U1 medicine - antimicrobial drugs pt 2 (protein synthesis active/other mechanisms)

aminoglycosides

mechanism - protein synthesis disruption

-binds to 30S ribosomal subunits which decreases protein synthesis

-increases misreading of mRNA leading to bactericidal activity

-poor penetration of lungs, CSF

adverse effects

-nephrotoxicity

-ototoxicity

aminoglycosides

black box warning for : nephrotoxicity/ototoxicity --> can be harmful/fatal and need to get drug levels

aminoglycosides

drugs (-cin)

-Gentamicin

-Tobramycin

-Amikacin

targets

Pseudomonas spp.

tetracyclines

-reversibly binds to 30S subunit on the ribosome, preventing protein synthesis

-bacteriostatic

-avoid tetracycline and minocycline in pts with renal and hepatic impairment

-Doxycycline good for MRSA in cellulitis, atypical pneumonia

tetracyclines

drugs

-Tetracycline

-Minocycline

-Doxycycline

Doxycycline targets

-MRSA

-atypical pneumonia

-Chlamydia

-legionella

-micoplasma

others target

-gram +/- aerobes

tetracyclines

adverse effects

-esophagus irritant (can't lay down)

-damage to kidneys (fanconi syndrome)

-hypersensitivity/ photosensitivity reactions

-depression of skeletal growth in children

-GI symptoms

-hepatotoxicity

-CNS symptoms (dizziness, vertigo, loss of balance)

-aggravation of pre-existing renal failure

macrolides

-good activity against atypical pneumonia

-erythromycin causes GI issues, nausea, vomiting, cramps, diarrhea, bad distribution and poor penetration

-azithromycin causes nausea, diarrhea, tinnitus and dizziness in high doses, good distribution only in lungs

macrolides

drugs

-Erythromycin

-Clarithromycin

-Azithromycin

targets

-Legionella

-Mycoplasma

-Chlamydophila

-Streptococcus

-H. Influenza

-H. pylori

-Borrelia burgdorferi

effects

-GI problems

lincosamides

mechanism - protein synthesis

-binds to 50S ribosomal subunit to decrease protein synthesis

-does not penetrate well into CSF

-excellent penetration into bone

-good for toxoplasmosis

lincosamides

drugs

-Clindamycin

targets

-MSSA

MRSA

-Streptococcus spp.

-B. fragilis

-Peptococcus/Peptostreptococcus

lincosamides

adverse effects

-GI problems, diarrhea, pseudomembranous colitis

-esophagus irritation, no laying down

fluoroquinolones

mechanism of action

-inhibits DNA gyrase which inhibits bacterial DNA synthesis and results in breaking bacterial DNA

-exhibit concentration dependent killing

-excellent penetration into bone

-good activity against atypical pneumonia

-avoid with milk, dairy, antacids for 2-4 hours

fluoroquinolones

drugs

-Ciprofloxacin

-Levofloxacin

-Moxifloxacin

targets

-Moxifloxacin targets Streptococcus spp., atypical pneumonia

-others target Pseudomonas spp., MSSA

fluoroquinolones

adverse effects

-mild gastrointestinal symptoms -mild headache and

-dizziness

-insomnia

-phototoxicity

-arthropathy w/ cartilage erosion

-tendon rupture, especially Achilles

-transient increases in LFTs, liver toxicity

-QTc prolongation (Torsades de pointes)

sulfas

mechanism of action

-inhibits bacterial folic acid synthesis results in inhibition of bacterial cell growth

-penetrates well into many tissues

-one of the few oral drugs for MRSA cellulitis

-must hydrate as susceptible to crystalluria

-increases anticoagulation of warfarin by displacing it from binding sites, increases INR

-should be avoided in hemodialysis patients

TMP-sulfas

drugs

-Trimethoprim

-Sulfamethoxazole

targets

-MRSA

-P. carinii

-gram +/- aerobes

-does not cover Pseudomonas, group A Strep, and Enterococcus

TMP-sulfa

adverse effects

-GI problems

-hypersensitivity

-can see Stevens-Johnson syndrome

-anemia, neutropenia, hyperkalemia

nitroimidazoles

metronidazole

mechanism

enters the cell and reduced to free radicals which damages the bacterial DNA

-bacteriocidal

-big drug interaction with warfarin

nitroimidazoles

drugs

Metronidazole

targets

-all anaerobes including C. difficle

-H. pylori

metronidazole

adverse effects

-metallic taste

-gastrointestinal disturbances

-reversible neutropenia

-dark urine

-rash

oxalinediones

linezolid

mechanism

-binds to 50S ribosomal subunit, inhibits early phase of protein synthesis

-in vitro activity has been demonstrated against many other organisms

-->Chlamydia pneumoniae, anaerobic Streptococci, and Mycobacteria

oxalinediones

drugs

Linezolid

targets

-Staph/Strep

-Enterococci

linezolid

adverse effects

-diarrhea, nausea

-taste perversion

-mild increase in liver function test

-thrombocytopenia

-no dose adjustment for renal/hepatic insufficiency

lipopeptides

daptomycin

mechanism

-binds to bacterial cell membranes, causing rapid depolarization of membrane potential, causing inhibition of protein synthesis and bacterial cell death

-first drug to be bacteriocidal against resistant gram + organisms

-widely distributed except lungs

lipopeptides

drugs

Daptomycin

targets

-Streptococci

-S. epidermis

-Enterococci

-S. aureus

-MSSA

-MRSA

daptomycin

adverse effects

-transient increases in CK elevation, measure often

-dose reduction in renal insufficiency