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Antimicrobials
Pharm drugs
106
Biology
Graduate
11/04/2012

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Term
Vancomycin (action, kinetics, uses, side fx)
Definition
  1. -Action
    -Cell wall synthesis inhibitor
    -Binds to D-Ala-D-Ala of cell wall, and inhibits transglycosylate
    -Also prevents cleavage of PG precrurors from phospholipids
    -Kinetics
    -Must be given parenternally
    -100% from kidney
    -Will last a full week in patient undergoing dialysys
    -Uses
    -G+, staph, strep, etnerococci
    -C. Dif
    -MRSA
    -Resistance: D-ala-D-lactate. No direct binding**
    -Side Fx
    -Ototoxicity or nephrotoxicitiy
    -Leukopenia
    -Red Neck syndrome: too rapid infusion leads to activation of mast cells. 
Term
Daptomycin
Definition
-Action
-Produces pore in the innter bacterial membrane
-Release of potassium leads to membrane depolarization and arrest of protein synthesis
-Also fxteichoic acid
-Kinetics
-Concentration dependent,
-Acts in calcium dependent manner
-Rapidly bactericidal
-Uses
-Useful in resistant forms
-Skin and wound infections
-MRSA, s pyogenes,
-Mainly G+ organisms
-NOT FOR PNeumoina
-Toxicity/side Fx
-Muscle discomfort
Term
Amikacin
Definition
-Actions: specifically most active, most powerful, an aminoglycoside
-Abnormal initiation complexes- so no new peptides are being formed
-Misreading of mRNA codons- if its in the process of making proteins, get misreading.
-Detachment of mRNA, due to block of translocation
-Kinetics
-IM or IV
-Half life is short, two hours
-Concentration dependent killing, given once a day
-Uses
-Serious infection in a hospitalized patient, sepsis, mixed infections
-Aerobic gram negative bacteria
-Can cover Gram+ when given with vancomycin and penicllin (open cell membrane so AGs can get inside)
specially for endocarditis caused by streptococci, staphylocci and enterocci. 
-Side Fx
-Resistance: enzymatic inactivation, impermeability, anaerobic conditions
- serious adverse fx. 
-10% patients serious fx
8th, nerve, renal toxicity, neuromuscular parlysis, fx p450s
Term
Gentamicin
Definition
-Actions:
-Abnormal initiation complexes- so no new peptides are being formed
-Misreading of mRNA codons- if its in the process of making proteins, get misreading.
-Detachment of mRNA, due to block of translocation
-Kinetics
-IM or IV
-Half life is short, two hours
-Concentration dependent killing, given once a day
-Uses
-Serious infection in a hospitalized patient, sepsis, mixed infections
-Aerobic gram negative bacteria
-Can cover Gram+ when given with vancomycin and penicllin (open cell membrane so AGs can get inside)
- specially for endocarditis caused by streptococci, staphylocci and enterocci. 
-Side Fx
-Resistance: enzymatic inactivation, impermeability, anaerobic conditions
- serious adverse fx. 
-10% patients serious fx
8th, nerve, renal toxicity, neuromuscular parlysis, fx p450s
Term
Tobramycin
Definition
-Actions: aminoglycoside
-Abnormal initiation complexes- so no new peptides are being formed
-Misreading of mRNA codons- if its in the process of making proteins, get misreading.
-Detachment of mRNA, due to block of translocation
-Kinetics
-IM or IV
-Half life is short, two hours
-Concentration dependent killing, given once a day
-Uses
-Serious infection in a hospitalized patient, sepsis, mixed infections
-Aerobic gram negative bacteria
-Can cover Gram+ when given with vancomycin and penicllin (open cell membrane so AGs can get inside)
-specially for endocarditis caused by streptococci, staphylocci and enterocci. 
more active vs pseudomonas, less nephrotoxicity
-Side Fx
-Resistance: enzymatic inactivation, impermeability, anaerobic conditions
- serious adverse fx. 
-10% patients serious fx
8th, nerve, renal toxicity, neuromuscular parlysis, fx p450s
Term
Streptomycin
Definition
-Actions: aminoglycosides
-Abnormal initiation complexes- so no new peptides are being formed
-Misreading of mRNA codons- if its in the process of making proteins, get misreading.
-Detachment of mRNA, due to block of translocation
-Kinetics
-IM or IV
-Half life is short, two hours
-Concentration dependent killing, given once a day
-Uses: this guy for TB or enterococci endocarditis, due to widespread resistance
-Serious infection in a hospitalized patient, sepsis, mixed infections
-Aerobic gram negative bacteria
-Can cover Gram+ when given with vancomycin and penicllin (open cell membrane so AGs can get inside)
-Side Fx
-Resistance: enzymatic inactivation, impermeability, anaerobic conditions
- serious adverse fx. 
-10% patients serious fx
8th, nerve, renal toxicity, neuromuscular parlysis, fx p450s
Term
Erythromycin
Definition
-Action: a macrolide
-Blocks translocation to P site of 50s, by binding to 23s rRNA
-Also inhibits formation of 50s
-Transpeptidation inhibition as well. Peptidly-tRNA is dissociated from ribosome
-Kinetics
-PO or IV
-Destroyed by stomach acid
-Excreted in bile
-No BBB
-Can be passed to fetus
- Resistance is methylation of 23srRNA binding site
