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INFECTION AND IMMUNOLOGY > J Letchford Lec 3 B-lactams > Flashcards

J Letchford Lec 3 B-lactams Flashcards

1
Q

Penicillin G is a naturally occurring antibiotic. It is an asexual sporing structure of ______ mould.

A

Penicillium

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2
Q

B lactams include drugs with different nuclei as follows:

1) P______ nucleus (5 mem)
2) C_____ nucleus (6 mem)
3) C_____ nucleus (5 mem)
4) M_____ nucleus (4 mem)

A

Penicillin
Cephalosporin
Carbapenem
Monobactam

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3
Q

Bioavailability of penicillins depends on their _ group.

This could determine whether the drug is given IM, IV or PO

A

R group

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4
Q

The R group of penicillins determines:
S______ G+ve, G-ve, (Ps. aeruginosa)
S______ Na+ & K+ salts more soluble
S______ e.g Methicillin vs ampicillin in acid
B______ e.g benzylpen vs benzathin benzylpen
B-l_____ ______ e.g ampicillin vs flucloxacillin

A 
Selectivity 
Solubility
Stability
Bioavailability 
B-lactamase resistance
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5
Q

Main types of penicillins:

1) B-______ sensitive
Benzylpenicillin (Pen _)
Benzathine benzylpenicillin
Phenoxymethylpenicillin (Pen _)

A

B-lactamase sensitive
Pen G
Pen V

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6
Q

Main types of penicillins:

2) B-lactamase resistant
Flucloxacillin: Co-fluampicil (____ active) - with ampicillin to broaden spectrum as fluclox is ____ spectrum

Temocilin - resistant to _-______ from G-ve

A

Orally
Narrow
B-lactamases

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7
Q

Main types of penicillins:

3) Broad - Spectrum
Am_____, Am____ (NOT Pseudomonas though)
Co-_____ (Augmentin)

All orally active

A

Amoxicillin
Ampicillin

Co-amoxiclav (amoxicillin and clavulonic acid)

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8
Q

Main types of penicillins:

4) Anti-pseudomonal
Pi____
Pi____ and tazobactam (_____)
Ticarcillin and clavulonic acid (_____)

A

Piperacillin
Piperacillin
Tazocin
Timentin

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9
Q

Benzylpenicillin (Penicillin G)

Mainly active against gram ____ but some gram ____.
It can/can’t be taken orally.
It is/isn’t sensitive to B-lactamases

A

Gram positive but some gram negative
It can’t be taken orally
It is sensitive to B-lactamases

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10
Q

Benzylpenicillin PKs

How is it given?

Is it toxic or non toxic?

Good diffusion into body tissues and fluids

Does it reach HIGH or LOW levels in the CSF?
What about in meningitis?

A

IM, slow IV injection or IV infusion

NON toxic (can reach high blood conc quickly)

Low levels in CSF as doesn’t cross BBB but weakness in BBB in meningitis so high levels in the CSF in these instances.

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11
Q

Benzylpenicillin has a long post _____ effect.

A

Antibiotic

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12
Q

Maintenance benzylpenicillin blood levels:

  • Administer ____ doses.
  • Give ____ doses.
  • Combine with benzathine benzlpenicillin (slow release from IM site)

Dose:

  • IM, Slow IV injection or IV infusion
  • Endocarditis 2.4g every _ hrs therefore _ doses a day = __._g!
  • Std dose 1.2g _DS
A

Large
Frequent

4 hourly
6 doses a day
14.4g a day! (in endocarditis)

Std dose is 1.2g QDS

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13
Q

Benzylpenicilin:

  • Throat infections
  • En_____
  • _______ (keep IM injection in cabinet to admin)
  • Pn_____
  • Cel_____
  • Osteomyelitis

Phenoxymethylpenicillin (Orally active) used in ____ infections.

A

Endocarditis
Meningitis
Pneumonia
Cellulitis

Throat

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14
Q

Meningitis is caused by…
N______ _______
S______ _______
H______ _______

You should use ______ immediately if meningitis suspected

A

Neisseria meningitidis
Streptococcus Pneumoniae
Haemophilus influenza

Benzylpenicillin

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15
Q

Oral penicillin: Amoxicillin
The R group makes it stable in ____.

Its peak blood conc is achieved after __ mins.

It achieves good ___ levels in meningitis

It can be used in conjunction with Clavulonic acid to produce __-_____.

A

Acid
90 mins
CSF

Co-amoxiclav

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16
Q

Amoxicillin is a ___ ____ antibiotic working against most gram +ve and -ve bacteria.

It is most commonly used to treat ___ infections, and ___. tract infections.

It is sometimes used to treat GIT infections and _____ meningitis alongside G_____.

A

Broad spectrum

Oral infections
Resp. tract infections

Listerial meningitis alongside Gentamicin

17
Q

Resistance to amoxicillin is __& in E.coli, __% in H. Influenzae but mostly S_______.

A

40% in E.coli
10% in Haemophilus Influenzae

but mostly Staphylococci

18
Q

Side effects of Penicillins:
H_______
1-10% = ___, fever
0.05% = _____

Neurotoxicity
Higher risk with ____ failure
Fits, ______, unconsciousness

____ failure
High ___ affects electrolyte balance
e.g injectables esp. ______ benzylpenicillin

_____ and pseudomembranous _____. (Due to C.diff infection - superinfection after treatment with broad spec antibiotics)

A

Hypersensitivity
Rash, Fever
Anaphylaxis

Renal failure (espesh in elderly)
Hallucinations

Renal Failure
Salt
Benzathine BenzylPenicillin

Diarrhoea & pseudomembranous colitis

19
Q

Oral broad-spectrum antibiotics kill ___ bacteria.

