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02 Pharmacology > V 1 Antibacterial lactams > Flashcards

V 1 Antibacterial lactams Flashcards

1
Q

Penicillin G, V Mechanisms of action

A

Bind penicillin-binding proteins (transpeptidases)
Block transpeptidase cross-linking of peptidoglycan in cell wall
Activate autolytic enzymes

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2
Q

Penicillin G, V Clinical use

A

Mostly used for gram-positive organisms (S. pneumoniae, S. pyogenes, Actinomyces)
Also used for gram-negative cocci (mainly N. meningitidis)
Spirochetes (namely T. pallidum)
Bactericidal for gram-positive cocci, gram-positive rods, gram-negative cocci, and spirochetes
Penicillinase sensitive, thus narrow spectrum

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3
Q

What is Benzathin penicillin

A

Long acting type, Thick suspension
Effective on Tertiary syphilis
IM, half life of 2 weeks (Respratory form)

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4
Q

Penicillin G, V Toxicity

A

Hypersensitivity reactions: 5-7% of I-IV HS reactions

Hemolytic anemia

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5
Q

Penicillin G, V Resistance

A

Penicillinase in bacteria (a type of β-lactamase) cleaves β-lactam ring

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6
Q

Treatment of Streptococcus agalactiae

A

ampicillin with an aminoglycoside or a cephalosporin

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7
Q

Treatment of Streptococcus pyogenes

A

Beta lactam drugs

Macrolides are used in the case of penicillin allergy.

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8
Q

Treatment of Pneumoccoci

A

Bacterial pneumonia–macrolides

Adult meningitis—Ceftriaxone or cefotaxime
Vancomycin is added if penicillin- resistant S. pneumoniae has been reported in the community

Otitis media and sinusitis in children–amoxicillin, erythromycin for allergic individuals

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9
Q

Treatment of Viridans Streptococci (S. sanguis, S. mutans)

A

Penicillin G with aminoglycosides for endocarditis

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10
Q

Treatment of Clostridium tetani

A 
Hyperimmune human globulin (TIG) to neutralize toxin plus metronidazole or penicillin
Spasmolytic drugs (diazepam); debride; delay closure
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11
Q

Treatment of Clostridium perfringens

A

Gangrene: Debridement, delayed closure, clindamycin and penicillin, hyperbaric chamber

Food poisoning: Self-limiting

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12
Q

Treatment of Actinomyces israelii

A

ampicillin or penicillin G and surgical drainage

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13
Q

Treatment of Treponema pallidum

A

Benzathine penicillin (long-acting form) for primary and secondary syphilis(no resistance to penicillin)

Penicillin G for congenital and late syphilis

Jarisch-Herxheimer reaction in treatment of syphilis

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14
Q

Treatment of Leptospira interrogans

A

penicillin G or doxycycline

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15
Q

Amoxicillin, ampicillin Mechanisms of action

A

Same as penicillin, Wider spectrum, changed solubility thus enter porines and reach cell wall of Gram -
penicillinase sensitive
Also combine with clavulanic acid to protect against destruction by β-lactamase

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16
Q

Amoxicillin Features

A

AmOxicillin has greater Oral bioavailability

than ampicillin

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17
Q

Ampicillin features

A

ampicillin undergoes enterohepatic cycling, but excreted by the kidney

18
Q

Amoxicillin, ampicillin Clinical use

A

H. influenzae, H. pylori (amoxicillin), E. coli, Proteus mirabilis, Salmonella, Shigella
Borrelia burgdoferi (amoxicillin)
Listeria monocytogenes (ampicillin)
Enterococci

19
Q

Amoxicillin, ampicillin Toxicity

A

Hypersensitivity reactions
rash
pseudomembranous colitis

20
Q

Amoxicillin, ampicillin Resistance

A

Penicillinase in bacteria (a type of β-lactamase) cleaves β-lactam ring

21
Q

Dicloxacillin, nafcillin, oxacillin Mechanism

A

Very narrow spectrum

penicillinase resistant because bulky R group blocks access of β-lactamase to β-lactam ring

