Antimicrobial Drugs, September 7th Flashcards
What are the main Classes of Cephalosporins and how do we distinguish them by name?
Class 1 have PHA/FA in their names Class 2 are random Class 3 contain ONE/TEN/IME at the ends Class 4 contain PI in it Class 5 contain ROL in it
The classes become more capable of dealing with Gram Negative Bacteria as they develop
Which agent that inhibits Protein Synthesis is Bactericidal?
Aminoglycosides
Give two examples of Aminoglycosides
Gentamicin and Amikacin
Give three examples of Macrolides
Azithromycin, Clarithromycin, Erythromycin
What is the Mechanism of Action of Aminoglycosides
Acts upon the 30S subunit on the ribosomes
What bacteria can Aminoglycosides affect?
Gram (+) (Staph) and Gram (-); Anti-pseudomonal
How are Aminoglycosides administered and what is the dosage?
IV Once a Day or TDS/BD (2/3)
What are the main side effects of Aminoglycosides
- Nephrotoxicity (Reversible)
- Ototoxicity (Vestibular is Reversible, Auditory not)
- NMJ Blockage at high dose
- Damages Eighth Nerve in Pregnancy
What are the main interactions of Aminoglycosides
Increased Nephrotoxicity with:
- Vancomycin
- Colistin (Polymyxin)
- Ambisome (Antifungal)
What is the Mechanism of Action of Macrolides
Acts upon the 50S subunit on the ribosomes
What bacteria can Macrolides affect?
Gram (+) and usually H.influenzae
How are Macrolides administered and what is the dosage
Oral and IV (Can cause Thromboplebitis)
Once or Twice a Day
Which Macrolide has shown excellent intracellular penetration
Azithromycin
What are the main side effects in Macrolides
Though safe in Children, it can:
- Erythromycin Inhibits P450
- Prolong QT
- Nausea and Vomiting
- Abdominal Pain
- Liver toxicity
Which bacteria are known to cause resistance in Aminoglycosides
Gram Negative Organisms (Acquired)
Which bacteria are known to cause resistance in Macrolides
Both Staphs and Streps
What drugs can affect Nucleic Acid Metabolism
- Quinolones (Ciprofloxacin Moxifloxacin, Levofloxacin)
- Rifampicin
- Metronidazole (Good against most Anaerobes)
What is the Mechanism of Quinolones
Inhibits DNA Gyrase and kills Bacteria
What types of Bacteria do Quinolones affect?
Gram + : Staph, not Streps
Gram - : Anti-pseudomonal too
How are Quinolones administered and what is the dosage?
Oral and IV
Twice a Day
What are the main side effects of Quinolones?
- Ruptures Tendons
- Photosensitivity
- Seizures and Prolonged QT
Human cells are known to not synthesise _____ and will lack _____?
Folic Acid
Lack Dihydropteroate Synthase
What are examples of Antifolates?
Sulphonamides
Trimethoprim
What is the mechanism of action of Sulphonamides?
Inhibiting Dihydropteroate Synthase
What is the mechanism of action of Trimethoprim?
Inhibiting Dihydrofolate Reductase
What types of drugs can affect the Membranes of Bacteria?
- Colistin (Polymyxin)
- Amphotericin (Antifungals)
- Daptomycin
What are qualities required for the IDEAL antibiotic?
- Magic Bullet (Selectively kills MO without harming body/microbiome)
- Reach and Concentrates within the Target Organ
- Reach good levels in Infected Body Fluids
- Non-Toxic
- Cheap
- No selection of resistance
Which antibiotics have the greatest influence throughout the Antimicrobial Spectrum?
Meropenem and Imipenem have the greatest, affecting both Gram Positive and Negative Bacteria
Which Antibiotics in the Antimicrobial Spectrum can only affect Gram Positive Bacteria?
Benzyl Penicillin
Flucloxacillin
Vancomycin/Teicoplanin (Glycopeptides)
What are the main infection issues with Antimicrobial Resistance?
- UTI
- RTI
- N. gonorrhoea
- M. tuberculosis
- Diarrhoea
What are the main reasons for Antimicrobial resistance in regards to specific drugs and bacteria?
- Multidrug Resistance
- Penicillin Resistance
- Beta-lactamase producing Coliforms
- Resistant Pneumococci and H.influenzae
- Resistant Salmonella and Shingles
What are some of the most dangerous resistant bacteria in Hospitals?
- MRSA
- Coagulase-Negative Staph
- Multi-resistant Enterococci
- Multi-resistant Gram Negative Rods
a. Pseudomonas, Klebsiella, Enterobacter, Acinetobacter
What is the difference between Synergistic and Antagonistic Combinations?
Synergistic: Combined activity > Sum of individual (Beta Lactam + Aminoglycoside)
Antagonistic: Activity of 1 drug is compromised by the other (Tetracylcine/Chloramphenicol with Beta-Lactam or Aminoglycoside, or Two Beta Lactams)
Which types of Drugs are mostly ANTI-GRAM Positive?
- Penicillins
- Fusidic Acid
- Macrolides
- Clindamycin
- Glycopeptides
- Oxazolidinones
- Daptomycin
Which types of Drugs are mostly ANTI-GRAM Negative?
- Trimethoprim
- Polymyxin (Colistin)
- Monobactams (Aztreonam)
- Aminoglycosides (Good against Strep, Staph, Enterococci too)
- Temocillin
What Drugs are Broad Spectrum Antimicrobials?
Beta Lactams
- Carbapenems
- Amoxicillin/Clavulanate
- Piperacilin/Tazobactam
- Cephalosporins
- Chloramphenicol
- Tetracycline (Spirochaetes)
(These two can deal with +/-/Atypicals/Anaerobes)
Which Drugs act upon the Cell Wall?
Beta Lactams
- Penicillin
- Cephalosporins
- Carbapenems
- Aztreonam
Glycopeptides
- Vancomycin
- Teicoplanin