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

Lecture 3, 4, and 5 Flashcards

1
Q

PK?

A

Absorption, Distribution, and Elimination

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2
Q

All drugs are?

A

Toxic at high concentrations

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3
Q

Xenobiotics?

A

Substances that are foreign to the body

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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

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5
Q

Phase II Reactions are mainly involved in?

A

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

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6
Q

Conjugation (Phase II Reactions)?

A

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

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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

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8
Q

Conjugation (OH)?

A

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

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9
Q

Conjugation (CH2CH2NH2)?

A

-Acetylation

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10
Q

Pathological factors that alter liver function can?

A

Influence a drug’s hepatic clearance

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11
Q

Congestive Heart Failure (Inefficient pumping) can?

A

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

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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

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13
Q

Liver is the main site of?

A

Serum-Albumin production and drug biotransformation

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14
Q

If you have more acetylators it will?

A

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

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15
Q

As the drug dosage increase?

A

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

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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

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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)

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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

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19
Q

In older people metabolizing enzymes?

A

Decline

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20
Q

Liver develops faster?

A

More Biotransformation = Inactivates

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21
Q

First-Pass Effect?

A

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

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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

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23
Q

Cigarette smokers have lower?

A

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

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24
Q

Polycyclic aromatic hydrocarbon component of cigarette smoke appear to?

