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The Public (Y2) > Inhibitors of protein synthesis > Flashcards

Inhibitors of protein synthesis Flashcards

1
Q

Protein synthesis must continue even when cells are dormant. True or false?

A

True

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2
Q

Which drug is biosynthesised from acetate by several species of streptomyces?

A

Tetracycline

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3
Q

Tetracycline binding to nucleic acid inhibits cellular function. True or false?

A

False - only ribosome binding does

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4
Q

Tetracycline is contraindicated in children. Why?

A

Stain tooth enamel

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5
Q

Oxytetracycline is used to treat conjunctivitis in cats. True or false?

A

False - used to treat acne

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6
Q

Which tetracycline is used to treat lyme disease?

A

Demeclocycline

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7
Q

Which tetracycline is an antibacterial also used in prophylaxis of malaria?

A

Doxycycline

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8
Q

Minocycline is broader spectrum than other tetracyclines and can treat Neisseria meningitidis. True or false?

A

True

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9
Q

Streptomycin, gentamycin, kanamycin and neomycin belong to which group of drugs?

A

Aminoglycosides

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10
Q

Which ribosomal subunit does streptomycin bind?

A

30S

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11
Q

Aminoglycosides are active against gram negative bacteria. True or false?

A

True

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12
Q

Aminoglycosides show nephrotoxicity. True or false?

A

True

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13
Q

Gentamicin is derived from streptomyces. True or false?

A

False - derived from micromonospora

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14
Q

Which aminoglycoside binds to both ribosomal subunits, preventing them combining?

A

Tobramycin

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15
Q

Amikacin is arrived from which other aminoglycoside?

A

kanamycin

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16
Q

Paramomycin is used to treat a protozoal infection. Which ribosomal subunit does is interact with?

A

30S

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17
Q

What is the name of the only clinically available oxazolidinone?

A

Linezolid

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18
Q

Linezolid is not active against MRSA. True or false?

A

False

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19
Q

Linezolid is used against hospital acquired gram positive infections. True or false?

A

True

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20
Q

Which ribosomal subunit does linezolid bind to?

A

50S

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21
Q

Linezolid is toxic to mitochondria. True or false?

A

True

22
Q

What is the soil bacterium that produces erythromycin?

A

Saccharopolyspora erythraea

23
Q

Structure of erythromycin A is based on proprionate. True or false?

A

True

24
Q

In what way are the structures of erythromycin and tetracycline similar?

A

both polyketides

25
Q

Erythromycin is a macrolide. True or false?

A

True

26
Q

Macrolides are first-line treatment in patients that are allergic to ______

A

penicillin

27
Q

Macrolides are gut motilide agonists. What is meant by this?

A

Sensitised patients find that erythromycin and food do not sit well - taste and bitter is foul and cannot be masked

28
Q

Macrolides give rise to a number of DDI. What is the reason for this?

A

They are metabolised by CYP450 3A4 in the liver

29
Q

What is the mode of action of erythromycin?

A

Blocks protein synthesis after several rounds and oligopeptides are released from the ribosome.
It blocks the exit tunnel of the bacterial ribosome

30
Q

What is the paediatric erythromycin that is used called and how does it work?

A

Erythromycin ethyl succinate - taste-free prodrug which hydrolyses in the blood.

31
Q

Paediatric erythromycin needs to be stored in the fridge. True or false?

A

True - hydrolyses in the bottle

32
Q

Are second generation macrolides more or less stable than erythromycin A?

A

More stable - so better in the stomach

33
Q

Second generation macrolides are more hydrophilic than erythromycin A. True or false?

A

False - more hydrophobic

34
Q

What is the half life of clarithromycin at pH 2.5 and 37 degrees?

A

310 mins

35
Q

What is the half life of erythromycin at pH 2.5 and 37 degrees?

A

<10 mins

36
Q

What is the only ketolide that is clinically used at the moment?

A

Telithromycin

37
Q

What are some mechanisms of macrolide resistance?

A

Modification of ribosomal proteins
Efflux pumps, pumping macrolides out of cell
Methylation of adenine 2058 in 23S RNA

38
Q

Chloramphenicol is only used to treat gram positive bacteria. True or false?

A

False - gram positive and gram negative

39
Q

How many chiral centres does chloramphenicol have?

A

2 - but only one is active

40
Q

Why is chloramphenicol not usually given internally and how is it mainly given?

A

Because it can cause aplastic anaemia.

It is typically found in eye drops

41
Q

Of the four possible stereoisomers of chloramphenicol, how many are active?

A

One

42
Q

Lincomycin is a natural product. True or false?

A

True

43
Q

How is resistance to lincomycin and clindamycin induced?

A

Methylation of adenine 2058 in 23S RNA - so assumed that mode of action is similar to macrolides

44
Q

Clindamycin is generally superior to lincomycin. True or false?

A

True

45
Q

Clindamycin can be used to treat both aerobic and anaerobic infections. True or false?

A

True

46
Q

Clindamycin is used in the treatment of toxic shock syndrome, often in combination with ________

A

vancomycin

47
Q

Fusidic acid is a fungal product. True or false?

A

True

48
Q

Fusidic acid is used to treat gram negative infections. True or false?

A

False - gram positive

49
Q

Fusidic acid is most commonly seen in eye drops. It cannot be given as tablets. True or false?

A

False - can be given as tablets

50
Q

What is the mode of action of fusidic acid?

A

Binds to EFG.GTP
the ternary complex binds to ribosome as normal
GTP is hydrolysed EFG.GDP is unable to leave the ribosome and protein synthesis is therefore stalled

The Public (Y2) (35 decks)

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