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107 Cards in this Set
- Front
- Back
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Which generation of cephalosporins provide gram positive coverage?
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"1st and 2nd generation cephalosporins, some 4th"
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Which generation of cephalosporins provide gram negative coverage?
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3rd and 4th generation cephalosporins
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What is the MOA of aminoglycosides?
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"Acts at the 30S subunit and inhibits formation of initiation complex, causing the misreading of mRNA."
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What is the MOA of tetracyclines?
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Acts at the 30S subunit and prevents attachmen of aminoacyl-tRNA to acceptor site.
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What is the MOA of chloramphenicol?
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Acts at the 50S subunit and inhibits peptidyl transferase.
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"What is the MOA of erythromycin, lindomycin, and clindamycin?"
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Acts at the 50S subunit and blocks the aminoacyl-tRNA complex translocation step. (Clindamycin also blocks initiation complex formation.)
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A bleeding disorder caused by penicillins.
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Drug-induced Coombs' positive hemolytic anemia.
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How do penicillins work?
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They bind to PBPs and block peptidoglycan cross-linking.
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What is the spectrum of penicillins?
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"Cocci. Treat gram positives (streptococci, enterococci), gram negative (Neisseria), and spirochetes (Treponma pallidum |penicillin G)."
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What is the advantage of using ampicillin (or amoxicillin) over penicillin?
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"Ampicillin has an extended spectrum of coverage. In addition to cocci, it covers gram-negative rods (H. influenza, E. coli, Listeria moncytogenes, Proteus mirabilis, Salmonella)."
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When is amoxicillin preferred to ampicillin?
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Amoxicillin is good for outpatient treatment because it can be given orally.
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What can be added to amoxicillin or ampicillin to broaden the specturm against gram-negatives through their ability to inactivate bacterial beta-lactamases?
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Clavulanic acid and sulbactam
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What beta-lactam drug provides coverage for Pseudomonas?
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Piperacillin
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What drug is added to piperacillin to provide added coverage against gram-negatives and S. aureus and what is its MOA?
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Tazobactam is a beta-lactamase inactivator (like clavulanic acid and sulbactam).
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"Which beta-lactamase can be used to treat UTIs (Klebsiella, Pseudomonas, Serratia) in penicillin allergic patients or patients who cannot tolerate aminoglycosides (renal insufficiency)?"
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Aztreonam (relatively resistant to beta-lactamases)
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Which drug is a broad spectrum antibiotic that is given with a second drug that prevents its inactivation in the rena tubules?
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Imipenem
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Which drug is given with impenem to extend its half-life through the inhibition of renal dihydropeptidase I?
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Cilastatin
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Which class of antibiotics can cause disulfiram-like reactions when given with alcohol?
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Cephalosporins
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What makes cephalosporins an attractive alternative to the penicillins?
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The cephalosporins are relatively resistant to beta-lactamases.
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What is the side effect profile with gentamicin?
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Nephrotoxic (ATN) with cephalosporins; ototoxic with loop diuretics; teratogen
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What is the MOA of gentamicin?
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"Like other aminoglycosides, it acts at the 30S subuit to inihibit the formation of an initiation complex leading to mRNA misreading."
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What is the spectrum of gentamicin and other aminoglycosides?
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"They are used to treat severe infections with gram-negative rods (sepsis, endocarditis/w/vanco, pneumonia, Pseudomonas)."
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What is one prominent side effect of clindamycin?
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It is a cause of pseudomembranous colitis.
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What is the spectrum of clindamycin?
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Its effective against some anaerobes and some gram-positive cocci. It can treat anaerobic infections above the diaphragm and as endocarditis prophylaxis before dental procedures.
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What is the MOA of clindamycin?
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It binds the 50S subunit and inhibits formation of the initiation complex and translocation of the aminoacyl peptide during protein synthesis.
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What is the MOA of linezolid?
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It is a protein synthesis inhibitor that acts at the 50S subunit to prevent the formation of the ribosomal complex.
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What is the spectrum of linezolid?
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Pretty narrow. Gram-positives including MRSA and VRE and Listeria (gram positive bacilli).
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What are the side effects of chloramphenicol?
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dose-dependent anemia and aplastic anemia; gray baby syndrome
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What is the MOA of chloramphenicol?
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It reversibly binds the 50S subunit inhibiting peptidyl transferase.
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When might chloramphenicol be used?
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As a last resort in patients with bacterial meningitis that are allergic to penicillins and other antibiotics.
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What is the MOA of erythromycin?
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"It blocks the 50S ribosomal subunit, inhibiting the formation of the initiation complex as well as the translocation of the aminoacyl peptide during protein synthesis."
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What is the spectrum of erythromycin?
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"Broad. Gram-postivie cocci, atypical organisms, Corynebacteria, and some gram-negatives. Used primarily to treat upper respiratory infections (but also some STDs, H. pylori, Corynebacteria)."
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What is a prominent side effect of methicillin?
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Interstitial neprhitis
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Why is methicillin an improvement over penicillin?
