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KG - Pharmacology > Fluoroquinolones & Drugs for UTIs > Flashcards

Fluoroquinolones & Drugs for UTIs Flashcards

1
Q

stats about UTIs?

A
  • 15% prescribed antibiotics in US
  • $1 billion spent on treating UTIs
  • account for 7 million office visits, a million ER visits, 100,000 hospitalizations per year
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2
Q

UTI common pathogens?

A
  • Escherichia coli = causes most community acquired infections (70-80%)
  • Staphylococcus saprophyticus, G+ organism = causes 10-15%
  • catheter associated UTIs caused by G- bacteria - proteus, klebsiella, seratia, pseudomonas
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3
Q

how do cranberries help w/ UTIs?

A

prevent flagella from forming in bacteria, help eliminate colonization

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4
Q

kidneys & UTI?

A

can become infected by urine back flow or blockage

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5
Q

ureters & UTI?

A

can carry bacteria between kidneys and bladder

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6
Q

bladder & UTI?

A

can become infected when urine collected there doesn’t empty completely

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7
Q

rectum & UTI?

A

normally has bacteria in it

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8
Q

urethra in women & UTI?

A

in women is short and near vagina, makes it easy for bacteria to enter urinary tract

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9
Q

vagina & UTI?

A

allows entry for bacteria from rectum or from outside body, bacteria may then enter urethra

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10
Q

prostate & UTI?

A

surrounds part of urethra, may enlarge w/ age and block urine flow, can cause infection

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11
Q

urethra in men & UTI?

A

longer in men, harder for bacteria to reach inner structure

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12
Q

penis & UTI?

A

comes in contact w/ bacteria that can travel up urethra

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13
Q

pharmacodynamics of fluoroquinolones?

A

target DNA, DNA replication (DNA gyrase)

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14
Q

which fluoroquinolone is the DOC for UTIs?

A

ciprofloxacin (cipro)

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15
Q

what is CIPROFLOXACIN (cipro) used for?

A
  • systemic infections
  • UTIs
  • anthrax prophylaxis
  • P. AERUGINOSA
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16
Q

what is NORFLOXACIN (noroxin) used for?

A
  • UTIs

- prostatitis

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17
Q

what is OFLOXACIN (floxin) used for?

A
  • prostatitis
  • STDs, not syphilis
  • some systemic
  • TB
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18
Q

what is LOMEFLOXACIN (maxaquin) used for?

A
  • UTIs

- bronchitis

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19
Q

what is LEVOFLOXACIN (levaquin) used for?

A
  • community acquired pneumonia (CAP)
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20
Q

what is MOXIFLOXACIN (avelox) used for?

A
  • active against penicillin resistant S. pneumonia

- anaerobes

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21
Q

what is GATIFLOXACIN (tequin) used for?

A
  • ocular application only
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22
Q

what is GEMIFLOXACIN (factive) used for?

A
  • active against penicillin resistant S. pneumoniae
  • anaerobes
  • CAP
23
Q

formula for fluoroquinolones?

A

medically important ones are synthetically fluorinated analogs of naladixic acid

24
Q

mechanism of fluoriquinolones

A
  • inhibition of DNA GYRASE prevents relaxation of positively supercoiled DNA that is required for normal transcription and replication (unwinds, replication, rewinds)
  • inhibition of TOPO IV interferes w/ separation of replicated chromosomes to daughter cells
  • BACTERICIDAL
25
Q

spectrum of fluoroquinolones

A
  • primarily effective against aerobic G- rods (incl Enterobacteriaeceae, Citrobacter, Serratia, Neisseria)
  • good G+ coverage (incl MRSA & pen resistant S. Pneum – moxi- & gemifloxacin)
  • antipseudomonal - CIPRO
  • effective prophylactic against anthrax - CIPRO = DOC
  • NOT EFFECTIVE against infections (except trove-, maxi-, gemifloxacin)
26
Q

pharmacokinetics of fluoroquinolones

A
  • well absorbed ORALLY - iron, Mg, Ca decrease absorption
  • widely distributed, excellent tissue penetration (prostatitis - norflox/oflox)
  • poor CNS penetration (newer ones better)
  • most excreted through kidney, can be blocked by probenecid
27
Q

resistance of fluoroquinolones

A
  • change in gyrase enzyme (mutation)
  • decreased permeability of bacteria
  • antibiotic modification (ciprofloxacin)
28
Q

adverse effects of fluoroquinolones

A
  • GI DISTURBANCES (nausea, vomiting, diarrhea)
  • headache, restlessness, dizziness, tremors
  • skin rxn (rash, pruritis)
  • all quinolones increase QT interval
  • transient elevations of serum transaminase, LDH, alkaline phosphatases, etc
  • CARTILAGE EROSIONS in animals (not to be used in children!)
  • TENDON RUPTURE
29
Q

contraindications of fluoroquinolones

A
  • pregnant women

- children (cartilage damage < 18 yrs)

30
Q

DOC Enterobacter/Citrobacter/Serratia?

A
  • TMP-SMZ
  • quinolone
  • carbapenem
31
Q

DOC shigella?

A

quinolone

32
Q

DOC salmonella?

A
  • TMP-SMZ
  • quinolone
  • cephalosporin (3rd gen)
33
Q

DOC brucella species?

