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Questions and Answers
What is one use of estrogen?
What is one use of estrogen?
Progestins are only used for contraceptive purposes.
Progestins are only used for contraceptive purposes.
False
An absence or decrease in estrogen produces the symptoms of ______.
An absence or decrease in estrogen produces the symptoms of ______.
menopause
Which of the following is a progestin?
Which of the following is a progestin?
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What is the function of oxytocin?
What is the function of oxytocin?
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Which drug is used as a fertility drug?
Which drug is used as a fertility drug?
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Estrogen protects the heart from atherosclerosis.
Estrogen protects the heart from atherosclerosis.
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What is one primary role of estrogens in the female reproductive system?
What is one primary role of estrogens in the female reproductive system?
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Which of the following drugs is classified as an oxytocic?
Which of the following drugs is classified as an oxytocic?
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What hormone is primarily associated with stimulating uterine contractions during childbirth?
What hormone is primarily associated with stimulating uterine contractions during childbirth?
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How do drugs that act like estrogen differ from natural estrogen?
How do drugs that act like estrogen differ from natural estrogen?
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Which of the following is a receptor modulator associated with estrogen?
Which of the following is a receptor modulator associated with estrogen?
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What is one of the main mechanisms by which progestins and estrogens function as contraceptives?
What is one of the main mechanisms by which progestins and estrogens function as contraceptives?
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Which of the following conditions is a contraindication for using estrogen?
Which of the following conditions is a contraindication for using estrogen?
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What are potential risks associated with the use of Drospirenone as a progestin?
What are potential risks associated with the use of Drospirenone as a progestin?
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Which of the following is NOT a pharmacokinetic property of estrogen?
Which of the following is NOT a pharmacokinetic property of estrogen?
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Which of the following conditions would require caution when prescribing progestins?
Which of the following conditions would require caution when prescribing progestins?
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Study Notes
Female Reproductive System
- The female reproductive system operates in a cyclical manner, unlike most other endocrine systems.
Hormones and Sites of Action
- Estrogens, progestins, androgens, and estrogen and progestin receptor modulators are all types of hormones that can affect the female reproductive system.
- Sites of action often include the uterus, vagina, cervix, fallopian tubes, ovaries, and pituitary gland.
Estrogens
- Examples include estradiol, conjugated estrogens, and estropipate
- Therapeutic actions include hormone replacement therapy, palliative care for menopausal symptoms, treatment of female hypogonadism and ovarian failure, prevention of postpartum breast engorgement, contraception, slowing bone loss in osteoporosis, and use in certain cancers with known receptor sensitivity.
- Estrogen plays a role in the development of the female reproductive system and secondary sex characteristics, affecting the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH).
- Estrogen also influences capillary dilatation, fluid retention, protein anabolism, cervical mucus thinning, calcium and phosphorus conservation, bone formation, ovulation inhibition, and prevention of postpartum breast discomfort.
- It is important to note that estrogen has various systemic effects, such as protecting the heart from atherosclerosis, retaining calcium in bones, and maintaining female secondary sex characteristics.
Progestins
- Examples include desogestrel, drospirenone, etonogestrel, levonorgestrel, medroxyprogesterone, norethindrone acetate, norgestrel, progesterone, and ulipristal.
- Therapeutic actions include use as contraceptives treating primary and secondary amenorrhea, functional uterine bleeding, and fertility programs.
- Progestins are also used in treating certain cancers.
- Progestins transform the proliferative endometrium into a secretory endometrium, inhibit FSH and LH secretion, and prevent...
Female Reproductive System
- The female reproductive system functions cyclically, unlike the steady-state functioning of the endocrine system.
- Drugs impacting this cycle can influence the entire body.
Sex Hormones and Estrogen Receptor Modulators
-
Estrogens:
- Estradiol, conjugated estrogens, esterified estrogens, and estropipate.
- Used for hormone replacement, to stimulate estrogenic effects, and to inhibit FSH and LH secretion.
- Involved in follicle maturation and ovulation inhibition, uterine contraction suppression, and anabolic and estrogenic effects.
- Absorbed through the gastrointestinal tract (GIT) and metabolized extensively in the liver.
- Excreted in urine.
- Cross the placenta and enter breast milk.
-
Progestins:
- Desogestrel, drospirenone, etonogestrel, levonorgestrel, medroxyprogesterone acetate, norethindrone acetate, norgestrel, progesterone, and ulipristal.
- Mechanism of action in contraceptives: potentially "tricking" the hypothalamus and pituitary to suppress GnRH, FSH, and LH release, preventing follicle development and ovulation.
- Well-absorbed, undergo hepatic metabolism, and excreted in urine.
- Cross the placenta and enter breast milk.
-
Estrogen Receptor Modulators (ERMs):
- Raloxifene (Evista) and toremifene (Fareston)
- Act on specific estrogen receptor sites, stimulating some and blocking others.
- Provide positive estrogen replacement effects while limiting adverse effects.
Contraindications and Cautions for Estrogens
- Allergies to estrogen.
- Idiopathic vaginal bleeding.
- Breast cancer or estrogen-dependent cancers.
- History of thromboembolic disorders (blood clots), including stroke, or heavy smokers.
- Hepatic dysfunction.
- Pregnancy.
- Not recommended during breastfeeding.
