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Pharmacology > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

What are the 3 parts of pharmacokinetics?

A

absorption, distribution, and elimination

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2
Q

What is absorption?

A

process where drugs enter systemic circulation

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3
Q

What is distribution?

A

where drugs reach the site of action; one part of the body to another

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4
Q

What type of method used has 100% absorption and can bypass absorption in organs?

A

IV

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5
Q

What happens during elimination?

A

drugs are enzymatically altered in the liver and excreted by the kidneys

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6
Q

Drugs must be …. to pass the membrane

A

hydrophobic

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7
Q

What are the factors of drug transfers across the membrane?

A
  1. molecular size and shape
  2. solubility
  3. weak acid/base
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8
Q

What form of a drug can readily cross the cell membrane?

A

non-ionized

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9
Q

What does the degree of ionization depend on?

A

pH

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10
Q

What is the formula to find the pH of a weak acid?

A

pH= pKa + log10 I/U

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11
Q

What is the formula to find the pH of a weak base?

A

pH= pKa + log10 U/I

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12
Q

Weak acids will be trapped on what side?

A

more basic

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13
Q

Weak bases will be trapped on what side?

A

more acidic

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14
Q

What is the most common process of drug transfer?

A

passive diffusion

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15
Q

How does passive diffusion affect conc. gradient?

A

moves down; high conc. to low conc.

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16
Q

How is the water partition coefficient affected with passive diffusion?

A

the faster the diffusion, the higher the water partition coefficient

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17
Q

Is passive diffusion saturable? Carrier mediated?

A

NO to both

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18
Q

What type of drug transfer process is the main transporter of drugs?

A

active transport

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19
Q

What type of drug transfer process need energy?

A

active transport

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20
Q

The drug can move …. the conc. gradient in active transport

A

up

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21
Q

Does active transport require a carrier? Can it be saturated?

A

YES to both

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22
Q

What is a xenobiotic?

A

foreign drug to body

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23
Q

In facilitated diffusion, drugs move … the conc. gradient

A

down

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24
Q

Does facilitated diffusion involve a carrier? Can be saturated?

A

YES to both

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25
Q

What is bulk flow in drug transfer?

A

movement of molecules through the capillary system

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26
Q

What is pinocytosis in drug transfer?

A

formation and movement of vesicles

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27
Q

Which drug transfer plays a MINOR role in drug transport across the membrane?

A

pinocytosis

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28
Q

What are the factors that influence drug ABSORPTION?

A
  1. solubility
  2. circulation
  3. surface area
  4. time
  5. concentration
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29
Q

What are the processes of drug transfer?

A
  1. passive diffusion
  2. active transport
  3. facilitated diffusion
  4. bulk flow
  5. pinocytosis
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30
Q

What can affect solubility?

A

pH

31
Q

What type of injection is NOT fully absorbed?

A

intramuscular

32
Q

“High conc. of drug preparations being absorbed more RAPIDLY” is the definition of which factor of drug absorption?

A

concentration

33
Q

What is the affect of circulation on drug absorption?

A

increase circulation -> increase absorption ( heat application or local massage )
decrease circulation -> decrease absorption (state of shock or disease state)

34
Q

What are the types of surface area that affect drug absorption?

A
  1. intestinal mucosa
  2. pulmonary alveolar epithelium
  3. skin
35
Q

Absorption is hard to take place unless it’s….

A

HIGHLY hydrophobic

36
Q

What is the first pass effect?

A

combined action of bacterial and liver enzymes on drugs BEFORE reaching systemic circulation

37
Q

What is the significance of absorption?

A
  1. liver is the main detox center
  2. plasma compartment: is where the med goes where it’s meant to be
38
Q

Where does IV bypass absorption?

A

plasma compartment

39
Q

What are the factors that influence drug absorption?

A
  1. blood flow
  2. lipid solubility of drug
  3. molecular size
  4. protein binding (reversible)
40
Q

What is the purpose of blood flow in drug distribution?

