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Endocrine > Pharmacology OCP > Flashcards

Pharmacology OCP Flashcards

1
Q

State 3 natural estrogens.

A
  1. Estradiol (also known as 17 β estradiol)
  2. Estrone
  3. Estriol
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2
Q

Compare Estradiol, Estrone and Estriol

A

Estradiol is the most potent estrogen produced and secreted by the ovary
- It is the principal estrogen in premenopausal women

Estrone is a metabolite of estradiol that has approximately one third the
estrogenic potency of estradiol
- Estrone is the primary circulating estrogen after menopause,
- it is generated mainly from conversion of androstenedione in peripheral tissues

Estriol another metabolite of estradiol, is significantly less potent than is estradiol
- It is present in significant amounts during pregnancy, because it is the principal
estrogen produced by the placenta

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3
Q

Why synthetic estrogen (EE) effective when

administered orally at lower doses?

A
  • Synthetic estrogens such as ethinyl estradiol, undergo less first pass metabolism than do naturally occurring steroids
  • Plant derived conjugated estrogen products are also available
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4
Q

ESTROGENS: MECHANISM OF ACTION?

A
  1. These hormones are transported carried by plasma protein
  2. After dissociation from their binding sites on sex hormone binding globulin or albumin in the plasma
  3. steroid hormones diffuse across the cell membrane and bind with high
    affinity to specific nuclear receptor proteins
  4. The activated steroid receptor complex interacts with nuclear chromatin to initiate hormone specific RNA synthesis
  5. This results in the synthesis of specific proteins that mediate a number of physiologic functions
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5
Q

Therapeutic use of estrogen?

A

Contraceptives
Postmenopausal HT
Replacement therapy in premenopausal patients
who are deficient in this hormone

*Estrogen deficiency can be due to inadequate functioning of the ovaries (HYPOGONADISM)
premature menopause, or surgical menopause

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6
Q

Explain estrogen THERAPEUTIC

USES as POSTMENOPAUSAL HT.

A

The primary indication for estrogen therapy in postmenopausal women is menopausal symptoms
- such as vasomotor instability (for example, hot flashes or hot flushes and vaginal atrophy

  • For women who have an intact uterus, a progestogen is always included with the estrogen therapy, because the combination reduces the risk of endometrial carcinoma associated with unopposed estrogen
  • Delivery of estradiol by transdermal patch or gel is also effective in treating postmenopausal symptoms

*Note The amount of estrogen used in replacement therapy is substantially less than the doses used in oral contraception
- Thus, the adverse effects of estrogen replacement therapy are usually less
pronounced than those seen in women taking estrogen for contraceptive purposes

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7
Q

Why HT with estrogen should be prescribed at the lowest effective dose for the shortest possible time to relieve menopausal symptoms?

A

Due to concerns over the risks of HT increased risk of cardiovascular events and breast cancer),

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8
Q

Explain therapeutic use of estrogen in Contraception?

A

The combination of an estrogen and progestogen

provides effective contraception via the oral, transdermal, or vaginal route

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9
Q

What are other use of estrogen, than HT and contraception?

A
  • primary hypogonadism to stimulate development of secondary sex characteristics
  • Premature menopause or premature ovarian failure
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10
Q

Compare Naturally occurring estrogens with Synthetic estrogen analogs.

A
  1. Naturally occurring estrogens
    - These agents are readily absorbed through the gastrointestinal tract, skin, and mucous
    membranes
    - Taken orally, estradiol is rapidly metabolized (and partially inactivated) by the microsomal enzymes of the liver
  2. Synthetic estrogen analogs ::(ethinyl estradiol, mestranol and estradiol valerate)
    - the synthetic estrogen analogs have a prolonged action and a higher potency compared
    to those of natural estrogens
    - These agents are well absorbed after oral administration
    - Being fat soluble, they are stored in adipose tissue, from which they are slowly released
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11
Q

ESTROGENS:

ADVERSE EFFECTS?

A
  • Refer picture in lecture note
  • Nausea and breast tenderness are among the most common adverse effects of estrogen
    therapy
  • the risk of thromboembolic events, myocardial infarction, and breast and endometrial
    cancer is increased with use of estrogen therapy
  • [Note The increased risk of endometrial cancer can be offset by including a progestogen
    along with the estrogen therapy
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12
Q

Name 4 SERMs.

