Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Block 1: Pharmacology > Lecture 3, 4, and 5 > Flashcards

Lecture 3, 4, and 5 Flashcards

1
Q

PK?

A

Absorption, Distribution, and Elimination

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

All drugs are?

A

Toxic at high concentrations

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Xenobiotics?

A

Substances that are foreign to the body

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Conjugation?

A

-Phase II Reaction
-Mainly involved in coupling of the drug, or frequently its polar metabolite from Phase I reaction using enzymes known as transferases to an endogenous substrate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Phase II Reactions are mainly involved in?

A

Coupling of the drug, or frequently its polar metabolite from Phase I reaction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Conjugation (Phase II Reactions)?

A

-Sulfate (“Sulfatation”) (ex. minoxidil)
-Acetyl (“Acetylation”)
-Methyl (“Methylation”)
-Glutathione, Glycine (Amino Acids)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Most conjugates are?

A

Highly polar (water soluble) and unable to cross plasma membrane, making them almost always pharmacologically inactive and of little or no toxicity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Conjugation (OH)?

A

-Glucoronidation
-Methylation
-Acetylation
-Sulfatation
-GSH (reduced glutathione0
-Amino Acids

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Conjugation (CH2CH2NH2)?

A

-Acetylation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Pathological factors that alter liver function can?

A

Influence a drug’s hepatic clearance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Congestive Heart Failure (Inefficient pumping) can?

A

-Decrease hepatic blood flow and distribution of drugs
-No Blood Pumping

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Alteration in albumin production can?

A

-Alter ratio of bound to unbound drug
-Means you do not have the carrier for the drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Liver is the main site of?

A

Serum-Albumin production and drug biotransformation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

If you have more acetylators it will?

A

Break down the drug faster so you will need a higher dose

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

As the drug dosage increase?

A

Drug concentration may saturate the metabolic enzyme (ex. acetaminophen)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

If Phase II enzymes are saturated?

A

-It gets metabolized by CYP450 enzymes
-Can lead to an Intermediate that causes Hepatic Cell Death

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

In young children, particularly in infants drugs may be?

A

More active, this is due to lack of complete development of some Phase I and Phase II enzymatic system (and not fully developed BBB and Kidneys)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

In older children, some drugs may be?

A

-Less active than in adults, if the drug is given based on weight
-Liver develops faster than the general increase in body weight

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

In older people metabolizing enzymes?

A

Decline

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Liver develops faster?

A

More Biotransformation = Inactivates

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

First-Pass Effect?

A

Combined action of bacterial enzyme within intestine and liver on the drug taken orally

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Drugs such as Phenobarbital and Rifampin appear to act as?

A

Enzyme inducers by increasing the synthesis or decreasing the degradation of certain drug metabolizing enzymes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Cigarette smokers have lower?

A

Plasma level of drugs such as theophylline, than non-smokers

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Polycyclic aromatic hydrocarbon component of cigarette smoke appear to?

A

Induce the N-demethylation (Phase I) pathway

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Enzyme induction can produce a condition known as?

A

Pharmacokinetic Tolerance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Enzyme Inhibition?

A

Inhibit enzyme that breaks another drug down, therefore increases concentration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Phenytoin is increased by co-administration of?

A

Chloramphenicol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Phenytoin?

A

Controls seizures

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Chloramphenicol?

A

Classic Enzyme Inhibitor, increases drug concentration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

Some drugs can decrease the?

A

Metabolism of other drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

Excretion?

A

-Milk
-Pulmonary (excreted through lungs)
-Can also be through sweat, saliva, and hair

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

Milk?

A

Important for nursing infant and as a residue in dairy products (Milk is slightly acid compared to plasma, a basic drug will get trapped in the milk)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

Pulmonary?

A

-Excreted through lungs
-Anesthetic gases
-Alcohol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

Clinical Pharmacokinetics?

A

Process of using drug concentration, pharmacokinetic principles, and pharmacodynamic criteria to optimize drug therapy in individual patients

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

Bioavailability?