A

Induce the N-demethylation (Phase I) pathway

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25
Enzyme induction can produce a condition known as?
Pharmacokinetic Tolerance
25
Enzyme Inhibition?
Inhibit enzyme that breaks another drug down, therefore increases concentration
26
Phenytoin is increased by co-administration of?
Chloramphenicol
27
Phenytoin?
Controls seizures
28
Chloramphenicol?
Classic Enzyme Inhibitor, increases drug concentration
29
Some drugs can decrease the?
Metabolism of other drugs
30
Excretion?
-Milk -Pulmonary (excreted through lungs) -Can also be through sweat, saliva, and hair
31
Milk?
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)
32
Pulmonary?
-Excreted through lungs -Anesthetic gases -Alcohol
33
Clinical Pharmacokinetics?
Process of using drug concentration, pharmacokinetic principles, and pharmacodynamic criteria to optimize drug therapy in individual patients
34
Bioavailability?
Parameter that measure drug absorption
35
Bioavailability Factor?
-F -Percentage or fraction the dose, which reaches the systemic circulation
36
IV drug will have a bioavailability of?
100%
37
Apparent Volume of Distribution?
Proportionality constant that relates the amount of the drug in the body to the serum concentration (Parameter that measures distribution of the drug)
38
Clearance?
Represents the rate of drug removal
39
Half-Life?
Time it takes for the concentration of drug in the plasma to decrease by 50% (parameter that measures Drug Elimination)
40
Pharmacodynamics?
Study of the biochemical and physiological effect of drugs and their mechanism of action
41
Mechanisms of Action include?
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
Site of drug action is often at specific protein macromolecules, called?
Receptors
43
Most drug receptors have an?
Endogenous Ligand
44
Action of drug is interplay of?
Drug Concentration and Endogenous Ligand Concentration
45
Most drugs are NOT?
Covalent
46
Most drugs you want to be?
Reversible
47
No Ligand means?
Mostly Inactive
48
If you increase the concentration of agonist ligand the more chance it will?
Interact with receptor and stabilize it in the active form
49
General Mechanisms for Signal Transduction?
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
Ion Channels?
A. Ligand-Gated B. Voltage-Gated
51
Receptor coupled to G-proteins?
To regulate generation of intracellular second messengers: cAMP and Ca2+
52
Receptors with intrinsic enzyme activity?
Tyrosine kinases
53
Receptors that are internalized to deliver receptor-complexes to intracellular targets?
Steroids
54
Ligand-Gated?
Binding of the agonist to the receptor will open an integral gate allowing flow of ions across the membrane
55
Nicotinic Acetylcholine Receptors?
(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
Binding of the agonist (acetylcholine) will result in?
Opening of the pore allowing Na+ and K+ ions to go across the membrane (causes depolarization and firing AP)
57
GABAa receptors?
(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
Barbituarates and Benzodiazepines are examples of drugs which?
Modulate GABAa receptors
59
Types of Voltage-Gated Channels?
-Calcium -Potassium
60
Voltage-Gated Sodium Channels?
-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
Transient change in the voltage (membrane potential) across membrane triggers?
Opening of the gate allowing passage of Na+ ions across membrane
62
Local Anesthetics bind to the?
Intracellular domain of voltage-gated sodium channel
63
Receptor coupled to G-proteins?
-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
Contain 7 membrane-spanning domains?
Receptors coupled to G-proteins
65
Ligand-regulated transmembrane enzymes?
(Tyrosine Kinase receptors) -Have their own kinase activity (phosphorylate things) -Ex. insulin and epidermal growth factor receptors
66
Intracellular Receptors?
-Ex. Steroids (estrogen, androgen) receptors -High lipid: H2O partition coefficient -Lipid soluble -Can cross cell membrane
67
Lower EC50 means?
More potent drug (takes less of the drug to get to 50%)
67
As concentration of a drug in contact with a tissue increases?
Magnitude of the effect increases
68
KD of a drug?
Concentration that produces 1/2 the maximum binding
69
EC50 value for a response is often smaller than the?
KD value
70
Agonist?
Drug or Ligand that binds to the same site as the endogenous ligand and produces a signal
71
2 Main Categories of Agonists?
-Full Agonists -Partial Agonists
72
Full Agonists?
Have affinity only for active site (can produce the greatest maximal response)
73
Partial Agonists?
Have higher affinity only for active than inactive state, won't reach 100% (produces a response that is less than a full agonist)
74
Potency?
Measurement of the amount of a drug needed to produce a given effect
75
Used to differentiate between a series of compounds?
Potency
76
Efficacy or Intrinsic Activity describe?
Properties of drugs that bind to the same receptor site but do not produce equal maximum effects
77
Most efficacious agonist is defined as?
The drug that can produce the greatest maximum effect
78
Antagonist?
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
Molecules that inhibit the action of the agonist or receptor?
Antagonists
80
Do not initiate a response on their own?
Antagonists
81
Doesn't change equilibrium of active to inactive?
Antagonists
82
If the inhibition can be overcome by increasing the concentration of an agonist, the antagonist is said to be?
Competitive
83
Competitive Antagonists are?
Reversible (Reversible Antagonists)
84
Non-Competitive Antagonist prevent?
Agonist, at any concentration, from producing a maximum effect on a given receptor
85
Non-Competitive Antagonists are?
Irreversible (Irreversible Antagonists)
86
Inverse Agonist?
Reduce the constitutive activity of a receptor (have affinity only for inactive state and shift equilibrium)
87
Continuous or Repeated Exposure to an Agonist may?
Decrease the number of receptors
88
Continuous or Repeated Exposure to an Antagonist may?
Increase the number of receptors
89
Tachyphylaxis?
Pharmacodynamic Tolerance
90
Receptor desensitization and down regulation is often responsible for?
Pharmacodynamic tolerance in which increasing doses of drug are required to produce a given magnitude of effect
91
Spare Receptors?
Maximal apparent effect is achieved when a relatively small fraction of receptors are occupied (max effect with lowest number of receptors)
92
More receptors = ?
More chance agonist will find = full effect without occupying more receptors
93
Quantal Dose-Effect Curves?
Plots the number (percent) of individuals responding to the drug against dosage
94
Effects of drugs are often assessed by?
Their outcome on populations of individuals
95
ED50?
(Median Effective Dose) median effective dose that causes 50% of individuals to respond
96
LD50?
(Median Lethal Dose) median lethal dose that kills 50% of tested animals
97
TD50?
(Median Toxic Dose) dose that produces a toxic effect in 50% of individuals
98
Therapeutic Index?
99
For a drug to be safe you want the ratio of TD50 and ED50 to be?
Large, you want High TD50 and Low ED50
100
Continued Stimulation of a receptor with its agonists generally results in?
Desensitization

Block 1: Pharmacology (9 decks)

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