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Renal Pharm > Prostate Cancer and BPH > Flashcards

Prostate Cancer and BPH Flashcards

1
Q

Contraindicated for concurrent use with PDE-5 inhibitors such as sildenafil (used for ED) due to increased hypotensive effect

Severe liver dysfunction with concurrent use of potent inhibitors of
P450 enzymes (e.g., ketoconazole)
A

Alfuzosin, doxazosin, tamsulosin, and

terazosin

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2
Q

(1) are effective in reducing symptoms independent of prostate size, have no
effect on serum levels of prostate-specific antigen (a tumor marker for
prostate cancer), and are associated with less sexual dysfunction than
(2)

A
  1. α1-Adrenergic receptor antagonists

2. 5α-reductase inhibitors

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3
Q

(1) are faster acting and more effective

than (2)

A
  1. α1-Adrenergic receptor antagonists

2. 5α-reductase inhibitors

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4
Q

5α-Reductase inhibitors

Block the enzyme 5α-reductase leading to decreased conversion of testosterone to
dihydrotestosterone (the principle androgen responsible for growth
of the prostate) —> decreased prostatic volume —> widening of the urethral
lumen —> increased urinary flow

A

Dutasteride & Finasteride

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5
Q

95% of the carcinomas arise from the (1) epithelium of the prostate

A
  1. glandular
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6
Q

FSH acts on the (1) cells within the testes to promote the maturation of LH receptors and to produce an androgen-binding protein

A
  1. Sertoli
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7
Q

Any severely symptomatic patient with BPH disease complications should
undergo?

A

surgical correction

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8
Q

BPH arises from the (1) regions of the prostate gland

A
  1. central or periurethral
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9
Q

calcium channel blockers (diltiazem and verapamil) inhibit P450 enzymes and can increase levels

PREGNANCY

A

Dutasteride

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10
Q

can ameliorate the disease flare caused by the initial surge of
LH/FSH release when initiating LH-RH agonist therapy

A

Bicalutamide & flutamide: Antiandrogens; Nilutamide

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11
Q

Cardiovascular: Orthostatic hypotension
CNS: Dizziness, somnolence
Genitourinary: Impotence

Increased hypotensive effect when given with antihypertensive drugs such as β-blockers, diuretics, ACEIs, calcium channel blockers

A

Alfuzosin, doxazosin, tamsulosin, and

terazosin

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12
Q

caution should be exercised when initiating therapy in patients with widely metastatic disease involving the spinal cord or having the potential for ureteral obstruction because irreversible complications may occur

A

LH-RH agonist

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13
Q

Competitive antagonists of dihydrotestosterone (and testosterone) at the
testosterone receptor

A

Bicalutamide & flutamide: Antiandrogens

Nilutamide

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14
Q

LH complexes with receptors on the (1) cell testicular membrane and stimulates the production of testosterone and small amounts of estrogen

A

Leydig

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15
Q

(1) composed of fibrous connective

tissue and smooth muscle, which is also embedded with (2)

A
  1. the capsule, or outer shell of the prostate
  2. α1-adrenergic
    receptors
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16
Q

Contraindicated in patients taking 1. anticoagulants or 2. hormone therapy

  1. prolongs bleeding time thus the drug can increase the effect of anticoagulants such as warfarin
  2. exhibits antiandrogen and antiestrogenic activity thus it should not be taken with any hormone therapy including oral
    contraceptive and hormone replacement therapy
A

Saw palmetto

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17
Q

DHT produced at target tissues with this enzyme, causes acne, increased body and facial hair, and male pattern baldness.

A

Type I 5α-reductase

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18
Q

stromal tissue, also known as smooth muscle tissue embedded with
(1)

A

α1-adrenergic receptors

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19
Q

Epithelial tissue is under _____ control

A

androgen

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20
Q

First line for BPH

A

Alfuzosin, doxazosin, tamsulosin, and

terazosin

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21
Q

GI disturbances (diarrhea or constipation, nausea)

A

Saw palmetto

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22
Q

good first choice agent in patients with a significantly enlarged prostate (> 40 g), who cannot tolerate the cardiovascular adverse effects of α1-adrenergic receptor antagonists

A

Finasteride; Dutasteride

23
Q

Hot flashes, gynecomastia, GI disturbances (nausea, diarrhea or
constipation), liver function test abnormalities (including hepatitis)

A

Bicalutamide & flutamide

Antiandrogens

24
Q

Hot flashes, gynecomastia, GI disturbances (nausea, diarrhea or
constipation), liver function test abnormalities (including hepatitis)

can cause interstitial pneumonitis

A

Nilutamide

25
Q

How does DHT exert its physiological effects?

A

DHT exerts its physiological effects by binding with a specific cytoplasmic
receptor. This DHT-receptor complex is then transported to the nucleus of the
cell, where transcription and ultimately translation of stored genetic material
occur

26
Q

i. Disease flare-up manifested clinically as increased bone pain or
increased urinary symptoms
ii. Endocrine-related including hot flashes, impotence, and decreased
libido

A

Leuprolide; Goserelin

27
Q

i. Genitourinary: ejaculation disorders (dry sex or delayed ejaculation) and erectile dysfunction (may be due to drug-induced inhibition of NO synthesis)
ii. Endocrine: gynecomastia
iii. Pregnancy category X - suppresses levels of DHT in male fetus inhibiting development of external genital organs and leading to feminization of a male fetus

A

Finasteride; Dutasteride

28
Q

If a therapeutic dose regimen of a single drug fails, combination drug
therapy with a 5α-reductase inhibitor and an α1-adrenergic receptor
antagonist could be attempted in patients with?

