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MODULE TITLE: Introduction to Medicine

MODULE CODE: BM-IM 401/1


SPECIFIC TOPIC TITLE: P’cology of Antimicrobial drugs – Protein Synthesis
Inhibitors (PSIs)—Review Questions

P’cology of Antimicrobial Drugs—Protein Synthesis


Inhibitors—Review Questions
1) List the drugs belonging from the antimicrobial drugs that inhibit protein
synthesis

P’cology of Tetracyclines(TTCs) & Glycylcycline


1) List the drugs belonging to tetracyclines (TTCs).

2) Describe the details of mechanism of action of TTCs.

3) Which two resistance mechanisms is the most important mechanism for TTC
resistance?

4) Which microbes expressing the following resistance mechanism?

 Tet(A-E) ---Efflux pump ______________________

 Tet(K) ---Efflux pump ___________________________

 Tet(M) ---Expressed ribosomal protection protein___________

 MDR--- efflux pump _____________________

5) Which TTC drugs are resistant in microbes expressing the following resistance
mechanism?

 Tet(A-E) ---Efflux pump___________________________

 Tet(K) ---Efflux pump _____________________________

Review Questions –Protein Synthesis Inhibitors (PSIs) -–By Endalk Gebrie ( B.


Pharm & MSc)-- Y12HMC-- Feb. 2023
Page 1
MODULE TITLE: Introduction to Medicine
MODULE CODE: BM-IM 401/1
SPECIFIC TOPIC TITLE: P’cology of Antimicrobial drugs – Protein Synthesis
Inhibitors (PSIs)—Review Questions

 Tet(M) ---Expressed ribosomal protection protein_________________________

 MDR ---Efflux pump ____________________________

6) Which TTC drugs are useful in the treatment of microbes expressing the
following resistance mechanism?

 Tet(A-E) ---Efflux pump _____________________

 Tet(K) ---Efflux pump _________________________

 Tet(M) ---Expressed ribosomal protection protein___________________

 MDR ---Efflux pump __________________________

7) Which two TTC drugs have an excellent bioavailability compared to other TTCs?

8) Which factors decrease oral absorption of TTCs and Why?

9) Which TTCs have adequate distribution to CSF?

10) Which TTC drug serum concentration decrease up to 50% by strong enzyme
inducers?

11) Which TTC drug do not need dose adjustment in renal impairment?

12) Classify TTCs based on duration of action and provide at least two drugs from
each class.

13) Discuss the adverse effects of TTCs mediated by direct effect on the GIT
mucosal tissues and on the microbes.

Review Questions –Protein Synthesis Inhibitors (PSIs) -–By Endalk Gebrie ( B.


Pharm & MSc)-- Y12HMC-- Feb. 2023
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MODULE TITLE: Introduction to Medicine
MODULE CODE: BM-IM 401/1
SPECIFIC TOPIC TITLE: P’cology of Antimicrobial drugs – Protein Synthesis
Inhibitors (PSIs)—Review Questions

14) What is the effect of TTCs on the teeth and bones? Provide mechanism of this
effect?

15) TTCs are contraindicated for pregnant mother, children (<8yrs) & nursing
mothers. Why?

16) TTCs are drug of choice for treatment of which microbes’ infection?

17) Discuss the clinical applications of TTCs other than the above mentioned
infections.

18) Though tigecycline has similar mechanism of action to TTCs it is quite effective
and used in the treatment of TTC resistant strains (producing efflux pump &
ribsomal protection). Why?

19) Tigecycline has no value in the treatment of UTIs & blood infection. Why?-

20) Which organ dysfunction decrease excretion of tigecycline? Liver or renal?

21) Which adverse effect of tigecycline is fatal?

P’cology of Macrolides & Ketolide


22) List the drugs belong to macrolide antibiotic.

23) Describe and illustrate the mechanism of action of macrolides.

24) Which protein synthesis inhibitors compute with the same receptor with
macrolides?

25) Elaborate the microbes resistance mechanism for macrolides antimicrobial


actions.

Review Questions –Protein Synthesis Inhibitors (PSIs) -–By Endalk Gebrie ( B.


Pharm & MSc)-- Y12HMC-- Feb. 2023
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MODULE TITLE: Introduction to Medicine
MODULE CODE: BM-IM 401/1
SPECIFIC TOPIC TITLE: P’cology of Antimicrobial drugs – Protein Synthesis
Inhibitors (PSIs)—Review Questions

26) What does MLS-type B resistance stands for? Which enzyme induced with this
type of resistance?

27) Which adverse effect of erythromycin is used for treatment of gastroparesis or


postoperative ileus?

28) Which salt form of erythromycin associated with acute cholestatic hepatitis?

29) Macrolides are known CYP inhibitor. Provide at least three drug whose serum
concentration increase significantly.

