Term
| Role of LH in the male? Role of FSH in the male? |
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Definition
LH acts on the Leydig cells to stimulate de novo sythesis of androgens (mainly testosterone).
FSH acts on the Sertoli cells to maintain spermatogenesis. The Sertoli cells also secrete INHIBIN, which is involved in negative feedback (on the pituitary) of FSH secretion. |
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Term
| What enzyme converts dihydrotestosterone (DHT) to testosterone? |
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Definition
|
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Term
| What does CYP19 in adipose tissue convert testosterone into? |
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Definition
|
|
Term
| What are some therapeutic uses of androgens? |
|
Definition
Male hypogonadism (testosterone deficiency)
Male senescence/andropause (age-related testosterone deficiency)
Female hypogonadism (serum levels of testosterone are below normal after ovariectomy)
Enhancement of athletic performance
Erectile dysfunction |
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|
Term
| How are androgens adminstered? |
|
Definition
| IM (oral formulations are ineffective due to high first pass metabolism and testosterone esters are highly lipophilic) |
|
|
Term
| What is the one testosterone analog to know? |
|
Definition
| Testosterone (patches and gels) |
|
|
Term
| Advantage to a testosterone patch? To a testosterone gel? |
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Definition
| Patches bypass first-pass inactivation and enable controlled release of testosterone. Testosterone gels provide more consistent release. |
|
|
Term
| Two testosterone esters to know? |
|
Definition
Testosterone enanthate
Testosterone cypionate |
|
|
Term
| Two 17 alpha-alkylated androgens to know? |
|
Definition
Methyltestosterone*
Oxandrolone |
|
|
Term
| Adverse effects of 17 alpha-alkylated androgens? |
|
Definition
Hepatotoxicity
Deleterious effects are more common with 17 alpha-alkylated compounds |
|
|
Term
| Adverse effects of synthetic androgen treatment? |
|
Definition
Decrease in testicle size with long-term use (suppression of LH secretion and intratesticular production of endogenous testosterone)
Gynecomastia
Increased LDL/Decreased HDL
Acne
Prostatic hypertrophy
Behavioral effects including excessive rage or hostility |
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|
Term
| Adverse effects of synthetic androgen treatment in women and children? |
|
Definition
Increased facial and body hair
Male pattern baldness
Acne
Enlargement of sex organs in males
Stunted growth due to premature closure of the epiphyseal plates |
|
|
Term
| Name the four categories of androgen antagonists? |
|
Definition
GnRH analogues
GnRH antagonists
Androgen Receptor antagonists
Steroid synthesis inhibitors
5alpha-reductase inhibitors |
|
|
Term
| Therapeutic used of anti-androgens? |
|
Definition
Benign prostatic hypertrophy
Palliative therapy of hormonally responsive tumors (prostate cancer)
Hirsutism in women |
|
|
Term
| What are the two GnRH analogs to know? |
|
Definition
|
|
Term
|
Definition
| For stimulation of gonadatropin (when given in PULSATILE form) or suppression of gonadotropins when give in CONTINUOUS form. |
|
|
Term
| What are the two GnRH antagonists to know? |
|
Definition
|
|
Term
| MOA of the GnRH antagonists? |
|
Definition
| They act as competitive antagonists at the GnRH receptors in the anterior pituitary. |
|
|
Term
| What are the three androgen receptor antagonists to know? |
|
Definition
Flutamide*
Bicalutamide
Spironolactone* |
|
|
Term
| Which androgen receptor antagonist is used most often? |
|
Definition
|
|
Term
|
Definition
| Mineralcorticoid with weak antiandrogenic effects (weak inhibitor of androgen receptor, weak inhibitor of testosterone synthesis) |
|
|
Term
| Therapeutic uses for androgen receptor antagonists? |
|
Definition
| Prostate cancer (Flutamide* and Bicalutamide are potent) |
|
|
Term
| What is used with androgen receptor antagonists to treat metastatic prostate cancers? |
|
Definition
GnRH analogs
Limited efficacy when androgen receptor antagonists are used alone because of a compensatory increase in LH secretion stimulates higher serum concentrations of testosterone. |
|
|
Term
| What is used to treat hirsutism in women? |
|
Definition
|
|
Term
| Adverse effects of androgen receptor antagonists? |
|
Definition
Hepatotoxicity (Flutamide, Bicalutamide)
Gynecomastia |
|
|
Term
| What is the ultimate stimulus for Benign Prostatic Hyperplasia (BPH)? |
|
Definition
|
|
Term
|
Definition
Urinary frequency
Urinary urgency
Incontinence, hesitancy, nocturia, post-voiding dribbling |
|
|
Term
| What are the two 5alpha-reductase inhibitors? |
|
Definition
Finasteride* (blocks type II only)
Dutasteride (type I and II) |
|
|
Term
| How long does it take for the 5alpha-reductase inhibitors to be effective? |
|
Definition
|
|
Term
| What can be done to relieve symptoms immediately? |
|
Definition
Combine with alpha1 blockers
Alpha1 blockers are the first line of treatment and very quick and safe. |
|
|
Term
| Side effects of 5alpha-reductase inhibitors? |
|
Definition
Impotence (rare)
Decreased libido
Erectile dysfunction
Gynecomastia
Do not donate blood
CI in pregnant women |
|
|
Term
| Other clinical uses for 5alpha-reductase inhibitors? |
|
Definition
Male pattern baldness
Hirsutism |
|
|
Term
| What three alpha1 blockers are used to treat BPH? |
|
Definition
Terazosin*
Doxazosin*
Tamsulosin* |
|
|
Term
|
Definition
| Blockade of alpha1-adrenergic receptors in bladder smooth muscle results in relaxation and decreased resistance to urine flow |
|
|
Term
| Adverse effects of alpha1 blockers? |
|
Definition
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