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Pharmacology of bacterial infections
Terms in this set (69)
The target ______ are enzymes in the replication for bacteria.
The target ______ are enzymes in the transcription that are catalyzed for the synthesis of single-stranded RNA transcripts from a DNA template.
The target ____ differ between bacterial and human ribosomes in the number and composition of the rRNA molecules.
The pharmacological agents that are inhibitors of Topoisemerases is ______.
The pharmacological agents that are inhibitors of transcription is_______.
The pharmacological agents that are inhibitors of translation are ____, ____, and .....
Aminoglycosides, tetracyclines, macrolides, lincosamides, etc
Explain the MOA for Fluoroquinolones (which are inhibitors of topoisomerases)...
Inhibits one or both of the type II bacterial topoisomerases, which prevents relaxation of supercoiled DNA preventing transcription/replication.
Fluoroquinolones targets mainly Gram + or Gram -.
Mainly Gram -, some Gram +.
Fluoroquinolones are well distributed and half-life is ____.
4 to 10 hours
Name some uses for Fluoroquinolones...
UTI's, bone, skin and joint infections, community-acquried pneumonia, bronchitis, sinusitis, Pseudomonas infections, prostatitis, conjunctivitis.
Fluoroquinolones are bactericidal or bacteriostatic?
What are some adverse reactions that differ in Fluoroquinolones?
Confusion, insomnia, visual impairment, photosensitivity, seizures, QT prolongations, arthralgias, cartilage damage and tendon rupture.
** avoid in children due to targeting in bones/joints.
How do bacteria evolve resistance to the quinolones?
Through chromosonal mutations in the genes that encode type II topoisomerases or through alterations in the expression of membrane porins and efflux pumps that determien the concentration of drug inside bacteria.
Name some examples of Fluoroquinolones?
Cipro, Gemifloxacin, Levofloxacin, Moxifloxacin, Norfloxacin, Ofloxacin
______ is an inhibitor of transcription (DNA is read and copied).
It inhibits bacterial RNA synthesis by binding to bacterial DNA dependent RNA-polymerase.
Rifampin is absorbed well, widely distributed, and half-life is____.
3-4 hours. Eliminated partly in feces and urine. Also distributed in CNS.
What are some uses for Rifampin?
Active TB, prophylaxis of meningococcal disease, Leprosy, in combination with another agent for serious staph infections.
Rifampin is bactericidal...t/f
What are some adverse reactions out of the norm for Rifampin?
Orange color of urine, sweat, and tears. Flu like symptoms, thrombocytopenia, acute renal failure, hepatotoxicity (extensively metabolized in liver).
Resistance evolves to Rifampin due to point mutations that decrease binding to _______.
Aminoglycosides binds to the ____ of the ribosomal subunit and irreversilby inhibits ____ synthesis.
inhibits protein synthesis
Aminoglycosides are Gram ____, and is the only one in the inhibitors of translation.
Gram (-) aerobes
Aminoglycosides have ____ GI absorption.
Poor...given IM or IV. Rectal excretion.
What are the uses for aminoglycosides?
Pseudomonas, E. Coli, Proteus, Resp tract inf, Skin and soft tissue infections, abdominal and UTI's.
Aminoglycosides are bactericidal...t/f
What are some abnormal adverse reactions to aminoglycosides?
Ototoxicity, vertigo, nephrotoxicity, thrombocytopenia
Resistance to aminoglycosides develops due to enzymes that inactive the aminoglycoside, impaired entry into the cell, and mutation of the 30s ribosomal subunit...t/f
Name the aminoglycosides...
Amikacin, Getamicin, Neomycin, Paromomycin, Streptinomycin, and Tobramycin.
What adverse reaction occurs if loop diuretics are given with aminoglycosides?
What aminoglycoside should we use less NDMR with?
The MOA of _______, binds REVERSIBLY to the 16S rRNA of the 3QS subunit of the bacterial ribosome stopping protein synthesis.
