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Block 1.11 Lees Stuff > Antibacterial Agents Targeting Protein Synthesis > Flashcards

Antibacterial Agents Targeting Protein Synthesis Flashcards

1
Q

What is the Post-Antibiotic effect (PAE)?

A

If a drug has PAE it means that even after the bacteria has been exposed it will continue to kill it off.

Concentration of the drug is going down but you still get effects of that drug

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2
Q

Which drugs bind at the 50s at the beginning of protein synthesis?

A

Oxazolidinones

Linazoid (Zyvox)

Tediozide (Sivextro)

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3
Q

Where do tetracycline bind>

A

On 30s which block tRNA binding

Doxycycline

Minocycline

Tigecycline

Eravacycline

Omdacycline

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4
Q

Where does chloramphenicol bind ?

A

It binds at the 50s and blocks peptide chain transfer

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5
Q

Where does Clindamycin and macrolides bind?

A

50s at the end and block translocation

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6
Q

Where do aminoglycosides bind?

A

30s at the end

Blocks translocation

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7
Q

What to know about clindamycin

A

Good oral bio = 90%

Lincosamide

No PAE

Bacterodies activity, CA MRSA, Aspiration pneumonia, Skin and soft tissue, acne, bacterial vaginosis

Cleared in RENAL and bile

No CYP3A4

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8
Q

What are the Macrolides?

A

Azithromycin (Zithromax)

Clarithromycin (Biaxin)

Not so good oral bioavailability

LIVER CYP3A4!!!!! Very big inhibitors have to watch for drug interactions (clarithromycin)

has PAE effects

Works on Atypicals

Has really big ring structure

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9
Q

What is important to note about clindamycin and drug resistance

A

It can create its own drug resistance

You must do the D-TEST which uses erythromycin to see if it is isolated to CA MRSA

Positive = can not use clindamycin

Negative = you can use

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10
Q

What is erythromycin used for when you see it in pharmacy?

A

Typically it will not be as an antibiotic but will be used in order to induce diarrhea

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11
Q

What is important to note about the half-life of azithromycin?

A

It is very long!

Serum = 60-70 hours

Intracelluar = 2-3 weeks!

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12
Q

What are the side effects of Clindamycin?

A

GI= N/V

BIG IN DIARRHEA and CDAD!!!!

Hepatotoxic

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13
Q

What are the side effects of Azithromycin and clarithroymcin

A

GI= N/V

Does cause moderate diarrhea (not as bad as clindamycin)

Does does CDAD but not near as bad as clindamycin

Hepatotoxic

These give QTc prolongation!!!! Clari is worse

Also have to watch for CYP3A4 interactions!!!! (They are inhibitors)

Clarithromycin is really bad at this!!!

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14
Q

What are the uses for Macrolides?

A

Azithromycin (Zithromax)

Clarithromycin (Biaxin)

Atypicals

CA acquired pneumonia

COPD exacerbation

Sinusitis

Some mycobacterial infections

Azithromycin = travelers diarrhea

H. pylori = clarithromycin

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15
Q

What is the route for the aminoglycosides?

A

They are only given IV

Tobramcyin

Gentamicin

Amikacin

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16
Q

How is the distribution of the aminoglycosides?

A

It’s poor, DOES NOT get into the CNS and the lungs!

Also it does have a PAE effect where it works even after the concentration has fallen off

***when given n the hospital the pharmacist will also choose the dose that is needed for the pt

17
Q

What do Aminoglycosides work against?

A

ONLY WORKS FOR GRAM NEGATIVE AEROBES!!!

** includes PSEUDOMONAS and ACINETOBACTER

Gentamicin**
Can be good with beta lactam or Vanco for MRSA and MSSA for endocarditis

18
Q

What are the side effects for Aminoglycosides?

A

Gentamycin

Tobramycin

Amikacin

Nephrotoxicity

Ototoxicity

19
Q

What is the clinical pearl when using this drugs (when would you use these) Aminoglycosides?

A

You would use gentamicin and tobramycin first

But they are already later choice drugs that are only brought out if resistance is a problem!!

Amikacin would be you last chance drug if the bacteria is resistant to genta and tobramycin

20
Q

What are the tetracycline and what is their MOA?

