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WEEK 2 SEM 4 > Pharmacology of androgens and antiandrogens > Flashcards

Pharmacology of androgens and antiandrogens Flashcards

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1
Q

Where are androgens secreted from?

A

testes, ovaries, adrenal cortex, adipose tissues (LITTLE BIT)

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2
Q

In the testes, what cels secrete testosterone?

A

Leydig cells

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3
Q

What are the 3 regions of the adrenal cortex and what do they secrete?

A

zona glomerulosa: mineralocorticoid secretion (aldosterone)
zona fasciculata: cortisol secretion
zona reticularis: androgen secretion

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4
Q

What are the 2 cell types in testes?

A

Leydig

Sertoli

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5
Q

What are the leydig cells and sertoli cells under the influence of?

A

Leydig- LH

Sertoli- FSH

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6
Q

Leydig cells release testosterone. What is the role of testosterone?

A
  1. stimulates sertoli cells for spermatogenesis

2. converted to DHT

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7
Q

What does FSH do?

A

act on sertoli cells:
spermatogenesis
releases AMH
release inhibin- inhibits FSH release from pituitary

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8
Q

What happens if there are no testosterone receptors in the body?

A

no negative feedback so high testosterone levels
high FSH and LH levels
no testosterone effects- so no male characteristics seen

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9
Q

What are the precursors of testosterone?

A

androstenedione and androstenediol

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10
Q

What does testosterone get metabolized to?

A
  1. androsterone and etiocholanolone
  2. dihydrotestosterone= under influence of 5 alpha reductase
  3. oestrogen= through aromatase
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11
Q

Can DHT be converted to oestrogen?

A

NO BITCH

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12
Q

Testosterone is converted to DHT in all cells except what?

A

muscles

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13
Q

What is testosterone converted to DHT by?

A

5 alpha reductase

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14
Q

What does DHT do?

A

external virilisation
sexual maturity at puberty
growth of prostate and penis at puberty
causes facial hair, acne, and temporal hairline recession particularly in males
hairline recession usually leads to more hair growing elsewhere

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15
Q

How can we treat prostate cancer?

A

prostate grows bc of DHT

so give 5 alpha reductase inhibitors

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16
Q

How to treat male baldness

A

DHT causes loss of hair

so give 5 alpha reductase inhibitors

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17
Q

There are 2 isotopes of enzyme 5 alpha reductase. What are they?

A

type 1: scalp and skin

type 2: genital skin and prostate

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18
Q

What happens with 5 alpha reductase deficiency?

A 
AUTOSOMAL RECESSIVE
testes can develop but NO PROSTATE
FEMALE external genitalia
puberty clitoris can enlarge
at puberty with the testosterone rise, if testosterone receptors are there you can develop external male genitalia
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19
Q

What is male pseudo hermaphrotidism?

A

type 2 5 alpha reductase mutation
primary sexual characteristic different to secondary sexual characteristic
fertile (can be father) but female external genitalia

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20
Q

If DHT is not metabolised properly, what happens?

A

prostatic hyperplasia
this is when DHT is not metabolized completely, and thus there will be enlargement of the prostate
there may also be acne and hirsutism (excess hair)

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21
Q

What secondary characteristics are DHT and testosterone responsible for?

A 
tall height
more muscle
deep voices- more larynx growth
external virilisation
more body hair
more muscle bulk
less subcutaneous fat so subcutaneous veins become more prominent
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22
Q

Give some names of androgens:

A

testosterone, nandrolone, oxymetholone, stanozolol

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23
Q

What is oxymethalone used for?

A

sold as anapolon or anadrol

treatment of anemia

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24
Q

What are the side effects if you abuse anabolic steroids?

