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Reproductive System Pharmacology > Reproductive System > Flashcards

Reproductive System Flashcards

1
Q

Estrogen receptor agonist

A

Ethinylestradiol

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2
Q

Estrogen receptor agonist and antagonist (SERM)

A

Tamoxifen,Raloxifene, clomiphene

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3
Q

Estrogen receptor antagonist

A

Fulvestrant

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4
Q

Aromatase inhibitors

A

Anastrozole

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5
Q

Synthetic progesterone analogue (progestins)

A

Medroxyprogesterone,Levonorgestrel,Dydrogesterone

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6
Q

Antiprogestins

A

Mifepristone

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7
Q

Estrogen effects

A

Endometrial and mammary gland proliferation (increase tumor risk),inhibits osteoclast activity, increase blood coagulation,promote water and electrolyte retention, decrease glucose tolerance,affect blood lipid level, increase bile lithogenicity

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8
Q

Progestins effects

A

Inhibit endometrial proliferaiphase and stimulate mammary gland proliferation (increase tumor risk),promote use of adipose tissue for energy metabolism, increase blood coagulation some prevent water retention,impair glucose tolerance,affect blood lipid level,do not affect bile lithogenicity

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9
Q

Both estrogen and progesterone are bad for

A

DM, hypercholesterolemia, obesity patients due decrease glucose tolerance,increase lipid content in blood

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10
Q

Both progesterone and estrogen provide feedback inhibion on

A

Release of FSH/LH secretion in adenohypophysis.also have effect on hypothalamic release of GnRH

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11
Q

Combination oral contraceptive (both estrogen and progesterone) fn

A

Change cervix environment,altered transportation of egg,sperm and fertilizer ovum, unfavorable endometrial environment

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12
Q

Estrogen and progesterone receptors are seen in

A

All organs mainly ovary,uterus,vagina,bones,breast, hypothalamus, pituitary gland, blood vessels

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13
Q

Estrogen receptors are

A

ER alpha and beta

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14
Q

Progesterone receptors are

A

PR-a and B

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15
Q

Both estrogen and progesterone receptors are

A

Nuclear receptors

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16
Q

Estrogen and progesterone cause

A

Estrogen and progesterone regulated gene transcription

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17
Q

Testesterone,5alpha dihydrotestosterone (DHT) receptor

A

Intranuclear Androgen receptor (ARs)

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18
Q

Symptoms of menopause

A

Hot flushes,nausea, headache, tachycardia,sweating , palpitations,night sweats

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19
Q

Increase in Gn RH and gonadotropin during menopause is due to

A

Decrease in feedback inhibition by estrogen

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20
Q

Symptoms of menopause are caused due to

A

Activation of thermoregulatory centers of hypothalamus by gonadotropin which is uncontrolled

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21
Q

Hormone replacement therapy can be done to

A

Reduce symptoms of menopause

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22
Q

Women with hysterectomy may use

A

Estrogen therapy

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23
Q

Women with preserved uterus can use

A

Combined estrogen and progesterone HRT

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24
Q

Combined therapy for uterus preserved women helps to reduce

A

Risk of endometrial Cancer

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25
Q

Hypogonadism treatment

A

HRT

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26
Q

Primary hypogonadism cause

A

Growth and puberty delay,which cause dysfunction of hypothalamus, pituitary gland and some genetic disorders

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27
Q

Secondary hypogonadism is caused by

A

Chronic diseases like tumor, hyperprolactinemia that affects GnRH secretion,also some medication,dooungs and radiation

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28
Q

Endometriosis

A

Endometrial implantation outside uterus cause severe pelvic pain

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29
Q

Endometriosis treatment

A

Hormonal therapy with progestins or GnRH agonists or surgery if necessary

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30
Q

Hormonal therapy with progestins will

A

Reduce the proliferation of endometrium and it also shrinks the endometrium ,which is good for endometriosis

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31
Q

GnRH agonists

A

First increase the amount of FSH and LH ,but then downregultes it in continuous use

