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Pharm Exam 3
Antimicrobials II
149
Other
Professional
03/04/2011

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Cards

Term
What drugs are in this Drug Class: Folic acid synthesis inhibition?
Definition
Sulfonamides & Trimethoprim
Term
What drugs are in this Drug Class: Inhibit DNA gyrase, DNA synthesis?
Definition
Fluoroquinolones
Term
What drugs are in this Drug Class: DNA damage?
Definition
Metronidazole
Term
What drugs are in this Drug Class: Inhibit mRNA synthesis?
Definition
Rifampin
Term
Sulfisoxazole is what type of drug?
Definition
sulfonamide antibiotic
Term
Sulfamethoxazole is what type of drug?
Definition
Sulfonamide antibiotic
Term
Sulfonamides are Analogs of _____
Definition
PABA (para-amino benzoic acid)
Term
Sulfonamides Compete with ____ in synthesis of folic acid a required precursor of ___ & ____ DNA bases
Definition
PABA
purine & pyrimidine
Term
Trimethoprim is what type of drug?
Definition
An antibiotic that inhibits folic acid synthesis
Term
Trimethoprim is a Competitive inhibitor of ______ and Inhibits ____ conversion to purines/pyrimidines
Definition
dihydrofolate reductase
folic acid
Term
Sulfamethoxazole + Trimethoprim
(Co-trimoxazole, SMZ/TMP or TMP-SMX, Bactrim, Septra)
Combination produces a _____ inhibition because two sequential steps in folic acid pathway are blocked
Definition
synergistic
* know bactrim
Term
Sulfonamides & Trimethoprim has ____ Toxicity
Definition
Selective
Term
Bacteria have no ____ transport for folate and must synthesize it. ____ inhibit this synthesis.
Definition
active
Sulfas
Term
Trimethoprim is 20,000 x more potent at inhibiting ______ dihydrofolate reductase than ____ enzyme.
Definition
bacterial
human
Term
Humans cannot synthesize folate – must obtain from diet via Active uptake. Human dietary folate deficiency causes ____.
Definition
megaloblastic anemia
Term
____ is another folate antagonist (inhibits dihydrofolate reductase) used clinically at high does to treat cancer & at low doses to treat RA (rheumatoid arthritis) and severe psoriasis
Definition
methotrexate
Term
Sulfonamides & Trimethoprim:
Bacterio____
Very ____ spectrum
Distribute to ___ body fluids including ___
Definition
static
broad
all
CSF
Term
Sulfonamides & Trimethoprim Use:
Wide use throughout world because cheap & effective
USA: less use because many resistant strains, allergic reactions, penicillins and other drugs to use
Most used is ____
Resistance developed:
(a) due to the ability of bacteria to ___ the drug
(b) to produce more ___ to counteract sulfonamide drug
Definition
TMP-SMX
destroy
PABA
Term
SMX-TMP is what type of drug?
Definition
Sulfamethoxazole + Trimethoprim
Term
Co-trimoxazole is what type of drug?
Definition
Sulfamethoxazole + Trimethoprim
Term
Bactrim is what type of drug?
Definition
Sulfamethoxazole + Trimethoprim
Term
Septra is what type of drug?
Definition
Sulfamethoxazole + Trimethoprim
Term
_____ is antibiotic used for Chronic and recurrent UTIs
_____ first choice for acute, uncomplicated UTI
Definition
SMX-TMP
Fluoroquinolone (Cipro)
Term
Trimethoprim concentrates in ____ & ____
Definition
prostate and vagina
Term
_______ is the antibiotic used for Acute gonococcal urethritis & oropharyngeal gonococcal inf.
Definition
SMX-TMP
Term
________ is the antibiotic (drug of choice) for Pneumocystis carinii pneumonia ->Most common opportunistic fungus infections of AIDS
Definition
SMX-TMP
Term
____ is the antibiotic used for GI infections & prophylaxis for travelers’ diarrhea -> E. coli, Proteus mirabilis, Salmonella typhi, Shigella
Definition
SMX-TMP
Term
_____ is the antibiotic used for Recurrent otitis media
Definition
Sulfas
Term
____ is the antibiotic used for Nocardiosis
Definition
sulfas
Term