A

an enlarged prostate gland that is greater than 40 g, and an elevated serum prostate-specific antigen level (>4 ng/mL)

29
Q

In target tissues with this enzyme, DHT causes prostate enlargement and prostate growth

A

Type II 5α-reductase

30
Q

Incidence of adverse effects varies among the different drugs; hypotension least likely with?

A

alfuzosin and tamsulosin

31
Q

LH-RH agonists

When administered continuously there is down-regulation of LH-RH
receptors in the pituitary which ultimately results in inhibition of
release of LH and FSH. Without LH/FSH, synthesis of testosterone
is blocked

A

Leuprolide; Goserelin

32
Q

localized to hair follicles,

sebaceous glands in the frontal scalp, liver, and skin

A

Type I 5α-reductase

33
Q

localized to the prostate, genital tissue, and scalp

A

Type II 5α-reductase

34
Q

Luteinizing hormone–releasing hormone (LH-RH) released from the
(1) stimulates the release of (2) from the (3)

A
  1. hypothalamus
  2. luteinizing hormone (LH) and follicle-stimulating hormone (FSH)
  3. anterior pituitary gland
35
Q

Monotherapy can be used as initial therapy with similar

response rates to orchiectomy

A

Leuprolide; Goserelin

36
Q

no clinically relevant drug interactions

PREGNANCY

A

Finasteride

37
Q

(1) produces prostatic secretions which are delivered into the urethra during ejaculation and contribute to the ultimate ejaculate volume

A

epithelial tissue, also known as glandular tissue

38
Q

Purported to inhibit 5α-reductase, COX-1 and COX-2, lipoxygenase, and to antagonize α1-adrenergic receptors and androgen receptors

A

Saw palmetto

39
Q

Contraindications: respiratory insufficiency

Severe hepatic impairment

A

Nilutamide

40
Q

selective for α1A-adrenergic receptor subtype which is the predominant subtype of α1-adrenergic receptor in the prostate

A

Tamsulosin

41
Q

Contraindications: Severe hepatic impairment

A

Bicalutamide & flutamide

Antiandrogens

42
Q

Stimulation of α1-adrenergic receptors by (1) causes smooth-muscle contraction, which results in an extrinsic compression of
the urethra, reduction of the urethral lumen, and decreased urinary bladder
emptying

A
  1. norepinephrine
43
Q

The growth and development of the prostate is under control of?

A

androgens

44
Q

The normal prostate is composed of a higher amount of (1) tissue
than (2) tissue, as reflected by a tissue ratio of (3). This ratio is further exaggerated to (4) in patients with BPH

A
  1. stromal
  2. epithelial
  3. 2:1
  4. 5:1
45
Q

The pathogenesis of BPH is often described as resulting from both static and
dynamic factors.
Dynamic factors relate to excessive (1) tone of the stromal component of the prostate gland, bladder neck, and posterior urethra, which results in contraction of the prostate gland around the urethra and narrowing of the urethral lumen

A
  1. α-adrenergic
46
Q

The pathogenesis of BPH is often described as resulting from both static and
dynamic factors.
Static factors relate to (1), which produces a physical block at the bladder neck and thereby obstructs urinary outflow. Enlargement of the gland depends on (2) stimulation of epithelial tissue and (3) stimulation of stromal tissue in the prostate.

A
  1. anatomic enlargement of the prostate gland
  2. androgen
  3. estrogen
47
Q

The prostate gland comprises three

types of tissue:

A

epithelial tissue,

stromal tissue, and the capsule

48
Q

used in the treatment and palliation of advanced prostate
cancer because prostatic epithelium undergoes atrophy when the normal
physiologic effect of androgens is reduced

A

androgen ablation

49
Q

When stimulated with (1), the capsule also contracts

around the urethra

A
  1. norepinephrine
50
Q

Why are α1-adrenergic receptor antagonists quickly effective in symptomatic
management of BPH? Why do 5α-reductase inhibitors only reduce an enlarged prostate gland?

A

The ratio of stromal to epithelial tissue in BPH is 5:1, and stromal tissue is embedded with alpha-1-adrenergic receptors.

51
Q

α1-Adrenergic receptor antagonists

Block α1-adrenergic receptors in the prostate and bladder neck —> relaxation of smooth muscle —> widening of the urethral lumen
—> increased urinary flow

block the three subtypes of α1-adrenergic
receptors (α1A, α1B, and α1D) equally

A

Alfuzosin, doxazosin,

terazosin

52
Q

blocks both type I and type II 5α-reductase

A

Dutasteride

53
Q

selective for type II 5α-reductase

A

Finasteride

54
Q

For advanced prostate cancer, indicated in combination with an LH-RH agonist

A

anti-androgens

Renal Pharm (14 decks)

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