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152 Cards in this Set
- Front
- Back
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Basic structure of penicillins
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a dicyclic nucleus that consist of a thiazolidine ring connected to a beta-lactam ring
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Classified into subgroups on the basis of
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their structure, beta-lactamase susceptibility, and spectrum of activity.
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how do penicillins work?
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Interfere with the synthesis of peptidoglycan which is an essential component of cell walls of susceptible bacteria
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which type of Gram bacteria are suceptible to penicillins?
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G+ such as streptoccoci, staphylococcus aureus
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what kinds of infections are penicillins used for? (3)
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Pneumococcal, streptococcal and meningococcal infections
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High doses of penicillin G in renal patients causes what?
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hyperkalemia and neurotoxicity
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10 million units of Penicillin G contains how much potassium?
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16 meq of potassium
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which route would you never give penicillins via? what does it cause?
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intrathecal-convulsant
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procaine is added to penicillin to do what?
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prolong penicillin
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how much procaine can be added to penicillin?
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120mg of procaine for every 300,000 units of penicillin
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penicillin excretion is via what organ?
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kidney
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which penicillins are not susceptible to hydrolysis by staphyloccoccal penicillinases that would otherwise hydrolyze the cyclic amide bond of the beta-lactum ring and render the antimicrobial inactive?
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Methicillin, oxacillin, nafcilin, cloxacillin, dicloxacillin
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examples of 2nd generation penicillins (3)
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Ampicillin, amoxicillin, carbenicillin
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Carbenicillin side effects
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CHF, metabolic alkalosis, hypokalemia, prolong bleeding time with normal platelet count
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carbenicillin has how much sodium?
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30-40g of sodium
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what is responsible for the side effects of cabenicillin?
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sodium content
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cephalosporin mechanism of action
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Inhibit bacterial cell wall synthesis
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do cephalosporins cross placenta?
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yes
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cephalosporins are used for what kind of cases? (5)
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CV, orthopedic, biliary, pelvic, and intraabdominal surgeries
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First generation cephalosporin, blood levels, and elimination
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Cefazolin-achieves higher blood levels and slower renal elimination
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Second generation cephalosporin, activity againsr Gram negative bacteria
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Cefoxitin-extended activity against gram negative bacteria
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Third generation cephalosporin and effect on beta-lactamases
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cefixine-resist hydrolysis by beta-lactamases.
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Choice of which generation of drug to use depends on what?
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the type of organism likely to be found during surgery
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cefazolin (Ancef) is given for procedures that have a likelihood of what kind of infection?
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Staff infections (gram +).
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Cefoxitin (Mefoxin) a second generation, is likely to be used in what kind of procedures and why?
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GI tract procedures because of its increased gram negative activity
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cephalosporin % of cross reactivity with penecillin?
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20%
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Is there a reliable skin test to predict allergic reactions to cephalosporins?
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no
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should patients who have had a recent severe, immediate reaction to a penicillin be given a cephalosporin?
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no, or if so with great caution
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A positive Coombs reaction appears frequently in patients who receive large doses of which kind of antibiotic?
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cephalosporin
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Imipenem is effective against what kind of bacteria?
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Effective against gram positive and gram negative bacteria
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Broadest spectrum of any beta-lactam antibiotic is which antibiotic?
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Imipenem
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Aztreonam is effective against what kind of bacteria?
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Effective only against gram negative bacteria
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what is notable about the structure of aztreonam?
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Lacks other chemical structures common to penicillins and cephalosporins
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Clavulanic acid is produced by what organism?
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Streptomyces clavuligerus.
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Clavulanic acid class
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β-lactamase inhibitor
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β-lactamase action
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inactivates most penicillins
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Clavulanic acid binding
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irreversible
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Clavulanic acid usually added to which drugs to create which drugs?
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ticarcillin (Timentin) and ampicillin (augmentin)
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Sulbactam class
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beta-lactamase inhibitor
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Sulbactam + ampicillin =
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unasyn
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Dosage of which drug must be adjusted for patients with impaired renal function?
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unasyn
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unasyn treats which kinds of microbes?
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gram-positive cocci
lactamase-producing strains of S. aureus gram-negative aerobes anaerobes |
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which types of Gram-negative aerobes are not suceptible to unasyn?
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resistant strains of E. coli or Pseudomonas
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unasyn is used for what type of infections?
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mixed intra-abdominal and pelvic infections.
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aminiglycosides are effective against what type of micribes?
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Gram negative
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effect of Renal excretion of aminoglycosides in patients with renal failure
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elimination can increase up to 40 fold
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Streptomycin older uses
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first, used for tularemia, and bubonic plague.