Sulfonamides & Trimethoprim Adverse Effects: Hypersensitivity

- Rashes common, angioedema, ____

- Many drugs are derivatives of sulfonamides, all these

  can cause hypersensitivity reactions, e.g., diuretics

  and sulfonylurea oral hypoglycemic agents

_____ in newborn

- Displaces bilirubin from albumin

- Contra-indicated if <__ months old, or __ at term ____________

- due to poor solubility of older sulfas

_____________

- In patients with G6PD deficiency

Definition
Steven’s-Johnson syndrome
Kernicterus
2
pregnant
Crystalluria
Hemolytic anemia
Term
Ciprofloxacin (Cipro) is what type of drug?
Definition
Fluoroquinolone
Term
Norfloxacin is what type of drug?
Definition
Fluoroquinolone
Term
Ofloxacin is what type of drug?
Definition
Fluoroquinolone
Term
Levofloxacin is what type of drug?
Definition
Fluoroquinolone
Term
Enoxacin is what type of drug?
Definition
Fluoroquinolone
Term
Sparfloxacin is what type of drug?
Definition
Fluoroquinolone
Term
Lomefloxacin is what type of drug?
Definition
Fluoroquinolone
Term
Moxifloxacin is what type of drug?
Definition
Fluoroquinolone
Term
Trovafloxacin is what type of drug?
Definition
Fluoroquinolone
Term
Fluoroquinolones Mechanism:
Inhibit _____ (_______)
Induces cleavage of ___
Bacterio____
Definition
DNA gyrase (topoisomerase II)
DNA
cidal
Term
Fluoroquinolones Use:
Relatively non-toxic, well tolerated, ____ spectrum, excellent ____ bioavailability.
Definition
broad
oral
Term
Fluoroquinolone names all end in _____
Definition
oxacin
Term
Fluoroquinolones Resistance:
Inappropriate overuse has led to increasing resistance. Don’t use for routine upper & lower ____ infections or ___ or ___ tissue infections
Mechanism: Mutated ____ or decreased permeability through ____
Definition
respiratory
skin
soft
gyrase
porins
Term
Fluoroquinolones Spectrum:
Very ___ spectrum but generally more active against gram (__) than gram (__) aerobes
Not effective against ____
Definition
broad
-
+
anaerobes
Term
Fluoroquinolones Pharmacokinetics:
Widely distributed in ___
Renal secretion of ____ drug in urine
Definition
tissues
active
Term
What antibiotic is used for Anthrax -> Bacillus anthracis?
Definition
Ciprofloxacin (Cipro)
Term
Fluoroquinolones are used in ___ Tract & __ Tract Infections
Gram (-) rods E. coli, Enterobacter, Klebsiella pneumoniae, Proteus mirabilis, Serratia marcescens, Shigella, H. influenzae, Legionella, Pseudomonas aeruginosa
Gonorrhea Gram (-) cocci – alternate choice
Definition
Urinary
GI
Term
Fluoroquinolones have Good penetration into ____
Definition
prostate
Term
What antibiotic is used for Resistant Respiratory Tract Infections -> Infections unresponsive to b-lactams?
Definition
Fluoroquinolones
Term
Fluoroquinolones are Not 1st choice for pneumonia because only ___ active vs. Strep. pneumoniae
Definition
weakly
Term
Fluoroquinolones Adverse Effects:
_____ tolerated
Nausea, vomiting, diarrhea
Occasionally, headache, dizziness, rash, abnormal LFTs
May cause erosion of ____ leading to tendinitis and tendon rupture for older patients (>60 years old)
Use not recommended if <___ yr old
Contraindicated in ______ and nursing mothers
Definition
Extremely well
cartilage
18
pregnant
Term
Metronidazole Forms cytotoxic compounds that damage ____ & ___
Definition
proteins and DNA
Term
Metronidazole is what type of drug?
Definition
antibiotic that damages DNA
Term
Metronidazole is An anti-____ drug that also has potent antibacterial activity against ____, including Bacteroides & Clostridium
Definition
protozoal
anaerobes
Term
Metronidazole is Well absorbed ___, well distributed including ___
Definition
orally
CSF
Term
Metronidazole Adverse effect:
____-like effect (if ingested with alcohol) , blocks conversion of ethanol, acetaldehyde accumulates, flushing, nausea&ventilation
GI upsets, ____ taste
Definition
disulfiram
metallic
Term
Which antibiotic doesn't have resistance issues except w/ H. Pylori?
Definition
Metronidazole
Term
What is the DOC for Amebiasis (E. histolytica)?
Definition
Metronidazole b/c is Antiprotozoal
Term
What is the DOC for Giardia?
Definition
Metronidazole b/c is Antiprotozoal
Term
What is the DOC for Trichomoniasis?
Definition
Metronidazole b/c is Antiprotozoal
Term
Metronidazole Bacterial Uses:

