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Antibiotics II
N/A
93
Pharmacology
Graduate
02/20/2010

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Term
Which drugs are the non-beta lactam cell-wall synthesis inhibitors?
Definition
Vancomycin, Bacitracin, Fosfomycin, Cycloserine
Term
Does Vancomycin target gram (+) or gram (-) bacteria?
Definition
Gram (+)
Term
Which drug works by binding to glycoprotein subunit dialanine residues to inhibit cell-wall synthesis
Definition
Vancomycin
Term
What are the side effects of Vancomycin?
Definition
  1. Nephrotoxicity
  2. Ototoxicity
  3. Histamine release (red man or red neck syndrome)
Term
How do bacteria develop resistance to Vancomycin?
Definition
Replace dialanine residues with lactict acid
Term
What drug is a synthetic lipoglycoprotein analogue of Vancomycin that disrupts bacterial membranes?
Definition
Televancin
Term
Which drug inhibits recycling of bactoprenol?
Definition
Bacitracin
Term
How is Bacitran administered, and why?
Definition
Topically. It is severely nephrotoxic systemically.
Term
Which drug inhibits synthesis of N-acetylglucosamine from N-acetyl muramic acid?
Definition
Fosfomycin
Term
What types of bacteria does Fosfomycin target?
Definition
Gram (-) and some gram (+); used for UTI's
Term
Which drug inhibits incorporation of dialanine residues into N-acetyl muramic acid?
Definition
Cycloserine
Term
What types of bacteria does Cycloserine target?
Definition
Gram (+), gram (-); used for TB
Term
Side effects of Cycloserine?
Definition
Headache, sedation, tremor, psychosis
Term
Which drugs are the Macrolides?
Definition
Erythromycin, Clarithromycin, Azithromycin
Term
What is the mechanism of action for Macrolides?
Definition
Reversibly bind to 50S subunit to prevent translocation of the peptidyl RNA to P site
Term
Are Macrolides bacteriostatic or bacteriocidal?
Definition
Bacteriostatic
Term
What are the side effects of Erythromycin?
Definition
  1. GI upset
  2. Ototoxic
  3. Inhibits CYP450
Term
What types of bacteria do Macrolides target?
Definition
Gram (+)
Term
What is the mechanism of action for aminoglycosides?
Definition
Irreversibly binds to the 30S subunit of bacterial RNA, causes mRNA misreading
Term
Are Aminoglycosides bacteriocidal or bacteriostatic?
Definition
Bacteriocidal
Term
What are the Aminoglycosides?
Definition
Gentamicin, Tobramycin, Neomycin, Amikacin, Kanamycin, Netilimicin
Term
Which Aminoglycoside is applied topically due to nephrotoxicity?
Definition
Neomycin
Term
How are most Aminoglycosides administered, and why?
Definition
Intramuscularly or parenterally; they are highly basic sugars that cannot cross membranes
Term
What types of bacteria do Aminoglycosides target?
Definition
Gram (+)
Term
What are the side effects of Aminoglycosides?
Definition
  1. Ototoxicity
  2. Nephrotoxicity
  3. Neuromuscular blockade
  4. Fetal damage
Term
Which class of antibiotic is responsible for the highest incidence of nephrotoxicity?
Definition
Aminoglycosides
Term
Name the Tetracyclines
Definition
Doxycycline, Minocycline, Tigecycline
Term
What is the mechanism of action for the Tetracyclines?
Definition
Binds reversibly to the 30S subunit of bacterial ribosomes, inhibiting the binding of tRNA to the A site
Term
How are Tetracyclines adminstered?
Definition
Orally or parenterally
Term
Are Tetracyclines bacteriostatic or bacteriocidal?
Definition
Bacteriostatic
Term
What are the side effects of Tetracyclines?
Definition
  1. Binds to cations including calcium
  2. Can cause bone deformation and mottled teeth of newborns
  3. Renal and hepatotoxicity
  4. Photosensitive and can degrade into renal and hepatotoxic compounds
Term
What types of foods are contraindicated with Tetracyclines?
Definition
Dairy
Term
What types of bacteria do Tetracyclines target?
Definition
Gram (+), some gram (-), Rickettsia (Rocky Mountain Spotted Fever), Spirochetes (Lyme disease and Syphilis), Helicobacter, Legionella
Term
What class of pregnancy-contraindicated drugs are Aminoglycosides?
Definition
Class D (risks = benefits)
Term
How are Tigecycline and Minocycline related?
Definition
Tigecycline is a broad-spectrum glycylglycine derivative of minocycline
Term
What is the mechanism of action for Chloramphenicol?
Definition
Inhibits 50S associated peptidyltransferase -- peptides cannot be transfered from tRNA to growing peptide chain
Term
What are the side effects of Chloramphenicol?
Definition

