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28 Cards in this Set

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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
Gentamicin
Gentamicin

Class: aminoglycoside - bactericidal

MOA: bactericidal, interfere with initiation protein synthesis @ 30s

Use: SERIOUS INFECTIONS DUE TO AEROBIC G- BACILLI (Pseudomonas, E.coli, Proteus, Serratia) - malignant otitis externa, pseudomonas infections, meningitis, intra-abdominal infections, NOT ANAEROBES - B/C REQUIRE O2 DEPENDENT TRANSPORT INTO BACTERIAL WALL
synergistic with cell wall inhibitors (penecillins) against G+ cocci [Staph (nafcillin/vancomycin +/- gentamicin), Strep (penecillin or vancomycin +/- gentamicin), Entero - penicillin/vancomycin + gentamycin)]

AE: nephrotoxicity... CN VII toxicity - dizziness, vertigo, deafness... neuromuscular paralysis w/ intraperitoneal/intrapleural application - decreases Ach release and decreases sensitivity of postsynaptic site

Contra: myasthenia gravis

Interaction:

Admin: IV/IM - need to monitor peak (30 min after) and trough level (before next dose)
Tobramycin
Tobramycin

Class: aminoglycosides - bactericidal

MOA: inhibit initiation protein synthesis @ 30s

Use: ocular infections, P. aeruginosa

AE: nephrotoxicity, CN VIII toxicity (vestibular/auditory)

Contra:

Interaction:

Admin: IV/IM - need to monitor peak (30 min after)and trough level (before next dose)
Streptomycin
Streptomycin

Class: aminoglycoside - bactericidal

MOA: inhibit initiation of protein synthesis @ 30s ribosome

Use: TB, plague, tularemia

AE: nephrotoxicity, CN VIII vestibular/auditory

Contra:

Interaction:

Admin: IV/IM - need to monitor peak (30 min after) and trough level (before next dose)
Tetracyclines:

Tetracycline

Doxycycline

Minocycline

Tigecycline
Tetracyclines - Tetracycline, Doxycycline, Minocycline, Tigecycline

Class: Tetracyclines

MOA: reversibly inhibit binding @ 30s ribosome A site (aminoacyl site) - bacteriostatic

Use: BROAD SPECTRUM
Tetracycline - Rocky Mtn spotted fever, Mycoplasma pneumoniae (ppl live in close confine pneumonia), syphilis and bite wounds if penicillin resistant... Doxycycline - cholera, lyme dz, chlamydia... Minocycline - acne vulgaris... Tigecycline - VRE, MRSA

AE: GI irritation, bacterial overgrowth superinfections (Candida, resistant staph, pseudomembranous colitis from C. diff), staining of teeth, enamel hypoplasia, photodermatitis, pseudotumor cerebri (benign intracranial HTN w/ headache/blurred vision), nephrotoxicity (outdated preps), hepatitis (pregnant)

Contra: bile duct obstruction, liver/kidney dysfxn *except can use doxycycline * NO GIVE PT <8 OR PREGNANT
Interaction: dairy foods, antacids, bivalent/trivalent cations decrease absorption

Admin: oral, doxy preferred IV/IM
Macrolide antibiotics

Erythromycin
Erythromycin

Class: Macrolide - static @ low dose, cidal @ high dose

MOA: irreversibly bind to 50s subunit - interfere with translocation of protein synthesis

Use: G+ cocci (strep, pneumo)
pharyngitis, sinusitis, bronchitis, otitis media, impetigo
DOC for DIPTHERIA, PERTUSSUS

AE: GI distress (pain, spasm), phlebitis w/ IV admin, ototoxicity with high dose

Contra: hepatic dysfxn

Interaction: inhibit P450 drug metab - increases theophylline, carbamazepine (CNS toxicity - severe ataxia, warfarin, lovastatin (myopathy, rhabdomyolysis)
food decreases

Admin: oral, low and variable bioavailability - destroyed by gastric acid so must be coated
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
Quinupristin + Dalfopristin
Quinupristin + Dalfopristin

Class:

MOA: bind to 50s subunit, prevent peptide elongation - bactericidal - penetrate macrophage and polymorphonucleocytes

Use: MRSA, VRE drug resistant G+

AE: pain and phelbitis @ injection site, arthalgia, myalgia (higher doses), hyperbilirubinemia

Contra:

Interaction: inhibit cytochrome P450 enzymes
esp digoxin (eliminates bacteria that inactivate digoxin, therefore greater reabsorption of drug from enterohepatic circulation

Admin: IV
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
Chloramphenicol
Chloramphenicol

Class:

MOA: bind 50 s ribosome, inhibit protein synthesis @ peptidyl transferase rxn

Use: life threatening infection by G+/G- aerobe/anaerobe , salmonella, rickettsia, meningococci, pneumo, H. influenza B/C TOXIC
RMSF, MENINGITIS, TYPHOID FEVER

AE: aplastic anemia - low G6PD, reversible microcytic anemia (inhibit incorporation of iron to heme by ferrochelatase), Gray baby syndrome (baby not enuf renal activity {gluconyltransferase} to metabolize drug, GI overgrowth of Candida

Contra:

Interaction: inhibit hepatic mixed fxn oxidases - block metab and increase [] of warfarin, phenytoin, tolbutamide, chlorpropamide

Admin: oral/IV - HIGH LEVELS IN CSF
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
Sulfonamide
Sulfonamide

Class:

MOA: inhibit bacterial folate synthase

Use: UTI, P. jiroveci, nocardia, salmonella/shigella alternative, burn wounds (silver sulfadiazine), ocular infections (topical sodium sulfacetamide), MRSA

AE: crystalluria (nephrotoxicity), hypersensitivity (rash, angioedema), hemolytic anemia (G6PD def), kernicterus in newborns

Contra: pregnancy, newborn, infant, pt taking methenamine for UTI

Interaction: potentiates tolbutamide hypoglycemic effect and warfarin anticoagulation and increases free methotrexate

Admin: oral - absorbed in small intestine... bind to serum albumin, greater binding @ lower pKa
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