Test 3 Flashcards

(66 cards)

1
Q

Why can’t lipophilic drugs be excreted by the kidney?

A

Liver converts lipophilic drugs to hydrophobic metabolites that can be easily excreted by the kidney.

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2
Q

What are xenobiotics?

A

Toxins, foreign/unwanted molecules

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3
Q

What are enzymes?

A

Proteins in nature, speeds up reaction

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4
Q

What is a co-enzyme?

A

Non-protien, helper

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5
Q

Is prodrug active or inactive?

A

Inactive

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6
Q

Hydrolase

A

Hydrolysis of substrate

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7
Q

Ligases

A

Bond formation

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8
Q

Transferases

A

Transfer of group between molecules

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9
Q

Lyases

A

Elimination and addition reaction

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10
Q

Isomerases

A

Rearrangement reactions

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11
Q

Oxidoreductases

A

Oxidation or reduction

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12
Q

Steps of drug metabolism in liver?

A
  1. Toxic substances are presented to liver via portal circulation
  2. Liver modifies these substances by “first pass metabolism”
  3. Phase 1 reactions are catalyzed by cytochrome P-450 enzymes
    • This includes oxidation, reduction, and hydrolysis
  4. Phase 2 reactions conjugate the substances. Once conjugated, the substance can be easily excreted.
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13
Q

What phase of drug metabolism is affected in old age?

A

Phases 1

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14
Q

What is intrinsic activity?

A

Drug’s ability to initiate response after binding to a receptor

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15
Q

What is an agonist?

A

Drug has an affinity for a receptor and stimulates it

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16
Q

What is an antagonist?

A

Drug has an affinity for a receptor but displays little or no intrinsic activity.

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17
Q

Two types of antagonist?

A

Competitive,non-competitive

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18
Q

Competitive Antagonist

A

Competes with agonist for receptor sites, occupies the receptor site = NO activity

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19
Q

Non-competitive antagonist

A

Binds to the site other than receptor site and changes the shape of receptor = NO activity

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20
Q

Phase 1 reaction

A

Oxidation, reduction, and hydrolysis

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21
Q

Phase 2 reactions

A

Conjugate the substances

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22
Q

Metabolic pathway

A

Sequence of chemical reactions

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23
Q

What happens during a metabolic pathway?

A
  • Each reaction is catalyzed by a different enzyme

- he product of one reaction serves as the substrate for the next

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24
Q

Enzyme activity is regulated and can be inhibited.

A

True

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25
How do feedback inhibition hinder metabolic pathways?
Inhibits an enzyme in the pathway so no product is available to feed the next reaction
26
How is drugs eliminated from plasma?
Urine/Bile, chemically converting to metabolites
27
What is pharmacodynamics?
What the drug does to the body
28
What is pharmacokinetics?
What the body does to the drug
29
What is a good indicator of pharmacokinetics?
Drug concentration in plasma
30
What affects the plasma level curve?
- route of administration | - ADME process
31
What is bioavailability?
A parameter that characterizes the extent of drug absorption from a product
32
What is the half life of a drug?
Time required for plasma drug concentration to decrease by one half of its value
33
How much plasma concentration is necessary for drug efficacy?
Minimum
34
What happens when you have a high concentration of a drug?
Toxicity
35
What is the therapeutic index?
Safety margin
36
Is a narrow therapeutic index safe or unsafe?
Unsafe
37
Is a wide therapeutic index safe or unsafe?
Safe
38
What is drug excretion?
Process by which a drug is eliminated from the body without any chemical change
39
What are ways of drug excretion?
Kidneys, saliva, bile, sweat, breast milk, exhaled air
40
What is the main form of excretion?
Kidneys
41
What are some functions of kidneys?
Water balance Remove waste Regulate electrolyte Regulate plasma pH
42
What are the structures of kidneys?
Nephron, Bowman's capsule, glomerular filtration, tubular reabsorption and excretion.
43
What is the structural unit of the kidney?
Nephron
44
What is the normal glomerular filtration rate?
120 mL/min
45
What happens when you decrease the GFR with kidney disease?
Decreases elimination of drugs
46
_______ __________ relates the rate of elimination of a drug to its plasma concentration.
Renal clearance
47
Is clearance the same with all drugs?
No
48
What is renal clearance?
Volume of plasma cleared of a substance per unit time
49
What is the unit time for renal clearance?
mL/min and mL/24hr
50
What happens to the drugs with the highest clearance?
They are filtered and secreted
51
What happens to drugs with the lowest clearance?
They are either not filtered -or- They are filtered and reabsorbed.
52
What happens when drugs are excreted by the liver?
Drug may be reabsorbed or excreted by bile and feces
53
What are capillaries for?
Exchange
54
What does the lymphatic system do?
Returns leaky fluid back to heart
55
How do you measure cardiac output?
Multiply heart rate by stroke volume
56
What is the stroke volume of the heart?
70 mL
57
What is the break down of blood?
Pic
58
What is the break down of total body weight?
Put diagram here
59
What does the rate of distribution depend on?
1. Type of capillary 2. Physiochemical properties of the drug 3. Blood flow 4. Binding of drug to plasma and tissue proteins
60
What form of drug can cross the cell membrane?
Unbound or free drugs
61
What are the types of Capillaries?
1. Continuous capillaries 2. Fenestrated capillaries 3. Discontinuous capillaries
62
What is the blood brain barrier?
Tight barrier formed by capillaries that lines the brain
63
Do meds pass the BBB?
No
64
What happens to the BBB during stroke and what can happen?
Broken up during stroke, high risk of dug poisoning
65
What is the formula for volume of distribution?
Put equation here
66
What is the total body water divided into?
Put pie chart here-ch 8