Burkin: Androgens Flashcards

(87 cards)

1
Q

Enzyme that converts testosterone to DHT

A

5alpha-reductase

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2
Q

Androgen receptor agonists used for anabolic effects

A

anabolic steroid

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3
Q

Genetic disease characterized by C1 esterase Inhibitor deficiency

A

hereditary angioedema

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4
Q

Androgens cause the conversion of the early bipotential gonad into (blank), (blank) of the male fetus, support (blank) production, (blank) enlargement, regulate (blank) drive and aggression, inhibit (blank) deposition, and increase (blank) mass.

A
testes;
masculinization;
sperm;
vocal chord;
sex drive;
fat;
muscle
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5
Q

Androgens are C(blank) steroid hormones

A

C19

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6
Q

95% of androgens are synthesized by the (blank), while 5% are synthesizes by the (blank)

A

testes; adrenal cortex

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7
Q

In females, androgens are synthesized in the (blank) and (blank)

A

ovaries; adrenal cortex

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8
Q

Plasma testosterone is (blank) times higher in males than in females

A

15x

2.5-10mg/day in males vs 0.3 mg/day in females

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9
Q

98% of testosterone circulating in blood is bound to (blank)

A

plasma proteins

albumin & sex-hormone binding globulin

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10
Q

The testes secrete small amounts of (blank). Larger quantities are synthesized from testosterone by their respective target cells.

A

DHT

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11
Q

A metabolite of testosterone
more potent than testosterone
produced by the adrenal cortex.

A

5alpha-dihydrotestosterone (DHT)

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12
Q

Produced from cholesterol in the adrenal cortex
precursor of natural estrogens
also known as dehydroisoandrosterone and dehydroandrosterone.

A

DHEA

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13
Q

Produced in the testes, adrenal cortex and ovaries.

converted metabolically to testosterone and other androgens

A

androstenedione (andro)

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14
Q

The steroid precursor which is believed to be the main regulator of gonadotrophin secretion in mammals.

A

androstenediol

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15
Q

What are the two active metabolites of androgens?

A

dihydrotestosterone

estradiol

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16
Q

Describe plasma testosterone levels over the course of a lifetime

A
Peak during fetal development
Drop to zero at birth
Peak in neonatal period
Drop to zero until puberty
Steady incline until adulthood
Decline in old age
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17
Q

This type of androgen increase skeletal muscle growth & stimulates erythropoiesis

A

anabolic androgens

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18
Q

This type of androgen produces the male reproductive phenotype, causes growth of male genitalia at puberty, stimulates long bone growth & eventual epiphyseal plate closure at puberty, & maintenance of male characteristics. Also increases libido & aggressive behavior.

A

androgenic androgens

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19
Q

Long acting testosterones are (blank) to allow for decreased dissolution from depo injection –> allows for infrequent administration. (blank) of the 17a position decreases hepatic metabolism allowing these agents to be administered orally.

A

esterified; alkylation (–CH3)

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20
Q

Give four uses for androgens clinically

A
  1. treatment of hypogonadism
  2. reverse negative nitrogen balance in certain catabolic states
  3. stimulate erythropoiesis in severe anemia
  4. stimulation of bone growth in children
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21
Q

infantile genitalia, long arms and legs, poor muscular development, increased body fat, reduced peak bone mass, high-pitched voice, sparse male-pattern body hair.

A

prepubertal androgen deficiency

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22
Q

How to treat prepubertal hypogonadism (androgen deficiency)?

A

therapy for 2-3 years

injections: T ethanate, cypionate, proprionate

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23
Q

17 methyl group increases oral bioavailability
Used to treat low T, post-pubertal hypogonadism, delayed puberty
frequently misused for its muscle-enhancing effects
Long term or high dose side effects:
heart disease, stroke, liver disease, ruptured tendons/ligaments, improper bone development in adolescents

A

methyltestosterone

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24
Q

When is testosterone therapy recommended in men?

A
  • *only for men with consistent symptoms AND unequivocally low serum T
  • *serum total testosterone less than 8nmol/L or serum free testosterone less than 225pmol/L

Don’t offer testosterone to older men w/ low T without clinically significant symptoms or androgen deficiency