A
  1. Tamoxifen,
  2. toremifene,
  3. raloxifene,
  4. clomiphene,
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13
Q

SERM: MECHANISM OF ACTION?

A
  • Tamoxifen toremifene and raloxifene compete with estrogen for binding to the estrogen receptor in breast tissue
  • [Note Normal breast growth is stimulated by estrogens Therefore, some breast tumors
    regress following treatment with these agents
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14
Q

MOA Raloxifene?

A
  1. acts as an estrogen agonist in bone leading to decreased bone resorption, increased bone density, and decreased vertebral fractures
  2. raloxifene does not have estrogen receptor agonist activity in the endometrium and, therefore, does not predispose to endometrial cancer
  3. Raloxifene also lowers serum total cholesterol and low density lipoprotein (LDL)
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15
Q

SERM:

THERAPEUTIC USES?

A
  • Tamoxifen is currently used in the treatment of metastatic breast cancer,
  • Both tamoxifen and raloxifene can be used as prophylactic therapy to reduce
    the risk of breast cancer in high risk patients
  • Raloxifene is also approved for the prevention and treatment of osteoporosis in postmenopausal women
  • Clomiphene is useful for the treatment of infertility associated with anovulatory cycles
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16
Q

SERM:

PHARMACOKINETICS?

A
  • The SERMs are rapidly absorbed after oral administration
  • Tamoxifen is extensively metabolized by cytochrome P 450 isoenzymes, including formation of active metabolites via the CYP 3 A 4 5 and CYP 2 D 6
    isoenzymes
  • Raloxifene is rapidly converted to glucuronide conjugates through first pass metabolism
  • These agents undergo enterohepatic cycling, and the primary route of excretion is through the bile into feces
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17
Q

What is the most frequent adverse effects of tamoxifen and toremifene?

A

hot flashes and nausea

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18
Q

endometrial hyperplasia have been reported with tamoxifen therapy.
True or false?

A

True.

Due to its estrogenic activity in the endometrium

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19
Q

What are common adverse effects with raloxifene?

A

Hot flashes and leg cramps

other include an increased risk of deep vein thrombosis pulmonary embolism

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20
Q

What are adverse effect of clomiphene?

A

include headache, nausea, vasomotor flushes visual disturbances, and
ovarian enlargement

21
Q

Which drug cause increases the risk of multiple births (twins or triplets)?

A

clomiphene

22
Q

Where are progestogens secreted?

A
  • females (secreted by the corpus luteum, primarily during the second half of the menstrual cycle, and by the placenta)
  • males (secreted by the testes)
  • It is also synthesized by the adrenal cortex in both sexes
23
Q

PROGESTOGENS: MECHANISM OF ACTION?

A

The high levels of progesterone that are released during the second half of the
menstrual cycle (the luteal phase) inhibit the production of gonadotropin and,
therefore, prevent further ovulation.

24
Q

THERAPEUTIC USES OF PROGESTOGENS?

A
  • contraception

- or the treatment of hormone deficiency

25
Q

For contraception, why progestogens are often used in combination with
estrogens?

A

because of its rapid metabolism, resulting in low bioavailability
- Synthetic progestogens used in contraception are more stable to first pass
metabolism, allowing lower doses when administered orally

26
Q

PROGESTOGENS: THERAPEUTIC USES OF PROGESTOGENS?

A
  1. Medroxyprogesterone acetate is an injectable contraceptive
  2. postmenopausal HT
  3. Progestins are also used for the control of dysfunctional uterine bleeding
  4. treatment of dysmenorrhea
  5. management of endometriosis and infertility
27
Q

PROGESTOGENS: PHARMACOKINETICS?

A
  1. is rapidly absorbed after oral administration
  2. It has a short half life in the plasma
  3. and is almost completely metabolized by the liver
28
Q

which progestin have half life of 30 days?

A

Oral medroxyprogesterone acetate

29
Q

The major adverse effects associated with the use of progestins are?

A

headache, depression, weight gain, and changes in libido

30
Q

Which progestogens may raise serum potassium due to antimineralocorticoid
effects?

A

Drospirenone

31
Q

What are the most common type of oral contraceptives?