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32
Q

Combined oral contraceptive eg

A

Levonorgestrel (contain both estrogen and progesterone

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33
Q

Targets of COC

A

Hypothalamus, pituitary gland, endometrium,ovary, cervix

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34
Q

COC fn

A

Inhibit both FSH and LH release and thereby prevent follicle maturation eliminate preovulatory LH wave and suppressed ovulation

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35
Q

Progestins additional fn

A

Affect cervical secretion,inhibits endometrial proliferation,inhibits ovarian and uterine peristalsis

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36
Q

COC indication

A

Endometriosis,acne, dysmenorrhoea, premenstrual syndrome

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37
Q

Dysmenorrhoea

A

Painful menstrual cramps

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38
Q

Premenstrual syndrome

A

Emotional,physical and behavioural changes 1 or 2 weeks before menstruation

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39
Q

Single phase COC

A

Fixed dose of estrogen and progesterone throughout the cycle

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40
Q

Progestins high dose

A

Completely inhibits follicle dev and ovulation,changes cervical mucus properties And cause endometrial changes

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41
Q

Intermediate dose of progestin

A

Inhibit ovulation,but doesn’t affect follicle dev

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42
Q

Low dose progestin cause

A

Doesn’t completely inhibits ovulation and give intrauterine contraceptive effect

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43
Q

POC full form

A

Progestin only regular oral contraceptive

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44
Q

POC is better contraceptive for women with

A

Cardiovascular disease and risk of dev of thrombosis,age over 35,smokers,lactating women,women with migraine type headache

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45
Q

POC (Progestin )effect

A

Thisckend cervical wall,inhibits endometrial proliferation, reduce tubal and uterine peristalsis

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46
Q

Emergency contraception is

A

High dose of progestins taken over next 72 hour after intercourse

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47
Q

Ethinylestradiol effect

A

Replace endogenous hormone,increase bone mineral density, estrogen replacement ,inhibits follicular maturation and ovulation, Hormonal suppressive effect

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48
Q

Clinical use of estrogen

A

Estrogen replacement therapy in menopause and postmenopause, hypogonadism

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49
Q

Ethinylestradiol has more bioavailability than

A

Estradiol

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50
Q

Estradiol is widely used in

A

Topical pharmaceutical formulation

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51
Q

Side effects of ethinylestradiol

A

Deep vein thrombosis,risk of dev of endometrial or breast cancer

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52
Q

Estrogen has positive effect on

A

Breast,endometrium and bone tissue

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53
Q

Only SERM that has positive effect on breast tissue

A

Estrogens

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54
Q

Tamoxifen has positive effect ion

A

Endometrium and bone ,but negative effects on breast tissue

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55
Q

Raloxifene has positive effect Only on

A

Bone tissue,it has negative effects on endometrium and breast

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56
Q

In estrogen and SERM ,positive effect on endometrium is given by

A

Estrogen and tamoxifen

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57
Q

In estrogen and SERM , positive effect on bone tissue are done by

A

Estrogen, tamoxifen and Raloxifene

58
Q

Difference in tissue sensitivity to SERM is caused by

A

Difference in localisation of receptor, effect of transcriptional cofactors on receptor (coactivators and corepressors)

59
Q

Dominant cofactor determine

A

Agonist or antagonist effect on SERM

60
Q

Tamoxifen is

A

ER antagonist in breast tissue and partial agonist in endometrium and bone

61
Q

Tamoxifen do not stimulate

A

DNA synthesis, but inhibit cell division causing regression of malignant cells(Antiproliferative)

62
Q

Tamoxifen indication

A

Breast cancer

63
Q

Tamoxifen SE

A

Deep vein thrombosis, endometrial hyperplasia

64
Q

Raloxifene action

A

Partial ER agonist in bone tissue,ER antagonist in endometrium and breast tissue (anti resorptive effect), Decrease LDL

65
Q

Indication of raloxifene

A

Osteoporosis prevention and therapy

66
Q

SE of raloxifene

A

Deep vein thrombosis

67
Q

Clomiphene

A

ER antagonist in hypothalamus and adenohypophysis, partial ER agonist in ovaries, stimulate release of FSH and LH(blocks negative feedback), stimulate formation and maturation of ovarian follicle and ovulation

