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169 Cards in this Set
- Front
- Back
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how do you administer penicillin G? penicillin V?
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- IV
- oral |
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what is the mechanism of action of penicillins?
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- bind penicillin binding protein
- block transpeptidase cross-linking of the cell wall - activate autolytic enzymes all of these contribute to cell wall destruction |
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what are the major side effects of penicillin use?
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- hypersensitivity reactions
- hemolytic anemia |
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which penicillins are resistant to penicillinase?
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- methicillin
- nafcillin - dicloxacillin |
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what can you give as adjunctive therapy with aminopenicillins to allow them to work against bacteria that make penicilliinase?
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clavulanic acid or sulbactam both inhibit penicillinase
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what penicillin family member causes interstitial nephritis?
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methicillin
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what bacteria are amoxicillin and ampicillin used against?
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- gram positive cocci
- H. influenzae - E. coli - Listeria monocytogenes - Proteus mirabilis - Salmonella - Enterococci |
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what class of penicillins are good against pseudomonas infections? name the different members of this class?
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- carboxypenicillins (antipseudomonals)
- Ticarcillin, Carbenicillin, Piperacillin |
|
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how do cephalosporins work?
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these are beta lactam drugs that inhibit cell wall synthesis and are less susceptible to penicillinases
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what bacteria are 1st generation cephalosporins (cefazolin, cephalexin) use to treat?
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- gram positive cocci
- Proteus mirabilis - E. coli - Klebsiella pneuomniae |
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|
how do you administer penicillin G? penicillin V?
|
- IV
- oral |
|
|
what is the mechanism of action of penicillins?
|
- bind penicillin binding protein
- block transpeptidase cross-linking of the cell wall - activate autolytic enzymes all of these contribute to cell wall destruction |
|
|
what are the major side effects of penicillin use?
|
- hypersensitivity reactions
- hemolytic anemia |
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which penicillins are resistant to penicillinase?
|
- methicillin
- nafcillin - dicloxacillin |
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what can you give as adjunctive therapy with aminopenicillins to allow them to work against bacteria that make penicilliinase?
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clavulanic acid or sulbactam both inhibit penicillinase
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|
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what penicillin family member causes interstitial nephritis?
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methicillin
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what bacteria are amoxicillin and ampicillin used against?
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- gram positive cocci
- H. influenzae - E. coli - Listeria monocytogenes - Proteus mirabilis - Salmonella - Enterococci |
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what class of penicillins are good against pseudomonas infections? name the different members of this class?
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- carboxypenicillins (antipseudomonals)
- Ticarcillin, Carbenicillin, Piperacillin |
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how do cephalosporins work?
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these are beta lactam drugs that inhibit cell wall synthesis and are less susceptible to penicillinases
|
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what bacteria are 1st generation cephalosporins (cefazolin, cephalexin) use to treat?
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- gram positive cocci
- Proteus mirabilis - E. coli - Klebsiella pneuomniae |
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what bacteria are 2nd generation cephalosporins (cefoxitin, cefaclor, cefuroxime) used to treat?
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- gram positive cocci
- H. influenzae - Enterobacter aerogenes - Neisseria - Proteus mirabilis - E. coli - Klebsiella pneumoniae - Serratia marcescens |
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what generation of cephalosporin would I give a patient with meningitis? why?
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- 3rd generation
- because they have good blood brain barrier penetration |
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what other class of antibiotics do you not give cephalosporins with due to nephrotoxicity?
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aminoglycosides
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it is ok to consume alcohol while taking a cephalosporin? what will happen?
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- it is not deadly but will cause a disulfiram-like reaction. Disulfiram is Antabuse and makes people very sick
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how does aztreonam work?
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binds to penicillin binding protein 3 and inhibits cell wall synthesis. it is resistant to beta lactamases
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what bacteria is aztreonam used to treat?
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Klebsiella, Pseudomonas, Serratia
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who gets aztreonam?
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patients who are allergic to penicillin and do not tolerate aminoglycosides due to renal insufficiency
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what must you always administer with imipenem? why?
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- cilastatin
- it inhibits renal dihydropeptidase I and prevents inactivation of renal tubules by imipenem |
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how does meropenem work? what other drug works like this?
|
- it is a beta lactam drug that inhibits cell wall synthesis
- imipenem |
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what do you uses meropenem or imipenem for?
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broad spectrum antibiotics for serious infections that you don't know the exact cause of
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what is the major toxicity of meropenem and imipenem when they are at high plasma levels?
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CNS toxicity especially seizures
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how does vancomycin work?
