Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Genital System > Drugs Affecting Fertility and Reproduction > Flashcards

Drugs Affecting Fertility and Reproduction Flashcards

1
Q

Estrogen and Progestin Drugs

A

Can be used alone for the Tx of various disorders or the two preparations can be used in combination for HRT in postmenopausal women or for the contraception in childbearing women

As HRT:
Maintains physiology function of estrogens (low
doses used to achieve normal estrogen levels, premarin)

As contraceptive:
It inhibits ovulation by feed back inhibition
of production of pituitary hormones (higher doses are used; estradiol derivatives).

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Types of Estrogens

A
  1. Natural Estrogen

2. Synthetic Estrogens

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Natural Estrogens

A

17β-Estradiol, Estrone, Estriol and Equilin

The natural estrogens: Are produced by the ovaries (Used in contraception)

17β-Estradiol is the major natural ES in humans, half-life of 0.5 - 2 hr.

Other human natural ES are, Estrone and estriol

The horse’s natural estrogens is quilin

Natural ES have a short half-life and unstable, as such, there are used only after modification to synthetic estrogens with better pharmacokinetic advantages

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Synthetic Estrogens

A

Most of the synthetic ES are derivatives of 17β-estradiol:

  1. Estradiol derivatives:
  • Modified estradiol: ethnylestradiol and mestranol
  • Estradiol esters: estradiol valerate and estradiol cyproate
  1. Conjugated estrogens:

-Estrone-SO4 and equilin-SO4
.-Premarin = 70% estrone and 30% equilin sulphates

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Estradiol Derivatives:

Modified Estradiol

A

Ethinylestradiol and Mestranol

Ethinylestradiol = ethynnylated estradiol (active)

Mestranol = methyl-ether-ethinylesradiol. In the body, it is converted back to ethinylestradiol (active form)

Advantage:

Reduced first pass metabolism, and longer half-life >20 hrs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Estradiol Derivatives:

Estradiol Esters

A

Estradiol Cyproate and Estradiol Valerate

Long acting (extended release) forms of estradiol.

Estradiol valerate = Estradiol plus the fatty acid valeric acid.

Estradiol cyproate = Estradiol plus the fatty acid cypionic acid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Conjugated Estrogens

A

The natural ES molecule is conjugated to a sulphate group via an ester bond => Estrone-SO4
, equilin-SO4

In the body, the ester is hydrolysed to release the ES (estrone/equilin)

Advantage: The sulphates exhibit less first pass metabolism

Products: Usually, the two estrogens sulphates are combined in different proportions to achieve optimum activity.

Primarin is a conjugated ES = 70% estrone-SO4 + 30% quilin SO4

Indication: treatment of postmenopausal symptoms or HRT

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

1

A

2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

MOA

A

Bind the ERs found inside and on the surface of target cells of the reproductive system and elsewhere.

ERs are members of the nuclear hormone receptor family which includes adrenal steroid, androgen, progesterone and thyroid hormone receptors.

There are two molecular forms of cytosolic estrogen receptor,which combine to form homo- and heterodimers upon activation by estrogen

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Estrogens:

Pharmacokinetics

A

Estrogens are metabolized by the liver

Undergo extensive enterohepatic metabolism & re-cycling

Excreted in the urine as conjugate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Estrogen:

Adverse Effects

A

Common:

Breast tenderness, Headache, Edema, Nausea, Vommiting, Anorexia and Changes in Libido

Serious:
-Hypertension- increased angiotensinogen synthesis and formation of angiotensin II

  • Thromboembolic disorders-increased hepatic synthesis of clotting factos
  • Gallbladder disease: Estogens increase cholesterol excretion in the bile,accounting for their tendency to cause gallstones

Estogens increases risk for Breast Cancer

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Estogens:

Contra-indications

A

During pregnancy

Should be avoided in women with Uterine fibroids

Used with great caution in women with hepatic diseases, Endometriosis, Thromboembolic diseases and Hypercalcaemia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Progestins:

Types

A
  1. Modified

2. Synthetic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Modified Progesterone

A

Modifed from progesterone:

  • Megestrol (oral),
  • Hydroxyprogesterone caproate (IM),
  • Medroxyprogesterone acetate (IM or oral).

Uses:

Suppression of Ovulation
Endometriosis
Abnormal Uterine Bleeding.(AUB)
2. Synthetic analogues:

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Synthetic Progesterone

A

Used mainly as OC
a)19-nortestosterone derivatives:

-Noretisterone,
-Norgestrel
-Levonorgesterol (have varying degrees of androgenic,
estrogenic, anti-estrogenic activity)

b) Newer products

  • Desogestrel, gestodene, norgestimate: → least androgenic
  • Drosperinone: 17α spirolactone derivative - closest to PG
  • It is progestogenic, anti-androgenic, anti-mineralocorticoid
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Progesterone:

Pharmokinetics

A

Progesterones undergoees extensive first pass metabolism after oral administration and has a short plasma half-life,thus esters have been developed(modified)

Following their absorption, the progesterone esters are bound to albumin in the circulation. The esters are converted to several hydroxylated metabolites and pregnanediol glucuronide in the liver and these metabolites are excreted in the urine.