1. Blood dyscrasias

2. Gray baby syndrome

3. Hemolytic anemia in patients with G6PD deficiency

Term
How does Chloramphenicol cause cardiovascular collapse in newborns?
Definition
It is metabolized by liver UDP glucuronyl transferase, which is low in newborns
Term
Chloramphenicol targets which organisms?
Definition
Salmonella, beta lactam resistant organisms
Term
Which drug is used sparingly in the US but widely in underdeveloped countries?
Definition
Chloramphenicol
Term
Name the Lincosamides
Definition
Clindamycin, Lincomycin
Term
What is the mechanism of Lincosamides?
Definition
Same as Erythromycin -- bind reversibly to 50S subunit of ribosomes to prevent transfer of tRNA to P site
Term
What are the side effects of Lincosamides?
Definition
C. Diff
Term
What are the targets of Lincosamides?
Definition
Gram (+) and gram (-) anaerobic infections, used prophylactically in dental patients with heart valve problems to prevent endocarditis
Term
What are the Streptogramins?
Definition
Quinupristin + Dalfopristin = Synercid
Term
How are Streptogramins administered?
Definition
Intravenously
Term
What is the mechanism of Streptogramins?
Definition
Quinupristin blocks both A and P sites of bacterial ribosomes; Dalfopristin blocks the P site
Term
What class of drug is Linezolid?
Definition
Oxazolidnones
Term
What is the mechanism of the Oxazolidnones?
Definition
Binds to 50S to inhibit the binding of met tRNA to the P site
Term
What are the side effects of the Oxazolidnones?
Definition
  1. Anemia
  2. Thrombocytopenia
  3. C. Diff
Term
What are the targets of Oxazolidnones?
Definition
Gram (+), including MRSA
Term
What antibiotics target protein synthesis?
Definition
Macrolides, Aminoglycosides, Tetracyclines, Chloramphenicol, Lincosamides, Streptogramins, Oxazolidnones, Mupirocin, Retapamulin
Term
What is the mechanism of Daptomycin?
Definition
Lipopeptide that disrupts the bacterial wall by forming pores in the membrane
Term
What are the side effects of Daptomycin?
Definition
Muscle pain and weakness
Term
What are the targets of Daptomycin?
Definition
Gram (+) bacteria, used for skin and soft tissue infections
Term
Of what class of drugs is Ciprofloxacin?
Definition
Fluoroquinolones
Term
What is the mechanism of Fluoroquinolones?
Definition
Inhibit bacterial topoisomerase II and IV without affecting mammalian topoisomerase
Term
What are the side effects of Fluoroquinolones?
Definition

