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DT4-Exam 1 > Pharm-IL-Androgens-Leah : ) > Flashcards

Pharm-IL-Androgens-Leah : ) Flashcards

1
Q

Failure of testes to make testosterone is called ____?

What levels define failure?

A

Hypogonadism

Defined as levels below 300 ng/dl in males under 30.

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2
Q

Signs of low testosterone (4)?

A
  • decreased energy
  • decreased libido
  • loss of muscle mass/ bone (osteoporosis)
  • anemia

*Just remember its like being in medical school + anemia

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3
Q

In hypogonadism, how is testosterone administered and why?

A
  • IM 2-3x/week or transdermal, but NOT orally

- low oral bioavailability

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4
Q

How/ where is transdermal testosterone applied?

A
  • gel, patch or buccal preparations
  • gel/patches replaced every 24 hours, usually placed on arm, abdomen, back but NOT scrotum
  • buccal patches applied to gums 2x/day
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5
Q

Why aren’t testosterone patches placed on the scrotum?

A
  • potential for very high absorption.

- Scrotum has very thin skin, therefore ^^ absorption

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6
Q

For what healthcare procedures must testosterone patches be removed?

A

-During an MRI due to aluminum content

activated aluminum can cause burns!!

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7
Q

How do testosterone patches affect female partners?

A

-Female should avoid physical contact with the patch, as laying on it (for example) may lead to abnormal hair growth

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8
Q

What black box warning is assc with testosterone patches?

A
  • Can cause virilization in children

- DO NOT allow children to contact the patch

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9
Q

What are testosterone cypionate and enanthate; how are they administered?

A
  • testosterone esters
  • prodrug: convert to testosterone in body
  • must be given IM every 2-4 weeks.
  • ^^^ lipophilicity –> lasts longer in the body
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10
Q

In addition to hypogonadism, for what purpose might testosterone enanthate be used?

A

-female metastatic breast cancer, antagonizes estrogen

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11
Q

17a alkylated testosterone: social implication? normal use?

A
  • THIS is the testosterone abused as an anabolic steroid

- intended for the same uses as testosterone, hypogonadism and met. breast cancer in females

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12
Q

Two specific 17 a alkylated testosterones?

A
  • Methyltestosterone
  • Fluoxymesterone

(remember: methyl + fluoxy)

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13
Q

What are the ADRs assc with (alkylated) testosterone (4)?

A

Cause Edema and Liver toxicity:

  • LIVER cancer
  • Decreased LIVER clotting factor synth (2,5,7, 10)
  • Cholestatic HEPatitis=jaundice + bleeding

*Essentially the same as all testosterones, but more severe (all = liver tox/cancer and edema)

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14
Q

When are (all) testosterone analogues contraindicatied? (3)

A
  • prostate cancer
  • pregnancy
  • MALE breast cancer
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15
Q

ADRs assc with (ALL) testosterones/ analogues (3)?

A
  • edema –> HTN
  • jaundice
  • hepatic carcinoma

(ADRs similary but amplified in alkylated versions)

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16
Q

Danazol:
Describe the compound –what is its MOA (3)?
Anabolic or androgeneric?

A

19-Nortestosterone derivative interacts w/ steroidR’s:
Supresses FSH/LH surge–> decreased ovarian E+P–> causes anovulation

*weak in terms of both anabolic/ androgeneric properties

17
Q

Danazol: Most common use and ADRs

A 
-Treats endometriosis
ADR:
1.  weight gain
2. mood swings/ acne
3. thrombosis

(just remember these ADRs are similar to the ADRs of OCPs)

18
Q

When is Danazol contraindicated?

A

pregnancy/ breast feeding

19
Q

Stanazolol MOA

anabolic or androgenergic?

A
  • 17a alkylated derivative of testosterone
  • anabolic&raquo_space; androgenergic
  • ^mRNA/ protein levels of C1 INH and C4
20
Q

What does stanazolol treat?

A

-hereditary angioedema

C1 esterase inhibitor deficiency

21
Q

ADRs and CI for Stanazolol

A
  • SAME ADRs as the other alkylated testosterones w
    1. exceptional HEPATOTOX
    2. acne, virilization, baldness in women

-Same CI as all testosterones + female breast cancer with ^^Ca++

22
Q

Oxandrolone MOA?
anabolic or androgenergic?
Most salient use?

A
  • synthetic testoserone
  • very high anabolic activity
  • used for weight gain post op/ post trauma etc in UNDERWEIGHT patients!

Aka what Melissa will give Leah and Stacee if we do not eat enough food. TRUTH!

23
Q

ADRs and CI for oxandrolone

A

-SAME ADRs as the other alkylated testosterones
+ irritability, aggression, excitation (-roid rage)
Contra: breast/prostate cancer & pregnancy

24
Q

Finasteride and Dutasteride:
MOA
Use x2

A
  • Reduce DHT by as much as 50%
  • Finasteride comp. inhibits type 2 5AR
  • Dutasteride comp. inhibits types 1 + 2 5AR
  • DUtasteride= DUal inhibition.
  • Used to treat BPH AND male pattern baldness
25
Q

Tamsulosin + Alfuzosin
MOA
Use

A
  • a1 antagonists –> SM relaxation –> allow urination in BPH
  • COMBINED with finasteride or dutasteride, do not treat the underlying cause of BPH
26
Q

How long does it take 5ARi drugs to reduce prostate size in BPH?

A

-6 months

27
Q

ADRs assc with 5ARi drugs (4)?

A
  • gynecomastia
  • ^^testosterone (DHT)
  • hepatic dysfunction
  • low PSA by 50%
28
Q

In what populations would 5ARi drugs be CI?

A
  • women, children, preggos, breastfeeding

- women who are pregnant should not even HANDLE the tablets.

29
Q

Leuprolide MOA :

2 Uses:

A
  • GnRH agonist –> decreased FSH/LH –> decreased testosterone
  • used in prostate cancer/ endometriosis
30
Q

How is Leuprolide andministered?

A

-SubQ/IM

31
Q

*Leuprolide ADRs (5)

A
  • hot flashes/ gynecomastia
  • edema/ thrombosis
  • osteoporosis/ bone pain
32
Q

Flutamide MOA/ 2 uses

A
  • prevents binding of testosterone/ DHT to target tissue

- used in prostate cancer and acne

33
Q

Flutamide 2 ADRs

A
  • hepatic tox (very common! ^ liver enzymes frequent reason to stop treatment)
  • gynecomastia
34
Q

List two “steroids” abused by athletes:

A

17a alkylated testosterones

  • fluoxymesterone
  • methyltestosterone
35
Q

Two drugs used to treat prostate cancer?

A

Leuprolide; GnRH agonist

Flutamide; prevents DHT binding to prostate tissue

36
Q

Drug used for weight gain:

A

Oxandrolone 🍔

37
Q

Two drugs used to treat BPH?

A

Finasteride; Dutasteride
5ARi
-may combine with a1 antagonists for symptomatic relief (Tamsulosis/ Alfuzosin)

38
Q

Drug used to treat hereditary angioedema

A

stanazolol + danazolol

39
Q

Drug most commonly used to treat endometriosis

A

danazolol

can also use Leuprolide

DT4-Exam 1 (17 decks)

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