A

Parameter that measure drug absorption

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

Bioavailability Factor?

A

-F
-Percentage or fraction the dose, which reaches the systemic circulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

IV drug will have a bioavailability of?

A

100%

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

Apparent Volume of Distribution?

A

Proportionality constant that relates the amount of the drug in the body to the serum concentration (Parameter that measures distribution of the drug)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

Clearance?

A

Represents the rate of drug removal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

Half-Life?

A

Time it takes for the concentration of drug in the plasma to decrease by 50% (parameter that measures Drug Elimination)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

Pharmacodynamics?

A

Study of the biochemical and physiological effect of drugs and their mechanism of action

41
Q

Mechanisms of Action include?

A

Initial interactions between drug and cellular macromolecules (receptors), and the consequent biochemical and physiological responses that lead to the ultimate effects of the drug on the body

42
Q

Site of drug action is often at specific protein macromolecules, called?

A

Receptors

43
Q

Most drug receptors have an?

A

Endogenous Ligand

44
Q

Action of drug is interplay of?

A

Drug Concentration and Endogenous Ligand Concentration

45
Q

Most drugs are NOT?

A

Covalent

46
Q

Most drugs you want to be?

A

Reversible

47
Q

No Ligand means?

A

Mostly Inactive

48
Q

If you increase the concentration of agonist ligand the more chance it will?

A

Interact with receptor and stabilize it in the active form

49
Q

General Mechanisms for Signal Transduction?

A

1) Ion Channels
2) Receptor coupled to G-proteins
3) Receptors with intrinsic enzyme activity
4) Receptors that are internalized to deliver receptor-complexes to intracellular targets

50
Q

Ion Channels?

A

A. Ligand-Gated
B. Voltage-Gated

51
Q

Receptor coupled to G-proteins?

A

To regulate generation of intracellular second messengers: cAMP and Ca2+

52
Q

Receptors with intrinsic enzyme activity?

A

Tyrosine kinases

53
Q

Receptors that are internalized to deliver receptor-complexes to intracellular targets?

A

Steroids

54
Q

Ligand-Gated?

A

Binding of the agonist to the receptor will open an integral gate allowing flow of ions across the membrane

55
Q

Nicotinic Acetylcholine Receptors?

A

(Excitatory)
-Found on muscle cell: in the neuromuscular junction and also in the CNS/PNS
-Made of 5 subunits, Every subunit snakes through the membrane 4 times (these subunits are highly homologous)

56
Q

Binding of the agonist (acetylcholine) will result in?

A

Opening of the pore allowing Na+ and K+ ions to go across the membrane (causes depolarization and firing AP)

57
Q

GABAa receptors?

A

(Main Ligand-Gated Ion Channel in CNS)
-Binding of the agonist (GABA) will result in the opening of the pore allowing Cl- ions to flow across the membrane

58
Q

Barbituarates and Benzodiazepines are examples of drugs which?

A

Modulate GABAa receptors

59
Q

Types of Voltage-Gated Channels?

A

-Calcium
-Potassium

60
Q

Voltage-Gated Sodium Channels?

A

-Present in the membrane of excitable nerve, cardiac and skeletal muscle cells
-Transient change in the voltage (membrane potential) across membrane triggers opening of the gate allowing passage of Na+ ions across membrane

61
Q

Transient change in the voltage (membrane potential) across membrane triggers?

A

Opening of the gate allowing passage of Na+ ions across membrane

62
Q

Local Anesthetics bind to the?

A

Intracellular domain of voltage-gated sodium channel

63
Q

Receptor coupled to G-proteins?

A

-To regulate generation of intracellular second messengers
-Have in excess of 500 different members including receptors fro light, odorants, hormones, neurotransmitters and other endogenous ligands

64
Q

Contain 7 membrane-spanning domains?

A

Receptors coupled to G-proteins

65
Q

Ligand-regulated transmembrane enzymes?

