microbio antimicrobials Flashcards
penicllin G (IV and IM) and penicillin V (oral)
bind penicillin binding proteins (transpeptidases) and block transpeptidase crosslinking of proteoglycans in the cell wall; used for gram pos (strep, actinomyces); also used for gram neg cocci (mainly meningococcus) and spirochetes (t. pallidum); bactericidal; can see hypersens reactions and hemolytic anemia
amoxicillin, ampicillin
same mechanism as penicillins but wider spectrum, but still penicillinase sens; can be used for H. influenzae, H. pylori, E coli, Liseria, proteus, salmonella, shigella, enterococci
dicloxacillin, nafcillin, oxacillin
these are the penicillinase-reistant penicillins; used for staph aureus (but not MRSA); can cause hypersens reactions or interstitial nephritis
piperacillin, ticarcillin
antipseudomonal penicilllins; used for pseudomonas and gram neg rods; susceptible to penicillinase; use with beta-lactamase inhib
beta-lactamase inhibitors
clavulanic acid, sulbactam, tazobactam; often added to the penicillin antibiotics
first generation cephalosporins
cephalexin, cefazolin; gram pos cocci, proteus, e coli, klebsiella; cefazolin is often used prior to surgery to prevent staph aureus wound infections
second generation cephalasporins
cefoxitin, cefaclor, cefuroxime; gram pos cocci, h flu, enterobacter, neisseria, proteus, e. coli, klebsiella, serratia
third gen cephalasporins
ceftriaxone, cefotaxime, ceftazidime; serious gram neg infections
fourth gen cephalasporins
cefepime; gram neg organisms, with increaed activity against pseudomonas and gram pos organisms
fifith gen cephalasporins
ceftaroline; broad gram pos and gram neg organism coverage, incl MRSA; does not cover pseudomonas
ceftazidime
good pseudomonas coverage
toxicity of the cephalasporins
hypersens reactions, autoimmune hemolytic anemia, disulfuram-like reaction, vit K def, exhibit cross-reactivity with penicillins; they increase the nephrotoxicity of aminoglycosides
carbapenems
imipenem, meropenem, ertapenem, doripenem; these inhibit cell wall synthese and are resistant to beta lactamase; used for gram pos cocci, GNR, and anaerobes; wide spectrum but signif side effects; toxicity includes GI distress, skin rash, and CNS toxicity (seizures) at high levels
imipenem
always administered with cilastatin to decreae inactivation of the drug in renal tubules
monobactams
aztreonam; inhibits cell wall synthesis; no cross-allergenicity with penicillins; used for gram neg rods only (no activity against gram pos or anaerobes); used in penicillin-allergic patients and those with renal insuff who cannot tolerate aminoglycosides; usually nontoxic, occasional GI upset
vancomycin
inhibits cell wall peptidoglycan formation by binding D-ala D-ala portion of cell wall precursors; not sucesceptible to beta lactamases; used for gram pos only (MRSA< staph epi, enterococcus, c. diff); nephrotoxicity, ototoxicity, thrombophlebitis, red man syndrome (diffuse flushing, but can be prevented with antihistamines and slow infusion rate); resistance develops when bacteria change D-ala D-ala to D-ala D-lac
aminoglycosides
gentamycin, neomycin, amikacin, tobramycin, and streptomycin; inhibit 30S subunit; use for severe gram neg rod infections; synergystic with beta lactams; toxicity is nephrotoxicity, neuromuscular blockade, ototoxicity (esp when used with loop diuretics), teratogen;
tetracylcines
tetracycline, doxy, minocycline; 30S inhibitor; limited CNS penetration; doxy is fecally eliminated and can be used in patients with renal failure; do not take teracyclines with milk, antacids, or iron-containing preparations bc divalent cations inhibit drug’s absorption in the gut; great intracellular accumulation, so good against rickettsia and chlamydia; also used to tx acne
toxicity of tetracyclines
GI distress, discoloration of teeth and inhib of bone growth in kids, photosens; contraindic in pregnancy
chloramphenicol
blocks peptidyltransferase at 50S ribisomal subunit; toxicity is anemia (dose-dep), apalstic anemia (dose-indep), gray baby syndrome (in premature infants)
clindamycin
block peptide transfer at 50S; used for anerobes in aspiration pneumonia, lung abscesses, and oral infections; also effective against invasive group A strep; “treats anaerobes above the diaphragm vs. metronidazole, which treats them below the diaphragm”; assoc with pseudomembranous collitis, fever, diarrhea
linezolid
inhibits protein synthesis at the 50S subunit; good for gram pos species, incl MRSA and VRE; can cause bone marrow suppression (esp thrombocytopenia), peripheral neuropathy, serotonin syndrome
macrolides
azithromycin, clarithromycin, erythromycin; inhibit 50S; use for atypical pneumonias (legionell, mycoplasma, chalamydia), STIs (chlamydia), gram pos cocci (strep), and b. pertussis; toxicity includes GI, arrythmia caused by prolong QT, acute cholestatic hepatitis, rash, eosinophilia; increases serum concentrations of theophyllines and oral anticoagulants; Clarithromycin adn erythromycin inhib P450
trimethoprim
inhibits bacterial dihydrofolate reductase; used in combo with sulfonamides, causing sequential block of folate synthesis; toxicity is megaloblastic anemia, leukopenia, granulocytopenia (may allev with suplemental folinic acid)
sulfonamides
inhibit folate synthesis; PABA antimetabolites inhibit dihydropteroate synthase (Dapson, used to treat lepromatous leprosy, is a closely related drug that also inhibits folate synthesis); treats GP, GN, nocardia, chlamydia; toxicity is hypersens reactions, hemolysis if G6PD def, nephrotoxicity (TIN), photosensitivity, kernicterus in infants, displace other drugs from albumin;
prophylaxis for TB
isoniazid
treatment for TB
rifampin, isoniazid, pyrazinamide, ethambutol (RIPE); isoniazid and ethambutol act on the cell wall, while rifampin inhibits mRNA synthesis, and pyrazinimide has unknown mechanism
rifamycins
rifampin, rifabutin; inhibit DNA-dep RNA polymerase; used for TB, also to delay resistance to dapsone when used for leprosy, used for meningococcal proph and chemoproph in contacts of kids with HIB; toxicity is minor hepatotoxicity and drug interactions (increases cyp450), organge body fluids; monotherapy rapidly leads to resistance
isoniazid
decreases synthesis of mycolic acids; treats TB; this is the only agent used as solo prophylaxis against TB; toxicity includes neurotoxicity, hepatotoxicity, pyridoxine (Vit B6) can prevent neurotoxicity; INH Injures Neurons and Hepatocytes
Pyrazinamide
mech unknown; used to treat TB; toxicity is hyperuricemia and hepatotoxicity
Ethambutol
decreases carbohydrate polymerization of mycobacterium cell wall; toxicity is optic neuropathy
fluoroquinolones
inhibit prokaryotic enzymes topoisomerase II and topoisomerase IV; must not be taken with antacids; used for GNR of urinary and GI tracts (incl pseudomonas), neisseria, some GP organisms; toxicity is GI upset, skin rashes, HA, dizziness; less commonly cau cause leg cramps and myalgias; contraindicated in pregnant women and nursing women; may prolong QT; may cause tendonitis or tendon rupture