Chapter 10 - Preclinical Studies Flashcards
What is the aim of preclinical pharmacological studies on a lead compound for a new drug?
To obtain data on the safety and effectiveness of the lead compound as a potential new drug.
_________ information in preclinical studies provides confidence about the drug’s safety.
Toxicity.
Pharmacological studies using animals are regulated under what guidelines?
Good Laboratory Practice
The random movement of molecules in fluid.
Diffusion
Equilibrium
When equal numbers of molecules are crossing a cell membrane in both directions.
Polar molecules cannot penetrate cell membranes readily via passive diffusion and rely on other transport mechanisms. True or false?
True.
Name a type of diffusion that is faster than passive diffusion.
Facilitated diffusion (Controlled by hormones or enzymes).
What does active transport require?
Energy to drive the transportation of drugs against the concentration gradient, from low to high. The transportation rate depends on the availability of carriers and energy supply.
Involves the engulfing of fluids by a cell.
Pinocytosis
What is the most common way of administering a drug?
Oral.
What is first-pass metabolism?
When the liver metabolizes the drug, which leads to reduction in the availability of the drug for interaction with receptors.
How can drugs be administered to avoid first-pass metabolism?
Buccal and sublingual (absorbed between the gums and cheek and underneath the tongue).
Which administration methods are used to deliver protein-based drugs?
Subcutaneous and intramuscular.
What does a drugs distribution pattern depend on?
The binding of the drug to blood plasma protein molecules, the vascular nature of the tissue, and the diffusion of the drug.
What do acid and basic drugs bind to in general?
Acid drugs bind to albumins and basic drugs to glycoproteins.
Lipid-soluble drugs can cross the cell membrane more readily than polar drugs and move into the tissues to interact with receptors. True or false?
True.
The sheath of connective tissues surrounding the brain, the astrocytes, forming a barrier to passive diffusion for polar drugs.
Blood-brain barrier
How can drugs be excreted from the body?
Via the kidneys, lungs, skin, intestine, and colon.
Water-soluble drugs are cleared more quickly than lipid-soluble drugs. True or false?
True.
Tumor-causing potential of a drug.
Carginogenicity
Determines if the drug compound can induce mutations to genes.
Genotoxicity
MRSD
Maximum Recommended Starting Dose
NOAEL
No Observed Adverse Effect Level - The highest dose level that does not produce a significant increase in adverse effects. Converted to Human Equivalent Dose (HED).
Most drugs that are administered to patients only contain APIs. True or False.
False.
