Androgens-valentovic Flashcards

(35 cards)

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
Oxandrolone MOA
High anabolic to androgenic ratio
26
Oxandrolone Use
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
Antiandrogens
Finasteride and dutasteride
28
Antiandrogens Finasteride and dutasteride MOA
Reduce DHT. Finasteride: competitive inhibitor of type 2 5a-reductase Dutasteride: both types 1 and 2
29
Antiandrogens Finasteride and dutasteride Use
BPH (may take 6 mos)
30
Antiandrogens Finasteride and dutasteride Combination
Combine with a1-adrenergic receptor inhibitors (tamsulosin and alfuzosin) to dec smooth mm tone and relieve bladder outlet obstruction
31
Antiandrogens Finasteride and dutasteride ADR
Lowers PSA levels by 50% Gynecomastia
32
Leuprolide MOA
GnRH agonist Down regulates LH and FSH Dec circulating testosterone
33
Leuprolide Use
Prostatic cancer Endometriosis
34
Flutamide Use
Prostatic cancer (oral) Acne (topical)
35
Flutamide ADR
Elevated liver function tests