Lecture 2- Pharmacokinetics Flashcards

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1
Q

Pharmacokinetics is

A

-A subfield of pharmacology
-Absorption, distribution, bio transformation and excretion of drugs
-Movement of drug to and from its site action

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2
Q

Factors that determine the movement of drugs to terminals

A

-How much gets there
-How fast it gets there
-How long it’s there

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3
Q

Factors affecting absorption

A

-Drug solubility
-Ionisation
-Blood circulation at the site of administration
-Surface area of the absorbing surface

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4
Q

What factors of absorption are determined by route of administration

A

-Blood circulation at site of administration
-Surface area of absorbing surface

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5
Q

What is PO

A

PreOral
Absorption through gastrointestinal tract (not mouth)

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6
Q

Routes that avoid 1st pass metabolism

A

-Nasal
-Sublingual
-Rectal
-Transdermal
-Pulmonary absorption

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7
Q

Levels of transmission

A

-Subcutaneous
-Intramuscular
-Intravenous

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8
Q

Where is the subcutaneous

A

Just below the skin

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9
Q

Where is the intramuscular level

A

In the muscle

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10
Q

Where’s the intravenous level

A

Just the spinal cord

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11
Q

Putting a drug in an oil solution can

A

Slow down the release of the drug

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12
Q

What is peak effect

A

Highest point of concentration in the blood

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13
Q

Drug peak concentration and half life vary by

A

Route of administration

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14
Q

Half life is

A

Time for plasma drug concentrations to fall to half of peak effect

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15
Q

Effects of route administration

A

-Amount of drug destroyed by 1st metabolism
-Blood circulation at the site of administration
-Surface area available for absorption
-Binding to inactive sites
-Number of cell layers to blood

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16
Q

Drug movement across membranes is a key factor influencing

A

The dose available at site of action

17
Q

Limiting factors of drug movement across membranes

A

-Size and shape of drug molecule
-Lipid solubility and ionisation

18
Q

Which reaches the brain first heroin or morphine

A

Heroin

19
Q

Drugs that are weak acids ionise more in

A

Basic (alkaline) environments (solvents)

20
Q

Drugs that are weak bases ionise more in

A

Acidic environments (solvents)

21
Q

The greater difference in environment and drug

A

The more ionised the drug is and less absorption

22
Q

To know whether a drug is lipid soluble, you have to know

A

-Whether it’s a weak acid or base
-Pka value
-Solution your putting it in

23
Q

What is ion trapping

A

Build up of a higher concentration of a chemical across a cell membrane due to the pka value of the chemical and difference of pH

24
Q

What is the blood brain barrier

A

Special barrier protecting the brain, molecules travel everywhere but the brain

25
Q

Brain areas outside the blood brain barrier

A

-Area postrema (vomiting center)
-Median eminence (hypothalamic hormones)

26
Q

Features of typical capillary membranes

A

-Made of endothelial cells
-Fenestration
-Pinocytotic vesicles
-Lipid soluble transport
-Intracellular cleft

27
Q

What can still diffuse through brain capillaries

A

Lipid soluble molecules such as psychoactive drugs

28
Q

Features of brain capillaries

A

-Made of endothelial cell
-Tight junction
-Surrounded by astrocytes

29
Q

Most of metabolism occurs in

A

The liver

30
Q

Inactivation usually due to

A

Metabolism

31
Q

What mechanism do psychoactive drugs most often move across cell membranes

A

Simple diffusion

32
Q

True or false Metabolites are always inactive

A

False

33
Q

True or false, there are sex differences in enzyme activity in the stomach

A

True

34
Q

True or false, metabolism usually reduces the solubility

A

True