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Pharmacology > Exam 2: Inhibitors Of Protein Synthesis 1 > Flashcards

Exam 2: Inhibitors Of Protein Synthesis 1 Flashcards

1
Q

What are the types of antibiotics that are inhibitors of protein synthesis? (7)

A 
Macrolides
Ketolides
Clindamycin
Streptogramins
Oxazolidinones 
Aminoglycosides 
Broad spectrum antibiotics
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2
Q

What are the two inhibitors of protein synthesis that bind to the 30s subunit of the ribosome?

A

Aminoglycosides and tetracyclines

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3
Q

What are the inhibitors of protein synthesis that bind to the 50s subunit?

A

Macrolides, chloramphenicol, Lincosamides, Oxaolidinones, and strepogramins

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4
Q

What are the 3 macrolides and what are their routes of administration?

A

Erythromycin- Oral, IV

Clarithromycin- Oral

Azithromycin (Zithromax) - Oral, IV

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5
Q

What bacteria do the macrolides work best on?

A

G+

Bacteriostatic, great choice for immune competent person with allergy to pencillins.

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6
Q

How does resistance to macrolides occur?

A
  • Efflux pumps

- Methylation of drug binding site so antibiotic cannot bind.

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7
Q

What is the DOC for chlamydia trachomotis or C pneumoniae?

A

Macrolides (Erythromycin, Clarithromycin, Azithromycin)

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8
Q

What is the DOC for Mycoplasma pneumoniae and Legionella Species?

A

Macrolides (Erythromycin, Clarithromycin, Azithromycin)

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9
Q

The majority of G- organisms are resistant to what macrolide?

A

Erythromycin

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10
Q

What are the main side effects of macrolides?

A

QT prolongation (torsades), Drug interactions with CYP34A drugs, and GI disturbances (mainly diarrhea)

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11
Q

Which macrolides has the most and which has the least adverse GI effects?

A

Clarithromycin has the least, erythromycin has the most

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12
Q

Erythrymycin is a potent inhibitor of ***.

A

CYP34A- this means it inhibits the hepatic metabolism of other drugs that require CYP34A, increasing their serum concentrations and potentially causing toxicity

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13
Q

What kind of drug is Telithromycin and how does it work?

A

A ketolide- binds tightly to two sites of ribosomal DNA and blocks bacterial protein synthesis

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14
Q

What site of the ribosome does telithromycin bind to?

A

50s

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15
Q

What bacteria is telihromycin effective against?

A

Broad spectrum. Bacteriostatic.
Good against respiratory pathogens including erythromycin and penicillin resistant pneumococci.
-Also has activity against intracellular and atypical bacteria

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16
Q

How is telithromycin taken?

A

Orally

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17
Q

Why was the approval for telithromycin on URIs withdrawn?

A

Serious hepatotoxicity was reported and the benefits of the medicine no longer supported the risks.

It remains on the marker for CAP, but not the first choice

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18
Q

How is telithromycin metabolized?

A

Hepatic cytochrome p450 isoenzymes, primarily CYP34A

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19
Q

How is Clindamycin adminstered?

A

Oral, parenteral, or topically

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20
Q

What bacteria is Clindamycin effective against?

A

A wide range of aerobic G+ cocci as well as several anaerobic G- and G+ organisms.

21
Q

Is Clindamycin bactericidal or bacteriostatic?

A

Either, depending on its concentration at the site of action and the susceptibility of the organism

22
Q

How is Clindamycin metabolized and excreted?

A

Metabolized by the liver, minimally excreted by the kidneys

23
Q

How is toxic shock syndrome treated?

A

Clindamycin in addition to Vancomycin, Nafcillin, or a first generation cephalosporin

24
Q

What is used to treat osteomyelitis and why?

A

Clindamycin because it obtains high concentrations in bones

25
Q

Clindamycin is a well known cause of what disease?

A

Pseudomembranous colitis, an overgrowth of C. Diff.

26
Q

If symptoms of a C. Diff infection arise while patient is taking Clindamycin, what should you do?

A

Immediately stop Clindamycin use and initiate Vancomycin treatment

27
Q

What are the two types of Streptogramins?

A

Dalfopristin and Quinupristin

28
Q

How does Dalfopristin work?

A

Binds to the 50s ribosomal particle and inhibits the early phase of protein synthesis

29
Q

How does Quinupristin work?

A

Bind to the 50s subunit and inhibits late phase of protein synthesis

30
Q

What happens wen dalfopristin and Quinupristin are administered together vs alone?

A

Together, they appear to act synergistically against susceptible bacteria and their effect is bactericidal

Alone they are bacteriostatic.

31
Q

What bacteria are dalfopristin and Quinupristin effective against?

A

Aerobic G+ including penicillin resistance S. pneumoniae, MDR streptococci, skin infections due to MSSA or MRSA, and VRE

32
Q

How are Dalfopristin and Quinupristin administered?

A

IV infusion

33
Q

What are the adverse reactions of Dalfopristin and Quinupristin?

A

Hepatotoxicity, nausea, vomiting, rash

- inhibits the P450 drug metabolizing system

34
Q

What are the contraindications of Dalfopristin and Quinupristin?

A

Breast feeeding, children, hepatic disease, pregnancy, and streptogramin sensitivity

35
Q

What class of drug is Linezolid?

A

Oxaxolidinones

36
Q

What bacteria is Linezolid effective against?

A

Predominately aerobic G+ organisms.

This is not a drug of first resort

37
Q

What is the MOA of Linezolid?

A

Prevents to the formation of a functional 70s subunit initiation complex.

  • Linezolid is a reversible, nonselective inhibitor of MAO.
  • Bacteriostatic, except cidal for streptococci
38
Q

What can overuse of Linezolid lead to?

A

It can speed up selection of resistant strains and lead to loss of use for this antibiotic

39
Q

What infections is Linezolid approved for?

A

Bacterial PNA, skin and skin structure infections, VRE infections, and MRSA

40
Q

How is Linezolid administered?

A

IV infusion or oral (oral bioavailability is 100%)

41
Q

How is Linezolid metabolized?

A

Oxidation but the oxidative metabolism of Linezolid is non-enzymatic and does not require the hepatic microsomal oxidative system

42
Q

What are the adverse reactions of Linezolid?

A

Diarrhea, headache, N/V, insomnia, constipation, possible superinfection, and the usual side effects and interactions as MAO inhibitors.

43
Q

What are the contraindications of Linezolid?

A

Hypersensitivity and pheochromocytoma (tumor in adrenal medulla that can lead to increased EPI, NE, and serotonin)

44
Q

Who should you never prescribe Linezolid to?

A

Someone who is on antidepressants such as SSRIs -this can lead to serotonin toxicity

45
Q

What the is the spectrum of clarithromycin?

A

Very similar to erythromycin, but clarithromycin is more active against Mycobacterium Adium complex (MAC), Mycobacterium leprae, and toxoplasma Gondii

46
Q

Out of the 2 macrolides, which is most likely to cause QT prolongation?

A

Azithromycin

47
Q

Out of the 3 macrolides, which has the most drug interactions?

A

Clarithromycin

48
Q

Are the macrolides bactericidal or bacteriostatic?

A

Bacteriostatic

Pharmacology (25 decks)

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