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Pharmacology (Topic C) > 8. Penicillins > Flashcards

8. Penicillins Flashcards

1
Q

List the Basic Penicillins.

A
  1. Penicillin G: given IV
  2. Penicillin V: oral
  3. Penamecillin: prodrug, metabolized into benzylpenicillin.
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2
Q

List the Staphylococcus B-Lactamase Resistant Penicillins (Anti-Staphylococci).

A
  1. Oxacillin
  2. Nafcillin
  3. Methicillin
  4. Cloxacillin
  5. Dicloxacillin
  6. Flucloxacillin
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3
Q

List the amino-penicillin ESP (Extended Spectrum Penicillins).

A
  1. Ampicillin
  2. Amoxicillin
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4
Q

List the ureidopenicillin ESP (Extended Spectrum Penicillins)/ (Anti-pseudomonal).

A
  1. Piperacillin
  2. Ticarcillin
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5
Q

What are the side effects of Penicillin therapy?

A

Penicillins are generally non-toxic and can be used in pregnancy.

  1. Allergy: T1 HS rxn; may be cross-reactive with cephalosporins
  2. Epileptic seizures: (↓ BBB pen → only at high serum levels, as in ↓ kidney function)
  3. Hematological reactions: drug-induced AI hemolytic anemia (via anti-penicillin IgG binding RBC surfaces)
  4. Morbilliform rash - sometimes occurs if given during viral infection (EBV, etc.)
  5. (Interstitial nephritis - mononuclear infiltrate)
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6
Q

What are the indications of basic penicillins?

A
  1. Gram + cocci: used to be good for staph, now 99% staph are resistant; still good against Streptococci (esp. S. pyogenes)
  2. Good for Pasteurella multocida (pet bites), Actinomyces (and other Gram + anaerobes in general, i.e. C. perfringens, oral strep, etc.); Leptospira; Borrelia; Treponema
  3. Syphilis; fever after cat/dog bite; upper respiratory infections (otitis, tonsillopharyngitis); soft tissue infections (Staph/Strep)
  4. Gram - cocci: good for Neisseria only (most meningococci, some gonococci)
  5. NOT effective for: Enterococci, Gram - rods (H. flu, E. coli, salmonella), Gram - anaerobes (B. fragilis, etc.)
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7
Q

How are the kinetic parameters of penicillins?

A
  1. Penetrate CNS, eye + prostate only in inflammation (compromised barrier)
  2. Does not enter abscesses
  3. Cross placenta + enter breast milk
  4. Excreted via kidney unchanged
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8
Q

What is the route of administration for penicillin G?

A

Penicillin G - gastric acid unstable → IV only

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9
Q

List the cell wall synthesis inhibitors.

A
  1. B-lactams (penicillins, cephalosporins, carbapenems, monobactams)
  2. Glycopeptides
  3. Others
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10
Q

What spectrum does Extended-Spectrum Penicillins cover?

A

Spectrum: similar spectrum to basic penicillins (Staph, Strep), plus activity against…

  1. Gram - rods - E. coli, Shigella, Salmonella etc. causing GI infections, UTIs, etc.Gram - rods often produce beta-lactamases, so ESPs are often combined with beta-lactamase inhibitors (Topic C-10) in these cases. B-Lase inhibitors have 100x ↑ affinity for B-Lase than the abx themselves and thus competitively inhibit it
  2. Gram - anaerobes (B. fragilis, often multi-resistant + causes abdominal infections: peritonitis, etc.)
  3. Enterococci (about 50%, many are multi-resistant); Listeria and some lower respiratory tract infections; Borrelia in early stages
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11
Q

What are the indications for Staph B-Lactamase Resistant Penicillins/ Anti-staphylococci penicillins?

A

They have larger R groups that inhibit B-lactamase binding so are generally good against Staph (except MRSA), but weaker against Strep than basic penicillins.

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12
Q

What are the indications for penicillin G?

A
  1. Rheumatic fever
  2. mitral endocarditis (S. viridans/bovis)
  3. intrapartum group B strep prophylaxis (agalactiae)
  4. IM form for syphilis (primary, secondary or early latent)
  5. Neisseria meningitis
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13
Q

What is the route of administration of Penicillin V?

A

Penicillin V - acid stable → oral admin.

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14
Q

What is Penamecillin?