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it inhibits the binding of D-Ala to D-Ala in bacterial cell wall synthesis
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what do you use vancomycin to treat?
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- MRSA
- Coagulation negative endocarditis due to Staph. epidermidis - can be given orally for pseudomembranous colitis (this is because it is not orally absorbed and stays in the gut to kill C. difficile) |
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what are the adverse effects of vancomycin?
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- nephrotoxicity
- ototoxicity - thrombophlebitis - red man syndrome (diffuse flushing) |
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which antibiotics inhibit the 30s ribosomal subunit?
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- Aminoglycosides
- Tetracyclines |
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which antibiotics inhibit the 50s ribosomal subunit?
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- Chloramphenicol
- Erythromycin - Lincomycin - Linezolid |
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name the aminoglycosides?
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- Gentamycin
- Neomycin - Amikacin - Tobramycin -Streptomycin |
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How do aminoglycosides work? are they bactericidal or bacteriostatic?
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- inhibit the formation of the initiation complex and cause misreading of the mRNA at the 30s ribosomal subunit
- they are bactericidal |
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which aminoglycoside is used for bowel surgery?
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Neomycin
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what are the adverse effects of aminoglycosides?
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- nephrotoxic esp. with cephalosporins
- ototoxic - teratogenic |
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what is the clinical use for aminoglycosides?
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gram negative rods
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how does linezolid work?
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binds to the 50s ribosomal subunit and interacts with bacterial initiation complex
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what are the uses for linezolid?
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- MRSA
- Vancomycin resistant Enterococci |
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name the tetracyclines?
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- Tetracycline
- Doxycycline - Demeclocycline - Minocycline |
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which tetracycline can be used as a diuretic in patients with SIADH?
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- Demeclocylcine; it is an ADH antagonist that can be used in SIADH
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how to the tetracyclines work? are they bactericidal or bacteriostatic?
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- bind the 30s ribosomal subunit and prevent attachment of the aminoacyl-tRNA
- they are bacteriostatic |
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what prevents tetracyclines from being absorbed in the gut?
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- divalent cations (Ca, Fe, Mg)
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can tetracyclines be used in pregnancy?
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they are contraindicated
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which tetracycline is safe to use in patients with renal failure?
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doxycycline because it is eliminated fecally
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what infections do the tetracyclines treat?
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- Vibrio cholerae
- Acne - Chlamydia - Ureaplasma urealyticum - Mycoplasma pneumoniae - Tularemia - H. pylori - Borrelia burgdorferi (Lyme disease) - Rickettsia |
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what are the adverse effects of tetracyclines?
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- discoloration of the teeth
- inhibition of bone growth in children - photosensitivity |
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a patient was put on an oral antibiotic for acne control. after being on the medication for a long time his acne got better but now he notices a blue skin discoloration. which antibiotic is he on?
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- Minocycline is a tetracycline that can cause blue skin discoloration with long term use
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name the macrolides?
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- Erythromycin
- Azithromycin - Clarithromycin |
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how do the macrolides work? are they bactericidal or bacteriostatic?
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- they bind the 23s rRNA of the 50s ribosomal subunit and block translocation
- they are bacteriostatic |
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what are the macrolides used for?
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P.U.S. = pneumonias, URIs, STDs
specifically gram positive cocci, mycoplasma, legionella, chlamydia, neisseria |
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what is the most common cause of noncompliance in patients taking macrolides?
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GI discomfort
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which antibiotic puts the patient at an increased risk for Torsades de Pointes?
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macrolides, especially erythromycin, because they prolong the QT interval
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how does Chloramphenicol work?
is it bactericidal or bacteriostatic? |
- inhibits 50s peptidyltransferase activity
- it is bacteriostatic |
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what is chloramphenicol used for?
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- Meningitis = H. influenzae, N. meningiditis, S. pneumoniae
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why do you not give infants chloramphenicol?
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it causes grey baby syndrome because infants lack liver UDP-glucuronyl transferase
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how does clindamycin work? is it bactericidal or bacteriostatic?
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- blocks peptide bond formation at the 50s ribosomal subunit
- it is bacteriostatic |
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what is clindamycin used for?
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- Bacteroides fragilis
- Clostridium perfringens |
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what are the adverse effects of clindamycin?
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- Pseudomonas colitis
- fever - diarrhea |
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name the sulfonamides?
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- Sulfamethoxazole (SMX)
- Sulfisoxazole - Sulfadiazine |
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how do sulfonamides work? are they bactericidal or bacteriostatic?
