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Pharm Antibiotics
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66
Medical
Professional
03/04/2013

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Term
Natural penicillins
Definition
Highest bacteria against gram positive bacteria
Some gram negative and anaerobic coverage
Inactivated by B-lactamase
NO antipseudomonal activity
V type more acid resistant
Eliminated by the kidney
Term
Penicillinase-resistant Penicillins (Nafcillin IV, Oxacillin, Dicloxacillin, Methicillin)
Definition
Lower activity against gram-positive bacteria
Some gram negative and anaerobic coverage
Acid stable
DOC against penicillinase-producing Staph aureus
Hepatic metabolism and renal excretion
Term
Extended-spectrum penicillins (Ampicillin, Amoxicillin)
Definition
Extended gram negative coverage (NOT Kleb because it produces B-lactamase)
Lower gram positive coverage
Anaerobic coverage
NO antipseudomonal activity
Acid resistant
Urinary excretion
Term
Antipseudomonal penicillins (Piparcillin, Ticarcillin)
Definition
Covere bacteria in extended spectrum penicillins and additional enteric gram negative bacilli (NOT Kleb)
Treats Pseudomonas
Susceptible to B-lactamase
Acid sensitive
Renal excretion
Resistance develops in combo with aminoglycosides
P more effective than T
Term
B-lactamase inhibitors (Clavulanic Acid, Sulbactam, Tazobactam) (Amoxicillin and Clavulanic acid is Augmentin)
Definition
Used in combination with penicillins to inhibit some penicillinases
Bacteria can develop some resistance
Not active against MRSA
Term
Penicillin G
Definition
Effective against gram + microbes, spirochetes, gram - cocci
NOT effective against amoebae, plasmodia, rickettsiae, fungi, viruses
Used to treat syphilis
Mixed with procaine and benzathine for longer-acting effects
Most rapidly secreted drug by the kidney
Probenecid can block tubular secretion to decrease secretion
It is an acid, so alkalinizing the urine decreases excretion
Baby is more acidic than mother, so less in baby than mother
Ampicillin rash in kids NOT hypersensitivity
Causes diarrhea, peaked T waves in EKG, enteritis
Term
Aztreonam
Definition
ICWS efffective only against gram - rods, including Pseudomonas
NO activity against gram + and anaerobes
MOstly used in ICU
NO cross sensitivity with penicillin derivatives (used with penicillin allergy)
Term
Carbapenems: Imipenem, Cilastatin, Ertapenem
Definition
ICWS given IV and have broad spectrum against gram positive, gram negative rods and anaerobes
I must be given with C to avoid inactivation by renal tubule dehydropeptidases
Pseudomonas resistant, give with an aminoglycoside
I can cause seizures
Mostly used in the ICU
Term
Ertapenem
Definition
ICWS that is used IV in ICUs
Term
First Gen Cephalosporins: Cefazolin, Cephalexin, Cefadroxil Monohydrate
Definition
More resistant to penicillinases than penicillins
Good activity against gram + (except enterococci, S. aureus, S. epi) and moderate activity against gram -
DOC E. coli, Kleb, Proteus
Effective against Kleb, Proteus
Term
Second Gen Cephalosporins: Cefoxitin, Cefaclor, Cefuroxime, Cefmetazole, Cefotetan, Cefprozil, Loracarbef
Definition
Increased activity against gram -
ICWS with better against B lactamases
KNOW each of the first-fourth C with specific ideas about unique drugs in each class
DOC for Moraxella, E. coli, Kleb, proteus
Term
Third Gen Cephalosporins: Ceftizoxime, Cefoperazone, Ceftazidime, Ceftriaxone, Cefixime, Cefditoren, Ceftarolime fosamil
Definition
TCWS that are more active against Enterobacteriaceae including penicillinase strains
Some are active against Pseudomonas
Most have good CNS penetration
DOC Salmonella, Moraxella
Term
Fourth Gen Cephalosporins: Cefepime
Definition
ICWS that are more resistant to some B lactamases
This class NOT effective against MRSA, Listeria, Enterococci, Atypicals
Excreted by the kidney
Probenecid slows the excretion rate
Can cause superinfections, pseudomembranous colitis, dose-dependent renal tubular necrosis (with aminoglycosides)
Term
Cefoperazone
Definition
Third gen cephalosporin that has NO CNS penetration
Metablized by the liver
Disulfiram-like reaction
Term
Ceftazidime
Definition
Third gen cephalosporin that is good against Pseudomonas
Term
