Sex Steroids II - Pharmacology II

Exam V

Describe Menopause

• Insomnia

• Lack of energy

• Cognitive issues

• Vasomotor symptoms

• Emotional problems

• Loss of bone density

• Altered lipid metabolism

• Low libido

• Urogenital atrophy

Describe Andropause

• Insomnia

• Lack of energy, endurance

• Cognitive issues/memory deterioration

• Excessive sweating

• Emotional problems

• Worse stress management and stress-related coping techniques

• Low libido

• ED

• Body hair loss

List the Oral Estrogens. What Population can use these products?

• Conjugated Estrogen — 0.3mg

• Micronized estradiol

• Estropipate

• Ethinyl Estradiol

Only women without a uterus

Describe the use of Estrogen transdermal patch

• Only women without a uterus

• Prevents osteoporosis

Describe the use of Vaginal Estrogen Cream

• Women with/without a uterus

• Prevents vaginal atrophy

What are the negatives on Estrogen Only products?

• Promotes endometrial cancer

• Increases HDL and Trigs

Describe the use of Progestin Treatment in Menopause

Medroxyprogesterone Acetate

• Relieves hot flashes, improves sleep and cognition

• Use when estrogen therapy is contraindicated

What are the negative effects of using Progestin Products?

• No improvement on Vaginal Atrophy

• No increase in HDL

What are the benefits of Using a Estrogen + Progestin Product?

• Can be used in women with or without a uterus

• Prevents Endometrial cancer (associated with estrogen only therapy)

• Prevents triglyceride increase

• Negates estrogen HDL increase

• Example: Prempro

What are the disadvantages of using a Estrogen + Progestin Product?

Does not increase HDL levels

Describe how dosage changes from Birth control to Menopause treatment with the combo products

Estrogen dose in 10x higher in menopause treatment

How do SERMs work?

Selective Estrogen Receptor Modulators

• In Bones, Drug cause cells to not recruit the cofactors and only 1 gene is expressed. This prevents osteoporosis

• In Breasts, drug blocks the cofactor and causes NO expression of genes in the breasts

• Bad effect → increases Vasomotor Symptoms

List the SERMs.

Bazedoxifene

Raloxifene

Tamoxifen

Toremifene

Ospemifene

Describe the effects of using Conjugated Estrogen + Bazedoxifene

• Treats vasomotor symptoms

• Prevents osteoporosis

• anti-estrogen effects on uterus

• No vaginal bleeding

• No increased breast pain

• Bad effect → increases triglycerides

What are the indications of using Androgens?

• Loss of Libido due to reduction in testosterone

• Improves sexual function and energy levels

Bad:

• Does not relieve VMS or osteoporosis

List Androgen Formulations

• Esterified Estradiol and Methyltestosterone (Estratest) (Add progestins with uterus)

• Testosterone patches (unapproved)

What are SEs of Androgen use?

Acne

Hirsutism

Masculinization

List the ‘Anti-Osteoclasts’

Bisphosphonates:

• Promotes osteoclast cell death

  • Oral (Alendronate)

  • IV (Ibandronate, zoledronic acid)

Anti-RANK ligand antibodies:

• Denosumab (Prolia)

SE of ‘Anti-Osteoclasts’

Worsens vasomotor symptoms

Describe Testosterone Cycle

• Per Hour: goes up and down four or five times/day

• Daily: higher in the morning and lower at night

• Monthly: Unique to each man, but men can actually track their moods and recognize they are related to hormonal changes through the month

• Seasonal: higher in November and lower in April

• Age: between 40 and 55 andropause onset

  • Hormonal changes in men going through relate to stress in man’s life

List SEs of Testosterone Replacement Treatments

• N/V

• HA

• Dizziness

• Rash, Burns, Blisters

• Increase risk of heart attack or stroke

• May worsen benign prostatic hypertrophy (1:2 males)

• May stimulate prostate cancer

• May worsen sleep apnea

• May cause blood clots and increase risk of thrombosis and pulmonary embolism