Session 3 - Pharmacology of Sex and Steroids Flashcards Preview

Semester 5 - Farmocology > Session 3 - Pharmacology of Sex and Steroids > Flashcards

Flashcards in Session 3 - Pharmacology of Sex and Steroids Deck (41)

Give 6 actions of oestrogens

o Mild anabolic
o Sodium and water retention
o Raise HDL, Lower LDL
o Decrease Bone Resorption
o Impair Glucose Tolerance
o Increase Blood Coagulability


Give 7 side-effects Oestrogens

o Breast tenderness
o Nausea, vomiting
o Water retention
o Increased Coagulability
o Thromboembolism
o Impaired glucose tolerance
o Endometrial hyperplasia & cancer


Give 5 actions of progesterone

o Secretory endometrium
o Anabolic
o Increase bone mineral density
o Fluid retention
o Mood changes


Give 8 side effects of progesterones

o Weight gain
o Fluid retention
o Anabolic
o Acne
o Nausea vomiting
o Irritability
o Depression
o Lack of concentration


Give three actions of testosterone

o Male secondary sex characteristics
o Anabolic
o Voice changes


Give 3 side effects of testosterone

o Acne
o Aggression
o Metabolic adverse effect on lipids


How are sex hormones transported?

o Transported bound to Sex Hormone Binding Globulin (SHBG) (except progesterone) and albumin (mainly progesterone).


How are sex steroids metabolised?

o Metabolism is via the Liver, Progesterone is almost totally metabolised in one passage through the liver
o Metabolites excreted in the Urine (as glucuronides and sulphates)


Outline the mechanism of action of sex steroids

Like all steroid hormones, sex steroids exert their effect via Nuclear Receptors. These receptors are found in the cytoplasm, complexed with heat shock proteins. Following the diffusion (or possibly transport) of their ligand into the cell and high-affinity binding, these receptors form a Homodimer with another ligand-receptor complex and translocate to the nucleus.

In the nucleus, the steroid-receptor complex homodimers can Transactivate or Transrepress genes by binding to Positive or Negative Hormone Response Elements. Large numbers of genes can be regulated in this way by a single ligand.

Steroids may also bind to receptors that are already present inside the nucleus, which will then bind to the HRE.


What are the two hormones used in hormonal contraception?



How does progesterone prevent conception?

o Thick, ‘hostile’ cervical mucus plug
 Prevents sperm from entering uterus
 Main contraceptive action of progesterone
o Negative feedback to hypothalamus / pituitary
 Decreases frequency of GnRH pulses
 Inhibits follicular development


How does oestrogen prevent conception?

o Oestrogen negatively feeds back on anterior pituitary
o Loss of positive feedback mid-cycle
 No LH surge


What does a COCP contain?

Oestrogen and progestogen (a progesterone analogue)


How does the CoCP work?

Mimics the luteal phase of hte menstriual cycle and suppresses the release of Gonadotrophins via negative feedback.
Follicular selection and maturation, LH sruge and ovulation does not take place.



What is the route of administration for the COCP?

 Oral
 One a day for 21 days, then break, placebo or iron pill for 7 days


Why is the COCP prescribed?

Menstrual symptoms


What are some contraindications for COCP?

 Pregnancy, breast feeding, history or risk factors of heart disease, hypertension, hyperlipidaemia or any prothrombotic coagulation abnormality, diabetes mellitus, migraine, breast or genital tract carcinoma, liver disease


Give some adverse effects of the COCP?

 VENOUS THROMBOEMBOLISM, HYPERTENSION, decreased glucose tolerance, headaches, mood swings, acne, flushing, nausea, vomiting, headache, amenorrhoea of variable duration on pill cessation


What is the effect of the progesterone only pill?

This causes thickening of cervical mucus, preventing sperm penetration. It also has an adverse effect on the endometrium, affecting implantation. Contraception is less reliable than the COCP. It also causes suppression of gonadotrophin secretion, and occasionally ovulation, but the latter effect does not occur in the majority of women


What is the route of administration of the POP?

 Oral
 Daily, at the same time, starting at day 1 of menstrual cycle. If delay in taking the pill is greater than 3 hours, contraceptive effect may be lost


What are the indications of the POP?

 Contraception – More suitable for heavy smokers and patients with hypertension or heart disease, diabetes mellitus, or other contraindications for oestrogen therapy (see above COCP)


What are the contradindications of the POP?

 Pregnancy, arterial disease, liver disease or breast or genital tract carcinoma


What are the adverse effects of the POP?

 Menstrual irregularities, nausea, vomiting and headache, weight fain, breast tenderness


What are the main side effects of the COCP?

o Venous Thromboembolism (rare)
o Hypertension
o Amenorrhoea of variable duration on pill cessation
o Flushing, headaches, nausea, acne, mood swings, weight gain (common)


What are the main drug interactions of the COCP? (2)

o Metabolism is by CYP450
 Therefore effected by inducers/inhibitors
 Enzyme inducers can lower levels of COCP causing contraception failure
o Broad spectrum antibiotics (e.g. Amoxicillin)
 Enterohepatic recirculation of oestrogen increases the efficacy of the COCP. If gut flora is killed by a broad spectrum antibiotic this is reduced and may cause contraception failure


What are some adverse effects of POP?

o Menstrual irregularities
o Nausea, vomiting and headache
o Weight gain
o Breast tenderness


What are some drug interactions of POP?

o Metabolism is by CYP450
 Therefore effected by inducers/inhibitors
 Enzyme inducers can lower levels of POP causing contraception failure


What is the most common route of sex steroid admin?



What are the advantage of transdermal sex steroid? (3)

o May reduce risk in turns of DVT, Thromboembolism by bypassing the Liver and giving smaller doses
o Important for people who complain of GI side Effects
o Slow, gradual release of steroid (Progestin)


What is the advantage of impants?

Slow, gradual release of steroid (Progestin)


Give five methods of sex steroid admin?



Give a long term method of contraception?

Depot progesterone
Intramuscular implant of progesterone giving long term contraception - same mechanism as POP


What is the morning after pill?

o ‘Morning after pill’ – Up to 72hrs after sex
 Very high oral doses of progesterone (1.5mg) alone, or a Progestogen with an oestrogen to prevent implantation of fertilised egg


What level of effectiveness is morning after pill?

 75% effective


What is indication for morning after pill?

– Emergency Contraception after unprotected sex


Contraindication for Morning after pill?

Oestrogen contraindications (see above), need to ask about cycle and when they had sex to determine if the woman is already pregnant.


What contraception can be used up to 120 hours after sex?

 Progesterone receptor modulator
 Copper IUD


How can you manage uterine bleeding?

The COCP can be used to manage abnormal uterine bleeding. Basically ‘tricks’ the body into thinking it is in the post ovulatory, luteal phase so offers a good method of cycle control.


What can be used to cure menopausal symptoms?

Hormone Replacement Therapy (HRT)


What are five risks of HRT?

 Unopposed oestrogen – Inc. endometrial and ovarian cancers
 Increase breast cancer risk
 Increased IHD and stroke risk
 Increased risk of thromboembolism
 Uterine bleeding


Give two adverse effects of HRT?

 Adverse effect on lipid profile
 Adverse effect on thrombophilia profile