A

Penamecilline is prodrug metabolized by esterases into benzylpenicillin.

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15
Q

What are the indications for Penicillin V?

A

DOC for group A strep (strep throat, rheumatic fever)

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16
Q

What are the kinetic parameters like for Penicillin V?

A
  1. Poor bioavailability
  2. 4x/day dosing
  3. Narrow spectrum
17
Q

What is the route of administration of Oxacillin?

A

Oxacillin has good oral absorption and it is often combined with aminoglycoside (gentamicin) in severe, life threatening infections (osteomyelitis, endocarditis, etc.)

18
Q

What is the route of administration of Nafcillin?

A

Nafcillin is only parenterally administered.

19
Q

What are the indications for Methicillin?

A

Methicillin is no longer used because of nephrotoxic side effects and is therefore only used for diagnostics.

20
Q

What are the indications of anti-staphylococci penicillins?

A
  1. Oral admin: mild or moderate localized skin / soft tissue infections (folliculitis, impetigo, abscesses) by methicillin-sensitive Staph.
  2. IV admin: severe systemic Staph infections such as tricuspid endocarditis or osteomyelitis.
21
Q

What is the resistance mechanism behind the anti-staphylococci penicillins?

A

Resistance occurs when Staph have altered PBPs + thus ↓ beta-lactam binding.

22
Q

What are the side effects of aminopenicillins?

A
  1. Aminopenicillins can cause dysbacteriosis due to effect on GI bacteria (potentially pseudomembranous C. difficile colitis)
  2. (rash, or in serious cases Stevens-Johnson syndrome)
  3. often combined with aminoglycoside (ampicillin + gentamicin) for severe cases
23
Q

What is the route of administration of Ampicillin?

A

Ampicillin is parenteral admin; often w/ sulbactam B-Lase inhibitor.

24
Q

What are the indications for Piperacillin?

A

Piperacillin is good for P. aeruginosa and resistant nosocomial infections.

25
Q

What is the MOA of Beta-Lactams?

A
  1. Beta Lactams all inhibit peptidoglycan synthesis by transpeptidase rxn inhibition.
  2. They bind to PBPs which are the transpeptidase enzymes themselves → bactericidal effect.
  3. Generally ineffective against intracellular bacteria.
  4. Generally low toxicity and ok in pregnancy.
26
Q

What is the resistance mechanism behind Beta-Lactams?

A
  1. Beta Lactamases - break down the abx molecules (penicillin > cephalosporins > carbapenems > monobactams). Extended Spectrum B-Lactamases - more effective + even break down carbapenems
  2. Altered PBPs - conveys resistance against all B-lactam abx via ↓ binding. ex: MRSA - resists all the staph B-lactamase-resistant penicillins
  3. Permeability Decrease - reduced or absent pores in cell (ex: Gram negatives)
  4. Efflux Pump - less common
27
Q

What are the indications of Ticarcillin?

A

Ticarcillin is a carboxypenicillin, also good for P. aeruginosa, with clavulanate.

28
Q

Which are the broadest spectrum penicillins?

A

Ureidopenicillins are the broadest spectrum penicillins.

29
Q

What are the pharmacokinetic paramters of Piperacillin?

A
  1. Parenteral admin only
  2. Often combined with gentamicin or tobramycin
  3. Also often w/ tazobactam B-Lase inhibitor
30
Q

What are the indications of ampicillin?

A
  1. severe anaerobic infections (aspiration pneumonia, Enterococcus, Listeria meningitis)
  2. accumulates in gallbladder → can be good for cholecystitis
31
Q

What is the route of administration of Amoxicillin?

A

Amoxicillin is orally administrated, often w/ clavulanic acid, a B-Lase inhibitor.

32
Q

What are the indications of Amoxicillin?

A
  1. common for Strep pharyngitis
  2. sinusitis, otitis media and pneumonia by Strep, H. flu, etc.
  3. dental surgery prophylaxis - against oral anaerobes in pts with endocarditis risk
  4. (part of H. pylori triple therapy; also for Borrelia)
  5. (prophylaxis against encapsulated microbes in asplenia )
33
Q

What are the side effects of Amoxicillin?

A
  1. Hepatotoxicity (common with amox + clav).
  2. common cause of morbilliform rash when given during EBV.

Pharmacology (Topic C) (20 decks)

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