19 Reproductive system Flashcards by Emma :)

19.01 OESTROGENS AND ANTI-OESTROGENS

Natural and synthetic oestrogens: raloxifene; anti-oestrogens: clomifene, tamoxifen - actions

oestrogen controls the proliferative phase of endometrium and exerts negative feedback on the anterior pituitary
in addition to the reproductive system, oestrogens have metabolic and vascular effects

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19.01 OESTROGENS AND ANTI-OESTROGENS

Natural and synthetic oestrogens, raloxifene; anti-oestrogens: clomifene, tamoxifen - MOA

bind to nuclear receptors and exert genomic effects
raloxifene has agonist effects at bone but antagonist on reproductive organs
clomifene is a competitive antagonist of oestrogen receptors at the anterior pituitary, and increases gonadotrophin secretion by preventing negative feedback

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19.01 OESTROGENS AND ANTI-OESTROGENS

Natural and synthetic oestrogens, raloxifene; anti-oestrogens: clomifene, tamoxifen - abs/distrib/elim

many different formulations available (oral, topical, implantable, transdermal)

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19.01 OESTROGENS AND ANTI-OESTROGENS

Natural and synthetic oestrogens, raloxifene; anti-oestrogens: clomifene, tamoxifen - clinical use

oestrogens are used in primary ovarian failure, menopausal symptoms and in female contraception
raloxifene is for osteoporosis
anti-oestrogens are used for inducing ovulation (clomifene) and for oestrogen-sensitive breast cancer (tamoxifen)

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19.01 OESTROGENS AND ANTI-OESTROGENS

Natural and synthetic oestrogens, raloxifene; anti-oestrogens: clomifene, tamoxifen - adverse effects

varies with formulation and clinical setting but may include breast tenderness, water retention, VTE
small increase in risk of breast and endometrial cancer in menopausal women
clomifene causes menopausal-like hot flushes, ovarian enlargement

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19.02 PROGESTOGENS AND ANTI-PROGESTOGENS

Progestogens: medroxyprogesterone, norethisterone, desogestrel, cyproterone; anti-progestogens: mifepristone - actions

progestogens control the secretory phase of endometrium and exert negative feedback on the anterior pituitary and hypothalamus
weak androgenic action

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19.02 PROGESTOGENS AND ANTI-PROGESTOGENS

Progestogens: medroxyprogesterone, norethisterone, desogestrel, cyproterone; anti-progestogens: mifepristone - MOA

bind to intracellular receptors and alter gene expression
cyproterone has weak progestational activity but is a partial agonist at androgen receptors in the hypothalamus

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19.02 PROGESTOGENS AND ANTI-PROGESTOGENS

Progestogens: medroxyprogesterone, norethisterone, desogestrel, cyproterone; anti-progestogens: mifepristone - abs/distrib/elim

many different formulations (oral, injectable, implantable device)
examples include levonorgestrel as a SC depot or as an intrauterine contraceptive system

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19.02 PROGESTOGENS AND ANTI-PROGESTOGENS

Progestogens: medroxyprogesterone, norethisterone, desogestrel, cyproterone; anti-progestogens: mifepristone - clinical use

female contraception, including post-coital emergency contraception
endometriosis
anti-progestogens (mifepristone) used in medical termination of pregnancy
cyproterone used to suppress hyperandrogenism

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19.02 PROGESTOGENS AND ANTI-PROGESTOGENS

Progestogens: medroxyprogesterone, norethisterone, desogestrel, cyproterone; anti-progestogens: mifepristone - adverse effects

acne, fluid retention, weight change, menstrual disturbance

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19.03 COMBINED ORAL CONTRACEPTIVE PILL

Oestrogen and a progestogen: ethinylestradiol + norethisterone; ethinylestradiol + desogestrel - actions and use

prevention of pregnancy

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19.03 COMBINED ORAL CONTRACEPTIVE PILL

Oestrogen and a progestogen: ethinylestradiol + norethisterone; ethinylestradiol + desogestrel - MOA

oestrogen suppresses the development of the ovarian follicle by inhibiting follicle-stimulating hormone (FSH) release from the anterior pituitary
progestogen prevents ovulation by inhibiting luteinizing hormone (LH) release
together, they make the endometrium unsuitable for implantation of the ovum

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19.03 COMBINED ORAL CONTRACEPTIVE PILL

Oestrogen and a progestogen: ethinylestradiol + norethisterone; ethinylestradiol + desogestrel - abs/distrib/elim

given orally
taken cyclically for 21 days out of 28 days

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19.03 COMBINED ORAL CONTRACEPTIVE PILL

