Protein Synthesis Inhibitors

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30s ribosome inhibitors

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tetracyclines, aminoglycosides

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tetracyclines

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chlortetracyclin, oxytetracycline, tetracycline, demecyclocyline, methacycline, doxycycline, minocycline, tigecycline

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tetracycline MOA

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reversibly binding to 30s ribosome (inhibit tRNA attached to the A site). Bacteriostatic. Broad spectrum, G+ and G-, anaerobes, rickettsiae, clamydia, vibrio, mycoplasma, spirochetes and some protozoa

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tetracycline mechanisms of resistance

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ribosome protection, increased efflux (active transport pump), impared influx, enzymatic inactivation

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tetracycline resistant strains may be susceptible to

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doxycycline, minocycline and tigecycline

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Drug absorption

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oral (doxycycline and minocycline are 95% absorbed)

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factors affecting oral absorption

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food (except for doxy and mino) divalent cations, dairy products, alkaline pH

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Which tetracycline is IV only

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tigecycline

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Drug distribution

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widely to tissues and body fluids, cross placenta and excreted in milk. Bound to and damage growing bones and teeth

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metabolized in

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liver

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eliminated by

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urine

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except for

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doxycycline and tigecyclin

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which have long acting half lives

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doxy, minocycline. Once daily dosing

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clinical uses of tetracyclines

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drug of choice for mycoplasma pneumoniae, chlamydiae, rickettsiae and some spirochetes

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in combination can be used to treat

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gastric and duodenal ulcer caused by helicobacter pylori

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usually combined with

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amino glycoside to treat plague, tularemia and brucellosis

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preferred oral and IV

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doxycycline

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treatment of skin and intraabdominal infections

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tigecycline

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adverse reactions

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GI effects (nausea and vomiting) pseudomembranous colitis. Damage on teeth and bone when given to pregnant women or children of young ages, discoloration in fetal teeth, deformity or growth inhibition of bones

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What should not be given to counteract the GI symptoms

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milk or antacids

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more adverse reactions

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liver tox, kidney tox, local tissue tox (venous thrombosis (IV)), photosensitization, vestibular reactions (dizziness, vertigo, nausea)

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aminoglycosides

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streptomycin, neomycin, kanamycin, amikacin, gentamicin, tobramycin, netilmicin

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aminoglycosides MOA

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irreversibly binding to 30s ribosome, interferes with proofreading process of mRNA, inhibits peptide-tRNA translocation from A to P site. Bactericidal

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active against

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G- and G+, not anaerobes

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How is it administered

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Poor GI absorption, usually IV/IM

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eliminated by

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kidney

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special

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rapid concentration dependant killing and great post antibiotic effect (once daily dosing)

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clinical uses of aminoglycosides

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often combined with a beta lactam antibiotic for the treatment of serious infections or infective endocarditis caused by enterococci eg with penicillin (synergistic effect)

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tox of aminoglycosides

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significant tox with > 5 days of use, ototox (irreversible), nephrotox (reversible). Monitoring serum conc. Is essential.

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streptomycin

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2nd line agent for tuberculosis, bubonic plague (yersinia pestis)

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neomycin

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not safe for systemic use (extremely nephrotoxic), only used topically or orally

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amikacin

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bacteria resistant to other aminoglycosides or tb (2nd line agent)

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gentamicin

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most often used aminoglycoside

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tobramycin

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interchangable with gentamicin, treat infections caused by pseudomonas aeruginosa

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netilmicin

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active against some bacteria that are resistant to gentamicin or tobramycin

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spectinomycin

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structurally related to aminoglycosides, used IM solely to treat drug resistant gonorrhea in pt allergic to penicillin

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aminoglycosides mechanism of drug resistance

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plasmid encoded aminoglycoside modifying enzyme, altered ribosomal binding sites

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50s ribosome inhibitors

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macrolides, clindamycin, chloramphenicol, streptogramins, oxazolidinones

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macrolides

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erythromycin, clarithromycin, azithromycin, thelothromycin, ketolides

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macrolide MOA

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bind to and inhibit 50s ribosomal subunit (inhibit translocation process)

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macrolides effective against

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G+, bacteriostatic or bactericidal at high conc.

