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Pharmacology 201 > Reproductive Pharmacology > Flashcards

Reproductive Pharmacology Flashcards

1
Q

What is Gonadotropin?

A

It is a hormone produced by the hypothalamus. It circulates and stimulates the release of LH and FSH.

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2
Q

What is negative feedback?

A

As the system produces more hormones, it tells the CNS that it doesn’t need anymore, and hence reduces the amount being made.

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3
Q

What are the Sex Steroids?

A

Estrogens, Progesterones and Androgens.

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4
Q

Describe the take home points of the Menstrual cycle?

A

1) FSH (follicle stimulating hormone) and LH (luteinizing hormone) stimulate follicle growth. The folic is a little ball of cells that contain the immature egg.
2) When the follicle grows, it releases estrogen that inhibits negative feedback since it becomes a secreting hormone of its own.
3) Around day 14 of the cycle, LH surges and stimulates ovulation. The highest levels of FSH and LH are at this point in the cycle. (positive feedback)
4) Post ovulation, the follicle turns into the corpus luteum.
Since the corpus luteum is a hormone secreting structure, it is a good source of estrogen and progesterone. It promotes endometrial growth, which is the thickening of the uterus lining. As a result, at this stage LH/FSH levels are reduced.
5) Degeneration of the corpus luteum results in menstruation in absence of hormonal support.

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5
Q

What are the two types of female contraception?

A

Hormonal and non-hormonal.

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6
Q

What are the two forms of hormonal contraceptives?

A

Synthetic estrogen + synthetic progesterone taken in combination
and Progesterone only pills.

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7
Q

How are combination contraceptives given?

A

Orally

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8
Q

What are the names of combination contraceptives?

A

Usually it is a combination of estrogen in the form of ethinyl estradiol and progestin (usually levonorgestrel or norethindrone).

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9
Q

How do combination contraceptives work?

A

They inhibit FSH and LH release through negative feedback, which prevents ovulation (prevents the release of the egg) and endogenous hormone release. Basically it increases negative feedback on the hypothalamus and inhibits Gonadotropin.

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10
Q

If the birth control inhibits FSH and LH how does the body get the necessary hormones?

A

The birth control provides exogenous estrogen and progesterone that are needed for bodily processes.

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11
Q

What is the standard prescription for this type fo birth control?

A

21 hormone tablets, and 7 placebo pills during the time of the period. The placebo pills are not necessary to be taken but it helps to build habit.

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12
Q

What are the variations in formulations for this type of birth control?

A

Monophasic formulations: identical estrogen/progestin doses

Biphasic/tri-phasic formulations: two/three different combination of doses.

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13
Q

What is the goal of having a birth control with varying dosage?

A

It is designed to more closely approximate natural hormonal variations.

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14
Q

Is one type of variation better than the other?

A

No, there is variability between them both. Universally, one is not better than the other.

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15
Q

What are extended cycle formulations?

A

These are pills that reduce the amount of periods per year.

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16
Q

What is the name of the extended formulations?

A

Seasonale - 84 hormone tablets, 7 placebo.

Lybrel/Amethyst - only combination hormone tablets (no placebo)

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17
Q

Are there long term problems with not having the menstrual component?

A

No significant effects while being on an extended formulation

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18
Q

What are progestin-only contraceptives?

A

Also known as the mini pill, progestin-only pills have a lower dose of progestin than in a combined contraceptive. This means there is less probability of negative feedback on the pituitary gland.

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19
Q

How do progestin-only contraceptives work?

A

It decreases sperm motility through the thickening of the uterine mucus lining. It may also suppress ovulation in some cases.

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20
Q

Why is progestin-only contraceptives used over combination?

A

It is useful when estrogen is inadvisable due to breastfeeding or estrogen–responsive cancers.

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21
Q

How does estrogen impact breastfeeding?

A

Conventional thinking previously believed that estrogen was important for milk production.

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22
Q

What are the potential downfalls of progestin only contraceptives?

A
  • It requires daily administration at the same time everyday.
  • sometimes periods may not occur, which can be worrisome for patients
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23
Q

What are the effectiveness of hormonal contraception?

A
  • Combination and progestin-only have similar rates of effectiveness.
  • When used perfectly: there are 3/1000 unplanned pregnancies
  • Typical use: 80 or 90 pregnancies per 1000 women
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24
Q

What is the discrepancy between perfect and typical use?

A
  • missed dosage, or improper dose timing
  • drug interactions such as St. John Worts, and Phenytoin. These are CYP 450 enzyme induces that cause drug to be metabolized faster
  • altered GI flora: some antibiotics like Rifampin reduce enterohepatic circulation and cause some of the drug to become non polar again and get absorbed.
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25
Q

What is enterohepatic circulation?

A

Liver to intestine

26
Q

What options for long term contraceptives are there?

A

Injectable treatments, subcutaneous implants or implantable devices.

27
Q

What are the key points about injectable treatments?

A
  • Usually they are progesterone only
  • slow release drug
  • Ex: Depo-provera (intramuscularly every 3 months)
28
Q

What are the key points about IUDS?

A

Progestin releasing IUD last 3-5 years and are slow release.

Copper IUDS last 10 years.

29
Q

How do Copper IUDS work?

A

Copper is thought to induce contraception due to its ability to inhibit sperm motility. The foreign copper causes an inflammatory response that makes fertilization not ideal.