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- inhibit dihydropteroate
- they are bacteriostatic |
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what do you use sulfonamides for?
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- gram positives
- gram negatives - especially Nocardia and Chlamydia |
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what are the adverse effects of sulfonamides?
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- hypersensitivity reactions
- hemolysis in G6PD deficient patients - nephrotoxic - kernicterus in infants - steven's johnson syndrome |
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what is dapsone?
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an antibacterial that is structurally different from sulfonamides but works the same way by inhibiting dihydropteroate synthase
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how does trimethoprim work? is it bactericidal or bacteriostatic?
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- inhibits bacterial dihydrofolate reductase
- it is bacteristatic |
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what do you use trimethoprim for?
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in combination with sulfonamides to treat:
- recurrent UTIs - Shigella - Salmonella - Pneumocystis jiroveci pneumonia |
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what are the adverse effects of trimethoprim? how can you alleviate these?
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- megaloblastic anemia, leukopenia, granulocytopenia
- give folinic acid |
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which drugs should patients with sulfa allergies avoid?
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- sulfonamides
- sulfasalazine - sulfonylureas - thiazides - acetazolamide - furosemide |
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how does nitrofurantoin work? is it bactericidal or bacteriostatic?
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- gets reduced by bacterial proteins to a reactive intermediate that inhibits bacterial ribosomes
- it is bactericidal |
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a pregnant woman has a UTI. what should you give her and why?
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- nitrofurantoin
- because it does not become active until it reaches the urine |
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name the fluoroquinolones?
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- Ciprofloxacin
- Norfloxacin - Ofloxacin - Sparfloxacin - Moxifloxacin - Gatifloxacin - Enoxacin - Nalidixic acid (a quinolone) |
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how do the fluoroquinolones work? are they bactericidal or bacteriostatic?
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- inhibit bacterial DNA gyrase (topoisomerase II)
- they are bactericidal |
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what are fluoroquinolones good for?
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- gram negative rods of the urinary and GI tracts including Pseudomonas, Neisseria, and some gram positives
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what are the adverse effects of fluoroquinolones?
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- tendonitis/tendon rupture
- leg cramps - myalgias |
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how does Metronidazole work?
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- it forms toxic metabolites in the bacterial cell that damages bacterial DNA
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what is Metronidazole good for?
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- Giardia
- Entamoeba - Trichomonas - Gardnerella vaginalis - Anaerobes (Bacteroides, Clostridium) - H. pylori |
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what are the adverse effects of Metronidazole?
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- Disulfiram like reaction with EtOH
- metallic taste |
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how does Polymixin B and Polymixin E work?
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they bind to cell membranes of bacteria and disrupt their osmotic properties
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what do we use Polymixins for?
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resistant gram negative infections
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what are the adverse effects of Polymixins?
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- Neurotoxicity
- Acute Renal Tubular Necrosis |
|
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what drug is used for prophylaxis of TB?
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Isoniazid
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what drug(s) is/are used for the treatment of TB?
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- Isoniazid
- Rifampin - Pyrazinamide - Ethnambutol - Streptomycin these are used in combinations never alone |
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why are the aminoglycosides ineffective against anaerobic bacteria?
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because they require O2 for uptake
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what drug do you use for prophylaxis against M. avium-intracellulare? what population of people would you give this to?
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- Azithromycin
- people with AIDS |
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how do you treat M. avium-intracellulare?
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- Azithromycin, Rifampin, Ethambutol, and Streptomycin all together
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how do you treat M. leprae?
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- Dapsone
- Rifampin - Clofazimine these are all used together |
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a patient has active TB. they were started on a drug regiment recently and now have difficulty with color vision. which drug is causing this?
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ethambutol causes optic neuropathy and/or decreased visual acuity
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how does isoniazid work?
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it decreases the synthesis of mycolic acids
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what are the adverse effects of isoniazid?
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- neurotoxicity (can be prevented by vitamin B6)
- hepatotoxicity - drug induced lupus |
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how does Rifampin work?
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inhibits DNA dependent RNA polymerase
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a patient was put on an antibiotic for chemoprophylaxis for H. influenzae type B. they come to you worried because they are sweating and urinating orange. what drug are they on?
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Rifampin
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how do bacteria become resistant to penicillins and cephalosporins?
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- beta lactamases
- alteration of penicillin binding proteins in the case of MRSA or S. pneumoniae |
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how do bacteria become resistant to vancomycin?
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replace the terminal D-Ala with a D-Lac
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how do bacteria become resistant to aminoglycosides?