-Usage
        - alternative to penicillin
         - covers gram positives organisms
        - for atypical pneumonias
        - gram negatives, rickettsia, tick borne, syphillis, campylo, 
-SideFx
       - resistance is plasmid encoded        
       - tremendous fx on the GI tract, diarrhea
        - acute hepatitis. 
       - deafness is rare and reversible
       - inhibitor of CYP450s, increases bioavailabilty many drugs. 
         - associated with sudden death, QT prolongation
Term
Azithromycin
Definition
-Action: a macrolide
-Blocks translocation to P site of 50s at 23s rRNA
-Also inhibits formation of 50s
-Transpeptidation inhibition as well. Peptidly-tRNA is dissociated from ribosome
-Kinetics
-PO or IV
-Destroyed by stomach acid
-Excreted in bile
-No BBB
-Can be passed to fetus
longer halif life, greater than 11 hours. tissue half life is 55-57 hours
- food decreases absorption
-Usage
        - alternative to penicillin
         - covers gram positives organisms
        - for atypical pneumonias
        - gram negatives, rickettsia, tick borne, syphillis, campylo,
        -lyme disease 
        - chlamydia, H. influenzae, and Moraxella
        - less active vs G+
-SideFx
       - less GI toxicity, no inhibition of p450
       - resistance is plasmid encoded        
       - tremendous fx on the GI tract, diarrhea
        - acute hepatitis. 
       - deafness is rare and reversible
       - inhibitor of CYP450s, increases many drugs. 
         - associated with sudden death, QT prolongation
Term
Clarithromycin
Definition
-Action: a macrolide
-Blocks translocation to P site of 50s at 23srRNA
-Also inhibits formation of 50s
-Transpeptidation inhibition as well. Peptidly-tRNA is dissociated from ribosome
-Kinetics
-PO or IV
-Destroyed by stomach acid
-Excreted in bile
-No BBB
-Can be passed to fetus
 - 4-6 hours half life, reduce dose in renal failure
-Usage
         -  H. influenzae, Moraxella, MAC, mycobacteria, Helicobacter
        - alternative to penicillin
         - covers gram positives organisms
        - for atypical pneumonias
        - gram negatives, rickettsia, tick borne, syphillis, campylo, 
-SideFx
       - still inhibits P450s, less GI toxicity. 
       - resistance is plasmid encoded        
       - tremendous fx on the GI tract, diarrhea
        - acute hepatitis. 
       - deafness is rare and reversible
       - inhibitor of CYP450s, increases many drugs. 
         - associated with sudden death, QT prolongation
Term
Telithromycin
Definition
-Action: a macrolide, called a ketolide
-Blocks translocation to P site of 50s
-Also inhibits formation of 50s
-Transpeptidation inhibition as well. Peptidly-tRNA is dissociated from ribosome
-Kinetics
-PO or IV
-Destroyed by stomach acid, more acid stable thatn erythroymcin
-Excreted in bile
-No BBB
-Can be passed to fetus
-Usage
active against macrolide and peniciliin resistant strep  pneumoniae (because its resistant to efflux)
         - use for chronic bronchitis, community acquired pneumonia,        sinusutis
        - 
-SideFx
          - exacerbations of myasethenia gravis
       - resistance is plasmid encoded        
       - visual disturbances
       - hepatotoxciity
       - tremendous fx on the GI tract, diarrhea
        - acute hepatitis. 
       - deafness is rare and reversible
       - inhibitor of CYP450s, increases many drugs. so drug interactions
         - associated with sudden death, QT prolongation
Term
Clindamycin
Definition
-Action
-Interferes with the formation of the initation complex and with aminoacyl translocation
- blocks pepetide bond formation at 50s ribosomal. bacteriostatic
-Kinetics
-Does not cross BBB
-Half life- 2-4 hours, modest dosage in severe liver or renal failure
-Resistance: altered ribosome, degradation. No Efflux pumps
-Uses
-Gram positives, aerobes and anaerobes( bacteroides)
- covers staph and strep in pen allergic patient
-Some gram negatives
-prophylaxis of endocarditis
-No coverage of enterococci and gram negative aerobic organisms
-Covers MRSA and bacteroides
-Some protozoal infections such as PCP- pneumocystiscariniipneuomina
-Sidefx/ toxicity
-Broad spectrum, opens up for C. dif infections, concerns for it
-hypernsitivity
hepatoxicity
-neuromuscular parlayisis
Term
Synercid(Quinuprustin-Dalfopristin
Definition
-Must know mechanisms of action (on the 50s ribosome, distinct synergism) effect up to 10 hours for staph aureus)
-Been superseded by lienzolid
-Not use, just no the pharmacology
-Made up of two streptrogramins as listeds
-Get synergist using them togeterh
-Dalforistin binds to 23s and inhibits peptidyltransferase, and enhances binding of quiniupristin, which inhibits peptide elongation
-Cidal overall.
-Useful for G+ cocci and pneuominia, atypical pneuomnia
p450 4A4 inhibition
- cyp 450, toxicity, server infusion related myaglias
- rapid bactericidal activity
Term
Linezolid
Definition
-Actions
-Binds unique site of 23ssubunts on 50s.
-Prevents formation of ribosome complex
- static
-Kinetics
-100%bioavailable
-Half
