Hormonal Contraception

Dewi Selvina Rosdiana

Reproduction module
UNIB, 17-18 N0v 2011

Regulation of estrogen and testosteron

Hormonal relationships of the human menstrual cycle

ESTROGENS
Sources
ovarium, testis, adrenal cortex, placenta
Preparations
Natural (steroidal) : estradiol, estrone, estriol
parenterally
Synthetic
- steroidal : ethinyl estradiol, mestranol, quinestrol
- nonsteroidal : diethylstilbestrol, dienestrol,
chlorotrianisene, methallenestril
orally

Physiologic effects
Responsible for pubertal changes in girls and
secondary sexual characteristics
Neuroendocrine control of the menstrual cycle
Metabolic Effects :
Bones : stimulates osteoblasts production & activity
osteocyte survival by inhibiting apoptosis
the number and activity of osteoclasts

Carbohidrat metabolism
slightly fasting glucose & insulin
doesnt have major effects on CH-metabolism

 Lipid metabolism
- Slightly serum triglycerides and
- Slightly total cholesterol, LDL & HDL
From 2 large trials of HRT, E+P or E-only
regiments dont provide any protection from
cardiovascular disease
- chol. secretion & bile acid secretion
leads to saturation of bile with chol
risk of gallstone formation

both coagulation & ffibrinolytic pathways

imbalance in these two opposing activities may
cause adverse effects

Pharmacokinetics
- oral, parenteral, topical complete absorption
- Binds srongly to 2 globulin (SHBG) sex
hormone-binding globulin
- Hepatic metabolism, by CYP3A4
- Excretion : urine & feses

PROGESTERONE
Sources of natural progesteron = Estrogen
a precursor of hormonal steroid
synthetic 19-nor testosterone derivatives

Physiologic effects
Decreasing the frequency of GnRH pulses
Leads to the development of a secretory
endometrium
Influences the endocervical glands
a scant, viscid material
Maintenance of pregnancy
Suppresses menstruation and uterine
contractility

CNS effects:
Increase the basal body temperature
May have depressant and hypnotic actions
Mamary gland
Development of the mammary gland
Acting with estrogen
Proliferation of the acini of the mammary gland
Metabolic effects
Stimulates lipoprotein lipase activity and seems
to enchance fat deposition
Increase LDL, reductions in serum HDL levels

PK:
Progest orally rapid metabolism
Low bioavailability short duration of action
Esters longer action : medroxyprogesterone
acetate (MPA)
Excretion : urine and feses

HORMONAL CONTRACEPTION
Contraception : to prevent conception
Methods : hormonal preparations
- Oral pill
- Injection
- Subcutaneous Implants
- Transdermal patches
- Intrauterine devices that release hormones

Combination oral contraceptive

Containing both an estrogen and a progestin
Mechanism of action:
Inhibition of pituitary function GnRH
LH & FSH inhibition of ovulation

Adverse effects :
Nausea, edema, mild headache
Withdrawal bleeding sometimes fails to occur
Acne and hirsutisme (mediated by androgenic activity of
norprogestin)

Combination oral contraceptive

Combination oral contraceptive

Adverse effects : dose dependent
development of current low dose preparation
Low dose preparation: the incidence of adverse effects
Changes in BP are not significant
Do not produce unfavorable lipid profiles, although
slight increases in TG have been reported
Minimal effect on hemostatic, but in smoker women
hypercoagulable condition
longterm users, > 5 years, with persisten HPV infection
risk of cervical cancer by about twofold

risk of colorectal cancer and endometrial cancer

No significant difference in cumullative risk of breast ca

Contraindication
Absolute :History of thromboembolic disease,
cerebrovascular disease, MI, CAD, known or
suspected breast ca, reproductive tract ca,
hormone-dependent neoplasia, abnormal
undiagnosed vaginal bleeding, impaired liver
function, women >35 years who smoke heavily
Relative : migraine, headaches, hypertension,
DM, gallbladder disease.

Progestine-only contraceptive
= Minipill
Slightly less efficacious than combination oral
contraceptive
Mechanism of action :
Thickening of cervical mucus
sperm penetration
Endometrial alterations that impair implantation
Prevent ovulation (in only 60-80% of cycles), by
decreasing the frequency of GnRH pulses.

Progestine-only contraceptive

Progestine-only contraceptive
Adverse effects :
Bleeding irregularities, spotting, longterm
amenorrhea
Headache, mood changes, weight gain, HDL ,
LDL , Acne
Contraindication :
Undiagnosed vaginal bleeding, benign or
malignant liver disease, breast ca,
thrombophlebitis or thromboembolic disorders.

The Morning-After Pill

= emergency contraceptive pills
= postcoital contraceptive
Mechanism of action :
Inhibits or delays the ovulation
Alterations in endometrial receptivity for implantation
Thickening of cervical mucus sperm penetration
Alterations in tubular transport of sperm, egg, or
embryo; effects on fertilization.
However, emergency contraceptives do not interrupt
pregnancy after implantation.

The Morning-After Pill

The Morning-After Pill

The 1st dose should be taken anytime within 72
hours after intercourse, and should be followed
12 hours later
Reduces risk of pregnancy following unprotected
intercourse (60-80%)
Adverse effects :
Nausea (50%), vomiting (20%)