Oestrogen and a progestogen: ethinylestradiol + norethisterone; ethinylestradiol + desogestrel - adverse effects

weight gain, flushing, mood changes, dizziness, acne or skin pigmentation, transient rise of blood pressure
some risk of thromboembolism

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19.04 GONADOTROPHINS

GnRH analogues (gonadorelin, leuprorelin) and inhibitors (danazol) - actions and MOA

pulsatile regimens of gonadotrophin-releasing hormone (GnRH) analogues stimulate gonadotrophin release but have inhibitory effects when given continuously
danazol is a modified progestogen that inhibits gonadal function by suppressing the mid-cycle surge of gonadotrophins

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19.04 GONADOTROPHINS

GnRH analogues (gonadorelin, leuprorelin) and inhibitors (danazol) - abs/distrib/elim

GnRH analogues are given by SC injection or nasal spray intermittently, or through a depot injection for continuous use
danazol is given orally

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19.04 GONADOTROPHINS

GnRH analogues (gonadorelin, leuprorelin) and inhibitors (danazol) - clinical use

GnRH analogues are used in infertility
longer term use for gonadal suppression in prostate cancer and endometriosis
danazol is used in the treatment of endometriosis and gynaecomastia

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19.04 GONADOTROPHINS

GnRH analogues (gonadorelin, leuprorelin) and inhibitors (danazol) - adverse effects

adverse effects of GnRH analogues vary depending on whether treatment is used for stimulation (hypergonadism) or inhibition (hypogonadism)
moderate effects are common with danazol: weight gain, acne, hot flushes, amenorrhoea, masculinisation (hirsutism, deepening of voice, etc.)

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19.05 UTERINE STIMULANTS

Oxytocin - actions

contracts the uterus causing coordinated contractions that travel from fundus to cervix with complete relaxation between contractions
has vasodilator action

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19.05 UTERINE STIMULANTS

Oxytocin - MOA

acts on oxytocin receptors in the smooth muscle of the myometrium
contracts myoepithelial cells in the breast to release milk
vasodilator and antidiuretic action

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19.05 UTERINE STIMULANTS

Oxytocin - abs/distrib/elim

usually given by IV infusion
can be given IM
inactivated by the liver and kidneys and by circulating oxytocinase

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19.05 UTERINE STIMULANTS

Oxytocin - clinical use

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induction or stimulation of labour when the uterine muscle is not functioning adequately
prevention and treatment of post-partum bleeding
treatment of incomplete abortion

19.05 UTERINE STIMULANTS

Oxytocin - adverse effects

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dose-related hypotension due to vasodilatation
water retention and hyponatraemia due to an antidiuretic hormone-like effect

19.06 UTERINE STIMULANTS

Ergometrine - actions

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contracts the relaxed uterus
has vasoconstrictor action

19.06 UTERINE STIMULANTS Ergometrine - MOA

not understood may act partly on α adrenoceptors, partly on 5-HT receptors

19.06 UTERINE STIMULANTS Ergometrine - abs/distrib/elim

given orally, IM or slow IV rapid onset of action duration: 3-6h a combined IM preparation of oxytocin and ergometrine is available

19.06 UTERINE STIMULANTS Ergometrine - clinical use

to treat post-partum haemorrhage

19.06 UTERINE STIMULANTS Ergometrine - adverse effects

nausea and vomiting due to action on dopamine receptors increase in BP and in some cases angina (due to vasoconstriction) headache, dizziness dysrhythmias

19.07 UTERINE STIMULANTS Analogues of prostaglandins E and F: carboprost, dinoprostone, misoprostol, gemeprost - actions

cause coordinated contractions of the pregnant uterus relax the cervix

19.07 UTERINE STIMULANTS Analogues of prostaglandins E and F: carboprost, dinoprostone, misoprostol, gemeprost - MOA

carboprost activates PGF2α (FP) receptors on uterine smooth muscle, whilst dinoprostone, misoprostol and gemeprost act on PGE receptors

19.07 UTERINE STIMULANTS Analogues of prostaglandins E and F: carboprost, dinoprostone, misoprostol, gemeprost - abs/distrib/elim

carboprost is given by deep IM injection, whereas dinoprostone and misoprostol are given intravaginally

19.07 UTERINE STIMULANTS Analogues of prostaglandins E and F: carboprost, dinoprostone, misoprostol, gemeprost - clinical use

carboprost for the treatment of post-partum haemorrhage unresponsive to oxytocin or ergometrine dinoprostone (PGE2) or misoprostol used intravaginally to augment or induce labour gemeprost (PGE1 analogue) used in pessary form for medical induction of abortion

