects of cephalosporins
allergic or hypersensitivity reaction - ocurrs in 1-3%
1st generation cephalosporins include
Cephalexin (Keflex) (PO)
Cefazolin (Ancef) (IV)
Spectrum of 1st generation cephalosporins
gram-pos - including staph
limited gram-neg
2nd gen. cephalosporins include
cefaclor (Ceclor) (PO)
cefoxitin (Mefoxin) (IV)
Spectrum of 2nd generation cephalosporins
gram-pos - less staph coverage
increased gram-neg
anaerobes (Cefoxitin ONLY)
Which of the cephalosporins is the only one that’s spectrum covers anaerobes?
Cefoxitin aka Mefoxin (2nd gen.)
3rd gen. cephalosporins include
Cefriaxone (Rocephin) (IV, IM)
Spectrum of 3rd gen cephalosporins
limited gram-pos
superior gram-neg coverage
Spectrum for both Carbapenems and Monobactams
gram-pos, gram-neg, anaerobes and pseudomonas. Also organisms that produce ESBLs.
The one monobactam has coverage only against aerobic gram-neg organisms.
Carbapenems include
Impenem/Cilastatin (Primaxin) (IV)
Why is cilastatin added to the carbapenem impenem?
to reduce the incidence of nephrotoxicity
The monobactam is
Aztreonam (Azactam) (IV)
Adverse effects of carbapenems and monobactams
nausea/vomiting
seizures
What is the mechanism of action of fluoroquinolones?
They inhibit bacterial DNA synthesis by inhibiting DNA-gyrase (topoisomerases) so the result is DNA strands breaking (bactericidal)
Fluoroquinolones include
Ciprofloxacin (Cipro) (IV, PO)
Levofloxacin (Levaquin) (IV,PO)
“Respiratory fluoroquinolones”
Spectrum of activity of the fluoroquinolones
- limited gram-pos - staph and strep
- exellent gram-neg - cipro and levofloxacin have activity against pseudomonas aeruginosa
- anaerobic activity
- atypical organisms: legionella, mycoplasma, chlamydophila
What are the safety considerations with fluoroquinolones?
contraindicated in: pregnant women and children 18 yrs or younger b/c of risk of cartilage destruction
Caution in elderly - may cause diziness
macrolides are commonly used for . . .
respiratory infections including rhinosinusitis, otitis media, bronchitis and community-acquired pneumonia
Macrolides mechanism of action
Binds to 50s ribosomal subunit of bacteria to inhibit RNA-dependent protein synthesis
Macrolides spectrum
gram-pos
limited gram-neg
limited anaerobe
Macrolides include
Erythromycin (IV, PO)
Clarithromycin (Biaxin) (PO)
Azythromycin (Zithromax) (IV, PO)
What are the most common adverse effects of macrolides?
GI symptoms
What is the mechanism of action of tetracyclines?
inhibition of 30S subunit which inhibits protein synthesis, causes cell wall impairment and cell death
tetracylclines spectrum of activity?
gram-pos: including community-aquired MRSA
gram-neg
anaerobes (limited)
Tetracyclines include
Doxycycline (IV, PO)
Tetracycline (PO)
Minocycline (IV, PO)
Adverse effects of tetracyclines
GI symptoms, phototoxicity, tooth discoloration. Contraindication in children under 8 and in pregancy .
What are the significant drug interactions of tetracyclines?
impaired w/ cations and dairy products
What is the spectrum of activity of sulfonamides?
gram-pos
gram-neg
protozoa
community-aquired MRSA
What is the most common form of a sulfonamide?
sulfamethoxazole combined with trimethoprim. Trimethoprim + sulfamethoxazole (TMP/SMX) (Bactrim®) is frequently prescribed for the treatment of urinary tract and skin infections, including skin infections caused by community-acquired MRSA
The sulfonamides include
Sulfamethoxazole
Trimethoprim
Mechanisms of action of sulfonamides
sulfamethoxazole - competes w/ para-amino benzoic acid to inhibit bacterial synthesis of dihydrofolic acid
Trimethoprim - inhibits dihydrofolate reductase which inhibits prodcution of tetrahydrofolic acid
both of which lead to a bactericidal effect
Adverse effects of sulfonamides
hypersensitivity or allergic reaction (3-5% have sulfa allergy)
What are the safety considerations for sulfonamides?
caution in 1st trimester and avoid in 3rd. avoid in infants less than 2 mos and breast feeding mothers of children less than 2 mos. causes kernicterus
Drug interactions of sulfonamides
Warfarin. Sulfamethoxazole increases anticoag effects increasing the risk for bleeding
Clindamycin is commonly used for ?
skin infections, vaginal infections, oral infections, acne and anaerobic coverage (above the diaphragm).
Spectrum of activity of clindamycin
gram-pos (including MRSA)
anaerobes
mechanism of action of clindamycin
binds to 50S and inhibits RNA-dependent protein synthesis
Adverse effects of clindamycin
Antibiotic-associated diarrhea may result from the overgrowth of Clostridium difficile; this infection in the GI tract may even lead to a severe colitis requiring colectomy in extreme cases
Metronidazole is commonly used in ?
anaerobic (below diaphragm) and protozoal infections. It is often added to an antimicrobial regimen for additional anaerobic coverage (GI, GU).
The name brand of metronidazole is ?
Flagyl (IV, PO, topical)
spectrum of activity of metronidazole
anaerobes
protozoa
c-diff
mechanism of action of metronidazole
inhibits nucleic acid synthesis resulting in cell death
Adverse effects of metronidazole
GI symptoms
disulfram like reactions occur when combined w/ alcohol
Vancomycin is commonly used when?
used in the hospital setting for empiric coverage for resistant Gram-positive organisms (e.g. MRSA). It should only be chosen for therapy when no other alternatives are available to reduce the incidence of resistance.
What is the spectrum of activity of vancomycin?
gram-pos - especially strep, staph, and enterococci (except VRE)
What is the mechanism of action of vancomycin?
inhibits bacterial cell wall synthesis (bactericidal) by inhibiting peptidoglycan polymerase
Adverse effects of vancomycin
Red Man’s Syndrome
Nephrotoxicity - uncommon
The aminoglycosides include
Gentamicin (IV)
Tobramycin (IV)
mechanism of action of aminoglycosides
Binds to 30S and 50S to inhibit bacterial protein synthesis (bactericidal)
Spectrum of activity of aminoglycosides
aerobic gram-negs: including pseudomonas aeruginosa and enterobacteriaceae
gram-pos (gentamicin only) but never alone, usually paired w/ beta-lactams
adverse effects of aminoglycosides
nephrotoxicity - often reversible
ototoxicity - often irreversible
What is a pathogen?
a microorganism capable of causing disease. not all bacterial are pathogens.
commensal pathogens
commonly found as part of our normal flora, meaning they live in or on our body (the host) in a non-infectious way.
colonize all “external” parts of the body where external would refer to access to the outside world (e.g., the respiratory tract and the GI tract are included in this definition of “external”)
given proper conditions, have the potential to cause disease
professional pathogens
a. are not a part of normal flora, but, when introduced to the body, can elude host defenses and cause infection fairly easily
b. only role in humans are as infectious agents
c. efficiently enter the body
d. are capable of multiplying rapidly
opportunistic pathogens
a. Are bacteria that can cause infection but normally require some alteration of the immune system
b. may or may not be part of the normal flora