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Infection and Immunity 2- Lecture 7
Aminoglycosides, Tetracyclines, and Glycycline
30
Medical
Professional
04/29/2013

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Cards

Term
Difference between the concentration of drug needed for concentration-dependent vs. time-dependent antimicrobials
Definition

Concentration dependent- conc. needs to be WELL above MIC

 

Time dependent- conc. needs to be above (about 4xs) the MIC

 

Term
Aminoglycosides are ___ dependent
Definition
concentration
Term
Aminoglycosides have activity against ___ and ___
Definition
Psuedomonas and other gram- bacteria
Term
4 potential toxicities associated with Aminoglycosides
Definition
nephrotoxicity, ototoxicity, teratogen, and neuromuscular blockade
Term
Describe the structure of Aminoglycosides
Definition
Six-membered ring  
with amino group substituents -aminocyclitol
Term
Give the MOA for Aminoglycosides
Definition
They bind the 30S ribosome of bacteria and cause misreading of mRNA
Term
What kind of environments reduce the activity of Aminoglycosides? (2)
Definition
acidic or anaerobic environment
Term
What are the 2 parts of the energy dependent phase of Aminoglycoside action?
Definition

initial slow energy-dependent phase (EDP- I)

+

Rapid energy-dependent phase (EDP-II)

 

(bacterial killing occurs between these 2 phases)

Term
2 methods by which bacteria have resistance to Aminoglycosides
Definition

Reduced entry/increased efflux

or

enzymatic modificaiton

Term
Which antibiotic tends to have a post-antibiotic effect (persistent suppression of bacterial growth)?
Definition
Aminoglycosides
Term
How aminoglycosides are administered
Definition
IV or intramuscular
Term
Where nephrotoxicity can occur in aminoglycoside use
Definition
proximal tubule
Term
Describe ototoxicity in aminoglycoside use
Definition
Irreversible high frequency hearing loss
Term

Describe neuromuscular paralysis in aminoglycoside use

- when

- how (2 ways)

- how to fix

Definition

Can occur when there's a rapid rise in drug concentration

 

Inhibits pre-synaptic release of acetylcholine
Blocks post-synaptic receptor

 

Reversible with calcium gluconate

Term
What Spectinomycin is used for and its MOA
Definition

For Gonorrhea where you can't use penicillins

 

30S ribosome, protein synthesis inhibitor

Term
What drug class has a Hydronaphthacene nucleus?
Definition
Tetracyclines
Term
MOA of Tetracyclines (against bacteria)
Definition
bind the 30S ribosome and block tRNA binding (so prevent elongation)
Term
Tetracyclines are effective against ___
Definition

Nearly everything

 

CAN WORK INTRACELLULAR (Broad spectrum -gram positive, gram negative, aerobes/anaerobes, spirochetes,  mycoplasma, rickettsia, chlamydia)

Term
Tetracycline and oxytetracycline are ___ acting tetracyclines
Definition
short acting (6hr)
Term
Demeclocycline is a ___ acting tetracyclines
Definition
intermediate (12 hr)
Term
Doxycycline and Minocycline are ___ acting tetracyclines
Definition
Long acting (up to 24 hr)
Term
List the possible toxicities of Tetracyclines (9, with 4 main ones)
Definition

- Rash/photosensitivity

- poor bone growth

- discolor teeth

- not for pregnancy

- esophageal ulcers

- superinfection

- fatty liver/necrosis

- azotemia

- benign intercranial hypertension

Term
A specific toxicity that can be caused by demeclocycline
Definition
photosensitivity rash
Term
Give a specific toxicity that can be caused by taking IV chlortetracycline in pregnancy
Definition
Fatty liver, necrosis
Term
name a toxicity that Minocycline can cause
Definition
Benign intercranial hypertension w/ vertigo
Term
What drugs tetracyclines interact with (2)
Definition

Food, minerals, antacids

+

Anticonvulsants (make tetracycline less effective)

Term
6 examples of diseases to use Tetracyclines in
Definition

Community acquired pneumonia & Atypical pneumonia

Genital Chlamidya, PID

MRSA

Leptospirosis

Malaria

Syphilis

Term
Glycylcycline is active against ___ (4)
Definition

– Most Enterobacteriaceae
– Bacteroides
– Staphylococcus aureus

- Streps

Term

Give the MOA of Glycylcycline

+

Where it doesn't go to in the body

Definition

Binds the 30S ribosome subunit of bacteria, blocking tRNA

 

stays out of blood, can't use for bacteremia

Term
4 diseases that Glycylcycline is approved for (assuming penicillin cannot be used)
Definition
Complicated skin, skin structure, or intra-abdominal infection, or community acquired pneumonia
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