A

doxycycline + rifampin or aminoglycoside

34
Q

DOC helicobacter pylori?

A

bismuth + metronidazole + tetracycline or amoxicillin

35
Q

DOC pseudomonas aeruginosa?

A

antipseudomonal penicillin + aminoglycoside

36
Q

DOC stenotrophomonas maltophilia?

A

TMP-SMZ

37
Q

DOC legionella species?

A

azithromycin + rifampin
OR
quinolone + rifampin

38
Q

characteristics METRONIDAZOLE (MOA)

A
  • prodrug - nonenzymatically reduced by reacting w/ reduced ferredoxin (only found in anaerobes)
  • metronidazole metabolites are taken up into BACTERIAL DNA and form unstable molecules - BACTERICIDAL
39
Q

spectrum of metronidazole

A
  • potent antibacterial activity against ANAEROBES
  • G- and G+ bacilli (anaerobes)
  • indicated for treatment of anaerobic or mixed intra-abdominal infections, vaginitis (bacterial), RTI, pseudomembranous colitis, endocarditis, acute gingivitis, dental infection
  • helicobacter pylori eradication therapy as part of multi drug regimen
40
Q

pharmacokinetics of metronidazole

A
  • oral, IV, topical
  • liver metabolism
  • eliminated in urine
41
Q

adverse rxns of metronidazole

A
  • GI disturbances
  • central and peripheral nervous system toxicity - convulsive seizures and peripheral neuropathy (w/ prolonged use) are serious adverse effects (rare)
  • candida superinfection
  • hypersensitivity
42
Q

exclusive UTI drugs?

A
  • nitrofuratoin
  • methenamine
  • naladixic acid
43
Q

properties of exclusive UTI drugs?

A
  • renally excreted
  • achieve HIGH URINARY CONCENTRATIONS - do not achieve therapeutic concentrations anywhere else in body
  • bactericidal activity in urine
44
Q

characteristics of NITROFURATOIN (furadantin)

A
  • DAMAGES BACTERIAL DNA (prodrug)
  • reduced in bacterial cells to highly reactive intermediate that can attack ribosomal proteins, DNA, metabolism, macromolecules
  • wide spectrum of antibacteriostatic & bactericidal activity against G- and G+ bacteria (E coli, S pyogenes, citrobacter, klebsiella, enterobacter, salmonella, shigella, serratia, indole positive proteus)
  • most proteus and pseudomonas = resistant
  • treatment of uncomplicated UTIs - alternative for treatment of E coli resistant to trimethoprim-sulfamethoxazole & fluoroquinolones
45
Q

absorption/activity of nitrofuratoin?

A
  • rapid/complete absorption after ORAL use
  • acidic urine increases therapeutic action (pH < 5.5)
  • drug activity decreased when glomerular filtration impaired
  • SHOULD NOT BE USED IF CREATININE CLEARANCE < 50 mL/min - w/ renal failure antibiotic does not reach sufficient levels in urine for antibacterial activity
  • colors urine brown
46
Q

toxicity of nitrofuratoin

A
  • nausea, vomiting, diarrhea common (less GI upset if taken w/ food)
  • allergic rxns - chills, fever, leukopenia, granulocytopenia, cholestatic jaundice, HEPATOCELLULAR DAMAGE, HEMOLYTIC ANEMIA (in G6PD deficiency)
  • INTERSTITIAL PULMONARY FIBROSIS (in chronic usage, esp in elderly)
  • neuro disorders - severe polyneuropathies & demyelination/degeneration of neurons
47
Q

contraindications of nitrofuratoin

A
  • pregnancy(38-42 wks gestation)
  • less than one month age
  • impaired renal function
  • allergy
48
Q

characteristics of METHENAMINE

A
  • ORAL (prodrug) - decomposes to FORMALDEHYDE & AMMONIA in the acid medium of urinary tract
  • acidic urine increases therapeutic action
  • well absorbed orally, but 10-30% occurs in stomach
  • methenamine active against G- organism, esp E. Coli
  • bacterial resistance to formaldehyde does not develop
49
Q

spectrum of methenamine

A
  • almost all bacteria are sensitive - those that increase pH of urine inhibit release of formaldehyde (proteus), combine w/ weak organic acid (hippuric acid)
50
Q

toxicity of methenamine

A
  • essentially non toxic bc little decomposition takes place in body until appearing in urine
  • GI distress, occasionally allergic rxns
51
Q

contraindications of methenamine

A
  • hepatic insufficiency - conversion to formaldehyde releases ammonia
  • renal insufficiency - crystalluria (low urinary output)
52
Q

characteristics of NALIDIXIC ACID

A
  • INHIBITS DNA SYNTHESIS of susceptible G- organisms
  • not for systemic antibacterial use
  • well absorbed ORALLY - iron, Mg, calcium lowers absorption
53
Q

toxicity of nalidixic acid

A
  • nausea, vomiting, abdominal pain, diarrhea
  • allergic rxns - rashes, urticaria, eosinophilia, photosensitivity, visual disturbances, photophobia, drowsiness, weakness, headache, dizziness, convulsions, occasionally cholestatic jaundice, blood dyscrasia, hemolytic anemia, etc
  • nitrofurantoin antagonizes action of nalidixic acid if both agents are used simultaneously

KG - Pharmacology (8 decks)

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