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116 Cards in this Set
- Front
- Back
what is an antimicrobial agent?
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chemical compounds biosynthetically or synthetically produced which either destroy or usefully suppress the growth or metabolism of a variety of microscopic or submicroscopic forms of life.
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what is the essential feature of effective antimicrobial agents?
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the ability to inhibit the growth of microorganisms at concentrations tolerated by the host.
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what do antimicrobial agents generally target?
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anatomic structures or biosynthetic pathways unique to microorganisms
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what is a bactericide?
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antibacterial which destroys bacteria
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what is a bacteriostatic agent?
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an antibacterial that mere suppresses growth
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what are the four classes of antimicrobial agents?
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antibacterial, antiviral, antifungal, and antiparasitic
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what are the two subcategories given for antifungals?
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fungistat and fungicide
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what are the two subcategories given for antiparasitic?
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antiprotozoal and antihelminthic
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define antibiotic.
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antimicrobials of microbial origin, most of which are produced by fungi or by bacteria of the genus Streptomyces
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define antimicrobial.
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any substance with sufficient antimicrobial activity that it can be used in treatment of infectious diseases.
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define chemotherapeutic.
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a broad term that encompasses antibiotics, antimicrobials and drugs used in the treatment of cancer. In the context of infectious diseases, it implies the agent is not an antibiotic.
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define Minimal inhibitory concentration.
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a laboratory term that defines the lowest concentration (ug/mL) able to inhibit growth of the microorganism.
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define minimal bacterial concentration
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minimum level to kill all of the bacteria.
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define resistant.
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organisms that are inhibited by clinically achievable concentrations of an antimicrobial agent.
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define sensitive.
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term applied to microorganisms indicating that they will be inhibited by concentrations of the antimicrobic that can be achieved clinically.
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define spectrum.
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an expression of the categories of microorganisms against which an antimicrobial is typically active
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what is a narrow-spectrum? Broad-spectrum?
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narrow: has activity against only a few organisms.
broad: has activity against organisms of diverse types |
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define susceptible.
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term applied to microoranisms indicating that they will be inhibited by concentrations of the antimicrobic that can be achieved clinically.
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what are the five considerations that determine which antimicrobial is appropriate for the infection?
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1) the infecting organism and its antimicrobial susceptibilities
2) the type of infection 3) host factors (age, drug allergies, renal function, etc) 4) factors associated with antimicrobial agents (dosage, routes of administration, etc) 5) public health considerations |
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what are the three possible sources of antimicrobial agents?
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biological origin, chemically synthesized and molecular manipulation
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what common antimicrobial has a biological origin?
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penicillin
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T/F
benzyl penicillin is a narrow-spectrum agent. |
TRUE
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what affect does benzyl penicillin have on gram positive cocci, gram negative cocci and enteric gram negative bacilli?
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Gram positive cocci- highly active
Gram negative cocci- highly active Gram-negative bacilli- little activity |
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If you needed an antibacterial antimicrobic that would inhibit cell wall synthesis, what are your two choices?
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B-lactams and glycopeptides.
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If you needed an antibacterial antimicrobic that would inhibit cell Protein synthesis, what are your four choices? what is the acronym?
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MCAT: Macrolides, Chloramphenicol, tetracyclines, and aminoglycosides
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If you needed an antibacterial antimicrobic that would inhibit nucleic acid synthesis, what are your four choices? What is the mnemonic?
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Queen Folate Married Rifampin:
Quinolones folate inhibitors metronidazole rifampin |
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If you needed an antibacterial antimicrobic that would act on the outer and cytoplasmic membrane, what are your two choices?
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polymyxin B and Colistin
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what are four subcategories of B-lactam?
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penicillins, cephalosporins, carbapenems, monobactams
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what are the two subcategories of glycopeptides?
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Vancomycin and teicoplanin
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what enzyme catalyzes the cross-linking of the amino acid side chains?
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transpeptidase
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what category of antimicrobials binds to transpeptidase preventing it from carrying out its function?
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B-lactams
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which antimicrobial binds directly to the amino acid of the cell wall preventing the binding of transpeptidase?
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vancomycin
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what infection is vancomycin used to treat?
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MRSA: methicillin Resistance Staphylococcous aureus
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T/F
the ring of the B-lactam is not essential for antibacterial activity. |
FALSE
It is absolutely essential! |
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T/F
B-lactams can only affect bacteria will cell walls. |
True.
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what is the classic example of a bacteria that is not sensitive to B-lactams?
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mycoplasm
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how are b-lactams classified?
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by chemical structure
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what is a B-lactam with one or more rings called?
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monobactam
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what is B-lactam with a ring that is fused to a five member penem ring?
