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Pharma > Lecture 4 > Flashcards

Lecture 4 Flashcards

1
Q

The study of the biochemical and physiological effects of drugs, in certain period is called ?

A

Pharmacodynamics

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2
Q

Give me another definition of Pharmacodynamics :

A

What the drug does to the body.

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3
Q

Pharmacodynamics have 4 stages , mention them :

A
  1. Drug receptors
  2. Effects of drug
  3. Responses to drugs
  4. Toxicity and adverse effects of drugs
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4
Q

Describe the pharmacodynamics in 2 points :

A

1- The actions of a drug on the body .
2- The influence of drug concentrations on the magnitude of the response .

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5
Q

Most drugs exert their effects, both beneficial and harmful, by ?

A

Interacting with receptors

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6
Q

The specialized target macromolecules that present on the cell surface or within the cell is ?

A

Receptors

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7
Q

The drug–receptor complex initiates alterations in biochemical and/or molecular activity of a cell by a process called ?

A

Signal transduction

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8
Q

Unoccupied receptor does influence intracellular processes . (T/F) ?

A

F—>( does not)

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9
Q

Receptor is actived . This sentence can be true if :

A

If the receptor is linked with the agonist

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10
Q

Drugs can act through three methods , mention them :

A
  1. Physical action
  2. Simple chemical reaction
  3. Receptors
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11
Q

Binding to different receptors and causing a biological response. This statement describe any method ?

A

Receptors

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12
Q

Drug can produce a therapeutic response because of it’s physical properties. Give me example to describe this statement :

A

Mannitol as diuretic because it increase osmalerity.

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13
Q

Drug may act through a chemical reaction . Give me examples to explain this statement :

A

1- Gastric antacids work by neutralizing the stomach acidity with a base
2- Chelating agents that bind heavy metals in body.

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14
Q

Drugs act as ……….., and their receptors act as ………… .

A

1- signals
2- signal detectors

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15
Q

How the receptor transduce their recognition of a bound “agonist” ?

A

By initiating a series of reactions that ultimately result in a specific intracellular response.

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16
Q

• “agonist” refers to ?

A

Naturally occurring small molecule or a drug that binds to a site on a receptor protein and activates it .

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17
Q

The part of the cascade of events that (( translates )) agonist binding into a cellular response named as ?

A

((Second messenger)) or effector molecules .

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18
Q

Cells have many different types of receptors, each of which is specific for a particular agonist and produces a same response .
(T/F) ?

A

F—> (produces a unique response) . 🌚

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19
Q

Cells have many different types of receptors, each of which is specific for a particular agonist and produces a unique response. Explain this statement with an example :

A

• Cardiac cell membranes, for example, contain β receptors that bind and respond to epinephrine or norepinephrine, as well as muscarinic receptors specific for acetylcholine.

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20
Q

What is the importance of having a different receptor populations ?

A

To control the organ vital functions.

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21
Q

The magnitude of the response is proportional to the number of drug–receptor complexes. (T/F) ?

A

True

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22
Q

These interactions have many common features , mention the most important one :

A

Specificity of the receptor for a given agonist.

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23
Q

How most receptors are named ?

A

For the type of agonist that interacts best with it (the receptor for histamine is called a histamine receptor).

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24
Q

Receptors exist in at least two states , mention them :

A

1- inactive (R)
2- active (R*)

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25
Q

The state that usually favouring is ?

A

Inactive state.

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26
Q

Binding of agonists causes ?

A

The equilibrium to shift from R to R* to produce a biologic effect.

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27
Q

…………… occupy the receptor but do not increase the fraction of R* and may stabilize the receptor in the inactive state.

A

Antagonists

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28
Q

Some drugs cause similar shifts in equilibrium from R to R* , but the fraction of R* is less than that caused by an agonist (but still more than that caused by an antagonist) named as ?

A

Partial agonists

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29
Q

The magnitude of biological effect is directly related to the fraction of R . (T/F) ?

A

F —>(R*) 😊

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30
Q

Agonists, antagonists, and partial agonists are examples of ?

A

Ligands, or molecules that bind to the activation site on the receptor

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31
Q

enzymes, nucleic acids, and structural proteins can act as receptors for drugs or endogenous agonists. (T/F) ?

A

True

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32
Q

The richest sources of therapeutically relevant pharmacologic receptors are ?

A

Proteins

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33
Q

The function of protein receptors is ?

A

Transduce extracellular signals into intracellular responses.

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34
Q

These receptors may be divided into four families , mention them:

A

1) ligand-gated ion channels,
2) G protein–coupled receptors,
3) enzyme-linked receptors, and
4) Intracellular receptors .

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35
Q

All drugs exert their effects, both beneficial and harmful, by interacting with receptors .
(T/F) ?

A

F—> (most not all)

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36
Q

The type of receptor a ligand interacts with depends on ?

A

The chemical nature of the ligand.

