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Pharm I: Exam 3 > Cell Wall Inhibitors (Antibiotic I) > Flashcards

Cell Wall Inhibitors (Antibiotic I) Flashcards

1
Q

What are the major ABX that function via inhibition of cell wall synthesis?

A
  • Beta-lactams (Penicillins and Cephalosporins)
  • Vancomycin
  • Daptomycin
  • Bacitracin
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2
Q

How do Penicillins function with respect to bacteria?

A

Bactericidal (Works best in rapidly proliferating organisms WITH cell wall)

Bind to Penicillin-Binding Proteins (PBPs) and inhibit transpeptidase (cross-linking of peptidoglycans → osmotically unstable membrane will rupture)

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3
Q

What are the three mechanisms of resistance in Penicillins?

A
  1. Inactivation by beta-lactamases (most common)
  2. Modification of PBP target
  3. Impaired penetration of drug to target PBP
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4
Q

What are the different sub-classifications of Penicillins?

A
  • Natural Penicillins
  • Aminopenicillins
  • Penicillinase-Resistant Penicillins
  • Antipseudonomal Penicillins
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5
Q

What are beta-lactamase inhibitors?

A

Considered “suicide inhibitors” → potent, irreversible inhibitors of most lactamase (extends the spectrum of ABX)

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6
Q

What ABX are considered Natural Penicillins? How is each PCN administered (if applicable)? [2]

A
  • Penicillin V (PO)
  • Penicillin G (IV, IM, Depot)
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7
Q

What ABX are considered Aminopenicillins? How is each PCN administered (if applicable)? [2]

A
  • Amoxicillin (PO)
  • Ampicillin (PO, IV)
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8
Q

What ABX are considered Penicillinase-Resistant Penicillins? How is each PCN administered (if applicable)? [5]

A
  • Nafcillin (PO, IV)
  • Oxacillin
  • Dicloxacillin
  • Methicillin (No longer available in the US)
  • Cloxacillin (No longer available in the US)
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9
Q

What ABX are considered Antipseudomonal Penicillins?How is each PCN administered (if applicable)? [3]

A
  • Piperacillin (IV)
  • Ticarcillin (IV)
  • Carbenicillin (IV)
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10
Q

What ABX are considered Beta-lactamase inhibitors? What PCN are each inhibitor used with (if applicable)? [3]

A
  • Clavulanic acid (Adjunct TX: Amoxicillin, Ticarcillin)
  • Sulbactam (Adjunct TX: Ampicillin)
  • Tazobactam (Adjunct TX: Piperacillin)
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11
Q

What are MOAs and General Target of Natural Penicillins?

A
  • Narrow spectrum
  • Acid labile (PCN-G)
  • Penicillinase sensitive
  • Gram-positive cocci (Does not include Staphylococcus)
  • Obligate anaerobes
  • Some gram-negative (E. coli, H. influenzae, N. gonorrhoeae, Trepnema pallidium and suseptible Pseudomona spp.)
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12
Q

What are Natural Penicillins used to TX/Prophylaxis?

A
  • Upper/Lower Respiratory Tract Infections
  • Throat infection
  • Skin infection
  • GU tract infection
  • PROPHYLAXIS Rheumatic fever, dental procedure (for those at risk of endocarditis, gonorrhoeae, syphilis exposure)
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13
Q

What are MOAs and Specific Target/Bacteria of Aminopenicillins?

A

PCN-G MOA + improved coverage of gram-negative cocci and Enterobacteriaceae

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14
Q

What are Aminopenicillins used to TX/Prophylaxis?

A
  • URI (sinusitis, otitis)
  • UTI (uncomplicated)
  • Meningitis
  • Salmonella infections (Not 1ST LINE)

No mentioned prophylactic measures

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15
Q

What are the MOAs and General Targets of Penicillinase-Resistant Penicillins?

A
  • Also called “Antistaphylococcal Penicillins”
  • Penicillinase resistant, narrow spectrum
  • General Target: staphylococcal infections with high beta-lactamase production
    • Not active against gram-negative or anaerobes
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16
Q

What is the name for Staphylococci spp. that are resistant to penicillinase-resistant penicillins?

A

MRSA (Methicillin Resistant Staphylococcus aureus)

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17
Q

What are Penicillinase-resistant penicillins used to TX/prophylaxis?

A
  • Cellulitis
  • Endocarditis
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18
Q

What are MOAs and Specific Target/Bacteria of Antipseudomonal penicillins?

A
  • PCN-G MOA + greater gram negative coverage (including Pseudomonas spp.)
  • Coverage: H. influenzae, Klebsiella sp.
  • No coverage: Treponema palladium, Actinomyces spp.
19
Q

What are the PK characteristics (Absorption, Distribution, Elimination) of Penicillins?

A

Absorption: Poor oral administration (food DEC absorption), IV preferred

Distribution: Widely distributed, poorly penetrate the eye, CNS (only when meninges are inflamed) and prostate

Elimination: Kidney unchanged (Antipseudomonal and naficillin→billary excretion)

20
Q

How does Probenecid interact with penicillins?

A

Prevents active secretion of Penicillin into urine

21
Q

What are important ADRs of Penicillins?

A
  • Hypersensitivity reaction (could lead to analphylasis, Serum sickness interstitual nephritis, hemolytic anemia)
  • GI effects (related to oral agents)
  • Diarrhea
  • Vaginal candidiasis (2ndary)
22
Q

What are some important Drug interactions of Penicillins?

A

Bacteriostatic agents (i.e. tetracycline, aminoglycosides): DO NOT give concurrently

Warfarin: metabolism affected by anti-pseudomonal PCN

23
Q

What are Cephalosporins?

