29 Antibacterial drugs Flashcards
(84 cards)
29.01 BETA-LACTAM ANTIBIOTICS
Penicillins - actions
bactericidal
interfere with cell wall synthesis in dividing bacteria
29.01 BETA-LACTAM ANTIBIOTICS
Penicillins - MOA
bind to and inhibit the enzyme that cross-links the peptide chain of the newly formed ‘building block’ to the peptidoglycan cell wall backbone
29.01 BETA-LACTAM ANTIBIOTICS
Penicillins - types of penicillins
beta-lactamase resistant (methicillin, flucloxacillin, temocillin), broad spectrum (ampicillin, amoxicillin), extended spectrum (piperacillin, ticarcillin)
29.01 BETA-LACTAM ANTIBIOTICS
Penicillins - abs/distrib/elim
oral absorption varies
can also be given IM or IV
pass into all body fluids
cross the placenta but not the blood-brain barrier unless the meninges are inflamed
excreted in the urine (blocked by probenecid)
29.01 BETA-LACTAM ANTIBIOTICS
Penicillins - clinical uses
bacterial meningitis - benzylpenicillin
skin, bone and joint infections - flucloxacillin
animal bites - co-amoxiclav
pharyngitis - phenoxymethylpenicillin
otitis media, bronchitis, pneumonia - amoxicillin
syphilis - procaine, or benzathine penicillin
endocarditis - benzylpenicillin (with aminoglycoside)
infections with Pseudomonas aeruginosa - piperacillin, ticarcillin
29.01 BETA-LACTAM ANTIBIOTICS
Penicillins - adverse effects
hypersensitivity reactions (rashes, urticaria, angioedema, fever, arthralgia, anaphylaxis)
29.02 BETA-LACTAM ANTIBIOTICS
Cephalosporins and cephamycins: ceftriaxone, cefotaxime, cefuroxime - actions
bactericidal
interfere with cell wall synthesis in dividing bacteria
29.02 BETA-LACTAM ANTIBIOTICS
Cephalosporins and cephamycins: ceftriaxone, cefotaxime, cefuroxime - MOA
bind to and inhibit the enzyme that cross-links the peptide chain of the newly formed ‘building blocks’ to the peptidoglycan cell wall backbone
29.02 BETA-LACTAM ANTIBIOTICS
Cephalosporins and cephamycins: ceftriaxone, cefotaxime, cefuroxime - abs/distrib/elim
some cephalosporins given orally, but most given IM or IV
pass into all body fluids
excreted in the urine (blocked by probenecid)
excretion mostly via kidneys, but 40% of ceftriaxone is eliminated in the bile
29.02 BETA-LACTAM ANTIBIOTICS
Cephalosporins and cephamycins: ceftriaxone, cefotaxime, cefuroxime - clinical use
septicaemia - cefotaxime, cefuroxime
pneumonia caused by susceptible organisms, meningitis - ceftriaxone, cefotaxime
biliary tract infections, urinary tract infections, sinusitis - cefadroxil
29.02 BETA-LACTAM ANTIBIOTICS
Cephalosporins and cephamycins: ceftriaxone, cefotaxime, cefuroxime - resistance
some pneumococci, meningococci and gonococci have decreased sensitivity
29.02 BETA-LACTAM ANTIBIOTICS
Cephalosporins and cephamycins: ceftriaxone, cefotaxime, cefuroxime - adverse effects
hypersensitivity reactions (rashes, urticaria, angioedema, fever, arthralgia, anaphylaxis)
GIT disturbances
rarely: hepatitis and cholestatic jaundice
29.03 BETA-LACTAM ANTIBIOTICS
Carbapenems: imipenem, meropenem, ertapenem - actions
bactericidal
interfere with cell wall synthesis in dividing bacteria
29.03 BETA-LACTAM ANTIBIOTICS
Carbapenems: imipenem, meropenem, ertapenem - MOA
bind to and inhibit the enzyme that cross-links the peptide chain of the newly formed ‘building blocks’ to the peptidoglycan cell wall backbone
29.03 BETA-LACTAM ANTIBIOTICS
Carbapenems: imipenem, meropenem, ertapenem - abs/distrib/elim
given by IV infusion
pass into all body fluids including the CSF
inactivated by renal enzymes so must be given with cilastatin which inhibits the relevant enzymes
29.03 BETA-LACTAM ANTIBIOTICS
Carbapenems: imipenem, meropenem, ertapenem - clinical use
broad spectrum: active against gram-positive, gram-negative and anaerobic bacteria
not active against MRSA
used to treat severe polymicrobial hospital-acquired infections, e.g. septicaemia, pneumonia, complicated urinary infections
29.03 BETA-LACTAM ANTIBIOTICS
Carbapenems: imipenem, meropenem, ertapenem - adverse effects
GIT disturbances, rashes, injection site reactions
29.04 BLOCKERS OF PEPTIDOGLYCAN SYNTHESIS
Glycopeptides: vancomycin, teicoplanin - actions
inhibits bacterial cell wall peptidoglycan synthesis
29.04 BLOCKERS OF PEPTIDOGLYCAN SYNTHESIS
Glycopeptides: vancomycin, teicoplanin - MOA
inhibit the synthesis of the cell wall in sensitive bacteria
these drugs are slowly bactericidal for dividing microorganisms
impair the permeability of the bacterial cell membrane and RNA synthesis
29.04 BLOCKERS OF PEPTIDOGLYCAN SYNTHESIS
Glycopeptides: vancomycin, teicoplanin - abs/distrib/elim
given IV
vancomycin plasma half-life ~8h
vancomycin given orally for treatment of Clostridium difficile
29.04 BLOCKERS OF PEPTIDOGLYCAN SYNTHESIS
Glycopeptides: vancomycin, teicoplanin - clinical use
vancomycin used in a wide range of serious infections, including septicaemia, and treatment of MRSA
29.04 BLOCKERS OF PEPTIDOGLYCAN SYNTHESIS
Glycopeptides: vancomycin, teicoplanin - adverse effects
hypersensitivity reactions, ototoxicity and nephrotoxicity
phlebitis at infusion site
29.04 BLOCKERS OF PEPTIDOGLYCAN SYNTHESIS
Glycopeptides: vancomycin, teicoplanin - special notes
daptomycin is a relatively new lipopeptide antibacterial with similar spectrum to vancomycin
used for treatment of MRSA
telavancin is also active against MRSA with longer duration of action than vancomycin
29.05 BACTERIAL PROTEIN SYNTHESIS BLOCKERS
Tetracyclines: doxycycline, tetracycline, oxytetracycline - actions and MOA
interfere with bacterial protein synthesis by competing with tRNA for the A site of the ribosome and reversibly inhibiting its binding to the mRNA codons in the 30S subunit