farm 2-3, 2-4
Terms
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- drugs that bind to 30s ribosomal subunit?
-
tetracyclines
aminoglycosides - drugs that bind to 50s ribosomal subunit?
-
macrolides
ketolide
chloramphenicol
quinupristin-dalfopristin
clindamycin
linezolid -
Macrolide antibiotics
Azithromycin -
Azithromycin
Class: Macrolide
MOA: irreversibly bind 50s ribosome - interfere with translocation
Use: upper resp infections + atypical pneumonias (H. influenza, M. catarrhalis, mycoplasma, chlamydia, legionella,
PLUS G- and protozoans
H. ducreyi - chancroid
AE: not as much GI,
Contra: hepatic dysfxn
Interaction: low serum levels - [] in neutrophil, macrophages, fibroblasts
Admin: oral, IV - longer half life and higher tissue levels - excreted in bile -
Macrolide antibiotics
Clarithromycin -
Clarithromycin
Class: Macrolides
MOA: irreversibly bind to 50s ribosome - interfere with translocation
Use: H. pylori (peptic ulcer), H. influenza, Chlamydia, Legionella, Moraxella, Ureaplasma
AE: less GI than erythro
Contra: hepatic dysfxn
Interaction: inhibit P450 drug metab Theophylline, carbamazepine - Food increases levels
Admin: oral -
Ketolide antibiotics
Telithromycin -
Telithromycin (deriv of erythro)
Class: Ketolide
MOA: binds to 50s subunit - ketone and methoxy groups make it more stable to stomach acid and increase ribosomal binding affinity - less susceptible to bacterial export pumps than macrolides
Use: upper resp infections, esp multidrug resistant strains - sinusitis, acute exacerbation of chronic bronchitis, mild to moderate community acquired pneumonia
give to renal compromise pts
AE: increase weakness in myasthenia gravis... impair visual accommodation
Contra: prolongs QT interval slightly (should not be taken with similar drugs or with congenital prolonged QT interval)
Interaction: may increase serum levels of hepatic enzymes - reversible hepatitis
Admin: oral - long t1/2 - once daily for 5 to 10 days - - Clindamycin
-
Clindamycin
Class:
MOA: irreversibly bind to 50s ribosome
Use: anaerobes (intraabdominal and pelvic, combine with drug for G- rod), G+ cocci (except entero), lung abscess, skin/soft tissue infections, acne, NECROTIZING FASCIITIS W/ PENECILLIN
AE: pseudomembranous colitis - C. difficile (resistant to clindamycin, RX with metronidazole or vancomycin), diarrhea, colitis
Contra: hepatic failure/renal compromised pt - accumulates
Interaction:
Admin: oral, parental, topical -
Oxazolidinone -
Linezolid -
Linezolid
Class: Oxazolidinone
MOA: bind 23s RNA of 50s subunit, prevents formation of 70s initiation complex
Use: MRSA, VRE, penecillin resistant pneumococci, G+ bacilli
AE: thrombocytopenia, some GI distress, N/Diarrhea, headaches, rash
Contra: no tyramine containng foods!
