Term
What drugs are in this Drug Class: Folic acid synthesis inhibition? |
|
Definition
Sulfonamides & Trimethoprim |
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|
Term
What drugs are in this Drug Class: Inhibit DNA gyrase, DNA synthesis? |
|
Definition
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|
Term
What drugs are in this Drug Class: DNA damage? |
|
Definition
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|
Term
What drugs are in this Drug Class: Inhibit mRNA synthesis? |
|
Definition
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Term
Sulfisoxazole is what type of drug? |
|
Definition
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|
Term
Sulfamethoxazole is what type of drug? |
|
Definition
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|
Term
Sulfonamides are Analogs of _____ |
|
Definition
PABA (para-amino benzoic acid) |
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|
Term
Sulfonamides Compete with ____ in synthesis of folic acid a required precursor of ___ & ____ DNA bases |
|
Definition
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|
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 |
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|
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 |
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Term
Sulfonamides & Trimethoprim has ____ Toxicity |
|
Definition
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|
Term
Bacteria have no ____ transport for folate and must synthesize it. ____ inhibit this synthesis. |
|
Definition
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|
Term
Trimethoprim is 20,000 x more potent at inhibiting ______ dihydrofolate reductase than ____ enzyme. |
|
Definition
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|
Term
Humans cannot synthesize folate – must obtain from diet via Active uptake. Human dietary folate deficiency causes ____. |
|
Definition
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|
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
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|
Term
Sulfonamides & Trimethoprim: Bacterio____ Very ____ spectrum Distribute to ___ body fluids including ___ |
|
Definition
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|
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
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|
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
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|
Term
_______ is the antibiotic used for Acute gonococcal urethritis & oropharyngeal gonococcal inf. |
|
Definition
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|
Term
________ is the antibiotic (drug of choice) for Pneumocystis carinii pneumonia ->Most common opportunistic fungus infections of AIDS |
|
Definition
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|
Term
____ is the antibiotic used for GI infections & prophylaxis for travelers’ diarrhea -> E. coli, Proteus mirabilis, Salmonella typhi, Shigella |
|
Definition
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|
Term
_____ is the antibiotic used for Recurrent otitis media |
|
Definition
|
|
Term
____ is the antibiotic used for Nocardiosis |
|
Definition
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|
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
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|
Term
Norfloxacin is what type of drug? |
|
Definition
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|
Term
Ofloxacin is what type of drug? |
|
Definition
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|
Term
Levofloxacin is what type of drug? |
|
Definition
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|
Term
Enoxacin is what type of drug? |
|
Definition
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|
Term
Sparfloxacin is what type of drug? |
|
Definition
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|
Term
Lomefloxacin is what type of drug? |
|
Definition
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|
Term
Moxifloxacin is what type of drug? |
|
Definition
|
|
Term
Trovafloxacin is what type of drug? |
|
Definition
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|
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
|
|
Term
Fluoroquinolone names all end in _____ |
|
Definition
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|
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
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|
Term
Fluoroquinolones Pharmacokinetics: Widely distributed in ___ Renal secretion of ____ drug in urine |
|
Definition
|
|
Term
What antibiotic is used for Anthrax -> Bacillus anthracis? |
|
Definition
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|
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
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|
Term
Fluoroquinolones have Good penetration into ____ |
|
Definition
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|
Term
What antibiotic is used for Resistant Respiratory Tract Infections -> Infections unresponsive to b-lactams? |
|
Definition
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|
Term