-Resistance: point mutation of 23s
-Uses
-MRSA, enterococci, pneumonia
-G+ ccoverage
-Nocardia
-Tb
-Static except for stretpocci
-Side fx/ toxicity
-Gi
-Bone marrow suppression
-Weak MAO inhibitor
-Neurological fx on optic nerve
-Expensive
Term
Chloramphenicol
Definition
-Actions
-Binds to 50s subunit of ribosome, static
blocks peptide bond formation at 50 s ribosome
-Interferes with transfer of peptide chain from A to P site, so interferens with transpeptidation
-Kinetic
-Crosses BBB
-Broad protein synthesis inhibitor
-No dosage reduction in renal failure, but reduce dose in liver
-Resistance: plasmid mediation. Reduced ribsomal binding
-Usage: very broad spectrum, carefully monitored
-Serious infections
-Meningitis
-Rocky mountain spotted fever
-Anaerobic infections
-Brain abcesses
-Side fx/ toxicity**
-Dose related suppression of bone marrow: leukopenia, anemia, thrombocytopenia
-Can lead to idiosynchaticaplastic bone marrow aplasia, possible leukemia
-Gray Baby syndrome: prematures and newborns only, cant get rid of it
-Antagonistic effects with a cell wall synthesis inhibitor
- anemia and aplastic anemia
Term
Tetracycline/ Doxycycline
Definition
-Action
-Bind to 30s subunit, and block tRNA from binding the A site
-Preventing the addition of amino acids
-bacteriostatic
-Kinetics
-Food, antacids effect absorption.
-Long acting. 16-18 hours. Mammalian cells lack active transport systom
-Doxy does not depend on kidney, diffusal of out of small bowel(can be used in someone with renal failure) 
-Resistance: efflux, ribosome alteration, inactivation, plasmid encoded
-Usage: broad spectrum
-Tx of inflammation of the prostate
-Affect G+ and G-
-Rickettsia
-Spirochetes
-Protozoa
-Rickettsia and lyme disease
-Syphillis
-Pneuomina, acne
-Malaria
-Toxicity
-Allergic response
-Significant GI fx, due to wipeage of GI
-Photosensitivity
-Adverse fx in children, bind calcium in teeth and bones. Get weakened, mottled and stained teeth
-Do not give to child less than 8 years old, pregnant mother, or lactating mother
-Liver toxic affect in women
-Anticoagulation effects
-Increase in intracranial pressure, increased eye pressure
-Open up patients to yeast infections
-Anatgonize the fx on penicllin
Term
Tigecycline
Definition
-Actions
-Binds 30s, prevents TRNA
-Kinetics
-IV only
-Bacteriostatic
-Resistance: not sure, but its not due to alteration or ribosome changes.. not affected by ribosomal alteration or efflux mechanisms
-Usage
-Highly resistant strains such as MRSA and vancomycin resistant enterocci
-Bacteroides
-Not useful in pseudomonas or proteus
-For serious hospital infections
-Side fx
-Check tetracyclines and doxycyclines
- mainly nausea and vomitting
Term
Sulfonamides
Definition
-Actions
-Blocks dihydropteratesynthetase
-Interferes with folic acid, competes with PABA
static
-Kinetics
-Cross BBB**
-Penetrates into cells
-Usually given with inhibitor of DHFR, or 2 other sulfonamides
-Resistance**: increased PABA or decrease in enzyme affinity
-Usage
-Nocardiosis
-toxoplasmosis
-Side fx/toxicity
-Hemolytic anemia in G6PD deficiency ppl
-Bone marrow suppression
-Precipiated in renal tubule.
-Fx on liver, hepaitits
-Kernicterus in newborns. – which is bilirubin released, from albumin and get encephalopathy
-Numerous drug interactions, tend to release other bound compounds (coumadin, methotrexate)
Term
Trimethorpim-Sulfamethoxazole
Definition
-Action
-Synergism.
-Sequestion inhibition of metabolic pathway of THF
-Fx dihydropheteratesynthetase and DHFr
- static
-Kinetics
-Eliminated via kidney
-Penentrate into prostate
-Dosage reduction via renal insufficiency
-Half life- 9-11 hours
-Resistance: change in enzyme affinity or quantity
-Usage: broad spectrum
-Bacteria and protozoa
-Malaria
-Not P.aeruginosa, pallidum, mycoplasma
-Important for PCP
-UTI, bronchitis, shigellosis, otitis media
- prostatitis
-Toxicity
-Bone marrow depression
-Renal injury
Term
Metrondiazole
Definition
-Action
-Pro drug. Must undergo rxn
-Reults in DNA damage leading to DNA stran scission
- forms free radical toxic metabolites in bacteria
-Kinetics
-Crosses BBB
-Renal elimination. 6-14 hours
-Usage- GET GAP on the Metro
      - giardia, enatmoeba, trichomonas, gardnerella, anerarobes, and pylori
-Only anaerobic organisms
-C. dif: for uncomplicated cases
-H. pylori
-Bacterioidesfragillis
-Side fx. Toxicity
-Metallic taste
-Vertigo, other neuropathies
-Leukopenia
-May turn urine brown
-No alcohol.
-Disulfiram like effect.
-Mutagenic and carcinogenc, no use in pregnant women, first trimester
Term
Tinidazole
Definition
-Action
-Similar to metron.
-DNA stranscisision
-Kinetics
-Substrate fir CYP3A4. 12-14 hours, take with food
-Usage
-Active against metronidazole resistant strains for trichomonas
-Also giardia, enatmoebahistolyic, pylori and fragillis
-Side fx/toxicity
-Expensive
-Nausea, metallic taste
-Vomiting, sizures
-Antabuse effect
-Neuropathy
-Single dose appears to be better tolerated than a signel dose ofmetronidazole**
-No during first emesetser
Term
Ciprofloxacin/ sulfonamides. any floxacin
Definition

