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50 Cards in this Set
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name the 1st gen tetracyclines
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Oxytetracyline
Tetracycline Demeclocycline |
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name the 2nd gen tetracyclines
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-doxycline
-minocycline |
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are first gen tetracyclines used?
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so much resistance now, not usually used, 2nd gen tetra are used more
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moa of tetracyclines
remember clean tag |
-Inhibit bacterial protein synthesis by binding to 30 S ribosomal subunit
-Entry into the cell - Gram (-): passive diffusion through the porin proteins followed by energy dependent active transport - Gram (+): less well understood, does require energy-dependent transport system |
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tetracyclines are static or cidal
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static
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macrolides are statis or cidal
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static
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spectrum of activity of tetracyclines
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In vitro activity greater for gram (+) than gram (-), high level of resistance for gram (-)
Gram (+) Streptococcus spp. Staph. aureus (mino>doxy>>tetra) Gram (-) H. influenzae Neisseria spp. (PCN sensitive only, high resistance) Vibrio cholerae - DOC Campylobacter jejuni Pasteurella multocida Anaerobes (G-) Bacteroides spp. (doxy>mino>tetra; doxy < other anaerobic antibiotic) Prevotella spp. Fusobacterium spp. (G+) Propionibacterium Peptococcus (limited activity) |
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do tetra cover gram neg rods
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no, high level of resistance for gram -
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doc of vibrio cholerae
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tetracyclines
Other H. pylori Clamydia spp. - DOC Mycoplasma pneumoniae Borrelia burgdorferi (Lyme disease) Rickettsial spp. - DOC Treponema pallidum (syphilis) Mycobacterium marinum Legionella spp. |
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doc for tetracyclines
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-vibrio cholerae
- rickettsial -clamydia spp |
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1st and 2nd gen tetra affect with food
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-TCN: 60 – 80%, decreased with food
- Doxycycline (95%), minocycline (100%) - effect of food is insignificant 1st gen is affected by food,2nd gen is not affected by food |
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tetracycline distribution
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-Wide distribution throughout the body
- Excellent penetration into most fluids and tissues including CSF - Doxycycline and minocycline are more lipid soluble superior tissue penetration - Crosses placenta and secreted in breast milk, accumulates in fetal bone and teeth |
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advantages of 2nd gen tetra
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- food does not affect absorption
- doxy and minocycline are more lipid soluble--> superior tissue penetration |
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tetracyclines are safe in pregancy and lactation
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no bc crosses placenta and secreted in breast milk, accumulated in fetal bone and teeth
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tcn elimination
doxycycline minocycline which needs dosage adjustment |
tcn- renal
doxy- renal + hepatic, no adj in renal or heaptic dysfxn minocycline- hepatic --> renal, dec dose in renal failure |
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do you have to dosage adjust for tetracycline in renal or hepatic
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no, dnt have to worry about in renal or hepatic
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half life of tcn, doxy, mino, who has the longest, shortest
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- tcn= 8-11 hr
-doxy= 12-15 hr -mino= 15 hrs |
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tetracycline adr
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- gi:
- Diarrhea (TCN) - N/V/epigastric discomfort - Esophageal ulcerations/strictures (TCN, doxy – avoid use at bed time) - Acute fatty necrosis of liver (rare, >2 gm/day TCN) Photosensitivity -Teeth/Bones: - Brown-to-yellow permanent discoloration of teeth in children under 8, dose & duration related - Deposition of drug in teeth and bones during calcification process - Depression of bone growth - Avoid in children under 8 and during pregnancy/lactation Renal: - Aggravates uremia in ESRD patients, provokes catabolic effect by inhibiting protein synthesis --> increased azotemia (TCN) - Nephrogenic diabetes insipius (demeclocycline) CNS: - vestibular toxicity: dizziness,ataxia, N/V (minocycline) |
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tetra unique adr for gi and how to avoid
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- esophageal ulcerations/strictures
(TCN, doxy- avoid use at bedtime) - take at dinner, and take w/ full glass of h20 |
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tetra pregnancy category
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D
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tetracycline drug interactions
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-Reduced absorption by divalent/trivalent cation chelation
- Antacids containing Ca++, Mg++, & Al+++ (take 4 hrs before or 2 hrs after TCN) - Iron & zinc supplements - Dairy products - TCN>>>Doxy>Mino - Decreased efficacy of OCP by reducing conjugated estrogen levels |
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provide some patient education when dispensing tetracycline abx
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- can cause esophageal ulcerations, so take at dinner w/ full glass of h20 and do not lie down for 30 mins
- do not give to children < 8yo bc it will permananetly discolor teeth - if you have preganant or plan to be pregnant, do not take - cz dizzziness, dec driving or any activity that require intense concentration |