1. Can damage developing cartilage -- Pregnancy category C (risks < benefits)
2. Tendonitis
3. Achilles tendon rupture

Term
What are the targets of Fluoroquinolones?
Definition
Gram (+), gram (-), acid fast bacteria
Term
What antibiotics act as antimetabolites?
Definition
Sulfonamides and Trimethoprim
Term
In what class of drugs is sulfisoxazole?
Definition
Sulfonamides
Term
What is the mechanism of action of the Sulfonamides?
Definition
Blocks purine synthesis: para-aminobenzoic acid analogues that reversibly inhibit dihydropteroate synthetase, preventing synthesis of THF
Term
What are the side effects of Sulfonamides?
Definition
  1. Stevens-Johnson syndrome
  2. Hemolytic anemia in G6PD deficient patients
  3. Displaces bound bilirubin in infants, causing jaundice
Term
What types of infections do Sulfonamides target?
Definition
UTI's
Term
Mechanism of Trimethoprim?
Definition
Blocks purine synthesis: inhibits dihydrofolate reductase, preventing synthesis of folic acid to dihydrolic acid and then to tetrahydrofolic acid
Term
What are the side effects of Trimethoprim?
Definition
  1. Megaloblastic anemia
  2. Leukopenia
  3. Granulocytopenia
Term
How can the side effects of Trimethoprim be mitigated?
Definition
Leucovorin, a folinic acid that does not require dihydrofolate reductase in order to be converted to THF
Term
Trimethoprim targets which organisms?
Definition
Gram (-) and organisms that cause UTI's
Term
What drugs are prodrugs that are converted to active form by their targets?
Definition
Nitrofurantoin and Metronidazole
Term
How is Metronidazole administered?
Definition
Intravenously
Term
For what types of infections is Metronidazole given?
Definition
Severe anaerobic infections
Term
What are the side effects of Metronidazole?
Definition
Causes seizures at high doses
Term
What is the mechanism of Metronidazole?
Definition
It is converted to a highly reactive free radical when taken up by obligate anaerobes
Term
What are the targets of Nitrofurantoin?
Definition
UTI's caused by E. Coli and S. aureus
Term
What are the side effects of Nitrofurantoin?
Definition
  1. Cough, chest pain
  2. Brown urine
  3. Hemolytic anemia in G6PD deficient patients
Term
Which antibiotics are contraindicated in pregnancy?
Definition
Fluoroquinolones, Tetracyclines, Aminoglycosides
Term
Which antibiotics are used topically?
Definition
Polymyxin B, Gramicidin, Mupirocin, Retapamulin, Neomycin, Bacitracin
Term
What is the mechanism of Polymyxin B?
Definition
Binds to negatively charged sites on LPS to increase membrane permeability
Term
What are side effects of Polymyxin if it is used systemically?
Definition
  1. Nephrotoxicity
  2. Neurotoxicity; can cause neuromuscular blockade
Term
What are the targets of Polymyxin B?
Definition
Gram (-)
Term
What is the mechanism of Gramicidin?
Definition
3 peptide-mixture that form pores in bacterial membranes
Term
What types of organisms does Gramicidin target?
Definition
Gram (+)
Term
What are the side effects of systemic Gramicidin use?
Definition
Severe toxicity for all organs
Term
What is the mechanism of Mupirocin?
Definition
Inhibits protein synthesis by inhibiting isoleucyl tRNA synthetase
Term
What organisms does Mupirocin target?
Definition
Staphylococcus aureus and Streptococcus pyrogenes
Term
What is the mechanism of Retapamulin?
Definition
Blocks P sites on ribosomes
Term
What are the targets of Retapamulin?
Definition
Impetigo (staphylococcus aureus and streptococcus pyrogenes)
Term
Neosporin consists of...
Definition
Neomycin, Polymixin, and Gramicidin
Term
Polysporin consists of...
Definition
Polymixin and Bacitracin
Term
Polytrim consists of...
Definition
Trimethoprim and polymixin
Term
Terak consists of...
Definition
Oxytetracycline and polymixin
Term
What drugs can cross the CNS?
Definition
3rd generation Cephalosporins, Cycloserine, Tetracyclines, Chloramphenicol
Term
What non-bacterial condition is Erythromycin used to treat?
Definition
Gastroparesis
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