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they modify the drug via acetylation, adenylation, or phosphorylation
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how do bacteria become resistant to chloramphenicol?
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modification via acetylation
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how do bacteria become resistant to macrolides?
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methylation of rRNA near erythromycin's ribosome binding site
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how do bacteria become resistant to tetracyclines?
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they decrease uptake or increase transport out of the cell
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how do bacteria become resistant to sulfonamides?
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they alter the bacterial dihydropteroate synthetase, decrease uptake, or increase PABA synthesis
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how do bacteria become resistant to fluoroquinolones?
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they alter the DNA gyrase or reduce uptake
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how does amphoteracin B work?
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- it binds ergosterol and forms membrane pores that allow leakage of electrolytes
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what is amphoteracin B used for?
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wide spectrum of systemic mycoses
- Cryptococcus - Blastomyces - Coccidiodies - Aspergillus - Histoplasma - Candida - Mucor |
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what are the adverse effects of amphoteracin B?
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- fever and chills
- hypotension - IV phlebitis - hepatotoxic - arrhythmias - nephrotoxic (can be reduced by hydration) |
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how does nystatin work?
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it binds ergosterol and disrupts the fungal membrane
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how is nystatin administered?
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-topical or swish-and-swallow. it is too toxic for IV use
|
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what is nystatin used to treat?
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Candida; oral, skin, vaginal
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name the azoles?
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- Fluconazole
- Ketoconazole - Clotrimazole - Miconazole - Itraconazole - Voriconazole |
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how do the azoles work?
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inhibit the conversion of lanosterol to ergosterol
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what do you use azoles to treat?
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systemic mycoses
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an AIDS patient has cryptococcal meningitis. what do you treat them with?
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Fluconazole
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what do you use Ketoconazole to treat?
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- Blastomyces
- Coccidiodies - Histoplasma - Candida albicans |
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what are the adverse effects of the azoles?
|
- gynecomastia
- liver dysfunction |
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how does flucytosine work?
|
it gets converted to 5-fluorouracil and inhibits DNA synthesis
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what is flucytosine used for?
|
systemic fungal infections with amphoteracin B
|
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what are the adverse effects of flucytosine?
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- bone marrow suppression
- nausea - vomiting |
|
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how does capsofungin work?
|
it inhibits the synthesis of beta-glucan which inhibits cell wall synthesis
|
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what is capsofungin used for?
|
invasive aspergillosis
|
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how does griseofulvin work?
|
it interferes with microtubule formation disrupting mitosis
|
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|
what is griseofulvin used for?
|
- superficial infections
- inhibits the growth of dermatophytes |
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what are the adverse effects of griseofulvin?
|
- teratogenic
- carcinogenic - confusion - increased P450 which increases warfarin metabolism |
|
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what is terbinafine used to treat?
|
- dermatophytoses esp. onychomycosis and tinea capitus
terbinafine is also called Lamasil |
|
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how does terbinafine work?
|
it inhibits the fungal enzyme squalene epoxide which converts squalene to lanosterol. this inhibits ergosterol synthesis and thus cell wall synthesis
|
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how does Amantadine work?
|
it blocks the M2 protein on viruses and prevents uncoating and penetration
|
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what is Amantadine used for?
|
- prophylaxis and treatment of influenza A
- Parkinson's: it causes the release of dopamine from nerves |
|
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what are the side effects of amantadine?
|
- ataxia
- dizziness - slurred speech - anti-cholinergic |
|
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what is Rimantidine?
|
it is a derivative of amantadine with fewer CNS side effects because it does not cross the BBB
|
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how is resistance to Amantadine confered?
|
mutated M2 protein. 90% of influenza A viruses are resistant so we don't use it any more
|
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how does Zanamivir and Oseltamivir work?
|
they inhibit influenza neuraminidase which decreases the release of progeny virus
|
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what is Oseltamivir and Zanamivir used for?
|
influenza A and B and Avian Influenza (H5N1)
|
|
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how does Ribavirin work?
|
it competitively inhibits IMP dehydrogenase which blocks the synthesis of guanine nucleotides
|
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when do we use Ribavirin?
|
chronic hepatitis C with interferon alpha
|
|
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what are the adverse effects of Ribavirin?
|
- hemolytic anemia
- severely teratogenic |
|
|
how does acyclovir work?
|
it is a guanosine analog that i monophosphorylated by HSV/VSV thymidine kinase and inhibits viral DNA polymerase by chain termination
|
|
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what are 2 drugs that work the same way as acyclovir?
