Antimicrobials Flashcards
in penicillin bactericidal or bacteristatic?
bactericidal
griseofulvin has what effect on P450?
inducer
methylation of a ribosomal binding site in bacteria is a common resisitance mechanism against which antibiotics?
aminoglycosides
what are the penicillinase-resistant penicillins?
nafcillin, dicloxacillin, oxacillin
what antimicrobials stop binding of aminoacyl-tRNA to 30S ribosomal subunit?
tetracyclines
what species and polymerase/RTase is the preferential target of ganciclovir?
what is different about valganciclovir?
CMV DNA polymerase; must be activated by CMV viral kinase
valganciclovir = better oral availability, is prodrug
how does NRTIs affect viral life cycle exactly?
incorporation into newly synthesised DNA, but cannot then form 3’-5’ phosphodiester bond to continue DNA replication
why does acyclovir affect HSV/VZV and not CMV/EBV?
CMV/EBV lacks the guanosine analog kinase that is needed to activate acylovir (and family) within the infected cell
what are the electrolytes that need monitoring with amphotericin B therapy?
K+ and Mg++
rifampin mechanism of action
adverse effects
inhibits bacterial DNA-dependent RNA polymerase
red-orange body fluids, cytopenia, GI upset
what is the difference between penicillin G and V?
G = IV and IM, V = oral
what advice must be given about taking tetracyclines PO?
do not take with milk or antiacids because divalent cations stop gut absorption of these drugs
aminoglycosides are ineffective against what kind of bacteria? why?
anaerobes
O2 is required for uptake
what generation are cefazolin and cephalexin? what bugs are they good against?
1st generation - PEcK = proteus, E coli, Klebsiella
rocky mountain spotted fever and meningites (H flu, n meningitidis strep pneumo) can all be successfully treated with?
chloramphenicol
what is the mechanism of action of terbinafine?
inhibits synthesis of ergosterol by inhibiting squalene epoxidase
how does vancomycin resistance occur?
in enterococcus by changing cell wall to D-ala-D-lac
what generation are cefaclor, cefoxitin and cefuroxime?what bugs are they good against?
2nd generation HENS PEcK = haemophillus, enterobacer, neisseria, serratia PEcK
what are the antipseudomonan penicillins?
piperacillin, ticaracillin
what is the indication for sofosbuvir?
RNA-dependent RNA polymerase inhibitor specific to hepatitis C
what are the main adverse effects of ganciclovir?
bone marrow suppression
what antifungal gives fever and chills upon administration?
does it get better or worse with subsequent administration?
amphotericin B
gets better, treatment with antipyretics and antihistamines can ameliorate
other than gram +ve’s, what can you use penicillin for?
gram -ve cocci (N meningitidis) and T pallidum spirochetes
what are 3 carbapenems?
Imipenem, meropenem, ertapenem
what antibiotics work against chlamydia trachomatis?
doxycycline and macrolides (azithromycin erythromycin)
what is the mechanism of action of saquinavir?
HIV protease inhibitor - saquinavir
protease coded by pol gene. protease inhibitors stops maturation of new virions
what are the specific fungal species and subcellular structure of griseofulvin?
dermatophites
microtubular proteins
what do enfuviride and maraviroc do? how are they different?
both HIV fusion blockers.
enfuvirtide - binds gp41 inhibiting viral fusion
maraviroc - blocs CCR5, inhibiting binding with gp120 (docking)
what antibacterials affect which portions of the bacterial ribosome?
buy AT 30, CCEL at 50
aminoglycosides, tetracycline - 30S
clindamycin, chloramphenicol, erythromycin (& macrolides), linezolid - 50S
what antiretroviral class gives hyperglycaemia and cushing-like syndrome as side effects?
protease inhibitors (-navirs)
what drug blocks peptidyltransferase at the 50S subunit?
cholamphenicol
of the penicillinase-sensitive penicillins, which has a greater oral bioavailability?
amOxicillin =Orally available
what antibiotics can affect long bone growth in children?
tetracyclines
what is red man syndrome and how do you stop it?
diffuse erythematous rash wtih vancomycin therapy.
prevent - pre-treat with antihistamine and slow infusion rate
HLA-B 5701 means you cannot give?
what would happen?
abacavir (NRTI) in HIV/AIDS treatment
alters MHC I resulting in hypersensitvity reaction (IV) with desquamating rash, GI upset, fever & malaise
why is chloroquine ineffective against vivax and ovale in particular?
these set up latent infection in the liver.
chloroquine kills plasmodium in the blood but not the exo-erythrocyte phase (liver)
for this treat with primaquine to eradicate hypnozoites
what are two distinguishing side effects of cephalosporin?
