Aminoglycosides and Tetracyclines Flashcards
Which antibiotics inhibit protein synthesis?
streptogramins aminoglycosides tetracyclines macrolides lincosamides oxazolidinones chloramphenicol
where do chloramphenicol antibiotics bind to on ribosome?
what does it inhibit?
50S
formation of peptide bond
where do erythromycin antibiotics bind to on ribosome?
what does it inhibit?
50S
prevents translocation
where do streptomycin antibiotics bind to on ribosome?
what does it do?
30S
causes code of mRNA to be read incorrectly
where do tetracyclines antibiotics bind to on ribosome?
what does it interfere with?
30S
attachment of tRNA to mRNA-ribosome complex
list all antibiotics that bind to the 30S ribosomal subunit
spectinomycin tetracycline (two different locations) pactamycin hygromycin B streptomycin paromomycin geneticin
list all antibiotics that bind to the 50S ribosomal subunit
thiostrepton avilamycin streptogramin A and B chloramphenicol puromycin pleuromutilins lincosamides macrolides
T/F aminoglycosides are typically natural products
True
aminoglycosides are isolated from what bacterial class?
actinomycetes
which two actinomycetes are used to create aminoglycosides?
streptomyces and micromonospora
aminoglycosides ending in ___ are streptomyces
mycin
aminoglycosides ending in ___ are micromonospora
micin
what is the active component of S. griseus that is effective against M. tuberculosis (bacteria causing TB)
streptomycin
T/F streptomycin was on of the first effective drugs to treat TB
true
is streptomycin used against anareobic/aerobic gram +? gram -? both?
aerobic gram -
what is the central structural component of aminoglycosides?
aminocyclitol ring
what structure is found in every aminoglycoside except for streptomycin?
2-deoxystreptamine
T/F aminoglycosides are usually given orally
False, given IM or IV
how are aminoglycosides transported inside the bacteria?
actively transported across the cell membrane by O2-dependent transport system
T/F Low pH and anaerobic conditions inhibit transport of aminoglycosides
True
where do aminoglycosides bind to on the 30S ribosomal subunit?
what do they inhibit?
16S rRNA
irreversibly inhibit protein biosynthesis and causes misreading of rRNA
Gentamicin targets what bacteria?
what family is it a part of?
Ps. aeruginosa and other gram - bacteria
Gentamicin Family
Kanamycin is used for?
what family is it a part of?
TB and dysentery
Kanamycin Family
Amikacin targets what bacteria?
what family is it a part of?
Ps. aeruginosa and TB
Kanamycin Family
Tobramycin is not used to treat what bacteria?
it is used to treat?
what family is it a part of?
TB
Ps. aeruginosa
Kanamycin Family
Neomycin is a part of what family?
Neomycin Family
Paromomycin is a part of what family?
it is used to treat?
Neomycin Family
amoebic dysentery
gentamicin family are produced by streptomyces or micromonospora?
micromonospora
Gentamicin is used topically for?
burn patients
Gentamicin is inhaled to treat?
cystic fibrosis
what side effect is a major problem with the use of Kanamycin?
ototoxicity
T/F neomycin is given orally and topically
True
what are the three ways bacteria develop resistance to the Aminoglycosides?
- Decrease Drug Uptake or Accumulation
- Alter Ribosomal Structure
- Aminoglycoside Modifying Enzymes (AMEs)
what are the three Aminoglycoside Modifying Enzymes (AMEs)?
Aminoglycoside O-Phosphotransferases (APH)
Aminoglycoside O-Nucleotidyltransferases (ANT)
Aminoglycoside N-Acetyltransferases (AAC)
Tetracyclines were produced by what strain of bacteria?
streptomyces
Tetracyclines are active against gram +? gram -?
both
what metal ion is required to allow tetracyclines to enter into gram - cells?
Mg2+
T/F Tetracyclines may increase the potency of birth control pills
False, may make them less effective
whats the name of the first tetracycline isolated?
Chlortetracycline
how is tetracycline made?
Produced by catalytic hydrogenation of chlortetracycline
what is the most frequently prescribed tetracycline?
Doxycycline
which tetracycline is best absorbed and has the longest half life?
Minocycline
how is tigecycline given?
injected only
what are the four mechanisms of resistance for tetracycline?
1) Enzymatic inactivation
2) Target modification
3) Energy-dependent efflux mechanism
4) Ribosomal protection proteins