Cefotaxime Sodium
Definition
Third gen cephalosporin with good CNS penetration
Used for meningitis
Term
Ceftriaxone
Definition
Third gen cephalosporin with good CNS penetration
Used for meningitis
DOC Strep pneumo, Neisseria gonorrhoeae
Term
Cefazolin
Definition
Surgery prophylaxis because it will be effective against skin infections
Term
Cefipime
Definition
ICWS IV fourth gen cephalosporin
Better against Pseudomonas, more stable against B lactamases
NOT effective against Enterococcus or Bacteroides
Renally excreted
Penetrates CSF
Term
Vancomycin
Definition
Inhibits cell wall synthesis by binding to D-ala D-ala terminus of peptidoglycan peptide, preventing cross-linking
Inhibits transglycosylation which inhibits elongation
D-ala D-lac mutation causes resistance
Synergistic with aminoglycosides
Gram + coverage so used against MRSA and gram + pts in penicillin resistance
Second DOC in pseudomembranous colitis
Ototoxic, nephrotoxic
Red man syndrome, flushing from histamine release (d-Tubocurarine, Morphine--perioral itching)
Term
Daptomycin
Definition
Lipopeptide antibiotics that bind to bacterial membranes
Damage cell membrane
Bactericidal against gram +
Given IV
Term
Fosfomycin
Definition
Inhibits cell wall synthesis at one of the first steps of peptidoglycan synthesis
Active against gram + and gram -
Oral, excreted by kidney
Used for uncomplicated UTI in women
Synergistic with beta-lactam
Term
Bacitracin
Definition
Interferes with dephosphorylation step in phospholipid carrier cycle, impedes transfer of growing cell wall
Active against gram +
Nephrotoxic, rarely used
Triple combo with neomycin and polymyxin for skin issues
Term
Cycloserine
Definition
Competes with D-ala for incorporation into bacterial cell walls
Big CNS toxicity, not used (only know this)
Term
Sulfonamides
Definition
Requires a free para-amino group for action
Compete for PABA for incorporation into folic acid
Bacteriostatic
Effective against gram + and gram - organisms
Use against Pneumocystis, chlamydia, Nocardia, Actinomyces
Used for UTIs, toxoplasmosis, trachoma
Metablized in the liver and excreted in the kidney
Nephrotoxic
Every organ system may be adversely affected
Can cause kernicterus because they cross the placental barrier becasue bilirubin is bound to plasma proteins
Hypersensitivity
Blood dyscrasia
Hemolytic anemia (anilines redox rxn with Fe to create Fe3+ methemoglobin), Stevens-Johnson syndrome
Term
Sulfasalazine
Definition
Prodrug sulfonamide used for UC; combination of sulfapyridine and mesalamine
Term
Trimethoprim
Definition
Inhibitor of DHF reductase, decreased folic acid synthesis, which is crucial to purines
Also Pyrimethamine (bacterial) and Methotrexate (human)
NOT used topically
Term
Co-trimoxazole or TMP-SMX (Bactrim)
Definition
Effective against Pneumocystis, shigellosis, salmonella, UTI, prostatitis, nontuberculous TB
DOC for uncomplicated UTIs and moraxella
Treat otitis media, second line for LIsteria
Term
Silver sulfadiazine
Definition
Topical sulfa drug used to treat wound infections of burns
Term
Pyrimethamine, Sulfadoxine
Definition
Inhibits protozoal DHFR
Used together as presumptive treatment of malaria
Not receommended for malaria prophylaxis due to fatal toxic epidermal necrosis
Term
Erythromycin
Definition
Macrolide antibiotic; safest antibiotics available
Inhibit protein synthesis; binds to 50S to interfere with formation of initiation complex
Used to treat gram positives, including Mycoplasma
Treats diphtheria
DOC for Legionella
Resistance developed that pumps drug out of cell, methylase that decreases drug binding to ribosome, esterases that degrade drug, chromosomal alterations that change 50S
Destroyed by gastric acid; excreted fecally; does not penetrate CNS
Causes diarrhea
Used in penicillin allergy
Term
Clarithromycin
Definition
Macrolide that penetrates lung macrophages better, so used for MAC
Used to treat CAP in children, H. pylori duodenal ulcer
Term
Azithromycin
Definition
Macrolide that can be dosed once a day and produces less GI effects
Food decreases bioavailability
Treats strep pharyngitis, chlamydia and gonorrhea, peds otitis media, MAC prophylaxis in HIV
Term
Telithromycin (Ketolide)
Definition
Binds to 50S subunit 23S rRNA
Used to treat respiratory bugs, as well as intracellular bugs