____ or mixed intra-abdominal infections
____ (trichomonas, bacterial vaginosis)
Antibiotic-associated _________________
____ abscess
In combinations for ___________________
Definition
Anaerobic
Vaginitis
enterocolitis
Brain
Helicobacter pylori
Term
Rifampin is what type of drug?
Definition
antibiotic that Inhibits mRNA synthesis
Term
Rifampin Inhibits DNA-dependent __________
Specific for _________
Resistance developed due to mutations in the ____ gene.
Definition
RNA polymerase
prokaryotes
RNA polymerase
Term
Rifampin is Bacteri____ for intra- & extracellular mycobacteria including M. tuberculosis, M. leprae, and atypical mycobacteria.
Definition
cidal
Term
Rifampin is the 1st line drug for _____
In combination with isoniazid, pyrazinamide, others
Definition
tuberculosis
Term
Triple therapy for leprosy?
Definition
Rifampin, dapsone, clofazimine
Term
What antibiotic Discolors urine, tears, contact lenses?
Definition
Rifampin
Term
Mupirocin is what type of drug?
Definition
antibiotic -> Natural product produced by Pseudomonas fluorescenes
Term
Mupirocin is Active against gram (__) cocci including ___
Definition
+
MRSA
Term
Mupirocin is available in an _______ for local application
Definition
Ointment
Term
Mupirocin Inhbits Staph. Isoleucyl ____ synthetase
Definition
tRNA
Term
Nitrofurantoin is what type of drug?
Definition
antibiotic
Term
Nitrofurantoin:
___ enzyme inhibitors
Used P.O. to treat GI infection (no ___ absorption)
Acts on ____ and ___ enteritis
Definition
Multiple
systemic
bacterial
protozoal
Term
Antibiotics that are Protein Synthesis Inhibitors: (5)
Definition
Tetracyclines
Aminoglycosides
Macrolides
Chloramphenicol
Clindamycin
Term
Doxycycline is what type of drug?
Definition
Tetracycline antibiotic
Term
Demeclocycline is what type of drug?
Definition
Tetracycline antibiotic
Term
Minocycline is what type of drug?
Definition
Tetracycline antibiotic
Term
Gentamicin is what type of drug?
Definition
Aminoglycoside antibiotic
Term
tobramycin is what type of drug?
Definition
Aminoglycoside antibiotic
Term
amikacin is what type of drug?
Definition
Aminoglycoside antibiotic
Term
Neomycin is what type of drug?
Definition
Aminoglycoside antibiotic
Term
Streptomycin is what type of drug?
Definition
Aminoglycoside antibiotic
Term
Netilmicin is what type of drug?
Definition
Aminoglycoside antibiotic
Term
Erythromycin is what type of drug?
Definition
macrolide antibiotic
Term
Clarithromycin is what type of drug?
Definition
macrolide antibiotic
Term
Azithromycin is what type of drug?
Definition
macrolide antibiotic
Term
Chloramphenicol is what type of drug?
Definition
Antibiotic -> Protein Synthesis Inhibitors
Term
Clindamycin is what type of drug?
Definition
Antibiotic -> Protein Synthesis Inhibitors
Term
Bacterial ribosomes differ from eukaryotic
Bacterial = __S with __S/__S subunits
Mammalian = __S with __S/__S subunits
Thus, antibiotics that bind and inhibit bacterial ribosome function have relatively selective toxicity for bacteria

____ ribosomes are more similar in bacteria and mammals
Toxicity of some of these drugs is at ___ ribosome
Definition
70
50S/30S
80
60S/40S

