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46 Cards in this Set

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1. Androgens are synthesized in:
a. Testicular Leydig cells
b. Ovarian theca cells
c. Adrenal glands
1. Androgens are Converted to dihydrotestosterone (DHT) by 5-alpha-reductase in target tissues including
a. Prostate
b. Hair follicles
c. Non-genital skin
1. Primary source of estrogens in men and postmenopausal women.
a. Testosterone is converted to estradiol in various extra-glandular tissues
1. Reduction of testosterone to DHT results in
a. Increased receptor affinity
b. More stable receptor-ligand complex
1. Esterification of androgens at C-17 results in:
a. Increased lipid solubility
b. Decreased release into general circulation
c. Longer effect
1. Alkylation of androgens at C-17 results in:
a. Decreased hepatic metabolism
b. Longer half-life
1. Androgens play a role in:
a. Development
b. Puberty
c. Fertility
d. Formation of EPO
e. Retention of electrolytes
f. And some anabolic effects
1. What role do androgens play in development
a. Development of the male phenotype
1. What role do androgens play in Puberty
a. Growth of penis and scrotum
b. Skeletal/musculature growth
c. Development of secondary sexual characteristics
d. Stimulation of sebaceous glands
e. Male pattern baldness
1. What role do androgens play in Fertility
a. Spermatogenesis,
b. maturation of sperm &
c. Controls the growth and function of the seminal vesicle and prostate.
1. Anabolic Effects of androgens
a. Muscle development
b. Pronounced in women, prepubertal boys or hypogonadal men than normal men
1. MOA of androgens
a. Testosterone and dihydrotestosterone (DHT) bind to a nuclear receptor
b. Receptor interacts with response elements in target gene
• Increased protein synthesis
c. Androgen receptor is encoded by a gene on the X chromosome.
1. Natural Androgens include
a. Testosterone
• IM injection (TESTOJECT-50)
b. Esters of testosterone:
• Testosterone cypionate (DEPO-TESTOSTERONE)
• IM injection, depot preparation
c. Dihydrotestosterone
• ANDRACTIM - topical gel, investigational
d. Transdermal testosterone:
• TESTODERM - patches applied to scrotum
• ANDRODERM - patches applied to nonscrotal skin
1. *****Daily application of 2 patches at 10 PM
a. **********plasma levels which mimic normal circadian rhythm.
1. Testosterone derivatives include
a. Fluoxymesterone (HALOTESTIN)
b. Methyltestosterone (VIRILON)
c. Oxandrolone (OXANDRIN)
• Methyl substitutions at C17
1. Methyl substitutions at C17 results in:
a. decreased hepatic metabolism
b. longer half-life
c. oral administration
1. Synthetic Androgens
a. Danazol (DANACRINE)
• Decreased hepatic metabolism
• Weak androgen
• Oral administration
1. DHEA and derivatives
a. Dehydroepiandrosterone
b. Fluasterone
1. How much of the androgens are protein bound
a. Extensively plasma protein bound (98%)
• Only 50% of testosterone in the general circulation is available
1. Metabolites of androgens
a. Primarily inactive metabolites
• Androsterone and androstenedione.
• Except small amounts of estradiol
1. Urinary excretion of androgens allows for
a. drug testing of athletes.
1. Therapudic uses of androgens
a. HYPOGONADISM - Primary use
b. Refractory Anemia
c. Hereditary Angioneurotic Edema
d. Systemic lupus erythematosus (SLE),
e. Diabetes mellitus type II
f. Nitrogen Balance/Muscle Development
g. BREAST CANCER
h. ENDOMETRIOSIS
i. ATHLETIC PERFORMANCE
1. How are androgens used for hypogonadism
a. Delayed puberty
• Primary testicular failure
• Hypopituitarism or decreased GnRH
• IM injections or patch most effective

b. Complete testicular failure or hypopituitarism
• Prolonged therapy required (years)
• Give concurrently with growth hormone for maximum effect.
• Monitor plasma testosterone concentrations
• If therapy is delayed until long after normal onset of puberty, results may be variable.

c. Alkylated testosterone derivatives should NOT be used for replacement therapy
• Risk of liver damage
1. How are androgens used for Refractory Anemia
a. Testosterone stimulates the production of renal erythropoietin
1. How are androgens used for Hereditary Angioneurotic Edema
a. Nonfunctional or decrease levels of inhibitor of 1st complement component
• Increase permeability of blood vessels and episodes of angioedema.

