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Pharmacology > 19 Reproductive system > Flashcards

19 Reproductive system Flashcards

1
Q

19.01 OESTROGENS AND ANTI-OESTROGENS

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

A

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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2
Q

19.01 OESTROGENS AND ANTI-OESTROGENS

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

A

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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3
Q

19.01 OESTROGENS AND ANTI-OESTROGENS

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

A

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

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4
Q

19.01 OESTROGENS AND ANTI-OESTROGENS

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

A

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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5
Q

19.01 OESTROGENS AND ANTI-OESTROGENS

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

A

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

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6
Q

19.02 PROGESTOGENS AND ANTI-PROGESTOGENS

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

A

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

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7
Q

19.02 PROGESTOGENS AND ANTI-PROGESTOGENS

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

A

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

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8
Q

19.02 PROGESTOGENS AND ANTI-PROGESTOGENS

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

A

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

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9
Q

19.02 PROGESTOGENS AND ANTI-PROGESTOGENS

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

A

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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10
Q

19.02 PROGESTOGENS AND ANTI-PROGESTOGENS

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

A

acne, fluid retention, weight change, menstrual disturbance

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11
Q

19.03 COMBINED ORAL CONTRACEPTIVE PILL

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

A

prevention of pregnancy

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12
Q

19.03 COMBINED ORAL CONTRACEPTIVE PILL

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

A

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

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13
Q

19.03 COMBINED ORAL CONTRACEPTIVE PILL

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

A

given orally
taken cyclically for 21 days out of 28 days

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14
Q

19.03 COMBINED ORAL CONTRACEPTIVE PILL

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

A

infrequent, but may cause weight gain, flushing, mood changes, dizziness and sometimes acne or skin pigmentation and a transient rise of blood pressure
some risk of thromboembolism

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15
Q

19.04 GONADOTROPHINS

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

A

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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16
Q

19.04 GONADOTROPHINS

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

A

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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17
Q

19.04 GONADOTROPHINS

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

A

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

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18
Q

19.04 GONADOTROPHINS

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

A

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
Q

19.05 UTERINE STIMULANTS

Oxytocin - actions

A

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

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20
Q

19.05 UTERINE STIMULANTS

Oxytocin - MOA

A

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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21
Q

19.05 UTERINE STIMULANTS

Oxytocin - abs/distrib/elim

A

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

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22
Q

19.05 UTERINE STIMULANTS

Oxytocin - clinical use

A

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

23
Q

19.05 UTERINE STIMULANTS

Oxytocin - adverse effects

A

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

24
Q

19.06 UTERINE STIMULANTS

Ergometrine - actions

A

contracts the relaxed uterus
has vasoconstrictor action

25
Q

19.06 UTERINE STIMULANTS

Ergometrine - MOA

A

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

26
Q

19.06 UTERINE STIMULANTS

Ergometrine - abs/distrib/elim

A

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

27
Q

19.06 UTERINE STIMULANTS

Ergometrine - clinical use

A

to treat post-partum haemorrhage

28
Q

19.06 UTERINE STIMULANTS

Ergometrine - adverse effects

A

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

29
Q

19.07 UTERINE STIMULANTS

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

A

cause coordinated contractions of the pregnant uterus
relax the cervix

30
Q

19.07 UTERINE STIMULANTS

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

A

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

31
Q

19.07 UTERINE STIMULANTS

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

A

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

32
Q

19.07 UTERINE STIMULANTS

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

A

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

33
Q

19.07 UTERINE STIMULANTS

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

A

uterine pain, nausea, vomiting, diarrhoea, vasodilation

34
Q

19.08 OXYTOCIN ANTAGONIST

Atosiban - actions

A

inhibits oxytocin-induced contractions of the pregnant uterus

35
Q

19.08 OXYTOCIN ANTAGONIST

Atosiban - MOA

A

antagonises oxytocin action on oxytocin receptors on uterine smooth muscle causing relaxation

36
Q

19.08 OXYTOCIN ANTAGONIST

Atosiban - abs/distrib/elim

A

given by IV injection followed by slow IV infusion

37
Q

19.08 OXYTOCIN ANTAGONIST

Atosiban - clinical use

A

to delay pre-term labour

38
Q

19.08 OXYTOCIN ANTAGONIST

Atosiban - adverse effects

A

vasodilation, nausea, vomiting, hyperglycaemia

39
Q

19.09 MALE SEX HORMONE

Testosterone - actions

A

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

40
Q

19.09 MALE SEX HORMONE

Testosterone - MOA

A

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

41
Q

19.09 MALE SEX HORMONE

Testosterone - abs/distrib/elim

A

administration can be oral, buccal, by IM injection or transdermally
oral formulations are rapidly metabolised in liver

42
Q

19.09 MALE SEX HORMONE

Testosterone - clinical use

A

replacement therapy in hypogonadism due to pituitary or testicular disease

43
Q

19.09 MALE SEX HORMONE

Testosterone - adverse effects

A

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

44
Q

19.10 ANTI-ANDROGENS

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

A

reduce the effect of testosterone, particularly at the prostate

45
Q

19.10 ANTI-ANDROGENS

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

A

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

46
Q

19.10 ANTI-ANDROGENS

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

A

given orally

47
Q

19.10 ANTI-ANDROGENS

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

A

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

48
Q

19.10 ANTI-ANDROGENS

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

A

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

49
Q

19.11 PHOSPHODIESTERASE TYPE V INHIBITORS

Sildenafil, tadalafil, vardenafil - actions

A

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

50
Q

19.11 PHOSPHODIESTERASE TYPE V INHIBITORS

Sildenafil, tadalafil, vardenafil - MOA

A

inhibit phosphodiesterase type V - an 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

51
Q

19.11 PHOSPHODIESTERASE TYPE V INHIBITORS

Sildenafil, tadalafil, vardenafil - abs/distrib/elim

A

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

52
Q

19.11 PHOSPHODIESTERASE TYPE V INHIBITORS

Sildenafil, tadalafil, vardenafil - clinical use

A

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

53
Q

19.11 PHOSPHODIESTERASE TYPE V INHIBITORS

Sildenafil, tadalafil, vardenafil - adverse effects

A

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

Pharmacology (34 decks)

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