 

-Action
-Cidal
-By inhibiting DNA gyrase, supercoiling unravels and cell burst
-DNA gyrase does negative supercoiling
-Gram –(topo II), Gram+, its topo IV
-Kinetics
-Orally
-High bioavailability
-Penetrate mammalian cells
-Don’t take with antacids
-Resistance: chromosomal mtuation of A subunit of DNA gyrase, changes in drug permeabiltiy
-Usage: broad
-Enteric gram negatives infections, E. coli and Salmonella
- focuses on gram negative rods of urinary and GI tracts
-Neisseria pneumonia
-Haemophils
-Pseudomonas
-MRSA
-Not active against anaerobes
-Repsiratoryquinolones active vs S. pneuomnia, mycoplasma, chlyamdia and legionella
-Good for treating strep and atypical pneumonias
-Tx for UTIs, except for moxifloxacin. Low lvls in urine
-Prostatitis
-Bacterial diarrheal
-Anthrax
-prophylaxis
-Toxicity/ side fx
-Cipro is inactive vs anaerobes and poorly active vs pneumococci
-Some interaction with eukarytoic DNA gyrase,
-BIG GI fx
-Lightheadhedness
-Cartilage erosion
-Seizure
-Not used for children, or pregnancy ppl
-Adults over 60, tendonitis. Achilles ruptures
-Cipro may interfere with theophyllin levels
-Some cause dysglycemia, gatifloxacin
-Prolong Qt interval
-False opiate screen

 

 

 

 

 

 

Term
Tb Treatment
Definition

INH, RIFampin, pyramidazine, streptoymcin, ethambutol

- need multiple drugs

Term
Isoniazid
Definition
-Action
-Pro drug, activated by KatG- catalaseperoxidase
-Inhibitsmycolic acid formation.
-Cidal for dividing organisms
-Kinetics
-Crosses BB
-Aluminumanatacids may inhibit absorption
-Metabolized by the liver
-Resistance: mechanism unknown, present
-Uses
-Tb
- solo prophylaxis
-Toxicity
-Liver toxicity. Reduce dose for liver dysfucntion, must monitor liver enzyme
-Produce a peripheral neuropathy, as it looks like B6
-Greater risk in alcoholics, pregnant women and liver disease
Term
Rifampin
Definition
-Action
-Protein synthesis inhibitor
-Inhibits DNA dependent RNA polymerase,
-Cidal
-Kinetics
-Crosses BBB
-Eliminated in the bile
-Metabolized in the liver:
-Uses: broad spectrum
-Tb
-Leprosy
-MRSA
-Pneumonia
-Meningitis
-Especially if there is biofilms
-Toxicity/ side fx***
-Liver dysfunction is an issue
-Resistance is rapid to it, alteration in bacterial polymerase
-Never used alone**
-Mitochondrial polymerase is susceptible at higher concentration
-Changes fluids into orange red color
-Serious effects on liver
-Worsened with intermittned therapy
-Causes flu like fever, kidney fx, thrombocytopenia, anemia
-Shock
-Many drug interactions due to induction of CYPs***major inducer of cyps
-Methoadone, birth control bills, predisone, steroids, sulfonyureas being treated for diabetes, ketoconazole, coumadin and blood thinners
-These all have reduced half life with this drug
Term
Pyrazinamide
Definition
-Action
-Sterizlie intracellular organisms. Reduces relapse rate
-Given in the first 2 months with INH and Rifampin
- inhibits mycolic acid production by blocking mycobacterial fatty acid synthase
-Kinetics
-Pro drug. Converted by pyrazinamidase
-Uses
-Tb
-Resistance builds up
-Side fx
-Increased incidence of gout
-Major fx on liver,
-
Term
Ethambutol
Definition
-actions
-Bacteriostatic
-Cell wall synthesis inhibitor
-Inhibits arabinoslytransferase, involved in polymerization
-Kinetics
-Oral, excereted in urine
-Reduce dose with renal failure
-Uses
-tb
-Side fx
-Eyes
-Optic neuritis
-Diminished acuity
-Color blindess
-All reversible
Term
Drugs for Leprosy
Definition

Dapsone: sulfonamide, can lead to hemolytic anemia

Rifampin

Clofaziminie: reedish brown color of skin

Thalidomide: teratogenic effects

Term
Amphotericin B
Definition
-Action: anti fungal
-Alters the permeability of the cell membrane by bind erogsterol and creating holes
-cidal
-Kinetics
-IV route
-Crosses BBB poorly
-Intrathecally if need be
-Usage
-For deap infections
-Does not cover dermatophytes
-Cryptococcal meningitis
-Side fx/ toxicity
-Tremendous chills and fever**
-Due to cytokine release
-Renalrubular damage
-Acidosis
-Loss of K+
-GI fx
-Anemia
-Inhibits EPO production
-Have to be given primer dose
Term
Flucytosine
Definition
-Action: anti fungal
-Inhibits nuclei acid synthase
-5 FU is inhibitor of thymidylatesynthase
-Remember cytosine deaminase and thymidylatesynthase
-Kinetics
-Pro drug, gets converted through cytosine deaminase to 5-FU
-Crosses BBB
-Given orally
-Renal elminatin
-Resistance: common if used alone, lose enzyme to convert it
-Usage
-Limited
-Cryptococcus, chromoblastomycosis
-Goes with amphotericin B
-
-Toxicity/ side fx
-Bone marrow depression
-Diarrhea
-Colitis
-hepatitis
Term
capsofungins
Definition
-Action: antifungal
-Cell wall synthesis inhibitor
-Inhibi the enzyme, beta, 1-3-D
-Kinetics
-Renal clearance
-Needs dosage for hepatic insuffiency
-Usage
-Aspergillus and candida
-No cryptococcus
-Side fx
-Well tolerate
-Flushing, GI, drug interactions
Term
Ketoconazole
Definition
-Action
-Blocks formation of ergosterol, no lanosterol to ergosterol
-Kinetics
-Can only be absorbed in acid conditions
-Must eat before hand
-Does not cross BBB
-Excreted by the kidney
-Usage
-Broad coverage
-Dermatohyte
-Oral or gastroesophagelcandidiasis
-Histoplasmosis, blastomycosis
-Sidefx
-Inhibits of P450
-Hepatic necrosis
-Interference with human steroid metabolism
-Breast deblopment, changes in steroid synthesis, changes in cortisol
-Major drug interactions** (
-Can interfere with absorption of rifampin
Term
Fluconazole
Definition
-Action
-Blocks formation of ergosterol, no lanosterol to ergosterol
-Most widely used
-High bioavailability
-Preferred over ketoconazole
-Kinetics
-Can be absorbed whenever
-Must eat before hand
-Crosses BBB
-Excreted by the kidney, dosage adjustment reuquires
-Usage
-Broad coverage
-Dermatohyte
-Not active against asergillus
-Oral or gastroesophagelcandidiasis
-Histoplasmosis, blastomycosis
-Sidefx
-Inhibits of P450
-Hepatic necrosis
-No FX on human steroid fx
-Major drug interactions** (
-Can interfere with absorption of rifampin
Term
Clotrimazole
Definition

