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SGU pharm II > Antimicrobial interfering bacterial protein synthesis > Flashcards

Antimicrobial interfering bacterial protein synthesis Flashcards

quiz 1

1
Q

What are the target bacterial ribosome for bacterial protein synthesis inhibitors?

A
  1. bacterial - 70s (50S/30S)

2. Mammalian - 80 S ( 60S/40S)

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2
Q

What are the 30S binders for inhibitors of bacterial protein synthesis ?

A
  1. Aminoglycosides

2. Tetraycyclines

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3
Q

what are the 50S binder for inhibitors of bacteria protein synthesis ?

A
  1. Macrolides
  2. Lincosamides
  3. Chloramphenicol and derivatives
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4
Q

what is the source for aminoglycoside ?

A
  1. streptomycin sp.

2. Micromonospora sp.

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5
Q

what are kinetics of amino glycoside ?

A
  1. Aminocyclitols
  2. basis polycation
  3. polar organic bases
  4. low lipid solubility
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6
Q

what are type of Aminoglycoside drugs?

A
  1. Streptomycin
  2. Neomycin
  3. Kanamycin
  4. Gentamicin
  5. Tobraymycin
  6. Apramycin
  7. Amikacin
  8. Paromomycin
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7
Q

what is the mechanism of action for aminoglycoside drugs?

A
  1. bactericidal
  2. penetration into bacterial cells- biphasic
  3. permeate susceptible bacteria
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8
Q

what are the phases in the mechanism of action for ahminoglycosides?

A
  1. passive diffusion ( concentr. dependent)

2. active transport ( O2 dependent )

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9
Q

What type of condition will inhibit transport of aminoglycoside ?

A

anaerobic conditions

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10
Q

what are the consequences of aminoglycosides binding irreversible to the receptor protein on 30S ribosomal subunit

A
  1. irreversible binids
  2. interfers w/ mRNA translation
  3. Non functional protein
  4. prevents initiation of DNA replication
  5. Irreversible lethal effects
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11
Q

What is the efficacy of aminoglycosides ?

A

type I - concentration dependent

-max [drug] = Max bactericidal action

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12
Q

what are characteristic of aminoglycosides?

A
  1. posses post - antibiotic effect
  2. single dose over 24 hrs
  3. administered long intervals
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13
Q

what are the antibacterial spectrum for aminoglycosides?

A
  1. gram - aerobic bacteria

2. Gram + aerobic bacteria

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14
Q

Can aminoglycosides be used to treat anaerobes ?

A

No

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15
Q

what are the most active aminoglycosides for treating gram - aerobic bacteria?

A
  1. Gentamicin
  2. tobramycin
  3. amikacin
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16
Q

what aminoglycoside is used to treat against few staphlococci sp. & mycobacterium sp. which are gram + aerobic bacteria?

A

Gentamicin

-parenteral

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17
Q

what are the antibacterial activity of aminoglycosides ?

A
  1. influenced by local environment pH
  2. Alkaline pH increases antimicrobial activity
  3. Acidic pH & presence of Ca & Mg cations decrease antimicrobial activity
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18
Q

what are the pharmacokinetics of absorption for aminoglycosides?

A
  1. Poor Oral absorption
  2. Parenteral : IM/SC/IV
  3. Eye/ear drops
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19
Q

Why does aminoglycosides have poor oral absorption ?

A

highly polar & cationic nature

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20
Q

What type of administration has rapid & good absorption in aminoglycosides?

A
  1. IM
  2. SC
    100%
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21
Q

what type of administration has a bioavailability of 40%?

A

intrauterine administration

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22
Q

what are the pharmacokinetics of distribution of aminoglycosides?

A
  1. low diffusion across cell membrane
  2. low concentr. in specific areas of the body
  3. Restricted to extracellular space ; accumulates in tissue
  4. 20% Protein binding
  5. Selective binding to anionic cell membrane in specific areas of the body
  6. long w/drawal period
  7. increase distribution in lean cachectic animals
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23
Q

What areas of the body is the distribution of aminoglycosides have low concentration ?

A
  1. brain
  2. CSF
  3. ocular fluid
  4. respiratory secretion
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24
Q

what areas of the body is the distribution of aminoglycosides has selective binding to anionic cells membrane phospholipids which causes accumulation?

A
  1. Proximal renal tubules cells ( renal cortex)

2. Cochlear tissue ( inner ear)

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25
Q

what is the pharmacokinetics of metabolism in aminoglycosides ?

A

not biotransformed

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26
Q

what are the pharmacokinetics of excretion in aminoglycosides?

A

kidney

- glomerular filtration

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27
Q

What should be done w/ the dose of aminoglycosides if the animal has renal insufficiency ?

A

adjusted

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28
Q

what are the adverse effects of aminoglycosides ?

