Antimicrobials Flashcards
What is an Antimicrobial?
- Drugs/chemicals that kill micro-organisms or inhibit their growth
- can be used to treat microbial infections
- most selective of all pharm agents because of selective toxicity
Most overused and misused therapeutic agents - leads to antimicrobial resistance
What are the different types of antimicrobials?
Antibiotics = against bacteria
Antifungals = against fungi
Antivirals = against viruses
What is selective toxicity?
Target microbial cells over mammalian cells (thru structural and metabolic toxicity) and cause greater harm to the micro-organisms than the host.
What are the antimicrobial actions?
Microbicidal KILL - decrease (immunocompromised preferred)
Microbiostatic PREVENT - remain constant
What are the antimicrobial spectrums of activity?
Narrow-spectrum - kills/inhibits narrow range (ex. Penicillin gram +)
Broad-spectrum - kills/inhibits a wide range (ex. Tetracyclines gram +/-, anaerobes, and aerobes)
What are examples of inappropriate antimicrobial use?
-antibiotics for viral infections
-inadequate dose/duration
-Rx w/out culture or data
-overuse of unnecessary broad spectrum
What should you consider in optimal antimicrobial therapy?
Efficacy, safety, decreasing microbial resistance
- Organism ID (culture, gram staining, morphology) and susceptibility testing
- Use of antimicrobial with the narrowest spectrum of activity, at adequate dose and appropriate duration
- Use of agents in combo if needed (synergistic effect)
- Consideration of client factors (immune status, age, pregnancy, renal function)
What are antibiotics?
Treat infections caused by bacteria that aren’t part of normal flora
What’s the diff b/w mammalian and bacterial cells?
- Bacteria has cell wall
- Essential metabolic pathways (i.e. synthesizes folic acid)
- Different macromolecule anabolism (protein synthesis and nucleic acid synthesis) [no nucleus - non-eukaryotic]
(Antibiotics target these!)
What are the mechanisms of action of antibiotics?
Inhibition of:
1) Cell wall synthesis
2) Protein synthesis
3) Nucleic acid metabolism
Essential metabolites (folic acid)
Describe the mechanism of cell wall inhibition?
Made of peptidoglycan and prevents cell from bursting. If cell wall is fucked with - osmotic pressure = cell lysis.
Interferes with cross linking of peptidoglycan
· Inhibited by glycopeptides (transglycosoylation and transpeptidation)
Inhibited by Beta-lactams (transpeptidation catalysed by penicillin binding proteins)
Describe the mechanism of Beta Lactams
Cell wall inhibition - Covalently binds to the active site of penicillin-binding proteins (penicillins and cephalosporins)
BACTERIACIDAL
Describe the mechanism of glycopeptides?
Binds to the d-alanyl-D-alinine resides to prevent cell wall synthesis. (Vancomycin)
BACTERIACIDAL
What is gram +?
Thick peptidoglycan layer
What is gram -?
Thin peptidoglycan layer. Outer layer contains phospholipids and lipopolysaccharides
What’s the deal with penicillin?
Cell wall inhibition VIA Beta Lactam
Primarily effective against Gram +
- R side chain determines the class of penicillin (determines: spectrum, susceptibility to acid (route), susceptibility to inactivation (resistance to resistance lol)
- Ends with -cillin
Beta-lactamase enzymes (penicillinase) destroy antibacterial activity causes resistance to penicillin.
Safe in pregnancy, unless anaphylaxis, allergy
What are the classes of penicillin?
Class 1: Narrow spectrum, Class 2 : Penicillinase Resistant, Class 3: Extended spectrum
What’s the deal with Narrow Spectrum penicillin?
Injected
Active against non-penicilinase producing Gram + an some Gram -
Penicillin G p used in group B strep, effective against streptococci
What’s the deal with Penicillinase Resistant penicillin?
Cell wall inhibition
Not as effective against other infections as pen G or pen V
cloxacillin, dicloxacillin (ORALLY ADMIN restricted for use against staphylococci) - MASTITIS
What’s the deal with extended spectrum penicillin?
NOT penicillinase-resistant
**Ampicillin (usually parenteral - non GI); **amoxicillin (oral)
Combined with clavulanic acid (irreversible inhibitor of penicillinase)
Active against gram+, but major use gram -
Many strains resistant due to overuse
What’s the deal with cephalosporins?
Cef-
Cell wall inhibition VIA beta lactam
Structural relatives of pen (so if someone anaphylactic against pen shouldn’t be prescribed ceph 5%)
Two R groups so more can be made
Classified by 5 generations Narrow —-> Broad *effectiveness against Beta lactamases and against Gram (-)
**Gen 1 = **Cefazolin, **Cephalexin (gram +, ok gram -)
** Gen 3 = ** Cefixime (gram -)