progesterone and oestrogen Flashcards

1
Q

Where is estrogen synthesized?

A

ovaries and placeta

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2
Q

The 3 main endogenous oestrogen types

A

oestradiol (most potent)
oestrone 1/3 potency
oestriol

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3
Q

functions of estrogen

A
  • sexual maturation
  • responsible for follicular proliferation
  • stimulate growth of milk ducts
  • decreases bone reabsorption and plasma cholesterol
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4
Q

Activation MOA of estrogen

A

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

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5
Q

Repressive MOA of estrogen

A

estrogen diffuses through membrane and binds to beta receptor on nucleus which has a repressor domain

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6
Q

therapeutic uses of estrogen

A
  • contraception
  • post-menopause hormone therapy
  • Osteoporosis
  • Primary hypogonadism
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7
Q

estrogen adverse effects

A
  • breast tenderness
  • nausea
  • hypertension
  • thromboembolism
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8
Q

Selective estrogen receptor modulators SERMs

A

Tamoxifen
Raloxifene
Clomiphene
Toremifen

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9
Q

Raloxifene indication and MOA

A

indication: prevention of osteoporosis
MOA: binds to estrogen receptors and inhibits bone reabsorption. Lowers total cholesterol and LDL

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10
Q

Toremifen Indication and MOA

A

Indication: hormone dependent breast cancer
MOA: Is an estrogen antagonist, in breast cancer tissue. does not increase risk of endometrial cancer

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11
Q

Tamoxifen Indication and MOA

A

Indication: hormone receptor positive breast cancer
MOA: Is an estrogen antagonist in breast cancer tissue. Partial agonist in the uterus

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12
Q

Clomiphene Indication and MOA

A

Indication: infertility associated with anovulatory cycle
MOA: partial estrogen agonist. Inhibits ER in hypothalamus and interfere with - feedback. Increases secretion of GnRH stimulating ovulation

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13
Q

Anti-estrogen drug, it indication and MOA

A

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

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14
Q

functions of progesterone

A
  • implantation and maintenance of pregnancy
  • stimulate development of alveoli in milk duct
  • alters endometrium from proliferative to secretive menstrual cycle
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15
Q

Therapeutic uses of progesterone

A
  • contraception
  • post-menopausal hormone therapy
  • endometriosis
  • menstrual disorders
  • luteal phase support
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16
Q

progestin adverse effects

A
  • Headache
  • Changes in libido
  • Weight gain
  • Depression
17
Q

Anti-progestin, it’s indication and MOA

A

Mifepristrone
Indication: Abortifacient, sensitizes uterus to action of prostaglandind
MOA: Synthetic progesterone antagonist, with partial agonistic activity. Given orally

18
Q

Types of oral contraceptives

A
  • combination
  • only progesterone
  • non-steroidal progestin
19
Q

Contra-indication for oral contraceptives

A
  • pregnancy
  • breast cancer
  • liver disease
  • hperlipideamia
20
Q

oral contraceptive adverse effects

A
  • oedema
  • weight gain
  • reversible hypertension
  • acne and vaginal infections
21
Q

Administration for combined contraceptives

A

Taken for 21 consecutive days, with placebo pill days

22
Q

estrogen and progesterone formulation for combined contraceptives

A

estrogen: ethinyloestradiol
Progesteon:
1st- norethisterone
2nd: levonorgestrel
3rd: desogestrel or gestodene

23
Q

which progesterone types are preferred for diabetic patients and why?

A

3rd gen desogesrel and gestodene. minimal impact on glucose levels and lipid profile

24
Q

progesterone only contraceptives

A
  • Norethisterone
  • Levonorgestrel
  • Evogestrel
25
Q

MOA of progesterone only contraceptives

A

Cervical mucus made inhospitable to sperm. Prevents endometrial implantation

26
Q

Non steroidal progestin contraceptives

A

Drospirenone
Yasimin and Yaz
Qlaira

27
Q

Adverse effects of NSP contraceptives

A
  • Irregular menstrual bleeding
  • Bloating, mood changes
  • nausea, headache, appetite disturbances
28
Q

Contraceptive interaction with drugs that induce CYP450 enzymes

A

drugs like rifampicin reduce absorption due to diarrhea and vomiting

29
Q

Contraceptive interaction with antibiotics

A

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

30
Q

Other drug interactions with contraceptives

A
  • Reduce efficacy of oral anticoagulants
  • protease inhibitors
  • adversely affects anti-hypertensive therapy by increasing renin conc
31
Q

mixed post coital contraception formula and dosage

A
  • ethinyloestradiol and levonorgestrel
  • 12 hourly for 2 doses within 72 hours
32
Q

Long acting reversible contraceptives

A
  • Long acting injectable
  • Intrauterine device(IUD)
  • ## Subdermal progesterone implants
33
Q

Preparations used in Hormone replacement therapy

A
  • Conjugated oestrogen
  • Medroxyprogesterone
    used in combination with premphase
34
Q

Contraindications for HRT

A
  • Oestrogen-dependent cancer
  • Pregnancy
  • Liver disease
  • Breast feeding
  • Breast nodules
35
Q

Adverse effects of HRT

A
  • Nausea & vomiting
  • Weight changes
  • Breast enlargement
  • PM like syndrome
  • Fluid retention