Chapter 10 - Preclinical Studies Flashcards

1
Q

What is the aim of preclinical pharmacological studies on a lead compound for a new drug?

A

To obtain data on the safety and effectiveness of the lead compound as a potential new drug.

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2
Q

_________ information in preclinical studies provides confidence about the drug’s safety.

A

Toxicity.

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3
Q

Pharmacological studies using animals are regulated under what guidelines?

A

Good Laboratory Practice

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4
Q

The random movement of molecules in fluid.

A

Diffusion

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5
Q

Equilibrium

A

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

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6
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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7
Q

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

A

Facilitated diffusion (Controlled by hormones or enzymes).

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8
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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9
Q

Involves the engulfing of fluids by a cell.

A

Pinocytosis

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10
Q

What is the most common way of administering a drug?

A

Oral.

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11
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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12
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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13
Q

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

A

Subcutaneous and intramuscular.

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14
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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15
Q

What do acid and basic drugs bind to in general?

A

Acid drugs bind to albumins and basic drugs to glycoproteins.

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16
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.

17
Q

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

A

Blood-brain barrier

18
Q

How can drugs be excreted from the body?

A

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

19
Q

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

A

True.

20
Q

Tumor-causing potential of a drug.

A

Carginogenicity

21
Q

Determines if the drug compound can induce mutations to genes.

A

Genotoxicity

22
Q

MRSD

A

Maximum Recommended Starting Dose

23
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).

24
Q

Most drugs that are administered to patients only contain APIs. True or False.

A

False.

25
Q

Drug molecules have to cross cell membranes to reach target sites in all routes of administration EXCEPT…

A

Intravenous Injection

26
Q

What characteristics affect a drug’s ability to permeate membranes?

A

Chemical composition, polarity, and size

27
Q

Lipid-soluble molecules are polar or non-polar?

A

Non-polar

28
Q

Lipid-soluble (non-polar) drugs can usually pass through cell membranes. True or False?

A

True.

29
Q

Polar drug molecules can cross cell membranes via carrier systems. True or False?

A

True.

30
Q

What is the primary pharmacokinetic factor determining the length of time it takes a drug to produce its effect?

A

Absorption

31
Q

Which is absorbed quicker by the stomach – weak acid drugs or weak basic drugs?

A

Weak acid drugs

32
Q

Which route of administration does NOT completely bypass the liver?

A

Rectal

33
Q

Why are intravenous drug dosages easier to control than drugs administered transdermally?

A

The entire dose is available in the bloodstream right away, to be distributed to the target site.

34
Q

What 3 factors affect a drug’s distribution to its target tissue?

A

The drug’s lipid-solubility, polarity, and the vascular nature of the target tissue