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Pharmacology -- Test #5 > Pharmacology of Androgens and Anabolic Steroids > Flashcards

Pharmacology of Androgens and Anabolic Steroids Flashcards

1
Q

Cyp 11A1 / 20,22 desmolase converts….

A

Cholesterol to Pregnenalone

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2
Q

Cyp 17A1/ 17 alpha hydroxylase converts…

A

Pregnenalone to 17a-hydroxypregnenolone

Progesterone to 17a-hydroxyprogesterone

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3
Q

C17,20 lyase/desmolase converts…

A

17a-hydroxypregnenolone to Dihydroepiandosterone

17a-hydroxyprogesterone to Androstenedione

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4
Q

17beta hydroxysteroid dehydrogenase is used to make…

A

Androstenediol and Testosterone

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5
Q

Important details on transport of androgens

A

2% free
SHBG 65%
albumin binds the rest weakly

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6
Q

SHBG is increased by… decreased by…

A

inc – estrogen, thyroid hormone

dec. – androgens, GH, obesity

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7
Q

How are androgens degraded?

A

Metabolized in the liver to inactive 17-ketosteroids

Excreted as conjugates of glucuronic and sulfuric acids

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8
Q

How are androgen molecules altered when given medicinally

A

Decrease absorption and/or decrease degradation and inactivation by the liver

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9
Q

Describe type A androgen preparations

A

Esterified Androgens

Makes it more soluble in lipid vehicles for injection. Slow release into the Blood stream

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10
Q

Describe type B androgen preparations

A

alkylation of androgens at 17alpha position

Retarded liven inactivation

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11
Q

Describe type C androgen preparations

A

Changes in the ring structure

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12
Q

Six clinical uses of androgenic and anabolic steroids

A

Androgen Replacement in Men
Protein Anabolic Agents
Growth Stimulators (Pituitary Dwarfish)
Endometriosis (use weak ones - Danazol)
Osteoporosis (Not anymore, now bisphosphonates)
Stimulation of Erythropoesis (Not anymore, now EPO)

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13
Q

Why can’t pregnant women have androgens?

A

Will fuck up the baby’s external genetalia

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14
Q

Contraindications for use of androgens

A

Pregnant women
Men with prostate or breast cancer
Infants

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15
Q

Important Androgens/Anabolic Steroids to remember

A 
Fluoxymesterone
Methyltestosterone
Nandrolone decanoate
Oxandrolone
Oxymethalone
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16
Q

Antiangrogens are used int he treatment of…

A

Hyperplasia/Carcinoma of the prostate
Acne, Baldness
Virilizing syndromes in females
Precocious puberty in boys

17
Q

Which antiandrogens inhibit synthesis

A

GnRH agonists+antagonists
Spironolactone
Ketoconazole

18
Q

Which antiandrogens block androgen action

A

Cyproterone Acetate
Flutamide
Finazteride (inhib. 5alpha reductase)

19
Q

How does GnRH inhibit testosterone synthesis?

A

Uncoupled GnRH receptors from their effectors, causing them to internalize.
Depletion of LH stores

20
Q

Important details about Abiraterone

A

Inhibits 17 alha hydroxylase

Used for metastatic prostate cancer

21
Q

Important details for spironolactone as an antiandrogen

A

Aldosterone Agonist with weak antiandrogenic properties.
Inhibits Cytochrome P450 used in synthesis
Competes with DHT and Testosterone for androgen receptor

22
Q

How does ketoconazole block adrenal/testicular androgen synthesis

A

Inhibits C 17,20 Lyase and cholesterol side chain clevage enzymes

23
Q

Which drugs block androgen action by competing for binding of testosterone and DHT at androgen receptor (5)

A
  1. Cyproterone Acetate
  2. Flutamide
  3. Bicalutamide
  4. Nilutamide
  5. Cimetidine
24
Q

Use Cyproterone Acetate to treat..

A

acne, baldness, hirsuitism, virilizing syndroms
Precocious puberty
Prostatic hypertrophy + carcinoma
Forced castration of convicts

25
Q

Flutamide is typically used to treat…

A

Prostatic Cancer

26
Q

Bicalutamide is typically used to treat…

A

Early Prostate Carcinoma

Hirsutism

27
Q

Nilutamide is typically used to treat…

A

Advanced Prostate Cancer

28
Q

Cimetidine is typically used to treat….

A

Peptic Ulcer Disease (H2 antagonist)

Hirsutism in women

29
Q

Main drugs that work by inhibiting 5alpha reductase

A

Finasteride (Benign Prostatic Hyperplasia, baldness)

Dutasteride (Benign Prostatic Hyperplasia)

Pharmacology -- Test #5 (12 decks)

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