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25
What are the sexual indications for testosterone therapy?
low libido & erectile dysfunction
26
What are the musculoskeletal indications for testosterone therapy?
osteoporosis or high risk of fracture due to low mineral density & contraindications for approved drugs for osteoporosis decreased muscle mass or strength in men greater than 65
27
What are some neuropsych indications for testosterone therapy?
impaired cognition irritability mood changes declining energy & stamina
28
This form of testosterone is given as an IM injection every 2-4 weeks
testosterone cypionate
29
This form of testosterone is given as a subQ pellet weekly
testosterone propionate
30
What are the adverse effects of testosterone therapy?
``` erythrocytosis (monitor hematocrit levels) acne, oily skin prostate cancer may increase risk of cvs events can induce/worsen OSA gynecomastia or breast tenderness reduced HDL cholesterol ```
31
Contraindications for testosterone therapy?
prostate cancer | erythrocytosis
32
``` Anabolic steroid Long half life (9.5 hrs) ~5x as potent as methyltestosterone Used to treat male hypogonadism and delayed puberty In women for breast neoplasms ```
Fluoxymesterone
33
Androgen receptor agonists used for anabolic effects mimic testosterone to build muscle tissue and promote muscle repair used to treat some breast cancers, endometriosis Large doses required to produce profound effects on skeletal muscle growth
Anabolic steroids
34
Synthetic anabolic steroid Derived from DHT High oral bioavailability Used to treat anemia & hereditary angioedema
Stanozolol **Nandrolone & Methenolone are two others
35
Side effects of anabolic steroids?
``` liver cancer or damage high blood pressure stroke heart disease/failure acne mood swings uncontrollable anger/aggression shrunken testes infertility baldness gynecomastia ``` **in women, irreversible masculinization (facial hair, deeper voice, no menses, smaller breasts)
36
What is cyproterone acetate used for?
severe hirsutisms
37
What is flutamide used for clinically?
in combo w/ GnRH analogs for metastatic prostatic carcinoma
38
What is finasteride used for clinically?
BPH
39
testosterone derivative mild androgenic activity Indirectly reduces estrogen production by lowering the output of FSH & LH. inhibits adrenal and gonadal steroidogenesis (binds to numerous steroid hormone receptors and blocks the synthesis of estradiol, progesterone, testosterone, and glucocorticoids) Used to treat endometriosis and hereditary angioedema
Danzol
40
Absence of GnRH | Virilization and fertility can be achieved when FSH and LH are given to stimulate testis function.
gonadotrophin deficiency (Kallmann syndrome)
41
Other syndromes that lead to GnRH deficiency?
Prader-Willi syndrome | Bardet-Biedl syndrome
42
Plasma FSH normal, serum LH and testosterone are low.
Isolated LH deficiency | "Fertile Eunuch"
43
Patients are normally virilized Testicular size is normal, and LH and T levels are normal. FSH levels are uniformly low and do not respond to stimulation with GnRH
Isolated FSH deficiency
44
In this disease, pituitary or testicular microinfarcts may cause infertility
sickle cell anemia
45
What effects does excess estrogen have on gonadotropin secretion? On testis?
decreases gonadotropin secretion | causes testis failure
46
What things can cause excess estrogen?
sertoli cell tumors obesity hepatic cirrhosis
47
What things can cause excess androgens?
anabolic steroids adrenal or leydig cell tumors CAH
48
What do excess glucocorticoids do to LH secretion? The the testis?
depress LH secretion; induce secondary testis failure
49
(blank) balance is important for normal hypothalamic hormone secretion and sex hormone-binding protein levels that govern the T:E ratio.
thyroid
50
0.5% of infertile men have deficient responses to (blank) and (blank) treatment improves semen quality
growth hormone
51
Excess or deficiencies in these hormones can cause infertility
``` excess estrogen excess androgens excess glucocorticoids hypo or hyperthyroidism growth hormone hyperprolactinemia pituitary insufficiency in general ```
52
What are some gonadotoxins that cause infertility?
radiation drugs: ketoconazole, spironolactone, alcohol all inhibit T synthesis Cimetidine is an androgen antagonist marijuana, heroin, methadone lower T
53
These systemic diseases decrease fertility
renal failure liver cirrhosis sickle cell disease
54
These are defects in androgen activity that can lead to infertility
5-alpha reductase deficiency | androgen receptor deficiency
55
These are injuries that the testis can undergo, which can lead to infertility
orchitis torsion trauma
56
What is crytorchidism? Why is it dangerous? What is performed by two years of age in this condition?
undescended testicle; increased risk of infertility & cancer; prophylactic orchidopexy (repair) performed at 2 yrs of age
57
Dilated and tortuous scrotal veins surgically correctable. 15% of all men and 40% of infertility patients
Varicocele
58
25-50% of cases of infertility are (blank)
idiopathic
59