b. 17-alkylated testosterones increase
• Concentration of clotting factors
• Complement component inhibitors
• Action not through the androgen receptor
c. Weak androgens (danazol) are commonly used
1. How are androgens used for Systemic lupus erythematosus (SLE), and Diabetes mellitus type II
a. DHEA and fluasterone currently in clinical trials
1. How are androgens used for Nitrogen Balance/Muscle Development
a. Promote weight gain after
• chronic infection
• severe trauma
• AIDS-associated wasting syndrome
b. Drug of choice: Oxandrolone
• Dihydrotestosterone - clinical trials
• Use is controversial.
1. How are androgens used for BREAST CANCER
a. Testosterone has a palliative effect.
b. May act as an antiestrogen.
c. Conventional chemotherapy is more effective, therefore this is not a common use.
1. How are androgens used for ENDOMETRIOSIS
a. Drug of choice: Danazol (DANACRINE)
b. Normal and ectopic endometrial tissue becomes inactive and atrophic
c. Danazol also used to symptomatically treat fibrocystic breast disease.
1. How are androgens used for ATHLETIC PERFORMANCE
a. NOT AN APPROVED USE!!
b. Promote muscle growth in boys and women, little effect in normal men
c. MASSIVE pharmacological doses required, many adverse effects:
• hepatic abnormalities
• increased aggression
• psychotic episodes
What is the time frame for an SDR when material is shipped to gov't activities?
15 days from receipt
1
1. Adverse effects of androgens in males
• Prostate hyperplasia
• Decrease testicular function, decreasing spermatogenesis
• Impotence, gynecomastia
1. Adverse effects of androgens in both females and males
a. Nausea, vomiting, diarrhea
b. Altered libido, acne
c. Edema, decreased HDL/LDL ratio
d. Jaundice, cholestatic hepatitis, may lead to hepatic adenocarcinoma (alkyl substituted androgens)
1. Contraindications to androgens
a. Pregnancy
b. Prostate or breast cancer
c. Hepatic or renal disease
d. Cardiac disease
e. Children - may cause premature closure of epiphysis, serious disturbances of growth and osseous development
1. Inhibitors of androgen synthesis
a. GnRH Analogs
b. Antifungal agents
c. 5-alpha Reductase Inhibitors
d. Finasteride
1. How do GnRH Analogs affect androgens
• Suppress LH production and synthesis of testosterone
• Therapeutic Uses: Advanced prostatic cancer
• Agents: Leuprolide (LUPRON)
• Adverse effects: decrease testicular size, bone pain
• Contraindicated in pregnancy, lactation
1. how do Antifungal agents affect androgens
a. Agent: Ketoconazole (high doses), oral
b. Block cytochrome P450 enzymes
c. Therapeutic Uses - Advanced prostatic cancer
d. Adverse Effects: GI effects, impotence, hepatotoxicity
e. Drug interactions: Antacids, warfarin benzodiazepines
1. How do 5-alpha Reductase Inhibitors affect androgens
a. Competitively inhibits synthesis of DHT
b. Blocks androgen action in prostate, hair follicles and non-genital skin
c. Therapeutic Use: Benign prostatic hyperplasia, male pattern baldness
d. Agent: Finasteride (PROSCAR, PROPECIA)
1. How does Finasteride affect androgens
a. Oral administration
b. Clinical effects: 3-6 months
c. 90% plasma protein bound
d. Half-life 5-6 hours
e. Accumulates, increased plasma levels by 50%
1. ADVERSE EFFECTS of Finasteride
a. Impotence, decreased libido
b. Gynecomastia
1. Contraindications to Finasteride
a. women and children
b. hepatic function impairment
c. obstructive uropathy
1. Androgen Receptor Antagonists
a. Nonsteroidal competitive receptor antagonists
• Flutamide
• Bicalutamide
b. Nonsteroidal irreversible receptor antagonist
• Nilutamide
1. Mechanism of Action of Androgen Receptor Antagonists
• Potent antagonists of DHT
1. Therapeutic Uses of Androgen Receptor Antagonists
• Flutamide and Bicalutamide
1. Metastatic prostatic carcinoma in combination with GnRH agonists
• Nilutamide
1. Metastatic prostatic carcinoma in combination with orchiectomy
1. Adverse Effects of Androgen Receptor Antagonists
a. Hepatitis, anemia, leukopenia
• Except bicalutamide
b. GI effects, anemia
1. Drug interaction of Androgen Receptor Antagonists
a. Warfarin
1. Contraindications of Androgen Receptor Antagonists
a. Liver disease
b. Pregnancy