A

hypertension and edema
cholestatic jaundice
SUPPRESS LH and FSH- smaller testicular size
premature closure of long epiphyseal bones
gynecomastia
increase muscle mass
acne
more agression
more LDL, less HDL- more vascular disease

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25
What are the 2 main reasons for the development of internal and external genitalia to fail?
androgen insensitivity syndrome | 21 hydroxylase deficiency
26
What happens in androgen insensitivity syndrome?
androgen is present but receptor isnt bc mutation in receptor
27
What are the symptoms of AIS?
XY with female genitalia short vaginal length testes in abdomen no female internal genitalia
28
How is AIS treated?
remove testes put patient on oestrogen therapy at puberty if mild with male external genitalia give high testosterone the patient is then assigned to the gender on which they feel more confortable
29
What is 21 hydroxylase deficiency?
congenital adrenal hyperplasia
30
What happens in CAH?
21 HYDROXYLASE makes mineralocorticoids, or glucocorticoids from progestogen if deficient, progestogens build up then get converted to testosterone
31
What are the symptoms of CAH?
females: ambiguous genitalia feminised testes internal genitalia both male and female males: premature puberty
32
What is an example of synthetic GnRH?
gonadorelin
33
What are examples of GnRH analogues?
buserelin | goserelin
34
What do GnRH analogues do?
desensitize the receptors for GnRH after an initial surge of LH and FSH release and then act as antagonists cause a reduction in testosterone in the long term they are useful for prostate and breast cancers and endometriosis
35
What does a GnRH antagonist do?
is a competitive antagonist of the GnRH receptor on the pituitary these negatively affect the pituitary cause no initial surge of LH and FSH use in IVF prevent women having an LH surge and thus help with breast cancer
36
What is an example of an androgen antagonist?
cyproterone
37
What is cryptorchidism?
failure of testes to descend
38
What can cryptorchidism cause?
infertility | tumour
39
What are the treatment of mild AIS?
High dose testosterone
40
What are the treatment for strong AIS?
OESTROGEN
41
What does mesterolone (methyltestosterone) do?
treats male infertility associated with hypogonadism
42
What does the drug danazol treat?
gynaecomastia mastalgia (breast pain) benign fibrocystic disease (breast tenderness) endometriosis and infertility menorrhagia (increased/heavy and prolonged menstrual bleeding)
43
What is danazol?
androgen derivative it does not get converted to oestrogen has antioestrogenic and antiprogestogenic effects
44
How does danazol work?
it inhibits the release of LH and FSH
45
What is a primary hypogonadal syndrome?
testes fail to produce adequate testosterone in response to LH
46
What is an example of hypogonadal syndrome?
Klinefelter’s syndrome (XXY)
47
What is Klinefelter's syndrome?
XXY deficient –ve feedback at the HPG axis bc of low testosterone so have high FSH and LH
48
What is the treatment of Klinfelter's syndrome?
GH testosterone will take 2 years to reach puberty growth hormone and testosterone, and it will take 2 years to reach puberty
49
What is a secondary hypogonadal syndrome?
deficiency in the pituitary hormones (FSH and LH) | OR pituitary dysfunction
50
What is an example of secondary hypogonadal syndrome?
Kallmann’s syndrome leads to delayed/absent puberty if untreated- lead to infertility
51
How do you treat kallman's?
``` give gonaderelin (synthetic GnRH) give LH or FSH ```
52
What is precocious puberty?
early puberty
53
How do you treat precocious puberty?
androgen antagonists the drug is: cyproterone acetate mechanism: inhibits peripheral androgen receptors
54
How can you treat a sex offender?
androgen antagonist with their consent
55
What is guserelin and boserelin?
GnRH analogue agonists when they are administered to reduce FSH and LH levels, there is an initial LH and FSH surge bc of this there is increase in testosterone in the body can use cyproterone to lower LH, FSH and testosterone levels
56
What can cyproterone be used for?
acne hirsutism loweing FSH and LH and testosterone treat precocious puberty
57
What does benign prostatic hypertrophy mean?
enlarged prostate in older men | causes urinary obstruction
58
Where is the prostate located between?
bladder and penis
59
How does BPH cause urinary obstruction?
urethra passes from bladder to penis through the centre of the prostate through the penis the prostate enlargement causes urinary obstruction can lead to pain and infection bc of the stagnated urine
60
How do you treat BPH?
5 alpha reductase inhibitor- finasteride | alpha 1 adrenergic blockers eg tamsulosin and alfuzosin
61
Give two examples of drugs that are 5 alpha reductase inhibitors?
``` finasteride = it inhibits type II 5 alpha reductase dutasteride = inhibits both type I and type II reductases = SO CANT USE FOR BPH ```
62
How does alpha 1 adrenergic blockers help with BPH?
help relax smooth muscle components of the prostate
63
What is the main way to treat prostatic cancer?
DHT and Testosterone grow prostatic cells | treatment needs to focus on reducing this
64
How do you treat prostatic cancer?
cyproterone acetate GnRH analogues such as goserelin and buserelin GnRH antagonists such as cetrorelix and ganirelix oestrogens such as ethinyloestradiol and diethylstilbestrol orchidectomy (castration) anti-androgens such as flutamide 5 alpha reductase inhibitors such as finasteride and dutasteride
65
What does cyproterone acetate do?
an androgen antagonist | it will inhibit peripheral androgen receptors
66
What do GnRH analogues do?
it can be given continuously to suppress Leydig cell function • this happens because the GnRH analogue will desensitize GnRH receptors and thus FSH and LH levels will reduce thus testosterone levels reduce
67
What do GnRH antagonists do?
block LH and FSH release leydig cells regression testosterone reduces
68
Why is orchidectomy good for helping prostate cancer?
if you remove the testes, then you will not produce much testosterone so possibly no prostate cancer
69
How does anti androgen help with prostate cancer?
compete with testosterone and DHT | block their action
70
What is erectile dysfunction?
consistent inability to sustain an erection of sufficient rigidity for sexual intercourse
71
Who can get erectile dysfunction?
40-70 year old men nerve damage endocrine disease depression
72
What is the pathway for eretction?
1. stimulations: mechanoreceptors on the penis respond to touching, stroking of penis. There are also thoughts, sights, smells which trigger the CNS 2. these signals go to neurons in penis 3. get an increase in parasympathetic NO activity and decrease in sympathetic activity 4. NO has vasodilating effect 5. blood fills in corpus cavernosum 6. erection 7. bc of erection, veins in the penis compress. this leads to more filling up of blood in the penis.
73
What would sympathetic activity do?
constrict arteries in the penis
74
People with erectile dysfunction produce less what?
NO
75
What do you treat erectile dysfunction with?
PDE5 inhibitors= SILDENAFIL, TADALAFIL, VARDENAFIL
76
What is the mechanism for PDE5 inhibitors?
NO activates guanylate cyclase which re leases cGMP from GTP cGMP is produced in the smooth muscles of the penis which modulates Ca2+ entry into the sarcoplasmic reticulum thus making less Ca2+ available (by activation of protein kinases) this leads to relaxation of the smooth muscle however, cGMP is broken down by PDE5 which removes its effect PDE5 inhibitors act by inhibiting PDE5 thus making the effects of cGMP last longer it blocks cGMP hydrolysis by taking its active s ite on the PDE5 enzyme
77
What are side effects of PDE5 inhibitors?
headache, vasodilation, flushing, reduction in BP, disturbances of colour vision due to inhibition of PDE6 in retina sometimes priapism, which is painful erections that do not go away
78
Why shouldn't PDE5 inhibitors be taken with nitrates?
BOTH PDE5 inhibitors and nitrates = vasodilators | if take together- big blood pressure fall
79
If patient has angina pectoris and takes PDE5 inhibitors and nitrates, what can happen?
heart attack because patients with angina require a higher than normal blood pressure to perfuse the heart if bp drops heart no get enough oxygenated blood= MI
80
What do sertoli cells release?
AMH= regresses mullerian duct in utero | Inhibin B= acts on anterior pituitary to reduce FSH release
81
What type of hormone is testosterone?
steroid so it diffuses through and binds to its receptor in the cytosol

WEEK 2 SEM 4 (6 decks)

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