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37
Q

Hydrophobic ligands interact with receptors that are found on the cell surface . In contrast, hydrophilic ligands enter cells through the lipid bilayers of the cell membrane to interact with receptors found inside cells .
(T/F)

A

F —> (“Hydrophilic” ligands interact with receptors that are found on the cell surface .
In contrast, “hydrophobic” ligands enter cells through the lipid bilayers of the cell membrane to interact with receptors found inside cells) 🌚

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38
Q

The extracellular portion of ligand-gated ion channels usually contains ?

A

Ligand binding site.

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39
Q

The function of ligand binding site is ?

A

Regulates the shape of the pore through which ions can flow across cell membranes

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40
Q

The channel is usually closed until the receptor is activated by an ………. , which opens the channel briefly for a few………. .

A

1- agonist
2- milliseconds

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41
Q

the receptor of ligand-gated ion channels have diverse functions , including ………..…………. .

A

neurotransmission, and cardiac or muscle contraction.

42
Q

Voltage-gated ion channels can’t possess ligand-binding sites .
(T/F)

A

F —> (Voltage-gated ion channels may also possess ligand-binding sites that can regulate channel function)

43
Q

Now, give me three examples about transmembrane ligand-gated ion channels :

A
  1. stimulation of the nicotinic receptor by acetylcholine results in sodium influx and potassium outflux, generating an action potential in a neuron or contraction in skeletal muscle.
  2. agonist stimulation of the γ-aminobutyric acid (GABA) receptor increases chloride influx and hyperpolarization of neurons.
  3. local anesthetics bind to the voltage-gated sodium channel, inhibiting sodium influx and decreasing neuronal conduction.
44
Q

The extracellular domain of this receptor contains the ligand-binding area, and the intracellular domain interacts (when activated) with a G protein or effector molecule. This sentence describe any method ?

A

Transmembrane G protein–coupled receptors

45
Q

Intracellular domain interacts with a G protein or effector molecule in any condition . (T/F)

A

F—>(the intracellular domain interacts (when activated) with a G protein or effector molecule) .

46
Q

There are many kinds of G proteins , give me three examples of these kinds :

A

Gs, Gi, and Gq

47
Q

G proteins ‏composed of three protein subunits , mention them ?

A
  • The α subunit binds guanosine triphosphate (GTP) .
  • β and γ subunits anchor the G protein in the cell membrane .
48
Q

Transmembrane G protein–coupled receptors take about ?

A

several seconds to minutes.

49
Q

Sometimes, the activated effectors produce ……..
……….. that further activate other effectors in the cell, causing a signal cascade effect.

A

second messengers

50
Q

Mention the reason that causing dissociation of the α-GTP complex from the βγ complex.

A

Binding of an agonist to the receptor increases GTP binding to the α subunit .

51
Q

“These two complexes” !! In this sentence, the doctor means in two complex ? 😊

A

GTP & α subunit

52
Q

These two complexes can then interact with other cellular effectors, usually an ………………., that are responsible for further actions within the cell

A

enzyme, a protein, or an ion channel

53
Q

The function of adenylyl cyclase is ?

A

produces the second messenger cyclic adenosine monophosphate (cAMP)

54
Q

A common effector, activated by…… and inhibited by……. , is adenylyl cyclase

A
  1. Gs
  2. Gi
55
Q

Gq activates ?

A

phospholipase C

56
Q

What happens when Gq activates phospholipase C ?

A

Generating two other second messengers: inositol 1,4,5-trisphosphate (IP3) and diacylglycerol (DAG).

57
Q

The function of DAG and cAMP is ?

A

activate different protein kinases within the cell, leading to a myriad of physiological effects.

58
Q

The function of IP3 is ?

A

regulates intracellular free calcium concentrations, as well as some protein kinases.

59
Q

This family of receptors consists of a protein that may form dimers or multisubunit complexes is called ?

A

Enzyme-linked receptors

60
Q

What happens when Enzyme-linked receptors activated ?

A

These receptors undergo conformational changes resulting in increased cytosolic enzyme activity, depending on their structure and function .

61
Q

Enzyme-linked receptors take about ?

A

minutes to hours.

62
Q

Mention the most common enzyme linked receptors :

A

A. epidermal growth factor, B. platelet-derived growth factor,
C. atrial natriuretic peptide,
D. insulin, and
E. others

63
Q

The most common enzyme linked receptors (epidermal growth factor, platelet-derived growth factor, atrial natriuretic peptide, insulin, and others) possess tyrosine kinase activity as part of their structure.(T/F)?

A

True

64
Q

The activated receptor phosphorylates tyrosine residues on other specific proteins and then itself . (T/F) ?

A

F —> (The activated receptor phosphorylates tyrosine residues on itself and then other specific proteins) .