Causes diarrhea, severe hepatoxicity
Term
Clindamycin
Definition
Binds to 50S subunit of bacteria
Used to treat gram positive and anaerobic gram negative
Either bacteriostatic or bacteriocidal
Low CSF concentrations, but can be used for Toxoplasma encephalitis
Reaches high concentrations in bones
Causes pseudomembranous colitis
Term
Dalfopristin; Quinupristin (streptogramins)
Definition
Inhibit bacterial ribosome function
Given IV
For vanco-resistant Enterococcus and S. aureus
Inhibit CYP450
Term
Oxazoladinones: Linezolid
Definition
Inhibits ribosome translation
Used against aerobic gram positives
Reversible, non-selective inhibitor of MAO
100% oral bioavailability
Used for gram positives, bacterial pneumonia, vanco-resistant entercoccoi, MRSA
Term
Aminoglycosides (Streptomycin, neomycin, gentamicin, kanamycin)
Definition
NONE penetrate CNS; not absorbed orally; excreted by kidney; due to polarity
Inhibit 30S
Used to treat gram negative enterics where there is suspicion of sepsis
Under aerobic conditions, they are bactericidal (exception to the rule that anything inhibits synthesis is -static)
Have post-antibiotic effect
Nephrotoxic; ototoxic
Term
Streptomycin
Definition
Inhibits 30S
Used to treat tularemia, plague, TB, endocarditis
Term
Spectinomycin
Definition
Aminoglycoside used to treat gonorrhea
Term
Chloramphenicol
Definition
Broad spectrum antibiotic
Associated with fatal aplastic anemia
Binds 50S subunit
Bacteriostatic
Side effects have to do with interactions with host mitochondria in bone cells (70S in humans)
Distributes to eyes and CNS
Metabolized in the liver with conjugation with glucuronic acid
Causes bone marrow depression, aplastic anemia in genetically susceptible people
Gray baby syndrome in infants, cyanosis, vasomotor, respiratory distress and death
Can cause bacterial and fungal superinfection during prolonged therapy
Used to treat typhoid fever, meningitis, eye infections, infections from gram negative organsism
INhibits tolbutamide and chlorpropramide
Term
Tetracyclines (Doxycyline, minocycline,
Definition
Broad spectrum antibiotic
Inhibition of 30S
Effective against gram positive and gram negative; can be used in amoebiasis, Plasmodium infection, bacillary dysentery due to Shigella
DOes NOT distribute to CNS or joints
Excreted through urine
Can cause GI side effects, overgrowth of resistant flora
Bind to calcium in growing bones; should NOT be given to pregnant women or children under 8
Liver damage
Kidney damage (Fanconi Syndrome; renal tubular acidosis)
Photosensitization
DOC cholera, Mycoplasma, Chlamydia, Rickettsia, Lyme, Vibrio
Term
Glycyclines Tigecycline
Definition
Derivative of minocycline
IV
Used for skin infections, intra-abdominal infections
Bacteriostatic
ACtivity against MRSA, MRSE, PRSP, VRE
Otherwise, same activity as tetracyclines
Term
Nitrofurantoin
Definition
UTI drug
Wide spectrum
Proteus and Pseudomonas are resistant
Interferes with bacterial enzymes
Colors urine brown
N/V diarrhea common
Causes interstitial pulmonary fibrosis
Polyneuropathies
CI pregnancy, impaired renal function, allergy
Term
Methenamine
Definition
UTI drug
Decomposes to formaldehyde; binds to amino groups, inactivates proteins of the bacteria
Bactericidal
Used against gram negative for chronic suppresive treatment of E. coli
Bacterial resistance does not develop
Non-toxic
Term
Fluoroquinolones (Ciprofloxacin, Ofloxacin, Levofloxacin or Levoquin)
Definition
Broad spectrum antibiotic used for UTIs, lower respiratory tract infections and infections of skin
Highly active against gram positive and negative including Pseudomonas
INhibits DNA gyrase
Bactericidal
NOT effective against anaerobic bacteria
Active against TB, M. kansasii
Poor CNS penetration
Used for UTI, GC, Traveler's diarrhea, bone and joint infections, anthrax prophylaxis
Causes QT prolongation, tendon rupture, transient elevations of transaminase, LDH, alkaline phos
Term
Moxifloxacin
Definition
Broad spectrum fluoroquinolone
Oral, once-a-day
Imrpoved activity against pneumococci
Used for acute and chronic bronchitis, acute sinusitis, pneumonia
Good penetration in resp tissue
Metabolized by glucuronide and sulfate conjugation
Term
Gatifloxacin
Definition
Topical fluoroquinolone
Term
Metronidazole (Flagyl)