68
Q

Indication of clomiphene

A

Anovulatory cycle, ovulation stimulation

69
Q

SE of clomiphene

A

Overstimulation of ovaries

70
Q

Fulvestrant (ER antagonist in all tissue) action

A

Inhibit intracellular dimerization and binding of ER to ER element and downregultes ER density (Antiproliferative)

71
Q

Fulvestrant indication

A

Breast cancer

72
Q

Androstenedione produced from adipose tissue (cholesterol) is converted to estrone by

A

Aromatase in post menopause,which is further converted to estradiol

73
Q

Anastrozole (aromatase inhibitor) action

A

Decrease estrogen synthesis ,so Antiproliferative

74
Q

Indication of anastrozole

A

Breast cancer in menopause

75
Q

SE of anastrozole

A

Decrease bone mineral density

76
Q

Medroxyprogesterone (progesterone receptor agonist) action

A

Inhibit proliferation phase, thickens cervical mucus,interfer with tubal and uterine peristalsis -so hormone suppressive effect

77
Q

Medroxyprogesterone use

A

Progestin contraception, endometriosis

78
Q

SE of medroxyprogesterone

A

Impaired menstrual bleeding, decrease bone density due to its antiestrogenic effect and glucocorticoid activity of it,that inhibit osteoblast

79
Q

Levonorgestrel (progesterone receptors agonists) action

A

Inhibit proliferation phase, thickens cervical mucus,impairs peristalsis in tubule and uterus -hormone suppressive effect , inhibits ovulation

80
Q

Indication of Levonorgestrel

81
Q

In Levonorgestrel used in IUD

A

Ovulation is not inhibited, contraceptive effect only in uterus

82
Q

Levonorgestrel used as Emergency contraception,basic mechanism is

A

Inhibition of ovulation, rather than POC mechanism

83
Q

Dydrogesterone (progestin receptor agonist) action

A

In uterus forms endometrial secretory phase in estrogen filled uterus,provide protection against elevated estrogen induced endometrial hyperplasia

84
Q

Dydrogesterone has no contraceptive effect

A

On therapeutic dose

85
Q

Dydrogesterone inhibits

A

Estrogen receptor synthesis in endometrium

86
Q

Indication of Dydrogesterone

A

Conditions caused by endogenous progesterone deficiency like dysmenorrhoea, endometriosis, impending abortion ,… Hormonal replacement therapy

87
Q

All progesterone receptors agonists have

A

Antiestrogenic effect

88
Q

Levonorgestrel and medroxyprogesterone has

A

Androgen action

89
Q

Antiandrogenic action is given by

A

Cyproterone only

90
Q

Levonorgestrel and medroxyprogesterone has both

A

Antiestrogenic action and Androgen action

91
Q

Cyproterone has both

A

Antiestrogenic action and antiandrogenic action

92
Q

Levonorgestrel is not recommended for

A

Women with hyperandrogenism

93
Q

Antiandrogenic effect of progestins helps against

A

Acne vulgaris (cyproterone)

94
Q

Mifepristone (progesterone receptors antagonist) action

A

It is is also glucocorticoid receptor antagonist,blocks progesterone effect on endometrium, stimulate prostaglandin release and thereby cause myometrium contractions

95
Q

Mifepristone use

A

Termination of pregnancy in first trimester,hypercortisolism(in high dose)

96
Q

Mifepristone SE

A

Severe vaginal bleeding

97
Q

LH stimulate release of testesterone from

A

Leydig cells

98
Q

In prostate cells testesterone is converted to 5 alpha dihydrotestosterone by the enzyme

A

5 alpha reductase

99
Q

5alpha dihydrotestosterone (DHT) has

A

10 fold more affinity to receptor than testesterone

100
Q

Testesterone is converted to estrogen in peripheral tissue by

101
Q

Aromatase also control LH secretion by

A

Negative feedback along with androgens

102
Q

Effects of testesterone

A

Stimulate spermatogenesis, promote erythropoiesis, increase skeletal muscle mass and strength,maintain bone mineral density

103
Q

Androgen receptor agonists

A

Testesterone and nandrolone

104
Q

Androgen receptor antagonist

105
Q

Androgen receptor antagonist and Progestin receptor agonist

A

Cyproterone

106
Q

5 Alpha reductase inhibitor

A

Finasteride

107
Q

Benign prostate hyperplasia

A

Benign Stromal and epithelial cell hyperplasia in periurethral area of prostate,cause urinary tract disorder, conservative therapy used

