Progesterone
INTRODUCTION:
- Progesterone is produced by theca cells of the corpus luteum and the placenta
- Metabolism:Liver and excreted in the urine as sodium pregnanediol glucuronide
- Natural progesterone is not active orally and is given only by intramuscular injection in an oil base.
Hypothalamus
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PULSATILE GnRH release
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FSH release from pituitary
↓
Development of G. Follicle.
↓
Oestrogen secretion→Inhibits FSH release
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High oestrogen peak (24 hrs before ovulation)
↓
LH secretion→(LH surge)→Ovulation
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Formation & functions of corpus luteum
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Progesterone (Secretory endometrium
Preparations:
- Progestogens are synthetic compounds belonging to two main groups:
Oestrone or 19-norprogestins :
- Structurally similar to testosterone and pregnane
- In OCPs
17-acetoxy compound :
- Structurally similar to progesterone.
- Used in pregnancy and AUB.
Classification:
| TYPE | EXAMPLES |
| Pure progesterone | Oral and vaginal micronized |
| Pregnane (Derived from progesterone molecule) |
Lynestrenol(allyloestrenol), medroxyprogesterone acetate (depot), megestrol acetate |
| Estrane(derivative of testosterone) | Norethisterone, norethandriol (first generation) |
| Gonane | Levonorgestrel(emergency contraceptive), norgestrel (second generation) |
| Third-generation progesterone | desogestrel, gestodene, norgestimate |
| Hybrid drospirenone | Yasmin 30 μg of EE2 (21 days);Janya 20 μg EE2 (24 days) |
Hybrids (drospirenone):
- Anti-androgens
- Antimineral corticosteroid effect
- Used in premenstrual tension
- Causes hyperkalaemia by decreasing potassium excretion in the urine, less water retention
- Weight gain.
Route Of Administration:
- Orally—Singly or with oestrogen.
- Intramuscular injection monthly, three-monthly as contraceptives.
- Implants—Norplant (contraceptives).
- IUCD impregnated with levonorgestrel (Progestasert, Mirena).
- Vaginal tablet and rings.
- Skin patches.
Action:
- Prepares the uterus for implanatation of the fertilized ovum.
- Swelling and secretory development of the endometrium
- Aids estrogen in myometrial hypertrophy
- Glands increase in tortuosity and excess of secretory substance is accumulated in glandular epithelial cells.
- Lipid and glycogen deposits also increase
- Decreases the frequency and intensity of utrine contractions, thereby helping to prevent expulsion of the implanted ovum but increases the amplitude of contraction.
- Maintenance of secretory activity of uterus during luteal phase
- Development of the breasts
- Negative feedback effects on FSH and LH secretion
- Mild thermogenic action
- Maintenance of pregnancy
- Raising uterine threshold to contractile stimuli during pregnancy
Uses:
Used in treatment of:
- Threatened and recurrent abortions, and in corpus luteal phase deficiency (CLPD):Pure progesterone inj.
- Endometrial cancer(Inj.)
- Contraception
- Endometrial hyperplasia (21 days)
- Abnormal uterine bleeding
- Dysmenorrhoea, premenstrual tension syndrome.
- Endometriosis.
- Endometrial ablation in AUB:Prior to the TCRE (transcervical resection of endometrium), endometrial shrinkageis achieved
- Amenorrhoea:Progesterone challenge test(PCOD):100 mg progesterone will induce withdrawal bleeding if endometrium is primed by oestrogen
- As Post-coital pill(Levonorgestrel 0.75 mg)
- With oestrogen in HRT
- Postponement of menstruation(5 mg norethisterone)
- Abortion(Allyl progesterone)
- Increase the tone of cervical sphincter
- Secretory hypertrophy
- Prevent osteoporosis and allow prolonged GnRH therapy.(‘add back’ therapy with GnRH)
Contraindications:
- Undiagnosed vaginal bleeding
- Breast cancer
- Thromboembolism.
Side Effects:
- Nausea, vomiting
- Headache, mastalgia, Sodium & water retention, leg cramps, weight gain.
- Hirsutism(androgen-related compounds.)
- Depression.
- ↑ LDL & cardiovascular accidents And ↓ HDL
- Deep venous thrombosis, pulmonary embolism(desogestrel and gestodene)
- Irregular menstrual bleeding(Depot medroxyprogesterone acetate)
- Breast tumours
- Withdrawal bleeding with progesterone seen in otherwise amenorrhoeic woman due to Anovulation
- Medroxyprogesterone acetate causes bone loss
- Metrorrhagia( subdermal progesterone implant)
Exam Important
- Effects of progesterone on lipids are Lowers HDL & increases LDL
- Actions of progesterone include Increase the tone of cervical sphincter, Sodium and water retention & Secretory hypertrophy
- Progesterone is produced by Granulosa luteal cells
- A patient with amenorrhea had bleeding after giving a trial of progesterone. This implies Sufficient estrogen, Intact pituitary axis & Normal ovarian function and Intact endometrium
- Positive progesterone challenge test in a patient of secondary amenorrhoea, seen in PCOD
- Withdrawal bleeding with progesterone seen in otherwise amenorrhoeic woman due to Anovulation
- Simple hyperplasia of the endometrium treated with progesterone for 21 days
- The progesterone of choice for emergency contraception is Levonorgesterel
- In a woman on subdermal progesterone implant, the menstrual abnormality seen is Metrorrhagia
- Depot medroxyprogesterone acetate is sparingly used as a contraceptive because it causes Irregular menstrual bleeding
- Progesterone pills Acts by altering cervical mucous secretion, Break ovulation cycle & causes Irregular bleeding
- Oral contraceptive pill containing progesterone which is given in small quantities for 30 days a month is known as Micro pill
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