30) Which macrolide is relatively safer to combine with other drugs because it is
free from drug interaction or CYP inhibition?

31) What is the difference between erythromycin and azithromycin in terms of


antimicrobial spectrum of actions?

32) Which macrolide antibiotics need caution/dose modification in the presence of


renal impairment?

33) Which pharmacokinetic properties permit azithromycin once daily dosing &
shorter duration of treatment in most infections?

34) Which agent is congener of macrolide and has the sugar l-cladinose substituted
with 3-keto group?

35) Though telithromycin has almost similar spectrum of action & MAO to
macrolide but it is effective for the treatment of macrolide resistance strains.
Why?

36) What would be the reason for now a days telithromycin use limited to CAP?

Review Questions –Protein Synthesis Inhibitors (PSIs) -–By Endalk Gebrie ( B.


Pharm & MSc)-- Y12HMC-- Feb. 2023
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MODULE TITLE: Introduction to Medicine
MODULE CODE: BM-IM 401/1
SPECIFIC TOPIC TITLE: P’cology of Antimicrobial drugs – Protein Synthesis
Inhibitors (PSIs)—Review Questions

37) Compare and contrast erythromycin, clarithromycin, azithromycin and


telithromycin in terms of the following pharmacokinetic parameters.

 Oral absorption ----------


 T1/2 (Hrs) ---------------
 Active metabolites--------------
 CYP inhibition----------------
 Excretion in the urine------------
 Dose adjustment in renal failure-----
 Caution in hepatic dysfunction ---

P’cology of Clindamycin
38) Discuss the mechanism of actions and resistances of clindamycin.

39) Which microbes are intrinsically resistant to clindamycin?

40) What is the reason for clindamycin not used in the treatment of UTIs?

41) A patient taking clindamycin for soft tissue infection suffered from bloody
diarrhea. What microbes cause the bloody diarrhea? Which two drugs are
commonly used to treat this predominate microbes?

42) Which infection treated with clindamycin in combination with primaquine?

43) Which infection treated with clindamycin in combination with pyrimethamine?

44) Which infection treated with clindamycin in combination with quinine?

45) Discuss other clinical uses of clindamycin.

Review Questions –Protein Synthesis Inhibitors (PSIs) -–By Endalk Gebrie ( B.


Pharm & MSc)-- Y12HMC-- Feb. 2023
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MODULE TITLE: Introduction to Medicine
MODULE CODE: BM-IM 401/1
SPECIFIC TOPIC TITLE: P’cology of Antimicrobial drugs – Protein Synthesis
Inhibitors (PSIs)—Review Questions

P’cology of Chloramphenicol(CAF)
46) What is the mechanism of actions of CAF?

47) Which microbial enzyme induction produces clinically important resistance to


CAF?

48) It is known that CAF causes hematologic toxicity and even because of this
adverse effect most authorities limit the use of CAF for serious infection. Discuss
these hematologic toxicities.

49) High dose of CAF for new born infants or above the recommended dose for
premature infants associated with adverse effect called Gray Baby Syndrome.
Describe the clinical presentation of gray baby syndrome and provide a reason
for why this happens in infants?

50) In general protein synthesis inhibitors such as CAF with the exception of
aminogycosides has antagonistic interaction with penicillins or bactericidal
agents. Why?

51) Provide at least 4 clinical conditions in which CAF is appropriate to be used.

P’cology of Streptogramins
52) Quinupristin (Streptogramin B) & Dalfopristin (Streptogramin A) are individually
bacteriostatic but when used in combination they are bactericidal. Why? Explain
your answer mechanistically.

53) Which resistance mechanism is responsible for the loss of efficacy of


quinupristin?

Review Questions –Protein Synthesis Inhibitors (PSIs) -–By Endalk Gebrie ( B.


Pharm & MSc)-- Y12HMC-- Feb. 2023
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MODULE TITLE: Introduction to Medicine
MODULE CODE: BM-IM 401/1
SPECIFIC TOPIC TITLE: P’cology of Antimicrobial drugs – Protein Synthesis
Inhibitors (PSIs)—Review Questions

54) Which microbial enzyme induction causes resistance to dalfopristin?

55) Streptogramins should not be given orally, must be given IV. Why

P’cology of Oxazolidinones
56) Describe the mechanism of action of linezolide.

57) Which adverse effects are the principal adverse effects of linezolide?

58) Which adverse effects limit the use of linezolide for less than 28 days?

59) Which drugs uses along with linezolide associated with serotonin syndrome?

P’cology of Fidaxomicin
60) What is the antimicrobial mechanism of action of fidaxomicin?

61) What pharmacokinetic property makes fidaxomicin ideal for the treatment of C.
difficile?