Mitochondrial
mitochondrial
Term
Tetracyclines (bacterio_____)
Binds to __S, block access of ____
Definition
static
30
acyl-tRNA
Term
Aminoglycosides (bacteri____; very toxic)
Binds to __S , interferes with ____ of functional ribosome &/or ___
Definition
cidal
30
assembly
misreading
Term
Macrolides (bacterio_____)
Bind irreversibly to __S, inhibits ____
Definition
static
50
translocation
Term
Chloramphenicol (bacterio_____)
Binds __S, inhibits ____ transferase reaction
Definition
static
50
peptidyl
Term
Clindamycin (bacterio______)
Bind irreversibly to ___S, inhibits ____
Definition
static
50
translocation
Term

Tetracyclines Pharmacokinetics:

Adequate but incomplete ___ absorption

Absorption decreased by ....(4)

     - Think antacids for PUD (Peptic ulcer disease), with

       tetracycline for _____ 

     - Concentrate in liver, kidney, spleen, skin & tissue

       undergoing _____ (teeth, bone) or tumors with

       high ____ (gastric carcinoma)

Do not give to ____

     - Chelation with calcium discolors developing teeth  

     - Can reduce growth of developing bone

Definition
oral
food, milk, cations, iron
H.pylori
calcification
calcium
children
Term
Tetracyclines Clearance:
_____ uniquely cleared as chelate in feces
Others in ____ metabolism or ___
Definition
Doxycycline
liver
kidney
Term
Tetracyclines Spectrum: very ____
Definition
broad
Term
Tetracyclines Especially useful for ... (3)
Definition
Chlamydia, Rickettsia, Mycoplasma
Term
Tetracyclines Resistance: Sensitive bacteria have intake system to concentrate drug inside bacteria
Resistant bacteria have both intake and ___ systems and could not accumulate drug inside bacteria
Definition
efflux
Term
Tetracyclines Side Effects:
Do not give to _____ –> teeth, bone
_____sensitivity
Superinfections with ____ -> (causes diarrhea and other intestinal disease when competing bacteria in the gut flora are wiped out by antibiotics.) -> (can be treated with oral ____ or ____)
Liver and kidney toxicity possible
Definition
children
Photo
C. difficile
vancomycin
metronidazole
Term

Tetracyclines Clinical Uses:

_____ infections

     - Lymphogranuloma venereum – STD

     - Psittacosis – pneumonia

_____

     - Rocky Mountain Spotted fever from ticks

_____ - spirochete

     - Lyme disease

_____ 

     - Also erythromycin (is a macrolide)

_____ G(-) bacilli

     - Vibrio cholerae – enterotoxin, diarrhea Doxycycline 

_____ in combinations

Actinomyces, Amoebae

Definition
Chlamydial
Rickettsia
Borrelia
Mycoplasma pneumonia (DOC)
Cholera
H. pylori
Term
Aminoglycosides are For aerobic gram ___ bacteria only
Definition
negative
Term
Aminoglycosides enter through ____ then through active transport by ____ -dependent process. Low ____ & ___ inhibit transport. Transport enhanced by ___ damage to wall = synergistic effect
Definition
porins
oxygen
pH & anaerobic
b-lactams
Term
Aminoglycosides are Effective against serious infection due to ___ gram(__) bacteria
Definition
aerobic
-
Term
Aminoglycosides Mechanism:
bacteri____, irreversible binding
Binds to ___S ribosomal subunit
blocks formation of _____ complex
____ of mRNA
Block ____ of mRNA chain
Definition
cidal
30
initiation
Misreading
translocation
Term
Aminoglycosides Resistance:
Bugs produce ___ that inactive drug
Impaired entry – mutant porin, or pH, O2
Mutant __S ribosomal protein
Definition
enzymes
30
Term
Aminoglycosides Pharmacokinetics:
Large, polar molecules
Poor ___ absorption
Must be given parenterally IM, IV, intrathecal if CSF
Distribution limited to _______
Do not reach ___
Eliminated by ____ filtration
Doses matched to creatinine clearance to avoid severe toxicity, blood levels monitored
Definition
oral
extracellular fluid
CSF
glomerular
Term

