Pharmacology: 45 and 46 review
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What three hormonal secretions control female reproduction? Where are they secreted from?
- GnRH (gonadotropin-releasing hormone): Hypothalamus --> Pituitary
- FSH (follicle stimulating hormone): Pituitary ---> ovary
- LH (lutieinizing hormone): Pituitary ---> ovary
The rising and falling of pituitary hormones in the female body creates what two interrelated cycles that occur on a monthly basis?
Ovarian and Uterine cycles
On approximately day 14 of a woman's ovarian cycles, a surge of ____ secretion causes one follicle to expel its oocyte in a process called ______.
After the ruptured follicle expels its oocyte during the ovarian cycle, what happens to it?
It is transformed into the hormone secreting corpus luteum.
What two hormones do ovarian follicles secrete as they mature?
- Estrogen (estradiol, estrone, and estriol)
Estrogen is actually a generic name for what 3 hormones?
____ is responsible for the maturation of the female reproductive organs and the appearance of secondary sex characteristics.
What is the age range in which women typically enter menopause? What hormone do the ovaries stop secreting at that point?
What action(s) does progesterone have in the female body in terms of reproduction?
- In combination with estrogen:
- promotes breast development
- influences the endometrium to become vascular and thicker in preparation for receiving a fertilized egg.
High progesterone and estrogen levels in the final third of the uterine cycle provide negative feedback to shut off the secretion of what three hormones?
How do oral contraceptive prevent pregnancy?
By inhibiting ovulation
Most oral contraceptives contain what two hormones?
Estrogen and Progesterone
How do estrogen-progestin combinations of OCs prevent ovulation?
Providing negative feedback to the pituitary, which then suppresses the secretion of LH and FSH. Without the effects of these pituitary hormones, the follicle cannot mature and ovulation is prevented.
True or False: In addition to preventing ovulation, the oral contraceptives also make the uterine endometrium a less favorable environment to receive an embryo, thus reducing the chances of implantation.
What are minipills? How do they work?
- They are oral contraceptives that contain only progestin
- They prevent pregnancy by producing thick, viscous mucous at the entrance to the uterus that discourages penetration by the sperm.
- They also tend to inhibit implantation of a fertilized egg.
True or False: Minipills are just as effective as normal OCs.
False. Minipills have a failure rate of 1-4%
The use of _____ as opposed to estrogen-progestin combination oral contraceptives is associated with a higher incidence of menstrual irregularities such as amenorrhea, prolonged menstrual bleeding, or breakthrough spotting.
Minipills (progestin-only OCs)
What two drug classes can reduce the effectiveness of oral contraceptives?
The efficacy of what drugs can be affected by oral contraceptives?
- some hypoglycemic agents
What cardiovascular effects have oral contraceptives been associated with? Why?
- Increased risk of hypertension and thromboembolic disorders
- The estrogen component of the pill can lead to venous and arterial thrombosis with resultant pulmonary embolism, myocardial infarction, or thrombotic stroke.
____ is the prevention of pregnancy following unprotected intercourse while ____ is the removal of an embryo by the use of drugs after implantation has occured.
- Emergency contraception
- pharmacologic abortion
How does the emergency contraceptive Plan B work?
- It involves taking levonorgestrel in two doses, twelve hours apart
- It acts in a manner similar to OCs: prevents ovulation and alters the endometrium the uterus so that implantation does not occur.
How soon must Plan B be administered after unprotected sex in order to be effective?
- As soon as possible: within 72 hours,
- After 7 days, it is ineffective.
____ is characterized by progressive decrease in estrogen secretion by the ovaries, resulting in the permanent cessation of the menses. Is it a disease or a disorder?
- Neither: it is a natural consequence of aging that happens to be accompanied by unpleasant symptoms.
What has been the mainstay of treatment for menopause over the past 40 years?
Hormone Replacement Therapy (HRT)
Why is their controversy regarding the use of hormone replacement therapy (estrogen/progestin combined) ?
Women taking estrogen/progestin combined therapy experienced statistically signifant increases in their risk for MI, stroke, breast cancer, dementia, and venous thromboembolism, with higher risks correlated with higher age.
What have been shown to be the effects of taking hormone replacement therapy with only estrogen?