A

(Tyrosine Kinase receptors)
-Have their own kinase activity (phosphorylate things)
-Ex. insulin and epidermal growth factor receptors

66
Q

Intracellular Receptors?

A

-Ex. Steroids (estrogen, androgen) receptors
-High lipid: H2O partition coefficient
-Lipid soluble
-Can cross cell membrane

67
Q

Lower EC50 means?

A

More potent drug (takes less of the drug to get to 50%)

67
Q

As concentration of a drug in contact with a tissue increases?

A

Magnitude of the effect increases

68
Q

KD of a drug?

A

Concentration that produces 1/2 the maximum binding

69
Q

EC50 value for a response is often smaller than the?

A

KD value

70
Q

Agonist?

A

Drug or Ligand that binds to the same site as the endogenous ligand and produces a signal

71
Q

2 Main Categories of Agonists?

A

-Full Agonists
-Partial Agonists

72
Q

Full Agonists?

A

Have affinity only for active site (can produce the greatest maximal response)

73
Q

Partial Agonists?

A

Have higher affinity only for active than inactive state, won’t reach 100% (produces a response that is less than a full agonist)

74
Q

Potency?

A

Measurement of the amount of a drug needed to produce a given effect

75
Q

Used to differentiate between a series of compounds?

A

Potency

76
Q

Efficacy or Intrinsic Activity describe?

A

Properties of drugs that bind to the same receptor site but do not produce equal maximum effects

77
Q

Most efficacious agonist is defined as?

A

The drug that can produce the greatest maximum effect

78
Q

Antagonist?

A

A drug that binds to the site used by the endogenous ligand (or a separate site) and diminishes or blocks the signal produced by the endogenous ligand

79
Q

Molecules that inhibit the action of the agonist or receptor?

A

Antagonists

80
Q

Do not initiate a response on their own?

A

Antagonists

81
Q

Doesn’t change equilibrium of active to inactive?

A

Antagonists

82
Q

If the inhibition can be overcome by increasing the concentration of an agonist, the antagonist is said to be?

A

Competitive

83
Q

Competitive Antagonists are?

A

Reversible (Reversible Antagonists)

84
Q

Non-Competitive Antagonist prevent?

A

Agonist, at any concentration, from producing a maximum effect on a given receptor

85
Q

Non-Competitive Antagonists are?

A

Irreversible (Irreversible Antagonists)

86
Q

Inverse Agonist?

A

Reduce the constitutive activity of a receptor (have affinity only for inactive state and shift equilibrium)

87
Q

Continuous or Repeated Exposure to an Agonist may?

A

Decrease the number of receptors

88
Q

Continuous or Repeated Exposure to an Antagonist may?

A

Increase the number of receptors

89
Q

Tachyphylaxis?

A

Pharmacodynamic Tolerance

90
Q

Receptor desensitization and down regulation is often responsible for?

A

Pharmacodynamic tolerance in which increasing doses of drug are required to produce a given magnitude of effect

91
Q

Spare Receptors?

A

Maximal apparent effect is achieved when a relatively small fraction of receptors are occupied (max effect with lowest number of receptors)

92
Q

More receptors = ?

A

More chance agonist will find = full effect without occupying more receptors

93
Q

Quantal Dose-Effect Curves?

A

Plots the number (percent) of individuals responding to the drug against dosage

94
Q

Effects of drugs are often assessed by?

A

Their outcome on populations of individuals

95
Q

ED50?

A

(Median Effective Dose) median effective dose that causes 50% of individuals to respond

96
Q

LD50?

A

(Median Lethal Dose) median lethal dose that kills 50% of tested animals

97
Q

TD50?

A

(Median Toxic Dose) dose that produces a toxic effect in 50% of individuals

98
Q

Therapeutic Index?

A
99
Q

For a drug to be safe you want the ratio of TD50 and ED50 to be?

A

Large, you want High TD50 and Low ED50

100
Q

Continued Stimulation of a receptor with its agonists generally results in?

A

Desensitization

Block 1: Pharmacology (9 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions