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Protein Synthesis Inhibitors

Examples of aminoglycosides Gentamycin. Streptomycin. Amikacin. Tobramycin. Neomycin. Netilmicin
MOA of aminoglycosides Bind to 30S subunit. Alter codon:anticodon recognition. Abnormal protein formed
Most common use of aminoglycosides Aerobic G- (some G+). (Transport through membrane is oxygen dependent)
Most common aminoglycoside Gentamycin
Aminoglycoside used for Pseudomonads Tobramycin
When is amikacin used? For gentamycin or tobramycin resistant strains of bacteria. When wide spectrum aminoglycosides are needed
What borders can aminoglycosides cross? Placenta. Joints. Pleura.
What borders can aminoglycosides not cross? BBB. Cells. Eyes. Secretions. Fluids
What should you beware of when prescribing aminoglycosides Drug accumulates to toxic levels rapidly during renal failure.
When should aminoglycosides be d/c'd? D/c of aminoglycosides can reverse tubule damage.
What should be looked out for in a patient when prescribing aminoglycosides? Dehydrated patient. Other nephrotoxins. Pre-existing renal failure. Each of these can exacerbate nephrotoxicity
What are 3 major S/Es of aminoglycosides? Nephrotoxicity. Ototoxicity. Paralysis.
What symptoms show in ototoxicity due to all aminoglycosides? Vertigo. Ataxia.
What aminoglycosides cause a loss of balance? Streptomycin and gentamycin
What aminoglycosides cause deafness? Neomycin and amikacin
How do aminoglycosides cause paralysis? They create a neuromuscular blockade. 1) They inhibit Ca2+ uptake. 2) This inhibits exocytotic release of ACh
Examples of tetracyclines Demecocycline, tetracycline, oxytetracycline, doxycycline, minocycline.
Are tetracyclines bacteriostatic or bacteriocidal? Bacteriostatic
MOA of tetracyclines They compete with tRNA for A site of 30S subunit of ribosome. Note - they require active transport into bacterial cells
Which tetracycline is used for Neisseria Meningitidis? Minocycline
Do tetracyclines cross the BBB? No
Do tetracyclines have narrow or wide distribution? Wide. They are distributed into placenta, breast milk and saliva.
Clinical uses of tetracyclines? Rickettsia, mycoplasma, chlamydia, brucellosis, cholera, plague, leptospirosis
Which tetracycline is used to treat acne? Minocycline
Which tetracycline is used to treat SIADH? Demeclocycline
What superinfection may be a side effect of tetracycline treatment? C Difficile superinfection
To whom should tetracycline be withheld, due to hepatotoxicity? Children, pregnant women and nursing mothers
Which tetracycline causes photosensitivity? Demeclocycline
Which tetracycline causes vestibular disturbance? Minocycline
What is a long term side effect of tetracycline treatment? Bone marrow suppression
Name the 30S inhibitors Aminoglycosides and tetracyclines
Which drugs does chloramphenicol show competition for? Erythromycin and clindamycin
What is the MOA of chloramphenicol? It inhibits transpeptidation which prevents protein production by the bacterial cell
Is chloramphenicol considered broad or narrow spectrum? Broad spectrum. It covers many G+, G- bacteria and Rickettsia
Is chloramphenicol bacteriostatic or bacteriocidal? For most bacteria, chloramphenicol is bacteriostatic. However, it is bacteriocidal for H. Influenza, N. Meningitidis and Strep Pneumoniae
How is chloramphenicol resisted by bacteria? Via plasmid mediated production of chloramphenicol acetyl transferase.
Does chloramphenicol cross the BBB? Yes. Only 60% of concentration is found in blood
How is chloramphenicol metabolised? 90% is metabolised via glucuronidation
When is chloramphenicol used? H. Influenza infections (due to resistance to other abx). Meningitis (when penicillin cannot be used). Topical eye drops for bacterial conjunctivitis. ┬▒Typhoid fever (other drugs are less toxic)
What are the major side effects of chloramphenicol? Bone marrow suppression (dose-dependent) and Grey baby syndrome
What are some examples of Macrolides? Erithromycin, Clarithromycin and Azithromycin
What is their structure? Multiple lactose rings with deoxy sugars attached
Are macrolides bacteriostatic or bacteriocidal? Depends on dose and microorganism
What drugs are macrolides in competition with? Chloramphenicol
Spectrum of activity of erithromycin? G+, Haemophilus Influenza, Neisseria Gonorrhoea. (Similar to penicillin so use if allergic)
Spectrum of activity of azithromycin? Main action: toxoplasmosis gondii. (More active than erithromycin for H Influenza and Legionella) Lyme disease
Spectrum of activity for clarithromycin H Influenza, myobacterium avium intracellulare. Lyme disease
Do macrolides cross the BBB or placenta? No to BBB, yes to placenta
Which macrolide inhibits P450? Clarithromycin - metabolite
Which bacteria may be seen with an opportunistic infection of GIT or vagina due to macrolide use? Candida Albicans
What class of drugs does clindamycin belong to? Lincosamides
What is the MOA of climdamycin? It inhibits translocation via binding to 50S subunit
Side effect of lincosamide? GIT and acute colon inflammation
Uses for clindamycin? G+ cocci. Penicillin resistant staph. Topical use - Staph Conjunctivitis
Sodium fusidate is an example of? A fusidic acid
What does fusidic acid treat that the other 50S inhibitors do not? Osteomyelitis. Other than that it is used in similar circumstances to clindamycin
What is the MOA of streptogramins? They block tRNA attachment to 50S and cause premature peptide release
What are two examples of streptogramins? Quinupristin and Dalfopristin
Are streptogramins first or last choice? They are only used for serious infections: MRSA, vancomycin-resistant enterococci, penicillin-resistant strep pneumoniae
What is linezolid an example of? An oxazolidinone
What is it used to treat? Serious cases: C Diff. G+s (e.g. MRSA). Vancomycin-resistant enterococci. Penicillin-resistant staph pneumoniae
Created by: 676084495