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3002 > 77 Drugs affecting reproductive function > Flashcards

77 Drugs affecting reproductive function Flashcards

1
Q

Where are oestrogens synthesised?

A
  • Ovary and the placenta

* Small amounts in adrenal cortex and testis

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2
Q

What are the 3 main endogenous oestrogens in humans?

A
  • Oestriol
  • Oestrone
  • Oestradiol
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3
Q

What is the most potent and principal oestrogen secreted by the ovary?

A

Oestradiol

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4
Q

What is the main mechanism of action of oestrogens?

A

Involves interaction with nuclear receptors in target tissues to regulate gene transcription

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5
Q

Clinical uses of oestrogens?

A
  1. Induce artificial menstrual cycle
  2. Contraception
  3. At or after menopause to prevent symptoms e.g. protect against osteoporosis, vaginal dryness and flushing
  4. Replacement therapy in primary ovarian failure (Turner’s syndrome) to promote sexual maturation
  5. Prostate and breast cancer
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6
Q

What are the side effects of oestrogens?

A
  • Increase risk of thromboembolism (osteoporosis)

* Cause feminisation in males

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7
Q

Oestrogen administration options?

A
  • Oral, transdermal, intramuscular, implantable and topical

* Well absorbed from the gut, across the skin and mucous membranes

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8
Q

What are the natural and synthetic oestrogens?

A
  • Natural - estradiol, estriol

* Synthetic - mestranol, ethinylestradiol, diethylstilbestrol

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9
Q

Binding of oestrogens in the blood?

A
  • To albumin and to a sex hormone-binding globulin

* Thus making the oestrogens inactive

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10
Q

What are SERMs?

A
  • Selective Estrogen Receptor Modulators
  • Competitive antagonists or partial agonists of oestrogens
  • Drugs that are selective oestrogen agonists in some tissues but antagonists in others are bing developed
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11
Q

3 examples of SERMs?

A
  1. Clomiphene
  2. Tamoxifen
    3 Raloxifene
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12
Q

Action of clomiphene?

A

Acts as an oestrogen antagonist in the hypothalamus and anterior pituitary to inhibit the negative feedback effect to induce ovulation

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13
Q

Use and action of tamoxifen?

A
  • Used in oestrogen-dependent breast cancer

* Anti-oestrogenic action on mammary tissue

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14
Q

Use and action of raloxifene?

A
  • Treat and prevent osteoporosis

* Oestrogen action on bone

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15
Q

What is progesterone secreted by?

A
  • Corpus luteum late int he menstrual cycle

* Placenta during pregnancy

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16
Q

What is the mechanism of action of progestogens?

A
  • Acts on the progesterone receptor to regulate gene transcription in target tissues
  • Oestrogen stimulates synthesis of PR • Progesterone inhibits the synthesis of oestrogen receptors
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17
Q

Why is progesterone not used therapeutically?

A

Due to rapid clearance

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18
Q

What are progestins?

A

Synthetic derivatives of progestogens

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19
Q

Name 3 examples of progestins?

A
  1. Medroxyprogesterone
  2. Hydroxyprogesterone
  3. Norethisterone (weak androgen)
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20
Q

Therapeutic uses for progestogens?

A
  1. Oral contraceptive pill along or combined with oestrogen
  2. Progesterone only injectable or implantable contraception or part of intrauterine contraceptive
  3. Combined with oestrogen for oestrogen replacement therapy (women with intact uterus) to prevent:
    • Endometrial hyperplasia
    • Carcinoma
    • Endometriosis
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21
Q

What is Danazol? Uses?

A

Modified progestogen used to treat sex-hormone dependent conditions:
• Endometriosis
• Breast dysplasia
• Gynaecomastia

22
Q

Mechanism of action of Danazol?

A

Acts via the progesterone receptor to inhibit gonadotrophin production

=> Reduces oestrogen synthesis in women and androgen synthesis in men

23
Q

Side effects of Danazol?

A
  • GI disturbances
  • Weight gain
  • Fluid retention
  • Dizziness
  • Headaches
  • Menopausal symtpoms
  • Androgenic activity so virlizing when given to women
24
Q

Adverse effects of progestogens?

A
  • Acne
  • Fluid retention
  • Weight gain
  • Depression
  • Change in libido
  • Breast discomfort
  • Menstrual cycle irregularity
  • Increased thromboembolism
25
Q

What is mifepristone and its use?

A
  • Anti-progestogen
  • Combination with prostaglandin analogues - effective medical alternative to surgical termination of early pregnancy (up to 9 wks)
26
Q

What is in the combined contraceptive pill?

A
  1. Oestrogen - ethinyloestradiol, mestranol
  2. Progestogen - norethisterone, levonorgestrel, ethynodiol or in 3rd generation pills (desogestrel, gestodene - more potent and have less androgenic actions)
27
Q

How are combined contraceptive pills meant to be taken?

A
  • Taken for 21 consecutive days followed by 7 days pill free to allow a withdrawal bleed
  • Menstrual cycles return quickly after discontinuation
28
Q

Mode of action of the combined contraceptive pill?

