t100 Antibiotics Flashcards
name an aminoglycoside
gentamicin
indications aminoglycosides
1) severe sepsis, inc where unidentified
2) pyleonephritis and complicated uti
3) biliary and intraabdo sepsis
4) endocarditis
spectrum of action aminoglycosides
gram negative aerobes
staphylococci
mycobacteria
Does NOT cover
streptococci
anaerobic bacteria
mechanism of action aminoglycosides
Inhibit protein synthesis 30S
bind irreversibly to bacterial ribosome(30S subunit) and inhibit protein synthesis.
when might aminoglycosides need to be combined with something else? what else?
combine with penicillin and/or metronidazole when organism unknown
(to cover streptococci and anaerobes)
most important adverse effects aminoglycosides?
nephrotoxicity and ototoxicity
aminoglycosides accumulate in tubular epithelial cells and cochlear and vestibular cells where they trigger apoptosis and cell death
nephrotoxicity = reduced urine output, rising serum creatinine and is potentially reversible
ototoxicty = hearing loss, tinnitus (cochlear damage) vertigo (vestibular damage) after infection, may be irreversible
routes of administration aminoglycosides
only IV
How to reduce the risk of adverse effects aminoglycosides? contraindications?
Administartion:
- diluted and infuses slowly over 30 mins to prevent high concs which can damage the ear
Patient:
-neonates, elderly, renal impaired most at risk - calculate dose correctly and monitor serum closely
- myasthenia gravis avoid unless absolutely neccessary (impairs neuromuscualr transmission
Interactons:
- ototoxicity more likely if coprescribed wirh loop diuretics or vancomycin
- nephrotoxicity more likely if co-prescribed with ciclosporin, platinum chemo, cephalosporins and vancomycin
Monitoring:
- renally excreted, monitor plasma drug concentartions with dose adjustment to prevent complications
name 2 cephalosporins and 1 carbepenem
- cefalexin
- cefotaxime
- meropenem
indications cephalosporins and carbepenems?
- oral cephalosporins are 2nd/3rd line option for urinary and respiratory tract infections
- IV cephalosporins and carbepenems are reserved for infections that are very severe or complicated or caused by resistant organisms
spectrum of action cephalosporins and carbapenems
broad spectrum
gram +/-
MoA cephalosporins and carbapenems?
B-lactam ring
Inhibit cell wall synthesis
inhibit enzymes responsible for cross linking petidoglycans in bacterial cell walls –> weakens cellw all –> cant maintain osmotic gradient –> bacterial swelling, lysis, death
more resistant ro b-lactamases than penicillins due to fusion of b-lactam ring with dihydrothiazine ring or uniqe side chain
adverse effects cephalosporins and cabapenems?
common: GI upset N&V
uncommon: c.diff
hypersensitivity including immediate and delayed reactions may occur (CARBAPENEMS - CAUTION IN PEN-ALLERGIC PATIENTS) cephalosporins are fine in pen allergy
CNS toxicity inc seizures with carbapenems (reduces seizure threshold) esp patients taking high dose or pts with renal impairment
routes of administration cephalosporins and carbepenems?
cephalosporins oral (eg cefalexin), tablets, capsulesm oral suspensipn OR injection IV, bolus, infusion or IM
carbapenems only IV injection or infusion
How to reduce risk of adverse effects cephalosporins and carbapenems?
Patient:
- CHECK NOT ALLERGIC TO OTHER B-LACTAM ABX
- use with caution in pts at risk of c,diff
- use caution in epilepsy
- dose reduction in renal impairment
Interactions:
- enhances anticoagulant effect of warfarin (INR increases)
- increase nephrotoxicuty of aminoglycosides
- reduces plasma conc and efficacy of valproate
Monitoring:
- symptoms and inflammatory markers
Name 3 macrolides
clarithromycin
azithromycin
erythromycin
indications macrolides
- resp and soft tissue as an alternative to penicilin when this is contraindicated by allergy
- in severe pneumonia added to a penicillin to cover atypical organisms
- eradication of h.pylori (with amox/metro and PPI)
spectrum of action macrolides
broad spectrum
better for gram +
atypical
synthetic eg clarith and azith have increased acitivity against gram negative comapred to eryth
MoA macrolides
Inhibit protein synthesis (50S)
bind to 50S ribosome subunit
inhibit bacterial protein synthesis and blocks translocation ‘bacteriostatic’ - stops bacterial growth - assist immune system in removing them
adverse effects macrolides?
adverse effects most common and severe with erythromycin
- irritant : N&V, abdo pain, diarrhoea
- thrombophlebitis when given IV
- allergy (but not related at all to penicillins)
- antibiotic-associated colitis
- liver abnormalities inc choleststic jaundice
- prolongation of QT interval
- ototoxicity in high doses = tinnitus
- E and C inhibit cytochrome P450 therefore increases plasma conc of drugs such as warfarin and statins .
- prescribe with caution in patients taking drugs that prolong the QT interval or cause arryth such as amiadarone, antipsychitics, quinine, quinolone abx, SSRIs
metabolism of macrolides
mostly hepatic with some renal contribution
how to reduce adverse effects macrolides
patient:
- dont prescribe if history of hypersensitivity
- caution in hepatic impairment
- dose reduction in severe renal impairment
Interactions:
- E and C inhibit cytochrome P450 therefore increases plasma conc of drugs such as warfarin and statins .
- prescribe with caution in patients taking drugs that prolong the QT interval or cause arryth such as amiadarone, antipsychitics, quinine, quinolone abx, SSRIs
Monitoring:
- symptoms, examination, inflammatory markers
routes of administration macrolides
oral or IV infusion
most commonly prescribed macrolide, why?
clarithromycin
fewer SE than erythromycin
cheaper than azithromycin
name 1 nitroimidazole abx
metronidazole
Indications metronidazole
- antibiotic associated colitis caused by c.diff
- oral infections (such as dental abscess) or aspiration pneumonia caused by gram negative anaerobes from the mouth
spectrum of action metronidazole
anaerobic bacteria
protozoa eg trichomonas, amoebic dystentry, giardia
MoA metronidazole
inhibit protein synthesis
by disrupting the DNA of the susceptible bacteria and inhibiting the protein synthesis of the cell wall leading to cell death;
adverse effects metronidazole?
Drug:
- GI upset
- immediate and delayed hypersensitivity
- if prolonged: peripheral and optic neuropathy, encephalopathy, seizures
Patient:
- dose reduce in liver disease
Interactions:
- inhibits acetylaldehyde dehydrogenase which clears alcohol metabolite so cannot drink on metro - will cause disulfiram-like reaction
- inhibits p450 so reduces metabolism of drugs such as warfarin and phenytoin
- p450 enzyme inducers such as phenytoin and rifampicin can reduce plasma conc of metro and reduce antimicrobial efficacy
routes of administartion metronidazole
oral
IV
rectal
topical gel
name 1 nitrofuran antibiotic
nitrofurantoin
indications nitrofurantoin
- first line antibiotic fro uncomplicated lower urinary tract infections