Lecture 18- Drug Developmetn Flashcards
Streptococcus and staphylococcus are gram negative/gram positive?
Gram positive
E. coli and salmonella are gram negative/gram positive?
Gram negative
Mycobacterium tuberculosis and spirochetes are ___ bacteria.
non-staining
Name two eukaryote parasites”
plasmodium which causes malaria, toxoplasma in cats
Name two eukaryotic fungi and molds
Candida and pneumocystis which causes pneumonia
Hep B and Herpes are which type of virus?
DNA virus
Hantavirus, polio, and the flu are which type of virus?
RNA virus
HIV iswhat type of virus?
retrovirus
Antibacterial drugs target what?
Antibacterial drugs target DNA replicationand unwinding.
The job of quinolones is to
Inhibit DNA from unwinding
The job of metronizadole is to
Bind and distort DNA
Which type of drugs target bacteria, yeasts, parasites,
living cells, but are usually not viral
Antibiotics
Is penicilin natural or synthetic? What about quinolones?
Penicilin is from common bread mold (natural), while quinolones are made (synthetic)
THe best activity against human cells is __x to __x above human activity against the pathogen.
100x to 1000x
Activity of drug against pathogen
versus
Activity of drug against human cells desribes the_____
Therapeutic index
You cannot use static and cidal drugs at the same time, T/F?
TRUE- one would inhibit and the other wouldn’t work
What are two ways drugs could be administered?
Oral or IV
Basic research in the __ stage is done with small molecules, genes, assays, drug targets
Drug discovery
Where is the ‘valley of death’ in drug development? How long of a stage is this?
Preclinical trials; 5-10 years
What is the issue with COVID drugs/trials?
time- becasuse existing drugs need to have later phases but we need them soon
Generic drugs can be cheap because… And where is the intended market?
Their patent expired; USA
Describe a human eukaryotic cell
Has a nucleus and other organelles in the cell
Some antimicrobials are __
Antibiotic
Which type of pathogen are drugs hardest to develop from?
Eukaryotic pathogens
Neuranimidase inhibitors are used for which pathogen drugs?
Flu drugs
Rifampiciin binds to an RNA polymerase which targets what stage?
Transcription (RNA produced from DNA)
When a cell membrane is targeted, what structures are important?
Lipids and polymyxins such as detergent
Vancomycin (last line of defense) interferes with ___
Cell wall integrity
Penicillin
Cephalosporins
Cephamycins interfere with
Cell wall synthesis
Low cost, low toxicity, low drug/drug
interactions, broad spectrum are the:
Macrolides, penicillins, tetracyclines
In vitro is grown in a
test tube
n vivo is grown in
Humans or animals
if a drug doesn’t work in vitro,
unlikely to be useful in vivo T/F?
True
TO understand a disease like cancer we need tyo consider at least two things:
Genetics and environment
Once we identify a target (which is usually?), we need to __ it.
A gene or protein target; validate (prove that inhibition will stop disease)
List 3 types of assays
enzyme, whole cell, fluorescent
High throughput screening (HTP)
Biotechnology is used to find a __ compound. What type of therapeutic index does ithave?
Lead; good
To improve a drug, we start with lead compound, and modify chemically how
Structure activity relation, stability, absorption, therapeutic index, pathogen penetration
What occurs inthe preclinical development stage?
Animal models, drug metabolism ,safety assessment, pharmacy, process chem
GxP protocols include
good lab practice, manufacturing practice, clinical and regulatory practice
Early tests ADMA/Tox stands for
Absorption, distribution to site, metabolism into active state, excretion, non toxic
Dose, dosing interval, infusion rate, serum concentration fall under what category?
Pharmacokinetics
COVID animal testing was on which animals?
mice/rats, golden jhamster, ferret/mink, pigs, monkeuy
How long is a patent good for ?>
20 years
A drug needs o generate profit of how much above the cost of making and marketing?
$1 billion
There has been no new __ since the 1970s
avatar
Vioxx has a lawsuit. What did it seek to treat?
Arthitis
Torcetrapib was to treat what? It was a pfizer lawsuit.
Cholesterol
