Tetracycline and Aminoglycosides Flashcards
What is a ribosome?
A large nucleoprotein complex that catalyzes the ordered polymerization of amino acids
What directs the ribosome to order the amino acids?
An mRNA template (mRNA translation)
How can drugs target bacterial ribosomes while not affecting human ribosomes?
Structural difference (70s prokaryote vs. 80S Eukaryote)
What are the 3 steps of protein synthesis?
- Initiation
- Elongation
- Termination
Which step of protein synthesis do most current protein synthesis inhibitors target?
Elongation
How to aminoglycosides inhibit protein synthesis?
Promote premature termination
Tetracyclines are named according to what?
The number of fused rings
Tetra = 4
Doxy = 2
Mino = 1
How do tetracyclines inhibit protein synthesis?
Bind to the 30S ribosomal subunit and inhibit binding of amino acylated tRNA to A site of ribosome
What helps tetracycline along in its effect on bacteria?
Bacteria concentrate tetracyclines inside the cell, eukaryotes and resistant bacteria do not
Are tetracyclines bactericidal?
No, bacteria start to grow again once the patient stops taking tetracycline.
What is the spectrum of activity for tetracycline?
Broad Spectrum: G+, G-, aerobe, anaerobe, atypical bacteria (rickettsiae, mycoplasma, Chlamydia)
Of Tetracycline, Doxycycline, and Minocycline: which has the lower bioavailability and higher risk of superinfection in the gut?
Tetracyclines
What inhibits the absorption of Tetracyclines?
divalent cations (Ca, Mg, Al, Fe). Think of Tetracycline binding to bone. Do not take w/ milk. Take 1-2 hrs prior to a meal. Tetracycline is a potent chelator
Of tetracycline, doxycycline and minocycline: which are the most lipophilic and are therefore more easily distributed?
Tetracycline and Doxycycline
What is a characteristic of tetracyclines that is useful in the treatment of adults with periodontal disease?
Concentrate in gingival crevicular fluid
Of Tetracycline, doxycycline, and minocycline: which has the shortest halflife and therefore must be dosed more often during the day?
Tetracycline (4/day)
Minocycline and doxycycline (2/day)
Of tretracycline, doxycycline, and minocycline: which is eliminated unchanged in the urine?
Tetracycline (whereas minocycline and doxycyclines undergo hepatic
metabolism and excretion as well as renal excretion)
When is tetracycline contraindicated?
In pregnant women and children less than 8. Uptake and concentrates in developing bones and teeth.
What are 3 common side effects of tetracycline?
Staining of teeth and altered rates of bone growth
GI disturbances
Phototoxic skin reactions
Is teeth staining reversible or irreversible?
Is it dose dependent or non-dose dependent?
Irreversible/permanent and dose dependent
What is the superinfection and its symptoms that can be caused by tetracycline (doxycycline has reduced risk)?
Colitis due to superinfection by C.diff (main symptom: bloody stools)
What can be a rare side effect from treating a meningococcal infection with minocycline?
Vestibular toxicity: dizziness, vertigo
What do doxycycline and minocycline do in the blood and what consideration must be made?
Depress plasma prothrombin. If patient is on anticoagulation therapy, dosing may need to be reduced