Aminoglycosides Adverse Effects

Very ____

___toxicity

     - Loss of equilibrium

     - Loss of hearing

____toxicity

____toxicity

____ blockade

     - reduces respiratory function, esp. after surgery

Definition
toxic
Oto
Nephro
Neuro
Neuromuscular
Term
Aminoglycosides are used for Gram (__) ___ bacteria, esp. when isolate is drug-resistant or sepsis
Definition
-
enteric
Term
Aminoglycosides Used in combo with ____, synergistic, extends spectrum to gram (__)
Definition
b-lactams
+
Term
Aminoglycosides used against Pseudomonas aeruginosa In combo with antipseudomonal _____
Definition
penicillins
Term
Aminoglycosides used for Enterococcal _____, Viridans streptococcal, & staph ____
Definition
endocarditis
endocarditis
Term
Aminoglycosides used for _____ UTI, Not for ___, uncomplicated UTI
Definition
Chronic
acute
Term
Aminoglycosides are used for E. coli or Klebsiella pneumonia along With ____ & ____
Definition
ampicillin & cephalosporin
Term
What is the 2nd line drug for TB?
Definition
Streptomycin (Aminoglycosides)
Term
Gentamicin is Active against Staph, coliforms, pseudomonas, proteus, Enterobacter, Klebsiella, Serratia, & other gram (__) ___ It is Mainly employed for severe infections, often ___ patient with bugs resistant to other antibiotics
Definition
-
rods
immunocompromised
Term
Macrolides Mechanism:
Inhibits ____ synthesis
Binds irreversibly to __S, inhibits translocation of the peptidyl molecule from ”__” site to “__” site
Bacterio_____
Bacterio_____ at high concentrations
Definition
protein
50
A
P
static
Cidal
Term
Macrolides Pharmacokinetics:
____ base is destroyed by stomach acid, so either enteric-coated or esterified forms given
____ & ____ stable to acid
All have adequate oral absorption
Distribute well to all tissues except __
Good levels in ___ and accumulates in ____
Definition
Erythromycin
Clarithromycin & azithromycin
CSF
prostate
macrophages
Term

Macrolides Spectrum

Erythromycin spectrum same as Penicillin G so used often when Pt ____ to penicillin

Especially useful for (3)

Gram (__) organisms

     - Pneumococci, streptococci, staphylococci,  

       corynebacteria

Aerobic Gram (__) & Others

     - Mycoplasma, Legionella, Helicobacter, Chlamydia,

       Listeria, Neisseria, Bordetella pertussis,

       Treponema, some Rickettsia

Definition
allergic
Chlamydia, Mycoplasma, Legionella
+
-
Term

Macrolides: Clinical Use: Erythromycin (or other macrolide) = Drug of Choice (DOC) for:

 

______ pneumonia

     - Spectrum includes pneumococcus, mycoplasma,

       legionella

     - Mycoplasma pneumonia “atypical pneumonia”

