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

Cell Wall Inhibitors (Antibiotic I) Flashcards

(43 cards)

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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?

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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?

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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?

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A

Prevents active secretion of Penicillin into urine

21
Q

What are important ADRs of Penicillins?

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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?

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A

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

Warfarin: metabolism affected by anti-pseudomonal PCN

23
Q

What are Cephalosporins?

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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]

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

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

25
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)?
* Added *Gram-negative coverage* * Cefuroxime (**IV, PO**) * Cefaclor (**IV, PO**) * Cefporzil (**IV, PO**) * Added *anaerobic coverage* * Cefotetan (**IV**) * Cefoxitin (**IV**)
26
What are **ABX** are considered **3rd Generation Cephalosporins**? How are ABX **administered** (if applicable)? [8]
* Cefpodoxime (**PO**) * Cefdinir (**PO**) * Cefixime (**PO**) * Cefditoren (**PO**) * Cefibuten (**PO**) * Cefotaxime (**IV, IM**) * Ceftriaxone (**IV, IM**) * Ceftazidime (**IV**)
27
What are **ABX** are considered **4th Generation** Cephalosporin? How are the ABX **administered** (if applicable)? [1]
* Cefepime (**IV, IM**)
28
What are **ABX** are considered **5th Generation** Cephalosporins? How are ABX **administered** (if applicable)? [2]
* Ceftaroline fosamil (**IV**) * Ceftolozane (**IV**)
29
What are the three mechanisms of **resistance** with **Cephalosporins**?
* Mutation in PBP * Production of Beta-lactamases * Alteration in cell-membrane porins in gram-negative organ
30
What are the **MOAs** and **General Target/Bacterias** of **1st Generation Cephalosporins**?
Similiar MOA to Penicillinase-Resistant (Anti-staph) PCN and Aminopenicillins General Target: * Aerobic Gram-positive * Above diaphragm anaerobes * Community acquired Gram-negative
31
What are **1st Generation Cephalosporins** used to **TX/Prophylaxis**?
GRAM-POSITIVE (patients who can't take PCN) * Septic arthritis (adults) * Skin infections * Acute otitis media * Pharyngitis * **PROPHYLAXIS**: Clean surgeries, UTI
32
How does **2nd Generation** **Cephalosporin** compare to **1st Generation** coverage?
**Somewhat** **_less_ Gram-positive coverage** than 1st Gen, but **significantly _greater_ Gram-negative coverage**
33
What is significant about the spectrum of **3rd Generation Cephalosporins**?
* Expanded Gram-negative coverage * Penetration of BBB
34
What are extra-defining features **Ceftriaxone, Cefotaxime, Ceftazidime**? (3rd generation Cephalosporins)
**Long Half-Life** * Ceftriaxone (**IV, IM**) * Cefotaxime (**IV, IM**) **INC Anti-pseudomonal coverage** * Ceftazidime (**IV**)
35
What are **3rd Generation Cephalosporins** used to **TX/Prophylaxis**?
**1st LINE TX:** * Meningitis * Pneumonia (Children and Adults) * Sepsis * Peritonitis Additional TX: * UTI * Skin infections * Osteomyelitis * *Neisseria* *gonorrheae*
36
What are **MOAs** and **General** **Target/Bacterias** of **4th Generation Cephalosporins**?
Good activity against **all gram bacteria** including **anaerobic coverage** (*P. aerugnosa, H.* *influenzae**, N. Meningitidis, N.* *gonorrheae; Enterobacteriaceae* resistant to other Cephalosporins)
37
What are **4th Generation Cephalosporins** used to **TX/Prophylaxis**?
* Intra-abdominal infections * Respiratory tract infections * Skin infections
38
What is important to know pertaining to **5th generation cephalosporins**?
* **Activity against MRSA** * **TX** complicated skin and intra-abdominal infections including CAP * Expensive (rarely used)
39
What are the **PK** characteristics (Absorption, Distribution, Elimination) of **Cephalosporins**?
**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
What are **General ADRs/Drug interactions** associated with **Cephalosporins**?
**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
What **specific** **ADRs** are associated with **Ceftriaxone**? (3rd Generation Cephalosporin)
* Cholestasis * **DRUG INTERACTION**: INC effects of Warfarin
42
What **specific ADRs** are associated with **Cefotetan**? (2nd Generation Cephalosporin, added anaerobic coverage)
Methylthiotetrazole side chains induce **disulfiram-like reaction** with **EtOH ingestion**
43
What are **Monobactams**?

Pharm I: Exam 3 (10 decks)

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