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132 Cards in this Set
- Front
- Back
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Aminoglycosides
3 |
- Neomycin
- Amikacin - Gentamicin |
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PK of aminoglycosides (solubility)
Distribution What about in neonates? |
- highly hydrophillic, lipid insoluble
- low volume of distribution - does not cross membranes well - better distribution in neonates due to increased % water in the body |
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Are aminoglycosides absorbed well from the gut? What is the exception?
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- not well absorbed from the gut
- neonates absorb orally for enteric infections |
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Are aminoglycosides protein bound?
What would they bind to? Name an example causing more to be bound, therefore decreasing efficacy |
- minimally protein bound
- bind to cellular debris - peritonitis will cause binding, decreased efficacy |
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MOA for aminoglycosides
static or cidal |
- protein synthesis inhibitor
- bactericidal |
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are aminoglycosides good for intracellular infections?
why or why not? |
- no
- hydrophyllic, so dont cross membranes well |
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aminoglycoside bacterial penetration is dependent on what factor?
what does this tell us about spectrum? |
- oxygen dependent
- NOT good for anaerobes |
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aminoglycoside spectrum
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- Aerobic Gram negative enterobacteriaciae
- Aerobic some gram + (strep) |
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what aminoglycoside has the broadest spectrum?
when might we use this vs. the others? |
- Amikacin
- may be used for bacteria resistant to gentamicin |
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ROA for aminoglycosides
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- IV
- IM - SC |
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name the 2 most important adverse effects of aminoglycosides
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- nephrotoxicity
- cochlear toxicity |
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primary route of excretion for aminoglycosides
excreted concentrations vs. serum concentratoins |
- renal excretion
- urine [ ] may be 100x serum [ ] |
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what effect does renal disease have on aminoglycoside [ ]?
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- renal disease will cause toxicity
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WDT for gentamicin
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- 18 months
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PD of aminoglycosides
what is the target MIC? |
- peak dependent bactericidal
- 8-10x MIC is target serum [ ] |
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what ROA is contraindicated in aminoglycosides
what is the dosing regimen recommended? |
- CRI
- once daily |
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what aminoglycoside has the most severe renal toxicity?
should it be used systemically? If not, how should it be used? |
- neomycin has most severe renal toxicity
- it should not be used systemically - enteric use only |
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nephrotoxicity from aminoglycosides is considered what?
name the 2 phases |
- bimodal nephrotoxicity
- initial non-azotemic phase - clinical azotemic phase |
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if a patient has azotemic nephrotoxicity from aminoglycoside therapy, will discontinuation of therapy stop the azotemia?
What might instead occur? |
- no
- azotemia may increase in severity |
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Ototoxicity of aminoglycosides:
cats present with? dogs present with? |
- cats show vestibular effects
- dogs show auditory effects |
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what drug ixn can occur with aminoglycosides?
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- potentiate neuromuscular blockade if given with anesthesia or neuromuscular blocking agents
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Gentamycin pig label
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- IM for pigs <3 days old
- trt colibacillosis - all other labels for oral use |
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Gentamicin beef label
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- ocular spray
- trt pinkeye - no tolerance for gentamicin in tissue |
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neomycin beef label
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- oral use only
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aminoglycoside WDT
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- 18 months
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what does FARAD stand for?
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- Food Animal Residue Avoidance and Depletion program
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name the only Aminocyclitol, what type of animal is it used for?
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- Spectinomycin
- mainly for food animal |
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PK of aminocyclitols
VD? |
- water soluble
- poorly lipid soluble - low volume of distribution |
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MOA for aminocyclitols
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- protein synthesis inhibitor
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aminocyclitols
static or cidal |
- bacteristatic
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Spectrum for aminocyclitols
plus what other microbe? |
- Aerobic Gram negative
- Aerobic some Gram positive (staph, strep) - includes Mycoplasma |
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Are aminoglycosides and aminocyclitols good for anaerobic infections?
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- NO NO NO
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ROA for aminocyclitols
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- IM
-IV - SC |
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oral administration of aminocyclitols is only good for what purpose?
