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77 Cards in this Set
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Antagonistic when used in combination with Beta lactam antibiotics
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Tetracyclines
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tetracycline mech of action
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Bacteriostatic
Binds reversibly to 30 S Inhibits attachment of aminoacyl-tRNA |
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Mechanism of Resistance
against tetracyclines |
*****facilitated efflux of drug****
Decreased entry |
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main usage spectrum of tetracyclines
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Atypical agents – Mycoplasma, Chlamydia, Chancroid, Rickettsia, Borrelia, Entamoeba
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Rickettsia causes
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rocky mt spotted fever
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DOC for rickettsia/rocky mt spotted fever
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tetracyclines
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Lyme Disease doc
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Lyme Disease (borrelia doc = ceftriaxone)
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tetracycline toxicity
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***Fetal and childhood effects on bones and teeth – Contraindication!
***Pseudotumor cebri ***Jarisch - Herxheimer reaction Hepatic necrosis (especially Doxy) may be fatal Photosensitivity Renal – renal tubular acidosis |
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Tigecycline mech of action
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Bacteriostatic
binds 30s post antibiotic effect |
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tigecycline metabolism
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metabolized in liver
excreted in bile/biliary tract |
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pseudotumor cerebri
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tetracycline and tigecycline
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chloramphenicol MOA
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bacteriostatic
binds 50s Inhibits peptidyl transferase |
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mech of resistance against chloramphenicol
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inactivating enzymes made by plasmid
reduced permeability |
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chloramphenicol clinical use
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drug of last choice for
brain abscess rocky mt spotted fever |
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chloramphenicol toxicity
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Idiosyncratic Aplastic anemia, irreversible
Dose related Aplastic anemia Gray baby syndrome – cant conjugate chloramphenicol because of immaturity/decreased levels of glucuronosyl transferase |
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which drug classes concentrate in respiratory secretions
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macrolides n ketolides concentrate here
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macrolides ex?
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Erythromycin
Clarithromycin Azithromycin |
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ketolides ex
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telithromycin
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which drug concentrates in phagocytic cells
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azithromycin concentrates here
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macrolides/ketolides MOA
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bacteriostatic
binds 50s Prevents ribosomal translocation down m-RNA |
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mech of resistance of macrolides/ketolides
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***Target alteration – receptor on ribosome is altered by a methylase, encoded by erm beta gene on the plasmid***
**Inactivating enzymes** dec permeability inc efflux |
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DOC salmonella (typhoid fever)
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azythromycin
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doc Legionnaire’s disease
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azythromycin
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DOC Mycoplasma
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azythromycin
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Bordetella pertussis
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azythromycin
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doc Atypical Mycobacteria
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Clarithromycin doc
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azythromycin doc for
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salmonella
legionnella mycoplasma bordetella pertusis |
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macrolide toxicity
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***pyloric stenosis in infants***
**rarely cardiotoxicity and death** |
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ketolides (telithromycin) toxicity
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***Blurred Vison
***Prolonged QT Interval ***Exacerbation of Myasthenia gravis*** |
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clindamycin MOA
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bacteriostatic
binds 50s prevents ribosomal translocation down the mRNA |
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clindamycin spectrum
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Excellent for g+ (including Staph aureus, severe invasive strep), NOT Enterococci
Excellent activity against anaerobes |
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clindamycin toxicity
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Pseudomembranous colitis secondary to C. diffocoel overgrowth.
+ the usual |
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synercid moa
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bacteriocidal
binds 50s prevents ribosomal translocation down mRNA prevents protein synthesis at elongation |
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mech of resistance against synercid
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efflux
inactivating enzymes target alteration |
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synercid spectrum
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Spectrum
Staph aureus and epidermidis, Strep pyogenes and aglacia, Some enterococci |
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synercid toxicity
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Precludes widespread use:
drug interactions, phlebitis 40%, jaundice 30%, arthralgia and myalgia 20% |
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this drug has Better penetration into lung (pneumonia) than Vancomycin
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linezolid
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linezolid mech of action
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bacteriostatic
binds 50s inhibits initiation complex n translocation of tRNA |
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linezolid resistance
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target alteration so dec affinity
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linezolid spectrum
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All aerobic gram positive organisms especially resistant staph, strep and enterococci
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linezolid toxicity
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Thrombocytopenia and neutropenia (reversable bone marrow suppression)
Weak MAO inhibitor ***Hyperserotonin effect [rare but severe] in patients on SSRI drugs (headache, syncope, palpitations) ***Rare Lactic acidosis |
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sulfonamides resemble
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paba
para amino benzoic acid |
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sulfa drugs ex
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salfisoxazole
sulfamethoxazole sulfadiazine |
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sulfonamides mech of action
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bacteriostatic
inhibit synthesis of folic acid via action on Dihydropteroate synthetase |
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trimethoprim action
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inhibit dihydrofolate reductase needed to make folic acid.