- anti fungal

no prescription

topical for dermatophytes

Term
Intraconazole
Definition

- azole of choise for histoplasma, blastomyce and espceially sporthris

active against aspergillus

Term
Voriconazole
Definition

tx of choice for aspergillosis

 ***

Term
Posaconazole
Definition
active vs mucormycosis
Term
Natural Pencillins (G and V)
Definition
  • Action:  block transpeptidation action by blocking PBPa
  • Kinetics: usually short half life, kidney excretion. can be fixed by giving propercidin//crosses the BBB but is excreted out. good for meningitis but not encephalitis. 
  • Usage: ear, nose and throat infections. 
  • Toxicity: allergic reactions, seizures
Term
Benzyl Penicllin
Definition
- used for treatment of syphillis
Term
Probencid
Definition

- substrate that can block excretion of penicllin

- can extend the half life. 

Term
Ampicillin/amoxicillin
Definition
  • Actions: blocks transpeptidation, more active against G-. these are aminopenicllins
  • Kinetics: crosses BBB. susceptible to beta lactamases//more acid resistant
  • uses: more g- rods, amoxicillin is primary choice for otitis media and upper respiratory.//also h influenzae, enterocci, shigella, salmonella, 
  • Toxicity: Gi fx due to changes in natural flora. 
  • amoxicillin has less diarrhea. 
Term
Piperacillin
Definition
  • Action: extended spectrum penicillins. 
  • kinetics: susceptible to beta lactamases, synergy with aminoglycosides
  • Uses: more coverage of G-, p. aeruginosa. enhanced ability to penetrate gram negatives
  • toxicity: low potassium due to excretion of sodium, conduction atlerations, qualitative platelet defects//false positve for aspergillosis
Term
Nafcillin/Oxacillin
Definition
  • action: beta lactamase resistant penicillin. aimed at beta lacatmase producing strains of G+ cocic
  • kinetics: corsses BBB. act on PBP2a. resistance is change in this. biliary clearance
  • uses: only staph and strep. espcially MRSA. no enterococcus
  • toxicity: nafcillin: interstitial nephritis, oxacillin causes hepatitis, both cause leukopenia
Term
Augmentin
Definition

- amoxicillin and clavulanic acid

- used for childhood otitis media. 

- clavulanic acid binds and inhibits many bacterial lactamases

Usage: s. aureus, fragillis, influenzae, moraxella, gonorrhea, not active vs pseudomonas

Toxicity: more diarrhea than amoxiccilii

Term
Primaxin
Definition

- imipenem and cilastin

- cilastatin a renal dyhdropeptidase inhibitor. , allows it to be active in urinary tract. 

 

-Actions
-Cilastin inhibits renal dehydropeptidase
-Used for infections resistant to other agents.
-Very broad spectrum
-Resistant to most beta lacatmases though it may induce them
-Kinetics
-Half life is 1 hours.
-Adjust with renal dysfunction
-Usage
-Hospital acquired gram negeative., P. aeruginosa
-Staph aureausNO MRSA
-Covers B fragillis
-Toxicity

Seizures more common

Term
Zosyn
Definition

piperacilllin and tazobactam

- Usage: broad spectrum, mixed infection, aerobnes, anaerobes, G+ and G-

Term
Cefazolin, Cephalexin
Definition
-Action: 1st gen cephlasporins
-Cell wall inhibitors
-Bactericidal
-Concentration independent bactericidal activity
-Kinetics: does not cross BBB
-Usage: G+, pneumococci, community acquired infections, no pseudomonas or bacteroides coverage. has coverage of klebsiella
tx of skin and soft tissue and urinary tract infections
-Toxicity : dosage reduced with renal impairment
Term
Cefuroxime, cefoxitin (cephamycin)
Definition
 
