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
Q

What can forth generation cephalosporins be used to treat?

A

Spectum is similar to gen 3 but also includes Pseudomonas aeruginosa. It is often used to treat lyme disease

26
Q

What is the 5th generation cephalosporin and what is it used to treat?

A

ceftaroline (IV) it is reserved for treating MRSA

27
Q

What are the two main ADRs for cephalosporins?

A

1) patients with severe allergic reactions to penicillins should not be given cephalosporins.
2) Some cephalosporins (cefotetan) have anti-vitamin K effects

28
Q

What is the monobactam and what is it used to treat?

A

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
Q

What is the main Carbapenem, what is it used to treat?

A

Imipenem/cilastatin is a broad spectrum agent

30
Q

Why is Imipenem co administered with cilastatin?

A

imipenem is hydrolyzed to a toxic metabolite by a renal dipeptidase. Cilastatin inhibits renal dipeptidase

31
Q

What are the two main Glycopeptide Antibacterials?

A

Vancomycin and Teicoplanin

32
Q

What are glycopeptides used to treat?

A

primary use in staph/strep infection in patients with penicillin/cephalosporin hypersensitivities. They are only effective against gram positive bacteria.

33
Q

What is the MOA of glycopeptides?

A

They bind the little peptide chains on glycan strands. This prevents transpeptidase from binding and crosslinking

34
Q

What are the 3 main ADRs of glycopeptides?

A

1) Adverse reactions from parenteral administraion
2) Ototoxicity (particularly when given with aminoglycosides)
3) Red man syndrome (due to large histamin release)