Androgens-valentovic Flashcards

1
Q

Testosterone

Not through oral route, why?

A

Extensive first pass

Low bioavailability

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2
Q

Testosterone

Topical

Application

A

24 h depot release (applied to shoulder and upper arm)

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3
Q

Testosterone

Patch

Application

A

Applied daily

Local irritation causes compliance issues

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4
Q

Testosterone

Patch

Application

A

Not to scrotum- to much testosterone absorption

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5
Q

Testosterone

Patch

Caution…

A

Acne or abnormal hair growth in female partner

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6
Q

Testosterone

Black box for gels and topicals

A

Virilization can occur in children exposed to topical testosterone

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7
Q

Testosterone esters

A

Testosterone cypionate and enanthate

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8
Q

Testosterone esters

Application

A

Administered IM: longer duration (2-4 wks)

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9
Q

Testosterone esters

Indicated for

A

Hypogonadism

Metastatic breast cancer

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10
Q

17a-alkylate testosterone

Types and application

A

Orally effective

Methyltestosterone, fluoxymesterone

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11
Q

17a-alkylated testosterone

Methyltestosterone, fluoxymesterone

Indications

A

Hypogonadism and metastatic breast cancer

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12
Q

17a-alkylated testosterone

Methyltestosterone, fluoxymesterone

Risk

A

High abuse potential for anabolic activity

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13
Q

17a-alkylated testosterone

Methyltestosterone, fluoxymesterone

Contraindications

A

Male breast cancer

Prostate cancer

Pregnancy

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14
Q

17a-alkylated testosterone

Methyltestosterone, fluoxymesterone

ADR

A

Cholestatic hepatitis

HIGHEST RISK OF HEPATOTOXICITY

Liver cancer

Bleeding (dec clotting factors)

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15
Q

Contraindications for all testosterone analogs

A

Prostate cancer

Male breast cancer

Pregnancy

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16
Q

ADR for all testosterone analogs

A

Salt and water retention (hypertension)

GREATEST RISK OF JAUNDICE WITH 17A-ALKYLATED TESTOSTERONE METHYLTESTOSTERONE AND FLUOXYMESTERONE

17
Q

Danazol

MOA

A

Depresses preovulatory surge in output of FSH and LH

Reduces ovarian estrogen and progesterone production

Suppresses FSH and LH surge=>anovulation

18
Q

Danazol

Uses

A

Endometriosis

19
Q

Danazol

ADR

A

Weight gain

Acne

20
Q

Danazol

Contraindications

A

Pregnancy

Breast feeding

21
Q

Stanazolol

MOA

A

Inc mRNA levels and protein levels of C1, INH, and C4

22
Q

Stanazolol

Use

A

Hereditary angioedema

23
Q

Stanazolol

ADR

A

Hepatic toxicity

24
Q

Stanazolol

Contraindications

A

Pregnancy

Male breast or prostate cancer

Female breast cancer with hypercalcemia

25
Q

Oxandrolone

MOA

A

High anabolic to androgenic ratio

26
Q

Oxandrolone

Use

A

For weight gain in pts who have undergone extensive surgery or have had severe trauma or long-term corticosteroid therapy and not gained weight

27
Q

Antiandrogens

A

Finasteride and dutasteride

28
Q

Antiandrogens

Finasteride and dutasteride

MOA

A

Reduce DHT.

Finasteride: competitive inhibitor of type 2 5a-reductase

Dutasteride: both types 1 and 2

29
Q

Antiandrogens

Finasteride and dutasteride

Use

A

BPH (may take 6 mos)

30
Q

Antiandrogens

Finasteride and dutasteride

Combination

A

Combine with a1-adrenergic receptor inhibitors (tamsulosin and alfuzosin) to dec smooth mm tone and relieve bladder outlet obstruction

31
Q

Antiandrogens

Finasteride and dutasteride

ADR

A

Lowers PSA levels by 50%

Gynecomastia

32
Q

Leuprolide

MOA

A

GnRH agonist

Down regulates LH and FSH

Dec circulating testosterone

33
Q

Leuprolide

Use

A

Prostatic cancer

Endometriosis

34
Q

Flutamide

Use

A

Prostatic cancer (oral)

Acne (topical)

35
Q

Flutamide

ADR

A

Elevated liver function tests