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Methicillin has a bulkier structure that resists beta-lactamase.
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What are some similar antibiotics to methicillin?
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"Naficillin, oxacillin, dicloxacillin"
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What is the MOA of tetracycline?
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It binds the 30S subunit and block the aminoacyl-tRNA from binding to the ribosome.
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What is the spectrum of tetracycline?
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"Broad. Gram positives and Gram negatives. Vibrio, chlamydia, rickettsiae, mycoplasmas, spirochetes, some anaerobes."
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What diseases does tetracycline treat?
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"Pneumonia (mycoplasma, chlamydia), Rocky mountain spotted fever, Lyme diseases, cholera, sexually transmitted chlamydia infections"
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What are some prominent side effects of tetracycline?
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"Teeth discoloration and bone deformity in children, Fanconi syndrome, photosensitivity"
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What drug that is similar to tetracycline can be used in renally insufficient patients?
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Doxycycline because it is eliminated in feces.
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What dietary considerations must be considered with tetracycline?
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"It cannot be taken with divalent cations due to inhibited absorption (i.e. antacids, milk, iron-containing substances)."
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What tetracycline related drug can be used to treat SIADH?
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Demeclocycline works as a competitive antagonist at the V2 receptor.
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What is the MOA of Trimethoprim-Sulfamethoxazole (TMP-SMX)?
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TMP works by inhibiting dihydrofolate reductase. Sulfamethoxazole acts as a structural analog of PABA and competitively inhibits dihydropteroate synthase.
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What is the spectrum for Trimethoprim-Sulfamethoxazole?
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"Broad. Gram positives and gram-negatives including enterics, Chlamydia, Nocardia, and P. jiroveci."
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What conditions does trimethoprim-sulfamethoxazole treat?
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Pneumonia and urinary tract infections.
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What are the prominent side effects of trimethoprim-sulfamethoxazole?
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"Steven-Johnson syndrome, hemolytic anemia, kernicterus in newborns, granulocytopenia that can be alleviated with folinic acid."
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What is the MOA of ciprofloxacin and other fluoroquinolones?
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"Inhibitors of bacterial DNA topoisomerase II, inducing strand breakage and cell death."
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What is the spectrum for ciprofloxacin?
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"Gram negatives. Neisseria, Haemophilus, Klebsiella, E. coli, Enterobacter, Mycoplasm, Legionella"
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What is ciprofloxacin used for?
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"UTIs, pneumonias, gonococcal infections, other respiratory tract infections, GI infections"
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What are the side effects of ciprofloxacin?
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"Tendonitis and tendon rupture, contraindicated in pregnant women and children"
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"Which antibiotic is preferentially reduced inside bacterial cells, increasing its reactivity and making it a useful treatment against UTIs?"
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Nitrofurantoin
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What is the MOA of vancomycin?
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"Binding of the D-ala D-ala terminus of bacterial cell wall precursors, inhibiting transglycosylase, limiting elongation and crosslinking."
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What is the spectrum of vancomycin?
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"Gram-positive bacteria. Staph, strep, enterococci."
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What are the uses for vancomycin?
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Gram-positive multi-drug-resistant infections like sepsis and endocarditis. Also used for pseudomembranous colitis.
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What are the side effects of vancomycin?
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"Red man syndrome, ototoxicity, nephrotoxicity"
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What is the MOA for polymyxins?
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Bind to bacterial cell membranes and increase the permeabiliyt of the cell membrane to polar molecules.
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Name one antibiotic that is used for anaerobic infections above the diaphragm and one that is used for anaerobic infections below the diaphragm.
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Clindamycin and metronidazole
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What is the MOA of metronidazole?
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"It is metabolized by bacterial proteins into reduced reactive compounds that damage bacterial DNA, protein, and membranes."
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What is the spectrum of metronidazole?
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"Anaerobic bacteria and protozoans. (Clostridium, Bacteriodes, Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis)"
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What precautions must a patient taking metronidazole be aware of?
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Disulfiram-like effect with alcohol
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What are some important drug interactions to be aware of with metronidazole?
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"Potentiates warfarin and other anticoagulants, levels decreased by phenytoin and phenobarbital, levels increased by cimetidine"
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What is the MOA of rifampin?
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Inhibition of bacterial DNA-dependent RNA polymerase.
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Under what circumstances is rifampin used prophylactially?
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"Contacts of patients with meningococcal meningitis, and H. influenza type B infection."
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What coverage does rifampin provide?
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"Mycobacteria, Neisseria meningococcus, H. influenza"
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What are a couple of key side effects of rifampin?
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Orange color in urine and sweat; hepatitis
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What are some of the drug interactions of rifampin?
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"Induces cytochrome P-450 affecting metabolism of warfarin, oral contraceptives, prednisone, ketoconazole, digoxin, and glyburide."
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What medication is used prophylactically against active tuberculosis?
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Isoniazid
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What is the MOA of isoniazid?
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It inhibits the synthesis of mycolic acid.
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What are some side effects of isoniazid?
