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Pharmacology > Week 4: antibiotics Anti-Bacterial Agents: Cell Wall Synthesis Inhibitors > Flashcards

Week 4: antibiotics Anti-Bacterial Agents: Cell Wall Synthesis Inhibitors Flashcards

1
Q

What are characteristics of Anaerobes?

A

Grow only in the absence of O2​
Found in oral and GI tract and vagina​
Most anaerobes are medically important to know​
Cause diseases when normal mucosal barriers do not function normally​
Can be classified as gram negative vs positive​

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2
Q

What color are gram positive vs gram negative microbs and why?

A

Gram positive are purple

Gram negative are pink since when cleaned with ethanol it becomes clear

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3
Q

Broad spectrum vs narrow spectrum bacteria

A

broad: effective against multiple organisms from more than a single class, more likely to disrupt normal flora, risk of superinfection by a second organism
narrow: effective against limited number of organism, unlikely to disrupt normal flora

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4
Q

bacteriostatic vs bactericidal?

A

bacteriostatic: capbale of inhibiting growth or reproduction of bacteria, does not kill them.

bacterialcidal:
capable of actively killing bacteria, 99.9% killing within 18 to 24 hours in lab condition

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5
Q

MIC (Minimum inhibitory concentration)

A

:the lowest concentration of antibiotics that inhibits bacterial growth

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6
Q

MBC (Minimum bactericidal concentration):

A

Lowest concentration of antibiotics that kills 99.9 % of bacteria

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7
Q

Cell Wall Synthesis Inhibitors

A 
Beta Lactams
-Penicillin
-Cephalosporins
-Carbapenems
-Monobactams
Beta-Lactamase Inhibitors
Vancomycin
Others
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8
Q

What is Atypical bacteria?

A

An inexact term applied to bacteria which are particularly “unusual” in structure, morphology, biochemistry, or life cycle.​

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9
Q

Gram positive

Cocci

A

Staphylococcus aureus
Streptococcus
Enterococcus

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10
Q

Gram positive

Rods

A

(Corney
Mike’s list of basic cars)

Corneybacterium
Mycobacteria 
Listeria 
Bacillus
Nocardia
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11
Q

Gram positive

Anaerobes

A

(CLAP)

Clostridium
Lactobacillus
Actinomyces
Propionibacterium

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12
Q

Gram negative

A

Aerobes:
Neisseria meningitidis (Meninogococcus)
Neisseria gonorrhoeae

Anaerobes: 
Haemophillus influenzae
Escherichia coli (E. coli)
Klebsiella pneumoniae
Proteus mirablilis 
Pseudomonas aeruginosa
Moraxella catarrhalis
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13
Q

Atypicals

A

Mycoplasma pneumoniae : Walking pneumonia​

Chlamydia trachomatis & pneumoniae: PID, STD , pneumonia​

Rickettsia : Rocky mountain spotted fever, typhus fever​

Legionella :Legionnaires’ disease (severe pneumonia)​

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14
Q

Enterococci

A

UTI, bacteremia, endocarditis, meningitis

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15
Q

strep pnumoniae

A

sepsis, pneumonia, meningitis, middle ear infection in children, sinusitis

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16
Q

Group B strep

A

sepsis, pna, meningitis in newborns, mostly not harmful, natrually comes and goes in our body,mild idsease UTI, vaginitis,

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17
Q

group A strep (s.pyogenes)

A

strep throat, rheumatic fever, post-streptococcal glomerulonephritis, impetigo, sinusitis, cellulitis, necrotizing fasciitis

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18
Q

Gram Positive: Clostridium Difficile risk factors

A

Diarrhea to life threatening inflammation of colon
older adults in hospital or nursing homes
after abx use

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19
Q

Gram Positive: Clostridium Tetani risk factors

A

tetanus

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20
Q

Gram Positive: Clostridium Perfringens risk factor

A

most common causes of food poisoning

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21
Q

Gram negative: Pseudomonas

A

UTI, respiratory, soft tissue infection, GI infection, sepsis, usually form hospitalized patients

