progesterone and oestrogen Flashcards
Where is estrogen synthesized?
ovaries and placeta
The 3 main endogenous oestrogen types
oestradiol (most potent)
oestrone 1/3 potency
oestriol
functions of estrogen
- sexual maturation
- responsible for follicular proliferation
- stimulate growth of milk ducts
- decreases bone reabsorption and plasma cholesterol
Activation MOA of estrogen
diffuses through membrane and binds to alpha receptor on nucleus, causing activation, which will result in interaction with chromatin to initiate hormone specific RNA synthesis. Resulting in the synthesis of proteins that mediate estrogen effects
Repressive MOA of estrogen
estrogen diffuses through membrane and binds to beta receptor on nucleus which has a repressor domain
therapeutic uses of estrogen
- contraception
- post-menopause hormone therapy
- Osteoporosis
- Primary hypogonadism
estrogen adverse effects
- breast tenderness
- nausea
- hypertension
- thromboembolism
Selective estrogen receptor modulators SERMs
Tamoxifen
Raloxifene
Clomiphene
Toremifen
Raloxifene indication and MOA
indication: prevention of osteoporosis
MOA: binds to estrogen receptors and inhibits bone reabsorption. Lowers total cholesterol and LDL
Toremifen Indication and MOA
Indication: hormone dependent breast cancer
MOA: Is an estrogen antagonist, in breast cancer tissue. does not increase risk of endometrial cancer
Tamoxifen Indication and MOA
Indication: hormone receptor positive breast cancer
MOA: Is an estrogen antagonist in breast cancer tissue. Partial agonist in the uterus
Clomiphene Indication and MOA
Indication: infertility associated with anovulatory cycle
MOA: partial estrogen agonist. Inhibits ER in hypothalamus and interfere with - feedback. Increases secretion of GnRH stimulating ovulation
Anti-estrogen drug, it indication and MOA
Fulvestrant
Indication: beast cancer after failure of tamoxifen
MOA: estrogen receptor down regulator. Binds to estrogen receptor competitively. Blocks trophic action of estrogen without having estrogen like activity
functions of progesterone
- implantation and maintenance of pregnancy
- stimulate development of alveoli in milk duct
- alters endometrium from proliferative to secretive menstrual cycle
Therapeutic uses of progesterone
- contraception
- post-menopausal hormone therapy
- endometriosis
- menstrual disorders
- luteal phase support
progestin adverse effects
- Headache
- Changes in libido
- Weight gain
- Depression
Anti-progestin, it’s indication and MOA
Mifepristrone
Indication: Abortifacient, sensitizes uterus to action of prostaglandind
MOA: Synthetic progesterone antagonist, with partial agonistic activity. Given orally
Types of oral contraceptives
- combination
- only progesterone
- non-steroidal progestin
Contra-indication for oral contraceptives
- pregnancy
- breast cancer
- liver disease
- hperlipideamia
oral contraceptive adverse effects
- oedema
- weight gain
- reversible hypertension
- acne and vaginal infections
Administration for combined contraceptives
Taken for 21 consecutive days, with placebo pill days
estrogen and progesterone formulation for combined contraceptives
estrogen: ethinyloestradiol
Progesteon:
1st- norethisterone
2nd: levonorgestrel
3rd: desogestrel or gestodene
which progesterone types are preferred for diabetic patients and why?
3rd gen desogesrel and gestodene. minimal impact on glucose levels and lipid profile
progesterone only contraceptives
- Norethisterone
- Levonorgestrel
- Evogestrel
MOA of progesterone only contraceptives
Cervical mucus made inhospitable to sperm. Prevents endometrial implantation
Non steroidal progestin contraceptives
Drospirenone
Yasimin and Yaz
Qlaira
Adverse effects of NSP contraceptives
- Irregular menstrual bleeding
- Bloating, mood changes
- nausea, headache, appetite disturbances
Contraceptive interaction with drugs that induce CYP450 enzymes
drugs like rifampicin reduce absorption due to diarrhea and vomiting
Contraceptive interaction with antibiotics
Lead to alterations in gut flora, result in interruption of enterohepatic cycle of OC’s, increasing fecal excretion of oestrogen and decreasing the efficacy of OC’s
Other drug interactions with contraceptives
- Reduce efficacy of oral anticoagulants
- protease inhibitors
- adversely affects anti-hypertensive therapy by increasing renin conc
mixed post coital contraception formula and dosage
- ethinyloestradiol and levonorgestrel
- 12 hourly for 2 doses within 72 hours
Long acting reversible contraceptives
- Long acting injectable
- Intrauterine device(IUD)
- ## Subdermal progesterone implants
Preparations used in Hormone replacement therapy
- Conjugated oestrogen
- Medroxyprogesterone
used in combination with premphase
Contraindications for HRT
- Oestrogen-dependent cancer
- Pregnancy
- Liver disease
- Breast feeding
- Breast nodules
Adverse effects of HRT
- Nausea & vomiting
- Weight changes
- Breast enlargement
- PM like syndrome
- Fluid retention
