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Therapeutics > Park lecture 1 > Flashcards

Park lecture 1 Flashcards

1
Q

What is endocrine signaling

A

Signaling molecule produced in specific organ, and diffuses across the whole body. Some cells have the receptor for this molecule and respond.

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2
Q

Juxtacrine signaling mechanism

A

Cell-Cell contact signaling.

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3
Q

Actual concentration of endocrine signaling is (high or low)?

A

Low (in Nm)

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4
Q

Paracrine signaling

A

Nearby cells release molecule and affects neighboring cells.

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5
Q

Synaptic signaling mechanism

A

Neurotransmitter travels very short distance (high local concentration)

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6
Q

Autocrine signaling

A

Made and functions in same cell

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7
Q

Cell surface receptor vs intracellular receptor

A

In cell surface receptor, signaling molecule does not enter the cell. It binds on the surface and activates 2nd messenger.
In intracellular receptors, some signaling molecules are hydrophobic enough to get into the cell (steroid hormones)

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8
Q

Steroid receptor mechanism of action once activated

A

They go into the nucleus and bind DNA, promoting expression of genes.

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9
Q

Precursor of steroid

A

Cholesterol

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10
Q

Remember cholesterol numbering system

A
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11
Q

In the planar form of cholesterol, bottom of plane is called

A

alpha (dash Dash)

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12
Q

Top of the plane in planar form

A

Beta (thick dark wedge)

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13
Q

main action of steroids

A

transcription regulation

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14
Q

what are the 3 sex and pregestational hormones

A

!7-B estradiol, testosterone, progestrone

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15
Q

What are the 2 adrenocortical hormones

A

Cortisol, aldosterone

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16
Q

Cortisol (glucocorticoids) use

A

Anti stress hormone and anti-inflammation

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17
Q

aldosterone(mineralocorticoids) use

A

Na+ uptake in kidney. Raises blood volume and blood pressure.

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18
Q

how would you tell cholesterol apart from other steroids

A

Cholesterol has a long chain at 17-C. (resembles fish)

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19
Q

How would you tell progesterone apart from other steroids

A

Has 20 and 21 carbons. and has 2 ketones.

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20
Q

How would you tell 17-B estradiol apart from other steroids

A

Aromatic group and 3-OH (di-ol= two hydroxy)

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21
Q

How would you tell testosterone apart from other steroids

A

Has a 3-ketone and 17-OH

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22
Q

How would you tell cortisol apart from other steroids (especially from aldosterone)

A

Bothe cortisol and aldosterone have 11-OH, but cortisol has a 17-OH

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23
Q

How would you tell aldosterone apart from other steroids(especially from cortisol)

A

has 11-OH, but no 17-OH

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24
Q

What are the 5 hormone receptors

A

Estrogen receptor, androgen receptor, corticosteroid receptor, aldosterone receptor, progesterone receptor. Sometimes there is cross reactivity

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25
Q

What are the two binding domains of steroid receptors

A

DNA binding domain
Hormone binding domain

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26
Q

How do hormones work

A

-Penetrate membrane and binds specific hormone receptor
-hormone receptor is surrounded by heat shock proteins (Protects the structure of hormone receptor)
-Once hormone is recognized by receptor they are activated and release heat shock proteins.
-hormone receptor is transported into nucleus
-dimer forms and binds to a specific part of DNA
-Activate transcription of genes

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27
Q

Once glucocorticoid receptors are activated, they bind to specific sequences called

A

Hormone response element (HRE)

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28
Q

Binding glucocorticoid to HRE alters the

A

rate of transcription

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29
Q

where is cortisol produced

A

Adrenal gland

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30
Q

What stimulates adrenal gland to release cortisol

A

ACTH (adrenocorticotropic hormone)

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31
Q

Where is ACTH produced

A

Pituitary

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32
Q

Production of ACTH is stimulated by

A

CTH (corticotropin hormone)

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33
Q

Where is CTH produced

A

Hypothalamus

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34
Q

What suppresses the release of CRH and ACTH

A

Cortisol (feedback)

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35
Q

First step of steroid hormone synthesis is catalyzed by

A

P 450 scc (side chain cleaving)

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36
Q

P 450 converts cholesterol to

A

pregnenolone

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37
Q

P 450 cleaves

A

long chain of cholesterol, converts to ketone.

