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Pharmacology Block 9 > Reproductive Pharmacology > Flashcards

Reproductive Pharmacology Flashcards

1
Q

Ethinyl estradiol and mestranol are modified by the addition of?

A

An ethinyl group to estradiol which reduces first pass metabolism, increases the half life to about 20 hours and results in greater oral potency compared with native estradiol

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2
Q

What is the major metabolic pathway for ethinyl estradiol both in rats and humans?

A

Aromatic hydroxylation

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3
Q

Ethinyl estradiol and mestranol are contraindicated in what population?

A

Women over 35 who smoke due to increased risk of serious cardiovascular side effects

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4
Q

Ethinyl estradiol and mestranol decrease the anti coagulant activity of which medication?

A

Warfarin

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5
Q

Ethynyl estradiol and mestranol decrease the effectiveness of which medication?

A

Thiazolidinedion

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6
Q

The therapeutic effect of acarbose can be decreased when used in combination with

A

Ethinylestradiol

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7
Q

The metabolism of ethinylestradiol can be decreased when combined with

A

Acetazolamide

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8
Q

Ethinylestradiol may decrease the excretion rate of which drug?

A

Amiodarone

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9
Q

Estrogens may ocasionally cause what

A

Breast tenderness

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10
Q

What are some serious adverse effects of estrogens?

A

Hypertension, thromboembolic disorders, formation of gallstones

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11
Q

Estrogens should be used with caution in women with what conditions?

A

Hepatic disease, endometriosis, thromboembolic disorders or hypercalcemia

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12
Q

Progesterone binds to what?

A

Progesterone and estrogen receptors

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13
Q

Once bound to the receptor, progesterone will slow the frequency of release of GNRH from the hypothalamus and blunt the pre-ovulatory

A

LH hormone surge

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14
Q

Progesterone acts to maintain what?

A

Pregnancy

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15
Q

Progesterone also stimulates what?

A

Growth of mammary alveolar tissue and relaxes uterine smooth muscle

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16
Q

What are some examples of progestins?

A

Megestrol, hydroxyprogesterone caproate, medroxyprogesterone acetate

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17
Q

The metabolism of progesterone is primarily

A

Hepatic

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18
Q

What is the half life of progesterone?

A

34 hours

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19
Q

What is the interaction between warfarin and megestrol?

A

Megestrol decreases the anticoagulant activities of warfarin

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20
Q

The therapeutic efficiency of 2,4-thiazolidinedione can be reduced when used with

A

Megestrol acetate

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21
Q

Megestrol may decrease the excretion rate of

A

Abacavir

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22
Q

Megesterol may decrease the anticoagulant activities of which other medication?

A

Acetylsalycilic acid

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23
Q

Which medication could cause a higher serum level of megestrol?

A

Acyclovir

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24
Q

What are some adverse effects of progesterones?

A

Coronary artery disease, stroke, pulmonary embolism

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25
Q

The first generation CHC consist of?

A

High concentration of estradiol

Contain 50 microgram of ethinylestradiol and progesterone as lynestrenol and norethisterone

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26
Q

The second generation CHC consist of?

A

Low concentration of hormones

Contain ethinylestradiol and contains levonogestrel and norgestrel as progestogen

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27
Q

The second generation CHC were made for?

A

Decreasing secondary effects

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28
Q

Third generation CHC consist of?

A

Low concentrations of hormones

Contains ethinylestradiol and contains desogestrel, gestodeno and norgesterone

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29
Q

Fourth generation CHC contain

A

Low concentration of hormones and ethinylestradiol cyproterone and drospirenone

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30
Q

Diethystilbesterol has a potential to be

A

Carcinogenic

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31
Q

Conjugated estrogens are a mix of?

A

Estrogens and soluble salts as sulfate esters

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32
Q

What happens if you forget to take your birth control pill?

A

Take a pill as soon as you remember

Then for the next one you take it at your usual time

Keep taking active pills as usual one each day

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33
Q

What happens if you forget to take more than one pill?

A

Follow the guidelines on what to do if you forget to take one pill and refrain from sex or use an extra method of protection for seven days

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34
Q

What should you do if miss more than one pill of the last seven active pills?

A
  1. Finish all active pills in the pack
  2. Do not take last inactive pills in the 28 pack
  3. Do not wait seven days to start a new 21 pill pack
  4. Start a new pack the next day
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35
Q

What is the effect of progesterone?

A

Slows the frequency and release of GnRH and blunts the LH surge

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36
Q

progesterone stimulates the growth of?

A

Alveolar tissue of the breast and relaxes uterine smooth muscle

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37
Q

What does estrogen do?

A

Suppreses FSH secretion

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38
Q

The combination of estrogen and progesterone suppreses the

A

Secretion of GnRH

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39
Q

What are some side effects of estrogen contraception?

A

Breakthrough bleeding
Nausea
Fluid retention
Non infective vaginal discharge

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40
Q

What are some progesterone side effects?

A

Vaginal dryness
Depression
Acne
Loss of libido

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41
Q

What are the principal risk factors for estrogen and progesterone contraceptives?

