Male Reproductive Meds

Question 1

androgen effects? primary androgen? where does it come from?

Answer 1

anabolic and masculinizing effects in males and females
primary androgen is testosterone
testosterone comes from Leydig cells in testes and in smaller amounts from the ovaries and cells of the zona reticularis in the adrenals

Question 2

testosterones target organs and effects?

Answer 2

brain: libido, mood
muscle: increase strength and volume
KD: stimulation EPO production
bone marrow: stimulate growth of stem cells
bone: accelerated linear growth, close epiphyseal plates
max sex organs: penile growth, spermatogenesis, prostate growth and fxn
liver: synthesis of serum proteins
skin: hair growth, balding, sebum production

Question 3

MOA of testosterone?

Answer 3

MOA of testosterone and all biologic and synthetic analogs is the alteration of gene transcription
attach to specific nuclear receptors and initiate a cascade of rxns that eventually result in alteration of gene transcription

Question 4

enzymes that metabolize testosterone? more active form of testosterone? 2 primary effects and overall effects?

Answer 4

testosterone is metabolized by 5-alpha reductase to dihydrotestosterone, also metabolized to estrogen by aromatase
androgenic effects: development of male genitalia, secondary male characteristic development as well as sperm production and male fertility and libido
anabolic effects: protein metabolism and development of muscle, bone mass and bone strength
also increases RBC production

Question 5

lifestyle things that decrease T?

Answer 5

falling in love and fatherhood (suggesting this promotes emotional and behavioral changes)

Question 6

when can exogenous T be used?

Answer 6

F to M transitioning
in males w/inadequate T production (hypogonadism)
to promote skeletal growth in pre-pubertal boys w/pituitary dwarfism

Question 7

manifestations of pre-pubertal hypogonadism?

Answer 7

infertility
abn of sexual fxn
alterations in behavior (irritability, depression)
loss of muscle mass and tone
increased rate of osteoporosis
possible loss of 2ndary sexual characteristics

Question 8

indications for T administration?

Answer 8

bone marrow stimulation, anemia
severe osteoporosis
hormone tx for transsexual men
unapproved use is as an androgenic steroid to increase lean body mass, muscle strength, anti-aging

Question 9

routes of administration of T? most efficacious? least efficacious?

Answer 9

IM, oral, buccal or sublingual lozenges, transdermal skin patches, transdermal creams or gels
most efficacious delivered IM or as a patch
oral is the least efficacious b/c of inactivation by 1st pass metabolism, can also increase risk of liver dz (hepatitis, hepatic carcinoma)

Question 10

ratio of androgenic:anabolic activity in exogenous T preparations?

Answer 10

1:1

Question 11

adverse effects of exogenous T?

Answer 11

acne
baldness
gynecomastia
priapism
increased risk of prostatic hyperplasia and prostatic CA
exacerbation of sleep apnea and subsequent reduction in sperm count and infertility
in children can cause abn rate of sexual maturation, can result in diminished ht dt premature closure of growth plates
abn lipid levels: increase LDL, lower HDL
increase risk of CAD and atherosclerosis
fluid retention
edema
increased RBCs can lead to increased risk for ischemia

Question 12

excess androgens in females can cause?

Answer 12

virilization such as excess body and facial hair, acne, deepening of voice, clitoral enlargement, menstrual irregularities

Question 13

class of T? indications? MOA? how to give? dosing?

Answer 13

class: androgenic hormone
indications: T replacement for anabolic and/or androgenic effects
MOA: alters gene transcription
give IM or patch preferably but can also use SL lozenges
dosed daily for patches or gel or one dose every 1-2 wks if IM

Question 14

what are anabolic steroids? approved uses?

Answer 14

synthetic derivatives of T which have anabolic effects that are greater than androgenic effects
approved to tx refractory anemia, severe osteoporosis, severe wasting conditions such as AIDS and CA
but muscle building capacity has led to widespread abuse

Question 15

what is anti-androgen tx? when is it used?

Answer 15

most often used for tx of advanced prostate CA: normal prostate tissue growth is regulated by T and DHT and androgen deprivation aims to prevent androgen-stimulated tumor growth
palliative, does not provide a cure

Question 16

class of leuprolide/lupron? indications? MOA? how to give? SE?

Answer 16

class: anti-androgenic hormone and anti-E hormone
indications: prostatic CA, precocious puberty, endometriosis, uterine fibroids, some protocols of IVF
MOA: synthetic analog of GnRH, interrupts production of T and E
give SQ, IM
SE: decreased libido, impotence, N/V, hot flashes, night sweats, arthralgias, myalgias, osteoporosis

Question 17

finasteride/proscar class? indications? high vs low dosing? MOA/

Answer 17

class: anti-androgen
indications: benign prostatic hyperplasia
in lower doses used to tx male-pattern baldness, in higher doses used to tx prostate CA
MOA: limits conversion of T to dihydrotestosterone by inhibiting type II 5-alpha reductase

Question 18

how to give finasteride/proscar/propecia? warning to women who are PG? SE?

Answer 18

PO, once daily dosing, no blood donation while taking proscar
women who are PG should not handle crushed or broken tablets b/c of risk of birth defects
SE: decreased libido, ED, impotency, depression, breast swelling and tenderness

Question 19

two meds for management of BPH? which is used as initial tx? MOA of intial tx? common SEs of initial tx?

Answer 19

5-alpha reductase inhibitors and alpha blockers
alpha blockers are commonly used as initial therapy in men w/BPH
MOA of alpha blockers: relax SM in prostate and bladder neck
SEs of alpha blockers: weakness, orthostatic hypotension, nasal congestion

Question 20

what are phosphodiesterase type 5 inhibitors used for? MOA? other uses dt MOA?

Answer 20

used for ED
block the degradative action of phosphodiesterase type 5 on cyclic GMP in SM cells lining the bvs supplying the corpus cavernosum of the penis
can also be used to tx pulmonary HTN as PDE5 is also present in arterial wall SM w/in the lungs

Question 21

class of sildenafil citrate/viagra? indications? MOA?

Answer 21

class: PDE5 inhibitor
indications: ED, pulmonary HTN
MOA: protection of cGMP from degradation by cGMP specific phosphodiesterase type 5 in the corpus cavernosum and arterial lining of lungs, NO binds to receptors of guanylate cyclase which = increased levels of cGMP = SM relaxation = vasodilation and increased blood flow

Question 22

should sildenafil cause an erection w/o sexual stimulation?

Answer 22

no b/c w/o sexual stimulation there is no activation of NO/cGMP system

Question 23

C/I to take sildenafil citrate/viagra?

Answer 23

should not be used by pts on NO donors, organic nitrites, nitrates, sexual intercourse is C/I dt CV risk factors such as recent stroke or MI, severe renal or liver fxn impairment, hypotension, hereditary degenerative retinal d/os

Question 24

adverse effects of sildenafil citrate/viagra?

Answer 24

H/A, flushing, dyspepsia, nasal congestion, impaired vision (photophobia, blurred vision), cyanopsia (blue tinted vision)
rare but serious adverse effects include increased intraocular P and acute angle closure glaucoma, ventricular arrhythmias, severe hypotension, MI, stroke, priapism