Resistant pathogenic ___ bacteria cause ____-_______.
This causes diarrhoea and _______ colitis: C.diff (spore)

A

Gut
Gut
Pseudomembranous colitis (inflame, debris, WBCs, pus, diarrhoea)

20
Q

Cephalosporin C is isolated from Cephalosporium Acre_____.

This has no antimicrobial activity but is related to B lactams and its derivative provide useful antibiotics.

They have a _ membered ring.

Their specificity, s_____ and activity is determined by composition of _ groups 1&2

A

Cephalosporium Acremonium

They have a 6 membered ring

Selectivity

R groups 1 (antibacterial action) & 2 (Metab and PK)

21
Q

Cephalosporins:

  • Resistance to B-lactamases (NOT ____s)
  • Active against both gram +ve and gram -ve after _____ have been produced
A

ESBLs

Derivatives (as only originally active against gram +ve)

22
Q

Cephalosporins:
Activity against gram+ve bacteria:
Affinity for ___’s
Resistance to B-lactamases

Activity against gram-ve bacteria:
Penetration through ____ _______.

A

PBP’s

Outer membrane (pores need to be large enough for B lactam to get in)

23
Q

Cephalosporins have a similar spectrum of activity to _______.

Used to treat:
Septicaemia, p______, men____, biliary-tract infections, per_____, UTIs

BUT cost and _.___ risk limit use

A

Penicillins

Septicaemia, pneumonia, meningitis, biliary-tract infections, peritonitis, UTIs

But cost and C.diff risk limit use

24
Q

Cephalosporins have similar PKs to ______.

  • Most given by . or . ______ or . ______
  • Some ____
  • LOW penetration into ___ (except ______)
  • ____ excretion
A

Penicillins

I.M or I.V infusion or I.V injection
Oral
CSF except Meningitis
Renal

25
Q 
Side effects of Cephalosporins:
H\_\_\_\_\_\_
1-10% rash, \_\_\_\_
\_\_\_% anaphylaxis 
0.5-6% \_\_\_\_\_ sensitive patients allergic to cephalosporins
A

Hypersensitivity
Fever
0.05%
Penicillin

26
Q

Side effects of Cephalosporins:

  • D______, N______, _.____ S____ I______
  • RARE (0.1% patients)
  • V______, headache, dizziness
  • Renal toxicity, H______ (in early cephalosporins that used to destroy bacteria that produced vitamin K)
A

Diarrhoea
Nausea
C.Diff super infections

Vomiting
Haemorrhage

27
Q

___ Generation Cephalosporins
e.g Cefazolin (inject) and Cefradine (oral)

Active against MOST G_ve cocci
except enterococci, MRSA, staph epidermis

Active against SOME G_ves
e.g E.coli, Klebsiella pneumonia, Proteus mirabilis

GENERALLY REPLACED

A

1st

G+ve

G-ves

28
Q

2nd Generation Cephalosporins

____ spectrum compared to 1st generation.

Active against more G_ve bacteria
e.g Haemophilus influenzae, Enterobacter, Proteus mirabilis, E.coli, Klebsiella pneumoniae

More resistance to _-______.

Examples of 2nd generation are:
Cef_____ (injection, oral)
Cefaclor (oral)

Used in ____ infections and prevention of infection after surgery (p______)

A

Broader
G-ve

B-lactamases

Cefuroxime

Severe

Prophylaxis

29
Q

3rd Generation Cephalosporins

_____ spectrum
Increased activity
Increased resistance to B-lactamases

e.g
Cef____ (injection)
Cef____ (injection) OD DOSING

FOR community acquired ______
Meningitis, infantile sepsis, gonorrhoea, hospital acquired infections

SUBSET active against P_____ A_____ (difficult to treat) e.g Cef______ (injection)

A

Broad

Ceftaxime
Ceftriaxone

Pseudomonas Aeruginosa

Ceftazidime

30
Q

4th Generation Cephalosporins
Extended spectrum agents
More resistant to _-_______
Many cross the ___ even if the _____ are not inflamed

Reserved for use against difficult to treat P______ A______ and severe infections

e.g Cef____ (injection) and Cef_____ (injection)

A

B-lactamases
BBB
Meninges

Pseudomonas Aeruginosa

Cefepime
Cefpirome

31
Q

Antibiotic inhibitors of cell wall synthesis: C_______.
e.g Imipenem, M_____, doripenem.

Highly resistant to _-_____ including ____s
Broad spectrum activity against +ve and -ve and _____.

Active against difficult to treat ______ ______.

Not active against M___ or E._____

A

Carbapenems
Meropenem

B-lactamases including ESBLs
Anaerobes

Pseudomonas Aeruginosa

MRSA or E.Faecium

32
Q

Carbapenems PK, uses and SE’s:

  • Similar to other B-lactams
- _._ for:
Septicaemia
\_\_\_\_\_ \_\_\_\_\_ pneumonia
Intra-abdominal infections 
Skin and soft tissue infections 
Complicated \_\_\_
  • Issues with emerging _____: NDM-1
A

I.V

Hospital acquired pneumonia
Complicated UTI

Resistance: NDM-1

33
Q

Antibiotic inhibitors of cell wall synthesis: M______
e.g A_____

Have _ B-lactam ___

Active against G___ aerobes

NOT active against G___ or _____

Stable to most _-_______

Used for I.M or I.V septicaemia, complicated UTI

SE’s ____ likely to cause hypersensitivity

A

Aztreonam

1 Ring

G-ve
G+ve or anerobes

B-lactamases

Less likely to cause hypersensitivity

INFECTION AND IMMUNOLOGY (14 decks)

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