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Botany > beta-lactam inhibitors - penicillin > Flashcards

beta-lactam inhibitors - penicillin Flashcards

1
Q

Vary in resistance to gastric acid
 Vary in their oral bioavailability
 Polar compounds
 Not metabolized extensively

A

penicillins

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2
Q

penicillins are excreted unchanged or changed

A

unchanged

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3
Q

penicillins Excreted unchanged in urine via

 Inhibited by probenecid

A

 Glomerular filtration

 Tubular excretion

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4
Q

Tubular excretion of penicillin is Inhibited by —

A

probenecid

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5
Q

Major antibiotics that inhibit cell wall synthesis

A

Penicillins

Cephalosporins

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6
Q

 Partly excreted in bile

A

Ampicillin and nafcililin

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7
Q

penicillins are Derivatives of ?

A

6-aminopenicillanic acid

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8
Q

Plasma half-life of penicillins vary from –

A

30 min to 1 h

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9
Q

Given intramuscularly
Long half-lives
Drug is released slowly
Cross blood-brain barrier when meninges are inflamed

A

Procaine and benzathine penicillin G

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10
Q

penicillin inhibit cell wall synthesis by the following steps

A
  1. Binding of the drug to specific receptors (penicillin-binding proteins [PBPs]) located in the bacterial cytoplasmic membrane
  2. Inhibition of transpeptidase enzymes that act to cross-link linear peptidoglycan chains
  3. Activation of autolytic enzymes that cause lesions in the bacterial cell wall
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11
Q

? hydrolysis of the beta-lactam ring results in the lost of antibacterial activity

A

Enzymatic

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12
Q

 Penicillinases

 Formed by most staphylococci and gram (-) organisms

A

beta lactamases

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13
Q

 Major mechanism for bacterial resistance

A

beta lactamases

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14
Q

Another mechanism of bacterial resistance
responsible for:
 Methicillin resistance in staphylococci
 Penicillin G resistance in pneumococci

A

Structural changes in target PBPs

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15
Q

 Contribute to resistance by impeding access of penicillin to PBPs
 Resistance in some gram (-) rods like P. aeruginosa

A

Changes in the porin structure in the outer membrane

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16
Q

3 types of resistance to penicillin

A

beta lactamases
Structural changes in target PBPs
Changes in the porin structure in the outer membrane

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17
Q

 Prototype Narrow-spectrum penicillinase-susceptible agents

A

penicillin G

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18
Q 
PENICILLIN G
	Prototype of narrow-spectrum penicillinase-susceptible agents
	Parenteral 
	Limited spectrum of activity
	Susceptible to beta-lactamases
A

PENICILLIN G

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19
Q 
	For infections caused by 
	Streptococci
	Meningococci
	Gram (+) bacilli
	Spirochetes
A

PENICILLIN G

20
Q

 Drug of choice for syphilis

 Activity against enterococci is enhanced by aminoglycoside

A

PENICILLIN G

21
Q

 Oral drug

 Oropharyngeal infections

A

PENICILLIN V

22
Q

Very-narrow-spectrum penicillinase-resistant agents (3)

A

METHICILLIN (prototype), NAFCILLIN, OXACILLIN

23
Q

 Treatment of known or suspected staphylococcal infections
 Methicillin-resistant S. aureus (MRSA) and S. epidermidis (MRSE) are resistant to other members of this subgroup and often to multiple antimicrobial drugs

A

METHICILLIN (prototype), NAFCILLIN, OXACILLIN

24
Q
  1. Wider spectrum penicillinase-susceptible agents
A

ampicillin and amoxicillin

PIPERACILLIN and TICARCILLIN

25
Q 
	Wider spectrum than pen G 
	Susceptible to penicillinases
	Uses similar to pen G  
	Enterococci		 L. monocytogenes
	E. coli			P. mirabilis
	H. influenzae		M. catarrhalis
	Enhanced activity in combination with inhibitors of penicillinases
	Synergistic (1+1=3) with aminoglycosides in enterococcal and listerial infections
A

ampicillin and amoxicillin

26
Q

 Activity against gram (-) rods
 Pseudomonas
 Enterobacter
 Some cases of klebsiella species
 Synergistic action with aminoglycosides
 Susceptible to penicillinases
 Enhanced activity in combination with inhibitors of penicillinases

A

PIPERACILLIN and TICARCILLIN

27
Q

toxcity of penicillin

A

allergy

GI disturbances

28
Q

toxcity of penicillin

A

allergy

GI disturbances

29
Q

can cause neutropenia

A

Nafcillin

30
Q

causes maculopapular rashes

A

Ampicillin

31
Q

causes interstitial nephritis more than other penicillins

A

Methicillin

32
Q

cross-allergenicity (complete or not)

A

Complete

33
Q

GI disturbances are caused by

A

 Oral penicillins especially ampicillin

34
Q

specific GI disturbances

A

nausea and diarrhea

35
Q

Pseudomembranous colitis

Maybe caused by (2)

A

direct irritation or by overgrowth of gram (+) organisms or yeasts

36
Q

An antimicrobial drug that can eradicate an infection in the absence of host defense
mechanisms; kills bacteria

A

bactericidal

37
Q

An antimicrobial drug that inhibits antimicrobial growth but requires host defense
mechanisms to eradicate the infection; does not kill bacteria

A

Bacteriostatic

38
Q

Drugs with structures containing a beta-lactam ring: includes the penicillins, cephalosporins
and carbapenems. This ring must be intact for antimicrobial action

A

Beta-lactam antibiotics

39
Q 
Bacterial enzymes (penicillinases, cephalosporinases) that hydrolyze the beta-lactam ring of
certain penicillins and cephalosporins
A

Beta-lactamases

40
Q

Potent inhibitors of some bacterial beta-lactamases used in combinations to protect
hydrolyzable penicillins from inactivation

A

Beta-lactam inhibitors

41
Q

Lowest concentration of antimicrobial drug capable of inhibiting growth of an organism in a
defined growth medium

A

Minimal inhibitory concentration (MIC)

42
Q

Bacterial cytoplasmic membrane proteins that act as the initial receptors for penicillins and
other beta-lactam antibiotics

A

Penicillin-binding proteins (PBPs)

43
Q

Chains of polysaccharides and polypeptides that are cross-linked to form the bacterial cell wall

A

Peptidoglycan

44
Q

More toxic to the invader than to the host; a property of useful antimicrobial drugs

A

Selective toxicity

45
Q

Bacterial enzymes involved in the cross-linking of linear peptidoglycan chains, the final step in
cell wall synthesis

A

Transpeptidases

45
Q

Cross allergenicity with penicillins (complete, incomplete, partial) is assumed

A

Complete cross allergenicity must be assumed

46
Q

T or F: 5-10% of patients with history of allergic rxns to penicillin will have the same rxn when given again

A

True

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