A
  • Class of Beta-lactam drugs, chemically similar to PCN with respect to MOA and toxicity
    • possess dihydrothiazine ring → INC resistant to beta lactamases
  • Bactericidal
  • Classified in 5 generations
24
Q

What ABX are considered 1st Generation Cephalosporins? How are the ABX administered (if applicable)? [3]

A
  • Cefazolin (IV)
  • Cephalexin (PO)
  • Cefadroxil (PO)

Only class that has “ph” instead of “f” in name

25
Q

What ABX are considered 2nd Generation Cephalosporins? What added coverages does each ABX have (Gram-negative vs. Anaerobic)? How are the ABX administered (if applicable)?

A
  • Added Gram-negative coverage
    • Cefuroxime (IV, PO)
    • Cefaclor (IV, PO)
    • Cefporzil (IV, PO)
  • Added anaerobic coverage
    • Cefotetan (IV)
    • Cefoxitin (IV)
26
Q

What are ABX are considered 3rd Generation Cephalosporins? How are ABX administered (if applicable)? [8]

A
  • Cefpodoxime (PO)
  • Cefdinir (PO)
  • Cefixime (PO)
  • Cefditoren (PO)
  • Cefibuten (PO)
  • Cefotaxime (IV, IM)
  • Ceftriaxone (IV, IM)
  • Ceftazidime (IV)
27
Q

What are ABX are considered 4th Generation Cephalosporin? How are the ABX administered (if applicable)? [1]

A
  • Cefepime (IV, IM)
28
Q

What are ABX are considered 5th Generation Cephalosporins? How are ABX administered (if applicable)? [2]

A
  • Ceftaroline fosamil (IV)
  • Ceftolozane (IV)
29
Q

What are the three mechanisms of resistance with Cephalosporins?

A
  • Mutation in PBP
  • Production of Beta-lactamases
  • Alteration in cell-membrane porins in gram-negative organ
30
Q

What are the MOAs and General Target/Bacterias of 1st Generation Cephalosporins?

A

Similiar MOA to Penicillinase-Resistant (Anti-staph) PCN and Aminopenicillins

General Target:

  • Aerobic Gram-positive
  • Above diaphragm anaerobes
  • Community acquired Gram-negative
31
Q

What are 1st Generation Cephalosporins used to TX/Prophylaxis?

A

GRAM-POSITIVE (patients who can’t take PCN)

  • Septic arthritis (adults)
  • Skin infections
  • Acute otitis media
  • Pharyngitis
  • PROPHYLAXIS: Clean surgeries, UTI
32
Q

How does 2nd Generation Cephalosporin compare to 1st Generation coverage?

A

Somewhat less Gram-positive coverage than 1st Gen, but significantly greater Gram-negative coverage

33
Q

What is significant about the spectrum of 3rd Generation Cephalosporins?

A
  • Expanded Gram-negative coverage
  • Penetration of BBB
34
Q

What are extra-defining features Ceftriaxone, Cefotaxime, Ceftazidime? (3rd generation Cephalosporins)

A

Long Half-Life

  • Ceftriaxone (IV, IM)
  • Cefotaxime (IV, IM)

INC Anti-pseudomonal coverage

  • Ceftazidime (IV)
35
Q

What are 3rd Generation Cephalosporins used to TX/Prophylaxis?

A

1st LINE TX:

  • Meningitis
  • Pneumonia (Children and Adults)
  • Sepsis
  • Peritonitis

Additional TX:

  • UTI
  • Skin infections
  • Osteomyelitis
  • Neisseria gonorrheae
36
Q

What are MOAs and General Target/Bacterias of 4th Generation Cephalosporins?

A

Good activity against all gram bacteria including anaerobic coverage (P. aerugnosa, H. influenzae**, N. Meningitidis, N. gonorrheae; Enterobacteriaceae resistant to other Cephalosporins)

37
Q

What are 4th Generation Cephalosporins used to TX/Prophylaxis?

A
  • Intra-abdominal infections
  • Respiratory tract infections
  • Skin infections
38
Q

What is important to know pertaining to 5th generation cephalosporins?

A
  • Activity against MRSA
  • TX complicated skin and intra-abdominal infections including CAP
  • Expensive (rarely used)
39
Q

What are the PK characteristics (Absorption, Distribution, Elimination) of Cephalosporins?

A

Absorption: PO rapidly absorbed, variable effects with food

Distribution: Extensive (2nd, 3rd, 4th Gen can cross BBB; think long half-life for 3rd Gen)

Elimination: Kidneys (most)

40
Q

What are General ADRs/Drug interactions associated with Cephalosporins?

A

Hypersensitivity: Similar to PCN, allergic reaction (rare; S/Sx rash, fever, eosinophilia, hives)

Superinfection: Resistant organisms/fungi may proliferate

GI effects: N/V/D (well tolerated)

Blood Dyscrasias (will resolve w/ DC drug): Eosinophilia, Thrombocytopenia, Leukopenia

DRUG INTERACTION:

  • Probenecid (INC serum levels of co-administered Cephalosporin)
  • Warfarin (INC effects; Cefotetan, Cefazolin, Cefoxitin, Ceftriaxone)
41
Q

What specific ADRs are associated with Ceftriaxone? (3rd Generation Cephalosporin)

A
  • Cholestasis
  • DRUG INTERACTION: INC effects of Warfarin
42
Q

What specific ADRs are associated with Cefotetan? (2nd Generation Cephalosporin, added anaerobic coverage)

A

Methylthiotetrazole side chains induce disulfiram-like reaction with EtOH ingestion

43
Q

What are Monobactams?

A

Pharm I: Exam 3 (10 decks)

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