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Streptomycin modern use
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Used to Tx TB
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Gentamicin is effective against which microbes? (2)
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p. aeruginosa and gram- bacilli.
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Gentamicin penetrates which types of fluids?
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Penetrates pleural, ascitic, synovial fluids in the presence of inflammation.
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what is important to monitor while on gentamicin
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auditory function
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Gentamicin toxic dose
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>9mcg/mL
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aminoglycosides mechanism of action
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bactericidal inhibitors of protein synthesis
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resistance to aminoglycosides can occur when what happens?
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Mutations affecting proteins in the bacterial ribosome (which is the target for aminoglycosides)
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What are aminoglycosides produced from?
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Aminoglycosides are natural products or semisynthetic derivatives of compounds produced by a variety of soil actinomycetes
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Streptomycin was first isolated from a strain of what?
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Streptomyces griseus
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Gentamicin and netilmicin are derived from species of?
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the actinomycete Micromonospora
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qhich drugs affect th eototoxicity effects of aminoglycosides? (2)
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furosemide and mannitol
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renal side effect of aminoglycosides
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Nephrotoxicity
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aminoglycoside effect on acetylcholine
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decreases Ach which causes muscle weakness
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use aminoglycosides in caution with patients with what type of disease?
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myasthenia gravis
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aminoglycoside effect on nondepolarizing neuromuscular blocking drugs
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Potentiates, increased duration
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aminoglycoside + lidocaine =
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increased blockade
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class of drug that has risk of super-infection with high doses
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tetracyclines
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tetracyclines use (2)
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rickettsal and mycoplasma pneumonia
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Long acting tetracycline
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doxycycline
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class of patients not to receive tatracyclines and reason
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children and pregnant women, discolors teeth of children/fetus
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are macrolides bacteriostatic or bacteriocidal?
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Bactereostatic but can be bactericidal in high doses
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macrolides mechanism of action
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Inhibit protein synthesis in sensitive organisms
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macrolides are distributed where with exception of which two areas?
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Most of this class of drugs distributes widely in most tissues except brain and CSF
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erythromycin class
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macrolide
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type of microbes suceptible to erythromycin
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most gram- and gram+ bacteria,
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erythromycin use
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treatment for atypical pneumonia.
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macrolides common GI side effects (3)
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GI upset , cholinergic stimulation-accelerated gastric emptying, increased lower esophageal sphincter tone
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macrolides effect on heart
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long Q-T interval syndrome,
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macrolides effect on ears
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tinnitus
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what class of antimicrobials can cause IV thrombophlebitis?
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macrolides
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Clindamycin class
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Lincosamides
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clindamycin effect against anaerobic bacteria in comparison to erythromycin
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More active
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clindamycin major effect on GI system
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severe pseumembranous colitis
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large doses of this drug causes long-lasting neuromuscular blockade in the absence of non-depolarizing muscle relaxants and after full recovery from succinylcholine has occurred
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clindamycin
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clindamycin is effective against which type of microbes?
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aerobic and anaerobic gram positive cocci
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clindamycin is used for what conditions?
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skin and soft-tissue infections
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what drug is a good alternative for patients with a penicillin allergy?
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clindamycin
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Vancomycin class
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bactericidal glycopeptide antimicrobial
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Vancomycin mechanism of action
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impairs cell wall synthesis of gram positive bacteria
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vancomycin is used for which conditions?
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enerococcal endocarditis patients who are allergic to penicillins or placement of prosthetic devices
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vancomycin dose
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10-15mg/kg over 60 minutes
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vacomycin administered quickly causes what?
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histamine release and hypotension
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vancomycin excretion
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90% by the kidneys
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Hemodialysis effect on Vancomycin
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clears from body
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microbes resistant to Vancomycin
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Gram negative bacilli and mycobacterium
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These two antimicrobials are the most potent of all to produce skeletal muscle weakness resembling nondepolaring neuromuscular blockade
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Polymyxin B and Colistimethate
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sulfonamides mechanism of action
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Inhibit microbial synthesis of folic acid
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sulfonamides use
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Used for UTI’s
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sulfonamides side effects
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rash, anaphalaxis
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sulfonamide increases teh effect of which drugs (5)
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oral anticoagulants, methotrexate, sulfonylurea, hypoglycemic drugs and thiazide diuretics
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fluoroquinolones mechanism of action
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Inhibit bacterial DNA gyrase, which is the enzyme responsible for maintaining the helical structure of DNA
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fluoroquinolones consideration for renal dysfunction
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Decrease the dose with renal dysfunction
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Amphotericin B class
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antifungal
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Amphotericin B use
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intrathecal for Coccidiodes meningitis
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Amphotericin B Renal excretion is fast/slow?; can be detected in urine for how long?
