- Estrogens are major female sex hormones produced by theca cells of overies.
- Estrogens are of two types: sterioidal and non-steriodal.
- Dietheylbetstrol is synthetic estrogen of non-steroid type.
- Estradiol and esterone are natural estrogens.
- Excellent oral absorption but have high first pass metabolism.
- Transdermal formulations of estrogens are used to prevent their first pass metabolism.
- Estradiol is most potent estrogen in clinical use.
- These hormones have intracellular receptors.
- Upon binding to intracytoplamic receptors, hormone-receptor complex migrates into the nucleus.
- This can then bind to hormone responsive element. Eventually, hormone modifies gene expression.
- Female genital tract
- Skeletal system
- Hypogonadal woman as replacement therapy.
- Prevention of postmenopausal osteoporosis
- Hormone replacement in postmenopausal women.
- Increases TAG & HDL
- Reduces LDL
- Total cholesterol
- Note that progesterone has opposite influence: it increases LDL and reduces HDL
- Acne treatment
- Advanced cancer of prostate
- Nausea, vomiting are common side effects.
- Breast tenderness and enlargement can occur.
- Melasma can occur in dark skin females. Endometrial hyperplasia (EH) is serious side effect. Note that tamoxifen has estrogenic activity and is associated with EH. Raloxifen, a SERM is not associated with EH but can cause vacular thrombosis.
- Gall bladder disease can occur. Migraine can become worse.
- Myocardial infarction, deep vein thrombois are other side effects.
- Risk of uterine cancer increase and increase in risk of breast cancer is equvivocal.
- Progesterone is major progestin.
- These are of two types: older (northindrone, norgesterol) and newer (norgestimate and desonorgestrel are
- Newer progestins are free from androgenic side effects.
- Progestins increase body temperature and have thromogenic actions.
- Have no significant effect on carbohydrate profile and are safe in diabetic patients.
- Increase LDL but decreases HDL. Break-through bleeding can occur. Androgenic side effects are common especially with older progestins.
Hormone replacement therapy
- Low dose estrogens are now a days favoured as HRT.
- Tansdermal and vaginal preparations are favoured compared to vaginal ones.
- LDL is reduced but HDL is also reduced (due to progesterone). Triacylglycerol are increased by HRT.
Oral contraceptive pills (AIIMS Nov 09)
- These are of 2 types:
- Minipills (also called as progesterone only pills)
- Combined pills
- Monophasic, biphasic and triphasic preparations.
- Combined pills act by inhibiting ovulation and progesterone only pills do not affect ovulation as much but have peripheral actions.
- Risk of anemia is less.
- Rheumatoid arthristis is less.
- Infections (e.g. PIDs).
- Ovarian cancer risk is less.
- Dysmenorohea and menorrhagia is less.
- Increased risk of endometrial cancer unless progesterone is there.
- Possible increase in risk of breast.
- Precipitation of migraine.
- Worsening of diabetes
- Testosterone is the main androgen. Dihydroepiandrosterone and epiandrostniodone are other androgens.
- Testosterone gets converted into dihydrotestosterone and this is mediated by 5-alpha reductase.
- Anabolic steroids include: stanazolol, nandrolone and oxandrolone etc.
- These are used to build muscles in patients with muscle wasting, those with HIV wasting and treatment of anemia.
- Hepatitis and testicular atrophy.
- Oral testosterone preparations include methyltestosterone and fluoxymesterone.
- Rarely, pelosis and cholestestatic hepatitis have occurred due to these drugs.
- HDL may decrease on chronic treatment. However, cardiovascular risk does not increase.
- BPH or prostatic cancer can get aggravated and erythrocyctosis is a side effect. Increase in frequency of sleep apnea episodes can also occur. Acne can produce cosemetic problem.
This is a male contraceptive and has been tested in china. The drug can produce reversible azoospermia and can cause hypokalemia and subsequent muscle weakness.
Flutamide and biclutamide are two potent androgens that are used for treatment of cancer of prostate.