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Reproduction Exam 1 > Pharmacology of Hormonal Contraceptives > Flashcards

Pharmacology of Hormonal Contraceptives Flashcards

1
Q

Estrogen receptor mechanisms?

A

Steroid/lipophilic
Binds to receptor in cytoplasm
Leads to altered gene expression and mRNA synthesis

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2
Q

What is the most potent estrogen?

A

Estradiol

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3
Q

What are the most common synthetic forms?

A

Ethinyl estradiol and mestanol

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4
Q

Estradiol is not used because?

A

Poor oral bioavailability due to rapid first pass metabolism

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5
Q

Ester does what?

A

Allows longer duration of action

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6
Q

Estrogens cause what?

A

Proliferative changes in the endometrium and increase the amount of cervical mucus

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7
Q

Estrogen ADME

A 
wide VofD
Free drug is the active form
Estradiol is eliminated rapidly but the synthetics are eliminated slower
Into the urine
Show enterohepatic re-circulation
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8
Q

Estrogen Adverse Effects

A

Increased risk of breast, endometrial, cervical, vaginal cancer
Increased risk of MI, DVT, or PE
Severe migraine, n/v, reactivation or exacerbate endometriosis

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9
Q

Pregnanes Example

A

Medroxyprogesterone acetate

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10
Q

Estranes Example

A

Nortestosterone

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11
Q

Estranes Properties

A

Exhibit progestational, androgenic (facial hair) and other activities

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12
Q

Gonanes Example

A

Norgestrel

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13
Q

Gonanes Properties

A

No estrogenic effects, diminished androgenic activity

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14
Q

Progestin activity on the reproductive tract development

A

Thickening of cervical mucous

Decrease progesterone at end of cycle –> menstruation

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15
Q

Progestin activity on CNS

A

Induce 0.6 degrees C –> depressant activity

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16
Q

Progestin activity on metabolic effects

A

Decreased effects of insulin, enhanced fat deposition

17
Q

Progestin Receptor Mechanisms

A

Lipophilic
Receptors in the cell
Leads to altered gene expression and mRNA synthesis

18
Q

Progestin ADME

A

Limited oral bioavailability due to hepatic metabolism
Broad distribution
In urine

19
Q

Progestins bind to?

A

SHBG and albumin (plasma proteins)

20
Q

Progestin adverse effects

A

Etopic pregnancy
Irregularm unpredictable spotting
Weight change
Abnormal glucose tolerance test

21
Q

Monophasic

A

21 days with hormones + 7 without

22
Q

Biphasic

A

Two different doses of hormones for 21 days

23
Q

Triphasic

A

Three different doses of hormones for 21 days

24
Q

Progestin only

A

Less effective
Needs to be taken at the SAME time every day
Irregular and unpredictable menstrual bleeding

25
Q

Combination Oral Contraceptives

A

Progestin + Estrogen
Alters cervical mucous
Inhospitable endometrial lining
PREVENTS ovulation

26
Q

Progestin in contraceptives?

A

Thicken cervical muculs
Slows sperm transport
Impairs implantation in the endometrium
Suppresses LH surge (ovulation)

27
Q

Estrogen in contraceptives?

A 
Stabilizes endometerial lining
Suppresses FSH (prevents a dominant follicle)
28
Q

Menstranol is?

A

50% less potent than ethinyl estradiol bc it has to be convert to it first

29
Q

Extended cycle OCs

A

84 hormone pills +7 days of placebo

4 menstrual cycles per year

30
Q

Continuous cycle OCs

A

Hormones for 21 days and then low-dose E&P for 4-7 days

31
Q

Both extended and continuous cycle can lead to

A

Decreased amount of bleeding and ultimately amenorrhea

32
Q

Side effects of OCs

A

N/V
MI, stroke, emboli
Breast enlargement
Breakthrough bleeding

33
Q

Serious Side Effects of OCs?

A

Blood clots
ACHES
Cancer
Gall bladder

34
Q

ACHES stands for

A 
Abdominal pain
Chest pain
Headaches
Eye problems
Swelling and leg pain (DVT)
35
Q

Precaution for use of COC

A 
>35
Smoking
HTN
Dyslipidemia
Diabetes
Headaches
Breast cancer
Thromboembolism
Obesity
36
Q

Obesity problem?

A

The hormones will go hide in the fat cells of the body and not cause the effects they needed

Reproduction Exam 1 (5 decks)

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