Pharm-IL-Androgens-Leah : ) Flashcards
Failure of testes to make testosterone is called ____?
What levels define failure?
Hypogonadism
Defined as levels below 300 ng/dl in males under 30.
Signs of low testosterone (4)?
- decreased energy
- decreased libido
- loss of muscle mass/ bone (osteoporosis)
- anemia
*Just remember its like being in medical school + anemia
In hypogonadism, how is testosterone administered and why?
- IM 2-3x/week or transdermal, but NOT orally
- low oral bioavailability
How/ where is transdermal testosterone applied?
- 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
Why aren’t testosterone patches placed on the scrotum?
- potential for very high absorption.
- Scrotum has very thin skin, therefore ^^ absorption
For what healthcare procedures must testosterone patches be removed?
-During an MRI due to aluminum content
activated aluminum can cause burns!!
How do testosterone patches affect female partners?
-Female should avoid physical contact with the patch, as laying on it (for example) may lead to abnormal hair growth
What black box warning is assc with testosterone patches?
- Can cause virilization in children
- DO NOT allow children to contact the patch
What are testosterone cypionate and enanthate; how are they administered?
- testosterone esters
- prodrug: convert to testosterone in body
- must be given IM every 2-4 weeks.
- ^^^ lipophilicity –> lasts longer in the body
In addition to hypogonadism, for what purpose might testosterone enanthate be used?
-female metastatic breast cancer, antagonizes estrogen
17a alkylated testosterone: social implication? normal use?
- THIS is the testosterone abused as an anabolic steroid
- intended for the same uses as testosterone, hypogonadism and met. breast cancer in females
Two specific 17 a alkylated testosterones?
- Methyltestosterone
- Fluoxymesterone
(remember: methyl + fluoxy)
What are the ADRs assc with (alkylated) testosterone (4)?
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)
When are (all) testosterone analogues contraindicatied? (3)
- prostate cancer
- pregnancy
- MALE breast cancer
ADRs assc with (ALL) testosterones/ analogues (3)?
- edema –> HTN
- jaundice
- hepatic carcinoma
(ADRs similary but amplified in alkylated versions)
Danazol:
Describe the compound –what is its MOA (3)?
Anabolic or androgeneric?
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
Danazol: Most common use and ADRs
-Treats endometriosis ADR: 1. weight gain 2. mood swings/ acne 3. thrombosis
(just remember these ADRs are similar to the ADRs of OCPs)
When is Danazol contraindicated?
pregnancy/ breast feeding
Stanazolol MOA
anabolic or androgenergic?
- 17a alkylated derivative of testosterone
- anabolic»_space; androgenergic
- ^mRNA/ protein levels of C1 INH and C4
What does stanazolol treat?
-hereditary angioedema
C1 esterase inhibitor deficiency
ADRs and CI for Stanazolol
- 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++
Oxandrolone MOA?
anabolic or androgenergic?
Most salient use?
- 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!
ADRs and CI for oxandrolone
-SAME ADRs as the other alkylated testosterones
+ irritability, aggression, excitation (-roid rage)
Contra: breast/prostate cancer & pregnancy
Finasteride and Dutasteride:
MOA
Use x2
- 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