62) Fidaxomicin produces cross allergy with macrolide. Why?

P’cology of Aminoglycosides
63) Discuss the mechanism of action of aminoglycosides.

64) Which factors associated with a decrease of aminoglycosides transport across


the cell membranes?

65) Which factor enhances aminoglycosides transport across the cell membranes?

Review Questions –Protein Synthesis Inhibitors (PSIs) -–By Endalk Gebrie ( B.


Pharm & MSc)-- Y12HMC-- Feb. 2023
Page 7
MODULE TITLE: Introduction to Medicine
MODULE CODE: BM-IM 401/1
SPECIFIC TOPIC TITLE: P’cology of Antimicrobial drugs – Protein Synthesis
Inhibitors (PSIs)—Review Questions

66) Penicillin &/or vancomycin combination with aminoglycoside enhances the


efficacy of aminoglycosides. Why?

67) Which mechanism of resistance considered as principal mechanism of resistance


for aminoglycoside?

68) Which microbes excellently killed with aminoglycosides? Gram negative or Gram
positive organisms?

69) List the drugs belonging to aminoglycosides.

70) All aminoglycosides are given parenterally because their oral bioavailability is
1% or less. Which drugs are an exception for this and why?

71) It is known that aminoglycosides have post antibiotic effect (PAE) and
concentration dependent killing characteristics. What is the clinical significance
of these properties?

72) Which adverse effects of aminoglycosides will increase in patients with renal
impairment?

73) Explain the concept of the excretion of aminoglycosides have linear relationship
with serum creatinine level.

74) Therapeutic drug monitoring (TDM) is important for in aminoglycosides therapy.


Why?

75) What is the expected trough [] in mcg/mL 18-24hrs after dosing, and which
serum concentration mcg/mL is predictive of toxicity of aminoglycosides such as
gentamicin, tobramycin & amikacin ?

Review Questions –Protein Synthesis Inhibitors (PSIs) -–By Endalk Gebrie ( B.


Pharm & MSc)-- Y12HMC-- Feb. 2023
Page 8
MODULE TITLE: Introduction to Medicine
MODULE CODE: BM-IM 401/1
SPECIFIC TOPIC TITLE: P’cology of Antimicrobial drugs – Protein Synthesis
Inhibitors (PSIs)—Review Questions

76) Describe the clinical manifestation and characteristics of aminoglycosides


caused ototoxicity.

77) Which aminoglycosides drugs most likely caused significant vestibular function
interference?

78) Which aminoglycosides drugs most likely caused significant cochlea/auditory


damage?

79) Which aminoglycosides drug affects both the vestibular and cochlea/auditory
functions?

80) Which aminoglycoside less ototoxic than others & preferred if prolonged
treatment required?

81) Which two diuretic agents potentiate the ototoxicity of aminoglycosides?

82) Which clinical factors increase the risk of aminoglycosides induced


nephrotoxicity?

83) Which drugs increase the nephrotoxicity effect of aminoglycosides?

84) Which aminoglycosides drugs are the most nephrotoxic and which
aminoglycosides agent is the least?

85) Aminoglycosides have a curare like effect. What is this? And why this happens?

86) What are the advantages of combination of penicillin with aminoglycosides?

87) Discuss all the potential clinical applications of aminoglycosides?

Review Questions –Protein Synthesis Inhibitors (PSIs) -–By Endalk Gebrie ( B.


Pharm & MSc)-- Y12HMC-- Feb. 2023
Page 9
MODULE TITLE: Introduction to Medicine
MODULE CODE: BM-IM 401/1
SPECIFIC TOPIC TITLE: P’cology of Antimicrobial drugs – Protein Synthesis
Inhibitors (PSIs)—Review Questions

88) Streptomycin associated with higher vestibular toxicity (irreversible). True or


false

89) Gentamicin associated with more of nephrotoxic (reversible) than streptomycin-


- preferred for most infection. True or false

90) Which aminoglycoside agent used in the inhalation form for the treatment of P
aeruginosa lower RTIs complicating cystic fibrosis?

91) Which aminoglycosides drug notably has antiparasitic activity & used for this
purpose than bacterial infections?

92) Which systemic, topical and intestinal parasites are treated by the drug you
mentioned in the above question (question 91)?

93) Aminoglycosides are pharmaceutically incompatible with penicillins, heparin,


amphotericin B & the various cephalosporins and should not be mixed in the
same vial or solution. Why?

P’cology of Spectinomycin
94) What is the mechanism of action of spectinomycin

95) What is the sole clinical application of spectinomycin? Provide the clinical
scenario for the use of spectinomycin.

Review Questions –Protein Synthesis Inhibitors (PSIs) -–By Endalk Gebrie ( B.


Pharm & MSc)-- Y12HMC-- Feb. 2023
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