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T/F: Testosterone is produced 100% by the testes
False; 95% produced by the testes and 5% by adrenal
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DHT is produced via ______ from ____
- 5-alpha reductase
- Testosterone
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Continuous GnRH receptor stimulation would _____ LH secretion and testicular testosterone production
Stop
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Anti-testosterone treatment strategies?
- Stop LH secretion and testicular testosterone production
- Remove testes (orchiectomy)
- Inhibit conversion of T to DHT
- Block androgen receptor
- Inhibit enzyme involved in androgen synthesis
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Symptoms of BPH:
- Urinary frequency
- Nocturia
- Weak stream
- Hesitancy
- Incomplete emptying
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Which drugs can exacerbate BPH symptoms?
- Antihistamines
- Phenothiazine
- Tri-cyclic antidepressants
- Anticholinergic
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What are Prostate drug targets in the management of BPH?
- 5 alpha reductase enzyme in the prostate
- Sympathetic alph-1a receptor in bladder and prostate
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Bladder outlet obstruction of BPH include _____ and ____ components
- Dynamic (physiologic, reversible)
- Fixed (structural)
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Which two classes of drugs are used to act upon the dynamic and fixed components of bladder outlet obstructions?
- Alpha-adrenergic antagonist
- 5-alpha reductase inhibitors
-
Agents of 5-alpha reductase inhibitors:
-
Finasteride and/or dutasteride cane prevent the formation of _____
Dihydrotestosterone
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Alpha-1 adrenoreceptors have which effects?
Promotes contraction of the smooth muscle of peripheral blood vessels, Bladder neck, prostate capsule and prostate fibromuscular stroma
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Alpha-1____ receptors are mainly located in non-vascular muscle, and Alpha-1____ receptors are located in vascular smooth muscle
-
Blood pressure is regulated via ______ receptors
Alpha 1B
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Which alpha adrenoreceptors are predominantly found in the prostate?
Alpha 1a
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Postsynaptic blockade of alpha 1 adrenergic receptors would _______ prostatic urethral resistance
Decrease
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What is the suffix of alpha-1 blocker drugs?
“-Osin”
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Which agents of alpha-1 blockers are selective for alpha 1-A
- Tamsulosin
- Silodosin
- (these are used for BPH)
-
Side effects of alpha-blocker?
- Tiredness
- Dizziness
- Postural hypotension
- Retrograde ejaculation
-
Side effects of 5 alpha reductase inhibitors?
- Reduced libido
- ED
- Gynecomastia
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Which class of drug could stop BPH progression?
5 alpha reductase inhibitors
-
Which class of drug could decrease prostate size?
5 alpha reductase inhibitors
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Of the two classes of drugs used to treat BPH, which has a peak onset that is 1-6 weeks? Which is 6 months to 1 year?
- 1-6 weeks: alpha 1 blocker
- 6 months to 1 year: 5 alpha reductase
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Targets in the management of prostate cancer:
- Gonadotropin releasing hormone receptor
- Androgen receptor in prostate
- Inhibit enzymes involved in androgen synthesis
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______ is medical/surgical castration, a therapy method for prostate cancer
- Androgen deprivation therapy
- LHRH agonist or antagonists
-
Which drug blocks androgen synthesis?
Abiraterone
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Which drug is used for castration-resistant prostate cancer?
Abiraterone (always used with prednisone)
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What is the MOA of Abiraterone?
- Inhibits enzyme CYP17
- Inhibit androgen/testosterone production by the testes, adrenal gland and prostate cancer cell
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T/F: Abiraterone only blocks testosterone production in the testes, has no effect in adrenal gland testosterone production
False; it blocks adrenal gland CYP17
-
T/F: LHRH is synonymous as GnRH
True
-
What are agents of GnRH receptor agonists?
- Leuprolide
- Histrelin
- Goserelin
- Triptoerilin
-
What are indications for GnRH agonist/ antagonist use?
- Infertility
- Endometriosis
- Precocious puberty prostate cancer
-
What is an agent of GnRH antagonist?
Degarelix
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Testosterone production by the testis is inhibited with ______ use
Sustained non-pulsatile administration of GnRH agonist
-
What are two options to decrease LH secretion?
- GnRH pituitary receptor blocker
- Sustained non-pulsatile GnRH
-
Side effects of GnRH agonist/antagonist male medical castration:
- Hot flashes
- Anemia
- Cognitive decline
- Erectile dysfunction
- Loss of libido
- Fatigue
- Gynecomastia
- Hyperlipidemia
- Weight gain
- Osteoporosis
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GnRH ______ has an initial flare of LH and FSH, vs GnRH____ does not.
-
_____ should precede or be co-administered with LHRH agonist and be continued in combination for at least 7 days for patients with prostate cancer
Antiandrogen therapy
-
What is the suffix of anti-androgens?
“-Lutamide”
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Why is prednisone always given with abiraterone?
Abiraterone given with oral prednisone to prevent hypertension and hypokalemia due to hyperaldosteronism
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T/F: 5 alpha reductase inhibitor is not effective in prostate cancer management
True; it is used to treat BPH
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