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Step 1 Pharm > Antimicrobials > Flashcards

Antimicrobials Flashcards

1
Q

What is the mechanism of action of penicillin?

A

Bind penicillin-binding proteins (transpeptidases). Block transpeptidase cross-linking of peptidoglycan in cell wall. Activate autolytic enzymes.

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2
Q

What are the clinical uses of penicillin?

A

Mostly used for gram positive organisms (*S. pneumoniae, S. pyogenes, Actinomyces). *

Also used for gram-negative cocci (N. meningitidis) and spirochetes (*T. pallidum). *

Bactericidal for gram-positive cocci, gram positive rods, gram-negative rods, gram-negative cocci and spirochetes.

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3
Q

Name two toxicities of **penicillin. **

A

Hemolytic anemia

Hypersensitivity reactions

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4
Q

What is the mechanism of penicillin resistance?

A

Penicillinase in bacteria (a type of ß-lactamase) cleaves ß-lactam ring.

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5
Q

Name two penicillinase-sensitive penicillins (aminopenicillins).

A

Ampicillin

Amoxicillin

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6
Q

What is the mechanism of action of the aminopenicillins (amoxicillin, ampicillin)?

A

Bind penicillin-binding proteins (transpeptidases). Block transpeptidase cross-linking of peptidoglycan in cell wall. Activate autolytic enzymes.

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7
Q

What are the clinical uses of the aminopenicillins (amoxicillin, ampicillin)?

A

Extended spectrum penicillins: H. influenzae, H. pylori, E. coli, Listeria monocytogenes, Proteus mirabilis, Salmonella, Shigella, **enterococci. **

HHELPSS kill **enterococci. **

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8
Q

Give three toxicities of aminopenicillins.

A

Hypersensitivity reactions, rash, pseudomembranous colitis.

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9
Q

What is the mechanism of resistance for the aminopenicillins?

A

Penicillinase in bacteria (a type of ß-lactamase) cleaves ß-lactam ring.

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10
Q

Name 3 penicillinase-resistant penicillins.

A

Oxacillin

Nafcillin

Dicloxacillin

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11
Q

What is the mechanism of action of the penicillinase-resistant penicillins?

A

Bind penicillin-binding proteins (transpeptidases). Block transpeptidase cross-linking of peptidoglycan in cell wall. Activate autolytic enzymes.

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12
Q

What makes dicloxacillin, nafcillin, and oxacillin penicillinase-resistant?

A

These drugs have a bulky R group that blocks access of the ß-lactamase to the ß-lactam ring.

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13
Q

What is the clinical use of the penicillinase-resistant penicillins (dicloxacillin, nafcillin, oxacillin)?

A

S. aureus

(except MRSA–resistant because of altered penicillin-binding protein sight).

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14
Q

Give two toxicities of the penicillinase-resistant penicillins (dicloxacillin, nafcillin, oxacillin).

A

Hypersensitivity reactions and interstitial nephritis.

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15
Q

Name two antipseudomonals.

A

Ticarcillin

Piperacillin

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16
Q

What is the mechanism of action of the antipseudomonals (piperacillin, ticarcillin)?

A

Bind penicillin-binding proteins (transpeptidases). Block transpeptidase cross-linking of peptidoglycan in cell wall. Activate autolytic enzymes.

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17
Q

What are the clinical uses of piperacillin and ticarcillin?

A

**Pseudomonas **species and gram-natative rods. (Susceptible to penicillinase–use with ß-lactamase inhibitors).

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18
Q

Name a toxicity of the antipseudomonals (piperacillin, ticarcillin).

A

Hypersensitivity reactions

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19
Q

Name three ß-lactamase inhibitors.

A

Clavulonic Acid

Sulbactam

Tazobactam

20
Q

What is the clinical use of clavulonic acid, sulbactam and tazobactam?

A

Added to penicillin antibiotics to protect the antibiotic from destruction by ß-lactamase (penicillinase).

21
Q

Which drug can we combine with amoxicillin and ampicillin to protect against destruction by ß-lactamase?

A

Claculanic acid

22
Q

What drug is the prototype ß-lactam antibiotic?

A

Penicillin

23
Q
A
24
Q

What is the mechanism of action of the cephalosporins?

A

These are bactericidal ß-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases.

25
Q

Which organisms are generally not covered by the cephalosporins?

A

LAME: **Listeria, *Atypicals (Chlamydia, Mycoplasma*), MRSA and Enterococci.

[Exception: ceftaroline covers MRSA]

26
Q

Name two first generation cephalosporins.

A

Cephalexin

Cefazolin

27
Q

What are the clinical uses of the first generation cephalosporins?

A

Gram-positive cocci: Proteus mirabilis, E. coli, Klebsiella pneumoniae

[PEcK]

28
Q

Which cephalosporin is used prior to surgery to prevent S. aureus wound infections?

A

Cefazolin

29
Q

Name three second generation cephalosporins.

A

Cefaclor

Cefuroxime

Cefoxitin

30
Q

What are the clinical uses of the second generation cephalosporins?

A

Gram positive cocci: Haemophilus influenzae, Enterobacter aerogenes, Neisseria spp., Proteus mirabilis, E. coli, Klebsiella pneumoniae, Serratia marcescens.

[HEN PEcKS]

31
Q

Name three 3rd generation cephalosporins.

A

Ceftriaxone

Cefotaxime

Ceftazidime

32
Q

What are the clinical uses of the third generation cephalosprins?

A

Serious gram-negative infections resistant to other beta-lactams.

Ceftriaxone: meningitis, gonorrhea, disseminated Lyme disease

Ceftazidime: Pseudomonas

33
Q

Name one fourth generation cephalosporin.

A

Cefepine

34
Q

What are the clinical uses of cefepime?

A

Gram negative organisms, with increased activity against Pseudomonas and gram-positive organisms.

35
Q

Name a 5th generation cephalosporin.

A

Ceftaroline

36
Q

What are the clinical uses of ceftaroline?

A

Broad gram-positive and gram-negative organism coverage, including MRSA.

[Exception: does not cover Pseudomonas]

37
Q

Cephalosporin toxicities (4)

A

Hypersensitivity reactions, autoimmune hemolytic anemia, disulfram like reaction, vitamin K deficiency.

38
Q

Name two drug-drug interactions seen with cephalosporins.

A

Exhibit cross-reactivity with penicillins and increase nephrotoxicity of aminoglycosides.

39
Q

What is the mechanism of resistance to cephalosporins?

A

Structural change in penicillin-binding proteins.

40
Q

Name four carbapenems.

A

Imipenem, meropenem, ertapenem, doripenem.

41
Q

What is the mechanism of action of imipenem?

A

Broad specturm, ß-lactamase-resistant carbapenem.

42
Q

Which drug is always administered with imipenem, and why?

A

Given with cilastatin (inhibitor of renal dehydropeptidase I) to decrease inactivation of the drug in the renal tubules.

43
Q

What are the clinical uses of the carbapenems?

A

Gram positive cocci, gram-negative rods and anaerobes.

[Wide spectrum but many side effects–limit use to life-threatening infections/after other drugs fail]

44
Q

Carbapenem toxicities?

A

GI distress, skin rash, and CNS toxicity (seizures) at high plasma levels.

45
Q

Which carbapenem has a lower risk of seizures and is stable to dehydropeptidase I?

A

Meropenem

46
Q

Name a monobactam antibiotic.

A

Aztreonam

47
Q
A

Step 1 Pharm (2 decks)

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