BIIC Pharmacology Lecture 3_Antimicrobials 1 antibacterials Flashcards

1
Q

What are the two bacterial enzymes associated with cell wall synthesis?

A

Transpeptidase and autolysin

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2
Q

What are three ways bacteria develop resistance to antibacterial medications?

A

1) Alteration of medications binding target (example PBPs)
2) Expression of efflux pumps
3) Degrading enzymes (example Beta Lactamase)

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3
Q

What are the common beta lactamase inhibitors?

A

Clavulanic Acid, sulbactam, tazobactam, avibactam

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4
Q

How are beta lactamase inhibitors used clinically?

A

They are coadministered with beta latam antibacterials to improve efficacy

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5
Q

What are the 4 main sub catagories of Penicillins?

A

1) Natural penicillins (penicillin G, penicillin V)
2) Anti-staphylococcal penicillins (oxacillin, dicloxacillin, nafcillin, methicillin)
3) Aminopenicillins (ampicillin, amoxicillin)
4) Antipseudomonal penicillins (piperacillin, ticarcillin)

NOTE: Both 3 and 4 are extended spectrum penicillins

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6
Q

What 5 things can natural penicillin often treat?

A

1) Pneumococcal infections (Streptococcus pneumoniae):
2) Gonorrhea (Neisseria sp.)
3) Gas gangrene (Clostridium perfringens)
4) Syphilis (Treponema pallidum)
5) Pharyngitis (ß-hemolytic streptococcus)

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7
Q

What are the two important Natural penicillins and how are they administered?

A
Penicillin G (IV or IM)
Penicillin V (oral)

NOTE: Penicillin G is stabilized by benathine for IM repository injections. Also, penicillin is renally eliminated and has a short half life)

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8
Q

What are the 5 typical ADRs for Penicillin?

A

1) Hypersensitivity
2) Diarrhea (because of disruption to gut flora)
3) Acute Nephritis
4) Contraindicated in epilepsy
5) Decreased coagulation and cytopenia with prolonged use

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9
Q

What are the three main Anti-staphylococcal (Penicillinase resistant) penicillins

A

1) Nafcillin (IV)
2) Oxacillin (IV)
3) Dicloxacillin (PO)

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10
Q

What are the three things Anti-staphylococcal (Penicillinase resistant) penicillins are used to treat?

A

MSSA, Penicillin-susceptible Streptococci, Pneumococci

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11
Q

How is nafcillin eliminated from the body?

A

Biliary excretion

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12
Q

What are the two main Aminopenicillins?

A

Ampicillin (IV) - coadminister sulbactam

Amoxicillin (PO) - coadminister clavulanate

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13
Q

What can aminopenicillins be used to treat?

A

Most gram positive bacteria and some gram negative

NOTE: Amoxicillin is the drug of choice for URI

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14
Q

What is the only antipseudomonal penicillin? What can it be used to treat?

A

Piperacillin (IV/IM) - coadminister tazobactam

Effective against many gram negative bacteria including Pseudomonas, Klebsiella pneumoniae

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15
Q

What are sephalosporins and what are they good for?

A
  1. Cephalosporins are ß-lactam drugs

2. Penicillinase resistant (not resistant to cephalosporinase)

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16
Q

What are the two main first generation cephalisporins?

A

Cefazolin (IV) - cant penitrate BBB

Cephalexin (PO)

17
Q

What can first generation cephalisporins be used to treat?

A
MSSA, streptococcal, and other penicillinase-producing
staphylococcal strains (not MRSA)
18
Q

What is the drug of choice for surgical prophylaxis and staph bacteremia?

A

Cefazoline

19
Q

What are the three main second generation cephalosporins?

A

Cefaclor (PO)
Cefuroxime (PO)
Cefoxitin (IV)

20
Q

What are second generation cephalosporins used to treat?

A

They have about the some coverage as first generation but with increased efficacy against gram negative bacteria.

21
Q

What are the three main thrid generation cephalosporins?

A

Cefotaxime (IV, IM)
Ceftazidime (IV, IM)
Ceftriaxone (IV, IM)

22
Q

What can thrid generation cephalosporins be used to treat?

A

Most drug resistant gram negative bacteria including Haemophilus and Neisseria Gonorrhoeae. Also third gen penitrates the BBB and can be used to treat menigitis

23
Q

How is Ceftriaxone eliminated from the body?

A

Biliary excretion

24
Q

What is the forth generation cephalosporin?

A

Cefepime (IV)

25
What can forth generation cephalosporins be used to treat?
Spectum is similar to gen 3 but also includes Pseudomonas aeruginosa. It is often used to treat lyme disease
26
What is the 5th generation cephalosporin and what is it used to treat?
ceftaroline (IV) it is reserved for treating MRSA
27
What are the two main ADRs for cephalosporins?
1) patients with severe allergic reactions to penicillins should not be given cephalosporins. 2) Some cephalosporins (cefotetan) have anti-vitamin K effects
28
What is the monobactam and what is it used to treat?
Aztreonam (IV or nebulized). It has no gram positive activity. It can treat most gram negative. Can treat menigitis as it penitrates the BBB. NOTE: Aztreonam is safe to be used in patients with penicillin allergies (except ceftazidime)
29
What is the main Carbapenem, what is it used to treat?
Imipenem/cilastatin is a broad spectrum agent
30
Why is Imipenem co administered with cilastatin?
imipenem is hydrolyzed to a toxic metabolite by a renal dipeptidase. Cilastatin inhibits renal dipeptidase
31
What are the two main Glycopeptide Antibacterials?
Vancomycin and Teicoplanin
32
What are glycopeptides used to treat?
primary use in staph/strep infection in patients with penicillin/cephalosporin hypersensitivities. They are only effective against gram positive bacteria.
33
What is the MOA of glycopeptides?
They bind the little peptide chains on glycan strands. This prevents transpeptidase from binding and crosslinking
34
What are the 3 main ADRs of glycopeptides?
1) Adverse reactions from parenteral administraion 2) Ototoxicity (particularly when given with aminoglycosides) 3) Red man syndrome (due to large histamin release)