     - Legionnaires’ Disease

______ infections during pregnancy

     - Alternative to tetracycline for uncomplicated

       urethral, endocervical, rectal or epididymal 

       Chlamydia infections

     - Tetracyclines also effective

______

     - Alternative if allergic to Penicillin G

______ 

     - Erythromycin or Pen to eliminate carrier state

______

     - UTI

Definition
Community-acquired
Chlamydial
Syphilis
Corynebacterium diphtheriae
Ureaplasma
Term
Clarithromycin is the DOC for ____ in combo with amoxicillin + PPI
Also active vs ______
Less GI upset than erythromycin
___ dosing vs. qid for erythromycin
Definition
H. pylori
Haemophilus influenzae
BID
Term
Azithromycin
___ dosing an advantage over other macrolides
Slightly better tissue penetration
Preferred for ___, also ___
Definition
Once-per-day
Chlamydia trachomatis
Haemophilus influenzae
Term
Macrolides Adverse Effects:
____ distress common
Cholestatic _________
___toxicity – at high doses
Definition
Epigastric
jaundice
Oto
Term
Macrolides Contraindication: patients with ___ dysfunction since drug ___ in liver
Definition
hepatic
accumulates
Term
Drug-drug interactions of macrolides: _____ & _____inhibit hepatic metabolism (by inhibiting cytochrome P450 enzymes) of theophylline, warfarin, and other drugs
Definition
Erythromycin & clarithromycin
Term
_____-____ is a combination of two streptogramins (30:70) for IV injection
Definition
Quinupristin-dalfopristin
Term
Streptogramins are Active against gram (__) ___including multidrug resistant Strep, pen resistant Strep. Pneuniae, methicillin- susceptible, and-resistant Staph, and vancomycin-resistant strain.
Definition
+
cocci
Term
Streptogramins Resistance is due to modification of (_____) drug-binding site
Definition
streptogramin
Term
Chloramphenicol is what type of drug?
Definition
antibiotic (protein synthesis inhibitor)
Term
Chloramphenicol is ___ spectrum against G(+) & G(-) organisms
Even ___
but is ___ so use is restricted to life-threatening infections in which there are no alternatives
Definition
broad
anaerobes
toxic
Term
Chloramphenicol Mechanism: Binds __S, inhibits ___ transferase reaction
Definition
50
peptidyl
Term
Chloramphenicol Resistance: Via increased metabolizing enzyme _______
Definition
acetyltransferase
Term
Chloramphenicol
IV or oral, enters CSF
Serious _____ [Rarely used]
Hemolytic anemia (G6PD deficiency)
aplastic anemia (fatal)
“___ baby syndrome” (cyanosis)
overgrowth of Candida
Definition
toxicity
Gray
Term
Chloramphenicol Use: Life-threatening ___ or ___ infections
Definition
Salmonella typhi
H. influenzae
Term
Clindamycin Mechanism:
Bactericidal inhibition of ___ synthesis
Bind irreversibly to __S, inhibits translocation
Definition
protein
50
Term
Clindamycin is used P.O. for treatment of ____ infections ex. Bacteroides fragilis
Definition
anaerobic
Term
Clostridium difficile is always resistant to ______ so for Incidences of pseudomembranous colitis (caused by C. difficile), treat with ____ or ____
Definition
Clindamycin
metronidazole or vancomycin
Term
_____ still the leading cause of death by infectious disease throughout the world
Definition
Tuberculosis
Term
Mycobacterium tuberculosis is Difficult to ___ & “____-___”
Definition
stain
acid-fast
Term
Tuberculosis Grows ____, treat for _ years
Many resistant strains so use multiple drug therapy
Definition
slowly
2
Term
Mycobacterium tuberculosis
Treatment divided into:

1. Treatment of ___ infection diagnosed by a positive PPD or
2. Treatment of ___ clinical TB
Definition
latent
active
Term
Tuberculosis
First Line Drugs
1.
2.
3.
4.
5.

Second Line Drugs
Ethionamide, Aminosalicylic Acid, Capreomycin, Cycloserine
Definition
1. Isoniazid
2. Rifampin (or Rifabutin)
3. Ethambutol
4. Pyrazinamide
5. Streptomycin
Term
Tuberculosis FYI
Empirical initial therapy until susceptibility reports are available (4 drugs regimen)
1. Isoniazid (INH)
2. Rifampin (or Rifabutin)
3. Ethambutol
4. Pyrazinamide

Continuation phase: INH +rifampin for 4 months
Definition
Term
Isoniazid (INH) in treatment of Tuberculosis:
Inhibits mycolic acid formation in outer membrane, this is unique to _____
INH acetylated in liver, “fast” acetylators have lower levels, “slow” acetylators may reach ____ levels
Side effects: peripheral neuritis, hepatitis, drug interactions
Definition
Mycobacteria
toxic
Term
Rifampin in treatment of Tuberculosis:
Inhibits DNA-dep. ___ polymerase
Definition
RNA
Term
Pyrazinamide in treatment of ____: Drug targets and mechanism of action are unknown.
Definition
tuberculosis
Term
Ethambutol in treatment of tuberculosis:
Inhibits ___ acid synthesis, can impair ___ vision
Definition
mycolic
color
Term
Streptomycin in treatment of tuberculosis:
Parenteral, bacterio____ _____ synthesis inhibitor
Definition
cidal
protein
Term
Mavium complex bacteremia in AIDS patients can be treated with a single daily dose of ____ (300 mg)


_____, 500 mg once daily or ____, 500 mg twice daily ca also be used
Definition
rifabutin
Azithromycin
clarithromycin
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