A
  1. Nephrotoxicity
  2. Ototoxicity
  3. Neuromuscular blockade
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29
Q

what type of toxicity is caused when aminoglycosides binds to basolateral membrane of renal proximal tubular epithelium to cause to acute tubular necrosis ?

A

Nephrotoxicity

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30
Q

What major condition can increase nephrotoxicity in aminoglycosides?

A

dehydration

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31
Q

what is ototoxicity caused by aminoglycosides ?

A
  1. accumulates in perilymph & endolymph of inner ear
  2. can affect auditory
  3. can affect vestibular function
  4. irreversible toxicity
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32
Q

what animal can you see ototoxicity that will affect the auditory ?

A

dogs

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33
Q

what animal can you see ototoxicity that will affect the vestibular function ?

A

cats

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34
Q

How can neuromuscular blockade toxicity by aminoglycosides be caused ?

A

rapid IV bolus administration

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35
Q

what is neuromuscular blockade toxicity that is cause by aminiglycosides?

A
  1. curare - like (non-depolarizing)

2. Respiratory arrest

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36
Q

what are the types of bacterial resistance to aminoglycosides?

A
  1. enzymatic inactivatyion
  2. ribosomal alteration
  3. reduced permeability of antibiotic
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37
Q

How can the bacteria cause enzymatic inactivation of aminoglycosides ?

A

acquires gene encoding enzymes

-inactivates antibiotics

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38
Q

what is the source for streptomycin?

A

streptomyces griseus

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39
Q

what is the source for gentamicin?

A

micromonospora purpurea

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40
Q

what is the source for Apramycin & tobramycin?

A

streptomyces tenebrarius

41
Q

what aminoglycoside can be added to the water or feed for pigs?

42
Q

what aminoglycosides can be used in small animals to treat P. aeruginosa?

A

Tobramycin

43
Q

what is the source for Neomycin?

A

Streptomyces fraidiae (sulfated)

44
Q

How can Neomycin be administered ?

A
  1. oral

2. Topical

45
Q

what is the source for amikacin?

A

semi-synthetic derived from kanamycin

-given parenteral

46
Q

what aminoglycosides is broad spectrum that can be used for treating gram + , gram - & protozoal?

A

Paromomycin

47
Q

what protozoa can paromomycin treat ?

A
  1. Giardia

2. entamoeba

48
Q

what is the source for parmomycin?

A
  1. streptomyces ramous var. paromomycin
49
Q

what is the source for tetracycline ?

A

streptomyces sp.

but now produced by hydrogenolysis of chlortetracycline

50
Q

what are the kinetics for tetracycline ?

A
  1. broad spectrum
  2. bacteriostatic
  3. acidic & hygroscopic compound
  4. hydrochloride formation to increase stability
51
Q

what are the 2 categories of tetracycline dugs ?

A
  1. natural

2. semisynthetic

52
Q

what are the natural tetracycline drugs?

A
  1. chlortetracycline
  2. tetracycline
  3. oxytetracycline
53
Q

what is the source of chlortetracycline ?

A

streptomyces aureofaciens

54
Q

what is the source of oxytetracycline?

A

streptomyces rimosus

55
Q

what are the semisynthetic tetracycline drugs?

A
  1. minocycline

2. doxycycline

56
Q

what is the mechanism of action for tetracycline ?

A
  1. penetration into bacterial cells

2. drug concentration in susceptible bacteria

57
Q

How does tetracycline drugs penetrate into the bacterial cells ?

A
  1. passive diffusion

2. active transport

58
Q

What is the mechanism of action for tetracycline in susceptible bacteria?

A

inhibits initiation step of DNA

  1. binds reversible to 30S ribosomal subunit
  2. blocks binding tRNA at acceptor site on mRNA-ribosomal complex
  3. inhibits new amino acids to peptide chains
59
Q

what is the microbial susceptibility of tetracycline?

A

broad bacteriostatic action

  1. gram + aerobic bacteria
  2. gram - aerobic bacteria
  3. anaerobes
  4. spirochetes
  5. intracellular organism
  6. intracellular organism
  7. rickettsia
60
Q

what species of gram + aerobic bacteria can be treated with tetracycline ?

A
  1. staphylococci

2. streptococci

61
Q

what species of gram - aerobic bacteria can be treat with tetracycline ?

A
  1. E.coli
  2. klebsiella sp.
  3. pasteurella
  4. salmonella
62
Q

what are the species of anaerobes that can be treat with tetracycline ?

A
  1. actinomycetes sp.
  2. clostridium sp.
  3. bactericides sp.
  4. fusobacterium sp.
63
Q

what species of spirochete can be treated by tetracycline ?

A

leptospira sp.

64
Q

what species of intracellular organism can be treated with tetracycline?

A
  1. Brucella
  2. Mycoplasma
  3. chlamydia sp.
65
Q

what is the species of rickettsia that can be treated with tetracycline ?

