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Year II Pharmacology Term 5 > The penicillins > Flashcards

The penicillins Flashcards

1
Q

Name 7 essential penicillins

A

Penacilin G
Aminopenicillins

Anti-staph penacillis (Nafcillin)

Anti-pseudomonal penicillins (piperacilin)

Penicillin combinations with beta lactamase inhibitors
- Amoxicillin/clavulate (Augmentin)
- Ampeicillin/sulbacteam (Ubasyn)
Pipracillin/tazobactam (zosyn)

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2
Q

Cell wall synethesuis dsrupters (7)

A 
Cycloserine
Vancomycin/teichoplanin
Bacitracin
Penicillins
Cephalosporins
Monobactams
Carbapenems
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3
Q

Where are beta lactamase inhibotors located

A

Periplasmic space

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4
Q

A ring

A

Penacilin made up of 2 rings

A ring: 4 carbons, carboxyl group & sulfer

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5
Q

B ring

A 
4 carbons in the ring
Amide bond (Amio group & carboxyl group)
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6
Q

Amide group in ring B can be destroyed by ring

A

Lactamase

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7
Q

Beside the amide bond name other location on penacllin molecule that can be disrupted

A

6th carbon amine group

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8
Q

Penacilin mechanism of action

A

Inhibit cell wall sythesis by disrupting mechanism of action of penicillin binding proteins

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9
Q

Beta lactam mechanism of action

A

analogs of the natural D-Ala-D-Ala substrate, and bind covalently to the PBP’s at the active site, thereby blocking the enzyme

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10
Q

Penicillin G Potassium Salt

Indications

Sensitive Bacteria

Resistant bacterial

Dosage

Interactions

SE/Toxicity

A

Indications

  • Step. phyrangitis
  • Skin infections
  • Pneumonia
  • Meningitis
  • Endocarditis
  • Dental infections
  • Rheumatic fever

Sensitive Bacteria

  • Strep
  • Enterococcus
  • Oral anerobes
  • Menigoccus
  • Syphilis

Resistant bacterial

  • Most staph
  • 30% pneumoccus
  • GN
  • Bowel anearobes

Dosage

  • IV or IM
  • Poor oral bioavability
  • Renal excretion

Interactions

  • Synergy: Gentamicin (cover staoh & enterocous)
  • Bad: Probenecid inhibits renal active tubulor secretion

SE/Toxicity
Allergy, anemia, & seizures with high dose

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11
Q

Ampicillin

Indications

Sensitive Bacteria

Resistant bacterial

Dosage

Interactions

SE/Toxicity

A

Indications

  • otis media
  • Neonatal sepsis
  • Lyme disease (rarely)
  • UTIs
  • Menegitis
  • URI
  • Endocarditis
  • H. infuenza

Sensitive Bacteria
- streptococci, enterococcus, oral anaerobes,Listeria, and some GNRs

Resistant bacterial
- most staph, some pneumococcus (>30%), some H. flu, bowel anaerobes

Dosage
- PO or oral (40% bioavalable)

Interactions
Syndergy: Gentamicin
Bad: Prpbenicid

SE/Toxicity
- Celluitis, allergu, seizures at high doses

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12
Q

Nafcillin

Indications

Mechanism

Sensitive Bacteria

Resistant bacterial

Dosage

Interactions

SE/Toxicity

A

Indications
- S. areus infection

Mechanism
- Binds PBPs

Sensitive Bacteria
- Staph aureus (MSSA), some species of pneumococcus and streptococci

Resistant bacterial
- Staph aureus (MRSA), some species of pneumococcus, oral and bowel anaerobes, most GNR

Dosage

  • IV only
  • Hepatic metabollis
  • Urine excretion

Interactions
Good: Gentamicin
Bad:: Probenecid & might inhibit methotrxate excretion

