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Antimicrobial interfering bacterial protein synthesis Flashcards

quiz 1 (99 cards)

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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
what is the pharmacokinetics of metabolism in aminoglycosides ?
not biotransformed
26
what are the pharmacokinetics of excretion in aminoglycosides?
kidney | - glomerular filtration
27
What should be done w/ the dose of aminoglycosides if the animal has renal insufficiency ?
adjusted
28
what are the adverse effects of aminoglycosides ?
1. Nephrotoxicity 2. Ototoxicity 3. Neuromuscular blockade
29
what type of toxicity is caused when aminoglycosides binds to basolateral membrane of renal proximal tubular epithelium to cause to acute tubular necrosis ?
Nephrotoxicity
30
What major condition can increase nephrotoxicity in aminoglycosides?
dehydration
31
what is ototoxicity caused by aminoglycosides ?
1. accumulates in perilymph & endolymph of inner ear 2. can affect auditory 3. can affect vestibular function 4. irreversible toxicity
32
what animal can you see ototoxicity that will affect the auditory ?
dogs
33
what animal can you see ototoxicity that will affect the vestibular function ?
cats
34
How can neuromuscular blockade toxicity by aminoglycosides be caused ?
rapid IV bolus administration
35
what is neuromuscular blockade toxicity that is cause by aminiglycosides?
1. curare - like (non-depolarizing) | 2. Respiratory arrest
36
what are the types of bacterial resistance to aminoglycosides?
1. enzymatic inactivatyion 2. ribosomal alteration 3. reduced permeability of antibiotic
37
How can the bacteria cause enzymatic inactivation of aminoglycosides ?
acquires gene encoding enzymes | -inactivates antibiotics
38
what is the source for streptomycin?
streptomyces griseus
39
what is the source for gentamicin?
micromonospora purpurea
40
what is the source for Apramycin & tobramycin?
streptomyces tenebrarius
41
what aminoglycoside can be added to the water or feed for pigs?
Apramycin
42
what aminoglycosides can be used in small animals to treat P. aeruginosa?
Tobramycin
43
what is the source for Neomycin?
Streptomyces fraidiae (sulfated)
44
How can Neomycin be administered ?
1. oral | 2. Topical
45
what is the source for amikacin?
semi-synthetic derived from kanamycin | -given parenteral
46
what aminoglycosides is broad spectrum that can be used for treating gram + , gram - & protozoal?
Paromomycin
47
what protozoa can paromomycin treat ?
1. Giardia | 2. entamoeba
48
what is the source for parmomycin?
1. streptomyces ramous var. paromomycin
49
what is the source for tetracycline ?
streptomyces sp. | but now produced by hydrogenolysis of chlortetracycline
50
what are the kinetics for tetracycline ?
1. broad spectrum 2. bacteriostatic 3. acidic & hygroscopic compound 4. hydrochloride formation to increase stability
51
what are the 2 categories of tetracycline dugs ?
1. natural | 2. semisynthetic
52
what are the natural tetracycline drugs?
1. chlortetracycline 2. tetracycline 3. oxytetracycline
53
what is the source of chlortetracycline ?
streptomyces aureofaciens
54
what is the source of oxytetracycline?
streptomyces rimosus
55
what are the semisynthetic tetracycline drugs?
1. minocycline | 2. doxycycline
56
what is the mechanism of action for tetracycline ?
1. penetration into bacterial cells | 2. drug concentration in susceptible bacteria
57
How does tetracycline drugs penetrate into the bacterial cells ?
1. passive diffusion | 2. active transport
58
What is the mechanism of action for tetracycline in susceptible bacteria?
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
what is the microbial susceptibility of tetracycline?
broad bacteriostatic action 1. gram + aerobic bacteria 2. gram - aerobic bacteria 3. anaerobes 4. spirochetes 5. intracellular organism 6. intracellular organism 7. rickettsia
60
what species of gram + aerobic bacteria can be treated with tetracycline ?
1. staphylococci | 2. streptococci
61
what species of gram - aerobic bacteria can be treat with tetracycline ?
1. E.coli 2. klebsiella sp. 3. pasteurella 4. salmonella
62
what are the species of anaerobes that can be treat with tetracycline ?
1. actinomycetes sp. 2. clostridium sp. 3. bactericides sp. 4. fusobacterium sp.
63
