Gonadal steroids & inhibitors Flashcards
What are the drug groups used in gonadal steroids and inhibiters?
Sex steroids: oestrogens, progestogens, androgens
Inhibitors & antagonists
Selective oestrogen receptor modulators (SERM)
Give some examples of sex steroids and what they are derived from?
Progesterone
Oestradiol
Testosterone
Derived from cholesterol
What are the actions of oestrogens?
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
What are the side effects of oestrogens?
Breast tenderness Nausea, vomiting Water retention Increase coagulability Thromboembolism Impaired glucose tolerance Endometrial hyperplasia & cancer
What are the ADRs of progesterone/progestogens?
Weight gain Fluid retention Anabolic Acne Nausea, vomiting Irritability Depression, PMS Lack of concentration
What are the actions/side effects of testosterone?
Male secondary sex characteristics Anabolic Acne Voice changes Aggression Metabolic adverse effects on lipids
What are the routes of administration of sex steroids?
Oral - Oestrogens - Synthetic derivatives - Progestogens - Synthetic derivatives: - Progesterone derivatives - Testosterone derivatives Transdermal Implants Nasal Vaginal
How are steroids transported?
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)
What are the different oral contraceptive pills?
Oestrogen + progestogen (COCP) Progestogen only (POP)
What are the different types of COCP?
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)
Name some different oestrogens used in COCP
Ethinylestradiol
Mestranol
Name some different progestogens used in COCP
Different generations
1st: norethynodrel
2nd: levonorgestrel, norethisterone
3rd: desogestrel, gestodene, norgestimate
4th: drospirenone
What is the mode of action of COCP?
Suppression of ovulation: inhibit FSH, LH
Adverse effect o cervical mucous
Adverse effect on the endometrium
(Metabolised by cytochrome P450)
What are the adverse effects of COCP?
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
Name some progestogens in the POP
Levonorgestrel
Norethisterone
Etynodiol diacetate
Desogestrel