17
Q

Progesterone:

MOA

A

Inhibits ovulation in 25-40%.
• Thickens cervical mucous, making it impenetrable by sperms
• Makes endometrium unfavorable for implantation (inhibition of
estrogen effects).
• Inhibits tube and uterine contractility

18
Q

Pharmokinetics

A

Progesterones undergoees extensive first pass metabolism after oral administration and has a short plasma half-life,thus esters have been developed(modified)

Following their absorption, the progesterone esters are bound to albumin in the circulation. The esters are converted to several hydroxylated metabolites and pregnanediol glucuronide in the liver and these metabolites are excreted in the urine.

19
Q

Indications

A

Contraceptive: with estrogen or PG only pill.
• Combined with estrogen for post-menopause HRT.
• Rx of endometriosis.
• Pre-menstrual syndrome (PMS)
• Dysmenorrhea (painful menses)
• Menorrhagia (menstrual high blood loss)
Uterine Bleeding

20
Q

Progesterone:

Preparations

A
  1. Dydrogesterone, Medrogestone:
  2. Medroxyprogesterone oral
  3. 19-nortestosterone derivatives.
  4. Anti androgens: cyproterone
21
Q

Dydrogesterone, Medrogestone:

A
  • No androgenic or estrogenic properties
  • Devoid of adrenocorticoid effect→ Do not ↓ adrenal function.
  • Do not ↓ pituitary function.
  • Do not ↑ body temperature.
    • Indications: abnormal uterine bleeding, endometriosis
22
Q

Medroxyprogesterone acetate:

A 
IM/Oral
• Indications:
- Dysfunctional uterine bleeding
- Secondary amenorrhea
- Menopausal symptoms
- Endometriosis (Danazol is better)
- Ca of prostate, breasts, endometrium
23
Q
  1. 19-nortestosterone derivatives.
A

More SE than dydrogesterone, medrogestone:
• Have some estrogenic, androgenic + anabolic
properties.

24
Q
  1. Anti androgens: cyproterone
A

Synthetic derivative of 17- hydroxyprogesterone
• MoA:- suppress androgen release, LH ↓ testoster.
• Indications: severe acne, hirsutism in ♀
- ♂ sexual deviation, inoperable prostate Ca
• Is used in some COCs and HRT
S/E = Weight gain, Hair loss & osteoporosi

25
Q

Progesterone:

Side Effects

A 
SE of progesterones
Responsible for many of the SE of COC or HRT
• Breast engorgement and tenderness
• Bloating
• Mood changes
• Disrupts Lipid profile
• Fluid retention
• Weight gain
• Acne
• Altered libido
26
Q

Use of estrogens in HRT:

A

• Treatment of menopausal symptoms, e.g., hot flushes and
vaginal dryness.
• Treatment of Acne vulgaris & dysmenorrhea
• Treatment of primary hypogonadism
• After surgical removal of ovaries
• Maintenance of the UTI and ↓ bladder problems
• Reduce osteoporosis in early menopause (< 45yr) =>
Slows bone loss from VERTEBRA + FEMORAL NECK in
early menopause.
Note: In HRT, low doses are used, aim is to achieve normal
estrogen levels and function
20

27
Q

Conditions in which estrogen is not

recommended for HRT anymore

A

o not use estrogens:
• To prevent IHD+ stroke!!!!
- Women’s Health Initiative study (WHI) => estrogen alone (premarin
0.625 mg/d) => increased risk of stroke, DVT in women 50 – 79 yrs
after 6.8- 7.1 yr of HRT.
• To prevent alzheimer or improve cognition:
- WHIM’s Study = sub-study of the WHI study => increased risk of
dementia in women 65 yrs after 5.2 yrs of HRT with estrogen; and after
4 yrs of combination therapy (estrogen + PG).
• To stop lactation: bromocriptine is preferred.
• Do not use Diethylstilbestrol any more: => Only for Prostate Ca.
- Was associated with vaginal adeno-Ca in young girls

28
Q

Treatment (Rx) and counseling of the

Post menopausal female

A

• Individualize therapy: weigh benefit vs. risk.
• Main indication: to relieve of vasomotor symptoms if no
contraindications
- it is the only drug that helps today.
• Start at low dose: evaluate at 1 month
• Review need once a year
• For early menopause (<45): Rx till 50 yrs to prevent
steoporosis.
• Note: Don’t use in patients over 60 yrs
- NB: For prevention of osteoporosis only: SERMS or
bisphophonates a better option.
• Self breast exam prn; mammogram q1 yr

29
Q

Contraceptives

A

Contraceptives are drugs or devices, or devices that release drugs that are used to prevent conception,the fertilization of an egg by sperm and resulting pregnancy

Contraceptives act locally in the female reproductive tract.

These include agents that kill sperms-called spermicides:

-Nonoxynol-9

Genital System (12 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions