Contraception and HRT Flashcards
Give the actions of oestrogens
o Mild anabolico Sodium and water retentiono Raise HDL, Lower LDLo Decrease Bone Resorptiono Impair Glucose Toleranceo Increase Blood Coagulability
Give some side effects of oestrogen
o Breast tendernesso Nausea, vomitingo Water retentiono Increased Coagulabilityo Thromboembolismo Impaired glucose toleranceo Endometrial hyperplasia & cancer
Give the actions of progesterone
o Secretory endometriumo Anabolico Increase bone mineral densityo Fluid retentiono Mood changes
Give some side effects of progesterone
o Weight gaino Fluid retentiono Anabolico Acneo Nausea vomitingo Irritabilityo Depressiono Lack of concentration
Give the actions of testosterone
o Male secondary sex characteristicso Anabolico Voice changes
Give some side effects of testosterone
o Acneo Aggressiono Metabolic adverse effect on lipids
Describe the pharmacology of sex steroids
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
Describe the receptors that bind sex steroids
Nuclear receptors- found in cyotplasm- are complexed with heat shock proteins
What happens when a ligand is bound to the sex steroid receptors?
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.
What action does progesterone have for hormonal contraception?
Gives rise to:- thick, hostile cervical mucus- negatively feeds back to decrease GnRH
What actions does oestrogen have as a hormonal contraception?
- Negatively feeds back on the anterior pituitary- Loss of positive feedback, therefore prevents an LH surge
Describe the the contents of the combined oral contraceptive pill
Contains oestrogen (ethinylestradiol) and progesterone (progesterone analogue). They mimic the luteal phase to suppress GnRH.
What parts of the menstrual cycle do not take place when the combined oral contraceptive pill is being taken?
There is no:- follicular secretion- follicular maturation- LH surge- ovulation
What are some contraindications for the COCP?
PregnancyBreast feedingHistory/risk factors for heart diseaseHypertension*HyperlipidaemiaAny prothrombic coagulation abnormalityDiabetes mellitusMigraineBreast/genital tract carcinomaAmenorrhoeaLiver disease
Give some adverse effects that can occur with the COCP
Venous thromboembolism HypertensionDecreased glucose toleranceHeadachesMood swingsAcneFlushingNauseaVomintingAmenorrhoea on pill cessation
Describe the Progesterone only pill
Consists of a low does progesterone analogueIs less reliable as a contraception compared to the COCP
What effect does the POP have on the menstrual cycle?
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
When would you use the POP?
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
What are some contraindications for the POP?
PregnancyArterial diseaseLiver diseaseBreast and genital tract carcinoma
What are the adverse effects of the POP?
Menstrual irregularities*NauseaVomitingHeadacheWeight gainBreast tenderness
Give some drug interactions that occur with the COCP
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.
What can the COCP be used for?
Manages abnormal/ heavy menstrual bleedingContraception
Define Hormone replacement therapy
Oestrogen and progesterone are given to replace lost hormones and to control menopausal symptoms.
Give some risks of HRT
Unopposed oestrogen - endometrial and ovarian cancersUterine bleedingIncreased risk of:- breast cancer- stroke and IHD- thromboembolism
Give some adverse effects of HRT
• Adverse effect on lipid profile• Adverse effect on thrombophilia profile
Describe anti-oestrogen
Weak oestrogens which are antagonist for oestrogen receptors
Give some examples of anti-oestrogens
Clomiphene - induces ovulation by inhibiting negative feedback, increasing GnRH as well as FSH and LHTamoxifen - treats breast cancer and induces ovulation
Describe anti-progesterones
MifepristonePartial agonist to progesterone receptor, inhibiting actionSensitises the uterus to prostaglandinsUsed for medical termination of pregnancy and inducing labour
Describe anti-androgens
CyproteroneIs a progesterone derivative with a weak progestogenic effect. Is a partial agonist to progesterone and competes with dihydrotestosteroneIs used in the COCP (dianette)
Describe SERM
Selective oestrogen receptor modulators- Raloxifen
Give the actions of SERMs
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