Fluoroquinolones are Not 1st choice for pneumonia because only ___ active vs. Strep. pneumoniae |
|
Definition
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|
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
|
|
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
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|
Term
Metronidazole is Well absorbed ___, well distributed including ___ |
|
Definition
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|
Term
Metronidazole Adverse effect: ____-like effect (if ingested with alcohol) , blocks conversion of ethanol, acetaldehyde accumulates, flushing, nausea&ventilation GI upsets, ____ taste |
|
Definition
|
|
Term
Which antibiotic doesn't have resistance issues except w/ H. Pylori? |
|
Definition
|
|
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
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|
Term
Rifampin is the 1st line drug for _____ In combination with isoniazid, pyrazinamide, others |
|
Definition
|
|
Term
Triple therapy for leprosy? |
|
Definition
Rifampin, dapsone, clofazimine |
|
|
Term
What antibiotic Discolors urine, tears, contact lenses? |
|
Definition
|
|
Term
Mupirocin is what type of drug? |
|
Definition
antibiotic -> Natural product produced by Pseudomonas fluorescenes |
|
|
Term
Mupirocin is Active against gram (__) cocci including ___ |
|
Definition
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|
Term
Mupirocin is available in an _______ for local application |
|
Definition
|
|
Term
Mupirocin Inhbits Staph. Isoleucyl ____ synthetase |
|
Definition
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|
Term
Nitrofurantoin is what type of drug? |
|
Definition
|
|
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
|
|
Term
Demeclocycline is what type of drug? |
|
Definition
|
|
Term
Minocycline is what type of drug? |
|
Definition
|
|
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
|
|
Term
Clarithromycin is what type of drug? |
|
Definition
|
|
Term
Azithromycin is what type of drug? |
|
Definition
|
|
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
|
|
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
|
|
Term
Chloramphenicol (bacterio_____) Binds __S, inhibits ____ transferase reaction |
|
Definition
|
|
Term
Clindamycin (bacterio______) Bind irreversibly to ___S, inhibits ____ |
|
Definition
|
|
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
|
|
Term
Tetracyclines Spectrum: very ____ |
|
Definition
|
|
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
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|
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
|
|
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
|
|
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
|
|
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
|
|
Term
Aminoglycosides Used in combo with ____, synergistic, extends spectrum to gram (__) |
|
Definition
|
|
Term
Aminoglycosides used against Pseudomonas aeruginosa In combo with antipseudomonal _____ |
|
Definition
|
|
Term
Aminoglycosides used for Enterococcal _____, Viridans streptococcal, & staph ____ |
|
Definition
|
|
Term
Aminoglycosides used for _____ UTI, Not for ___, uncomplicated UTI |
|
Definition
|
|
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
|
|
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
|
|
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
|
|
Term
Macrolides Contraindication: patients with ___ dysfunction since drug ___ in liver |
|
Definition
|
|
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
|
|
Term
Streptogramins Resistance is due to modification of (_____) drug-binding site |
|
Definition
|
|
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
|
|
Term
Chloramphenicol Mechanism: Binds __S, inhibits ___ transferase reaction |
|
Definition
|
|
Term
Chloramphenicol Resistance: Via increased metabolizing enzyme _______ |
|
Definition
|
|
Term
Chloramphenicol IV or oral, enters CSF Serious _____ [Rarely used] Hemolytic anemia (G6PD deficiency) aplastic anemia (fatal) “___ baby syndrome” (cyanosis) overgrowth of Candida |
|
Definition
|
|
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
|
|
Term
Clindamycin is used P.O. for treatment of ____ infections ex. Bacteroides fragilis |
|
Definition
|
|
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
|
|
Term
Mycobacterium tuberculosis is Difficult to ___ & “____-___” |
|
Definition
|
|
Term
Tuberculosis Grows ____, treat for _ years Many resistant strains so use multiple drug therapy |
|
Definition
|
|
Term
Mycobacterium tuberculosis Treatment divided into:
1. Treatment of ___ infection diagnosed by a positive PPD or 2. Treatment of ___ clinical TB |
|
Definition
|
|
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
|
|
Term
Rifampin in treatment of Tuberculosis: Inhibits DNA-dep. ___ polymerase |
|
Definition
|
|
Term
Pyrazinamide in treatment of ____: Drug targets and mechanism of action are unknown. |
|
Definition
|
|
Term
Ethambutol in treatment of tuberculosis: Inhibits ___ acid synthesis, can impair ___ vision |
|
Definition
|
|
Term
Streptomycin in treatment of tuberculosis: Parenteral, bacterio____ _____ synthesis inhibitor |
|
Definition
|
|
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 |
|
|