A

Minocycline (minocin)

Doxycycline

It binds to the 30s subunit and prevents tRNA from binding

The structure has 4 rings back to back

21
Q

What are the new agents of tetracyclines?

A

Omadacycline

Eravacycline

Tigecycline

**these drugs are used held off on because these you only use when a bacteria has MDR. So you must avoid it unless really needed

22
Q

What are the pharmacokinetic considerations when it comes to the tetracyclines?

A

Doxycycline and Minocycline

Very good oral, has good distribution EXPECT the CNS

Metabolism is in the liver (none-CYP3A4)

Eliminated in the bile and thro feces

New agents:

Same as above but the oral bioavailability for omadacycline is really poor. Around 35%

23
Q

What are some drug interactions when it comes to the tetracyclines

A

Doxycycline, minocycline, omadacycline, tigecycline, eravacycline

Have to watch for cations of magnesium and calcium (milk, and antacids)

**these will cause it to bind and form participates which effect the absorption of the drug

24
Q

What are the clinical uses for Doxycycline and Minocycline?

A

Atypical bacteria

  • CA pneumonia
  • STD - Chlamydia

COPD exacerbation

Sinusitis

Skin and soft-tissue infection (cellulitis)

Acne

Spirochete diseases

Bioterrorism

Malaria prophylaxis

25
Q

When would you use the new type of tetracyclines?

A

They are not first line agents and will only be used if there is a MDR bacteria that you needed to work on

26
Q

What are the warnings / adverse effects of Doxycyline and minocycline? And the new ones!

A
  1. GI upset
  2. Esophageal irritation- drink with H20!!
  3. N/V
  4. Diarrhea
  5. CDAD
  6. Pancreatitis and Liver toxicity!!!!!!!!
  7. Tissue and bone discoveration as well as inhibitor of bone growth (CAN NOT GIVE TO CHILDREN)!! (It can sit inside the bones and cause issues later on in life for kids)
  8. Photosensitivity - watch out for sun exposure these two are quite prone for this
  9. Psuedotumor cerebri (increased intracranial pressure (rare))
  10. Infection site rxn/ phebilitis (buring in veins)

The new ones cause increase in N/V and infusion rxns

27
Q

What are the oxazolidinones and their MOA?

A

Linezolid (Zyvox)

Tedizolid (Sivextro)

MOA: they block the 50s subunit at the start of the process and prevent the two from binding together

28
Q

What are the Pharmacokinetics of the Oxazolidinones?

A

Linezolid (Zyvox) and Tedizolid (Sivextro)

They have good bioavailability (90-100%)

***HAVE MAO-INHIBITOR ACTIVITY!!! Linezolid more so than tedizolid but must watch for interaction of these when taking antipsychotics!!!!

29
Q

What are the clinical uses for Oxazolidinones?

A

Linezolid (Zyvox) and Tedizolid (Sivextro)

Used for gram (+) bacterial infections!!!
Can be used for everything!!! Including up to VRE!!!!!

CAN NOT BE USED FOR BACTERMIA ( infection of the blood)!!

**these will be used for gram (+) that has MDR

30
Q

What are the adverse effects for the Oxazolidinones?

A

Linezolid (Zyvox) and Tedizolid (Sivextro)

generally well-tolerated

But can cause Bone marrow suppression - thrombocytopenia

Also when used for a long time must watch for Peripheral Neurophathy!!!! (When used for months!!!!!!)

WATCH FOR MAO-INHIBITORS!!!!!!! - do not use for those things!!!

31
Q

What is Chloramphenicol (include MOA and pharmacokinetics)

A

It is not used in the US

MOA: Block peptide chain transfer by binding to the 50s subunit of the bacterial ribosome

Pharmacokinetics:
Good bioavailability (75-90)
Gets excreted not thro kidney and non-fecal

32
Q

What are the chloramphenicol adverse effects?

A
  1. Hypersensitivity rxn (rash, hives (urticaria) and anaphylaxis
  2. Aplastic anemia
    • Agranulocytosis (loss of granulocytes, macro neutrophils)
  3. Gray baby syndrome (in newborns)
  4. Altered mental status
  5. Leukemia

These bad effects are why this drug is not used in the US.

Block 1.11 Lees Stuff (5 decks)

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