Pharm 747 Exam 1 Flashcards

1
Q

Describe the basic Mechanism of Action for B-Lactam Antiobiotics

A

B-lactam antibiotics are bactericidal, and act by inhibiting the synthesis of the peptidoglycan layer of bacterial cell walls.

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2
Q

Why is the final transpeptidation step in biosynthesis of peptidoglycan a critical drug target step?

A

It is facilitated by transpeptidases (PBPs) that are inhibited by the B-Lactams.

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3
Q

What are B-Lactam antibiotics analogs of in normal peptidoglycan synthesis?

A

the D-alanyl-Dalanine terminal amino acid residue that is the precursor for NAM/NAG peptide subunits of peptidoglycan layer

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4
Q

Why is the structural similarity between B-lactam antibiotics and the D-alanyl-D-alanine important?

A

B-lactam replaces the D-alanyl-D-alanine and inhibits the active site of PBPs

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5
Q

How do B-Lactam antibiotics act upon PBP?

A

They irreversibly bind to the Serine on the PBP active site, which prevents the final crosslinking (transpeptidation) of the peptidoglycan layer and disrupts the bacterial cell wall biosynthesis.

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6
Q

How can bacterium disrupt B-lactam antiobiotics?

A

By hydrolysis of B-lactam ring by B-lactamase or penicillinase, which will break open the ring and render the drug ineffective.

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7
Q

How can Bacterium ignore B-Lactam antibiotics?

A

They can possess altered PBPs which do not allow B-lactams to bind effectively.

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8
Q

where are transpeptidase enzymes found within gram positive and negative bacterium?

A

They are located along the exterior of the cytoplasmic membrane (+)
They are located in the periplasmic space (-)

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9
Q

What is the general structure of Penicillins?

A

6-aminopenicillanic Acid (6-APA) and a azetidinone 4-sided ring

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10
Q

What is the general structure of Cephalosporins?

A

7-amino Cephalosporanic Acid (7-ACA) and a free carboxyl on C4

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11
Q

Benzylpenicillin

Class, Brand, PO or IV, +/- , B-lactamase resistant

A
Natual Penicillin
Penicillin G
IV administration
Gram (+)
Hydrolyzed by B-lactamase
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12
Q

Phenoxymethylpenicillin

Class, Brand, PO or IV, +/- , B-lactamase resistant

A

Penicillin V
Oral administration
Gram (+)
Hydrolyzed by B-lactamase

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13
Q

Methicillin

Class, Brand, PO or IV, +/- , B-lactamase resistant

A
B-Lactmase Resistant strain
Staphcillin
IV administration
gram (+)
stable against B-lactamase
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14
Q

Nafcillin

Class, Brand, PO or IV, +/- , B-lactamase resistant

A
B-Lactamase resistant strain
Unipen
Oral Administration
Gram (+)
Stable against B-lactamase
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15
Q

Oxacillin

Class, Brand, PO or IV, +/- , B-lactamase resistant

A
B-lactamase resistant/Isoxazoyl
Prostaphlin (X1, X2 = H)
Oral Administration
Gram (+)
stable against B-Lactamase
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16
Q

Cloxacillin

Class, Brand, PO or IV, +/- , B-lactamase resistant

A
B-lactamase resistant/Isoxazoyl
Tegopen (X1 = CL, X2 = H)
Oral administration
Gram (+)
Stable against
17
Q

Dicloxacillin

Class, Brand, PO or IV, +/- , B-lactamase resistant

A
B-lactamase resistant/isoxazoyl
Dynapen (X1 , X2 = Cl)
Oral Administration
gram (+)
Stable against B-lactamase
18
Q

Ampicillin/Bacampicillin

Class, Brand, PO or IV, +/- , B-lactamase resistant

A
Aminopenicillin
Polycillin
Oral administration
Gram (+), small gram (-)
Hydrolyzed
19
Q

Amoxicillin

Class, Brand, PO or IV, +/- , B-lactamase resistant

A
Aminopenicillin
Amoxil
Oral administration
gram (+), small gram (-)
hydrolyzed
20
Q

Carbenicillin

Class, Brand, PO or IV, +/- , B-lactamase resistant

A
Carboxypenicillin
Geopen
Oral and IV administration
Gram (+) and Gram (-)
hydrolyzed
21
Q

Ticarcillin

Class, Brand, PO or IV, +/- , B-lactamase resistant

A
Carboxypenicillin
Ticar
IV administration
Gram (+) and Gram (-)
Hydrolyzed
22
Q

Pipericillin

Class, Brand, PO or IV, +/- , B-lactamase resistant

A
Acylureidopenicillin
Piperacil
IV administration
Gram (+) and (-)
hydrolyzed
23
Q

Azlocillin

Class, Brand, PO or IV, +/- , B-lactamase resistant

A
Acylureidopenicillin
Azlin
IV administration
Gram (+) (-)
hydrolyzed
24
Q

Mezlocillin

Class, Brand, PO or IV, +/- , B-lactamase resistant

A
Acylureidopenicillin
Mezlin
IV administration
Gram (+) (-)
hydrolyzed