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- GIT infections
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adverse effects of aminocyclitols vs. aminoglycosides, better or worse?
what effect is similiar for both? When might this be important? |
- less adverse effects
- both will have neuromuscular blockade - may have to bag a patient under anesthesia |
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Beta Lactam aka what?
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- penicillins
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Penicillin G forms
3 |
- Na and K PenG
- Procaine PenG - Benzathine PenG |
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Na/K Pen G ROA
Dosing rate? |
- IV injection
- Q 6 hours |
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Procaine PenG PK
What is special? ROA |
- flip flop kinetics
- rate of absorption determines elimination, not elimination from the body - SC admin |
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Benzathine PenG PK (peak and tail?)
Size? |
- flip flop kinetics
- low peak and long tail, creates a residue - largest of PenG forms |
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name the 2 penicillinase-resistant penicillin
is MRSA still resistant? |
- oxacillin
- cloxacillin - MRSA still resistant |
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aminopenicillins
name 2 what do these drugs add to the Pen spectrum? |
- ampicillin
- amoxicillin - extended the gram negative spectrum |
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antipseudomonal (extended spectrum) penicillin
name 1 |
- ticarcillin
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potentiated penicillins
name 2 |
- amoxicillin-Potassium clavulanate (Clavamox, Augmentin)
- Ampicillin-sulbactam |
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name the 2 trade names for amoxicillin-potassium clavulanate
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- Clavamox
- Augmentin |
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what is the purpose of the clavulanate in amoxicillin-potassium clavulanate? (Clavamox, Augmentin)
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- clavulanate is a suicide inhibitor
- penicillinase bacteria act on the clavulanate and not the penicillin - allows the penicillin to be effective |
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Penicillin solubility
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- water soluble
- poorly lipid soluble |
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what is in the penicillin molecule that has antibacterial activity?
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- beta lactam ring
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penicillinase enzyme destroys what part of the molecule?
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- beta lactam ring
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what penicillins can be given IV?
2 |
- Na/K PenG
- Amoxicillin |
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what penicillin can cause toxicity if given IV?
in what scenario would this be important? |
- Procaine PenG
- important for horse racing, will cause a positive on a lidocaine test |
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penicillin MOA
what occurs in the bacteria? |
- inhibit cell wall synthesis
- cell wall crosslinking is defective, as the bacteria tries to replicate the cell wall is weakened - death due to osmotic pressure |
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penicillins are most active against bacteria that are doing what?
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- rapidly growing and dividing
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does penicillin trt mycoplasma infections?
why or why not? |
- no
- mycoplasma has no cell wall |
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name an aminoglycoside and a penicillin often used in combo?
why do we do this? |
- gentamicin for Gram negative aerobes
- PenG for Anaerobic activity |
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what spectrum of bugs are penicillins most noted for?
what are they not so great for? |
- used for anaerobe activity
- not so great for Gram neg aerobe |
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name a penicillin group that has spirochete activity?
name the two drugs in this category name the two bugs |
- aminopenicillins
- amoxicillin and ampicillin - leptospira and borrelia |
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why might we use aminopenicillin vs a PenG?
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- aminopenicillins have an oral use
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antipseudomonal (extended spectrum) penicillin spectrum
Increased for what group at the expense of what other group? do they have anaerobic activity? |
- increased Gram neg aerobe at the expense of gram pos aerobe
- no anaerobic activity |
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potentiated penicillins are used to increase activity against what 2 bacteria
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- penicillinase producing Staph
- beta hemolytic Strep |
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how do Gram pos and neg penicillinases differ?
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- Gram pos penicillinase diffuses out into the surrounding environment
- Gram negative penicillinase concentrates between the membrane layers |
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name the penicillinase-resistant penicillin
what bacteria is it used for? |
- oxacillin
- Staph spp. |
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Penicillin resistance is mediated by what in:
Gram positive: 1 way Gram negative: 3 ways |
- gram positive: inducible, plasmid mediated extracellular enzymes that destroy the beta lactam ring
- gram negative: inherent resistance due to lack of penicillin binding proteins, low permiability of beta lactam ring, beta lactamase enzymes |
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Na/K PenG ROA
which is most important? |
- IV: PenG for IV use
-IM -SC |
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procaine PenG ROA
which one is contraindicated? |
- IM
-SC - contraindicated for IV use |
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Benzathine penicillin ROA
which will result in an extended residue? |
- IM: residue potential
- SC |
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are penicillins static or cidal
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cidal
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what is the only oral PenG?
