Androgens Flashcards

1
Q

Testosterone is produced in

A

Leydig cells in men
Corpus Luteum and Adrenal cortex in women

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2
Q

Function of 5a reductase

A

converts Testosterone to DIhydrotestosterone and Estradial

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3
Q

Uses of Androgens

A

male hypogonadism
aplastic anemia
Osteoposrosis
Puberty for Testosterone deficient boys
incr. athletic performance: anabolic steroids

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4
Q

AEs of Androgens

A

Excessive masculinization
decr. sperm production
decr. testicular size
Gynecomastia
Virilization in females
Hepatotoxic
Aggressive behavior

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5
Q

Effects of Virilisation in females

A

Hyperandrogenism
Temporal balding
male body physique
muscle building
incr. clitoris size
Hirsutism

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6
Q

Admin of Testosterone derivatives

A

Implant as it undergoes extensive 1st pass metabolism when taken orally=inactivation

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7
Q

CIs of Testosterone impkant

A

Breast, prostate neoplasm

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8
Q

Effects of Testosterone implant

A

May cause premature closing of epiphyses if administered early in puberty
Stimulates endogenous EPO production

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9
Q

DIs of Testosterone Implant

A

Incr. effects of warfarin:=incr. bleeding
May decr blood glycose levels

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10
Q

Which are the Testosterone Esters

A

Testosterone Undecanoate: T deficiency
Enanthate: incr. muscle mass
Cypionate: T. deficiency

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11
Q

Uses of Testosterone Esters

A

improve sexual performance
libido

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12
Q

What is Methyltestosterone

A

17-a-alkyl derivative of T with an oral bioavailability>T.
*its an Ester of T

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13
Q

Uses of Methytestosterone

A

treats men with T. deficiency

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14
Q

Cautions with Methytestosterone

A

Prolonged periods of se
Hepatotoxic

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15
Q

What is Mesterolone

A

dihydroT. derivative that is not metabolised to estrogen
Has an oral bioavailability>T

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16
Q

Indications of Mesterolone

A

Patients with hepatic disease and those woth estrogenic synptoms of other testosterone

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17
Q

What is Nandrolone

A

An anabolic effec with hight anabolic effects and lower androgneic effects

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18
Q

Indications of Nandrolone

A

Treatment of Osteoporosis and Aplastic anemia

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19
Q

Effects of Nandrolone

A

incr. muscle growth
incr. appetite
incr. RBC production
incr. bone density

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20
Q

Larger doses of Nandrolone leads to

A

Gynecomastia
decr. libido

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21
Q

AEs of Nandrolone

A

Erectile dysfunction
CV damage
decr liver hepatic enzymes
liver tumors
cholestatic jaundice

22
Q

Name an Antigonadotropin

A

Danazol

23
Q

MOA of Danazol

A

binds to estrogen Rs–> inhibits Gonadotropin secretion

24
Q

Activities of danazol

A

Weak pregestational, androgenic and glucocorticoid activities

25
Q

Danazol induces

A

Endometrial atrophy

26
Q

AEs of Danazol

A

greasy skin
acne
voice changes
weight gain

27
Q

Clinical uses of Danazol

A

For Sex hormone dependent conditions:
Endometriosis
Breast dysplasia
Gynecomastia

28
Q

What are Antiandrogens

A

are inhibitors of Testosterone synthesis

29
Q

MOA of Antiandrogens

A

GNRH analogues that inhibit LH secretion thus they inhibit Testosterone synthesis

30
Q

Name the Antiandrogens

A

Flutamide
Spironolactone
Cyproterone acetate
Goserelin
Leuprorelin
Triptorelin
Buserelin

31
Q

What is Flutamide

A

potent androgen receptor antagonists

32
Q

Indications of Flutamide

A

treats metastatic cancer: GnRH analogue
blocks action of adrenal glands

33
Q

AEs of Fluatmide

A

Gynecomastia
Galactorrhea
NV
decr. libido
Hepatotoxic

34
Q

What is Spironoloactone

A

Weak inhibitor of Androgen Rs thus weak testosterone inhibition
Aldosterone inhibitor
Competitive inhibitor of DHT at target organs

35
Q

Indications of Spironolactone

A

Hirsutism in females

36
Q

What is Cyproterone Acetate

A

its a competitve agonist to DHT
is a progestin
has antiandrogenic properties

37
Q

Indications of Cyproterone Acetate

A

Hirsutism
Severe acne

38
Q

AEs of Cyproterone Acetate

A

weight gain
decr. libido
dry vagina

39
Q

CIs of Cyproterone Acetate

A

Pregnancy: teratogenic

40
Q

What is Finasteride

A

A 5a-reductase inhibitor
–> blocks conversion of Testosterone to DHT (reversible within 4 months of therapy)

41
Q

Indications of Finasteride

A

Treatment of BPH: shrinkage of prostate gland in 3-6monthes
Male pattern baldness
hisutism

42
Q

AEs of Finasteride

A

infrequently causes impotence
RARE: decr libido, gynecomastia, erectile dysfunction, decr. ejaculation

43
Q

Pulsatile admin of GnRH analogues cause

A

incr. circulating gonadotropines–> treats infertility

44
Q

Sustained admin of GnRH analogues cause

A

reduction in steroid secretion–> treatment of hormone dependent cancer

45
Q

Indications of Goserelin

A

Breast and prostate cancer
Dysfunctional uterine bleeding

46
Q

AEs of Goserelin

A

Headache
depression
hot flushes
vaginal dryness

47
Q

Indications of Leuprorelin

A

advanced and metastatic prostate cancer
Endometriosis
Infertility

48
Q

AEs of Leuprorelin

A

Ovarian hyperstimulation
headache
mood disorders
visual disturbances

49
Q

Indications of Triptorelin

A

Advanced prostate cancer
Central precocious Puberty
Endometriosis
Infertility

50
Q

AEs of Triptorelin

A

Ovarian hyperstimulation
headache
mood disorders
visual disturbances

51
Q

Indications of Buserelin

A

Decr. Testosterone production
Advanced and metastatic prostate cancer
Endometriosis
Infertility

52
Q

AEs of Buserelin

A

hot flushes
loss of libido