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152 > Antibiotics (Pens) > Flashcards

Antibiotics (Pens) Flashcards

1
Q

What are the major antibiotic categories (there are more)

A
  • Beta-lactams: penicillins, cephalosporins, carbapenems, monobactams
    • Macrolides and clindamycin
    • Tetracyclines/ glycylcyclines
    • Glycopeptides
    • Aminoglycosides
    • fluoroquinolones
    • Sulfonamides and trimethoprim
    • Metronidazole
      • Linezolid
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2
Q

What are the types of beta lactams:

A
  • Penicillins , cephalosporins, carbapenems, monobactams
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3
Q

What is the structure of penicillins

A
  • All penicillins share the same basic structure (6-aminopenicillanic acid: thiazolidine ring attached to a beta-lactam ring)
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4
Q

Are penicillins bacteriostatic or bactericidal

A
  • Bactericidal
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5
Q

MOA of penicillins

A
  • Bind to penicillin binding protein (PBP) which results in inhibition of peptidoglycan synthesis and activation of autolytic enzymes in cell wall
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6
Q

How does resistance to penicillins develop

A
  • Production of beta-lactamases
    • Lack of PBPs or altered PBPs
    • Efflux of drug out of cell
    • Failure to synthesize peptidoglycans such as mycoplasmas or metabolically inactive bacteria
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7
Q

What are the pharmacokinetics of penicillins

A
  • Oral bioavailability (F) varies
    • Wide tissue distribution including CNS
    • Most are excreted by the kidneys
    • Short half life meaning frequent dosing
    • Concentration independent drug
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8
Q

Are penicillins concentration independent or dependent drugs

A
  • Independent
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9
Q

What are concentration independent or dependent drugs

A

a) Concentration dependent drug: higher the concentration the greater effect
- Would want to give as much drug without giving toxicity
b) Independent: once you reach a specific threshold there is no greater effect
- Want to maintain that threshold concentration
- this means that ideally you would administer continuous intravenous drip however this is very inconvenient

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10
Q

Are penicillins safe in pregnancy, breast feeding

A
  • Safe in pregnancy
    • Distributed to breast milk but not a contra indication
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11
Q

Drug interaction between penicillins and oral contraceptives

A
  • Potential drug interaction
    - With penicillins you get destruction of estrogen and this can reduce the efficacy of the oral contraceptives
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12
Q

What penicillin can be taken with food

A
  • Amoxicillin
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13
Q

What adverse effects with penicillins (considered the safest antibiotics)

A
  • Allergic reactions (most common drug allergy)
    • Anaphylactic shock
    • Serum sickness (fever, joint pain, and rash)
    • Skin rashes
    • Fever nephritis (inflammation of the nephron) , eosinophilia (higher levels of eosinophils)
    • Seizures, encephalopathy delirium (brain disorder)
    • Electrolyte imbalances
    • Neutropenia (to few neutrophils), thrombocytopenia (platelet count in your blood is too low)
    • Diarrhea, gi upset
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14
Q

Types of natural penicillin

A
  • Penicillin G
    • Penicillin V (oral formulation)
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15
Q

What makes penicillin V different then penicillin G

A
  • Penicillin V is oral
    • More acid stable but still needs to be taken on an empty stomach
    • Penicillin G is acid labile (not used orally)
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16
Q

What destroys natural penicillins

A
  • Beta-lactamases
17
Q

What is penicillin G available as

A
  • Aqueous Pen G, procaine Pen G, and benzathine Pen G
    • Procaine/ benzathine IM only: toxic IV
    • The salts have different durations of activity
18
Q

What are natural penicillins spectrum of activity

A
  • Highly active against gram positive bacteria and spirochetes
    • Often DOC for streptococci, pneumococci, meningococci, spirochetes, clostridia, anaerobic, gp robs and actinomyces
    • Enterococci
19
Q

Isoxazole penicillins

A
  • Methicillin, cloxacillin, nafcillin, flucloxacillin, dicloxacillin
20
Q

What is an MRSA

A
  • Methicillin resistant staph aurous
21
Q

What is the canadian drug used for MSSA

A
  • Cloxacillin is the Canadian drug used for MSSA
22
Q

How do the isoxazole penicillins react with beta-lactamases

A
  • Relatively resistant
23
Q

What were isoxazole penicillins designed for

A
  • Staph aureus
24
Q

What are isoxazole penicillins uses

A
  • Staphylococcal infections
    • Not MRSA
25
Q

Aminopenicillins (spectrum and what destroys them)

A
  • Destroyed by beta lactamases
    Active against both gp and gn organisms
26
Q

What are the types of aminopenicillins

A

a) Ampicillin
- Used IV
- More acid stable than natural penicillins but poor bioavailability
b) Amoxicillin
- Used orally
- Better absorption then ampicillin
- Available combined with clavulanic acid

27
Q

Uses of aminopenicillins

A
  • Streptococci, enterococci, Neisseria sp, non-beta-lactamase producing H. influenzae, E. Coli, P. mirabilis, salmonella..
28
Q

What is clavulanic acid

A
  • Beta-lactamase inhibitor
29
Q

What is H. influenzae

A
  • A bacteria and not the same as influenza virus
30
Q

What do beta lactamases do

A
  • Open the beta lactam ring of penicillins and cephalosporins meaning they are no longer active
31
Q

What are ESBLs

A
  • Extended spectrum beta lactamases found in E.coli and klebsiella pneumoniae
32
Q

What is NDM-like

A
  • New Delhi metallo-beta-lactase
    • Found in acinetobacter baumannii
    • Destroys even more beta lactam rings then ESBLs
33
Q

What is the drug within ureidopenicillins

A
  • Piperacillin
34
Q

What are the uses of ureidopenicillins

A
  • Increased activity against gn rods
    Active against pseudomonas aeruginosa
35
Q

What formulations are ureidopenicillins found

A
  • Parenteral only (IV and IM)
    • Available combined with beta lactamase inhibitor tazobactam
36
Q

What is tazobactam

A

Beta lactamase inhibitor

37
Q

What is the similar structure between cephalosporins

A
  • 7-aminocephalosporonic acid

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