-
-Action: 2nd generation cephalsporins
-Cell wall inhibitors
-Bactericidal
-Concentration independent bactericidal activity
-Kinetics
-Crosses BBB
-Usage
-Cerufoxime- H influenzae
-Cefoxitin- fragillis
-Sinusitis, otitis, lower resp infections, community acquire pneumonia.
-Active against lacatmase producing H influenzae or K pneumonia
-Toxicity
-Like penicillin
-
Term
Cefotaxime-ceftazidime-cefoperazone
Definition
  • 3rd gen cephlasporin
  • coverage for hospital infections. coverage over some P. aeruginosa and resistant meningitis***
  • toxicity like penicillin
  • ceftazadime 3rd gen, good for Pseudomonas Aeruginosa
    c
Term
Ceftriaxone
Definition
  • action: 3rd gen cephlasporin
  • pharm: not dependent on kidney, eliminated via bile, must know biliary shit
  • usage: meningitis(first line treatment for this***), gonorrhea, community acquired pneumoina, lyme disease, osteomyelitis
  • Toxicity: biliary concretion, diarrhea, avoid coadmin with calcium IV solutions as it leads to pulmonary precipitations. avoid in hyperbilburinemic neonates as it may displace bilirubin causing bilirubin encephalopathy
Term
Cefepime
Definition
-Action
-4thgeneerationcephlasporin
-Kinetics
-More resistance to chromosomal beta lactamases, but still hydrolyzed by enterobacter stuff
-Crosses BBB
-Renal elimination
-Usage
-Equalvs gram positive and gram negetiave
-S. aureus, strep, p aeruginosa, haemophilus and neissure
-Broad spectrum

Toxicity

Term
Ceftaroline
Definition

- against MRSA

- broad gram negetaive activity

- some activity against enterocci butnot many

causes hypersensitivity reaction, diarrhea, nausea, rash

Term
Aztreonam
Definition
-Actions
-Similar to 3rd generation ceftazdime
-A beta lactam structure, just that
-Literally no immunogenicity
-Kinetics
-Renal elimination, dose adjust.
-Crosses BBB
-Usage
-Only active against aerobic gram negatives (PBP3)
-Not active against gram positive or anaerobes
-Toxicity
-Minimal cross immunogenicity
-
Term
Carbapenems
Definition

- used for infections resistant to other agents such as P. aerugunoisa, mized aerobic and anaerobc infections. 

ex such as primaxin. 

Term
Meropenem/ doripenem
Definition

- carbapenem

- more activity against gram negative aerobes, less activity against gram positives

Term
Ertapenem
Definition
- less active carbapenems
Term
Acyclovir
Definition
-These are nucleic acid inhibitors
-Actions
-Nucleic acid inhibitors
-Phosphorlylation against first enzyme. Only active in cells infected with a virus
-Competitive inhibit viral DNA polymerase, no DNA synthesis
-Incorporated into the DNA and result in chain termination
-Nucleoside analgous of guanosine**, results in chain termination
-Kinetics
-Prodrugs
-Initial phosphorlyation by, gets triphosphorlated
-Way more effective on viral plymerase
-Low bioavailability
-Eliminated by kidney
-Crosses BBB***
-Resistance: viral strain doesn’t have thymidinekinase, no phosphorlytaion, chain in kinase, change in polymerase
-Usage
-Herpes 1 and 2
-German measles: chicken ox
-Shingles
-Varicella zoster
-Epstein Barr
-Toxicitiy
-Minimal
-Reversible renal dysfucntion
-Neurotixicity
-Can use it all the time
Term
Ganicyclovir
Definition
-Action
-Has to bephosphorlyated to become active (different enzyme than acyclovir
-Inhibits DNA polymerase activity
-
-Kinetics
-Intraceullar half life more important than serum half life
-Valgancylovir has better bioavailability
-Usage
-Broad spectrum
-CMV mainly***, severe
-HSV mainly, that are resistant to acyclovir
-Toxicity
-Terminal 3’ hydoxy ring, incorporated both into host cell and viral DNA
-Leads to Bone marrow suppression, 25-50% developing graunlocytpoenia
Term
Cidofovir
Definition
-Action
-It is a nucleotdie, already phosphorlyated
-Diphosphate is active, inhibits viral DNA polymerase**
-Kinetics
-Given with Probenecid
-Kidney secretion
-IV only
-Usage
-Broad spectrum. Various herpes, pox, paipilloma
-CMV retinitis
-Toxicity
-Nephrotoxicity,
Term
Foscarnet
Definition
-Action
-Inhibits viral DNA polymerase (different locus than ayclovir)
-Inhibits reverse transcriptase
-Kinetics
-IV only
-BBB
-Enters mphages
-Renal
-Usage
-Herpes viruses
-Primarily CMV retinitis and acyclovir resistant HSV infections
-Synergism with ganicyclovir
-Toxicity
-Impaired renal fxn
-Anemia
-Tremor
-Seizures
-hypocalcemia
Term
Interferon Alpha
Definition
-Actions
-Inhibiting translation of mRNA into viral proteins
-Stimulate immune defense
-Kinetics
-IM or SC
-No kidney
-Stay in cells for a long time
-Usage
-Usage is in viruses that induce tumor formation
-Hep C
-Condylomaacuminata
-Kaposia, hairy cell
-Toxicity
-Very toxic
-Flu like symtpoms
-Bone marrow suppression
-Neuroticivity
-Alopecia
-Liver enzymes
-Thyroiditis
-Renal and cardiac toxicity
Term
Ribavirin
Definition
-Actions
-Inosinemonophosphatedehydrogenase block
-Depletion of guanuanosine nucleotides and inhibition of viral RNA synthesis
-Kinetics
-Crosses BBB
-Renal elimination
-Inhalation, oral
-Usage
-RSV
-Hep C with IFN alpha
-Toxicity
-Anemia, hemolytic anemia
-Tetrogenic in pregnancy
Term
Amantadine
Definition
-Actions
-M2 protein block, early stage of Influenza A, uncoating, target is M2 proteins
-Kinetics
-Renal elimiation
-Excreted unchanged in urine
-Lower dose in elderly
-Usage
-Prophylaxis for flu A epidemic
-Toxicity
-CNS, neurotoxicity. Confusion, nervousness, coma,
-Anticholinergicfx. Dry mouth. Palpitations, dry mouth
-Use with caution in glaucoma and BPH**
Term
 Zanamivir, oseltamivir
Definition
-Actions
-Neuraminidiaseblcok
-Reduce viral spread, decrease virons being released
-Kinetics
-80% bioavailabilty
-Inhalation or orally
-Use within 48 hours of contact with influenza
-Usage
-Influenza A and B prophylaxis
-Toxicity
-Zan: throat discomfort, bronchospasm
-Oselatmivir= nausea, vomiting, headache
Term
Zidovudine
Definition

