Dna Transcription & Translation Inhibitors

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Fluoroquinolones
-target
-cidal or static?
-MOA
-Spectrum
-PHK
-Adverse effects
-Contraindications

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"--floxacin"

*Target: DNA Gyrase

CIDAL

MOA: Prevents relaxation of positively supercoiled DNA that is required for normal transcription and replication

Spectrum: Variable spectrum throughout the class (fairly broad)

PHK: Oral
Excellent tissue penetration
Poor CNS penetration

Adverse effects:
*Cartilage erosions (don't use in children!)
*Tendon rupture

Contraindications:
*Pregnant women
*Children <18yrs (cartilage damage)

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Fluoroquinolone that is Antipseudomonal

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Ciprofloxacin

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*Ciprofloxacin

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Fluoroquinolone
Antipseudomonal

*DOC: Effective prophylactic agent against Anthrax

If Gonorrhea is unresponsive to Ceftraixone, can use Cipro

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Fluoroquinolones that are used for Prostatitis

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Norfloxacin & Ofloxacin

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Fluoroquinolones that are Anerobes

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Moxifloxacin & Gemifloxacin

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Norfloxacin

Back 6

Fluoroquinolone
used for Prostatitis

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Ofloxacin

Back 7

Fluoroquinolone
used for Prostatitis

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Moxifloxacin

Back 8

Fluoroquinolone
Anaerobe

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Gemifloxacin

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Fluoroquinolone
Anaerobe
active against PRSP

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Metronidazole
-used by?
-MOA
-Static or Cidal?
-Spectrum
-Used for?
-PHK
-Adverse Rxns

Back 10

Used by: Dentists

MOA: Taken up into bacterial DNA, and form unstable molecules --> inhibiting DNA

CIDAL

Spectrum: ((ANaerobes G+ & G-

Used for: **Pseudomembranous colitis (caused by Clindamycin)

PHK: Oral, IV, Topical

Adverse Rxns: Central & Peripheral nervous system toxicity (convulsive seizures & peripheral neuropathy w/ prolonged use)

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Sulfonamides
-names
-MOA
-Static or Cidal
-Spectrum
-PHK
-Toxicity
-Contraindications
-Resistance

Back 11

Names: Bactrim & Silvadene

MOA:
Competes w/ PABA (Para-AminoBenzoic Acid) for incorporation into FOLIC ACID --> no folic acid --> no purine synthesis --> no DNA synthesis --> no RNA synthesis --> no protein synthesis

STATIC

Spectrum: G+ & G- (used in AIDs pts)

PHK: Oral & IV (freely crosses the placenta & BBB)

Toxicity:
*Drug sensitivity (#2 drug for allergic rxns!!)
Steven Johnson Syndrome
**Kernicterus (sulfonamides compete with the binding of bilirubin to plasma proteins --> INCREASE bilirubin)

Contraindications:
*INFANTS <2months of age (b/c sulfonamides INC bilirubin and it can get into the CNS)*
*Avoid in near term or in nursing premature or jaundiced infants*

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Bactrim

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Sulfonamide
PHK: Oral, IV

Synergistic relationship (2 drugs):
one is a sulfonamide that competes with PABA
the other is not a sulfa drug and inhibits downstream pathway

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Silvadene

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Sulfonamide
only one that is TOPICAL!

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Lipopeptide Antibiotics
-name
-MOA
-Cidal or Static
-Spectrum
-PHK

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Name: Daptomycin

MOA:
Does not penetrate bacterial cytoplasm
Binds to bacterial membrane (Forming transmembrane channels) --> rapid depolarization --> inhibition of protein, DNA, & RNA synthesis --> bacterial cell death

CIDAL

Spectrum: G+
MRSA, MSSA --last resort drug!

PHK: IV
*Suitable for empiric therapy in pts w/ serious G+ infections

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Daptomycin

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Lipopeptide Antibiotic

*Suitable for empiric therapy in pts with serious G+ infections

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Mupirocin
-Target
-Spectrum
-Static or Cidal?
-PHK
-Use

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*Target: Isoleucyl-tRNA synthetase
--> inhibition of protein & RNA synthesis

Spectrum: G+ & G-

Static at low conc
Cidal at high conc

PHK:
*Topical to the nose or nares

Use:
*Impetigo
*Intranasal application for pts carrying MRSA

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Polypeptide Antibiotics
-names
-Target
-MOA
-Static or Cidal?
-Spectrum
-Toxicity
-PHK:
-Use

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Names: Polymyxin B & Colistin

*Target: Lipid A (only on G-)

MOA: bind to G- bacterial membranes (lipid A)

CIDAL

Spectrum: G-

Toxicity: *Nephrotoxicity

PHK: *ONLY USED TOPICALLY! (too toxic orally)

Use:
*Topical in combo w/ Neomycin & Bacitracin
*Topical application to wounds, burns, etc & eye

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Polymyxin B

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Polypeptide Antibiotic

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Colistin

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Polypeptide Antibiotic

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Kernicterus

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Toxic effect of Sulfonamides

Due to the Increase in bilirubin from sulfonamides and

Should not use Sulfonamides in infants <2 months of age! Or in mothers near term, or nursing premature or jaundiced infants