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penicillins and carbapenems
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what is a b-lactam with a ring fused to a six member cephnem ring?
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cephalosporins
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from what genus is penicillium derived from?
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streptomyces
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which type of penicillin is injectible? which can be taken orally?
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injectible: Penicillin G
Orally: Penicillin V |
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what is penicillin G active against?
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gram positive organisms, gram negative cocci, and some spirochete
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what can broad spectrum penicillins do?
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penetrate the outer membrane of some Gram-negative bacteria
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what are the four types of penicillins?
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penicillin G, Penicillin V, broad spectrum penicillins and penicillinase-resistance pencillins
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what are the three subcategories of broad spectrum penicillins?
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ampicllin, carbenicillin, and ticracillin
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what are the three subcategories of penicillnase-resistance penicillins?
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methicillin, nafcillin, oxacillin
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what is the purpose of penicillinase-resistant penicillins?
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inhibits enzyme penicillinase produced by certain pathogens
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how are cephlosporins classifed?
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by generation
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what does a fourth generation cephalosporin have in relation to a first generation?
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a wider spectrum
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what is manipulated in cephalosporins to create more generations?
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side chain
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what is the activity of the first generation cephalosporins?
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gram positive organisms that resembles that of penicillinase-resistance penicillin
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what are the two subcategories of cephalosporins?
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cephazolin and cephalexin
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what is the activity of the second generation cephalosporins?
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expanded activity against B-lactams producing Gram-negative organisms. Expanded activity against enterobacteriacea species and activity against anaerobes.
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what is the number one normal flora in the gut that second generation cephalosporins act against?
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Bacteroides fragilis
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what are the three third generation cephalosporins?
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ceftriaxone, cefotaxime and cetazidime
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what are the two subcategories of second generation cephalosporins?
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cefoxitin and cefaclor
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what is ceftazidime used against? what is the clinically correlation?
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pseudomas aeruginosa; chosen in a febrile bone marrow transplant patient.
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what can ceftriaxone or cefotaxime be used against?
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childhood meningitis
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what are the three major causes of childhood meningitis?
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Neisseria meningitidis, streptococcus pneumoniae, and hemophilus influenzae
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what is the most common cause of meningitis in neonatals?
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steptocococcus pneumoniae
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what is the most common cause of meningitis period?
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neisseria meningitidis
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what is the activity of a fourth generation cephalosporin?
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wide spectrum antimicrobial effects: enhanced ability to penetrate the outer membrane of many gram-negative bacteria; resistant to many Gram-negative B-lactamases. Also active against wider spectrum of enterobacteriaceae.
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what is the only fourth generation cephalosporin?
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cephepime
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what are the two types of carbapenems? which one requires a coadministration of cilastatin and why?
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imipenem and meropenem; imipenem requires the cilastatin coadministration because imipenem is rapidly hydrolyzed by renal tubular dehydropeptidase 1 and cilastatin is an inhibitor of that enzyme.
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which B-lactam has the broadest spectrum? why?
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carbapenems: combination of easy penetration of gram-negative and gram-positive bacterial cells and a high level of resistance to B-lactamases.
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what was the first monobactum licensed in the US?
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aztronam
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to what specifically is the spectrum of aztreonam limited to?
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aerobic and facultatively anaerobic gram-negative bacteria
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why are anaerobic superinfections and major distortions of the bowl flora less common with aztreonam?
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because aztreonam does not produce a general suppression of gut anaerobes
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what is the main use of glycopeptides?
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against multiresistant Gram-positive infections including those caused by strains of staphylococci that are resistant to the penicillinase resistant penicillins and cephalosporins.
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where do the aminoglycosidases bind to in order to prevent protein synthesis of microbials?
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bind to multiple sites on both the 30S and 50S ribosomes--> preventing tRNA from forming initiation complexes.
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where do tetracyclines bind in relation to protein synthesis?
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30S ribosomes
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what does chloramphenicol block?
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formation of the peptide bond between the amino acids
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what does erythomycin and macrolides block?
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translocation of tRNA from the acceptor to the donor side on the ribosome.
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what are three important aminoglycosides used?
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steptomycin, gentomyocin and aminocasin
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what do sulfonamides block?
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folate precursors of DNA synthesis
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what affect does metronidazole have on DNA?
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inflicts breaks in the DNA itself
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what does rifampin inhibit?
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synthesis of RNA from DNA by inhibiting DNA polymerase
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what do quinolones inhibit?
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DNA topoisomerase and thus prevent the supercoiling required for the DNA to "fit" inside the bacterial cell.
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what affect to polymyxin B and colistin have on cell membranes?