Contraindications and Cautions for Progestins
- Pelvic inflammatory disease (PID), sexually transmitted diseases (STDs), endometriosis, or pelvic surgery.
- Drospirenone: Risk of hyperkalemia due to renal disorders, liver disease, or adrenal dysfunction.
- Epilepsy, migraine headaches, asthma, cardiac or renal dysfunction.
Adverse Effects of Estrogens
- Gastrointestinal (GIT): Bleeding, menstrual irregularities, dysmenorrhea, amenorrhea, changes in libido, nausea, vomiting, abdominal cramps and bloating, colitis.
- Systemic: Fluid retention, electrolyte disturbances, headache, dizziness, mental changes, weight changes, and edema.
Adverse Effects of Progestins
- Systemic: Similar to estrogen.
- Dermal patch contraceptives: Systemic effects, plus local skin irritation.
- Vaginal gel: Headache, nervousness, constipation, breast enlargement, perineal pain, local irritation, and swelling.
- Intrauterine system: Abdominal pain, endometriosis, abortion, PID, and expulsion of the IUD.
Therapeutic Actions and Indications of ERMs
- Produce positive estrogen replacement effects while limiting adverse effects.
Pharmacokinetics of Raloxifene
- Administered orally.
- Absorbed from the GIT and metabolized in the liver.
- Excreted in feces.
- Crosses the placenta and enters breast milk.
Contraindications and Cautions for Raloxifene
- Allergy to raloxifene.
- Pregnancy and lactation.
- Caution in patients with history of venous thrombosis or smoking.
Adverse Effects of Raloxifene
- GI upset, nausea, vomiting.
- Changes in fluid balance: Headache, dizziness, visual changes, mental changes.
- Hot flashes, skin rash, edema, vaginal bleeding.
- Increased risk of multiple births and birth defects.
Adverse Effects of Toremifene
- Ovarian overstimulation: Abdominal pain, distention, ascites, pleural effusion.
- Headache.
- Fluid retention.
- Nausea.
- Bloating.
- Uterine bleeding.
- Ovarian enlargement.
- Gynecomastia.
- Febrile reactions.
Uterine Motility Drugs
- Used to influence uterine contractions, aiding labor (oxytocics) or inducing abortion (abortifacients).
- Tocolytics: Drugs that slow uterine activity, e.g., terbutaline (beta2-selective adrenergic agonist).
Oxytocics
- Stimulate uterine contractions, similar to the action of hypothalamic oxytocin.
- Methylergonovine (Methergine) and oxytocin (Pitocin).
Therapeutic Actions and Indications of Oxytocics
- Directly stimulate neuroreceptor sites to contract the uterus.
- Stimulate lacteal glands in the breast to contract.
- Prevent and treat uterine atony after delivery.
Pharmacokinetics of Oxytocics
- Rapidly absorbed after parenteral or oral administration.
- Metabolized in the liver.
- Excreted in urine and feces.
- Crosses the placenta and enters breast milk.
Administration of Oxytocics
- Methylergonovine: Administered intramuscularly (IM) or intravenously (IV) immediately after delivery, followed by oral administration to promote uterine involution.
- Oxytocin: Administered IM or IV, or nasally to stimulate milk "let down" in lactating women.
Contraindications and Cautions for Oxytocics
- Allergies to oxytocics.
- Cephalopelvic disproportion, unfavorable fetal position, complete uterine atony, or early pregnancy.
- Coronary disease, hypertension, previous cesarean birth, hepatic or renal impairment.
Adverse Effects of Oxytocics
- Headache, nausea, vomiting, diarrhea, diaphoresis, backache, and rash.
Male Reproductive System
- Male steroids, produced in the testes, influence the entire male reproductive system.
- Drugs affecting the male reproductive system include androgens (male steroid hormones), anabolic steroids, and drugs treating penile dysfunction.
Androgens
- Testosterone and androgens, including testosterone (Durates, Testoderm, etc.), danazol, fluoxymesterone, and methyltestosterone.
- Testosterone is the primary natural androgen used for replacement in hypogonadism and treating certain breast cancers.
Therapeutic Actions and Indications of Androgens
- Promote growth and development of male sex organs.
- Maintain secondary male sex characteristics.
- Increase retention of nitrogen, sodium, potassium, and phosphorus, and decrease calcium excretion.
- Enhance protein anabolism and decrease protein catabolism.
- Increase red blood cell production.
- Danazol: Used for endometriosis, fibrocystic breast disease, and hereditary angioedema.
Pharmacokinetics of androgens
- Depot injections, buccal system, topical gels, sprays, urethral pellets, and a dermal patch.
- Danazol: Synthetic androgen (long-acting), available only orally.
- Methyltestosterone and fluoxymesterone: Long half-lives, available orally.
- Well-absorbed and widely distributed throughout the body.
- Metabolized in the liver and excreted in urine.
Contraindications of Androgens
- Allergies to the drug or its ingredients.
- Existing conditions may require additional contraindications.
Anabolic Steroids
- Oxandrolone and oxymetholone.
Drugs for Treating Erectile Dysfunction
- Alprostadil, avanafil, sildenafil, tadalafil, and vardenafil.
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Description
Explore the intricate workings of the female reproductive system, its hormonal regulation, and the key organs involved. This quiz covers various hormones, their therapeutic uses, and the cyclical nature of the reproductive processes. Test your understanding of the female endocrine system's functionality and the importance of estrogens.