A
  1. most highly perfused organs receive MOST of the drug during first few minutes AFTER absorption
  2. delivery of drug to muscle, viscera, skin, and fat is SLOWER
41
Q

What type of drug is restricted during drug distribution?

A

lipid soluble drugs

42
Q

How does molecular size influence drug distribution?

A

extremely large drugs are mainly confined to the plasma compartment

43
Q

How can protein binding influence drug distribution?

A

only unbound drugs cross the cell membrane

44
Q

What do acidic drugs bind ?

A

serum albumin

45
Q

What do basic drugs bind?

A

alpha-1 glycoprotein

46
Q

How are plasma proteins drug reservoirs?

A

many drugs bind to plasma proteins

47
Q

Binding with plasma proteins is predominantly what?

A

reversible

48
Q

Fat acts as a drug reservoir for what type of drugs?

A

highly lipophilic drugs

49
Q

How can bone be a drug reservoir?

A

drug can accumulate in bone by absorption onto bone-crystal surface and eventual incorporation into the lattice

50
Q

How can a cellular reservoir be a drug reservoir?

A

drugs accumulate in the muscle or other cells at HIGHER conc. than in extracellular fluids

51
Q

What type of cellular barrier is adaptive?

A

blood-brain barrier

52
Q

Is placenta a barrier?

A

NO; fetus is exposed to ALL drugs taken by the mother

53
Q

Drugs are enzymatically altered in the … and excreted by the ….

A

liver; kidneys

54
Q

Biotransformation has what affect on the water solubility of drugs?

A

increases

55
Q

What can be a result of biotransformation?

A
  1. inactive metabolite
  2. metabolite with similar or altered activity
  3. bioactivated metabolites
56
Q

What is an inactive metabolite?

A

when the hydrolysis of procaine to p-aminobenzoic acid results in loss of anesthetic activity

57
Q

What happens when a metabolite retains similar activity?

A

codeine is demethylated to the more active analgesic morphine

58
Q

What happens when a metabolite has an altered activity?

A

vitamin A is isomerized to antiacne agent isoretinoic acid

59
Q

What is the main characteristic of bioactivated metabolites?

A

prodrug: BEFORE drug

60
Q

What occurs in the phase 1 reaction of biotransformations?

A

reactions are mainly degradative resulting in inactivation, change in activity, or conversion of a pharmacologically inactive compound to active drugs

61
Q

What are the main reactions of phase 1?

A

oxidation, reduction, and hydrolysis

62
Q

What occurs in the phase 2 reaction of biotransformations?

A

mainly involved in coupling of the drug or polar metabolite from phase 1 reaction to an endogenous substrate

63
Q

Do phase 1 and 2 reactions have to happen in a specific order?

A

NO; interchangeable

64
Q

What is the main reaction of phase 2?

A

conjugation

65
Q

What is the main reaction of phase 1?

A

oxidation

66
Q

What is the enzyme that is most responsible for oxidation reactions?

A

cytochrome P450 system

67
Q

Where is the cytochrome P450 enzyme system found?

A

in microsomal fraction (smooth ER), liver, lung, and kidney

68
Q

What are the 2 components of the cytochrome P450 system?

A

cytochrome P450 oxireductase and cytochrome P450

69
Q

What enzyme requires molecular oxygen and NADPH?

A

cytochrome P450 system

70
Q

What are the main reactions catalyzed by oxidation?

A
  1. dealkylation (N,O,S)
  2. hydroxylation (aromatic ring, side chain, N)
  3. sulfoxide formation
  4. N-oxidation
  5. deamination of primary and secondary amines
71
Q

What are the 2 most important enzymes if the non-microsomal oxidation system?

A
  1. alcohol dehydrogenase
  2. aldehyde dehydrogenase
72
Q

What are hydrolysis reactions carried out by?

A
  1. esterases (acetylcholine, procaine)
  2. amidases (lidocaine, procainamide)
  3. peptidases
73
Q

Where are hydrolysis enzymes found?

A

liver, plasma, GI tract

74
Q

What can the enzymes responsible for reduction do?

A

catalyze the reduction of nitro group, azo, and carbonyl group

Pharmacology (5 decks)

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