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- penicillin V
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which 2 penicillins have intramammary formulations?
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- cloxacillin
- amoxicillin |
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ampicillin ROA
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- IV
- IM and SC - oral |
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amoxicillin ROA
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- IV
- IM and SC - oral - intramammary |
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Cloxacillin ROA
what group is this in? |
- intramammary
- penicillinase resistant group |
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amoxicillin clavulanate ROA
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oral
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ticarcillin ROA: general
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- injectible
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do penicillins penetrate the CNS?
when might they? |
- no
- meningitis or inflammation of the membranes |
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elimination for penicillins?
why is this important? |
- renal elimination
- can be used for cystitis |
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is amoxicillin or ampicillin better for oral admin?
why? IMPORTANT!! |
- amoxicillin better
- about twice the %F oral |
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Beta lactam bactericidal activity is based upon time above MIC, how does this relate to the MOA?
what does the optimal drug curve look like? |
- penicillin needs to be present when the cells are rapidly dividing
- want a long slow curve to keep serum [ ] above MIC for a longer time |
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an adverse effect of penicillin can be anaphylaxis, is this considered an adverse effect for all penicillin classes?
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- yes
- consider all penicillins cross reactive |
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what penicillin could cause violative residues in a horse?
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- Procaine PenG
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what penicillin would cause "squirts" in a horse after IV injection
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- K PenG
- increased propulsion |
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Penicillin G may be fatal to what animals?
name 2 |
- guinea pigs
- rabbits - non-ruminant herbivores |
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what penicillin should never be given IV
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- Procaine PenG
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what penicillin can lead to cardiac arrest if given too rapidly IV
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- K PenG
- due to rapid release of K |
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what penicillin should be avoided in animals with bleeding disorders?
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- ticarcillin
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beta lactamase inhibitors
what is their nickname? name the 3 drugs |
- suicide inhibitors
- clavulanic acid - sulbactam - tazobactam |
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do clavulanic acid and sulbactam have antimicrobial activity by themselves?
what is their function? |
- no
- bind with penicillinase |
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what spectrum (bacteria) is added by having the clavulanic acid-amoxicilin versus the amoxicillin
name 1 spectrum, 2 bacteria |
- anaerobic activity improved
- enterobacteriaceae - staph |
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what is an adverse effect of amoxicillin/clavulanic acid in cats?
what can continued dosing cause? |
- GIT upset, inappetance
- hepatic lipidosis can occur due to inappetance |
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name 2 animals that clavulanic acid or sulbactam should never be used in
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- guinea pigs
- rabbits |
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how are cephalosporins classified?
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- by activity
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name the 4 first generation cephalosporins
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- cefadroxil
- cephalexin - cefaprin - cefazolin |
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what is the most common use for cefazolin?
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- prophylactic antimicrobial for soft tissue surgery
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name the only ORAL third generation cephalosporin and give its trade name
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- cefpodoxime
- VL simplicef |
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name the 5 third generation parenteral cephalosporins
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- cefotaxime
- ceftazidime - ceftriaxone - ceftiofur Na, hydrochloride, and crystalline free acid - cefovecin |
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name the only 4th generation cephalosporin
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- cefepime
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general spectrum for 1st generation cephalosporins
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- heavy Gram positive aerobe
- light Gram negative aerobe |
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general spectrum for 2nd generation cephalosporins
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- heavy Gram positive (same as 1st gen)
- increased Gram negative |
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general spectrum for 3rd generation cephalosporins
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- some strep and staph
- increased Gram negative more than 2nd |
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what 3rd generation cephalosporin has the best anaerobe activity?
