Chapter 10 - Preclinical Studies Flashcards

1
Q

What happens after a lead compound for a new drug has been identified?

A

It undergoes a development process to optimize it’s properties in regards to its effects on toxicity, carcinogenicity, mutagenicity, and reproductive development.

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2
Q

What does toxicity information in preclinical studies provide?

A

Confidence in the safety aspect of a potential drug.

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3
Q

What are pharmacological studies with animals regulated under?

A

Good Laboratory Practice

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4
Q

Name the methods by which drugs can be administered.

A

Intravenous, oral, buccal, sublingual, rectal, rectal, subcutaneous, intramuscular, transdermal, topical, and inhalation.

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5
Q

Diffusion

A

The random movement of molecules in fluid.

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6
Q

Equilibrium

A

When equal numbers of molecules are crossing a cell membrane in both directions.

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7
Q

Polar molecules cannot penetrate cell membranes readily via passive diffusion and rely on other transport mechanisms. True or false?

A

True.

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8
Q

Name a type of diffusion that is faster than passive diffusion.

A

Facilitated diffusion (Controlled by hormones or enzymes).

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9
Q

What does active transport require?

A

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.

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10
Q

Pinocytosis

A

Involves the engulfing of fluids by a cell.

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11
Q

What is the most common way of administering a drug?

A

Oral.

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12
Q

What is first-pass metabolism?

A

When the liver metabolizes the drug, which leads to reduction in the availability of the drug for interaction with receptors.

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13
Q

How can drugs be administered to avoid first-pass metabolism?

A

Buccal and sublingual (absorbed between the gums and cheek and underneath the tongue).

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14
Q

Which administration methods are used to deliver protein-based drugs?

A

Subcutaneous and intramuscular.

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15
Q

What does a drugs distribution pattern depend on?

A

The binding of the drug to blood plasma protein molecules, the vascular nature of the tissue, and the diffusion of the drug.

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16
Q

What do acid and basic drugs bind to in general?

A

Acid drugs bind to albumins and basic drugs to glycoproteins.

17
Q

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?

A

True.

18
Q

Blood-brain barrier

A

The sheath of connective tissues surrounding the brain, the astrocytes, forming a barrier to passive diffusion for polar drugs.

19
Q

How can drugs be excreted from the body?

A

Via the kidneys, lungs, skin, intestine, and colon.

20
Q

Water-soluble drugs are cleared more quickly than lipid-soluble drugs. True or false?

A

True.

21
Q

Carginogenicity

A

Tumor-causing potential of a drug.

22
Q

Genotoxicity

A

Determines if the drug compound can induce mutations to genes.

23
Q

MRSD

A

Maximum Recommended Starting Dose

24
Q

NOAEL

A

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).