Antibiotics ✅ Flashcards
What groups can antibiotics be divided into?
- Beta-lactam agents
- Macrolides
- Tetracyclines
- Aminoglycosides
- Glycopeptides
- Fluoroquinolones
What can beta-lactam agents be further divided into?
- Penicillins
- Cephalosporins
- Carbapenums
Give 4 examples of penicillins
- Penicillin
- Flucloxacillin
- Amoxicillin
- Piperacillin
Give 2 examples of cephalosporins
- Ceftriaxone
- Cefuroxime
Give 2 examples of carbapenums
- Meropenum
- Imipenum
Give 3 examples of macrolides
- Erythromycin
- Azithromycin
- Clarithromycin
Give an example of a tetracycline
Doxycycline
Give 2 examples of an aminoglycoside
- Gentamicin
- Amikacin
Give 2 examples of glycopeptides
- Vancomycin
- Teicoplanin
Give an example of a flouroquinolone
Ciprofloxacin
What does pharmacokinetics describe?
The change in drug and metabolite concentrations in the body over time
What does pharmacodynamics consider?
The concentration of a drug at the site of action and the effect it produces on that site, both in terms of clinical effect and adverse effects, at different concentrations
Why is it important to understand pharmacokinetic-pharmacodynamic profiles for antimicrobial drugs?
It guides dosage and dose frequency
What factors decide dose frequency of antibiotics?
- Half life
- Mechanism of action of antibiotic
Give an example of an antibiotic with a short half life
Penicillins
What is the implication of an antibiotic having a short half life?
It needs to be given more frequently
Give an example of an antibiotic with a very long half life?
Azithromycin
What aspect of a drugs mechanism of action is important when considering dosing intervals?
The way the activity of a drug is affected by it’s concentration
In what ways may the activity of a drug be affected by it’s concentration?
- Activity may be related to time drug exceeds the minimum inhibitory concentration (MIC)
- Activity may be related to the peak antibiotic concentration reached
Give an example of an antibiotic whose activity is related to the time that the concentration exceeds the minimum inhibitory concentration
Penicillin
Give an example of an antibiotic whose activity is related to the peak antibiotic concentration
Gentamicin
What does the therapeutic index of a drug describe?
How likely the drug is to cause toxicity to the host
How is the therapeutic index of a drug calculated?
The maximum tolerated dose divided by the minimum effective dose
What is the minimum effective dose of an antibiotic determined by?
The lowest dose that will give the required MIC at the site of infection
Give an example of class of antibiotic with a high therapeutic index
Beta-lactam agents
What is required for antibiotics with a low therapeutic index?
Serum level monitoring and dose adjustment
Give an example of a class of antibiotics with a low therapeutic index
Aminoglycosides
What are the ways that antibiotics can exert their antimicrobial effects?
- Disruption of bacterial cell wall
- Inhibition of protein synthesis
- Inhibition of DNA replication
- Interruption of microbial chemical pathways
What classes of antibacterial agents exert their actions by disruption of the bacterial cell wall?
- Beta-lactams
- Glycopeptides
How do beta-lactams and glycopeptide agents disrupt the bacterial cell wall?
They prevent cross-linkage of peptidoglycan
What is peptidoglycan?
A key component of the bacterial cell wall
What kind of infections are beta-lactams used to treat?
Predominantly gram +ve infections caused by Streptococci
Which beta-lactam agents have activity against a broader spectrum?
Third-generation cephalosporins
Give an example of a third-generation cephalosporin
Ceftriaxone
Are third generation cephalosporins active against gram -ve or gram +ve organisms?
Can be either
What organisms does ceftriaxone have poor action against?
- Pseudomonas
- Enterococci
What kind of bacteria are glycopeptide antibiotics used to treat?
Gram +ve bacteria only
Why is the use of glycopeptides limited to use against gram +ve bacteria?
The large molecules are not able to penetrate the outer membrane of gram -ve bacteria
What classes of antibiotic exert their actions by inhibiting protein synthesis?
