GENERAL PRINCIPLES OF PHARMACOLOGY - PHARMACOKINETICS

Question 1

Pharmacokinetics

Answer 1

The study of absorption, distribution, metabolism and excretion of drugs.

Question 2

What does “pharmacokinetics” include?

Answer 2

• Drug biotransformation in the organism
• Distribution of drugs in the organism
• Excretion of substances

Question 3

The main mechanism of most drugs absorption in GI tract is

Answer 3

Passive diffusion (lipid diffusion)

Question 4

What kind of substances can’t permeate membranes by passive diffusion?

Answer 4

Hydrophilic substances

Question 5

A hydrophilic medicinal agent has the following property

Answer 5

Low ability to penetrate through the cell membrane lipids.

Question 6

What is implied by «active transport»?

Answer 6

Transport against concentration gradient

Question 7

What does the term “bioavailability” mean?

Answer 7

Fraction of an uncharged drug reaching the systemic circulation following any route administration.

Question 8

The reasons determing bioavailability are

Answer 8

Extent of absorption and hepatic first-pass effect

Question 9

Pick out the appropriate alimentary route of administration when passage of drugs through liver is minimized

Answer 9

Rectal

Question 10

Which route of drug administration is most likely to lead to the first-pass effect?

Answer 10

Oral

Question 11

What is characteristic of the oral route?

Answer 11

Absorption depends on GI tract secretion and motor function.

Question 12

Tick the feature of the sublingual route

Answer 12

Pretty fast absorption

Question 13

Pick out the parenteral route of medicinal agent administration

Answer 13

Inhalation, IV.

Question 14

Parenteral administration

Answer 14

Usually produces a more rapid response than oral administration

Question 15

What is characteristic of the intramuscular route of drug administration?

Answer 15

Oily solutions can be injected

Question 16

True or False. Intravenous injections are more suitable for oily solutions.

Answer 16

FALSE.

Question 17

True or False. Intravenous administration provides a rapid response

Answer 17

TRUE

Question 18

True or False. Intramuscular administration requires a sterile technique

Answer 18

TRUE

Question 19

True or False. Subcutaneous administration may cause local irritation

Answer 19

TRUE

Question 20

True or False. Most of drugs are distributed homogeneously.

Answer 20

FALSE

Question 21

Biological barriers include

Answer 21

• Cell membranes
• Capillary walls
• Placenta

Question 22

What is the reason of complicated penetration of some drugs through brain-blood barrier?

Answer 22

Absence of pores in the brain capillary endothelium

Question 23

The volume of distribution (Vd) relates

Answer 23

The amount of a drug in the body to the concentration of a drug in plasma.

Question 24

For the calculation of the volume of distribution (Vd) one must take into account

Answer 24

Concentration of a substance in plasma

Question 25

True or False. Small amount of the volume of distribution is common for lipophylic substances easy penetrating through barriers and widely distributing in plasma, interstitial and cell fluids.

Answer 25

FALSE

Question 26

The term “biotransformation” includes

Answer 26

Process of physicochemical and biochemical alteration of a drug in the body.

Question 27

Tick the drug type for which microsomal oxidation is the most prominent

Answer 27

Lipid soluble

Question 28

True or False. Microsomal oxidation results in an increase of ionization and water solubility of a drug

Answer 28

TRUE

Question 29

Stimulation of liver microsomal enzymes can

Answer 29

Require the dose increase of some drugs.

Question 30

Metabolic transformation (phase 1) is

Answer 30

Transformation of substances due to oxidation, reduction or hydrolysis.

Question 31

Biotransformation of a medicinal substance results in

Answer 31

Faster urinary excretion.

Question 32

Conjugation

Answer 32

Coupling of a drug with an endogenous substrate

Question 33

Which of the following processes proceeds in the second phase of biotransformation

Answer 33

Acetylation

Question 34

Conjugation of a drug includes

Answer 34

- Glucoronidation - Sulfate formation - Methylation

Question 35

True or False. Metabolic transformation and conjugation usually results in an increase of a substance biological activity

Answer 35

FALSE

Question 36

In case of liver disorders accompanied by a decline in microsomal enzyme activity the duration of action of some drugs is

Answer 36

Enlarged

Question 37

Half life (t ½) is the time required to

Answer 37

Change the amount of a drug in plasma by half during elimination.

Question 38

Half life (t ½) doesn’t depend on

Answer 38

Time of drug absorption

Question 39

Half life (t ½) depends on

Answer 39

- Biotransformation - Concentration of a drug in plasma - Rate of drug elimination

Question 40

Elimination is expressed as

Answer 40

Clearance of an organism from a xenobiotic.

Question 41

Elimination rate constant (Kelim) is defined by the following parameter

Answer 41

Half life (t ½)

Question 42

True or False. The most rapid eliminated drugs are those with high glomerular filtration rate and actively secreted but aren’t passively reabsorbed

Answer 42

TRUE

Question 43

Systemic clearance (CLs) is related with

Answer 43

Volume of distribution, half life and elimination rate constant.