Antibacterial Agents Overview Flashcards by Kim Grace

Cell Wall Synthesis Inhibitors

Penicillins, cephalosporins, carbapenems, and miscellaneous drugs

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Active on cell walls, inhibiting transpeptidase and promoting cross-linking for a stronger wall

Penicillins

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Penicillins are ________ on cell walls, inhibiting _____________ and promoting cross-linking for a stronger wall

active; transpeptidase

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Defense mechanisms of Cell Wall Synthesis Inhibitors

Beta-lactamase enzymes countered by inhibitors like clavulanic acid

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Resistance mechanisms of Penicillins:

Beta-lactamase, structural changes in proteins, or alterations in the outer wall.

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Cell walls have sites that are amenable to ___________

transpeptidation

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Cross-linking is facilitated by proteins acting on _____________ of the cell wall, linking them together

peptidoglycans

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Penicillins have a ________ ring that binds to the protein

B-lactam

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By inhibiting the penicillin binding protein, __________ of the cell wall will occur.

autocatalysis

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B-lactamases (penicillinases) ___________ the B-lactam ring

break down

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mechanism of most types of resistance

B-lactamases (penicillinases) break down the B-lactam ring

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The breaking down of the B-lactam rings are countered by inhibitors of these enzymes

Clavulanic acid (i.e. amoxicillin-clavulanate)
Sulbactam (ampicillin sulbactam)
Tazobactam (i.e. piperacillin-tazobactam)

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amoxicillin-clavulanate

Clavulanic acid

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ampicillin sulbactam

Sulbactam

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piperacillin-tazobactam

Tazobactam

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Changes in the porin structures in the outer wall (i.e. pseudomonas aeruginosa are seen in __________ resistance

methicillin resistance

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Penicillins that have very narrow spectrum

Methicillin, nafcillin, oxacillin

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__________________ are resistant to all penicillins

methicilin resistant staphylococcus aureus

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Penicillin linked to interstitial nephritis

Methicillin

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Penicillin associated with neutropenia

Nafcillin

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Penicillins that have wider spectrum but are still susceptible to B-lactamases

Ampicillin, amoxicillin

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Ampicillin, amoxicillin are enhanced when used with ____________

clavulanate

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In ______________ infections, ampicillin is complementary with ________

eneterococcal; aminoglycosides

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Penicillins that have strong activity against gram-negative organisms

Piperacillin, ticarcillin

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Penicillins that have compelmetary actions with aminoglycosides

Piperacillin, ticarcillin

These are susceptible to penicillinases, used with tazobactam to limit resistance

Piperacillin, ticarcillin

Piperacillin, ticarcillin are susceptible to penicillinases, used with _________ to limit resistance

tazobactam

First generation cephalosporins

Cefalozin, cephalexin

Used in surgical infections

First generation cephalosporins (Cefalozin, cephalexin)

Minimal effectiveness against gram-negative bacteria

First generation cephalosporins (Cefalozin, cephalexin)

Second generation cephalosporins

Cefotetan, cefoxitina, cefamandole, cefuroxime, cefactor

More active against gram-negative

Second generation cephalosporins (Cefotetan, cefoxitina, cefamandole, cefuroxime, cefactor)

Will also work against Haemophilus influenzae

Second generation cephalosporins (Cefotetan, cefoxitina, cefamandole, cefuroxime, cefactor)

Third generation cephalosporins

Ceftazidime, cefoperazone, cefotaxime, ceftriaxone

Even more active against gram-negative

Third generation cephalosporins (Ceftazidime, cefoperazone, cefotaxime, ceftriaxone)

Will often work against organisms that are resistant to penicillin

Third generation cephalosporins (Ceftazidime, cefoperazone, cefotaxime, ceftriaxone)

We only use these drugs in serious infections

Third generation cephalosporins (Ceftazidime, cefoperazone, cefotaxime, ceftriaxone)

Fourth generation cephalosporins

Cefepime,

More resistant to B-lactamases

Fourth generation cephalosporins (Cefepime, ceftaroline)

Eneterobacter, Haemophilus, Neisseria

has activity in infections caused by methicillin resistant staphylococci

Ceftaroline

less likely to cause rashes and allergic reactions than penicillins

Cephalosporins

Anti-infectives

Ceftaroline, ceftobiprole Ceftaroline Ceftobiprole

Community acquired pneumonia

Ceftaroline

Skin/soft tissue infections, inlucidng MRSA

Ceftaroline

Hospital acquired pneumonia

Ceftobiprole

Resistant to B-lactamases

Aztreonam

No activity against gtam-positive drugs

Aztreonam

Binds to penicillin-binding protein 3 (PBP3)

Aztreonam

Half-life is prolonged in renal failure

Aztreonam

Aztreonam ADE

GI upset Vertigo, headache No cross allergy with penicillins

Broad-spectrum activity against gram positives, gram negatives, anaerobes, and Pseudomonas.

Carbapenems

Carbapenems that are chemically unique, but still containing a B-lactam ring

Imipenem, doripenem, meropenem

Low susceptibility to penicillinases

Imipenem, doripenem, meropenem

Very susceptible to renal dehydropeptidases

Imipenem, doripenem, meropenem

Imipenem, doripenem, meropenem are very susceptible to renal dehydropeptidases, thus Administered with ______________

silastatin

Imipenem, doripenem, meropenem are wide ranging activity against:

gram -positive cocci Gram-negative rods Anaerobes Pseudomonas and acinetobacter species

Used for severe infections, especially against resistant strains.

Vancomycin

Binds to a bacterial glycoprotein, causing "red man syndrome" (histamine release-induced severe cutaneous flushing).

Vancomycin

histamine release-induced severe cutaneous flushing

Red man syndrome

Bactericidal glycoprotein that binds to the alanine terminal of the peptidoglycan

Vancomycin

Resistant organisms have an altered terminal - decreased affinity for vancomycin

Vancomycin

Used for serious infections only

Vancomycin

Vancomycin does not cross the blood brain barrier - used ____________

intrathecally

Used orally for luminal infections of the gut

Vancomycin

Toxicity of Vancomycin

Red man syndrome Phlebitis, otototxicity, nephrotoxicity

Topical treatment and decontamination for Staphylococcus colonization.

Bacitracin

Bacitracin is used in caution due to potential __________.

nephrotoxicity

Used in topical treatment and decontamination syndromes

Bacitracin

Used in staphylococcus colonization of the skin

Bacitracin

Marked nephrotoxicity - not used parenterally

Bacitracin

Cyclic lipopeptide for vancomycin-resistant strains.

Daptomycin

Requires close monitoring of creatinine kinase levels due to potential muscle disease.

Daptomycin

Cyclic lipopeptide

Daptomycin

For the treatment of VRE and VRSA

Daptomycin

During treatment of Daptomycin, creatinine kinase during treatment must be monitored because it is _____________

myopathic