30
Q

What are the non-contraceptive uses?

A

They are used as hormone replacement therapy in response to various disorders/

31
Q

How is estrogen used in a non-contraceptive purpose?

A

Primary Hypogonadism - This is what happens when you have lack of female hormones. Estrogen is used to help stimulate growth.
Postmenopausal hormone therapy - estrogen is used to help treat postmenopausal side effects

32
Q

How are progestins used in a non-contraceptive purpose?

A
  • Used to treat Dysmenorrhea (painful menstruation)

- Endometriosis: abnormal growth outside the uterus

33
Q

What are the mild/moderate effects of contraceptives?

A
  • mid-cycle bleeding
  • no period
  • weight gain
  • acne or hirsutism (increased hair growth) this is because some progestins are more androgenic than others and can stimulate testosterone receptors
34
Q

Severe effects of contraceptives?

A
  • depression
  • thromboembolic disease (blood clots)
  • cardiovascular event/stroke
35
Q

How does hormonal contraception relate to cancer?

A
  • it can induce growth stimulating effects due to the estrogen
  • combined contraceptives can increase the risk compared to progestin- only contraceptives
  • use of birth control can increase risk for cervical and breast cancer, although it is temporary
  • contraceptives can also decrease the risk for ovarian and womb cancer
36
Q

What are the three emergency contraceptions?

A

Copper IUD, high-dose progestins and anti-progestins

37
Q

How do Copper IUDS work as an emergency contraceptive?

A

Since it is a foreign substance, it causes a local inflammatory response that causes toxicity to the sperm and ova.

38
Q

How do high dose progestins work as an emergency contraceptive?

A

It aims to inhibit ovulation.

39
Q

How do anti-progestins work as an emergency contraceptive?

A

Ex: Ulipristal

This drug works by preventing fertilization by delaying ovulation by preventing progestins from releasing hormones?

40
Q

What is Mifegysmiso?

A

Mifegymiso a combination treatment with Misoprostol as an emergency contraceptive (induces menstruation)

41
Q

What is the purpose of male pharmacological contraception?

A

it is used to reduce the amount of sperm by reaching “severe oligozoospermia.”

42
Q

What is severe oligozoospermia?

A

It is when the sperm count reaches < 1 million per mL.

43
Q

What is the male contraceptive?

A

it is a progestin/testosterone injection given every two months

44
Q

Case Study 2016

A

Case Study 2016: injectable progestin/testosterone every 6-8 weeks
-was terminated early due to undesirable effects such as acne, increased libido, mood disorders

45
Q

Case Study 2019

A

Case Study 2019: given orally with synthetic testosterone derivative and progestional and endergonic activities
- Side effects: fatigue, headache, decreased libido, mild ED

46
Q

What is erectile dysfunction?

A

the inability to produce of maintain an erection

47
Q

Where does erectile dysfunction stem from?

A

It may arise from chronic disease, medication use, spinal injury (nervous system) circulatory issues, aging and lifestyle factors

48
Q

What drugs can cause ED?

A

cardiovascular drugs like diuretics and psychotropic drugs

49
Q

What is the physiology behind an E?

A

An E is mediated by testosterone, prostaglandins and Nitrous Oxide.
- When sympathetic tone is reduced, it allowed for increased blood flow due to dilation of the cavernosal artery, which as a result, increases corporal spaces (swelling). The E can be maintained by compression of venues that help retain the blood.

50
Q

What does cGMP and cAMP do?

A

It causes smooth muscle relaxation

51
Q

What are the pharmacological treatments available for ED?

A
  • If testosterone levels are low, using a testosterone supplement should be the first line treatment.
  • If testosterone levels are normal, PDE5 inhibitors should be the first line treatment.
  • PGE1 is a second line treatment
52
Q

What are PDE5 inhibitors?

A
  • Phosphodiesterase Type 5 inhibitors (oral)

- these drugs end with “afil” including, sildenafil (viagra), tadalafil (Cialis), Vardenafil (Levitra)

53
Q

What can PDE5 inhibitors not do?

A

They cannot initiate an E, but they can prolong it, hence they would need an E initiator.

54
Q

What is the mechanism of action for a PDE5 inhibitor?

A

PDE5 inhibits the metabolism of cGMP, which mediates the vasodilation by decreasing the calcium concentration.

55
Q

What is a PGE1?

A

Prostoglandin analogue

56
Q

What is the name for a PGE1 ?

A

Alprostadil (Muse and Caverjet)

57
Q

How do PGE1’s work?

A

They stimulate adenylyl cyclase

58
Q

What can PGE1’s do that PDE5 inhibitors cannot?

A

They can initiate an E.

59
Q

What are the side effects of PDE5?

A
  • headache, nasal congestion, facial flushing, myalgia, and altered colour perception due to interaction with PDE6 in retina
  • those on nitrate therapy (alpha adrenoreceptors) should avoid because it will cause too much dilation
    Sidenafil and Vardenafil have shorter half lives than tadalafil
60
Q

Why are PGE1’s a second line treatment?

A
  • requires a direct injection into corpus cavernosum or though urethra
  • training is required
  • lack of spontaneity: must be injected 5-20 minutes before intercourse and lasts < than 1 hour.
61
Q

What are the side effects of PGE1’s?

A
  • pain/bleeding and or bruising at the injection site

- priapism: painful or persistent erection

Pharmacology 201 (20 decks)

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