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**mech of resistance agaisnt sulfonamides
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**porin mutations - dec intracellular accumulation
**dec sensitivity of dihydropteroate synthetase **inc production of PABA |
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combo of tmp-sulfa called
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Cotrimoxazole
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sulfonamides spectrum
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Gram negative bacteria: Neisseria meningitidis, E. coli
Gram positive bacteria: Strep pyogenes, Strep pneumoniae, some MSSA and MRSA Chlamydia (but not for neonate) Nocardia ****Toxoplasma ****Pneumocystis |
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sulfonamides clinical uses
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Uncomplicated urinary tract infections (TMP – Sulfa methoxazole)
Otitis Media (TMP – Sulfamethoxazole) Topical burn prophylaxis (Mafenide acetate – Sulfamylon) (Silver sulfadiazine) Ulcerative colitis (Salicylazosulfapyridine – Azulfidine) Toxoplasmosis (pyrimethamine added as second drug) PCP prophylaxis and treatment (TMP – Sulfa) |
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drug for toxoplasmosis
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sulfonamides + pyrimethamine****
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drug for PCP prophylaxis n tx
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tmp-sulfa
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sulfonamides resemble
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paba
para amino benzoic acid |
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sulfa drugs ex
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salfisoxazole
sulfamethoxazole sulfadiazine |
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sulfonamides mech of action
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bacteriostatic
inhibit synthesis of folic acid via action on Dihydropteroate synthetase |
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trimethoprim action
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inhibit dihydrofolate reductase needed to make folic acid.
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**mech of resistance agaisnt sulfonamides
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**porin mutations - dec intracellular accumulation
**dec sensitivity of dihydropteroate synthetase **inc production of PABA |
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combo of tmp-sulfa called
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Cotrimoxazole
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sulfonamides spectrum
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Gram negative bacteria: Neisseria meningitidis, E. coli
Gram positive bacteria: Strep pyogenes, Strep pneumoniae, some MSSA and MRSA Chlamydia (but not for neonate) Nocardia ****Toxoplasma ****Pneumocystis |
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sulfonamides clinical uses
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Uncomplicated urinary tract infections (TMP – Sulfa methoxazole)
Otitis Media (TMP – Sulfamethoxazole) Topical burn prophylaxis (Mafenide acetate – Sulfamylon) (Silver sulfadiazine) Ulcerative colitis (Salicylazosulfapyridine – Azulfidine) Toxoplasmosis (pyrimethamine added as second drug) PCP prophylaxis and treatment (TMP – Sulfa) Rheumatic Fever Prophylaxis (in PCN allergic) |
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drug for toxoplasmosis
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sulfonamides + pyrimethamine****
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drug for PCP prophylaxis n tx
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tmp-sulfa
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drug for Topical burn prophylaxis
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Silver sulfadiazine
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sulfonamides toxicity
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Hypersensitivity (Stevens-Johnson Syndrome)
Severe hepato-toxicity in HLA-B 5701 positive recipients, Transaminase elevation Neonatal hyperbilirubinemia with resultant kernicterus [cerebral palsey and deafness] (contraindicated in late pregnancy) Pancytopenia (bone marrow suppression) Acute haemolytic anemia in G6PD deficiency Phototoxicity Nephrotoxicity, Severe dysglycemia in elderly |
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ceftriaxone can displace bilirubin in neonates n give kernictirus. substitute for ceftriaxone?
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cefotaxime
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FLUROQUINOLONES examples
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Ciprofloxacin Levofloxacin Moxifloxacin
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quinolones oral absorption hindered by
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oral absorption hindered by antacids
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quinolones mech of action
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Bacteriocidal inhibition of DNA Gyrase topoisomerase II and IV
Exhibit post-antibiotic effects |
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mech of resistance against quinolones
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***Alteration of DNA gyrase (target mutation)
Increased efflux Alteration of bacterial permeability to drug |
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quinolones spectrum
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Gram negatives, including pseudomonas, H. influenzae, morexella, salmonella, shigella, E.coli, campylobacter,
Gram positive (especially newest fluoroquinolones) including PCN resistant Strep pneumonia Atypicals: Legionella, chlamydia, Mycoplasma |
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fluroquinolones dont work against
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anaerobes
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3 drugs for anaerobes
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cefoxitin
cefotetan clindamycin |
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quinolones spectrum
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***Prostate infections
***Respiratory infections; including those caused by atypical agents, sever community (CAP), and ventolator (VAP) acquired pneumonias Urinary tract infections; gonorrhea Enteric infections and Typhoid fever Osteomyelitis Soft tissue infections Pseudomonas infections (resistance may develop rapidly |
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DOC for prostate infections
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quinolones/fluoroquinolones
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DOC for community and ventilator acquired pneumonia
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quinolones/fluoroquinolones
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quinolones toxicity
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****Achilles tendon rupture in adults
***Articular cartilage injury in under 18yo. So NOT USEED IN UNDER 18 YEARS OF AGE ***CONTRAINDICATED IN PREGNANCY Older quinolones demonstrate serious neurotoxicity (seizures) G.I. upset is common (5%) Increase QT interval Candida overgrowth (superinfection) |
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Imipenem is given with which drug and why
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cilastatin. it decreases imipenem's renal inactivatin by dehydropeptidase 1
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role of cilastatin
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given with imipenem to decrease its renal inactivation by dehydropeptidase 1.
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