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cefotaxime
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what 3rd generation cephalosporin has the best Pseudomonas activity
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ceftazidime
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what was the purpose of the 4th generation cephalosporins?
for use on what 2 bacteria? name the drug |
- attempt to overcome resistance
- Pseudomonas, enterobacteriaceae - cefepime |
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is there a milk or slaughter WDT with cephalosporins?
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- no milk WDT
- there is a slaughter WDT |
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solubility of cephalosporins
what other group are they similar to? |
- high water soluble, low lipid soluble
- similar to penicillins |
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cephalosporins
static or cidal killing is dependent on what |
- cidal
- killing dependent on time above MIC |
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name a 3rd generation cephalosporin with an extremely long half life
why is that? |
- cefovecin
- very high protein binding |
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how long does the therapeutic free drug concentration of cefovecin last after a single admin?
7 days for what 2 bugs 14 days for what 1 bug |
- staph intermedius, P. multocida
- strep canis |
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does cefovecin reach the MIC 90 for E. coli, Pseudomonas, or enterococci?
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- no
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ceftiofur administration
IV or IM/SC why? |
- PK values no different for the ROA
- IM and SC values the same - better to just go SC |
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ceftiofur hydrochloride is different from ceftiofur sodium in what way?
name the trade name drug |
- ceftiofur hydrochloride comes ready to use (RTU) in a cottonseed oil carrier
- excenel |
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best ROA for ceftiofur hydrocholride and sodium
why? |
- SC
- no PK difference from IM and IV |
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ceftiofur crystalline free acid trade name
approved ROA |
- Excede
- under skin of the ear - at the base of the ear |
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why would you give excede SC in the neck?
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-you wouldn't/can't
contaminate meat - WDT will increase to 120 days |
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for bovine, swine, and equine, what is ceftiofur crystalline free acid labeled for?
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- treatment of respiratory disease
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what is special about cefpodoxime proxetil?
what is the trade name? |
- oral admin
- simplicef |
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does oral cefpodoxime proxetil work for pseudomonas?
what other 3rd gen is not recommended for Pseudomonas? |
- no
- similiar to cefovecin |
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what bacteria is showing increased resistance to cephalosporin?
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- Salmonella Newport
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what 4 cephalosporins reach the CNS in human patients?
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- ceftazidime
- ceftriaxone - cefipime - cefotaxime |
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what is desfuroylceftiofur, and why is it important
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- active metabolite in ceftiofur
- this is what has the antimicrobial activity |
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what can be an adverse effect of cephalosporins?
similar to what other group? |
- anaphylactic/allergic reactions
- similar to penicillins |
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what 3 adverse effects can occur after oral cephalosporin admin?
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- vomiting
- anorexia - diarrhea |
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what drug is contraindicated for patients being treated for seizures?
name the cephalosporin and the other drug involved |
- cephalexin
- phenobarbital |
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what is the one big NO-NO for cephalosporins?
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- no extra label use of cephalosporins for food animals
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name the 2 carbapenems
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- imipenem
- meropenem |
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name the 4 drug groups that make up the beta lactams
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- penicillins
- cephalosporins - carbapenems - monobactams |
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imipenem is toxic to what?
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- brush border of proximal tubule cells in kidney
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name the carbapenem (beta lactam) known to have the widest spectrum
it has good activity against what 2 important bacteria(s) |
- imipenam
- pseudomonas aeruginosa - enterbacteriaceae |
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ROA for imipenem is usually done this way
can it be given IM and SC? what is added? why? |
- usually done IV over 15-30 minutes
- can be given IM or SC reconstituted with 1% lidocaine to control pain |
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meropenem ROA in dogs
why different than imipenem? |
- SC
- imipenem is painful on injection |
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carbapenem adverse effects: general
2 things Avoid use when??? |
- GIT disturbance
- CNS toxicity (imipenem) - avoid in seizure patients |
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name the 1 monobactam
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- aztreonam
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what is the only spectrum aztreonam is used for
what is it used to replace? |
- Gram negative aerobes
- used to replace aminoglycosides in combo therapy |
