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MUSCULOSKELETAL DRUGS 2
Chlormaphenicol, Tetracyclines, Clindamycin, Ketolides
57
Pharmacology
Professional
02/21/2012

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Cards

Term
How do tetracyclines work?
Definition
Reversibly block the 30s ribosome to prevent protein synthesis
Term
What are two ways tetracyclines enter susceptible bacteria?
Definition
Simple diffusion AND active transport
Term
What 3 drugs are effective against resistant bacterial strains because they are not a substrate for the efflux pump in resistance?
Definition
Doxycycline, minocycline, tigecycline
Term
What are the 3 mechanisms by which bacteria convey resistance to tetracycline?
Definition
1- impaired influx or enhanced efflux by an active transport pump
2- ribosome protection
3- enzymatic inactivation of the drugs
Term
What drug is effective even against the Tet (A) efflux-expressing gram negative strains that have resistance to older tetracyclines?
Definition
Tigecycline
Term
Tet(K) in staph confers resistance to what drugs?
What drugs does it not confer resistance to?
Definition
Resistance to Tetracyclines
Not to doxycycline, minocycline, or tigecycline
Term
Tet(K) ribosomal protection expressed by gram positive strains confers resistance to what drugs?
What drugs does it not confer resistance to?
Definition
Resistance to Tetracyclines
Not to doxycycline, minocycline, or tigecycline
Term
Which of the tetracycline family drugs is absorbed most readily? Least readily?
Is given IV?
Definition
Most readily= Doxycycline and Minocycline
Least readily= chlortetracycline
Tigecycline is given IV
Term
What impairs absorption of tetracyclines except for doxycycline and minocycline?
Definition
Food in the GI tract impairs absorption
Term
Which tetracycline attains high concentrations in saliva and tears making it useful for eradication of the meningococcal carrier state?
Definition
Minocycline
Term
How are tetracyclines excreted?
Definition
Mainly in urine and in bile with enterohepatic circulation
Term
What two tetracyclines are eliminated via non-renal mechanisms and don't require does adjustments for renal failure?
Definition
Doxycycline and tigecycline
Term
What tetracyclines are short acting?
Definition
COT- Chlortetracycline, Oxytetracycline, Tetracycline
Term
What tetracyclines are intermediate acting?
Definition
Demeclocycline, Methacycline
Term
What tetracyclines are long acting?
Definition
Doxycycline, Minocycline
Term
Which tetracycline has a half life of 36 hours?
Definition
Tigecycline
Term
For what infections are tetracyclines most useful?
Definition
T-SCRAM- Trachoma, Spirochetes, Chlamydia, Rikettsiae, Anthrax, Mycoplasma Pneumonia
Term
How are tetracyclines used to treat H. Pylori-induced ulcers?
Definition
In combination with a proton-pump inhibitor and other agents
Term
What are tetracyclines combined with to treat plague, tularemia, and brucellosis?
Definition
Aminoglycosides
Term
For what protozoa are tetracyclines sometimes given?
Definition
Entamoeba Histolytica
Plasmodium Falciparum
Term
What tetracycline may be used in some ADH secreting tumors?
Definition
Demeclocycline
Term
What broad-spectrum tetracycline is useful against coagulase negative staph, staph aureus, and methicillin resistant strains?
Definition
Tigecycline
Term
Proteus and pseudomonas aeruginosa are resistant to what tetracycline?
Definition
Tigecycline
Term
What do tetracyclines do to the kidneys?
Definition
Cause nitrogen retention and (except for doxycycline and tigecycline) tend to accumulate in renal insufficiency
Term
Which tetracycline is especially likely to cause photosensitivity?
Definition
Demeclocycline
Term
What is the mechanism of action of Clindamycin?
Definition
Binds EXCLUSIVELY to the 50S ribosome and inhibits protein synthesis
Term
What bacterium are usually susceptible to clindamycin?
Definition
Streptococci, staphylococci, and pneumococci
Bacteroides are usually susceptible
Term
What bacterium are resistant to clindamycin?
Definition
Enterococci and gram negative aerobic organisms
Term
What is the mechanism of resistance to clindamycin?
Definition
-mutation of ribosomal receptor site
-constitutive expression of methylase causing modification of receptors
-enzymatic inactivation of clindamycin
Term
Gram negative aerobes are intrinsically resistant to what drug due to the poor permeability of their outer cell wall?
Definition
Clindamycin
Term
What drug penetrates well into abscesses and concentrates in phagocytic cells via active transport?
Definition
Clindamycin
Term
How is clindamycin used to treat penetrating wounds to the abdomen or gut?
Definition
In combination with cephalosporin or aminoglycosides
Term
What drug is used for septic abortion?
Definition
Clindamycin
Term
What drug is used for pelvic abscesses?
Definition
Clindamycin
Term
What drug is used in aspiration pneumonia?
Definition
Clindamycin
Term
What drug is used for prophylaxis against endocarditis in patients with valvular heart diseases?
Definition
Clindamycin
Term
Clindamycin is used with what drug as an effective alternative to trimethoprim-sulfamethozazole against moderate to severe pneumocystis jirovei in AIDS patients?
Definition
Primaquine
Term
What drug is combined with clindamycin to treat AIDS-related toxoplasmosis of the brain?
Definition
Pyrimethamine
Term
Severe diarrhea and pseudomembranous colitis as a result of clindamycin administration are most likely caused by what bug?
Definition
Clostridium difficile
Term
What is the mechanism of action of chloramphenicol?
Definition
Inhibits 50S ribosome
Term
What drug is active against rickettsia but NOT against chlamydia?
Definition
Chloramphenicol
Term
Haemophilus influenza is highly susceptible to:
Definition
Chloramphenicol
Term
N. Meningitis is highly susceptible to:
Definition
Chloramphenicol
Term
What is the mechanism of resistance to chloramphenicol?
Definition
Production of chloramphenicol acyl transferase, a plasmid-encoded enzyme
Term
What drug is conjugated in the liver (glucuronic acid) and eliminated in the urine? (probably a bunch, I know, but specific to this lecture)
Definition
Chloramphenicol
Term
When must the dose of chloramphenicol be reduced?
Definition
In hepatic insufficiency, but NOT in renal insufficiency
Term
What drug causes bone marrow disturbances/ decreased production of red blood cells?
Definition
Chloramphenicol
Term
What drug causes aplastic anemia?
Definition
Chloramphenicol
Term
What drug causes GRAY BABY SYNDROME?
Definition
Chloramphenicol
Term
What is gray baby syndrome?
Definition
Vomiting, flaccidity, hypothermia, gray color shock and collapse
-caused by chloramphenicol
Term
What drugs are metabolized a slower rate in the presence of chloramphenicol?
Definition
Phenytoin, tolbutamide, chlorpropamide, and warfarin
-causes increase in half-life
Term
Chloramphenicol can antagonize the effects of what drugs?
Definition
Penicillin and aminoglycosides
Term
What do we use PREFERENTIALLY to treat Chlamydial Conjunctivitis?
Definition
CHLORTETRACYCLINE
Term
What do we use to treat malaria and why?
Definition
Doxycycline- fewer effect on GI
Term
How do we treat Rocky Mountain Spotted Fever? (first line, second line)
Definition
Tetracyclines- first line; Chloramphenicol- second line
Term
How do we treat haemophilus influenza?
Definition
Chloramphenicol
Term
What drug penetrates the CNS well?
Definition
Chloramphenicol
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