- Macrolides
- Tetracyclines
- Aminoglycosides
- Clindamycin
Where do antibiotics act to inhibit protein synthesis?
At the level of the ribosome
What is the advantage of antibiotics that inhibit protein synthesis?
As a group, they are active against a wide range of bacteria
What organisms are covered by macrolides?
Similar spectrum to penicillin, but also active against Mycoplasma, Mycobacteria, and Chlamydia
What kind of organisms do aminoglycosides have very good action against?
Gram -ve
Which class of antibiotics inhibit DNA replication?
Fluroquinolones
How do fluroquinolone inhibit DNA replication?
They inhibit enzymes involved in coiling and uncoiling of DNA
What kind of organisms do fluroquinolones have good activity against?
Gram -ve
What kind of organisms do fluroquinolones have poor activity against?
Gram +ve organisms such as Streptococci and Staphylococci
Give an example of an antibiotic which works by interrupting microbial chemical pathways
Trimethoprim
How does trimethoprim interrupt microbial chemical pathways?
It inhibits the conversion of dihydrofolate to tetrahydrofolate
What is the result of trimethoprim inhibiting the conversion of dihydrofolate to tetrahydrofolate?
It prevents purine and pyrimidine metabolism
Why do bacteria produce their own folate?
Because they cannot absorb folate from the host
What kind of organisms is trimethoprim active against?
Gram +ve and gram -ve
Why is trimethoprim most commonly used to treat UTIs?
Due to its excretion and high concentrations in the urine compared to blood
What can antibiotics be considered narrow or broad spectrum based on?
The range of bacteria they are active against
When should broad spectrum antibiotics be used?
- When a wide range of bacteria may be responsible for an infection
- When polymicrobial infection may be present
What is meant by bactericidal antibiotics?
Ones that kill the bacteria they are effective against
Give two classes of antibiotics that are bactericidal
- Beta lactams
- Aminoglycosides
Who should bactericidal antibiotics be used in?
- Serious infections
- Immunosuppressed patients
What is meant by bacteriostatic antibiotics?
They inhibit bacterial growth but do not kill them
What do bacteriostatic organisms rely on to kill the bacteria?
The immune system
Give two bacteriostatic antibiotics or classes of antibiotics
- Tetracycles
- Trimethoprim
Where does knowledge of likely sensitivities of bacteria come from?
- Laboratory tests
- Epidemiological data
What are the principles of antimicrobial stewardship?
- Only use antibiotics when there is clinical evidence of bacterial infection
- Obtain cultures before initiation
- Document route, indication, dose, and duration
- Review clinical diagnosis and need for antibiotics daily
- Decide whether to stop, change routes, change antibiotics, continue, or use OPAT
Is bacterial resistance innate or acquired?
Can be either
Give an example of a bacterium that has innate resistance
Pseudomonas
What is pseudomonas innately resistant to?
Penicillin
How can bacteria acquire immunity?
Through a genetic change which results in a survival advantage, which results in the mutated strain of bacteria outgrowing the sensitive population
What is the main driver for emergence of resistant bacteria?
Inappropriate and overdose of antibiotics
Why is inappropriate and overuse of antibiotics the main driver for antibiotic resistance?
Antibiotics exert a considerable selection pressure on bacterial population, favouring populations that are able to withstand them
Why is it important to reduce resistance caused by inappropriate use of antibiotics?
Due to the shortage of new antibiotics, it is essential to maintain the efficacy of current ones
How should the inappropriate use of antibiotics be reduced?
Follow principles of selection of antibiotics and antimicrobial stewardship
What are the main factors when selecting the most appropriate antibiotic?
- Consideration of most likely organisms causing infection
- Knowledge of likely sensitivities of the suspected or isolated organism(s)
- Site of infection
- Illness severity
- Immune status of the host
When is a bacterium considered resistant to an antibiotic?
When its growth cannot be inhibited by a concentration of a drug that is achievable in the blood