Antimicrobial agents Flashcards
Aminoglycides act by
Inhibiting bacterial ribosomes thus inhibiting DNA translation / protein synthesis -> inhibiting bacterial replication.
Aminoglycosides can only work on gram negative AERObic bacteria why?
- Cannot enter the thick cell wall layer of gram positive bacteria.
- Aminoglycosides require O2-dependent cotransporters on the cell membrane - therefore cannot enter anerobic bacteria.
Which Aminoglycoside is used in the treatment of Mycobacterium terberculosis?
Streptomycin
What are examples of aminoglycosides?
Gentamicin
Steptomycin
Tobramycin - topical for eye infections
What kinds of conditions are treated by Aminoglycosides?
Infections in the:
1. Respiratory tract
2. Urinary tract
3. Blood
4. Bone
5. Soft tissue
What is combined with Aminoglycosides to treat Gram positive bacteria?
A cell wall synthesis inhibitor (Beta-lactam antibiotic) such as Penicillin or Vancomycin. These antibiotics reduce the structural integrity of the cell wall thus providing entry points for the Aminoglycosides.
*Used to treat enterococci infections such as infective endocarditis.
What is the route of administration for Aminoglycosides?
Not absorbed via gut therefore administration via:
* IV
* IM
* Topical (creams, gels, drops).
Red flag Aminoglycosides
Unwanted effects of critical importance inlcude:
1. Ototoxic - damage hair cells and cochlea. The risk increases if the pt is taking Loop diuretics (as they are also ototoxic).
2. Nephrotoxic - can lead to kidney failure (monitor kidney function).
3. Contraindicated for Myasthenia Gravis - can cause fatal respitory paralyis at high does.
*As Myasthenia Gravis antibodies bind post synaptic Ach neurons the effect of Aminoglycosides reducing the release of Ach at the presynaptic neuron proivdes a double hit to Ach neurons causing weakness, paralysis in skeletal muscles (ie diaphram)!
Are Aminoglycosides safe in pregnancy?
No! They have teratogenic effects (deafness).
Non-specific side effects of Aminoglycosides include:
- Nausea
- Vomitting
- Allergic reaction
What is the MOA of Antimetabolites?
Antimetabolites, such as sulfonamides and trimethoprim, act by inhibiting bacteria folate synthesis.
Without folate the bacteria cannot produced the building blocks for DNA / RNA > thus reducing bacterial cell functioning and inhibiting cell division.
What are the two main groups of Antimetabolites?
- Sulfonamides
- Trimethoprim
Are Antimetabolites bacteriostatic or bacteriocidal?
When used individually these are bacteriostatic, however when used in combination they are bactericidal (synergistic effect) as they inhibit folate synthesis via two pathways (enzyme in step 1 of the bacterial folate synthesis pathway and step 2).
What microbial agents are antimetabolites used to treat.
Antimetabolites such as sulphonamides and trimethoprim are broad spectrum and are used to treat both Gram positive and negative bacteria.
They are effective in travellers diarrhea, UTI, Pneumonia, sinus infect MRSA, Pheumocystis Jirovecii (yeast lung infection in immunocompromised pts).
General unwanted effects of Sulfonamides include?
- Nausea,
- Photosensitivity,
- Crystalluria,
- Nephritis