- increased risk of stroke and thromboembolytic disease
- No effect on risk for MI
True or False: Women taking estrogen/progestin combined HRT experienced an increased risk of hip fractures and colorectal cancer.
False. Decreased risk.
Given that there are many known and serious side effects to HRT, why does its use remain controversial instead of merely discouraged?
HRT does offer relief from the immediate distressing menopausal symptoms, prevents osteoporosis-related fractures, and may offer protection against colorectal cancer.
Short term use of HRT for relieving acute symptoms of menopause may be appropriate for women without a history of what?
- Cardiovascular disease
Regarding HRT: why is the use of estrogen without progesterone contraindicated in all patients that have not had a hysterectomy?
When used alone, estrogen increases the risk of uterine cancer.
High doses of estrogen may be used to treat what kind of cancer(s)?
- Breast Cancer
- Prostate Cancer
____ is a condition in which hemorrhage occurs on a noncyclic basis or in abnormal amounts.
Dysfunctional uterine bleeding
____ are the drugs of choice for treating uterine abnormalities.
What structure secretes endogenous progesterone before pregnancy (or in the absence of it)? During pregnancy?
- Corpus Luteum
- Ovaries, then Placenta
If pregnancy occurs, the ovary continues to secrete ____ to maintain a healthy endometrium until the placenta develops sufficiently to begin producing the hormone.
Causes of this disorder include early abortion, pelvis neoplasms, thyroid disorders, pregnancy, infection, and a history of hysterectomy.
Dysfunctional uterine bleeding
Dysfunctional Uterine bleeding is broad category encompassing many uterine problems:
A. ______ : the absence of menstruation
B. Endometriosis: ______________
C. ______: infrequent menstruation
D. ______:Prolonged or excessive menstruation
E. Breakthrough bleeding: ______________
F_______: symptoms that develop during the luteal phase
G. Postmenopausal Bleeding:_________
H. _______: Cancer of the Endometrium
- A. Amenorrhea
- B: Abnormal location of the endometrial tissues
- C: Oligomenorrhea
- D: Menorrhagia
- E: Hemorrhage between menstrual periods
- F: PMS
- G: Hemorrhage following menopause
- H: Endometrial carcinoma
Dysfunctional Uterine Bleeding is most often caused by what? Why?
- A hormonal imbalance between estrogen and progesterone.
- Estrogen increases the thickness of the endometrium, but bleeding occurs sporadically unless it is balanced by an adequate amount of progesterone.
What drugs are frequently prescribed in order to treat dysfunctional uterine bleeding (2)?
- Oral Contraceptives: balance hormones
- NSAIDs: reduce bleeding and ease painful menstrual flow
____ are agents that stimulate uterine contractions to promote the induction of labor.
____ are used to inhibit contractions during premature labor.
What action does endogenous oxytocin have in the pregnant woman? In the lactating woman?
- Uterine contractions
- Ejection of milk (in response to suckling)
True or False: Oxytocin increases the volume of milk ejected at lactation.
False: it only stimulates lactation. The pituitary hormone prolactin controls the volume and synthesis of breast milk.
Several ____a____ are used as uterine stimulants. Unlike most hormones, ____a____ are local hormones that act directly at the site where they are secreted.
The ____ may be used to induce pharmacological abortion.
When are oxytocin and other uterine stimulants used to induce labor?
Only when their are demonstrated risks to the mother or fetus in continuing pregnancy; they should never be used for elective labor do to risks.
In what situation would tocolytics be administered?
If a pregnant woman goes into labor before the baby has reached a normal stage of development.
_____ are uterine relaxants prescribed to suppress preterm labor contractions. How much additional time do these medications typically buy?
What drugs are in the Tocolytic class?
- None that are approved for use in the United States
- Caclcium Channel blockers and Beta Blockers may be used, but they are not approved for this indication.
_____ regulates sperm production in men. What does it regulate in women?
- Development of the follicle
What is the name for luteinizing hormone in the male reproductive system?
What is its role?
- ICSH (Interstitial Cell-Stimulating Hormone
- Regulates the production of Testosterone.
The _____ secretes testosterone, and is regulated by the _____, a pituitary hormone.
- ICSH (Interstitial-Cell-Stimulating Hormone
Lack of insufficient testosterone secretion in males can result in male _______. Is it acquired or congenital?
