Mechanism of action of hormonal contraceptives (3 diff ways)
Inhibit hormone release, inhibit sperm migration or inhibit ovum implantation
Inhibition of hormone release- contraceptives
inhibits the release of gonadotropin releasing hormone from the hypothalamus
results in the pituitary gland not being stimulated to release follicle stimulating hormones and luteinizing hormones
- results in no follicular maturation and the inhibition of ovulation
Gonadotropin
Hormone that stimulates the pituitary gland
Inhibition of sperm migration- contraceptives
Progestins alter the secretions of the endocervical gland into a scant thick fluid that makes sperm migration difficult
Progestins
Progesterone like hormones
- sometimes has androgenic properties
Inhibition of ovum implantation- contraceptives
Hormonal contraceptives cause the endometrium to not fully develop making it unsuitable for a fertilized ovum
Oral contraceptives
One of the most effective
- fixed combination, multiphasic and progestin only
- convenient, cheaper non invasive and self administered but absorption varies in individuals and is subject to first pass effect
Fixed combination oral contraceptives
Type of oral contraceptive
- fixed combination of estrogen and progestin
- take for 21 out of 28 days of a cycle ( many pill menstruate in the week off it)
- some people fully eliminate menstruation
-99.7 percent effective with perfect use and 92 percent with typical use
Multiphasic oral contraception
Oral contraception
- Fixed amount of estrogen and variable
amounts of progestin increasing week to week
- reduces the hormonal dose , adverse effects and mimic bodies natural cycle more closely
Progestin only oral contraceptive and effetiveness
A daily low dose of progestin that’s taken for as long as the patient needs
- less excepted by all patients,
- breakthrough bleeding can occur
- slightly less effective 98 percent perfect use 92 typical
Mild adverse affects of oral contraceptives
Nausea, Edema, headache HEN
-Nausea is caused by estrogen but usually stops after 1 or 2 cycles
Edema- swelling in the bodies tissue, often in feet, legs, hands, face and abdomen
Headache- drug will be stopped if severe
Moderate effects of oral contraceptives
WG,BB,A,PH,I
Weight gain, breakthrough bleeding, increased skin pigmentation from estrogen, acne from progestin
Hirsutism- abnormal growth of hair on the face or body due to progestin
Increased Utis and vaginal infections
- sometimes lose period (amenorrhea)
Serious adverse effects of combined pill contraceptives
BHSCH
Blood clots- estrogens induce production of some factors for blood coagulation changes from 1/1000 chance to 3/1000 chance
Heart attack- Mix of estrogen and progestin increases risk mostly in smokers and obese patients- this is associated with progestin
Stroke- increased risk esp in those over 35
Hypertension- Cardiovascular disease more prevalent esp over 35
cancer- endometrial, colorectal and ovarian risk is REDUCED
When can you not take combined oral contraceptives
Thromboembolic disease, blood clotting, cerebrovascular disease, impaired liver function, liver disease, estrogen dependent neoplasia, pregnancy (congenital effects on child, limb deformities masculization or undescended testes aka cryptor chidism), undiagnosed bleeding, carcinoma of breast
Non contraceptive benefits of oral contraceptives
DEPOT contraceptive
Intramuscular shot
- A slows release formulation contraceptive injection
- progestin dose is injected every 3 months with contraception in that time
PRO: dose not controlled by patients, steady supply, avoids first past effect
CONS: more invasive, volume od drug is limited
99.7 pervcent perfect use, 97 typical use
Adverse effects of depot contraceptives
Similar to the progestin only pill
- breakthrough bleeding, alter profile of plasma lipids, increase low density lipid proteins and decrease high density
- small increase in risk of coronary vascular cancer in older versions
-
IUD- intrauterine devices
Implanted into the uterus
- the most common type releases levonorgestrel which is a progestin
- sometimes effective up to 8yrs
- long term and reversible
99.9 percent effective rate for typical and perfect use
Adverse effects of IUDS
Heaving menstrual flow(often resolves within a couple of months)
- pelvic discomfort
- increased risk of UTIs
Transdermal Contraceptive patch
- pros, cons and how effective is it
Estrogen and progestin patch that’s applied to the skin
- the drug is delivered at a constant rate for 7 days (3 patches per cycle)
- same mechanism of action as other estrogen-progestin contraceptives
PROS: convenient, steady drug supply avoiding first pass effect
CONS: expensive and can cause irritation to skin
99.7 percent perfect use, 92 percent perfect use
Male contraceptives
Spermatogenesis
Hypothalamus releases gonadotropin which stimulates anterior pituitary gland to release follicle stimulating hormone seminiferous tubules that make sperm and luteinizing hormone Ludwig cells that produce testosterone
testosterone is responsible for male sex characteristics and the prescene of it in the body prevents hypothalamus from releasing more gonadotropin preventing overpdouction of testosterone
this is why male attemptd at contraceptives lead to decreased testosterone and decrease sex drive
Androgen based potential male contraceptives
Androgen can inhibit the release if gonadotropin and spermatogenesis
Injectable form
2 main problems: only eighty percent responded with lowering of less than 4 millimeter
- excess androgen led to increased sex characteristics including aggression
Estrogen based male contraceptive
Suppress GNRH release and spermatogenesis
issue: decrease in testosterone, sex drive and feminine characteristics were observed
attempted to add androgens
- only 60 percent of people responded and became infertile, many adverse effects