Definition
Selective for anaerobes
Disrupts DNA helical structure
Bactericidal
Used for septicemia, endocarditis, pseudomembranous colitis
Has disulfiram-like effect, candida overgrowth
FOR THESE MISCELLANEOUS, KNOW NAME, MECHANISM AND ADVERSE EFFECTS
Term
Fidaxomicin
Definition
Narrow-spectrum, active against gram positive aerobes and anaerobes
Inhibits protein synthesis by binding to RNA polymerase
Used to treat pseudomembranous colitis
Term
Mupirocin (Bactroban)
Definition
Bacteriostatic at low concentrations
Bacteriocidal at high concentrations
Protein and RNA synthesis inhibitied
Given topically for impetigo
LIttle potential for cross-resistance with other antibiotics
Term
Polymyxin B
Definition
Polypeptide
Used for gram negative infections
Effective against gram negative bacilli
Bind to gram negative cell membrane phospholipids, results in loss of metabolites essential to bacterial existence
Bactericidal
Used to treat UTI, septicemia, bacteremia when other antibiotics are ineffective or CI
Nephrotoxicity
Term
Isoniazid
Definition
Can be given for latent TB
Four first line drugs given to TB to reduce resistance
Inhibits biosythesis of mycolic acid
Resistance develops quickly when given alone
Blocks InhA gene, several mutations cause resistance; these resistances are all chromosomally-based in mycobacteria (NOT plasmid-based)
Cuases liver damage in pts over 35
Bacteriostatic but with Rif bacteriocidal
Can reach intracellular bacilli
Inactivated by acetylation
Also causes peripheral neuritis, CNS stiumation, hemolysis in pts with G6PD
Term
Rifampin
Definition
Can be given for latent TB
Inhibits DNA dep RNA polymerase
NOT narrow spectrum
rpoB mutations cause resistance
Used for pulmonary TB, leprosy
Tx carriers of N. menigitidis
Inhibits growth of gram pos and neg
NO serious side effects
Induces P450 system; decreases effectiveness of oral contraceptives and protease inhibitors
Orange color to urine
Term
Ethambutol
Definition
Front line for TB
Low toxicity
Slow drug resistance development
NEVER given alone
Inhibits arabinosyl transferases in the synthesis of arabinogalactan
Bacteriostatic
Cuase decreased visual acuity; not recommended in children
CAuses allergy, GI distress, numbness, joint pain or peripheral neuritis
Term
Pyrazinamide
Definition
Front line for TB
DNK mode of action
Prodrug; mutation in pncA gene confer resistance
Active at acidic pH
Best against dormant organisms
Can cause hepatic dysfunction
Critical first line drug; decreased duration of treatment by 6 months
Term
Rifabutin
Definition
Recently became a first line drug, replacement therapy for rifampin in treatment of TB in HIV pts
Similar to rifampin
Prophylaxis of MAC complex in HIV
Inhibits DNA dep RNA polymerase
ONLY front line in HIV infected pt; otherwise it is second line
Term
Streptamycin
Definition
Older drug used to treat TB in monotherapy
Causes ototoxicity
IV
Term
Dapsone
Definition
Treats leprosy if you see 1-5 patches
Most widely used and least expensive drug
Similar to sulfonamides, PABA antagonist
Oral
Can cause dose-related hemolysis
Nasal obstruction that improves with time
Term
Clofazimine
Definition
Treats multibacillary leprosy
A phenazine dye
Bactericidal against TBB and M. leprae
Binds preferencially to mycobacterial DNA
Insoluble in water, incompletely absorbed in Gi
Steady state in 30 days
Can cause GI disturbances, hepatitis, crystalline deposits in tissues and organs
Term
Thalidomide
Definition
Used in 50s as morning sickness drug
Teratogenic
Reduces level of TNFa by accelerating degradation of TNFa mRNA
Used to treat leprosy, especially erythema nodosum leprosum, an immune-complex reaction painful lesions
Causes increase in lean body mass; used in wasting in HIV pts
Orphan drug status, only used for certain diseases, can't become generic
Most heavily regulated drug in the US
Cause drowsiness, peripheral neuropahty, constipation, hypersensitivity rash
Term
Para-aminosalicylic acid
Definition
For second line TB, know side effects and site of action
Term
Ethionamide
Definition
Second line TB
Term
Capreomycin
Definition
Second line TB
Term
Kanamycin/amikamycin
Definition
Second line TB
Term
Fluoroquinolones
Definition
Second line TB
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