A
  1. Ehrlichia sp.
  2. Anaplasma
  3. Haemobartonella
66
Q

what is the drug of choice for treating Chlamydia psittaci in birds ?

A

Doxycycline

67
Q

what’s the drug of choice for treating Equine monocytic Ehrlochiosis ?

A

Oxytetracylinie

68
Q

what is the drug of choice for treating staphylococcus aureus ?

A

minocycline

69
Q

Why is doxycycline administration important in heart worm infected dogs?

A
  1. sterilized female peartworms
  2. prevents infected dogs from infecting other dogs by mosquitoes
  3. improves heart worm adulticide treatment
  4. reduce inflammation & risk of serious adverse rxn to melarosmine drug
70
Q

what is the pharmacokinetics of oral absorption for tetracycline ?

A
  1. well oral absorption
  2. absorption varies on formulation / species
  3. half life → 7- 19 hrs
  4. forms chelation complexes w/ divalent & trivalent cations
71
Q

what tetracycline drug has complete absorption?

A

doxycycline

72
Q

what is the pharmacokinetic of parenteral absorption for tetracycline ?

A
  1. oxytetracycline good absorption
    - IM/IV for immediate release
    - deep IM for long acting
73
Q

what type of animals can be treated w/ ophthalmic oxytetracycline ?

A
  1. dogs
  2. cats
  3. cattle
  4. horses
74
Q

what is the pharmacokinetics of distribution for tetracycline ?

A
  1. widely distributed
  2. lipid solubility
  3. binds to plasma proteins
75
Q

what tetracycline drugs bind to plasma protein to have a prlonged 1/2 life ?

A
  1. doxycycline
  2. minocycline
    - 80 & 90 % binding
76
Q

what tetracycline drug has 18- 50% of binding to plasma proteins ?

A

oxytetracycline

77
Q

What tetracycline drugs are the most lipid soluble ?

A
  1. minocycline

2. doxycycline

78
Q

Where does tetracycline drugs accumulate in the body?

A
  1. liver

2. kidneys

79
Q

where does minocycline and doxycycline penetrate in the body?

A
  1. brain
  2. spinal fluid
  3. bronchial fluid
  4. prostate
80
Q

What are adverse effects of tetracycline drugs when they form chelate complexes w/. Ca?

A
  1. deposit in active sites of ossification in bone

2. developing teeth of young animals

81
Q

what is the pharmacokinetics of metabolism in tetracycline?

A

very low except Minocycline & doxycycline

-oxidation in liver

82
Q

What is the pharmacokinetics of excretion of tetracycline ?

A
  1. excreted in urine (about 60% of dose)- glomerular filtration
  2. excreted in feces (about 40%)
  3. undergoes enterophepatic circulation
83
Q

what tetracycline is excreted in bile & by bile diffusion in to large intestine & excreted in feces?

A

Doxycycline

84
Q

What type of patient is it preferred using doxycycline ?

A

renal function impaired patients

85
Q

What are the adverse effects of tetracycline ?

A
  1. GI disturbances
  2. Esophageal lesions
  3. hepatotoxicity
  4. local irritaton
  5. collapse
  6. anaphylactic shock
  7. Photoxicity
86
Q

what are the types of GI disturbances as adverse effects in tetracycline?

A
  1. vomiting
  2. anorexia
  3. diarrhea
87
Q

What type of tetracycline will cause esophageal lesion in cats given oral adminstration?

A

doxycycline hyclate

88
Q

What type of patients will you see Hepatoxicity as an adverse effect of tetracycline ?

A

Renal disease pt

89
Q

What type of administration will you see local irritation as an adverse effect of tetracycline ?

A

IM injection

90
Q

How does rapid IV injection cause collapse as an adverse effect of tetracycline ?

A
  1. Chelates Ca in blood
  2. decrease Ca availability for heart concretion
  3. collapse
91
Q

what type of administration will cause anaphylactic shock in the dogs?

A

IV injection

92
Q

What adverse effect will doxycycline cause in horses when given IV?

A

cardiac arrhythmia ( fatal)

93
Q

what adverse effect will oxytetracycline in horses when given orally?

A

alters commensal microflora → enteritis

94
Q

what adverse effect will chronic administration or outdate products of tetracycline cause ?

A

Renal damage

95
Q

what adverse effects will chelation of tetracycline to Ca deposit in teeth dentin?

A

tooth mottling

96
Q

What type of animals will you see inhibit growth of long bones?

A

young animals

97
Q

what animal can you see hypersensitivity & drug fever as an adverse effect of tetracycline?

98
Q

What are the type of bacterial resistance for tetracycline?

A
  1. impaired permeation of drug
  2. Tetracycline efflux
  3. ribosomal alteration
99
Q

what is the efficacy of tetracycline?

A

Type III antimicrobial

-time dependent killing kinetics w/ moderate persistent effects

SGU pharm II (5 decks)

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