- nucleoside analgo, reverse transcriptase block

- competition with natural nucleoside, chain termination

most active against HIV 2. 

toxic

lipodystrophy is common

cross resistant is variable

Term
Didanosine
Definition

- nucleoside analgo, reverse transcriptase block

- competition with natural nucleoside, chain termination

most active against HIV 2. 

toxic

lipodystrophy is common

cross resistant is variable

Term
Stavudine
Definition

- nucleoside analgo, reverse transcriptase block

- competition with natural nucleoside, chain termination

most active against HIV 2. 

toxic

lipodystrophy is common

cross resistant is variable

Term
zalcitabine
Definition

- nucleoside analgo, reverse transcriptase block

- competition with natural nucleoside, chain termination

most active against HIV 2. 

toxic

lipodystrophy is common

cross resistant is variable

Term
lamivudine
Definition

- nucleoside analgo, reverse transcriptase block

- competition with natural nucleoside, chain termination

most active against HIV 2. 

toxic

lipodystrophy is common

cross resistant is variable

Term
Abacavir
Definition

- nucleoside analgo, reverse transcriptase block

- competition with natural nucleoside, chain termination

most active against HIV 2. 

toxic

lipodystrophy is common

cross resistant is variable

Term
Tenofovir disoproxil fumarate
Definition

- nucleoside analgo, reverse transcriptase block

- competition with natural nucleoside, chain termination

most active against HIV 2. 

toxic

lipodystrophy is common

cross resistant is variable

Term
Emtricitibane
Definition

- nucleoside analgo, reverse transcriptase block

- competition with natural nucleoside, chain termination

most active against HIV 2. 

toxic

lipodystrophy is common

cross resistant is variable

Term
Nevirapine
Definition

- Non nucleoside reverse transcriptase inhibitors

- rapid resistance

- HIV1 only

CNS effects

Term
Efavirenz
Definition

- Non nucleoside reverse transcriptase inhibitors

- rapid resistance

- HIV1 only

CNS effects

Term
Delavirdine
Definition

- Non nucleoside reverse transcriptase inhibitors

- rapid resistance

- HIV1 only

CNS effects

Term
Enfuvirtide
Definition

- fusion block

binds gp41 on viral envelope

for HIV

Term
Maraviroc
Definition

CCr5 antagonist

for HIV, doesnt bind

Term
Elviegravir
Definition

integrase block

for HIV 1 and 2

Term
Saquinavir
Definition

protease inhibitor

protease block

HIV 1 and 2

gi symptoms, lipodystrophy

Term
Indinavir
Definition

protease inhibitor

protease block

HIV 1 and 2

gi symptoms, lipodystrophy

Term
Ritonavir
Definition

protease inhibitor

protease block

HIV 1 and 2

gi symptoms, lipodystrophy

Term
Nelfinavir
Definition

protease inhibitor

protease block

HIV 1 and 2

gi symptoms, lipodystrophy

Term
Amprenavir
Definition

protease inhibitor

protease block

HIV 1 and 2

gi symptoms, lipodystrophy

Term
Fosamprenavir
Definition

protease inhibitor

protease block

HIV 1 and 2

gi symptoms, lipodystrophy

Term
Diloxanide Furoate
Definition
-Action
-Dichloroacetamide derivative
-Unknown
-Amebicidal in virtrol
-Kinetics
-oral
-Usage
-ameobas
-Toxicity
-Flatuelence, vomiting, pruritius, gives
Term
Iodoquinol
Definition
-Actions
-Luminal amebicide
-Kinetics
-Poorly absorbed, only effective in GI tract
-Usage
-amoebas
-Toxicity
-Rash, acne, enlarged thyroid
-Subacutemyelooptic neuropathy, optic atrophy, visual loss
-
Term
Paromomycin
Definition
-Action
-Aminoglycoside antibiotics
-Intestinal amebiasis
-cryptosporidosis
-Kinetics
-Very little absorbed
-Usage
-amoebas
-Toxicity
-GI fx
-Rarely 8th nerve or renal damage if taken orally
Term
Treatment levels for ameobas
Definition

- asymptommatic: diloxanide furoate

- mild to moderate- add metrondizaole or tinidazole

- severe- as above, give fluid

- hepatic abcess- add chlorquine

Term
Pentamidine
Definition
  1. action not well established
  2. does not cross BBB, half life is 6 hours
  3. useage for Pneumonia caused by pneumocytis jirvicii, also trypansomes and leismaniasis
  4. hypotension, sterile abcess, hypoglycemia, pacnreatitis, liver and kdiey dysfunction, hematologic issues
Term