- disulphiram reaction with alcohol
- vitamin K deficiency
3 drugs for MRSA, mechanism of action and side effects
- vancomycin - binds D-ala-D-ala - red man syndrome, nephrotoxic
- daptomycin - pore in membrane - CPK elevation & myopathy
- linezolid - binds 50s ribosomal subunit - thrombocytopenia, optic neuritis
are antipseudomonals susceptible to penicillinase?
yes - ‘pip-taz’.. always give with penicillinase inhibitor
what antifungals target the cell wall? the cell membrane?
wall = capsofungin
membrane = amphotericin, nystatin (bind ergosterol), -azoles (inhibit synthesis)
when is famicyclovir indicated mainly?
herpes zoster
what does and integrase inhibitor do?
what is the common part of the names to identify these ARVs?
inhibit integration of dsDNA to integrate into host cell chromosome, so no new viral mRNA is transcribed
integrase inhibitor = raltegravir, dolutegravir, elvitegravir
what is the mechanism of action of oseltamavir and what bug does it work against?
inhibits neuraminidase without need for intracellular activation
prevents influenza A/B from exiting the cell
in what patient group is doxycycline particularly useful and why?
renal failure, faecal excretion
how does vancomycin work?
binds D-ala-D-ala motif of cell wall precursor
c/o penicillin which acts as decoy D-ala-D-ala
what is the mechanism of action of foscarnet?
does this require intracellular activation?
foscarnet = pyrofosphate analog
binds & inhibits viral DNA/RNA polymerase and HIV reverse transcriptase
does not require kinase/intracellular activation
what must be given with imipenem?
cilastatin - inhibitor of renal dehydropeptidase I, slows renal inactivation of the carbapenem
are cephalosporins bactericidal or bacteristatic?
bactericidal (same mechanism as penicillins)
what are the adverse effects of acyclovir and family?
obstructive crystalline nephropathy and AKI if not adequately hydrated
what is the mechanism of action of acyclovir?
nucleoside analog that is activated intracellularly by viral enzyme thymidine kinase - hence few side effects in human tissue
inhibits herpesvirus DNA polymerase
what is the mechanism of penicillin resistance in MRSA?
mutation of the PBP target site
what bugs are killed by extended-spectrum penicillins?
HHELPSS haemophilus, H pylori, E coli, Proteus mirablis, Salmonella, Shigella
what class is neomycin?
aminoglycoside
what generation are ceftriaxone, cefotaxime, ceftazidime?
what bugs are they used against?
3rd generation - gram negatives resistant to other beta-lactams, cross BBB
ceftriaxone = meningitis, lyme disease, neisseria.
ceftazidime = pseudomonas
what are the penicillinase inhibitors?
claulanic acid, avibactam, sulbactam, tazobactam (CAST)
what are the side effects of aminoglycosides?
ototoxic, nephrotoxic, neuromuscular blockade
teratogenic
what is the mechanism of resistance against tetracyclines?
decrease intracellular accumulation by increased efflux or decreased uptake by different drug transporter coded for on a plasmid
what is the mechanism of action for acyclovir?
inhibitor of viral DNA polymerase
what is the mechanism of resistance against acyclovir (& family)
mutation of viral thymidine kinase, which is the viral enzyme required for phosphorylation and activation of these nucleoside analogs
what is the mechanism of resistance against cephalosporins?
structural change of PBPs
flattened eggs seen on the perianal tape test are treated with what?
bendazoles or pyrantel pamoate
nafcillin is useful for what bug?
staph aureus
what are the adverse effects of vancomycin?
NOT without trouble
nephrotoxic, ototoxic, thrombophelbitis
Red man syndrome
what is the mechanism of action for cidofovir?
intracellular activation?
indication?
inhibits viral DNA polymerase preferentially (still works on human protein a bit though)
no intracellular activation/phosphorylation required
CMV retinitis, acyclovir-resistant HSV
what does valacyclovir do better than acyclovir?
better oral availability
what antibiotics change the colour of your teeth?
tetracyclines
what medication interferes with bacterial DNA gyrase?
quinolones - good against gram-negatives
what is the toxicity of cidofovir and how do you get past this?
nephrotoxic
administer with probenecid and IV fluids
azole antifungals have what effect on P450?
inhibit P40
what is the mechanism for sulfonamides?
sulfamethoxazole (SMX), sulfisoxazole, sulfadiazine
antimetabolite = competes with para-aminobenzoic acid for incorporation into folic acid
mechanism of action of isoniazid? side effects?
inhibits mycolic acid synthesis
vitamin B6 deficiency, neurotoxic - give with pyridoxine
Hepatotoxic
what antimicrobial works through inhibition of arabinosyl transferase?
side effect?
ethambutol - optic neuropathy
what are the side effects of carbapenems?
seizures, GI upset, rash
what is a D-Ala-D-Ala analog?
penicillin - allows binding of PBPs (transpeptidases)
what bugs does ceftaroline cover that other cephalosporins do not? (3)
Listeria, MRSA and enterococcus faecalis
5th gen cephalosporin
what enzyme is needed to activate isoniazid?
intracellular catalase peroxidase
what class is streptomycin?
aminoglycoside
what is an antibiotic good against multi-drug resistant organisms that binds to the 30S subunit of bacterial ribosome
Tigecycline - tetracycline derivative
what is the benefits of using meropenem rather than other carbapenems? (2)
meropenem is resistant to renal dehydropeptidase I and has decreased risk of seizures
what generation is cefepime? what is it used for?
pseudomonas
what is the best drug for tinea corporis, a common dermatophytosis?
terbinafine
squalene epoxidase inhibitor
what is the main difference between NRTIs and NNRTIs?
NNRTIs (delavridine/efavirenz/nevirapine) do not require intracellular activation
how does isoniazid cause B6 deficiency?
direct hepatocyte damage
what class is amikacin?
aminoglycoside
what are the penicillinase-sensitive penicillins?
amox ampicillin aminopenicillins