Interaction:
Admin: oral/IV - 100% bioavailability - Mupirocin
-
Mupirocin
Class:
MOA: prevents formation of tRNA
Use: G+ cocci (impetigo, nasal colonization of MRSA, infected skin)
AE: skin irritation
Contra:
Interaction:
Admin: topical - Trimethoprim
-
Trimethoprim
Class:
MOA: inhibit bacterial dihydrofolate reductase - decrease purine, pyrimidine, aa synthesis
Use: prostate/UTI, pneumonia (P. jiroveci, Nocardia), salmonella/shigella alternative
AE: folic acid defiency symptoms
Contra:
Interaction:
Admin: oral - Sulfonamide + trimethoprim
-
sulfonamide + trimethoprim
Class:
MOA: synergistic effect- inhibit folate synthetase and dihydrofolate reductase
Use: UTI, resp infection, P. jiroveci (IV), resistant salmonella, NOCARDIA, PROSTATIC INFECTIONS
AE: N/V, glossitis, skin rxn, {megaloblastic anemia, leukopenia, thrombocytopenia}prevented by folinic acid
GI IRRITATION; HEADACHE; G6PD DEF HEMOLYTIC ANEMIA
Contra:
Interaction: prolongs PT w/ warfarin, increase phenytoin t1/2, increase methotrexate b/c displaces it from albumin
Admin: oral, IV, topical ocular... metab by acetylation, excreted in urine... *TAKE WITH LOTS OF FLUID SO URINE [] NOT HIGH* -
Fluoroquinolones -
ciprofloxacin
oxfloxacin -
ciprofloxacin
Class: 1st generation fluoroquinolone - cidal
MOA: inhibit type II, IV DNA topoisomerase - bind A subunit of DNA gyrase and inhibit rxn
Use: UTI, gonorrhea/chlamydia alternative, anthrax, traveler's diarrhea, prophylaxis in surgery, shigellosis/typhoid fever alternative, bone and joint
CIPRO-pseudomonas and pseudomonas in CF - TYPHOID FEVER, intra-abdominal infection, prostate, bone, joints, skin, eye
AE: N/V, diarrhea, phototoxicity, arthropathy, tendonopathy, CNS excitation - insomnia, seizures
Contra: pregnancy, kids <18 - articular cartilage erosion (arthropathy)
Interaction: inhibit metab of theophylline - can cause seizures, inhibit caffeine metab.. metal ions decrease bioavailability
Admin: IV, oral - oxfloxacin high [] in CSF -
Fluoroquinolones -
levofloxacin
gatifloxacin
moxifloxacin
gemifloxacin -
levofloxacin, gatifloxacin, moxifloxacin, gemifloxacin
Class: 2nd generation fluoroquinolones
MOA: inhibit type II (DNA gyrase) and type IV DNA topoisomerase
Use: UTI, prostatitis, BRONCHITIS, COMMUNITY ACQUIRED PNEUMONIA, skin/eye infections
LEVO - PROSTATITIS, STD (NO SYPHILIS), skin, eye
MOXI - AEROBE + ANAEROBE (E.COLI)
Gati/Gemi/Moxi - community acquired pneumonia, sinusitis, bronchitis
AE: prolonged QT intervals, N/V, diarrhea, arthropathy, tendonopathy, CNS excitation (insomnia, seizures)
Contra: arrythmia pt
Interaction: GATI - ineraxn warfarin, caffeine, cephalosporin.. cimetidine interferes w/ elim
Admin: oral, topical, intravenous - Nitrofurantoin
-
Nitrofurantoin
Class:
MOA:
Use: LOWER URINARY TRACT (BLADDER) INFECTIONS, E.coli, Staph saprophyticus.. prophylaxis/rx of UTI 6 mo->1 yr
AE: macrocrystalline form causes less GI upset -
neutropenia, neuropathy
Contra:
Interaction:
Admin: rapidly excreted in urine - greater activity in acidic - Polymyxin
-
Polymyxin
Class:
MOA:
Use: G-bacilli, superficial skin/ocular.mucous membrane infections
AE: renal damage - only use for systemic infections
Contra:
Interaction:
Admin: topical w/ bacitracin, neomycin, or trimethoprim - Daptomycin
-
Daptomycin
Class: cyclic lipopeptide
MOA: disrupts plasma membrane
Use: MRSA, VRE, VRstaph
skin, soft tissue, diabetic foot ulcers, burn infections
AE:
Contra:
Interaction:
Admin: - Rifamixin
-
Rifamixin
Class:
MOA:
Use: E. coli, salmonella, shigella
traveler's diarrhea in ppl >12
AE:
Contra: ppl w/ fever, blood in stool, Campylobacter jejuni infection
Interaction:
Admin: not absorbed from gut - what group of bacteria does DNA gyrase primarily target
- G-
- what group of bacteria does DNA topoisomerase primarily target
- G+
- what is the only use for norflaxacin
- UTI - b/c excreted rapidly in urine
- what are the ab against MRSA and VRE
-
daptomycin
linezolid
tigecycline
quinupristin-dalfopristin