Clinical Uses of Antibiotics Flashcards
how are most penicillins administered
IM or IV
not very soluble or stable in stomach acid
what does the R-group of a penicillin determine
selectivity, solubility, stability, bioavailability, beta-lactamase resistance
what penicillins are beta-lactamase sensitive
benzylpenicillin, phenoxymethylpenicillin
what penicillins are beta-lactamase resistant
flucloxacillin, temocillin
what are some broad spectrum penicillins
ampicillin, amoxicillin, co-amoxiclav
what penicillins are anti-pseudomonal
piperacillin
what are the pharmacokinetics of benzylpenicillin
IM or IV slow infusion, high blood conc achieved rapidly, non-toxic, good diffusion into body and tissues, low CSF levels, long post-antibiotic effect, rapid excretion in urine
how to maintain benzylpenicillin blood levels
administer large doses
frequent dosing
what is benzylpenicillin used for
mild to moderate throat infections, otitis media, cellulitis, pneumonia, endocarditis, meningitis
what causes meningitis
neisseria meningitis, stapholococcus pneumoniae, haemophilus influenzae
what are the pharmacokinetics of amoxicillin
70-90% absorption, peak blood conc after 90 min, good CSF levels in meningitis, mainly excreted in urine
what are the clinical uses of amoxicillin
RTIs, oral infections, otitis media, sinusitis, UTIs, GI, listerial meningitis
what are the side effects of amoxicillin
hypersensitivity, neurotoxicity, renal failure, diarrhoes and pseudomembranous colitis (c. diff)
what is the origin of cephalosporins
isolated from cephalosporium acremonium
what are the properties of cephalosporins
resistant to beta lactamases, originally active against gram positive bacteria, risk of c.diff
what is the cephalosporin activity aainst gram positive bacteria
affinity for PBPs, resistant to beta lactamases
what is the cephalosporin activity against gram negative bacteria
penetration through outer membrane
what are second generation cephalosporins
active against gram positive and some gram negatives
more resistance to beta lactams
used for severe infections
what are third generation cephalosporins
broad spectrum, increased activity and increased resistance to beta lactamases
active against pseudonomas
what are carbapenems
inhibitors of cell wall synthesis
highly resistant to beta lactamases, broad spectrum activity
what are glycopeptides
inhibitors of cell wall synthesis
only active against gram positive (too large to pass through membrane of gram negative)
what are some examples of glycopeptides
vancomycin, teicoplanin
what is vancomycin used for
systemic infections (IV) orally (c.diff)
what is teicoplanin used for
IM or IV injection for systemic infections
also for infection from b-lactam resistant organisms (MRSA)
what are some features of vancomycin and teicoplanin
penetrate CSF, excreted by kidney, cannot be absorbed through the gut, can be used orally for c.diff
what are the side effects of vancomycin and teicoplanin
pain at injection site, renal toxicity, ototoxicity, blood disorders, anaphylactoid reactions
what antimicrobials affect bacterial membranes
polymyxin (colistin) - active on gram negative bacteria (disrupt membrane and cause leakage of cytoplasm)
what are polymyxins used for
IV for resistant gram negative infections, nebulised or DPI for p.aeruginosa in GF patients
what are the side effects of polymyxins
highly neurotoxic and nephrotxic
what antimicrobials affect bacterial membranes
lipopeptides like daptomycin
how does daptomycin (lipopeptide) work
active on gram positive bacteria
rapid depolarisation of cytoplasmic membrane resulting in loss of function due to leakage of ions and depolarisation of cell
what are the uses of lipopeptides
IV for skin and soft tissue infections, endocarditis caused by resistant gram positives (MRSA)
what are some side effects of lipopeptides
nephrotoxicity, myopathy, peripheral neuropathy, colitis
what are examples of metabolic inhibitors of nucleic acid synthesis
sulphonamides, trimethoprim
sulfonamides more selective than trimethoprim
where do sulphonamides act
on para-amino benzoic acid conversion to dihydropteroic acid in nucleic acid synthesis
where does trimethoprim work
on dihydrofolic acid in nucleic acid synthesis
what are the uses of sulphonamides
limited uses
what are the uses for trimethoprim
UTI and acne