SE/Toxicity
- Allergy, antibiotic associated collitis

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13
Q

PIPERACILLIN

Indications

Mechanism

Sensitive Bacteria

Resistant bacterial

Dosage

Interactions

SE/Toxicity

A

Indications

  • Pseudomonal infections
  • Nosocomial pneumoniacaused by GNR in ICU

Mechanism
- Binds PBPs

Sensitive Bacteria
- streptococci,some enterococcus, many anaerobes, most GNRs including most pseudomonas

Resistant bacterial
- some pneumococcus, most Staph aureus, increasing resistant GNRs

Dosage

  • IV only
  • Renal clearance

Interactions
Good: Pseudomonas infections (usually given with gent or tobramycin for synergy

Bad: Probenecid & might inhibit methotrxate excretion

SE/Toxicity

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14
Q

Oral version of Pen G

A

Pen V

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15
Q

Penacillin that can be used oral or IV

A

Ampicilin

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16
Q

Oral version of anti-staph nafcillin

A

Dicloxacillin

17
Q

Oral version of anti-pseudomonal peiperacillin

A

Carbenicillin

18
Q

Augmentin

Dosing
Combination
Coverafe/Use

A

Oral amoxicillin plus clavulanic acid

Extends activity of amoxicillin to pathogens using this enzyme (e.g. B catarrhalis, H influenza, N gonorrhoeae, S aureus)

Used in otitis media, sinusitis, lung, skin, urine infections, bites

19
Q

Unasyn

Dosing
Combination
Coverafe/Use

A

IV ampicillin plus sulbactam

Extends activity of ampicillin to pathogens using this enzyme (e.g S aureus, H influenza, E coli, Klebsiella, bowel anaerobes)

Used for skin, intra-abdominal, pelvic, bite, head/neck infections

20
Q

Zosyn

Dosing
Combination
Coverafe/Use

A

IV piperacillin plus tazobactam

Extends activity to pathogens using this enzyme (e.g. S aureus, H influenza, Bacteroides, other GNR)

Used for pneumonia, UTI, skin, gyn, bone, intra-abdominal, septicemia infections

21
Q

Why is penicillin given frequently

A

Very short half life

22
Q

How is structure of of cephalosporin, monobactem and carbapenem different from penacillin

A

Cephalosporin
- A ring has 6 instead of 5 rings

Monobactem
- Absent A ring

Carbapenem
- A ring has 3 carbons

23
Q

What is a beta lactame

A

All contain Ring A (thiazolidine ring) attached to Ring B (beta-lactam ring)

The beta-lactam ring always has a secondary amine at the corner, with an –R group attached
The beta-lactam ring is essential for activity

If the beta-lactam ring is cleaved, then the product (penicilloic acid) lacks antibacterial activity

24
Q

What unit is penacillins ordered in

A

Ordered/measured in units (or million units) for Pen G only; mg for all others!!(As near as we can tell, this is part of a nasty plot by the NBME to torture medical students in Year 2 micro courses.)

25
Q

H. influenza

A

Ampicillin

26
Q

Major side effecto of methicillin?

  • When was it used
  • Better alternative
A

Methacillin - nephrotoxicity

Used for anti-staph

IV - Nafcillin
Oral - Dicloxacillin

27
Q

S. areus

IV
Oral

A

Nafcillin - IV only

Dicloxacillin - PO

28
Q

Only oral penicillin/beta-lactamase inhibitors

A

Augmentin amoxicillin plus clavulanic acid

29
Q

Cat & dog bites oral treatment

A

amoxicillin

30
Q

Penicillin for gram - coverage

A

Ampicilin or amoxicillin (causes less GI upset & fungal infections) so used for UTI

Gram - coverage but only IV

31
Q

Piperacillin dose

A

Gram - coverage but only IV

32
Q

Benefit of penacillin G over V

A

Penicillin G benzathine suspensin - IM in muscle over a month

V or G orally given 4 times a fay PO

Year II Pharmacology Term 5 (9 decks)

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