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December 26, 2017Male sex hormones Antagonists
January 2, 2018Oestrogens and HRT
Oestrogens are necessary for the development of female secondary sexual characteristics; they also stimulate myometrial hypertrophy with endometrial hyperplasia. In terms of oestrogenic activity natural oestrogens (estradiol (oestradiol), estrone (oestrone), and estriol (oestriol)) have a more appropriate profile for hormone replacement therapy (HRT) than synthetic oestrogens (ethinylestradiol (ethinyloestradiol) and mestranol). Tibolone has oestrogenic, progestogenic and weak androgenic activity.
ESTRADIOL-DYDROGESTERONS:
Indications: Menopausal symptoms and osteoporosis prophylaxis.
Contraindications: pregnancy; oestrogen-dependent cancer, history of breast cancer, active thrombophlebitis, active or recent arterial thromboembolic disease (e.g. angina or myocardial infarction), venous thromboembolism, or history of recurrent venous thromboembolism (unless already on anticoagulant treatment), liver disease (where liver function tests have failed to return to normal), Dubin-Johnson and Rotor syndromes (or monitor closely), untreated endometrial hyperplasia, undiagnosed vaginal bleeding, breast-feeding.
Dose and Administration: Menopausal symptoms and osteoporosis prophylaxis, in women with a uterus, 1 red tablet daily for 14 days, starting within 5 days of onset of menstruation (or any time if cycles have ceased or are infrequent) then 1 yellow tablet daily for 14 days; subsequent courses repeated without interval; where therapy required for menopausal symptoms alone.
ESTRADIOL VALERATE-NORGETREL:
Indications: Menopausal symptoms and osteoporosis prophylaxis.
Contraindications: pregnancy; oestrogen-dependent cancer, history of breast cancer, active thrombophlebitis, active or recent arterial thromboembolic disease (e.g. angina or myocardial infarction), venous thromboembolism, or history of recurrent venous thromboembolism (unless already on anticoagulant treatment), liver disease (where liver function tests have failed to return to normal), Dubin-Johnson and Rotor syndromes (or monitor closely), untreated endometrial hyperplasia, undiagnosed vaginal bleeding, breast-feeding.
Dose and Administration: Menopausal symptoms and osteoporosis prophylaxis, in women with a uterus, 1 white tablet daily for 11 days, starting on day 5 of menstruation (or at any time if cycles have ceased or are infrequent), then 1 brown tablet daily for 10 days, followed by a 7-day tablet-free interval
CONJUGATED OESTROGENS:
Indications: Menopausal symptoms and osteoporosis prophylaxis.
Contraindications: pregnancy; oestrogen-dependent cancer, history of breast cancer, active thrombophlebitis, active or recent arterial thromboembolic disease (e.g. angina or myocardial infarction), venous thromboembolism, or history of recurrent venous thromboembolism (unless already on anticoagulant treatment), liver disease (where liver function tests have failed to return to normal), Dubin-Johnson and Rotor syndromes (or monitor closely), untreated endometrial hyperplasia, undiagnosed vaginal bleeding, breast-feeding
Dose and Administration: Menopausal symptoms, 0.3–1.25 mg daily continuously; osteoporosis prophylaxis, 0.625–1.25 mg daily continuously; with cyclical progestogen for 12–14 days of each cycle in women with a uterus
ESTRADIOL:
Indications: Menopausal symptoms and osteoporosis prophylaxis.
Contraindications: pregnancy; oestrogen-dependent cancer, history of breast cancer, active thrombophlebitis, active or recent arterial thromboembolic disease (e.g. angina or myocardial infarction), venous thromboembolism, or history of recurrent venous thromboembolism (unless already on anticoagulant treatment), liver disease (where liver function tests have failed to return to normal), Dubin-Johnson and Rotor syndromes (or monitor closely), untreated endometrial hyperplasia, undiagnosed vaginal bleeding, breast-feeding
Dose and Administration: Menopausal symptoms (and osteoporosis prophylaxis, 1 patch to be applied twice weekly continuously, with cyclical progestogen for 12 days of each cycle in women with a uterus; therapy should be initiated with TTS 50 for first month, subsequently adjusted to lowest effective dose. Oral 1–2 mg daily continuously; osteoporosis prophylaxis, 2 mg daily continuously; with cyclical progestogen for 12 days of each cycle in women with a uterus.
TIBOLONE:
Indications: short-term treatment of symptoms of oestrogen deficiency (including women being treated with gonadotrophin releasing hormone analogues); osteoporosis prophylaxis in women at risk of fractures (second-line). Contraindications: hormone-dependent tumours, history of cardiovascular or cerebrovascular disease (e.g. thrombophlebitis, thromboembolism), uninvestigated vaginal bleeding, severe liver disease, pregnancy, breast-feeding. Dose and Administration: 2.5 mg daily. Unsuitable for use in the premenopause (unless being treated with gonadotrophin-releasing hormone analogue) and as (or with) an oral contraceptive; also unsuitable for use within 12 months of last menstrual period (may cause irregular bleeding); induce withdrawal bleed with progestogen if transferring from another form of HRT.
RALOXIFENE HYDROCHLORIDE:
Indications: treatment and prevention of postmenopausal osteoporosis.
Contraindications: history of venous thromboembolism, undiagnosed uterine bleeding, endometrial cancer, hepatic impairment, cholestasis, severe renal impairment; pregnancy and breast-feeding.
Dose and Administration: 60 mg once daily.
Progestogens
DYDROGESTERONE:
Indications: Endometriosis, Infertility, irregular cycles, Recurrent miscarriage, Dysfunctional uterine bleeding, Dysmenorrhoea, Amenorrhoea, Premenstrual syndrome, Hormone replacement therapy, with continuous oestrogen therapy.
