Term
| Vancomycin (action, kinetics, uses, side fx) |
|
Definition
-
-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.
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|
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Term
|
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 |
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Term
|
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 |
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Term
|
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 |
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Term
|
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 |
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Term
|
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
|
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 |
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|
Term
|
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 |
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|
Term
|
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 |
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Term
|
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 |
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|
Term
|
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 |
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|
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
|
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
|
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 |
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|
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
|
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 |
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|
Term
|
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) |
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|
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
|
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 |
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|
Term
|
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 |
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|
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
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|
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Term
|
Definition
INH, RIFampin, pyramidazine, streptoymcin, ethambutol
- need multiple drugs |
|
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Term
|
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
|
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 |
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Term
|
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,
- |
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|
Term
|
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 |
|
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Term
|
Definition
Dapsone: sulfonamide, can lead to hemolytic anemia
Rifampin
Clofaziminie: reedish brown color of skin
Thalidomide: teratogenic effects |
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Term
|
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
|
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
|
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
|
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
|
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
|
Definition
- anti fungal
no prescription
topical for dermatophytes |
|
|
Term
|
Definition
- azole of choise for histoplasma, blastomyce and espceially sporthris
active against aspergillus |
|
|
Term
|
Definition
tx of choice for aspergillosis
*** |
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Term
|
Definition
|
|
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
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Term
|
Definition
| - used for treatment of syphillis |
|
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Term
|
Definition
- substrate that can block excretion of penicllin
- can extend the half life. |
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Term
|
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.
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|
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Term
|
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
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Term
|
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
|
|
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Term
|
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
|
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
|
Definition
piperacilllin and tazobactam
- Usage: broad spectrum, mixed infection, aerobnes, anaerobes, G+ and G- |
|
|
Term
|
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
|
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
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Term
|
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 |
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Term
|
Definition
- against MRSA
- broad gram negetaive activity
- some activity against enterocci butnot many
causes hypersensitivity reaction, diarrhea, nausea, rash |
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Term
|
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
- |
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Term
|
Definition
- used for infections resistant to other agents such as P. aerugunoisa, mized aerobic and anaerobc infections.
ex such as primaxin. |
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Term
|
Definition
- carbapenem
- more activity against gram negative aerobes, less activity against gram positives |
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Term
|
Definition
| - less active carbapenems |
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Term
|
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 |
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Term
|
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 |
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Term
|
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, |
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Term
|
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 |
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Term
|
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 |
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Term
|
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 |
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Term
|
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** |
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Term
|
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 |
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Term
|
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 |
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Term
|
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
|
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
|
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
|
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 |
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Term
|
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 |
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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
|
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 |
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Term
|
Definition
- Non nucleoside reverse transcriptase inhibitors
- rapid resistance
- HIV1 only
CNS effects |
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Term
|
Definition
- Non nucleoside reverse transcriptase inhibitors
- rapid resistance
- HIV1 only
CNS effects |
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Term
|
Definition
- Non nucleoside reverse transcriptase inhibitors
- rapid resistance
- HIV1 only
CNS effects |
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Term
|
Definition
- fusion block
binds gp41 on viral envelope
for HIV |
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Term
|
Definition
CCr5 antagonist
for HIV, doesnt bind |
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Term
|
Definition
integrase block
for HIV 1 and 2 |
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Term
|
Definition
protease inhibitor
protease block
HIV 1 and 2
gi symptoms, lipodystrophy |
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Term
|
Definition
protease inhibitor
protease block
HIV 1 and 2
gi symptoms, lipodystrophy |
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Term
|
Definition
protease inhibitor
protease block
HIV 1 and 2
gi symptoms, lipodystrophy |
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Term
|
Definition
protease inhibitor
protease block
HIV 1 and 2
gi symptoms, lipodystrophy |
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|
Term
|
Definition
protease inhibitor
protease block
HIV 1 and 2
gi symptoms, lipodystrophy |
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Term
|
Definition
protease inhibitor
protease block
HIV 1 and 2
gi symptoms, lipodystrophy |
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|
Term
|
Definition
-Action
-Dichloroacetamide derivative
-Unknown
-Amebicidal in virtrol
-Kinetics
-oral
-Usage
-ameobas
-Toxicity
-Flatuelence, vomiting, pruritius, gives |
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Term
|
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
- |
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Term
|
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 |
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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 |
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Term
|
Definition
- action not well established
- does not cross BBB, half life is 6 hours
- useage for Pneumonia caused by pneumocytis jirvicii, also trypansomes and leismaniasis
- hypotension, sterile abcess, hypoglycemia, pacnreatitis, liver and kdiey dysfunction, hematologic issues
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Term
|
Definition
- action is mitochondrial membrane depolarization
- stays in plasms for 2.2 days, oral with gi absorption, fecal elimination
- used in Pneumocytis carioveci, babesiios, patients are intolerant of TMP smx
- rash, nausea, diarrhesa, has decreased concentration in plasma when administered with rifampin or tetracycline
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Term
|
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.
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Term
|
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
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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 |
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Term
|
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 |
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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
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Term
|
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 |
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Term
|
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 |
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Term
| Treating nematodes, pinworms, hookworks, roundworms |
|
Definition
- albendazole
- membendazol
- pyrantel pamoate
- threatworms, Strongyloides, tx with ivermectin
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|
|
Term
|
Definition
- shistsomiasis you treat with praziquantel-
- |
|
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Term
|
Definition
- beef and fish and tapeworks you go after with praziquantel
- albendazole for hyatide disease |
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|
Term
|
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.
- |
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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
- |
|
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Term
|
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 |
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Term
|
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 |
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|
Term
|
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
- |
|
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Term
|
Definition
- aminoglycoside
- poor bioavailabity
- used before bowel surgery to decrease aerobic flora.
- also treats hepatic encephalopathy |
|
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Term
|
Definition
| - IM, solue use is for treatment of antibiotic resistant gonococcal infectiors or gonococcal infections in penicllin allergic patients |
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