The inhibitors of translation that target both Gram neg and Gram pos are...
Tetracyclines, Macrolides and Chloramphenicol
Name the uses for Tetracyclines...
Mycoplasma pneumonia, Chlamydia trachomatis, Helicobacter pylori, Corynebacterium acnes.
Tetracyclines are bacteriostatic....t/f
What are the abnormal reactions to Tetracyclines?
Dizziness, photosensitivity, candidal infections, teeth discoloration.
Name Tetracycline drugs...
Doxycycline, Minocycline, Tetracyline, Glycylcyclines, Tigecycline
The MOA of ______, is that it binds to the 23S rRNA of the 50s ribosomal subunits of bacteria and inhibits translation of protein synthesis.
Name the uses for Macrolides...
Bacterial sinusitis, community-acquired pneumoina, mild to mod resp tract, skin and soft tissue infections, Mycobacterial infections, Pertussis, Pharyngitis.
Macrolides are bacteriostatic...t/f...
What are some abnormal adverse reactions to Macrolides?
Hepatitis, QT prolongation, pruritis
Resistance to _____ evolves due to reduced influx of increase efflux, Esterases that degrade, and alteration of ribosomal binding site.
Name the Macrolides...
Azithromycin(new black box warning for QT prolong), Clarithromycin, Erythromycin. Ketolides which includes Telithromycin
The MOA of ______ is binding to the 23S rRNA of the 50s ribosomal subunits of bacteria and inhibits protein synthesis by preventing the positioning of the aminoacyl moiety of tRNA.
Chloramphenicol is well absorbed ___ and ___.
PO and IV
What are the uses for Chloramphenicol?
Rarely used (so why are we learning about it?)
it's potential for toxicity, bacterial resistance and availability make it a rare drug.
Chloramphenicol is bacteriostatic but for some strains can be bactericidal...t/f...
What are the abnormal adverse reactions to Chloramphenicol?
Aplastic anemia and gray baby syndrome.
The MOA of ______ is the binding to the 50s ribosomal subunits of bacteria and inhibits protein synthesis.
Name the Gram + antibiotics...
Lincosamides, Streptogramins, Oxazolidinones
Lincosamides are extensively metabolized in the _____.
What are the uses for Lincosamides?
Strepococci and staph soft tissue and skin infections, MSSA, bacteroides anaerobic infections, surgical prophylaxis with PCN allergies.
Lincosamides are bacteriostatic...t/f...
What are some abnormal adverse reactions to Lincosamides?
Name the Lincosamide drug...
How does resistance to clindamycin develop?
Mutation of ribosomal receptor site and enzymatic inactivation.
The MOA of ______ is binding to the 50s ribosomal subunits which induces a conformational change in the ribosome of bacteria and inhibits protein synthesis.
What are the uses for Streptogramins?
Multidrug resistance strains of strep pneumonia, MSSA, Vanco resistant Enterococcus faceium
Streptogramins are eliminated by the ____.
Streptogramins are bactericidal...t/f...
What are the abnormal adverse reactions to Streptogramins?
Headache, myalgias, pseudomembranous colitis, elevation of liver enzymes
Resistance to Streptogramins develops due to ____ type pump.
Name a Streptogramin drug...
The MOA of ______ is the inhibition of bacterial protein synthesis by binding to the 23S ribosomal RNA of 50s subunit.
What are the uses for Oxazolidinones?
Community and hospital acquired pneumonia, bacterimia cause by VRE, MRSA pneumonia.
Oxazolidinones are bacteriostatic...t/f...
What are some abnormal adverse reations to Oxazolidinones?
Headache, thrombocytopenia, optic and peripheral neuropathy and lactic acidosis.
Resistance to Oxazolidinones develops from mutation to binding site on ____.
23S ribosomal RNA.
The drug _____ is an example of an Oxazolidinone.
The drug ____ is used for impetigo caused by MSSA or Strep pyogenes.
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