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38
Q

How do we get progesterone from pregnenolone

A

3-B dehydrogenase isomerase adds a ketone on C-3 and a double bond between C4 and C5

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39
Q

Steps to go from pregnenolone to DHEA

A

17-a hydroxylase adds an OH to 17 carbon to form an intermediate 1. Intermediate 1 is acted on by 17,20 lyase removes 20, 21 carbon and there will be a ketone on 17

40
Q

How is DHEA converted to andronstenedione

A

3b-dehydrogenase isomerase adds a ketone on C-3 and a double bond between C4 and C5

41
Q

androstenedione will eventually lead to the formation of

A

Testosterone and estradiol

42
Q

progesterone will eventually lead to formation of

A

aldosterone

43
Q

intermediate 1 to intermediate 2 catalyzed by

A

3 B dehydrogenase isomerase

44
Q

Intermediate 2 will lead to formation of

A

Cortisol

45
Q

progesterone to intermediate 2 catalyzed by

A

17-a hydroxylase

46
Q

Intermediate 2 to androstenedione catalyzed by

A

17,20 lyase

47
Q

progesterone to aldosterone steps

A

21 hydroxylase adds OH to C-21
11 B hydroxylase adds OH to C-11 (aldosterone)

48
Q

Intermediate 2 to cortisol steps

A

21 hydroxylase adds OH to C-21
11 B hydroxylase adds OH to C-11 (cortisol)

49
Q

17-a- hydroxylase deficiency causes

A

Overproduction of mineralocortecoids and deficiency of corticosteroids and sex hormones

50
Q

symptoms of 17-a-hydroxylase deficiency

A

Hypocortisolism—–> enlargement of adrenal gland
hyperaldosteronism
ambigous genitalia

51
Q

Why does hypocortisolism cause enlargement of adrenal gland

A

Body will lack cortisol. Body releases CRH and ACTH to stimulate adrenal gland again and again, even though it can not produce cortisol. It gets bigger

52
Q

21 hydroxylase deficient people can not produce

A

Can not produce either aldosterone or cortisol.
Only produce sex hormones (overproduction of sex hormones)

53
Q

Symptoms of 21 hydroxylase deficiency

A

Hypocortisolism- no negative feedback, leads to overexpression of CRH and ACTH, leads to adrenal gland enlargement.

Hypoaldosteronism- lose sodium to urine, dangerous to infants.

premature androgen exposure
- hirsutism
-early epiphyseal closure
-ambiguous genitalia in female

54
Q

Why is there an overexpression of sex hormones in 21 hyrdroxylase deficiency

A

21 hydroxylase not being sufficient causes all the intermediates to be sent to sex hormones instead of being made into cortisol and aldosterone.

55
Q

Why is there an overexpression of sex hormones in 21 hydroxylase deficiency

A

21 hydroxylase not being sufficient causes all the intermediates to be sent to sex hormones instead of being made into cortisol and aldosterone.

56
Q

Two possible routes of andronstenedione

A

Androstenedione is acted on by 17B-hydroxysteroid dehydrogenase to for testosterone.
It can also be acted on by aromatase to form an intermediate that is then acted on by 17B-hydroxysteroid dehydrogenase to form 17B-estradiol

57
Q

How is testosterone converted into 17B-Estradiol?

A

Acted on by aromatase

58
Q

Steroids are transported in blood by

A

Plasma transport proteins

59
Q

What are some plasma transport proteins

A

Corticoid binding globulin (glucocorticoids and progesterone)
Sex hormone binding globulin (testosterone and 17B-estradiol)

60
Q

Steroids are metabolized in

A

Liver

61
Q

Where are the steroids excreted to after being metabolized by liver

A

Progesterone, androgen and glucocorticoids- Urine
Estrogen- Bile

62
Q

Two drugs that control the synthesis of steroid hormones

A

Aminoglutethimide and ketoconazole

63
Q

What does aminoglutethimide do?