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22
Q

Gram Negative: Hemophilus influenzas

A
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23
Q

Gram negative: escherchia coli

A

most strain is not harmful, diarrhea, UTI

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24
Q

Gram Negative: Kiebsiella Pneumoniae

A

mostly not harmful, lives in GI and feces normally, can cause pneumonia, UTI, cellulitis, etc

25
Q

Gram negative: moraxella catarrhalis

A

normally present in oropharynx, skin and genital area, could cause conjunctivitis, upper and lower respiratory infection in kids and adults

26
Q

Gram negative: shigella and salmonella

A

shigellosis-diarrhea, fever, stomach cramp, salmonellosis

27
Q

inhibitors of metabolisms

A

sulfonamides, trimethoprim

28
Q

inhibitors of cell wall synthessis

A

Beta-lactams, daptomycin, fosfomycin, lipoglycopeptide, vancomycin

29
Q

inhibitors of protein synthesis

A

ahminoglycosides, chloramphenicol, clindamycin, macrolides, oxazolidinone, tetracyclines

30
Q

inhibitors of cell membrane function

A

amphotericin B, isonizaid, polymyxins

31
Q

inhibitors of nucleic acid function or synthesis

A

fluoroquinolones, rifampin

32
Q

Penicillin

A

PCNs: 1st Antibiotic: 1928​
For Streptococcal and staphylococcal infections​
Synthetic PCNs: Developed to overcome resistance issues​
Classified based on the spectrum of activity​
Have both narrow and broad spectrum

33
Q

What is the penicillin class/clinical indication?

A

Narrow and Broad spectrum
Time-dependent bactericidal

Effective for Gram-positive organisms : Upper /Lower respiratory . UTI, STIs, Endocarditis
Extended spectrum PCNs: Pseudomonas​ (G -)

34
Q

Penicillin pharmacokinetics

A

Oral formulations are acid-stable​
PO absorption is inhibited by co-ingestion of food​
Widely distributed​

Penetrate CSF in presence of inflammation​ ( penicillin can cross BBB well without inflammation)

Excreted by kidneys​
Dosage adjustment with impairment​

Prolonged effects by administration with Probenecid by inhibiting tubular secretion
Half-life is typically 30 – 90 minutes​

35
Q

What are drawbacks of penicillin?

A

Seizure activity: high-dose with renal impairment
Rare: leukopenia, thrombocytopenia and hemolytic anemia

Allergic reactions:​
Urticaria to hemolytic anemia and anaphylaxis,​
Assume cross-reactivity throughout class,: 10% of persons who are allergic to PCN are also allergic to Cephalosporins​
GI Disturbances:​
N/D caused by oral
medications via direct irritation or over growth of G+ organisms or yeast;​
Ampicillin implicated in pseudomembranous colitis​

Drug Interaction
Rare

36
Q

What are action of resistance in penicillin?

A

β-lactamase produced by bacteria cause enzymatic hydrolysis of the B-lactam ring, resulting in loss of antibacterial activity​
​

37
Q

Cephalosporins

A

Structurally similar to PCNs​
“Generations”​
Based on spectrum of activity
1st → 5th : increase in gram (-) coverage and loss of gram (+) activity ​

38
Q

What class are Cephalosporins?

A
  • Time-dependent bactericidal effect
  • Gram positive to Gram negative
  • newer generation covers more gram negative
39
Q

Cephalosporins pharmacokinetics?

A

A: IV and PO,
Well-absorbed from GI tract
Food may enhance absorption
D: Most 1st & 2nd –generation do not cross BBB, even with inflamed meninges
M: Cephalosporins with side chains may undergo hepatic metabolism
E: Majority excreted unchanged in urine via active tubular secretion; EXCEPT
cefoperazone and ceftriaxone, which are mainly excreted in bile

40
Q

What are drawback of Cephalosporins

A 
Safe with favorable toxicity profile
Allergic Reactions:
5-15% of persons allergic to PCN are also allergic to cephalosporins
Anaphylaxis
Fever
Skin rash
Nephritis
Granulocytopenia
Hemolytic anemia
Other reactions:
MT sidechain causes hypoprothrombinemia and inhibits aldehyde dehydrogenase (can cause disulfiram-like reaction with ETOH ingestion)
Local irritation at injection site
Drug Interaction
Rare
May ↑ aminoglycoside toxicity
Probenecid & loop diuretics Increases half-life of some cephalosporins, inhibiting tubular secretion
41
Q

What are action of resistance for Cephalosporins?