|
- Valacyclovir
- Famcyclovir |
|
|
what is acyclovir used to treat?
|
- HSV
- VSV - EBV it is not effective against latent infections, only active infections |
|
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what is the major side effect with acyclovir? how do you prevent it?
|
- at high concentrations it crystalizes in the kidneys and is nephrotoxic
- give aggressive IV hydration to prevent this |
|
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what is the mechanism of resistance against acyclovir?
|
virus lacks thymidine kinase
|
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how does gancyclovir work?
|
it is a guanosine analog that is monophosphated by CMV viral kinase or HSV/VSV thymidine kinase and inhibits viral DNA polymerase
|
|
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what is gancyclovir used for?
|
CMV
|
|
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how do viruses become resistant to gancyclovir?
|
mutated CMV DNA polymerase or lack of thymidine kinase
|
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how does foscarnet work?
|
it binds to the pyrophosphate binding site of viral DNA polymerase inhibiting the enzyme
|
|
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what do we use foscarnet for?
|
CMV when gancyclovir fails and HSV when acyclovir fails
|
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what is the mechanism of resistance for foscarnet?
|
mutated viral DNA polymerase
|
|
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what are the HIV therapy classes?
|
- protease inhibitors
- nucleoside reverse transcriptase inhibitors - non-nucleoside reverse transcriptase inhibitors - fusion inhibitors |
|
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name the protease inhibitors?
|
- Saquinaivr
- Ritonavir - Indinavir - Nelfinavir - Amprenavir |
|
|
name the nucleoside reverse transcriptase inhibitors?
|
- Zidovudine
- Didanosine - Zalcitabine - Stavudine - Lamivudine - Abacivir |
|
|
name the non-nucleoside reverse transcriptase inhibitors?
|
- Nevirapine
- Efavirenz - Delavirdine |
|
|
name the fusion inhibitors?
|
Enfuvirtide
|
|
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how do the protease inhibitors work?
|
they inhibit maturation of new virus by blocking protease in progeny virion
|
|
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what are the side effects of protease inhibitors?
|
- hyperglycemia
- thrombocytopenia (esp. indinavir) - lipodystrophy (HAMMAS; buffalo hump, redistribution of fat) |
|
|
which anti-HIV drug can cause a false positive cannabinoid test?
|
Efavirenz
|
|
|
how do the reverse transcriptase inhibitors work?
|
- preferentially inhibit reverse transcriptase of HIV
- prevent the incorporation of the DNA copy of the viral genome into the host DNA |
|
|
what are the adverse effects of HIV reverse transcriptase inhibitors?
|
- bone marrow suppression (give GM-CSF and epo)
- peripheral neuropathies - lactic acidosis (nucleosides) - pancreatitis - megaloblastic anemia |
|
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what is Zidovudine's main toxicity?
|
bone marrow suppression
|
|
|
which HIV drugs cause hepatic steatosis?
|
Didanosine and Stavudine
|
|
|
which HIV drugs cause confusion and crazy dreams?
|
Non-nucleoside reverse transcriptase inhibitors
|
|
|
what do you use for HIV prophylaxis or during pregnancy to reduce the risk of fetal transmission?
|
Zidovudine plus Lamivudine
|
|
|
what is Highly Active AntiRetroviral Therapy?
|
the treatment for AIDS (white count < 500) or a high viral load
it consists of a combination of protease inhibitors and reverse transcriptase inhibitors |
|
|
how do HIV fusion inhibitors work?
|
bind to viral gp41 and prevent the conformational change needed for cell penetration
|
|
|
what are the adverse effects of HIV fusion inhibitors?
|
- hypersensitivity reactions
- reactions at injection site - increased risk of bacterial pneumonia |
|
|
when do we use HIV fusion inhibitors?
|
in HIV positive patients with persistent viral replication in spite of antiretroviral therapy
|
|
|
how do the interferons work?
|
- block various stages of viral RNA and DNA synthesis
- induce ribonuclease that degrades viral mRNA |
|
|
what is interferon alpha used for?
|
- chronic hepatitis B
- chronic hepatitis C with Ribavirin - Kaposi's sarcoma |
|
|
what is interferon beta used for?
|
treatment for multiple sclerosis
|
|
|
what is interferon gamma used for?
|
treatment for NADPH oxidase deficiency
|
|
|
what antimicrobials should be avoided during pregnancy?
|
- sulfonamides
- aminoglycosides - fluoroquinolones - erythromycin - clarithromycin - metronidazole - tetracyclines - ribavirin - griseofulvin - chloramphenicol |