This accounts for 1-2% of infertility cases 80% of these patients will have a detectable CF mutation The vas deferens, seminal vesicles, and ejaculatory ducts are usu atrophic or absent, causing obstruction
CAVD - congenital absence of the vas deferens
60
What are some other congenital blockages of the reproductive tract that lead to infertility?
Young syndrome (abnormally viscous mucous) Idiopathic epididymal obstruction Adult polycystic kindey disease Blockage of ejaculatory ducts
61
What are some acquired blockages of the repro tract that lead to infertility?
vasectomy groin/hernia surgery E.coli or chlamydia
62
What are some things that can cause a functional blockage of the reproductive tract and lead to infertility?
nerve injury or medications can impair contractility of seminal vesicle or vasal musculature
63
Abnormalities in the motor apparatus or axoneme of sperm and other ciliated cells nonmotile but viable sperm in normal numbers
immotile cilia syndromes
64
After vasectomy reversal due to elevated epididymal intratubular pressure and epididymal dysfunction normal sperm counts but sperm do not regain the usual maturation and motility capacities
maturation defects
65
Implicated as a cause of infertility in 10% of infertile couples
immunologic infertility
66
These things can cause disorders of sperm function or motility
immotile cilia syndromes maturation defects immunologic infertility infection
67
What are some disorders of coitus...?
impotence: low libido or ED penile abnormalities: abnormal curvature, phimosis, hypospadias --> result in placement of the semen too far from the cervix
68
What kinds of things are associated with pyospermia, or elevated numbers of leukocytes in the semen? What can be done to treat pyospermia?
subclinical GU tract infection elevated ROS poor sperm function & infertility; treat both partners with antibiotics!
69
What is immunologic infertility?
corticosteroid suppression of the immune system **IVF and ICSI are effective
70
What to use for hyperprolactinemia?
bromocriptine
71
What to use for hypothyroidism?
replacement of low TSH or removal of excess!
72
excessive androgen levels suppress GnRH rare and classically presents as precocious puberty treated with corticosteroids.
congenital adrenal hyperplasia (21-hydroxylase deficiency)
73
What can you do for testosterone excess or deficiency?
GnRH replacement in a pulsatile manner by a portable infusion pump jump start the testis with hCG & FSH
74
What can be done for idiopathic infertility?
Clomiphene citrate --> for low sperm count, acts as an antiestrogen by blocking the action of estrogen on the male axis
75
up to 40% of infertile men have increased (blank) levels in the reproductive tract (blank) scavengers may protect sperm from damage
ROS; free radical **glutathione, Vit E
76
may become a new and effective treatment for oligospermia
growth hormone!!!!
77
What are some meds associated with impaired ejaculation in men?
antihypertensives alpha-blockers: prazosin, phentolamine, thiazides antipsychotics: mellaril, haldol, librium antidepressants: SSRIs, imipramine, amitriptyline
78
What happens when men get an erection?
stimulus --> release of NO from nerves --> smooth muscle relaxation --> blood flow dramatically increases --> veins get compressed which blocks outflow
79
Explain how NO is involved in an erection...
NO --> GC --> converts GTP to cGMP --> activates a protein kinase --> stimulates uptake of Ca++ by the ER --> reduces levels of cytoplasmic Ca++ cause the muscle cells to relax --> vasodilation
80
T/F: Both physical and emotional problems can lead to erectile dysfunction...
True ``` Physical: Heart Disease Clogged blood vessels (atherosclerosis) High blood pressure Diabetes Obesity Metabolic syndrome, a condition involving increased blood pressure, high insulin levels, body fat around the waist and high cholesterol Parkinson's disease Multiple sclerosis Low testosterone ``` Emotional: Depression Anxiety Mental health conditions Stress Relationship problems due to stress, poor communication or other concerns Sometimes a combination of physical and psychological issues causes erectile dysfunction
81
This enzyme terminates the signal for erection by converting cGMP to GMP
phosphodiesterase (PDE)
82
Oral administration of (blank) inhibitors increases blood flow to the penis and offsets ED
PDE-5
83
Four drugs used for erectile dysfunction
Sildenafil (Viagra) Vardenafil (Levitra) Tadalafil (Cialis) Avanafil (Stendra)
84
Contraindications for penis pills?
``` nitrate drugs blood thinners alpha blockers for enlarged prostate heart disease/failure stroke hypotension or hypertension uncontrolled 'betes ```
85
Side effects of viagra?
vision probs | blindness
86
Two types of priapism?
non-ischemic: usu from an injury to the penis/peritoneum - often goes away on its own ischemic: blood flows into the penis but can't flow out --> loss of circulation, can damage erectile tissues or perma loss of function
87
What can be done for ischemic priapism?
therapeutic aspiration --> draw blood from the penis | inject sympathomimetic agents: phenylephrine (less cardiovascular effects) or epi