A

Less than seen with PCNs due to more stable β-lactam ring
Via production of β-lactamase
Via decreased membrane permeability to cephalosporins
Via mutation in the binding site on cell membrane

42
Q

What are the First generation of Cephalosporins and spectrum of activity

A

-cefazolin, cefadroxil, cephalexin
-Best for G + cocci​
G – (P. mirabilis, E coli, K. pneumoniae)
Susceptible to B-lactamase​
Does not cross BBB
-

43
Q

First generation of Cephalosporins clinical use and indication

A

Skin Infections​
Pneumococcal respiratory infections​
UTI​
Surgical Prophylaxis​

44
Q

What are the second generation of Cephalosporins and spectrum of activity

A 
Cefaclor
Cefprozil
Cefuroxime sodium
Cefuroxime axetil
Cefotetan/Cefoxitin
-----
Extended G – coverage​ (H. flu)
Less activity against G+ organisms than 1st Generation​
Does not cross BBB
45
Q

Second generation of Cephalosporins clinical use and indication

A

CAP​
Respiratory infections​
Skin infections​

46
Q

What are the third generation of Cephalosporins and spectrum of activity

A

Cefdinir
Cefixime
Cefotaxime
Ceftazidime/Ceftriaxone
—–
Active against G- bacilli​ (H. flu, Meningococcus)
May be useful for G + infections​ (Pneumococcus)

47
Q

Third generation of Cephalosporins clinical use and indiciations

A

Generally reserved for serious infections (i.e. Bacterial meningitis)​
PCN-resistant Neisseria gonorrhoeae infection

Pseudomonas
Lyme disease

48
Q

What are the fourth generation of Cephalosporins and spectrum of activity

A

Cefepime

G+ activity of 1stGeneration​
Active for G- organisms​ as 3rd generation
More resistant to β-lactamases produced by G- organisms​
Does cross BBB

49
Q

Fourth generation of Cephalosporins clinical use and indiciation?

A

Better or infections caused by Beta-lactamase-producing G- organisms: Enterobacter, Haemophilus, Neisseria​,
Pseudomonas, nosocomial bacterial infection
In general, administer with other agents(aminoglycosides) to prevent resistance​
As the generation increases, so does the potency and spectrum, esp. against G- species​

50
Q

What are the fifth generation of Cephalosporins and spectrum of activity

A

Ceftaroline
Broad spectrum
Does not cross BBB

51
Q

Fifth generation of Cephalosporins clinical use and indications

A

MRSA

52
Q

Beta-Lactamase Inhibitors

A

Prevents the breakdown of the beta-lactam ring by beta lactamase producing the bacteria
But NO significant antibacterial activities or cause side effects
Usually used as combination drugs
Bacteria can produce penicillinases or beta-lacatmases​ 🡪 Inactivate PCN and cephalosporines​

53
Q

Beta-Lactamase Inhibitors class/clinical indications

A

Broad spectrum
Intraabdomen and GYN infections
Skin & Soft tissue infection: human and animal bites
Diabetic foot infections
Respiratory track aspiration: pneumonia sinusitis abscess

54
Q

Beta-Lactamase Inhibitors pharmacokinetics

A

Penetrates most body tissues
Exception: CNS/Brain
Elimination: glomerular filtration: renal dysfunction & dialysis necessitate dosage change

55
Q

Beta-Lactamase Inhibitors action of resistance

A
  • Bacteria produce β-lactamase → breaks down β-lactam → penicillin inactive
  • Diminishes cell wall permeability to drug
  • Via mutation in the binding site on cell membrane
56
Q

Vancomycin

A

cell wall synthesis inhibitor, bactericidal, mostly gram positive (including MRSA) but covers gram negative for c.diff
serum concentration needed for IV

57
Q

Which generation achieves therapeutic level at CSF for cephalosporin?

A

3rd generation

58
Q

which generation of cephalosporin treats MRSA?

A

5th generation

59
Q

Which PCN have pseudomonas coverage?

A

ampicillin, amoxicillin

Pharmacology (4 decks)

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