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Drugs and Disease > Class Test 1 > Flashcards

Class Test 1 Flashcards

1
Q

How do you calculate Kd?

A

[H] x [R] / [HR]

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2
Q

In what ways can drugs be classified by the components involved?

A

Receptors
Ion channels
Carrier molecule
Enzymes

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3
Q

What are cells, tissues and organs controlled by?

A

Nervous system
Humoral agents
Local factors

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4
Q

In what ways can a drug be classified?

A

By nature
By action
Which cell components are involved
Which of the body systems does the drug affect
How does the drug help in the disease state

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5
Q

What is strength of signal replayed by the receptor dependent on?

A

Concentration of hormone-receptor complex

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6
Q

Where can other drugs block signal transduction?

A

Inside the membrane

Intracellular signal reception points

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7
Q

Common features of receptors?

A

Saturable

Activated by binding of an endogenous ligand

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8
Q

What does the fraction of total membrane receptors occupied by Ligands determine?

A

Size of transmembrane signal transduction

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9
Q

What is affinity of a drug?

A

Ability of a drug to bind to a receptor

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10
Q

What do drugs participate in?

A

Intracellular communication via chemical signals

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11
Q

What happens upon recognition of an appropriate chemical signalling molecule (ligand)?

A

Receptor proteins transmit the signal into a biochemical change in the target cell

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12
Q

What are the important steps of hormone initiated signal transduction?

A

Biosynthesis of hormone
Storage and secretion of hormone
Transport of hormone to target cell
Recognition by the hormone receptor protein
Relay and amplification of the signal that leads to defined biochemical reactions within the target cell
Removal of hormone

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13
Q

What properties do receptors have

A

Recognition

Transduction

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14
Q

What does the signalling cascade allow?

A

Signal to be amplified to produce multiple responses

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15
Q

Examples of responses produced by signal transduction?

A 
Modulation of gene translation
Hormone secretion 
Energy production 
Cell division 
Cell motion
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16
Q

Examples of intracellular second messenger signalling molecules

A

Cyclic nucleotides (cAMP, cGMP)
Calcium ions
IP3 and DAG

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17
Q

What do second messengers regulate?

A

Function of specific cellular effectors

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18
Q

Other examples of ligand-gated ion channels

A

GABA A receptor
Iontropic glutamate receptor
5-HT3 receptor

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19
Q

What type of receptors are on ligand gated ion channels

A

Multimeric transmembrane receptors

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20
Q

What does gaba a receptors do and used for?

A

Opens Cl- channel

Used as tranquillisers and anticonvulsant

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21
Q

What’s the composition of GPCRs?

A

2 highly conserved cysteine residues in extracellular loops that form an intramolecular disulphide bond to stabilise the receptor structure

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22
Q

What are the physiological roles of GPCRs

A 
Sensation 
Immune system and inflammation 
Metabolism 
Behaviour 
Autonomic nervous system
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23
Q

What do nuclear receptors affect

A

Gene transcription

Directly bind to DNA

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24
Q

What kind of responses are consequence of this increase in membrane permeability?

A

Postsynaptic excitatory or inhibitory responses

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25
Q

What is a second messenger?

A

Intracellular substance that mediates cell activity by relaying a signal from an extracellular molecule

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26
Q

Types of responses GPCRs allow?

A

Amplification

Diversity

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27
Q

What is efficacy?

A

Effect of a drug

More effect more efficacious the drug

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28
Q

What is potency?

A

Refers to the concentration of the drug

Less concentration required more potent the drug

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29
Q

What are nuclear receptors

A

Ligand activated transcription factors

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30
Q

What do GPCRs do?

A

Activate signal transduction inside the cell

E.g. cAMP

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31
Q

What does tyrosine receptor kinases do?

A

Act as an enzyme

Activated by hormones and growth factors

32
Q

What is the structure and function of RTKs?

A

For cell growth differentiation
Contain tyrosine (intracellular)
Carry out messages through signal transduction

33
Q

What is a kinase?

A

Something that has the ability to transfer phosphorus molecules, usually from a high energy substance like ATP

34
Q

What are the types of heterotrimeric G-proteins

A

Gi- activated Cyclase to increase cAMP
Gs- inhibits adenylate cyclase to decrease cAMP
Gq- activates phospholipase C to produce IP3 and DAG

35
Q

What do beta- adrenoceptors do?

A

Activate adenylate Cyclades

36
Q

What are the effects of increased cAMP?

A

Heart (beta 1)- increased heart rate

Lungs- relaxes bronchial smooth muscle

37
Q

Effects of agonists in the lung?

A

Dilates bronchial smooth muscle

Eases respiration

38
Q

Effects of antagonists in the heart

A

Slows heart rate and reduces force of beat

39
Q

What activates alpha alpha1-adrenoceptor?