- It may be acquired or congenital.
When male hypogonadism is caused by a testicular disorder, it is called ________ hypogonadism.
When the testes lack sufficient stimulation form FSH and LH (ICSH) to form testosterone, the condition is known as _____ hypogonadism.
What does the pharmacotherapy of hypogonadism involve?
Replacement therapy with testosterone or other androgens.
Why do men usually have a slightly hematocrit than women?
Testosterone promotes the synthesis of erythropoietin.
____ are testosterone-like compounds with hormonal activity that are taken inappropriately by athletes who hope to build muscle mass and strength, thereby obtaining a competitive edge.
True or False: Anabolic steroids tend to raise cholesterol and sperm counts in men.
False: They raise cholesterol, but lower sperm counts and may even cause impotence.
Why are most androgens classified as Schedule III drugs?
Because of their potential for abuse (Anabolic steroids).
Are anabolic steroids safe for long term use?
True or False: Male infertility may occur with or without signs of hypogonadism.
Erectile dysfunction, also called _______, is a common disorder among men. What is the defining characteristic?
- Consistent inability to either obtain or sustain an erection long enough to achieve successful intercourse.
What is the drug of choice for treating erectile dysfunction?
sildenafil (Viagra), a phosphodiesterase inhibitor
How do phosphodiesterase inhibitors like sildenafil help with impotence?
They do not cause an erection; rather, they enhance the erection resulting from physical contact or other sexual stimuli by maintaining relaxation of the smooth muscle in the penis and increasing blood flow.
Sildenafil and other phosphodiesterase inhibitors are not as effective in promoting erections in men who do not have what?
The three phosphodiesterase inhibitors currently approved for use in treating impotence are equally effective at promoting erections in ___% to ___% of male patients.
Patients participating in pharmacotherapy involving which drugs should not use phosphodiesterase inhibitors?
- Contraindicated in patients taking nitrates
- May produce hypotension in patients who are taking multiple antihypertenisves as well.
What is the most common benign neoplasm in men?
Benign prostatic hyperplasia (BPH)
____ is characterized by enlargement of the prostate gland that decreases the outflow of urine by obstructing the urethra, causing difficult urination.
Benign prostatic hyperplasia
What are the symptoms of a benign prostatic hyperplasia?
- Increased urinary frequency with small amounts of urine
- Increased urgency
- Postvoid leakage
- Decreased force of urine stream
- Sensation that the bladder did not empty completely
Why are there two different classes of drugs with two different mechanisms to treat benign prostatic hyperplasia?
There are two mechanisms of the disease: Static and Dynamic
Describe the static mechanism of the pathogenesis of benign prostatic hyperplasia.
Anatomic enlargement of the prostate gland: the gland can double or triple its size with aging and cause a physical block of urine flow at the neck of the bladder.
Describe the dynamic mechanism of the pathogenesis of benign prostatic hyperplasia.
Excessive numbers of alpha1 adrenergic receptors located in the smooth muscle cells in the neck of the urinary bladder and the prostate gland compress the urethra (when activiated) and provide resistance to urine outflow from the bladder.
What drugs can worsen BPH (benign prostatic hyperplasia)?
______ men should avoid these drugs.
- Alpha-Adrenergic Agents
- Drugs with Anticholinergic effects, including:
True or False: BPH is a progressive disease, so patients will eventually need pharmacotherapy to deal with it.
False: BPH is not always a progressive disease: patients who are asymptomatic or present with mild symptoms generally do not receive pharmacotherapy.
What are the drugs of choice in the treatmnent of benign prostatic hyperplasia? How do they exert their effects?
- Alpha1- Adrenergic blockers.
- They relax smooth muscle in the prostate gland, bladder neck, and urethra, thus easing the urinary obstruction.
Reflex____ due to stimulation of baroreceptors is common with alpha blockers.
Alpha-Reductase Inhibitors treat benign prostatic hyperplasia by what mechanism?
They interfere with testosterone metabolism, thus shrinking the enlarged prostate.
_____ are used when BPH is due to an enlarged prostate, and _____ are used when BPH is due to excessive activation of Alpha1 receptors.
- Alpha-Reductase Inhibitors
- Alpha1 Adrenergic Blockers
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