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Renal excretion is slow, can be detected in the urine up to 8 weeks
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Amphotericin B side effect on potassium
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decreases- (hypokalemia)
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Amphotericin B side effect on magnesium
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decreases- (hypomagnesemia)
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Amphotericin B side effect on blood pressure
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decreases- (hypotension)
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Amphotericin B side effect on CNS
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seizures
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which antimicrobial can cause anemia?
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Amphotericin B
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Amphotericin B side effect on temperature
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fever, chills
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major possible side effect of Amphotericin B
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allergic reaction
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drug that is a potent inhibitor of corticosteroids
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Ketoconazole
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effect most -azole drugs have on the CYP 450 system
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inihibtion
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what makes micobacterium difficult to treat?
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Most of this class of bacteria have a thick waxy cell wall which makes them difficult to treat
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Rifampin class
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Rifamycins
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Rifamycins effective against which type of microbes?
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Inhibit growth of many gram positive and well as gram negative organisims
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Rifampin interferes the anticoagulant effects of which drug?
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coumadin
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Rifamycins have what kind of effect on the CYP 450 system?
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induction- speeds metabolism of other drugs so drug levels will be decreased
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Isoniazid use
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tuberculosis
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Isoniazid mechanism of action
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Inhibits the multiplication of the tubercle bacillus
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drug that is a potent inhibitor of MAO
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Isoniazid
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Isoniazid metabolism and excretion
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Metabolized by hepatic acetylating to acetylisoniazid which is then excreted by the kidney
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isoniazid effect on rapid acetylators
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Rapid acetylators produce more acetylisoniazid and are more prone to hepatotoxicity and higher fluoride levels with to nephrotoxicity especially when administered with rifampin
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rifampin + isoniazid when given to rapid acetylators
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especially produce more acetylisoniazid and are more prone to hepatotoxicity and higher fluoride levels with to nephrotoxicity
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isoniazid + VAA
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Deflorination
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deflorination of VAA causes
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nephrotoxicity
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isoniazid ususally administered in combination with which drug?
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rifampin
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which drug be given with isoniazid to combat the side effects?
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pyridoxine- vitamin B6
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what develops in about 2% of patients on isoniazid?
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peripheral neuritis
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3 major seide effect of isoniazid
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malnutrition, diabetes, anemia
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The prophylactic administration of pyridoxine with isoniazid does what?
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virtually eliminates all the neurological side effects
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isoniazid causes what to the CYP 450 system
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enzyme induction- administer other drugs with cautionq
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Viruses are composed of what?
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a nucleic acid core surrounded by a protein-containing outer coat called a capsid either RNA or DNA
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Idoxuridine class
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antiviral
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amantadine use
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Parkinsons disease
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amantadine CNS side effects (3)
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CNS toxicity, seizures, coma
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Vidarabine use
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herpes encephalitis
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drug that is mutagenic and carcinogenic
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Vidarabine
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acyclovir use
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herpes
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acyclovir renal effects
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increased BUN, increase creatine with rapid IV infusions
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acyclovir effect on veins
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thrombophlebitis
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acyclovir CNS side effecs
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headache
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HIV is what kind of virus?
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RNA virus
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How does HIV replicate?
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When it infects the cell it makes a viral copy of DNA which then enters the host cell nucleus to produce more copies of viral RNA
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HIV has an affinity for a receptor found mostly on which type of cells?
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CD4 (helper) T-lymphocytes
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Zidovudine class
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anti-retroviral
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what is attrubuted to AZT's anti-retroviral effects?
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The incorporation of zidovudine triphosphate (AZT)into an elongating nucleic acid by reverse transcriptase and its competitive inhibition with thymidine-5’-triphosphate
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side effects of AZT (6)
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anemia, leukopenia, myopathy,
Nephro/hepato toxic, bluish nail pigmentation |
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ritonavir increases plasma levels of which drugs/classes? (8)
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amiodarone,quinidine, encainide, hypnotics, benzodiazapines, antihistamines, terfenadine, and cisapride
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antiretrovirals increase plasma concentrations of which drugs?
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analgesic, fentanyl, lidocaine, antimicrobials, anticonvulsants, anticoagulants, antiemetics, odansetron, calcium channel blockers, corticosteroids, neuroleptics,
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ritonavir class
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anti-retroviral
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What procedures may require antimicrobials?
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GYN
ORTHOPEDIC GENERAL UROLOGIC OROPHARYNGEAL CARDIOTHORACIC AND VASCULAR NEUROSURGY |
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cefazolin is used for what type of microbes? (3)
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staphylococci, streptococci, entericgram-negative rods
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cefazolin is used for what type of surgeries?
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cardiac with median sternotomy, non-cardiac, thoracic, vascular- abdominal and lower extremity
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