Contraception and HRT

Question 1

Give the actions of oestrogens

Answer 1

o Mild anabolico Sodium and water retentiono Raise HDL, Lower LDLo Decrease Bone Resorptiono Impair Glucose Toleranceo Increase Blood Coagulability

Question 2

Give some side effects of oestrogen

Answer 2

o Breast tendernesso Nausea, vomitingo Water retentiono Increased Coagulabilityo Thromboembolismo Impaired glucose toleranceo Endometrial hyperplasia & cancer

Question 3

Give the actions of progesterone

Answer 3

o Secretory endometriumo Anabolico Increase bone mineral densityo Fluid retentiono Mood changes

Question 4

Give some side effects of progesterone

Answer 4

o Weight gaino Fluid retentiono Anabolico Acneo Nausea vomitingo Irritabilityo Depressiono Lack of concentration

Question 5

Give the actions of testosterone

Answer 5

o Male secondary sex characteristicso Anabolico Voice changes

Question 6

Give some side effects of testosterone

Answer 6

o Acneo Aggressiono Metabolic adverse effect on lipids

Question 7

Describe the pharmacology of sex steroids

Answer 7

Are transported bound to sex hormone binding globulin and albumin (for progesterone)Metabolism occurs via the liverMetabolites are excreted in the urine as glucaronides and sulphates

Question 8

Describe the receptors that bind sex steroids

Answer 8

Nuclear receptors- found in cyotplasm- are complexed with heat shock proteins

Question 9

What happens when a ligand is bound to the sex steroid receptors?

Answer 9

They will form a homodimer with another ligand-receptor complex and translocate to the nucleus. Once in the nucleus, the complex can transactivate or transrepress genes by binding to positive or negative hormone reponse elements.

Question 10

What action does progesterone have for hormonal contraception?

Answer 10

Gives rise to:- thick, hostile cervical mucus- negatively feeds back to decrease GnRH

Question 11

What actions does oestrogen have as a hormonal contraception?

Answer 11

• Negatively feeds back on the anterior pituitary- Loss of positive feedback, therefore prevents an LH surge

Question 12

Describe the the contents of the combined oral contraceptive pill

Answer 12

Contains oestrogen (ethinylestradiol) and progesterone (progesterone analogue). They mimic the luteal phase to suppress GnRH.

Question 13

What parts of the menstrual cycle do not take place when the combined oral contraceptive pill is being taken?

Answer 13

There is no:- follicular secretion- follicular maturation- LH surge- ovulation

Question 14

What are some contraindications for the COCP?

Answer 14

PregnancyBreast feedingHistory/risk factors for heart diseaseHypertension*HyperlipidaemiaAny prothrombic coagulation abnormalityDiabetes mellitusMigraineBreast/genital tract carcinomaAmenorrhoeaLiver disease

Question 15

Give some adverse effects that can occur with the COCP

Answer 15

Venous thromboembolism HypertensionDecreased glucose toleranceHeadachesMood swingsAcneFlushingNauseaVomintingAmenorrhoea on pill cessation

Question 16

Describe the Progesterone only pill

Answer 16

Consists of a low does progesterone analogueIs less reliable as a contraception compared to the COCP

Question 17

What effect does the POP have on the menstrual cycle?

Answer 17

Thickening of cervical mucus to prevent sperm penetrationAffects the endometrium, to limit implantingSuppresses GnRH secretion and sometime suppresses ovulationUsually have normal ovulation and normal menstruation

Question 18

When would you use the POP?

Answer 18

Is a more suitable form of contraception than the COCP for heavy smokers, patients with hypertension, heart disease, diabetes mellitus and other contraindications for the COCP

Question 19

What are some contraindications for the POP?

Answer 19

PregnancyArterial diseaseLiver diseaseBreast and genital tract carcinoma

Question 20

What are the adverse effects of the POP?

Answer 20

Menstrual irregularities*NauseaVomitingHeadacheWeight gainBreast tenderness

Question 21

Give some drug interactions that occur with the COCP

Answer 21

Metabolised by CYP450, so affected by inducers/inhibitors. Inducers lower levels of COCP such as carbamezepine and phenytoinBroad spectrum antibiotics e.g. amoxicillinAntibiotics kill the gut flora, which is involved in enterohepatic recirculation of oestrogen, so potentially can cause contraception failure.

Question 22

What can the COCP be used for?

Answer 22

Manages abnormal/ heavy menstrual bleedingContraception

Question 23

Define Hormone replacement therapy

Answer 23

Oestrogen and progesterone are given to replace lost hormones and to control menopausal symptoms.

Question 24

Give some risks of HRT

Answer 24

Unopposed oestrogen - endometrial and ovarian cancersUterine bleedingIncreased risk of:- breast cancer- stroke and IHD- thromboembolism

Question 25

Give some adverse effects of HRT

Answer 25

• Adverse effect on lipid profile• Adverse effect on thrombophilia profile

Question 26

Describe anti-oestrogen

Answer 26

Weak oestrogens which are antagonist for oestrogen receptors

Question 27

Give some examples of anti-oestrogens

Answer 27

Clomiphene - induces ovulation by inhibiting negative feedback, increasing GnRH as well as FSH and LHTamoxifen - treats breast cancer and induces ovulation

Question 28

Describe anti-progesterones

Answer 28

MifepristonePartial agonist to progesterone receptor, inhibiting actionSensitises the uterus to prostaglandinsUsed for medical termination of pregnancy and inducing labour

Question 29

Describe anti-androgens

Answer 29

CyproteroneIs a progesterone derivative with a weak progestogenic effect. Is a partial agonist to progesterone and competes with dihydrotestosteroneIs used in the COCP (dianette)

Question 30

Describe SERM

Answer 30

Selective oestrogen receptor modulators- Raloxifen

Question 31

Give the actions of SERMs

Answer 31

Protects against osteoporosisHas no proliferative effect on endometrium and breastHas oestrogenic effects on bone, lipid metabolism and blood coagulationReduced risk of invasive breast cancer in post menopausal women with osteoporosisIncreases hot flushes