65
Q

Phosphorylation can substantially modify the structure of the target protein, thereby acting as a molecular switch. Give me example to explain this statement :

A

When the peptide hormone insulin binds to two of its receptor subunits, their intrinsic tyrosine kinase activity causes autophosphorylation of the receptor itself.

66
Q

The phosphorylated receptor phosphorylates other peptides or proteins that subsequently activate other important cellular signals , result to :

A

cascade of activations results in a multiplication of the initial signal, much like that with G protein–coupled receptors.

67
Q

The receptor is entirely intracellular, and, therefore, the ligand must diffuse into the cell to interact with the receptor. This method called ?

A

Intracellular receptors

68
Q

What the ligand need in order to move across the target cell membrane ?

A

The ligand must have sufficient lipid solubility.

69
Q

The primary targets of these ligand–receptor complexes are ?

A

Transcription factors in the cell nucleus.

70
Q

Binding of the ligand with its receptor generally activates the receptor via ?

A

Dissociation from a variety of binding proteins.

71
Q

The activated ligand–receptor complex then translocates to the …………

A

Nucleus

72
Q

The activated ligand–receptor complex dimerizes before binding to transcription factors that regulate gene expression . This process happens when?

A

The activated ligand–receptor complex translocates to the nucleus

73
Q

The activation or inactivation of these factors causes ?

A

Transcription of DNA into RNA and translation of RNA into an array of proteins .

74
Q

The time course of activation and response of these receptors is on the order of ?

A

Hours to days .

75
Q

Give me example of Intracellular receptors method :

A

Steroid hormones exert their action on target cells via intracellular receptors.

76
Q

Mention Other targets of intracellular ligands :

A

1- structural proteins
2- enzymes
3- RNA
4- ribosomes

77
Q

Give me example to describe the other targets of intracellular ligands :

A
  1. Tubulin is the target of antineoplastic agents such
    as paclitaxel .
  2. The enzyme dihydrofolate reductase is the target of
    antimicrobials such as trimethoprim .
  3. The 50S subunit of the bacterial ribosome is the target of macrolide antibiotics such as erythromycin.
78
Q

Mention two characteristics of signal transduction :

A

1) the ability to amplify small signals
2) mechanisms to protect the cell from excessive stimulation

79
Q

Give me example about signal amplification ?

A

A single agonist–receptor complex can interact with many G proteins, thereby multiplying the original signal many folds.

80
Q

Activated G proteins persist for a longer duration than does the original agonist–receptor complex . (T/F) ?

A

True

81
Q

Give me other example related to signal amplification :

A

Binding of albuterol, for example, may only exist for a few milliseconds, but the subsequent activated G proteins may last for hundreds of milliseconds.

82
Q

Further prolongation and amplification of the initial signal are mediated by ?

A

The interaction between G proteins and their respective intracellular targets ?

83
Q

only a fraction of the total receptors for a specific ligand may need to be occupied to elicit a maximal response . Explain this statement :

A

Because of this amplification

84
Q

Systems that exhibit this behaviour are said to have ………

A

spare receptors.

85
Q

Spare receptors are exhibited by………… receptors, where it is estimated that 99% of receptors are spare.

A

Insulin

86
Q

in the human heart, only about 5% to 10% of the total ………. are spare.

A

β-adrenoceptors

87
Q

little functional reserve exists in the failing heart . Why !!

A

Because most receptors must be occupied to obtain maximum contractility .

88
Q

When a receptor is exposed to repeated administration of an agonist, the receptor becomes ………….. resulting in a diminished effect.

A

Desensitized

89
Q

due to either phosphorylation or a similar chemical event that renders receptors on the cell surface unresponsive to the ligand. This phenomenon called ?

A

tachyphylaxis

90
Q

The receptors are internalized and sequestered within the cell, unavailable for further agonist interaction. This method called?

A

Down-regulation

91
Q

These receptors my be ?

A

1- recycled to the cell surface, restoring sensitivity
2- further processed and degraded, decreasing the total number of receptors available.

92
Q

particularly ion channels, require a finite time following stimulation before they can be activated again. This finite time called ?

A

Refractory period

93
Q

During this recovery phase, unresponsive receptors are said to be……….. .

A

“refractory.”

94
Q

repeated exposure of a receptor to an antagonist may result in ?

A

up-regulation of receptors

95
Q

How the up-regulation of receptors happens

A

in which receptor reserves are inserted into the membrane, increasing the total number of receptors available.

96
Q

Up-regulation of receptors can make the cells more sensitive to agonists and/or less resistant to the effect of the antagonist. (T/F) ?

A

F —>( Up-regulation of receptors can make the cells more sensitive to agonists and/or more resistant to the effect of the antagonist ) .

97
Q

The fastest receptors family is ?

A

ligand-gated ion channels

98
Q

The lowest receptors family is ?

A

Intracellular receptors

99
Q

The picture in slide ( 11,15,18,19) is

A

U know the answer bro , go to study them

100
Q

Love u all 💕

A

Pharma (8 decks)

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