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

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
Danazol induces
Endometrial atrophy
26
AEs of Danazol
greasy skin acne voice changes weight gain
27
Clinical uses of Danazol
For Sex hormone dependent conditions: Endometriosis Breast dysplasia Gynecomastia
28
What are Antiandrogens
are inhibitors of Testosterone synthesis
29
MOA of Antiandrogens
GNRH analogues that inhibit LH secretion thus they inhibit Testosterone synthesis
30
Name the Antiandrogens
Flutamide Spironolactone Cyproterone acetate Goserelin Leuprorelin Triptorelin Buserelin
31
What is Flutamide
potent androgen receptor antagonists
32
Indications of Flutamide
treats metastatic cancer: GnRH analogue blocks action of adrenal glands
33
AEs of Fluatmide
Gynecomastia Galactorrhea NV decr. libido Hepatotoxic
34
What is Spironoloactone
Weak inhibitor of Androgen Rs thus weak testosterone inhibition Aldosterone inhibitor Competitive inhibitor of DHT at target organs
35
Indications of Spironolactone
Hirsutism in females
36
What is Cyproterone Acetate
its a competitve agonist to DHT is a progestin has antiandrogenic properties
37
Indications of Cyproterone Acetate
Hirsutism Severe acne
38
AEs of Cyproterone Acetate
weight gain decr. libido dry vagina
39
CIs of Cyproterone Acetate
Pregnancy: teratogenic
40
What is Finasteride
A 5a-reductase inhibitor --> blocks conversion of Testosterone to DHT (reversible within 4 months of therapy)
41
Indications of Finasteride
Treatment of BPH: shrinkage of prostate gland in 3-6monthes Male pattern baldness hisutism
42
AEs of Finasteride
infrequently causes impotence RARE: decr libido, gynecomastia, erectile dysfunction, decr. ejaculation
43
Pulsatile admin of GnRH analogues cause
incr. circulating gonadotropines--> treats infertility
44
Sustained admin of GnRH analogues cause
reduction in steroid secretion--> treatment of hormone dependent cancer
45
Indications of Goserelin
Breast and prostate cancer Dysfunctional uterine bleeding
46
AEs of Goserelin
Headache depression hot flushes vaginal dryness
47
Indications of Leuprorelin
advanced and metastatic prostate cancer Endometriosis Infertility
48
AEs of Leuprorelin
Ovarian hyperstimulation headache mood disorders visual disturbances
49
Indications of Triptorelin
Advanced prostate cancer Central precocious Puberty Endometriosis Infertility
50
AEs of Triptorelin
Ovarian hyperstimulation headache mood disorders visual disturbances
51
Indications of Buserelin
Decr. Testosterone production Advanced and metastatic prostate cancer Endometriosis Infertility
52
AEs of Buserelin
hot flushes loss of libido