Prescribing Sex Hormones and Antiestrogens

Flashcards on prescribing sex hormones and antiestrogens, covering hormone substitution in menopause and hormonal therapy of sterility.

What are some potential benefits of hormone substitution in menopause?

Decreased risks of developing osteoporosis and colon cancer.

What are some potential side effects of hormone substitution in menopause?

Increased risk of developing breast cancer, endometrial cancer, ovary cancer, and stroke.

What is the generally agreed-upon duration for sex hormone substitution in healthy women?

Up to 10 years.

What are the age and time-since-menopause requirements for sex hormone substitution?

Age under 60, and less than 10 years elapsed since the cessation of menstrual cycles.

Who should not receive sex hormone substitution?

Women who have already had breast, endometrial or ovarian cancer, who have already had venous thrombosis, myocardial infarction or stroke, as well as in those who have not regulated their hypertension or have liver disease.

When does substitution of sex hormones begin?

After the cessation of normal menstrual cycles.

What hormone is substituted in women whose uterus is surgically removed?

Only estrogen.

Why are preparations containing both estrogen and progesterone analogues used in women with preserved internal sex organs?

Progestogens reduce the risk of cancer of the endometrium, which estrogens themselves increase.

Why are transdermal estrogen preparations favorable?

They contain a lower total dose of estrogen and successfully control menopausal symptoms.

In what patients are transdermal preparations used?

Women who have had their uterus removed and have diabetes, hypertriglyceridemia, obesity, increased risk of thrombosis, migraine or liver disease.

What are the two types of hormone substitution preparations?

Cyclical and continuous.

What do cyclic preparations contain during the first 15 days (monthly) or 13 weeks (three-monthly)?

Only estrogen analogues.

What do cyclic preparations contain for the rest of the cycle?

Only analogues of progesterone.

What do continuous hormone preparations contain?

Both an estrogen analogue and an analogue of progesterone in each tablet.

What is a consequence of using continuous hormone preparations?

Female patients who take these preparations do not have menstrual bleeding at all.

What are the forms of applying hormone substitution preparations?

Vaginal cream, tablets, vaginal tablets, transdermally, or in the form of implants.

How are hormone substitution preparations discontinued?

Gradually, after 5-10 years of use, to prevent the reappearance of menopause symptoms.

What are women also recommended to use to prevent vaginal dryness?

Vaginal creams without hormones.

What are women recommended to use to prevent osteoporosis?

Bisphosphonates or denosumab.

What is gonadotropin-releasing hormone (GRH)?

A polypeptide of 10 amino acids secreted in the hypothalamus that leads to the release of FSH and LH.

What is GRH used for?

To induce ovulation in people suffering from infertility.

How must GRH be administered to achieve the desired effect?

In the form of an intravenous infusion, pulsed (a small dose is injected every hour for several days).

Why must GRH be administered in pulsed doses?

Because only then does the secretion of FSH and LH increase.

How is the effect of GRH monitored?

By measuring LH excretion in urine and ultrasound examinations of the ovaries.

Where can FSH and LH be obtained in larger quantities?

From the urine of women in postmenopause.

What is the name of the preparation obtained from the urine of women in postmenopause?

Human menopausal gonadotropin (HMG) or urofollitropin.

What is the synthetic FSH hormone called?

Follitropin.

What can be used instead of LH?

Human chorionic gonadotropin (hHG).

Where is human chorionic gonadotropin found?

In large quantities in the urine of pregnant women.

What is HMG used to induce?

Ovulation in patients suffering from sterility and to stimulate spermatogenesis in men.

What does HMG contain?

75 IU FSH and 75 IU LH per milliliter.

When is HMG primarily used?

In patients with primary amenorrhea due to hypopituitarism, or in secondary amenorrhea that has not responded to the use of other ovulation inducers.

What are common side effects of gonadotropins?

Ectopic pregnancy, multiple pregnancy, spontaneous abortion, rupture and torsion of the ovary, and ovarian hyperstimulation syndrome.

What is ovarian hyperstimulation syndrome characterized by?

Enlargement of the ovary, accumulation of fluid in the interstitial space and peritoneal cavity (ascites and the like), hemoconcentration, hyponatremia and hyperkalemia.

What can happen if hyperstimulation syndrome is not treated on time?

Acute renal failure and thrombosis.

How is hyperstimulation syndrome treated?

