inhibitors of protein synthesis Flashcards

1
Q

name the eye ointment name of tetracyclines

A

terramycin

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2
Q

why are they called “tetracyclines”?

A

they are called tetracyclines because they have 4 rings that are fused to each other. in addition to this they have 4 R groups that impart activity to the structure.

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3
Q

what is the MOA of tetracyclines

A

they enter by passive diffusion and an energy dependant transport protein. they bind reversibly to the 30 S subunit of bacteria thereby inhibiting bacterial protein synthesis

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4
Q

name the tetracycline drugs

A

tetracycline capsules 250 mg
oxytetracycline terramycin eye ointment
doxyclycline doxydar capsules 200 mg and IV injection
minocycline minocin capsule 100,200 mg and IV injection

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5
Q

tetracyclines should not be taken with specific products? name them and give reason why?

A

tetracyclines should not be taken concomitantly with
dairy products, aluminium and magnesium antacids or iron preparations because it decreases the absorption of tetracyclines due to formation of non absorbable chelates.

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6
Q

describe the absorption of tetracyclines

A

they are absorbed adequately but incompletely orally

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7
Q

tetracyclines should be administered

a. with food
b. without food

A

b. without food

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8
Q

where do tetracyclines concentrate

A

in the liver, kidneys, spleen, skin and tissues undergoing calcification (teeth and bone)

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9
Q

do tetracyclines enter the CSF

A

yes but in inadequate therapeutic concentrations

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10
Q

do tetracyclines cross the placental barrier, where do they concentrate in foetus

A

yes, they concentrate in the fetal bone and dentition

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11
Q

how are tetracyclines excreted

A

they are secreted in the bile. reabsorbed in the intestine and excreted in the urine by glomerular filtration

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12
Q

which tetracycline would you recommend to a patient with compromised renal function and why? name the component excreted.

A

recommend doxycycline because it is preferentially excreted in bile via feces.
doxycycline glucoronide

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13
Q

only ____________ provides therapeutic concentrations in the CSF.

A

minocycline

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14
Q

any organism resistant to one tetracycline is resistant to all. true or false

A

true

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15
Q

give 2 reasons for resistance to tetracyclines?

A

inability of the drug to accumulate due to the R factor, energy dependant efflux pumps
enzyme modification of tetracycline binding site

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16
Q

what are the adverse effects of tetracyclines

A
GI disturbance 
staining of teeth 
hyperplasia 
bone deformities 
fatal hepatotoxicity 
phototoxicity
superinfection
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17
Q

what are the CI of tetracyclines

A

pregnant women
first trimester : abnormal skeletal development of baby
2nd and 3rd trimester ; dental discolouration and maternal hepatotoxicity
lactating females : drug may pass to baby via breast milk leading to dental discolouration and abnormal skeletal development
renally impaired patients except doxyclycline
children under 8 yrs : dental discolouration and abnormal skeletal development

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18
Q

name the aminoglycoside drugs

A
  1. streptomycin (streptomycin sylfate injection)
  2. trobramycin (nebcin injection)
  3. netromycin/netilmicin (netromycin sulfate injection)
  4. neomycin (neomycin and bacitracin cream)
    neospora ( gramicidin + neomycin) eye drops
  5. amikacin (amikin) injection
  6. gentamycin, genticin ear and eye drops, garamycin sulfate inj. and garamycin eye drops
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19
Q

aminoglycosides have been the mainstays of treatment for?

A

the serious infections caused by aerobic gram negative bacilli.

20
Q

aminoglycosides have a broad therapeuic index. true or false?

A

false. they have a narrow therapeutic index

21
Q

why are aminoglycosides rarely used

A

due to their serious toxicities

22
Q

aminoglyclosides are now replaced with :

a. vancomycin, bacitracin, penicillins
b. 3rd gen cephalosporins. fluroquinolones, imipenem/cilastatin
c. imipenem, cilastain, penicillins

A

b. 3rd gen cephalosporins, fluoroquinolones and imipenem/cilastatin

23
Q

what is the MOA of aminoglycosides

A

aminoglycosides bind to the 30S ribosomal subunit leading to

a. inhibition of the initiation of protein synthesis
b. misreading of mRNA leading to abnormal proteins. or premature chain termination

24
Q

aminoglycosides are

a. bacteriostatic
b. bactericidal

A

b. bactericidal

25
Q

why do aminoglycosides not work against anaerobic micro organisms?

