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| Has a nucleus and other organelles inside the cell (human) |
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| bacteria, yeasts, parasites, living cells, usually not viral |
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same as antibiotic
bacteria, yeasts, parasites,
living cells, usually not viral |
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-Exploit differences between pathogens and humans
-Biochemical pathways
-Rigid cell walls (bacteria and yeasts) |
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| What drug is the hardest to develop? |
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Definition
Eukaryotic pathogens (parasites, fungi)
pathogens close to humans |
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Target DNA replication and unwinding
Inhibit unwinding of DNA |
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Definition
Target DNA replication and unwinding
binds and distorts DNA |
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Definition
Target Transcription-Interfere with RNA production from DNA
-Binds RNA polymerase |
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Definition
-Lipids in membrane
-Polymyxins- detergent, interacts with cell membrane (polyscporin, bacitracin, neosporin) |
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Definition
-Interfere with cell wall synthesis
ex: penicillin, Cephalosporins, cephamycins |
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Definition
Activity of drug against pathogen vs. activity of drug against human cell
-Best if activity against human cells is 100x to 1000x above activity against pathogen |
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Definition
Kill growing bacteria (don't kill static cells)
ex: quinolones, penicillins |
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Definition
Inhibit growth
Ex; tetracyclines, macrolides, cholamphenicol |
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Definition
| Drugs that can cross mucosal membranes and enter blood stream |
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Definition
| Drugs that cannot cross mucosal membrane and enter blood stream on their own must be given through IV. |
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Term
| Host cell permeability is important for: |
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Definition
| Intracellular pathogens whether they can penetrate (macrolides, tetracyclines) or do not penetrate (penicillin) |
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-Immune system- major control of pathogens
-drugs- assist immune system in the war
BEST way to treat is restore immune system |
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Definition
Screening soil samples and decaying plants for inhibitory microorganisms
ex: penicillin came from common bread mold, Penicillium |
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| Synthetic drug development |
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Definition
| Quinolones- Chemically synthesized |
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Definition
-Compound identified from screen-natural or synthetic
-Shows some activity against pathogen |
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Definition
-Compound identified from screen-natural or synthetic
-Shows some activity against pathogen |
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Term
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Definition
-Select a target enzyme
-Determine its structure and shape
-Determine its active site
-Fit small chemicals into the active site
-Test these small chemicals for activity |
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Definition
Drug Discovery ->
Preclinical ->
Clinical I, II, II ->
Approval IV ->
Consumers |
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| Three dimensions in drug development (FDA) |
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Definition
Safety
Medical utility
Industrialization |
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Definition
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| How many compounds does a certain drug usually start with? |
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Definition
-Basic research- 10s of mil
-Animal models- 10s of mill
-Clinical trials- 100s of mil
A drug needs to generate profit of 0.5 billion above cost of making and marketing drug |
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Definition
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| How long are drugs normally good for until they become ineffective from resistance? |
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Definition
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| Failure of drug in a patient |
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Definition
-Host: immune system, location (brain)
-Drug: cidal/static, oral/IV
-Pathogen: is it susceptible or resistant |
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Term
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Definition
| how much drug does it take to kill an organism? |
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