With the infusion of an isotonic saline solution, the infusion of a 25% albumin solution and the use of prophylactic doses of heparin.

What is clomiphene?

A drug that blocks estrogen receptors in the pituitary gland and hypothalamus.

What is the effect of clomiphene?

The secretion of gonadotropins increases, and thus enables the occurrence of ovulation.

How is the occurrence of ovulation monitored when using clomiphene?

By measuring the excretion of LH in the urine.

When does ovulation usually occur after an increase in secreted LH?

After a day or two.

Who is clomiphene most commonly used to induce ovulation in?

Polycystic ovary syndrome patients.

What are some adverse effects of clomiphene?

Thickening of cervical mucus, hot flashes, vaginal dryness, and ovarial hyperstimulation syndrome.

What is metformin?

An oral antidiabetic drug that increases the sensitivity of peripheral tissues to the action of insulin.

What can be used if gonadotropin and testosterone production is not within normal limits in infertile men

Clomiphene or human menopausal gonadotropin.

What happens if the patient's gonadotropin production is normal and there is oligospermia or azoospermia?

The in vitro fertilization procedure is started.

What are the two types of intracellular estrogen receptors?

Alpha and beta.

What effects does estrogen binding to alpha receptors have?

A strong signal for cell proliferation.

What effects does estrogen binding to beta receptors have?

Inhibition of cell proliferation.

What type of estrogen receptors are functional in breast tumor cells?

Only alpha estrogen receptors.

How can the growth of breast tumors be stopped?

By using alpha estrogen receptor blockers.

What is tamoxifen?

A drug from the group of selective modulators of estrogen receptors that blocks alpha estrogen receptors in breast tumor cells.

What is fulvestrant?

A drug from the group of selective destroyers of estrogenic receptor, which has been successfully used to treat breast tumors that contain alpha estrogen receptors.

What is the problem in the clinical application of tamoxifen and fulvestrant?

The rapid development of tumor resistance.

What do selective modulators of estrogen receptors do in breast tissue?

Block alpha estrogen receptors.

What do selective modulators of estrogen receptors do in bones, liver and blood vessels?

Act as agonists of these receptors.

What are tamoxifen and raloxifene used for?

To treat and prevent breast tumors.

What side effects are associated with tamoxifen due to its agonistic action?

A greater tendency to thrombosis and an increased risk of cancer of endometrium.

What side effects are associated with raloxifene?

Increases the tendency for the occurrence of venous thromboses.

What benefits are associated with tamoxifen?

Reduces the risk of myocardial infarction and lowers serum cholesterol levels.

What is aromatase?

An enzyme found in adipose tissue, muscle, liver and mammary gland that converts androgen androstenedione into estriol.

What is the main source of estrogen in menopausal women?

Estriol.

What is used for adjunctive therapy for breast cancer in postmenopausal women?

Medicines that inhibit aromatase, provided the cancer contains estrogen receptors.

Name some selective aromatase inhibitors.

Letrozole, anastrozole and exemestane.

What are cyclin-dependent kinase 4 and 6 (CDK 4/6) inhibitors used for?

Have been combined with aromatase inhibitors for breast cancer treatment.

What signaling pathway are Cyclin D1 and CDK 4/6 parts of?

A signaling pathway that leads to the progression of the cell cycle from G1 to S phase in breast cells with estrogen receptors.

Name some CDK 4/6 inhibitors.

Palbociclib, ribociclib and abemaciclib.

What are some unwanted effects of CDK 4/6 inhibitors?

A higher frequency of infections, depression of blood lines (anemia, leukopenia, thrombocytopenia), interstitial lung disease (pneumonitis), peripheral neuropathy and thromboembolism.

When are destroyers of estrogen receptors used?

As second-line drugs in the treatment of breast tumors containing alpha estrogen receptors.

What happens when the metastatic breast tumor becomes resistant to tamoxifen, raloxifene or aromatase inhibitors?

Fulvestrant is used.

What does fulvestrant do?

Binds to alpha estrogen receptors and includes them in proteosome, where they are quickly destroyed.

What function does fulvestrant not have?

Agonistic effect on estrogen receptors.

What is used to suppress the function of the ovaries in women who are in premenopause?

Leuprolide, an analog of gonadotropin-releasing hormone.

How does Leuprolide work?

Prevents the release of FSH and LH from the pituitary gland.