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[THER 201] 1st Lecture Exam > [SIM] Mechanism of Drug Action > Flashcards

[SIM] Mechanism of Drug Action Flashcards

1
Q

What is the receptor for Norepinephrine?

A

Beta-2

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2
Q

What is responsible for phosphorylation of Myosin?

A

Myosin Light Chain Kinase

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3
Q

What state does Myosin have to be to have a greater affinity for Actin in muscle contraction?

A

Phosphorylated

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4
Q

Function: Salbutamol

A

Binds to B2 Adrenergic Receptors, mimicking Norepinephrine causing relaxation of airways

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5
Q

Differentiate Salbutamol at Low Doses and High Doses

A

Low Dose: Specific to B2 Adrenergic Receptors

High Dose: Decreased specificity to B2 Adrenergic Receptors; may cause tremors and tachycardia

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6
Q

What are the receptors of Acetylcholine?

A

Nicotinic

Muscarinic

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7
Q

[Type of Receptor]

Nicotinic

A

Ionotropic

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8
Q

[Type of Receptor]

Muscarinic

A

G Protein Coupled Receptor

Phospholipase C/IP3 Pathway

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9
Q

Function: M2 Receptors

A

Bringing the heart back to normal after actions of the sympathetic nervous system

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10
Q

Components: Atropine

What is the component responsible for most of its physiologic effects?

A

D-Hyoscyamine
L-Hyoscyamine

L-Hyoscyamine

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11
Q

This is a competitive inhibitor of Acetylcholine

A

Atropine

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12
Q

[Type of Receptor]

Insulin

A

Ligand-gated Tyrosine Protein Kinase

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13
Q

Components of Insulin Receptors

A

2 Alpha Subunits
2 Beta Subunits

Linked by disulfide bonds

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14
Q

Where is the insulin-binding domain located?

A

Extracellular Alpha Sub-units

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15
Q

Which component of the insulin receptor has the cytoplasmic kinase activity?

A

Beta Sub-unit

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16
Q

Effect of Tyrosine Kinase Receptor Activation (Insulin Receptors)

A

Releases Phosphatidyl Inositol-3-Phosphate (PI3P) and increases the number of GLUT4 on the outer membrane, allowing entry of Glucose into the cell

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17
Q

What causes Type II Diabetes?

A

Insulin insensitivity or decrease in Insulin Receptor Signaling

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18
Q

Differentiate Tyrosine Kinase receptors from GPCRs in terms of Gene Expression

A

Tyrosine Kinases affect downstream events in gene expression

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19
Q

What is the most prevalent form of Estradiol and Estrone?

A

Estrogen

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20
Q

Where is Estrogen produced?

A

Ovaries

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21
Q

2 Main Targets of Estrogen

A

Breast

Uterus

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22
Q

Estrogen receptors are stabilized by?

A

Heat Shock Proteins

HSP90

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23
Q

Differentiate the 2 Kinds of Estrogen Receptors

A
  1. ER-Alpha
    - Made up of 500 AAs
    - Mostly in Endometrium and Breast Cancer
  2. ER-Beta
    - Made up of 600 AAs
    - Present in Granulose Cells and Osteoblasts
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24
Q

What activates transcription in the ER-Alpha Receptor?

A

ER-Alpha:Estradiol Complex

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25
Q

What do Breast Tumor Cells need for growth and proliferation?

A

Estrogen

26
Q

Drug for Breast Cancer Patients

How does it work?

A

Tamoxifen

Competitive, partial agonist inhibitor of Estrogen

27
Q

Tamoxifen requires processing in the liver to become this activate metabolite that has a higher affinity to Estrogen Receptors

A

4-Hydroxytamoxifen (Endoxifen)

28
Q

Limitations of Tamoxifen Therapy

A
  1. Only efffective in women who have ER+ BRCA

2. More than 1/3rd of these do not respond to Tamoxifen though

29
Q

Lack of this liver enzyme may interfere with Tamoxifen metabolite production

A

Cytochrome P450 2D6

CYP2D6 and CYA3P4

30
Q

2 Mechanisms of Sensitization

A

Homologous

Heterologous

31
Q

Differentiate Homologous and Heterologous Sensitization

A

Homo: Loss of responsiveness of the specific receptor that has been exposed repeatedly