108
Q

Hyperandrogenism/polycystic ovarian syndrome

A

Elevated levels of male hormones in women

109
Q

PCOS risks and symptoms

A

Miscarriage, pregnancy complications, Hirsutism, acne,adipositate

110
Q

Testesterone action

A

Androgenic action in prostate and testicles , protein anabolic action in muscle,bone, hematopoiesis,liver)

111
Q

Testesterone has

A

First pass effect

112
Q

Use of testesterone

A

Hypogonadism

113
Q

Nandrolone (Androgen receptor agonists) has

A

Enhanced anabolic effect and reduce androgenic effect ,is a testesterone derivative

114
Q

Andrew action

A

Stimulate erythropoietin secretion,increase BOne mineral density, promote protein synthesis, stimulate carbohydrate and lipid metabolism

115
Q

Nandrolone used a d

A

Doping drug -prohibited

116
Q

Use of nandrolone

A

Refractory anemia, osteoporosis (not used in women due to virilizing effect)

117
Q

High doses of anabolic steroids may cause secondary cause of hypogonadism and infertility due to

A

Inhibition of gonadotropin secretion, testesterone formation and spermatogenesis

118
Q

Prostate cells without Androgen will undergo

119
Q

Androgen receptor antagonist are of 2 types

A

Non steroidalor pure anti androgens like flutamide
Steroidal anti Androgen like cyproterone

120
Q

Steroidal anti Androgen also have properties of

121
Q

Flutamide action (anti Androgen non steroidal)

A

Antiproliferative

122
Q

Use of Flutamide

A

Prostate cancer (together with GnRH receptor agonists)

123
Q

SE flutamide

A

May increase LH secretion due to feedback mechanism

124
Q

Cyproterone (steroidal Androgen receptor antagonist and Progestin receptor agonist ) action

A

Inhibition of Androgen activity in target tissue, action of Progestin receptor agonist inhibits LH secretion through feedback,inhibits testesterone synthesis - so Antiproliferative and anti gonadotropic effect

125
Q

Use of cyproterone

A

Prostate cancer, Hirsutism and severe acne in women(hyperandrogenisity)

126
Q

Contraindications of cyproterone

127
Q

Finasteride (5 alpha reductase inhibitor) action

A

Prevent conversation of testesterone to DHT,triggers prostate epithelial cell apoptosis,so decrease prostate size and urination disorders, it has both antiandrogenic and Antiproliferative effect

128
Q

Use of finasteride

A

Benign prostate adenoma or hyperplasia,androgenic alopecia, Hirsutism in women

129
Q

SE of finasteride

A

Decrease in libido and erectile dysfunction

130
Q

Contraindications of finasteride

A

Pregnant women or women who is going to be pregnant

131
Q

While using transdermal testesterone gel(androgel) should be advised to avoid

A

Skin to skin contact with pregnant women

132
Q

While prescribing Androgen to male patients advice that

A

Cholestatic hepatitis and jaundice may occur with low doses of Androgen

133
Q

Sildenafil use

A

Primary hypertension and erectile dysfunction

134
Q

Women with migraine are not advised to use estrogen because

A

Increased risk of stroke

135
Q

Medroxyprogesterone injection has SE

A

Depression

136
Q

Sildenafil (Viagra)SE

A

Dev of chest pain or dizziness

137
Q

Raloxifene a ta on estrogen receptor in

A

Bone ,endometrium

138
Q

Interactions of sildenafil with nitrates cause

A

Fatal hypotension

139
Q

Androgens are used for

A

Symptomatic treatment of male deficiency,female libido, endometriosis, postmenopausal symptoms, increased muscle mass

140
Q

Estrogen effects

A

Main bone density by increasing bone reabsorption, maintain normal structure of skin and blood vessels

141
Q

Progesterone inhibits endometrial proliferation phase.True or false

142
Q

Pheromones are examples of

A

Ectohormone

Reproductive System Pharmacology (2 decks)

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