Penicillins Flashcards

1
Q

What is the general structure of Penicillins?

A

B-Lactam Ring with a Thiazolidine ring and an acyl side chain

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2
Q

What is the MoA of penicillins?

A

Inhibit bacterial cell wall synthesis by blocking the crosslinking of adjacent peptidoglycan strands

Results in lysis

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3
Q

What is the target of B-lactam antibiotics?

A

Penicillin-binding proteins

Transpeptidases, transglycolases and D-alanine carboxykinase

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4
Q

What are the resistance mechanisms to penicillins?

A

B-lactamase production

Alterations in penicillin binding proteins

Decreased penetration to site of action

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5
Q

What is the primary route of elimination of penicillins?

A

Renal excretion

Must adjust dose for renal insufficiency

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6
Q

What is the Cockroft-Gault equation?

A

(140-age) x weight(kg) / (SerumCreatinine) x (72)

Can be used for majority of renally excreted drugs

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7
Q

When do most penicillins achieve peak levels?

A

1-2 hours after ingestion

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8
Q

What three penicillins does food not affect absorption for?

A

Amoxicillin, Pen V, and Carbenicillin

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9
Q

Penicillins don’t distribute well to what locations?

A

Brain

CSF

Prostate

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10
Q

What is the most common adverse effect of penicillins?

A

Hypersensitivity reactions

Hypersensitivity to one means probably to all

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11
Q

What are other major adverse effects of penicillins?

A

Eosinophilia

Interstitial Nephritis (Methicillin)

Pseudomembranous Colitis

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12
Q

What are the penicillinase resistant penicillins?

A

IV - Methicillin, Oxacillin, Nafcillin

PO- Cloxacillin, Dicloxacillin

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13
Q

What are the aminopenicillins?

A

Ampicillin (QID) and Amoxicillin (TID)

Amino group allows for penetration into gram negative cell wall

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14
Q

What is the spectrum for aminopenicillins?

A

Streptococcus and Enterococcus

Haemophilus

Salmonella/Shigella

Proteus, E. coli, Klebiella

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15
Q

What are the adverse effects of aminopenicillins?

A

Hypersensitvity

Diarrhea - take with food to decrease sx

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16
Q

What are the carboxypenicillins?

A

Carbenicillin/Ticarcillin

Increased permeability to the cell wall

17
Q

What is the activity of the carboxypenicillins?

A

Streptococcus

Piddly/PEK

SPACE bugs

18
Q

What is carbenicillin?

A

Indanyl salt

Body normally cannot tolerate high dosages necessary for concentrations to treat systemic infections

19
Q

Describe Ticarcillin.

A

2-4x more active that Carbenicillin against Pseudomonas

20
Q

What are the AE’s of carboxypenicillins?

A

Hypersensitivity

Platelet dysfunction

Na+ overload

21
Q

What are the ureidopenicillins?

A

Mexlocillin

Piperacillin

22
Q

What is the spectrum of ureidopenicillins?

A

Bacteroides fragilis

Strep/Enterococcus

PEK and SPACE bugs

23
Q

What are the B-lactamase inhibitor/penicillin combinations?

A

Augmentin - amoxicillin/clavulanic acid

Unasyn - ampicillin/sulbactam

Timentin - ticarcillin/clavulanic acid

Zosyn - Piperacillin/taxobactam

24
Q

What microbes are added to coverage for penicillin/B-lactamase inhibitor combinations?

A

Staph and anaerobes