22
Q

Nafcillin, oxacillin pharmacokinetics

A

Nafcillin and oxacillin eliminated largely in bile

23
Q

Dicloxacillin, nafcillin, oxacillin Clinical use

A

S. aureus (except MRSA: resistant )

24
Q

Dicloxacillin, nafcillin, oxacillin Toxicity

A 
Hypersensitivity reactions
Interstitial nephritis (methicillin)
25
Q

Dicloxacillin, nafcillin, oxacillin Resistance

A

because of altered penicillin-binding protein target site

26
Q

Treatment of Enterococcus faecalis/faecium

A

Some vancomycin-resistant strains of Enterococcus faecium or E. faecalis have no reliably effective treatment

In general for low-level resistance, use ampicillin+gentamicin, or streptomycin

27
Q

Treatment of Listeria monocytogenes

A

ampicillin with gentamicin added for imrnunocompromised patients

28
Q

Treatment of Neisseria meningitidis

A

Neonates/infants: ampicillin and cefotaxime

Older infants, children, and adults: cefotaxime or ceftriaxone with or without vancomycin

29
Q

Treatment of Salmonella enterica Subspecies Other Than typhi

A

For gastroenteritis self-limiting, antibiotics are contraindicated

For invasive disease, ampicillin, third-generation Cephalosporins, fluoroquinolones, or TMP-SMX

30
Q

Treatment of Clostridium botulinum wound

A

Amoxicillin and antitoxin respiratory support

31
Q

Treatment of Moraxella catarrhalis

A

Drug resistance is a problem; most strains produce a β-lactamase

Amoxicillin + clavulanate, second or third generation cephalosporin or TMP-SMX

32
Q

Treatment of Helicobacter pylori

A

Myriad of regimens
Omeprazole + amoxicillin + clarithromycin is one example of triple therapy - Treat for 1 0-14 days

Quadruple therapy is used in areas where clarithromycin resistance is more than 1 5%, e.g., PPI + bismuth + 2 antibiotics (metronidazole + tetracycline)

33
Q

Treatment of Pasteurella multocida

A

Amoxicillin/clavulanate for cat bites

Resistant to macrolides

34
Q

Treatment of Borrelia burgdorferi

A

Doxycycline, amoxicillin, or azithromycin/clarithromycin (primary)
Ceftriaxone for secondary
Doxycycline or ceftriaxone for arthritis

35
Q

Treatment of Staphylococcus aureus

A

Gastroenteritis is self-limiting
Nafcillin/oxacillin are drugs of choice because of widespread antibiotic resistance
For methicillin-resistant Staphylococcus aureus (MRSA): vancomycin
For vancomycin-resistant Staphylococcus aureus (VRSA) or vancomycin intermediate S. aureus (VISA): quinupristin/dalfopristin

36
Q

Piperacillin, ticarcillin, azlocillin, carbenicillin mechanism

A

Extended spectrum

37
Q

Piperacillin, ticarcillin, azlocillin, carbenicillin clinical use

A

Pseudomonas spp. and gram-negative rods
susceptible to penicillinase, use with β-lactamase
inhibitors

38
Q

Piperacillin, ticarcillin, azlocillin, carbenicillin toxicity

A

Hypersensitivity reactions

39
Q

β-lactamase inhibitors mechanism

A

Include Clavulanic Acid, Sulbactam, Tazobactam
suicide inhibitors, irreversibly inhibit enzyme

Often added to penicillin antibiotics to protect the antibiotic from destruction by β-lactamase (penicillinase)

40
Q

Treatment of pseudomonas

A

antipseudomonal penicillin (Piperacillin, ticarcillin, azlocillin, carbenicillin) + an aminoglycoside

41
Q

Penicillin pharmacokinetics

A

Most are eliminated via active tubular secretion with secretion blocked by probenecid

dose reduction needed only in major renal dysfunction

42
Q

DOCs in penicillin hypersensitivities

A

Gram + use macrolide

Gram - use Aztreonam

02 Pharmacology (3 decks)

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