Gonadal steroids & inhibitors Flashcards

1
Q

What are the drug groups used in gonadal steroids and inhibiters?

A

Sex steroids: oestrogens, progestogens, androgens

Inhibitors & antagonists

Selective oestrogen receptor modulators (SERM)

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2
Q

Give some examples of sex steroids and what they are derived from?

A

Progesterone
Oestradiol
Testosterone

Derived from cholesterol

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3
Q

What are the actions of oestrogens?

A
Mild anabolic
Sodium and water retention
Raise HDL, Lower LDL
Decrease bone resorption
Impair glucose tolerance
Increase blood coagulability
?Improve mood, concentration
?reduce Alzheimer's disease
?avoiding first pass effect more favourable
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4
Q

What are the side effects of oestrogens?

A
Breast tenderness
Nausea, vomiting
Water retention
Increase coagulability
Thromboembolism
Impaired glucose tolerance
Endometrial hyperplasia & cancer
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5
Q

What are the ADRs of progesterone/progestogens?

A
Weight gain
Fluid retention
Anabolic
Acne
Nausea, vomiting
Irritability
Depression, PMS
Lack of concentration
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6
Q

What are the actions/side effects of testosterone?

A
Male secondary sex characteristics
Anabolic
Acne
Voice changes
Aggression
Metabolic adverse effects on lipids
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7
Q

What are the routes of administration of sex steroids?

A
Oral
- Oestrogens - Synthetic derivatives
- Progestogens - Synthetic derivatives:
   - Progesterone derivatives
   - Testosterone derivatives
Transdermal
Implants
Nasal
Vaginal
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8
Q

How are steroids transported?

A

Transport bound to SHBG (except progesterone) and albumin
Liver metabolism, progesterone almost totally metabolised in one passage through liver
Metabolites excreted in urine (as glucuronides and sulphates)

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9
Q

What are the different oral contraceptive pills?

A
Oestrogen + progestogen (COCP)
Progestogen only (POP)
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10
Q

What are the different types of COCP?

A

Oestrogen + Progestogen

Monophasic = 21
(Both hormones for 21 days)

Triphasic = 21
(Combination of different doses of the two steroids)

Every Day: ED = 21+7 placebo
(Both hormones for 21 days then 7 days placebo)

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11
Q

Name some different oestrogens used in COCP

A

Ethinylestradiol

Mestranol

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12
Q

Name some different progestogens used in COCP

A

Different generations

1st: norethynodrel
2nd: levonorgestrel, norethisterone
3rd: desogestrel, gestodene, norgestimate
4th: drospirenone

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13
Q

What is the mode of action of COCP?

A

Suppression of ovulation: inhibit FSH, LH
Adverse effect o cervical mucous
Adverse effect on the endometrium

(Metabolised by cytochrome P450)

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14
Q

What are the adverse effects of COCP?

A
Venous thromboembolism
Myocardial infarction
Hypertension
Decrease glucose tolerance
Increase risk of stroke in women with focal migraine
Headaches
Mood swings
Cholestatic jaundice
Increase incidence of gallstones
Precipitate porphyria
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15
Q

Name some progestogens in the POP

A

Levonorgestrel
Norethisterone
Etynodiol diacetate
Desogestrel

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16
Q

What other progestogens are used?

A

Medroxy Progesterone Acetate
- Depot provera: MPA

Etonogestrel

  • Female implants: Implanon
  • Male implants
  • Vaginal ring
17
Q

What is the mode of action of the POP?

A

Adverse effect on cervical mucous
Adverse effect on the endometrium

NB: Poor cycle control

18
Q

Describe emergency contraception

A

Up to 72 hrs after
- Levonorgestrel (levonelle) 1.5mg

Up to 120 hrs
- Ullipristal acetate (ellaOne) 30mg - progesterone
receptor modulator
- Cu IUD