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"Peripheral neuropathy (unless given with vitamin B6), drug-oinduced lupus, hepatitis, G6PD-deficient hemolytic anemia"
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What fact of pharmacokinetics is important to remember when administering isioniazid?
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"Some patients are fast metabolizers due to genetic differences in the liver enzyme N-acetyltransferase, so serum level should be monitored to assure therapeutic levels."
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Which antimycobacterial agents are used in combination with other medications (like rifampin and isoniazid) to treat TB?
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Ethambutol and pyrazinamide
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Which antimicrobial can be used in combination with rifampin to treat leprosy?
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Dapsone
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What's the MOA of ethambutol?
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Inhibits mycobacterial arabinosyl transferase which is important for mycobacterial cell wall synthesis.
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What's the MOA of dapsone?
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It’s a PABA antagonist that inhibits folic acid synthesis in a manner similar to sulfonamides.
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What is a prominent side effect of dapsone?
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G6PD-deficient hemolytic anemia
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What is a prominent side effect of ethambutol?
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Retrobulbar neuritis
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What is a prominent side effect of pyrazinamide?
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Hepatotoxicity
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What are some prominent side effects of nucleoside reverse transcriptase inhibitors?
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Megaloblastic anemia (AZT) and pancreatitis (ddI)
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List seven nucleoside revers transciptase inhibitors.
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"zidovudine (AZT), didanosine (ddI), zalcitabine (ddC), lamivudine (3TC), stavudine (d4T), emtricitabine (FTC), and abacavir"
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What are the names and MOAs of two medications used to treat HIV infection (one of which can also be used for hepatitis B).
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Tenofovir and adefovir (hep B effective) are nucleotide analog reverse transcriptase inhibitors that also inhibit viral reverse transcriptase.
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Which nucleoside reverse transcriptase inhibitor is used in the treatment of chronic hepatitis B.
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Lamivudine
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What are the treatments for gonorrhea and Chlamydia?
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Ceftriaxone and azithromycin or doxycycline (7 days)
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What is the MOA of non-nucleoside reverse transcriptase inhibitors (NNRTIs)?
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"They bind specifically to HIV reverse transcriptase, blocking DNA synthesis."
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What are the NNRTIs (3)?
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"Nevirapine, efavirenz, delavirdine"
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What are NNRTIs used for?
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Treatment of HIV infection.
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What are some of the side effects of nevirapine?
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"Induction of cytochrome P-450 system (OCPs, warfari, metronidazole, ketoconazole, protease inhibitors affected), Stevens-Johnson, fulminant hepatits"
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What are some of the side effects of efavirenz?
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CNS disturbances including nightmares and delusions
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What are some of the suffixes of the protease inhibitors?
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*nivir and *navir
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What is the MOA of protease inhibitors?
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They prevent replication by interfering with the maturation process (precursor cleavage) of viral core proteins.
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What are protease inhibitors used for?
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Treatment of HIV infection.
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What are some side effects of protease inhibitors?
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"Altered distribution of body fat (buffalo hump, truncal obesity), insulin resistance, hyperlipidemia."
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Which protease inihibitor has the side effect profile of inhibiting cytochrome P-450?
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Ritonavir
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What is the MOA of acyclovir?
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It is phosphorylated by viral thymidine kiase to an analogue of dGTP that inhibits DNA synthesis by chain termination.
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What is acyclovir used for?
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"HSV-1 and 2, VZV, and EBV. Genital herpes, herpes encephalitis, acute VZV infection and oral hairy leukoplakia associated with EBV."
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What are some of the side effects of acyclovir?
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"Neurotoxicity (tremor, delirium)"
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How might a virus become resistant to acyclovir?
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It may lack thymidine kinase.
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Which drugs are related to acyclovir?
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"valacyclovir, penciclovir, famciclovir"
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What is the MOA of ganciclovir?
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It is a guanosine analogue that when phosphorylated by a viral kinase into a nuleotide analogue preferentially inhibits CMV DNA polymerase.
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What is ganciclovir used for?
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CMV infections; particularly CMV retinitis
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What is a major side effect of ganciclovir?
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Pancytopenia
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What is foscarnet?
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A pyrophospate analog that inhibits viral DNA polymerase.
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What is foscarnet used for?
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It is a second-line treatment of CMV retinitis and other CMV infections. Side effect is nephrotoxicity.
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What is the MOA of amantadine?
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"Binds to the M2 surface protein proton channel on influenza A, blocking the uncoating of the viral RNA within the host cell."
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What are the clinical uses of amantadine?
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"Amantadine reduces the duration of the influenza A symptoms and also stimulats the release of dopamine from the nigra striatum, making it a useful treatment for Parkinson disease."
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What are the side effects of amantadine?
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"CNS symptoms including ataxia, slurred speech, and dizziness."
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What is the MOA of zanamivir?
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"It inhibits neuraminidase, preventing viral replication and release of viral particles from infected cells."
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What are the clinical uses of zanamivir?
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It is used in the treatment and prophylaxis of both influenza A and B.
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