A

because anaerobes do not have an O2 dependant carrier system. susceptible organisms have an oxygen dependant system that tranports the antibiotic across the cell membrane.

26
Q

what is the synergistic relationship between aminoglycosides and beta lactam?

A

beta lactam destroys the cell wall allowing aminoglycosides to enter and inhibit protein synthesis

27
Q

what are the typical therapeutic indications of aminoglycosides

A

enterococcal infections : gentamycin/stretomycin + vancomycin/ other beta lactam
psuedomonas infection : tobramycin alone or tobramycin + antipseudomonal penicllin eg. piparcillin

28
Q

name the macrolides

A
  1. erythromycin
    erythrocin tablets, erythrocin syrup, erythromycin injection
  2. clarithromycin, klacid tablets, klacid powder for suspension
  3. azithromycin, zithromax capsules, zithromax oral suspension
29
Q

what is MOA of macrolides

A

they act by binding irreversibly to the 50 S subunit of bacterial ribosome and inhibiting the translocation step of bacterial protein synthesis

30
Q

name the therapeutic indications of erythromycin

A

Used in oral infections, urethritis, respiratory tract diseases (including Legionella), skin infections, chronic prostatitis, diphtheria prophylaxis and carrier state, acne vulgaris.

31
Q

clarithromycin is additional active against which organisms?

A

H. influenzae and intracellular pathogens such as chlamydia. legionella and ureaplasma

32
Q

_____________ is used as treatment in H.pylori eradication regimen.

A

clarithromycin

33
Q

azithromycin is not as effective as erythromycin against ________ and _________.

A

streptococci and staphylococci

34
Q

if the bacteria is resistant to erythromycin, can we administed azithromycin/clarithromycin? why?

A

no because Both azithromycin and clarithromycin show cross resistance with erythromycin

35
Q

name the adverse reactions of macrolides

A

epigastric distress
cholestatic jaundice
ototoxicity (transient)

36
Q

what happens when azithromycin and clarithromycin eliminate the intestinal flora?

A

the intestinal flora that inactivates digoxin is eliminated hence this leads to digoxin toxicity.

37
Q

describe the MOA of chloramphenicol

A

binds reversibly to 50S ribosmal unit of bacteria and inhibits peptidyltransferase enzyme

38
Q

why does chloramphenicol cause bone marrow toxicity at high doses?

A

this is due to the similarity between the organelles and due to inhibition of mitochondrial protein synthesis

39
Q

describe the antibacterial spectrum of chloramphenicol

A

Broad spectrum, effective against bacteria and other microorganisms including anaerobes (except chlamydia and pseudomonas)

40
Q

describe the resistance towards chloramphenicol

A
  1. inability of the antibiotic to penetrate the enzyme

2. prescence of an enzyme that inactivates chloramphenicol

41
Q

what are the adverse reactions of chloramphenicol

A
Hemolytic anemia in G6PD deficient patients
Reversible anemia (dose related)
Aplastic anemia (dose independent)
hepatic enzyme inhibition 
gray baby syndrome
42
Q

why does gray baby syndrome occur with chloramphenicol?

A

Occurs due to inability of the baby to glucuronidate chloramphenicol effectively if doses were miscalculated.

43
Q

describe the MOA of clindamycin

A

They act by binding irreversibly to the 50S ribosomal subunit of bacterial ribosomes inhibiting the translocation step in bacterial protein synthesis.

44
Q

describe the therapeutic indications of clindamycin

A

Used in bone and joint infections, peritonitis and endocarditis prophylaxis
infections caused by Bacteroides fragilis
in acne caused by Propionibacterium acnes
dental infections or prophylaxis prior to dental procedures

45
Q

clostridium difficile is resistant to clidamycin. this might cause _____________.

A

pseudomembranous colitis

46
Q

what is the resistance mechanism of clindamycin

A
  1. inability of the antibiotic to penetrate organism.
  2. decreased affinity for 50 s ribosomal subunit.
  3. plasmid associated synthesis of esterase enzyme.