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obtained from streptomyces erythreus

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erythromycin

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semisynthetic derivitaves of erythromycin

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clarithromycin and azithromycin

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mechanism of resistance for macrolides

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active efflux or decreased cell permeability. Hydrolyzed by esterases, modification of the ribosomal binding site (ribosomal protection). Chromosomal mutation by inducible or constitutive methylase

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constitutive methylase productions confers resistance to

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clindamycin and streptogramin (MLS type B resistance

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which macrolide is destroyed by stomach acid

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erythromycin and must be administered with enteric coating

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more stable in stomach acid and better absorbed

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clarithromycin and azithromycin

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longest half life of macrolides

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azithromycin 2-4 days once daiy dosing

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how is azithromycin taken

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empty stomach food affect absorption

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which macrolides inhibit liver cytochrome p450 enzymes

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erythromycin and clarithromycin

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what does this do

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icrease serum concentration of theophylline, oral anticoagulants, cyclosporin, carbamazepine and methylprednisolone

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clinical uses of macrolides

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diptheria, cornebacterial sepsis, erythrasma. Respiratory, neonatal, ocular or genital chlamydial infections, CAP, staph infections in penicillin allergig pt's.

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DOC for chlamydia

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azithromycin

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erythromycin adverse reactions

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GI intolerance, liver tox (acute cholestatis hepatitis)

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Ketolides

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telithromycin

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describe the structure

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semisynthetic 14 membered ring macrolide

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How do ketolides work and what do they do

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inhibit p450 enzymes, respiratory infections

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side effects of ketolides

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GI tox and severe liver failure

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use of clindamycin

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broad spectrum especially effective against anaerobes

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Clindamycin MOA

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inhibits bacterial protein synthesis by binding to the 23s rRNA of the 50S subunit

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mechanism of resistance for clindamycin

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mutation of the ribosomal site, modification of the binding site by a constitutively expressed methylase (MLS-type B resistance). Enzymatic inactivation

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clinical uses of clindamycin

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treat infections caused by bacteriods and other anaerobes associated with mixed infections. Recommended for prophylaxis of endocarditis in pts with valvular heart disease whoare undergoing dental procedures

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adverse rxs of clindamycin

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increased risk for diarrhea and colitis due to clostridium difficile

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chloramphenicol MOA

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binds to 50s ribosome (inhibits the peptidyltransferase reaction) bacteriostatic broad spectrum.

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use of chloramphenicol

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aerobic and anaerobic G+ and -

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pharmakokinetics of chloramphenicol

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inactivated in the liver via conjugation and excreted in urine. Dosage adjustment needed in pts with hepatic failure. Inhibit liver p450 enzymes (potential drug interactions)

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mech of resistance

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decrease drug permeability, production of plasmid encoded chloramphenicol acetyltransferase

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clinical use of chloramphenicol

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topically in the treatment of eye infections, alternative agent for treating meningitis in pts who are allergic to penicillin

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side effects of chloramphenicol

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aplastic anemia (irreversible), grey baby syndrome

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streptogramins

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quinupristin, dalfopristin

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quinupristin and salfopristin moa

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binds to 50s ribosomal subunit (bactericidal

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quinupristin and salfopristin active against

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g+ cocci including VRSA and VRE

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pharmakokinetics of quinupristin and dalfopristin

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inhibit cyp3a4 enzymes which metabolize warfarin, diazepam

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quinpristin resistance

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modification of binding site by a methylase (MLS-B type)

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dalfopristin resistance

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enzymatic inactivation

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tox of quinupristin and dalfopristin

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infusion related pain and arthralgiamyalgia syndrome (muscle pain)

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oxazolindiones

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linezolid

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linezolid MOA

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inhibits protein synthesis by binding to the 23s rRNA of the 50s subunit (blocks initiation).. Bacteriostatic

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linezolid use

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G+ organisms. Reserved for treatment of multidrug resistant G+ bacteria ie MRSA VRE

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major side effect

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hamatologic toxicity

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cheapest g-

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gentamicin, tobramycin

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expensive g-

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imipenem-cilastatin, ceftriaxone

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bactericidal protein synthesis inhibitors

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streptogramins, aminoglycosides