what species of spirochete can be treated by tetracycline ?
leptospira sp.
64
what species of intracellular organism can be treated with tetracycline?
1. Brucella 2. Mycoplasma 3. chlamydia sp.
65
what is the species of rickettsia that can be treated with tetracycline ?
1. Ehrlichia sp. 2. Anaplasma 3. Haemobartonella
66
what is the drug of choice for treating Chlamydia psittaci in birds ?
Doxycycline
67
what's the drug of choice for treating Equine monocytic Ehrlochiosis ?
Oxytetracylinie
68
what is the drug of choice for treating staphylococcus aureus ?
minocycline
69
Why is doxycycline administration important in heart worm infected dogs?
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
what is the pharmacokinetics of oral absorption for tetracycline ?
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
what tetracycline drug has complete absorption?
doxycycline
72
what is the pharmacokinetic of parenteral absorption for tetracycline ?
1. oxytetracycline good absorption - IM/IV for immediate release - deep IM for long acting
73
what type of animals can be treated w/ ophthalmic oxytetracycline ?
1. dogs 2. cats 3. cattle 4. horses
74
what is the pharmacokinetics of distribution for tetracycline ?
1. widely distributed 2. lipid solubility 3. binds to plasma proteins
75
what tetracycline drugs bind to plasma protein to have a prlonged 1/2 life ?
1. doxycycline 2. minocycline - 80 & 90 % binding
76
what tetracycline drug has 18- 50% of binding to plasma proteins ?
oxytetracycline
77
What tetracycline drugs are the most lipid soluble ?
1. minocycline | 2. doxycycline
78
Where does tetracycline drugs accumulate in the body?
1. liver | 2. kidneys
79
where does minocycline and doxycycline penetrate in the body?
1. brain 2. spinal fluid 3. bronchial fluid 4. prostate
80
What are adverse effects of tetracycline drugs when they form chelate complexes w/. Ca?
1. deposit in active sites of ossification in bone | 2. developing teeth of young animals
81
what is the pharmacokinetics of metabolism in tetracycline?
very low except Minocycline & doxycycline | -oxidation in liver
82
What is the pharmacokinetics of excretion of tetracycline ?
1. excreted in urine (about 60% of dose)- glomerular filtration 2. excreted in feces (about 40%) 3. undergoes enterophepatic circulation
83
what tetracycline is excreted in bile & by bile diffusion in to large intestine & excreted in feces?
Doxycycline
84
What type of patient is it preferred using doxycycline ?
renal function impaired patients
85
What are the adverse effects of tetracycline ?
1. GI disturbances 2. Esophageal lesions 3. hepatotoxicity 4. local irritaton 5. collapse 6. anaphylactic shock 7. Photoxicity
86
what are the types of GI disturbances as adverse effects in tetracycline?
1. vomiting 2. anorexia 3. diarrhea
87
What type of tetracycline will cause esophageal lesion in cats given oral adminstration?
doxycycline hyclate
88
What type of patients will you see Hepatoxicity as an adverse effect of tetracycline ?
Renal disease pt
89
What type of administration will you see local irritation as an adverse effect of tetracycline ?
IM injection
90
How does rapid IV injection cause collapse as an adverse effect of tetracycline ?
1. Chelates Ca in blood 2. decrease Ca availability for heart concretion 3. collapse
91
what type of administration will cause anaphylactic shock in the dogs?
IV injection
92
What adverse effect will doxycycline cause in horses when given IV?
cardiac arrhythmia ( fatal)
93
what adverse effect will oxytetracycline in horses when given orally?
alters commensal microflora → enteritis
94
what adverse effect will chronic administration or outdate products of tetracycline cause ?
Renal damage
95
what adverse effects will chelation of tetracycline to Ca deposit in teeth dentin?
tooth mottling
96
What type of animals will you see inhibit growth of long bones?
young animals
97
what animal can you see hypersensitivity & drug fever as an adverse effect of tetracycline?
Cats
98
What are the type of bacterial resistance for tetracycline?
1. impaired permeation of drug 2. Tetracycline efflux 3. ribosomal alteration
99
what is the efficacy of tetracycline?
Type III antimicrobial | -time dependent killing kinetics w/ moderate persistent effects

SGU pharm II (5 decks)

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