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Pharmacokinetics Flashcards

(74 cards)

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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
What is bulk flow in drug transfer?
movement of molecules through the capillary system
26
What is pinocytosis in drug transfer?
formation and movement of vesicles
27
Which drug transfer plays a MINOR role in drug transport across the membrane?
pinocytosis
28
What are the factors that influence drug ABSORPTION?
1. solubility 2. circulation 3. surface area 4. time 5. concentration
29
What are the processes of drug transfer?
1. passive diffusion 2. active transport 3. facilitated diffusion 4. bulk flow 5. pinocytosis
30
What can affect solubility?
pH
31
What type of injection is NOT fully absorbed?
intramuscular
32
"High conc. of drug preparations being absorbed more RAPIDLY" is the definition of which factor of drug absorption?
concentration
33
What is the affect of circulation on drug absorption?
increase circulation -> increase absorption ( heat application or local massage ) decrease circulation -> decrease absorption (state of shock or disease state)
34
What are the types of surface area that affect drug absorption?
1. intestinal mucosa 2. pulmonary alveolar epithelium 3. skin
35
Absorption is hard to take place unless it's....
HIGHLY hydrophobic
36
What is the first pass effect?
combined action of bacterial and liver enzymes on drugs BEFORE reaching systemic circulation
37
What is the significance of absorption?
1. liver is the main detox center 2. plasma compartment: is where the med goes where it's meant to be
38
Where does IV bypass absorption?
plasma compartment
39
What are the factors that influence drug absorption?
1. blood flow 2. lipid solubility of drug 3. molecular size 4. protein binding (reversible)
40
What is the purpose of blood flow in drug distribution?
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
What type of drug is restricted during drug distribution?
lipid soluble drugs
42
How does molecular size influence drug distribution?
extremely large drugs are mainly confined to the plasma compartment
43
How can protein binding influence drug distribution?
only unbound drugs cross the cell membrane
44
What do acidic drugs bind ?
serum albumin
45
What do basic drugs bind?
alpha-1 glycoprotein
46
How are plasma proteins drug reservoirs?
many drugs bind to plasma proteins
47
Binding with plasma proteins is predominantly what?
reversible
48
Fat acts as a drug reservoir for what type of drugs?
highly lipophilic drugs
49
How can bone be a drug reservoir?
drug can accumulate in bone by absorption onto bone-crystal surface and eventual incorporation into the lattice
50
How can a cellular reservoir be a drug reservoir?
drugs accumulate in the muscle or other cells at HIGHER conc. than in extracellular fluids
51
What type of cellular barrier is adaptive?
blood-brain barrier
52
Is placenta a barrier?
NO; fetus is exposed to ALL drugs taken by the mother
53
Drugs are enzymatically altered in the ... and excreted by the ....
liver; kidneys
54
Biotransformation has what affect on the water solubility of drugs?
increases
55
What can be a result of biotransformation?
1. inactive metabolite 2. metabolite with similar or altered activity 3. bioactivated metabolites
56
What is an inactive metabolite?
when the hydrolysis of procaine to p-aminobenzoic acid results in loss of anesthetic activity
57
What happens when a metabolite retains similar activity?
codeine is demethylated to the more active analgesic morphine
58
What happens when a metabolite has an altered activity?
vitamin A is isomerized to antiacne agent isoretinoic acid
59
What is the main characteristic of bioactivated metabolites?
prodrug: BEFORE drug
60
What occurs in the phase 1 reaction of biotransformations?
reactions are mainly degradative resulting in inactivation, change in activity, or conversion of a pharmacologically inactive compound to active drugs
61
What are the main reactions of phase 1?
oxidation, reduction, and hydrolysis
62
What occurs in the phase 2 reaction of biotransformations?
mainly involved in coupling of the drug or polar metabolite from phase 1 reaction to an endogenous substrate
63
Do phase 1 and 2 reactions have to happen in a specific order?
NO; interchangeable
64
What is the main reaction of phase 2?
conjugation
65
What is the main reaction of phase 1?
oxidation
66
What is the enzyme that is most responsible for oxidation reactions?
cytochrome P450 system
67
Where is the cytochrome P450 enzyme system found?
in microsomal fraction (smooth ER), liver, lung, and kidney
68
What are the 2 components of the cytochrome P450 system?
cytochrome P450 oxireductase and cytochrome P450
69
What enzyme requires molecular oxygen and NADPH?
cytochrome P450 system
70
What are the main reactions catalyzed by oxidation?
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
What are the 2 most important enzymes if the non-microsomal oxidation system?
1. alcohol dehydrogenase 2. aldehyde dehydrogenase
72
What are hydrolysis reactions carried out by?
1. esterases (acetylcholine, procaine) 2. amidases (lidocaine, procainamide) 3. peptidases
73
Where are hydrolysis enzymes found?
liver, plasma, GI tract
74
What can the enzymes responsible for reduction do?
catalyze the reduction of nitro group, azo, and carbonyl group

Pharmacology (5 decks)

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