A

Epinephrine

Expressed in smooth muscle

40
Q

How does alpha-adrenoceptor increase intracellular Ca2+ concentration?

A

Release from SR (IP3)
Through membrane channels (DAG)
Ca2+ stimulates smooth muscle contraction

41
Q

What is hypertension

A

High blood pressure

42
Q

What is hypotension

A

Low blood pressure

43
Q

What other cell responses are regulated by Gq inositol-phospholipid signalling

A

Liver- vasopressin- glycogen breakdown
Pancreas- acetylcholine- amylase secretion
Smooth muscle- acetylcholine- contraction
Blood platelets- thrombin- aggregation

44
Q

What is dimerisation?

A

Coupling by an agonist binding to 2 receptors

45
Q

Examples of drugs that inhibit RTK signalling

A

Imatinib (Gleevec)- for leukaemia
Lapatinib (Tykerb)- EGF receptor inhibitor for breast cancer
Trastuzumab- antibody against EGF for breast cancer

46
Q

What is thioureylene?

A

Converts T4 to T3

47
Q

What do thyroid hormones promote the synthesis of?

A

Adrenoceptors

48
Q

What is hypothyroidism for Hashimoto’s thyroidtis?

A

Lack of hormone

Treated by giving T4

49
Q

What does TSH act on?

A

Receptors on the membrane of the thyroid follicle cells through the mechanism that involves cAMP

50
Q

What do thyroid hormones do?

A

Increase basal metabolic rate
Increase heat production
Increase glucose uptake

51
Q

How can hyperthyroidism be treated

A

With beta adrenoceptors antagonists

52
Q

Zones of adrenal cortex

A

Glomerulosa- aldosterone

Fasiculata and reticularis- adrenal androgens and cortisol

53
Q

Adrenal medulla secretes

A

Catecholamines
E.g. Epinephrine and norepinephrine
Adrenaline in response to sympathetic nervous system

54
Q

What are adrenocortical hormones?

A

Steroid hormones

55
Q

What does failure of adrenal medulla cause?

What does tumour of adrenal medulla cause?

A

Failure- hypotension
Tumour- hypertension
E.g. Phrenocheomocytoma, neuroblastoma

56
Q

What are glucocorticoids

A 
Cortisol 
Actions
Metabolic 
Negative feedback on AP and H
Anti inflammatory and immunosuppressive effects
57
Q

What are mineralcorticoids

A

Aldosterone

58
Q

What are sex hormones

A

Testosterone

59
Q

What are HREs?

A

Short segments of DNA able to bind a specific hormone receptor complex affecting transcription

60
Q

What are oestrogen receptor antagonists for?

A

Prevention and treatment of breast cancer (tamoxifen)

61
Q

What is the composition of a typical ligand

A

Lipophillic hormones with steroid hormones and dedicates of vitamin A and D

62
Q

When is a mineralcorticoid receptor antagonist used?

A

Liver cirrhosis and heart failure

63
Q

What are oestrogen receptor agonists used for?

A

Hormone replacement therapy in postmenopausal women

64
Q

Adverse effects of glucocorticoids

A 
Osteoporosis 
Cushing's syndrome
Metabolic effects
Suppression of infection 
Suppression endogenous glucocorticoid synthesis
65
Q

What is glucocorticoid receptor agonist for?

A

Inflammation

66
Q

What are the actions of adrenalin in tissues

A

Increase cyclic AMP

67
Q

What do anti-inflammatory and immunosuppressive activity reduce?

A

Blood vessel dilation and leakage
Glucocorticoids inhibit phospholipase A2- blocks production of arachidonic acid, pstoglanduns and leukotrienes from cell membrane phospholipid

68
Q

What are androgen receptor antagonists used for?

A

Prostate cancer treatment

69
Q

How do ADR and Na maintain blood pressure

A

Iontropic effects on heart and vasoconstrictor

I.e. Increases heart rate and contracts blood vessels

70
Q

Dose vs concentration?

A

Dose- amount of drug (micro grams, nanomoles)

Concentration- amount of drug per unit volume (micromolar, nanomolar)

71
Q

What are drug receptor controls?

A

Selectivity of drug effect
Magnitude of response
Mechanisms to prevent/mimic physiological function

72
Q

What is magnitude of response?

A

Hyperbolic
[AR] = [A]
[RT] Kd + [A]

73
Q

What is EC50?

A

Concentration required to get half the maximum response

74
Q

How do allosteric Ligands produce effects

A

By increasing/decreasing potency

Causing an increase/decrease in efficacy

75
Q

What is implied by receptors ability to spontaneously adopt an active site

A

Level of constitutive activity

76
Q

What is an inverse agonist?

A

Ligand that binds to the receptor and limits constitutive activity

Drugs and Disease (25 decks)

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