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Pharmacology > Steroids > Flashcards

Steroids Flashcards

1
Q

What are Anabolic Steroids?

A

Small cholesterol based drugs related to the endogenous androgenic endocrine hormones, including testosterone.

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2
Q

What are two main important actions of steroids?

A
  1. Androgenic. 2. Anabolic.
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3
Q

What is the androgenic action of steroids?

A

Promotes male characteristics.

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4
Q

What is the anabolic action of steroids?

A

Promotes protein synthesis/build lean muscle mass.

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5
Q

What are endogenous steroid hormones? How do they work?

A

Small lipid-based hormones based on cholesterol. They activate intracellular receptors that act as hormone regulated transcription factors.

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6
Q

What do Glucocorticoids do?

A

They regulate inflammation and metabolism.

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7
Q

What do Mineralocorticoids do?

A

They regulate fluid and salt balance.

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8
Q

What do sex steroids do?

A

They regulate reproductive physiology, bone density, muscle mass, etc.

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9
Q

Where is testosterone produced?

A

Leydig cells in the testes.

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10
Q

What part(s) of the brain regulate the production of testosterone and the creation of sperm?

A

Endocrine signals from the hypothalamus/anterior pituitary,

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11
Q

When do Leydig cells synthesize testosterone?

A

When LH binds to the extracellular LH receptor on the Leydig cell.

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12
Q

What are the metabolites of testosterone metabolized by?

A

By cytochrome p450 enzymes.

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13
Q

What is testosterone? What is it converted into and why?

A

The major form of androgen in circulation. It can be converted to dihydrotestosterone (DHT). It is 10x more potent and is converted to this form to target peripheral tissues.

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14
Q

What converts testosterone into DHT?

A

5-alpha-reductase.

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15
Q

How are testosterone concentrations kept up in the testis? Is testosterone converted into DHT in the testes.

A

By androgen binding proteins synthesized by Sertoli cells in the seminiferous tubes. It is not converted in the testes (thus, the concentration must be kept up).

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16
Q

What do Sertoli cells do?

A

They stimulate spermatogenesis.

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17
Q

How are hormones transported to their target tissues?

A

After synthesis, they diffuse into the plasma. Then they bind to carrier proteins including sex-hormone binding globulin (SHBG) and Albumin. They can diffuse out of the blood and cross freely into target tissues.

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18
Q

What are androgen receptors? What happens when an androgen binds?

A

An intracellular receptor that trans-locates into the nucleus, binds DNA, and alters transcription upon androgen binding.

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19
Q

What disorder is caused by mutations in androgen receptors?

A

Androgen Insensitivity Syndrome (AIS). Genetically XY, but are female.

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20
Q

What are reasons to antagonize androgen action? (Anabolic steroids would make them worse.)

A

Treatment of: prostate cancer, male pattern baldness, benign prostatic hyperplasia.

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21
Q

What are two ways to antagonize androgen?

A
  1. Use GnRH agonists. 2. Use GnRH receptor antagonists.
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22
Q

How does using GnRH agonists antagonize androgen activity?

A

They suppress the hypothalamus-pituitary-gonadal axis, which decreases the production of FSH and LH, which shuts down testosterone production.

23
Q

What can GnRH agonists treat? How is it administered?

A

Prostate cancer and some breast cancers. It is administered continuously.

24
Q

How does using GnRH receptor antagonist reduce androgen activity?

A

They block the release of FSH and LH.

25
Q

How do 5-alpha-reductase inhibitors work?

A

They block the conversion of testosterone into the more potent DHT.

26
Q

What can 5a-reductase inhibitors do to prostate tissue?

A

Slows the growth of prostate tissue and cause cell death.

27
Q

What is Finasteride?

A

It is a selective inhibitor of type 2 5a-reductase.

28
Q

What can topical Finasteride (Propecia) treat?

A

Male-pattern baldness.

29
Q

What can oral Finasteride treat? How much can it reduce prostate size in one year?

A

Benign prostatic hyperplasia (BPH). It can reduce prostate size by up to 25%.

30
Q

What are the adverse effects of oral Finasteride?

A

Decreased libido and erectile dysfunction.

31
Q

What is the mechanism of action for androgen receptor antagonists? (Not 5a reductase.)

A

Completely inhibits the binding of endogenous androgens to the androgen receptor.

32
Q

What are 3 androgen receptor antagonists?

A
  1. Flutamide. 2. Enzalutamide. 3. Bicalutamide.
33
Q

What are Androgen receptor antagonists used to treat?

A

Metastatic prostate cancer and benign prostatic hyperplasia.

34
Q

What is CYP17?

A

An enzyme needed for the synthesis of androgens, including testosterone.

35
Q

What is Abiraterone (Zytiga)? What can it be used for?

A

A CYP17 inhibitor. It can be used in the treatment of castration-resistant prostate cancer.

36
Q

What are some medical uses of Anabolic steroids?

A

Hormone deficiency, treat muscle loss associated with trauma or disease. Gender re-assignment. Anti-aging (controversial) and male contraceptive (experimental).

37
Q

What is hypogonadism? Can the treatment be administered orally?

A

Not enough male hormones are made. Can’t be administered orally because it is subject to first-pass metabolism by the liver.

38
Q

What is Enanthate?

A

Inject-able testosterone.

39
Q

What is Cypionate?

A

Inject-able testosterone.

40
Q

How are Enanthate and Cypionate administered? What does it do?

A

Intramuscularly every 2-4 weeks. It increases plasma testosterone to the normal level.

41
Q

What are the two types of pill contraceptives for women?

A
  1. Estrogen/progestin combinations. 2. Progestin only.
42
Q

How do Estrogen-progestin combination contraceptives work?

A

Suppresses GnRH, LH, and FSH secretion and follicular development. It works to primarily prevent ovulation.

43
Q

What are two progestin-only contraceptive drugs?

A

Norgestrel and Norethindrone.

44
Q

How are progestin-only contraceptives thought to prevent ovulation?

A

They alter the frequency of GnRH pulsing and decrease anterior pituitary gland responsiveness to GnRH.

45
Q

How effective are progestin-only drugs in preventing ovulation?

A

They prevent it 70-80% of the time.

46
Q

How effective are progestin-only contraceptive drugs in preventing pregnancy?

A

96-98%.

47
Q

Why are progestin-only contraceptive drugs ~97% effective instead of ~75%?

A

Due to secondary mechanisms: alterations in cervical mucus, endrometrial receptivity, and tubal peristalsis.

48
Q

What is the goal of male contraceptives?

A

To suppress endogenous production of sperm reversibly.

49
Q

What male contraceptives based on testosterone have been tried? How do they work?

A

Testosterone enanthate which significantly suppresses gonadotropin release, resulting in reduced levels of LH and FSH that can’t stimulate Sertoli cell function.

50
Q

What 2 male contraceptives based on androgen and progestin have been tried?

A
  1. Testosterone enanthate and levonorgestrel. 2. Testosterone undecanoate and inject-able medroxyprogesterone acetate.
51
Q

How effective were male contraceptives based on androgens and progestin at creating azoospermia in the population on average?

A

Only about 60% of men achieved the state.

52
Q

Do Anabolic steroids increase strength and muscle mass without exercise?

A

Yes.

53
Q

What are some side-effects of using anabolic steroids?

A

Hypertension, liver damage, male infertility, acne, mood/behavior changes, early death.

54
Q

How can you detect steroid use?

A

By measuring the ratio of testosterone to its metabolites, such as epitestosterone. >4:1 is evidence of use.

Pharmacology (20 decks)

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