GENERAL PRINCIPLES OF PHARMACOLOGY - PHARMACOKINETICS Flashcards

1
Q

Pharmacokinetics

A

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

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2
Q

What does “pharmacokinetics” include?

A
  • Drug biotransformation in the organism
  • Distribution of drugs in the organism
  • Excretion of substances
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3
Q

The main mechanism of most drugs absorption in GI tract is

A

Passive diffusion (lipid diffusion)

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4
Q

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

A

Hydrophilic substances

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5
Q

A hydrophilic medicinal agent has the following property

A

Low ability to penetrate through the cell membrane lipids.

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6
Q

What is implied by «active transport»?

A

Transport against concentration gradient

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7
Q

What does the term “bioavailability” mean?

A

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

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8
Q

The reasons determing bioavailability are

A

Extent of absorption and hepatic first-pass effect

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9
Q

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

A

Rectal

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10
Q

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

A

Oral

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11
Q

What is characteristic of the oral route?

A

Absorption depends on GI tract secretion and motor function.

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12
Q

Tick the feature of the sublingual route

A

Pretty fast absorption

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13
Q

Pick out the parenteral route of medicinal agent administration

A

Inhalation, IV.

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14
Q

Parenteral administration

A

Usually produces a more rapid response than oral administration

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15
Q

What is characteristic of the intramuscular route of drug administration?

A

Oily solutions can be injected

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16
Q

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

A

FALSE.

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17
Q

True or False. Intravenous administration provides a rapid response

A

TRUE

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18
Q

True or False. Intramuscular administration requires a sterile technique

A

TRUE

19
Q

True or False. Subcutaneous administration may cause local irritation

A

TRUE

20
Q

True or False. Most of drugs are distributed homogeneously.

A

FALSE

21
Q

Biological barriers include

A
  • Cell membranes
  • Capillary walls
  • Placenta
22
Q

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

A

Absence of pores in the brain capillary endothelium

23
Q

The volume of distribution (Vd) relates

A

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

24
Q

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

A

Concentration of a substance in plasma

25
Q

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.

A

FALSE

26
Q

The term “biotransformation” includes

A

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

27
Q

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

A

Lipid soluble

28
Q

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

A

TRUE

29
Q

Stimulation of liver microsomal enzymes can

A

Require the dose increase of some drugs.

30
Q

Metabolic transformation (phase 1) is

A

Transformation of substances due to oxidation, reduction or hydrolysis.

31
Q

Biotransformation of a medicinal substance results in

A

Faster urinary excretion.

32
Q

Conjugation

A

Coupling of a drug with an endogenous substrate

33
Q

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

A

Acetylation

34
Q

Conjugation of a drug includes

A
  • Glucoronidation
  • Sulfate formation
  • Methylation
35
Q

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

A

FALSE

36
Q

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

A

Enlarged

37
Q

Half life (t ½) is the time required to

A

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

38
Q

Half life (t ½) doesn’t depend on

A

Time of drug absorption

39
Q

Half life (t ½) depends on

A
  • Biotransformation
  • Concentration of a drug in plasma
  • Rate of drug elimination
40
Q

Elimination is expressed as

A

Clearance of an organism from a xenobiotic.

41
Q

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

A

Half life (t ½)

42
Q

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

A

TRUE

43
Q

Systemic clearance (CLs) is related with

A

Volume of distribution, half life and elimination rate constant.