Lec6 Flashcards
Antimicrobials
Have the ability to kill or suppress the multiplication or growth of microorganisms
Bacteriocidal
Antimicrobial that kills microbes
Bacteriostatic
Antimicrobial that inhibits growth or replication of microbes
What are the goals of Antimicrobials?
- Kill / Disable pathogen without killing the host (patient)
-Microbe must be susceptible to the antimicrobial - Must reach the site of infection and at high enough concentrations to kill or inhibit the microorganism
- Patient must tolerate concentrations necessary to achieve therapeutic range
- Patient’s immune system must be competent (Especially when using STATIC medications)
Antimicrobial Mechanisms of Action
- Inhibition of cell wall synthesis (cidal by inhibition of enzymes for cell wall synthesis)
- Alteration in cell membrane permeability (static or cidal due to loss of cellular substances/cell lysis)
- Inhibition of protein synthesis (static or cidal due to interference with protein synthesis)
- Interference with metabolism (static due to lack of essential materials for bacterial metabolism)
- Nucleic acid impairment (cidal due to nucleic acid enzyme inhibition)
Spectrum
range of bacteria on which an antibiotic is effective
(Gram +,Gram –, Aerobic, Anaerobic)
What is the function of sensitivity testing?
Identify antibiotic effectiveness
Zone of Inhibition
Determines the ability of the drug to prevent growth (Sensitive, Intermediate, Resistant)
The zone sizes are looked up on a standardized
chart to give a result of sensitive, intermediate or resistant
Many charts have a corresponding column that also gives the MIC for that drug
MIC
(Minimum Inhibitory Concentration)
- MIC represents the lowest concentration of drug at which growth of the bacterium is inhibited
- It is a measurement of susceptibility of a bacterial strain to the effects of an antimicrobial agent
What are the antibiotics that target the cell wall?
Penicillins, Cephalosporins, Bacitracin, Vancomycin
What drug am I?
- Cidal group derived from a mold (natural)
- Mainly semi-synthetic today
- Contain a beta–lactam ring in their structure that interferes with cell wall synthesis
- Recognized by having the suffix “cillin” in the generic drug name
- Rapidly distributed to most tissues
Penicillins
What are the features of Penicillins?
- The first penicillins were narrow spectrum with activity against mostly Gram(+) bacteria
- Pen G was one of the first developed but must be used by parenteral routes due to inactivation by stomach acid and is commonly in a suspension
- Pen G is also available as a Na+ or K+ salts that can be given IV and is also well absorbed IM
- Pen V then became available in oral tablets due to better absorption from the GI tract and is also available in Na+/K+ injectable salts
What is important about Penicillin G suspensions?
- Procaine and Benzathine molecules are added to IM suspensions to delay absorption and increase duration of action
- Pen G suspensions should never be given IV!!!
How are Broad spectrum penicillins different? (name some examples of these penicillins)
- Semisynthetics that have greater activity against Gram(–) bacteria
- Includes amoxicillin, ampicillin,carbenicillin, ticarcillin, and methicillin
- Food affects the bioavailabilty of oral penicillins, so they should be given 1-2 hrs before eating
- Amoxicillin may be given with food
Resistance Factors of Penicillins
- Due to the penicillinase/beta-lactamase I enzyme found in some bacteria that destroys the beta-lactam ring and renders the antibiotic less effective
- oxacillin, dicloxacillin, cloxacillin, floxacillin and methicillin have a narrower spectrum but are “penicillinase resistant” and used mainly for treatment of skin, osteomyeleitis, and mastitis infusions
How are Potentiated Penicillins different? (and an example of this drug)
- A “potentiated” drug has an additional chemical(s) added to enhance the effects of both drugs
- Clavulanic acid binds to beta-lactamase
- When added to amoxicillin, the beta-lactam ring is protected against destruction by beta-lactamase producing bacteria
- Clavamox® is the amoxicillin/clavulanic acid combination used in animals (Augmentin® human product)
What are the adverse effects of Penicillins?
- One of the safest antibiotics, but may see anorexia, vomiting and diarrhea (v/d) when given orally
- Severe allergic reactions, even anaphylaxis may occur, especially when given IV
- GI superinfections from death of gut lactobacilli (beneficial bacteria) resulting in diarrhea, dehydration, and possibly death are prevalent in guinea pigs, rabbits, and hamsters with oral administration of penicillins
- May use Ben-e-bac lactobacillus supplement to off set superinfections
What drug am I?
- Cidal, broad sectrum, semisythetic group derived from cepalosporin C
- Structurally and chemically similar to penicillin
- Contain a beta-lactam ring in their structure
- Recognized by most having the prefix “ceph” or “cef” in their generic or trade names
Cephalosporins
What are the features of Cephalosporins?
- Classified into four “generations”
- Well distributed to most tissues
- First generation are well absorbed by the GI whereas third and fourth generations are usually injectable
- Used frequently when penicillin is not effective
- cephalexin (Keflex®) is a commonly used injectable
What are the differences between the generations of Penicillins?
- First-generation is most commonly used in veterinary medicine and spectrum is mostly Gram(+) and some Gram(-)
- Second-generation has broader spectrum against Gram(–) and slightly less Gram(+) than first generation
- Third-generation have even broader Gram – spectrum of activity and are beta-lactamase II (cepalosporinase) resistant
- Fourth-generation like the third with activity against Pseudomonas aerugnosa and some Enterobacteriaceae (Gram(-) GI rods)
What are the adverse effects of Cephalosporins?
- Similar to penicillin, so animals allergic to penicllin may also be allergic to cephalosporins
- Hypersensitivity reactions can cause fever and rashes
- Superinfection and GI signs (more common in cats) may occur (v/d, anorexia)
- When given orally, GI signs may be reduced by administration with a small meal IM injection can cause local pain and inflammation
- Adverse effects worsen as the generation increases
What drug am I?
- Polypeptide that disrupts the cell wall like penicillins and cephalosporins, but has no beta-lactam ring
- Primary spectrum is Gram(+)
- Toxic to the kidneys and used mainly for topical treatment of skin, mucous membranes, and ocular surfaces
- Due to poor GI absorption, may be used a feed additive for intestinal pathogens
- Often seen in combination “triple antibiotic ointments” with neomycin and polymyxin B to create a wide spectrum topical
Bacitracin
What Drug am I?
- Cidal glycopeptide used primarily for treatment of infections resistant to penicllins and cephalosporins
- Only available for IV administration
- Primary spectrum is Gram(+)
- Used mainly in humans for treatment of drug resistant Staph aureus
- Rarely used in non-humans to avoid development of resistance
- Adverse effects in animals are rare but include ototoxicity, nephrotoxicity and pain on IV injection
Vancomycin
What are the antibiotics that target the cell membrane?
Polymyxin B