Hetero: Desensitization of one receptor also results in desensitization of another receptor not directly activated by agonist in question

32
Q

Function: Chelating Agent

A

Prevent/Reverse heavy metal toxicity on enzymes or cellular targets by binding to them

33
Q

Used for serious lead poisoning and lead encephalopathy

A

Ethylene Diamine Tetraacetate

CaNaEDTA

34
Q

[Treatment]

Dimercaprol

A

Arsenic, Mercury, Gold, Lead, Antimony, and other Toxic Metal Poisoning

35
Q

[Treatment]

Succimer

A

Lead Poisoning

36
Q

[Treatment]

Penicillamine

A

Copper Poisoning

37
Q

[Treatment]

Antacids

A

Patients with dyspepsia and acid-peptic diseases

38
Q

[Treatment]

Mannitol

A

 Use to treat oliguric phase of ARF
 Promotes the excretion of toxic substances
 Use to reduce intracranial pressure
 Used in the treatment of cerebral edema

39
Q

[Treatment]

Ammonium Chloride

A

Lowers blood pH after being metabolized to Urea and Hydrochloric Acid

40
Q

[Treatment]

Ascorbic Acid

A

Acidifies urine, providing hydrogen ions and lowering urine pH

41
Q

[Treatment]

Acetazolamide

A

Increases excretion of Bicarbonate Ions, lowering blood pH

42
Q

Who experimented on chicks (the animal) with Curare and Nicotine?

A

Langley (1905)

43
Q

Any cellular macromolecule that a drug binds to initiate its effects; a component of the organism with which a drug acts in some specific manner to cause an action which results to observable effects

A

Receptor

44
Q

Agents that bind to receptors (include drugs, hormones, autacoids, growth factors, neurotransmitters, etc.)

A

Ligands

45
Q

An agent that elicits a biological effect by binding to a receptor.

A

Agonist

46
Q

Drugs binding to receptors but do not initiate change in cellular function. Blocks the binding of agonists.
An agent that by itself is devoid of biological activity but binds to the receptor and prevents the biological effect of an endogenous agonist.

A

Antagonist

47
Q

Endogenous substances (generated by the agent-receptor complex which) which serve as signaling mechanisms that enable drugs/endogenous substance to exert their biologic effects.

A

Second Messengers

48
Q

The measure of tightness with which a drug binds to a receptor.

A

Affinity

49
Q

Measure of the ability of a drug, once bound to the receptor, to produce measurable physiologic effects

A

Intrinsic Activity

50
Q

Receptors are present in finite numbers.

A

Saturability

51
Q

Binding is a noncovalent interaction due to weak intermolecular forces.

A

Reversibility

52
Q

Many natural occurring agonists exist as optical isomers (+ or -, l or d, S or R); preference for naturally- occurring stereoisomers (e.g. 1- vs d-norepinephrine)

A

Stereoselectivity

53
Q

Preference for specific or closely related, agonist and should not recognize chemically dissimilar endogenous agents

A

Agonist Specificity

54
Q

Binding should be present in tissues known to be biologically sensitive to the hormone/drug and should take place at concentrations consistent with the physiological concentrations of the endogenous agents

A

Tissue Specificity

55
Q

Neurotransmitter used by all motor neurons

A

Acetylcholine

56
Q

Components of Acetylcholine Receptors

A

5 Subunits:

2 Alpha Sub-units
1 Beta Sub-unit
1 Gamma Sub-unit
1 Delta Sub-unit

57
Q

How many units of Acetylcholine is needed to activate the Nicotinic Acetylcholine Receptor?

A

2

58
Q

[Treatment]

Turbocurarine

A

Neuromuscular blocking drug

Skeletal muscle relaxant

59
Q

[Mechanism of Action]

Turbocurarine

A

Competitive antagonist of ACH that acts predominantly on Nicotinic Receptor Sites

60
Q

Where are the Nicotinic Receptor Sites found on the ACH Receptors?

A

Alpha Sub-units

61
Q

Differentiate Tachyphylaxis and Tolerance

A

Tachyphylaxis: Rapid desensitization as a result of acute effects

Tolerance: Long term effect

[THER 201] 1st Lecture Exam (10 decks)

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