19.07 UTERINE STIMULANTS Analogues of prostaglandins E and F: carboprost, dinoprostone, misoprostol, gemeprost - adverse effects

uterine pain, nausea, vomiting, diarrhoea, vasodilation

19.08 OXYTOCIN ANTAGONIST Atosiban - actions

inhibits oxytocin-induced contractions of the pregnant uterus

19.08 OXYTOCIN ANTAGONIST Atosiban - MOA

oxytocin receptor antagonist on uterine smooth muscle causing relaxation

19.08 OXYTOCIN ANTAGONIST Atosiban - abs/distrib/elim

given by IV injection followed by slow IV infusion

19.08 OXYTOCIN ANTAGONIST Atosiban - clinical use

to delay pre-term labour

19.08 OXYTOCIN ANTAGONIST Atosiban - adverse effects

nausea, vomiting, vasodilation, hyperglycaemia

19.09 MALE SEX HORMONE Testosterone - actions

has the same actions as endogenous testosterone the effects will depend on the age of the patient

19.09 MALE SEX HORMONE Testosterone - MOA

converted by 5α-reductase to dihydrotestosterone, which interacts with nuclear receptors to initiate transcription of some genes (resulting in DNA-directed RNA and protein synthesis) and repression of others dihydrotestosterone has greater activity than testosterone

19.09 MALE SEX HORMONE Testosterone - abs/distrib/elim

given orally, buccal, IM injection or transdermally oral formulations are rapidly metabolised in the liver

19.09 MALE SEX HORMONE Testosterone - clinical use

replacement therapy in hypogonadism due to pituitary or testicular disease

19.09 MALE SEX HORMONE Testosterone - adverse effects

eventual decrease of gonadotrophin release resulting in infertility oedema due to salt and water retention

19.10 ANTI-ANDROGENS 5α-reductase inhibitors (finasteride, dutasteride) and androgen antagonists (flutamide, bicalutamide, etc.) - actions

reduce the effect of testosterone, particularly at the prostate

19.10 ANTI-ANDROGENS 5α-reductase inhibitors (finasteride, dutasteride) and androgen antagonists (flutamide, bicalutamide, etc.) - MOA

finasteride and dutasteride block intracellular type II 5α-reductase (enzyme that converts testosterone to the more active variant, dihydrotestosterone) androgen antagonists block the action of testosterone on cell receptors

19.10 ANTI-ANDROGENS 5α-reductase inhibitors (finasteride, dutasteride) and androgen antagonists (flutamide, bicalutamide, etc.) - abs/distrib/elim

given orally

19.10 ANTI-ANDROGENS 5α-reductase inhibitors (finasteride, dutasteride) and androgen antagonists (flutamide, bicalutamide, etc.) - clinical use

finasteride is used in benign prostatic hyperplasia (often in conjunction with α-adrenoceptor blockers), and for male pattern hair loss androgen antagonists are used to treat prostate cancer

19.10 ANTI-ANDROGENS 5α-reductase inhibitors (finasteride, dutasteride) and androgen antagonists (flutamide, bicalutamide, etc.) - adverse effects

erectile dysfunction, libido loss gynaecomastia and breast tenderness are particularly common with androgen blockers

19.11 PHOSPHODIESTERASE TYPE V INHIBITORS Sildenafil, tadalafil, vardenafil - actions

enhance penile erection relax the non-vascular smooth muscle of the corpora cavernosa blood at virtually arterial pressure then flows into the cavenosa sinuses resulting in swelling and erection of the penis do not cause erection independent of sexual stimulation

19.11 PHOSPHODIESTERASE TYPE V INHIBITORS Sildenafil, tadalafil, vardenafil - MOA

inhibit phosphodiesterase type V (enzyme that normally converts cGMP to 5′-GMP) this increases the concentration of cGMP, which inhibits the contractile mechanisms of the muscle, allowing relaxation vascular relaxation also improves perfusion of the prostate and bladder

19.11 PHOSPHODIESTERASE TYPE V INHIBITORS Sildenafil, tadalafil, vardenafil - abs/distrib/elim

given orally peak action occurs in 30-120 min as tadalafil has a longer half-life, the exact timing of administration prior to anticipated sexual activity is less crucial

19.11 PHOSPHODIESTERASE TYPE V INHIBITORS Sildenafil, tadalafil, vardenafil - clinical use

usually for erectile dysfunction, but sildenafil is also licensed for pulmonary arterial hypertension tadalafil is also licensed for benign prostatic hyperplasia

19.11 PHOSPHODIESTERASE TYPE V INHIBITORS Sildenafil, tadalafil, vardenafil - adverse effects

fall in blood pressure, headache and flushing (due to the action of these drugs on other vascular beds)

19 Reproductive system Flashcards

(53 cards)