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they bind to cell membranes of susceptible Gram-negative bacteria and alter their permeability resulting in loss of essential cytoplasmic components and bacterial death.
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polymyxin B and colistin use are now limited to what kind of applications?
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topical
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what are the consequences of indiscriminate use of antibacterial drugs?
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- can lead to a plethora of side effects and drug interactions
- hypersensitivity reactions - microbial superinfections - drive up the cost of health care - antagonisms between certain agents - foster the emergence of bacterial resistance, rendering previously valuable drugs useless |
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what are the unique viral events that occur in viral replication?
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attachment, penetration, uncoating, RNA-directed DNA synthesis (reverse transcription) and assembly and release of the intact virion.
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how can viral attachment be inhibited?
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by having an antibody bind to the extracellular virus and prevent the attachment of the virus to a cell receptor on the host cell
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how can we inhibit penetration of the virus?
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by using a neuraminidase inhibitor which will inhibit the fusion of an viral enveloped protein with the host cell membrane.
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what are the 2 neuraminidase inhibitors that selectively inhibit the neuraminidase of influenza A and B viruses? which one is oral and which one is a spray?
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oseltamivir (oral) and zanamivir (spray)
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what does neuraminidase do?
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aids in the release of newly formed viral particles form infected cells
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what are the agents in the antiviral inhibiting viral uncoating group? which one should be used cautiously with renal impaired patients?
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Rimantadine and amantadine (cautious in renal impaired patients)
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what is the activity of rimantadine and amantadine? How effective are these antivirals?
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active against ONLY influenza A. 70% effective in preventing influenza A illness when given daily during influenza outbreaks.
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what are idoxiuridine and trifluorothymidine used to treat? what type of treatment?
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herpetic keratitis; topical
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what is acyclovir used to treat? how?
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herpes simplex viruses (1 and 2), varicella zoster virus (less than HSV), and cytomegalovirus (least). Inhibits the thymidine kinase.
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what is gancyclovir used to treat? what is it in relation to acyclovir?
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cytomegalovirus and other herpes viruses; an analogue of acyclovir
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what is a classic example of an inhibitor of viral RNA synthesis/
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ribavirin
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this drug is standard treatment for HCV infections and is somewhat beneficial in RSV infections of infants.
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ribavirin
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what is the job of foscarnet? how?
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to inhibit viral DNA polymerase by blocking the pyrophosphate-binding site of viral DNA polymerase.
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what are interferons?
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host cell encoded proteins synthesized in response to double stranded RNA.
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what do interferons inhibit? what does it protect?
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viral protein synthesis and protects uninfected cells
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what are interferons effective against?
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hepatitis C and B and papilloma virus infections
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what are higher rates of replication associated with?
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higher rates of spontaneous mutation
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what is the selective pressure of the drug?
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probability of mutation is increased to the point that virus replication is substantially reduced
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T/F
single stranded RNA viruses have a slower rate of mutation than double. |
false.....
single has a higher rate. |
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T/F
some genes within a virus are more susceptible than others. |
true :)
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what are the two groups of chemotherapeutics against parasitic infections?
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antiprotozoan drugs and antihelminthic drugs
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what do antiprotozoan drugs do?
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interfere with nucleic acid synthesis (majority) or with carbohydrate metabolism (less common)
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what do antihelminthic drugs do?
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compromise worm's glycolytic pathways or neuromuscular function
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what are arsenicals used against?
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trypansomiasis
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what do heavy metals do to parasitic enzymes?
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binds and inactivates the SH group
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what are the four antimalarial quinolones? which one is the safest?
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quinine, 4-aminoquionolines (safest), 8-aminoquionolines, and 4-quinolinemthanols
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what do antimalarial quinolones do?
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accumulate in the parasitized host cells and inhibit nucleic acid synthesis. Also inhibits heme peroxydase leading to accumulation of heme metabolites lethal to parasites.
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which antimalarial quinolones is used against chloroquine resistant parasites?
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4- quinolinemethanols
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what does quinone inhibit?
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parasites electron transport chain resulting in specific blockade of pyrimidine biosynthesis.
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what are the two example of folate antagonists?
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sulfonamide and trimethoprim
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what does benzimidazole inhibit? what does protozoan does this taregt?
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fumerate reductase and polymerization of tubulin (cytoskeleton protein); helminths
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what member of the benzimidazole group is used against intestinal nematodes and trichinosis?
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thiabendozole
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which member of the benzimidazole group is effective against cestodes (tapeworms, hymenolepis, and echinococcus)?
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mebendzole
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what is praziquantel used to treat?
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schistosomiasis and clonorchiasis.
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