Atovaquone

Definition
  1. action is mitochondrial membrane depolarization
  2. stays in plasms for 2.2 days, oral with gi absorption, fecal elimination
  3. used in Pneumocytis carioveci, babesiios, patients are intolerant of TMP smx
  4. rash, nausea, diarrhesa, has decreased concentration in plasma when administered with rifampin or tetracycline
Term
Chloroquine
Definition
  • for malaria
  • schizonticide, in blood. take it before going in
  • treat in areas without resisance to P. falciparum
  • safe to be used in pregnancy
  • lots of resistance, but preferred antimalarial
  • lowest number of side effects.
  • concentrated in RBCs
  • reistance is increase in P glycoprotein, gets effluxed out
  • adverse effects: changes in ECG very common//skin and hearing problems//visual disturbacences//gastric lavage. 
Term
Mefloquine or Malarone
Definition

- tx for malarina in areas with resistant to P. falciparum

  • 5-30x more potent than quinine, but slower acting
  • heme polymerase
  • long half life, not used in women liable to become pregnant
  • minor side fx, local irritant, GI, nauzea
  • higher doses has neuropsychiatric symptoms
  • contra with history of epilepsy or psychiatric disorders
Term
Doxycycline, tetra cycline or clindamycin
Definition

- fo rares with multi drug resistant P. falciparum

anti biotics used against it

- clindamycin is safe in neonates and pregnacy

Term
Primaquine
Definition

- termianl prophylaxis for P. vivax and P. ovale.

-Actions
-Only tissue schizontoside
-Gets rid of latent infections
-For vivax andovale
-Mechanism not well known
-Kinetics
-Only given orally
-Concentrated in various tissues
-Usage
-For Vivax and ovale
-Toxicity
-Never give parenternally
-Results in profound changes in blood pressure
-Changes the ECG
-Becareful is G6PD patients
-Hemolysis, risk of cyanosis
Term
Artesunate, artemether, aretmotil
Definition

- an artemisinin

treatment for malaria in the ER

- most rapid active anti malarial anget

- rapid acting

 

-Action
-New and very little reistance
-Formation of free radicaly which modify and damage malarial proteins
-Kinetics
-Prophylactically, have to be combined with another agent
-Usage
-Acute attack of malaria
-Most rapidly acting schiztonizde
-Toxicity
-Very safe
Term
Lumefantrine
Definition
-Action
-Kinetics
-Given with coartem, only used in combination with arthmether
-Given orally with fatty food to prolong anti malaria affect
-Usage
-marlaria
-Toxicity
-No significant heart or arythmia risk
Term
Proguanil
Definition
-Actions
-Inhibitor of DHFR
-Blood schizonticide
-Interferes with sporozites in blood stream and those penetrating the liver
-Inhibits primary stage of P. falciparum,
-Kinetics
-Pro drug
-Never given alone, comibned with chlorquine, malrone or atovaquon
-Usage
-Inhibiting primary tissue stage.
-Toxicity
-Safe in pregnancy
-infrequent
Term
Treating nematodes, pinworms, hookworks, roundworms
Definition
  1. albendazole
  2. membendazol
  3. pyrantel pamoate
  4. threatworms, Strongyloides, tx with ivermectin
Term
Tx Trematodes
Definition

- shistsomiasis you treat with praziquantel-

Term
Tx: cestodes
Definition

- beef and fish and tapeworks you go after with praziquantel

- albendazole for hyatide disease

Term
Albendaole/ mebendazole
Definition
-Actions
-Bind to tubulin, inhibition of microtubulepolymeraization
-Impaired glucose uptake and ATP production
-Kinetics
-Usage
-Nematodes except strongyloide
-Forhyatid cyst disease
-For cystercosis.
-Toxicity
-Minimal toxicity
-Contra in pregnancy and young children, less than 2
-Contra cirrhosis.
-
Term
Diethyl carbamazine citrate
Definition
-Action
-Cell membranehyperpolarization
-Immobilizes the worm
-Kinetics
-Orally for 2-3 weeks
-Usage
-Microfilarie, wucherica, loaloa, onchocerca
-Toxicity
-Minimal
-Dying worms can elicit rxns
-Give with antihistamines
-
Term
Ivermectin
Definition
-Actions
-Increase GABA
-Paralyzes nematode by intensifying inhibitory GAB
-Kinetics
-Orally, 1 to 2 days
-Usage
-Nematodes, strongyloides, andonchocerca
-Toxicity
-Minimal drug toxicity
-Pruirtis
-Allergic reactions to dying shit
Term
Praziquantel
Definition
-Actions
-Increases permeability of cell membranes to calcium
-Leads to parlysis and death
-Muscular depolarization
-Tegument vaculozation
-Kinetics
-Single or oral doses over 2 days
-Highly effective
-Crosses BBB
-Usage
-Cestodes and trematodes
-Mosttrematodes, tapeworms
-Toxicity
-Many mild adverse effects
-Headache, nausea, vomitting, diziness, drowing
-Antihistamines for dying worms
- head ache, rash, sedation
Term
Pyrantel Pamoate
Definition
-Actions
-Increases Ach release and blocks acetycholinesterase in susceptible worms
-Leads to neuromusclarparlyisis and cell death
-Kinetics
-Single dose highly effective
-Heavy use hookworm
-Usage
-First line drug for common nematode infections (hookworm, pinworms, ascariasis)
-Available without a prescription
-Toxicity
-Minimal
-
Term
Neomycin
Definition

- aminoglycoside 

- poor bioavailabity

- used before bowel surgery to decrease aerobic flora.

- also treats hepatic encephalopathy

Term
Spectinomycin
Definition
- IM, solue use is for treatment of antibiotic resistant gonococcal infectiors or gonococcal infections in penicllin allergic patients
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