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tigercycline brand name
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tygacil
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tigecycline class of antibiotics
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glycylcyclines
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tigercycline substitution is important bc
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-broader spectrum of activity
-allows defense against efflux pump and ribosomal resistance mechanisms |
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moa of tigercycline
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-Inhibit bacterial protein synthesis by binding to 30S ribosomal subunit
- Binding is 5 times stronger than TCNs |
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which gram + is Tigecycline effective vs
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S. aureus (MSSA & MRSA)
Enterococcus faecalis |
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tigecycline has the strongest coverage for gram positive, gram neg or anaerobes
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anerobes
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tigercycline spectrum of activity
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Gram +
S. aureus (MSSA & MRSA) Streptococcus agalactiae Streptococcus pyogenes Streptococcus anginosus Enterococcus faecalis Gram - ( bacilli and rods) (think ceck) E. coli Klebsiella spp. Citrobacter freundii Enterobacter cloacae Anaerobes Bacteroides fragilis Bacteroides thetaiotaomicrons Bacteroides uniformis Bacteroides vulgaris Clostridium perfringens Peptostreptococcus micros |
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tigercycline has no activity vs
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-Pseudomonas aeruginosa
-Proteus mirabilis -Serratia marscens -Stenotrophomonas maltophilia |
psps
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class of abx that have bfrag converage
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- pcn
-amox + sulbactam -cephs (2nd gen only) -pip/ticar -carbapenems -tigecycline |
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tigercycline only available formulation is
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iv
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abosrption of iv tigercycline is
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poor (iv formulation only)
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distribution of tigercycline, tissue or serum
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Distribution
-extensively distributed, tissue concentration > serum |
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tigecycline elimination
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mixed, mostly hepatic
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clinical indications for tigecycline
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- Complicated skin and skin structure infections
- complicated intra abdominal infections - community acquired pneumonia ( not clinically effective ) |
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hallmark tigecycline adr
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-nausea and vomitting
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tigercycline adr
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1) GI: nausea, vomiting, diarhhea
2) liver: mild inc in ast/alt 3) other: fever, ha, dizziness |
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pregnancy category
tetracycline tigercycline nitrofurantoin |
-tetra and tiger =D
-nitro= B |
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nitrofurantoin moa
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-Poorly understood
- Undergoes enzymatic reduction (bacteria>>mammalian cells) to and active metabolite which inhibits bacterial protein synthesis and damage DNA |
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nitrofurantoin is static or cidal?
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Mostly bacteriostatic, bactericidal at very high concentrations
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nitro spectrum of activity
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E. coli
Citrobacter spp Staph. saprophyticus Enterococcus (including VRE) |
see c
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nitrofurantoin absorption
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-Rapid and complete absorption from the GI tract
-Food enhances absorption\ |
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nitrofurantoin distribution
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Achieves high concentration in urine but subtherapeutic concentration in
blood and tissue |
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nitrofurantoin elimination
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renal
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nitrofurantoin crcl limit
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Avoid use in CrCl < 40 ml/min, efficacy compromised due to minimal
urinary excretion |
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nitrofurantoin clinical indication and dosage
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UTI treatment = q 6 hr
UTI prophylaxis = qd |
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nitrofurantoin pregnancy category
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B
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nitrofuratoin adr
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GI: N/V/D, macrocrystalline preparation better tolerated
Take with food -Pulmonary: Acute pneumonitis - reversible hypersensitivity reaction - occurs within hours to weeks - accompanied by eosinophilia and infiltrates Subacute & chronic pulmonary reactions - Onset 1 or 6 months - Direct toxic effect on the lung - Gradual onset of progressive nonproductive cough, dyspnea, fever, & infiltrates - May be irreversible and fatal - Hematologic: Hemolytic anemia (rare, higher in pt with G6PD deficiency) Leukopenia & aplastic anemia (very rare) - Urine discoloration to brown color |
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nitrofuratoin counseling tip
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- take w/ food to inc absorption of drug
- may discolor urine to brown color, wont hurt you |
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