Pharm Spring Exam 2- Inhibitors Of Cell Wall Synthesis

Front 1

Natural Penicillin

Drugs

Back 1

1) Penicillin G (IV, IM, Oral?)
2) Benzathine penicillin (IM depot)
3) Procaine Penicillin G (IM)
4) Penicillin V (acid resistant, Oral)

Front 2

Natural Penicillin

Characteristics

Back 2

1) Highest activity against G+
2) Some G- coverage
3) Some anaerobic coverage
4) Inactivated by B-lactamase
5) No antipseudomonal activity
6) Eliminated by kidney
7) No CNS penetration

Front 3

Penicillinase resistant Penicillins
(Antistaphyloccocal penicillins)

Drugs

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1) Nafcillin (IV/IM, liver metabolism)
2) Cloxacillin (Liver metabolism)
3) Oxacillin (Liver metabolism)
4) Dicloxacillin
5) Methicillin

Front 4

Penicillinase resistant Penicillins
(Antistaphyloccocal penicillins)

Characteristics

Back 4

1) Lower activity against some G+
2) Some G- and anaerobe coverage
3) Some acid stable
4) DOC penicillinase making S.Aureus
5) Hepatic metabolism and Renal excretion

Front 5

Extended spectrum penicillins

Drugs

Back 5

Ampicillin
Amoxacillin

Front 6

Extended spectrum penicillins

Characteristics

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1) Lower G+ coverage
2) Extended G- coverage (E.Coli, Salmonella, Shigella, H. Flu, Proteus)
3) Anaerobic coverage with penicillinase inhibitor
4) Acid resistant
5) Urinary excretion

Front 7

Antipsuedomonal penicillins

Drugs

Back 7

1) Piperacillin
2) Ticaricillin
3) Mezlocillin
4) Carbenicillin
In order of most activity

Front 8

Antipsuedomonal penicillins

Characteristics

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1) Spectrum: all covered by extended spectrum penecillins, plus some G- bacteria (Proteus, Enterobacter, Providencia, Serratia)
2) Major use: Pseudomonas and actinetobacter
3) Suceptible to B-lactamase
4) Acid sensative
5) Renal excretion

Front 9

Combinations with B-lactamase inhibitors

Drugs

Back 9

1) Ampicillin and Sulbactam
2) Amoxicillin and Clavulanic Acid
3) Piperacillin and Tazobactam
4) Ticarcillin and Clavulanic acid

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Combinations with B-lactamase inhibitors

Characteristics

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1) Addition of B-lactamase inhibitors extends spectrum of these agents
2) Not all B-lactamases are inhibited
3) MRSA as resistant still.

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Penicillin G

Bacteria susceptibility

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Short list
1) Strep pneumo
2) N. Gonorrhea
3) Clostridia

Front 12

Penicillin G

Mechanism

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1) Bactericidal
2) Inhibit final stage of bacterial cell wall synthesis
3) Leads to lysis

Front 13

Penicillin G

Bacterial resistance

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1) B-lactamase
2) Decrease permeability of outer membrane
3) Alter PBPs
4) Autolytic enzymes not being activated
5) Lack of cell wall
6) Non peptidoglycan based cell wall

Front 14

Penicillin G

Pharmacokinetics Oral

Back 14

not good, especially for syphilis, subacute bacterial endocarditis, actinomycosis

Front 15

Penicillin G

Pharmacokinetics Parenteral

Back 15

IM/IV high but transient concentration
Painful
Intrathecal should never be done=seizures
IM=procaine penicillin G
Benzathine Penicillin G-long lasting but low concentrations, used for syphilis

Front 16

Penicillin G

Distribution

Back 16

1) Widely distributed
2) Poor CNS penetration
3) Bound in excess of 70%
4) Need to give twice the loading dose

Front 17

Penicillin G

Excretion

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1) Most rapidly excreted drug by normal kidney.
2) Can excrete 3million U per hour
3) Partially blocked by probenecid

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Penicillin G

Toxicity

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1) Allergy
2) Tissue irritation
3) Excess Na+/K+ (Cardiac/renal)
4) Superinfection
5) Soft frothy stools, diarrhea
6) Jarisch-Herxheimer Reaction

Front 19

Penicillin G

Allergy

Back 19

Penicillin are the foremost
Cross allergic potential and cross sensitizing
Ampicillin Rash not allergy

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Monobactams

Back 20

Aztreonam

G - rods
no activity against G+ or anaerobes
Safe in patients with a penicillin allergy

Front 21

Carbapenems

Drug

Back 21

1) Imipenem
2) Cilastatin
3) Meropenem
4) Ertapenem

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Carbapenems

Characteristics

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1) G+, G-, anaerobic
2) Imipenem can cause seizures
3) Combination of Cilastatin and imipenem to increase half life
4) Metabolite nephrotoxic

Front 23

Carbapenems

Ertapenem

Back 23

1) Highly stable against beta lactamases
2) Has activity against G-, G+, anaerobic particular Enterobacteriaceae
3) IV/IM