Contraindications: Progestogens should be avoided in patients with a history of liver tumours, and in severe liver impairment. They are also contra-indicated in those with genital or breast cancer (unless progestogens are being used in the management of these conditions), severe arterial disease, undiagnosed vaginal bleeding and porphyria. Progestogens should not be used if there is a history during pregnancy of idiopathic jaundice, severe pruritus, or pemphigoid gestationis.
Dose and Administration: Endometriosis, 10 mg 2–3 times daily from day 5 to 25 of cycle or continuously. Infertility, irregular cycles, 10 mg twice daily from day 11 to 25 for at least 6 cycles. Recurrent miscarriage, 10 mg twice daily from day 11 to 25 of cycle until conception, then continuously until week 20 of pregnancy and then gradually reduced. Dysfunctional uterine bleeding, 10 mg twice daily (together with an oestrogen) for 5–7 days to arrest bleeding; 10 mg twice daily (together with an oestrogen) from day 11 to 25 of cycle to prevent bleeding. Dysmenorrhoea, 10 mg twice daily from day 5 to 25 of cycle. Amenorrhoea, 10 mg twice daily from day 11 to 25 of cycle with oestrogen therapy from day 1 to 25 of cycle. Premenstrual syndrome, 10 mg twice daily from day 12 to 26 of cycle increased if necessary.
MEDROXYPROGESTERONE ACETATE:
Indications: Abnormal Uterine Bleeding due to Hormonal Imbalance, Endometrial Hyperplasia Prevention, Secondary Amenorrhea, Endogenous Estrogen Production Test, Polycystic Ovarian Syndrome, Post-Menopausal Symptoms.
Contraindications: Breast Carcinoma, Cerebrovascular Hemorrhage, Metrorrhagia, Pregnancy, Severe Hepatic Disease, Thromboembolic Disorder, and Thrombophlebitis.
Dose and Administration: By mouth, 2.5–10 mg daily for 5–10 days beginning on day 16 to 21 of cycle, repeated for 2 cycles in dysfunctional uterine bleeding and 3 cycles in secondary amenorrhoea. Mild to moderate endometriosis, 10 mg 3 times daily for 90 consecutive days, beginning on day 1 of cycle. Progestogenic opposition of oestrogen HRT, 10 mg daily for the last 14 days of each 28-day oestrogen HRT cycle.
HYDROXYPROGETRONE CAPROATE:
Indications: Habitual abortion, Threatened abortion, Infertility due to corpus luteum insufficiency and Primary & secondary amenorrhea.
Contraindications: History of herpes of pregnancy, previous or existing liver tumours.
Dose and Administration: Habitual abortion 250-500 mg IM wkly during the initial mths of pregnancy. Threatened abortion 500 mg 2-3 times wkly until bleeding ceases. Continue treatment w/ 250 mg IM twice wkly until bleeding stops despite mobilisation. Infertility due to corpus luteum insufficiency 250 mg IM about 3 days after the rise in basal body temp. Primary & secondary amenorrhea 1st day.
NORETHISTERONE:
Indications: Endometriosis, Dysfunctional uterine bleeding, menorrhagia, Dysmenorrhoea, Premenstrual syndrome and Postponement of menstruation.
Contraindications: Progestogens should be avoided in patients with a history of liver tumours, and in severe liver impairment. They are also contra-indicated in those with genital or breast cancer, undiagnosed vaginal bleeding and porphyria, Progestogens should not be used if there is a history during pregnancy of idiopathic jaundice, severe pruritus, or pemphigoid gestationis.
Dose and Administration: Endometriosis, by mouth, 10–15 mg daily for 4–6 months or longer, starts on day 5 of cycle. Dysfunctional uterine bleeding, menorrhagia, by mouth, 5 mg 3 times daily for 10 days to arrest bleeding; to prevent bleeding 5 mg twice daily from day 19 to 26. Dysmenorrhoea, by mouth, 5 mg 3 times daily from day 5 to 24 for 3–4 cycles. Premenstrual syndrome, by mouth, 5 mg 2–3 times daily from day 19 to 26 for several cycles. Postponement of menstruation, by mouth, 5 mg 3 times daily starting 3 days before expected onset.
PROGESTERONE:
Indications: infertility due to inadequate luteal phase, premenstrual syndrome and post-natal depression, dysfunctional uterine bleeding, recurrent miscarriage due to inadequate luteal phase.
Contraindications: Breast Carcinoma, Cerebrovascular Hemorrhage, Metrorrhagia, Pregnancy, Severe Hepatic Disease, Thromboembolic Disorder, and Thrombophlebitis.
Dose and Administration: By vagina (Crinone), infertility due to inadequate luteal phase, insert 1 applicatorful daily starting either after documented ovulation or on day 18–21 of cycle. In vitro fertilisation, daily application continued for 30 days after laboratory evidence of pregnancy.
By vagina or rectum (cyclogest), premenstrual syndrome and post-natal depression, 200 mg daily to 400 mg twice daily; for premenstrual syndrome start on day 12–14 and continue until onset of menstruation, rectally if barrier methods of contraception are used, in patients who have recently given birth or in those who suffer from vaginal infection or recurrent cystitis.
By deep intramuscular injection(Gestone) into buttock, dysfunctional uterine bleeding, 5–10 mg daily for 5–10 days until 2 days before expected onset of menstruation. Recurrent miscarriage due to inadequate luteal phase or following in vitro fertilisation or gamete intra-fallopian transfer, 25–100 mg 2–7 times a week from day 15, or day of embryo or gamete transfer, until 8–16 weeks of pregnancy; max. 200 mg daily.
