Fluoroquinolones

Question 1

Amphoretic and zwitter ionic nature enable the drugs to act

Answer 1

as acids/bases and neutral

Question 2

are we using 1st generation drugs?

Answer 2

no

Question 3

2nd generation drugs

Answer 3

• Ciprofloxacin
• Enrofloxacin
• Marbofloxacin
• Danofloxacin
• Difloxacin

Question 4

3rd generation drugs

Answer 4

Orbifloxacin

Question 5

4th generation drugs used?

Answer 5

not really. at least not for this course.

Question 6

static or cidal?

Answer 6

CIDAL

Question 7

How does it go about inhibiting DNA synthesis?

Answer 7

Inhibits bacterial DNA gyrase / Type II topoisomerase

Question 8

Which enzyme is Responsible for maintaining bacterial dna in the chromosome?

Answer 8

DNA gyrase / Type II topoisomerase in GRAM - bacteria!

Question 9

What do the drugs target?

Answer 9

DNA gyrase enz

Question 10

What do the drugs do to the DNA G enzyme?

Answer 10

prevents it from doing negative supercoiling so now the DNA strand has a whole bunch of positive supercoiling and the replication can’t be completed. dead bacteria.

Question 11

So, Gram- have the Type II topoisomerase enzyme that these drugs can target.
What about Gram + bacteria?

Answer 11

Gram + have Type IV topoisomerase enzyme and if the drugs can target that one as well, BAM. broad spectrum baby.

Question 12

Spectrum aka What can these drugs kill?

Answer 12

mostly G-.
Can kill PA with combo or CIPRO and MARBO!

Can do some G +

Intracellular

Rickettsia

Mycoplasma

Question 13

CIPRO and MARBO together treats

Answer 13

PA

Question 14

ENRO and MARBO together treats

Answer 14

Canine pyoderma
 Rickettsial infections
 Acute Ehrlichiosis in dogs
 Bartonella infections in cats
 Mycoplasma and Mycobacteria infections

Question 15

PREMA treats

PRADO treats

Answer 15

MRSA and enterococci resistant to Vancomycin

Gram- and Gram+ enzymes/ocular lesions/uti/soft tissue

Question 16

Factors that affect the fluoroquinolone action

Answer 16

1) Cations at the site of infection…Just like Aminos!

2) acidic pH

Question 17

ORAL absorption…what’s the deal?

Answer 17

it’s pretty good.
not affected by food.
100% in small animals but low in ruminants. variable in horses.

Question 18

ENRO and SARA treat

Answer 18

poultry infections

Question 19

Distribution where and what are the exceptions?

Answer 19

really good and can get tissue concentrations comparable to that in the plasma EXCEPT EYE AND CNS

Question 20

Enro has great concentration in

Answer 20

bone prostate skin

Question 21

Enro, Marbo, Orbi= EMO

great for?

Answer 21

Prostate tissue.

Your prostate is sick and looks so EMO. So depressed man…

Question 22

Why’s this group of drugs so good with treating intracellular pathogens?

Answer 22

Because they accumulate really well in phagocytic cells (Macs and neu’s)

Question 23

Drugs are metabolized where?

Answer 23

liver via oxidation

Question 24

3 MAIN ACTIVE METABOLITES!

Answer 24

DIFLO->SARAFLO
ENRO->CIPRO
PEFLO->NORFLOXACIN hey!

Question 25

Enterohepatic circulation?

Answer 25

yep

Question 26

Excretion happens where?

Answer 26

kidneys: glom and tubular secretion

bile

there’s an exception….

Question 27

Where does DIFLO get excreted?

Answer 27

POOP! just like Doxy.

Question 28

“Basic” Adverse effects

Answer 28

Photosensitivity like doxy
crystalluria
CNS effects

Question 29

Unique Adverse effects

Answer 29

ARTHROPATHY UNIQUE. SEEN IN YOUNG ANIMALS. LAMENESS AND JOINT SWELLING SEEN WITH ENRO/MARBO/ORBI…REVERSIBLE

OCULAR TOXICITY IS UNIQUE AS WELL. Can end up in blindness.
Cataracts with ENRO

Issues with tendons as well. Tendinopathy.

CNS Excitation just like in horses with PENICILLIN

Question 30

How does the joint arthopathy come about?

Answer 30

chelation of Mg2+ from the membrane= proteoglycan loss in articular cartilage

Question 31

How can resistance come about?

Answer 31

can have mutations in that A gene for the DNA gyrase enzyme that would then allow structural modification.

can also decrease the amount of concentration intracellularly by reducing the number of porins on the target cells

Efflux

Question 32

Type 1 2 or 3?

Answer 32

TYPE 1