A
  • Oestrogen inhibits the secretion of FSH via -ve feedback on the anterior pituitary and thus surpasses development of the ovarian follicle
  • Progestin inhibits LH secretion and prevents ovulation
  • Oestrogen and progestin act in concert to alter the endometrium in such a way to discourage implantation
  • May interfere with the coordinated contractions of the cervix, uterus and fallopian tubes that facilitate fertilisation and implantation
29
Q

Side effect of the combined contraceptive pill?

A
  • Mild nausea, flushing, dizziness and bloating
  • Weight gain, skin changes (acne or pigmentation), depression or irritability
  • Amenorrhea of variable duration after cessation of taking the pill
  • Serious withdrawal effects are rare
  • Small no. of women develop reversible hypertension
  • Small increase in the risk of thromboembolism
30
Q

3 examples of progestin only contraceptive pill?

A
  1. Norethisterone
  2. Levonorgestrel
  3. Ethynodiol diacetate
31
Q

How often is progestin only contraceptive pill taken?

A

Taken daily without interruption (unlike combined)

32
Q

Mode of action of progestin only contraceptive pill?

A
  • Primarily on the cervical mucous which is made inhospitable to sperm
  • Probably also hinders implantation through its effect on the endometrium and on the motility and secretions of the fallopian tubes
33
Q

Progestin only contraceptive pill is a suitable alternative to whom?

A
  • To women in whom oestrogen-containing pills are contraindicated
  • Suitable for women whose blood pressure rises unacceptably during treatment with the combined pill
34
Q

What is a post-coital (emergency) contraception?

A

Oral administration of levonogestrel alone or in combination with oestrogen is effective if taken within 72 hours and repeated 12 hours later

35
Q

What is 2 long-acting progestogen only contraception?

A
  1. Medroxyprogesterone acetate - given intramuscularly as a contraceptive
  2. Levonorgestrel - implanted subcutaneously - capsules release their progestogen slowly over 5 years
36
Q

Symptoms of menopause?

A
  • Headaches and hot flashes
  • Hair becomes thinner and loses lustre
  • Teeth loosen and gums recede
  • Risk of CVD
  • Breasts droop and flatten
  • Nipples become smaller and flatten
  • Backaches
  • Skin and mucous membrane become drier, skin develops a rougher texture
  • Abdomen loses some muscle tone
  • Body and pubic hair becomes thicker and darker
  • Stress or urger incontinence
  • Vaginal dryness, itching and shrinking
  • Bones lose mass and become more fragile
37
Q

What is the process of postmenopausal HRT?

A

Involves either cyclic or continuous administration of low dose oestrogen’s (estradiol, estriol) with or without progestogens

38
Q

Uses of postmenopausal HRT?

A
  • At menopause ovarian function decreases and oestrogen levels fall
  • Improves the symptoms caused by reduced oestrogen e.g. hot flushes and vaginal dryness
  • Prevents and treated osteoporosis
39
Q

Drawbacks of postmenopausal HRT?

A
  • Withdrawal bleeding
  • Increased risk of endometrial cancer (if oestrogen’s unopposed by progesterone)
  • Increased risk of thromboembolsim
40
Q

Testosterone synthesis?

A
  • Testosterone is the main androgen
  • Synthesised by Leydig cells in testes and in smaller amounts in the adrenals and ovaries
  • GnRH acts on the anterior pituitary to release both FSH and LH
  • LH stimulates androgen secretion
41
Q

Clinical uses of androgens?

A

Intramuscular depot injections or patches of testosterone esters used for replacement therapy in:

  • Male hypogonadism dues to pituitary or testicular disease
  • Female hypo sexuality following ovariectomy
42
Q

Mechanism of action of androgens in HRT?

A

Via nuclear receptors and control gene expression

43
Q

Name 2 anti androgens and their use?

A
  1. Flutamide
  2. Cyproterone

• Used a part of treatment of prostatic cancer

44
Q

Name a dihydrotestosterone synthesis inhibit and their use?

A

Finasteride - used in benign prostatic hypertrophy

45
Q

What anabolic steroid increases protein synthesis and muscle development?

A

Nandrolone

46
Q

Uses of anabolic steroids?

A
  • Therapy of aplastic anaemia

* Increase protein synthesis and muscle development - abused by some athletes

47
Q

Side effects of anabolic steroids?

A
  • Infertility
  • Salt and water retention
  • Coronary heart disease
  • Liver disease
48
Q

Name 2 gonadotrophin-releasing hormone analogues?

A
  1. Gonadorelin - same AA sequence as the endogenous form but made synthetically
  2. Nafarelin - more potent analogue
49
Q

Mechanism of action of gonadotrophin-releasing hormone analogues (e.g. Gonadorelin, Nafarelin) ?

A

Given in pulsatile fashion will stimulate release of the gonadotrophin (FSH and LH)

50
Q

Uses of gonadotrophin-releasing hormone analogues (e.g. Gonadorelin, Nafarelin) ?

A
  • Administration of GnRH in a continuous regimen will induce gonadal suppression
  • Used in sex hormone-dependent conditions (e.g. prostate and breast cancers, endometriosis and large uterine fibroids)
51
Q

Uses of gonadotrophins?

A
  • Gonadotrophin (FHS and LH) preparations are used to treat infertility caused by lack of ovulation as a result of hypopituitarism following failure of treatment with clomiphene
  • Treat meant with infertility due to hypogonadotropic hypogonadism

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