Aminoglycodides Flashcards
Modes of antibacterial action : concentration dependent
- Some drugs and aminoglycosides
- As the PLASMA LEVEL IS INCREASED ABOVE THE MIC, the drug kills an increasing proportion of bacteria at a more rapid rate
Plasma Level + = Kills bacteria faster
MODES OF ANTIBACTERIAL ACTION :
TIME DEPENDENT
- Any antibiotics, including Penicillin and
Cephalosporins - Directly related to time above MIC
- Independent of concentration once
the MIC is reached
MIC : Minimum Inhibitory Concentrations
MODES OF ANTIBACTERIAL ACTION : POSTANTIBIOTIC EFFECT
- Aminoglycosides’ killing action continues when the plasma levels have declined below measurable levels
- It is a phenomenon where the antibiotic continues to inhibit bacterial growth even after the drug has been removed.
MODES OF ANTIBACTERIAL ACTION : POSTANTIBIOTIC EFFECT
- Greater efficacy when administered as a SINGLE LARGE DOSE than when given as multiple smaller doses
AMINOGLYCOSIDES : PHARMACOKINETICS
- Structurally related amino sugars
attached by glycosidic linkages - Polar compounds
- Not absorbed orally
AMINOGLYCOSIDES : PHARMACOKINETICS
- Given intramuscularly or intravenously
for systemic effects - Limited tissue penetration
- Do not readily cross the blood-brain barrier
Major mode of excretion
Glomerular Filtration
Plasma levels are affected by the changes of ?
Renal Function
Excretion is directly propotional to ?
Creatine Clerance
With normal Renal funtion, elimination half-life is ?
2-3 Hours
Dosage adjsutment must be made in__________to avoid_______?
Made in Renal Insufficiency to avoid Toxicity accumulation
Monitoring what levels is needed for safe anf effective dosage selection and adjustment ?
Plasma levels
Traditonal Dosing regiments ?
2 to 3 times a day
When is the Peak serum levels ?
30-60 minuties after administering
Trough serum levels
Refers to the lowest concentration of a drug in the bloodstream, reached just before the next dose is administered.
Bactericidal
- Substances that destroys microorganisms.
- They are Irreversible inhibitors of protien synthesis
Penetration of bacterial cell wall is partly dependent on ?
O2 dependent active transport
Transport is enhanced by ?
Cell wall synthesis inhibitors
- Due to the accumulation of intermediates in the cell wall synthesis pathway, which increases the concentration of substrates available for transport
Bactericidal
Kills the bacteria.
● Something like suicide or homicide
● Actually kills the intended bacteria
Minimum Inhibitory Concentration
The lowest concentration of an antimicrobial (like an antifungal, antibiotic, or bacteriostatic) drug that will inhibit the visible growth of a microorganism after overnight incubation.
● In-vitro quantitative measure of how much concentration of antibiotic will be able to inhibit the growth of bacteria.
Selective Toxicity
The aim of antimicrobial therapy is TO KILL or INHIBIT the INFECTIVE ORGANISIM WITHOUT DAMAGING THE HOST.
Bacteriostatic
Prevents the growth of bacteria.
- Does not kill bacteria but it prevents its reproduction, thereby allowing the immune system to take over.
ANTIMICROBIALS
- Drugs that inhibit the growth/replication or kill microorganisms.
○ Antibacterial
○ Antifungal
○ Antiviral
○ Antiprotozoal
○ Antiparasitic
BACTERIAL STRUCTURE
○ Cell membrane
○ Nucleus (no nuclear membrane, but has nucleoid structure to contain their chromosomes)
○ Fmbriae
○ Pili
○ Some may develop a capsule