A

Blocks steroid production in some hormone dependent tumors.

64
Q

How does aminoglutethimide block steroid production

A

Inhibit P450SCC and aromatase

65
Q

What does ketoconazole do?

A

Antifungal at low concentration

66
Q

How does ketoconazole work

A

Block synthesis of ergosterol by inhibiting P450SCC, 17A-hydroxylase and 11B-hydroxylase

67
Q

Two types of cells in testes

A

Leydig cells and sertoli cells

68
Q

Leydig cells are stimulated by

A

Luteinizing hormone (LH)

69
Q

Sertoli cells are stimulated by

A

Follicle stimulating hormone(FSH)

70
Q

What do leydig cells produce

A

Testosterone

71
Q

What do sertoli cells produce

A

Spermatogenesis

72
Q

LH and FSH are released by what gland? What hormone activates this gland?

A

Anterior pituitary. GnRH.

73
Q

What releases GnRH

A

Hypothalamus

74
Q

FSH stimulates

A

Sertoli Cells

75
Q

LH stimulates

A

Leydig cells

76
Q

What are the two requirements for spermatogenesis in sertoli cells

A

FSH+testosterone

77
Q

What are the two gonadotropins

A

LH
FSH

78
Q

How is testosterone regulated in the body?

A

Feedback inhibition

79
Q

What enzyme catalyzes testosterone at target cell

A

5a-reductase

80
Q

What does 5a-reductase convert testosterone into

A

5a-dihydrotestosterone

81
Q

Which one is more potent and has more activity out of testosterone and 5a-dihydrotestosterone

A

5a-dihydrotestosterone

82
Q

How does 5a-reductase convert testosterone to 5a-dihydrotestosterone

A

Removes double bond from testosterone and adds an alpha hydrogen to position 5

83
Q

In people with hypopituitarism, we can supplement them with testosterone. Would that make the person fertile?

A

No. FSH needed for sperm formation.

84
Q

Why do we use synthetic androgens

A

Testosterone is metabolized too quickly

85
Q

How is testosterone metabolized

A

oxidation of 17-hydroxy group

86
Q

How will adding groups to 17-carbons affect testosterone?

A

longer half life

87
Q

Name 3 synthetic androgens and their ROA

A

Methyltestosterone- ORAL
Testosterone enanthate-IM
testosterone cypionate-IM

88
Q

What is the modification to methyltestosterone and what effect does it have?

A

17-alkyl addition. Makes it more orally active and longer half life

89
Q

Testosterone enanthate and Testosterone cypionate structural changes compared to testosterone and what effects they have

A

Both have 17 esters with long hydrocarbon chains. Makes it more lipophilic. They are injected IM so they stay in injection site and slowly diffuse. Esters will hydrolyze and testosterone will form. SO they are prodrugs.

90
Q

Adverse effects of testosterone in women

A

Hirsutism
deepening of voice
ammenorhea
clitoral enlargement
acne

91
Q

Adverse effects of Testosterone in men

A

Acne
sleep apnea
gynecomastia
increased aggressiveness and psychotic symptoms
azoospermia and testicular atrophy

92
Q

What are the two anti androgens

A

5a- reductase inhibitors
androgen receptor inhibitor

93
Q

5a- reductase inhibitors action

A

Block conversion from testosterone to 5a-dihydrotestosterone

94
Q

Androgen receptor inhibitors

A

Block binding of endogenous androgens to receptors

95
Q

Example of 5a-reductase inhibitors

A

Finasteride and dutasteride

96
Q

5a- reductase (Finasteride and dutasteride) pharmacologic uses

A

BPH and Male pattern baldness

97
Q

androgen receptor inhibitor pharmacologic uses

A

cyproterone and spironolactone
Hirsutism in women
Acne
Excessive sex drive in men

Therapeutics (46 decks)

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