A

Products containing a combination of an estrogen and a progestin

32
Q

Differentiate monophasic and triphasic OCP

A
  • Monophasic combination pills contain a constant dose of estrogen and
    progestin given over 21 to 24 days
  • Triphasic oral contraceptive products attempt to mimic the natural
    female cycle and most contain a constant dose of estrogen with
    increasing doses of progestin given over three successive 7 day
    periods

With most oral contraceptives, active pills are taken for 21 to 24 days,
followed by 4 to 7 days of placebo for a total regimen of 28 days

33
Q

The most common estrogen in the combination pills is?

A

ethinyl Estradiol

34
Q

Withdrawal bleeding?

A

Withdrawal bleeding occurs during the hormone free (PLACEBO) interval

Use of extended cycle contraception (84 active pills followed by 7 days of
placebo) results in less frequent withdrawal bleeding

35
Q

Name one POP

A

Norethindrone

36
Q

effectiveness of POP?

A

These preparations are less effective than combination products and they may produce irregular menstrual cycles more frequently

Progestin only pills deliver a low, continuous dosage of drug
taken daily on a continuous schedule

37
Q

progestin only pill may be used for patients who are?

A
  1. Breast feeding (unlike estrogen, progestins do not have an effect on milk
    production) ,
  2. intolerant to estrogen,
  3. smokers
38
Q

CONTRACEPTIVES MECHANISM OF ACTION?

A
  • Estrogen provides a negative feedback on the release of LH and follicle
    stimulating hormone (FSH) by the pituitary gland thus preventing ovulation.
  • Progestin also thickens the cervical mucus, thus hampering the transport of
    sperm.
  • Withdrawal of the progestin stimulates menstrual bleeding during the placebo
    week.
39
Q

most common adverse effects with estrogens?

A

breast fullness , fluid retention ,
headache , and nausea .
- Increased blood pressure may also occur.

40
Q

Adverse effect progestin?

A

Progestins may be associated with depression , changes in libido , hirsutism , and acne .

  • Although rare, thromboembolism, thrombophlebitis, myocardial infarction , and stroke may occur
  • These severe adverse effects are most common among women who are over age 35 and smoke.
  • Combination oral contraceptives should not be used in patients over the age of 35 who are heavy smokers.
41
Q

The androgens are required for?

A

1) normal maturation in the male,
2) sperm production,
3) increased synthesis of muscle proteins and hemoglobin,
4) decreased bone resorption.

42
Q

Drug interaction with contraceptive?

A

Drugs that induce the CYP 3 A 4 isoenzyme (for example, rifampin and bosentan) may significantly reduce the efficacy of oral contraceptives

Concurrent use of these agents with oral contraceptives should be avoided, or an alternate barrier method of contraception should be utilized.

Antibiotics that alter the normal gastrointestinal flora may reduce enterohepatic recycling of the estrogen component of oral contraceptives, thereby diminishing the effectiveness.

Patients should be warned of the possible interaction between antibiotics and oral contraceptives , along with the potential need for an alternate method of contraception during antibiotic therapy.

43
Q

ANDROGENS:

THERAPEUTIC USES?

A

Androgenic steroids are used for males with primary
hypogonadism (caused by testicular dysfunction) or
secondary hypogonadism (due to failure of the
hypothalamus or pituitary).

Anabolic steroids can be used to treat chronic wasting
associated with human immunodeficiency virus or cancer.

An unapproved use of anabolic steroids is to increase
lean body mass, muscle strength , and endurance in
athletes and body builders.

44
Q

ANDROGENS:

PHARMACOKINETICS?

A

This agent is ineffective orally because of inactivation
by first pass metabolism.

Testosterone cypionate or enanthate) are administered
intramuscularly.

Transdermal patches, topical gels, and buccal tablets
of testosterone are also available.

45
Q

Adverse effect androgen in male?

A

In males:
Excess androgens can cause priapism, impotence, decreased spermatogenesis, and gynecomastia. Cosmetic changes such as those described for females may occur as well. Androgens can also stimulate growth of the prostate.

46
Q

Testosterone, the most important androgen in humans?

A

Testosterone

47
Q

What is androgens?

A

The androgens are a group of steroids that have anabolic and/or masculinizing
effects in both males and females.

48
Q

Other androgens secreted by the testes? selain testosterone

A

5 α dihydrotestosterone ( DHT ), androstenedione , and dehydroepiandrosterone DHEA ) in small amounts.

49
Q

Where is testosterone synthesized?

A

is synthesized by Leydig cells in the testes and, in smaller amounts, by thecal cells in the ovaries and by the adrenal gland in both sexes.

Endocrine (4 decks)

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