A

VTE
Venous thromboembolic disease

Arterial thromboembolism

Myocardial infarction

Haemorrhagic stroke

Ischemic stroke

Stroke in pregnancy

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42
Q

What are the two most important independant risk factors for Myocardial infarction and ischaemic stroke?

A

Hypertension and smoking

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43
Q

What are other principal risks for estrogen and progesterone contraception?

A

Blood pressure and breast cancer

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44
Q

What are some benefits of using estrogen and progesterone contraception?

A

Reduced risk of ovarian, colon and endometrial cancer, PID as well as many period related problems

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45
Q

Progesterone only pills can be indicated in what situations?

A

Breast feeding and in those whose estrogens are contraindicated

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46
Q

Progesterone only pills are taken how?

A

Every day!

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47
Q

Progesterone only pills are effective within

A

24 hours

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48
Q

What is an advantage of taking progesterone only pills?

A

Reversible without estrogen associated risk

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49
Q

What are some side effects of progesterone only pills?

A

Amenorrhea, ovarian cysts, if ovulation is not inhibited ectopic pregnancy is more likely and also breakthrough bleeding

50
Q

What is the principal risk of taking progesterone only pills?

A

Breast cancer

51
Q

What are some contraindications for progesterone only pills?

A

Breast cancer and ovarian cancer

52
Q

What are some pharmacological effects of POP’s?

A

Decrease the amount of cervical mucus
Increase viscosity
Produce a thin and atrophic endometrial tissue

53
Q

Low doses of POP’s block what percentage of ovulations?

A

50%

54
Q

Middle doses (subdermal implants) of POP’s block what percentage of ovulations?

A

97-99%

55
Q

High doses of POP’s (depot injectable) block what?

A

Follicular development and ovulation

56
Q

Emergency contraceptives is recommended to use when?

A

First 120 hours after unprotected intercourse but most effective during the first 72 hours

57
Q

Clomiphene has both what?

A

Estrogenic and anti-estrogenic properties

58
Q

Clomiphene has the ability to

A

Stimulate the release of gonadotropins, FSH, LH at low concentrations but can block the release of these substances at high concentrations

59
Q

What are the indications of clomiphene?

A

Anovulatory infertility and PCOS

60
Q

The metabolism of warfarin can be decreased when interacting with?

A

Clomifene

61
Q

The serum concentration of clomifene can be increased when it is combined with

A

Acetaminophene

62
Q

The serum concentration of clomifene can be increased when it is combined with

A

Albendazole

63
Q

The serum concentration of acetylsalycilic acid is increased when used with

A

Clomifene

64
Q

Which drug causes the serum concentration of clomifene to increase?

A

Atorvastatin

65
Q

What is one adverse effect of clomiphene?

A

Multiple births

66
Q

which three drugs cause the serum concentration of clomifene to increase?

A

Acetaminophen, albendazole and atorvastatin

67
Q

what is the MOC of tamoxifen?

A

Non steroidal agent that binds to estrogen receptors inducing a conformational change. This results in a blockage or change in the expression of estrogen dependant genes

68
Q

The prolonged binding of tamoxifen to the nuclear chromatin results in

A

Reduced DNA polymerase activity, impaired thymidine utilization, blockage of estradiol uptake, and decreased estrogen response

69
Q

What effect does tamoxifen have on warfarin?

A

Increases the anticoagulant activities

70
Q

Which drug increase the serum level of tamoxifen?

A

Acetaminophen

71
Q

The risk or severity of bleeding can be increased when tamoxifen is combined with

A

Acetylsalycilic acid

72
Q

The risk or severity of liver damage can be increased when tamoxifen is used with

A

Verapamil

73
Q

Which drug increases the serum level of tacrolimus?

A

Tamoxifen

74
Q

What is an indication for tamoxifen?

A

Breast cancer

75
Q

Tamoxifen increases the risk of which cancer?

A

Endometrial cancer

76
Q

What enzyme does anastrozole and letrozole inhibit?

A

Aromatase

77
Q

Anastrozole can decrease the metabolism of which drugs?

A

Warfarin, alprazolam, aprepitant and azithromycin

78
Q

what are the indications for anastrazole and letrozole?

A

Breast cancer and metastatic breast cancer

79
Q

Mifepristone increases the serum concentration of?

A

Warfarin and amiodarone

80
Q

There is a risk of what if mifepristone and thiazolidinedione are taken together?

A

Hypoglycemia

81
Q

The risk or severity of QTc prolongation can be increased when mifepristone is combined with

A

Amlodipine

82
Q

Mifepristone is used to

A

Terminate a pregnancy

83
Q

The adverse effects of mifepristone are

A

Nausea, vomiting, abdominal pain, anorexia, heavy uterine bleeding, fatigue

84
Q

Which cells produce testosterone in males?

A

Leydig cells of the testes

85
Q

What stimulates the secretion of testosterone by leydig cells?

A

LH

86
Q

For what conditions is testosterone indicated in women?

A

Palliative treatment of androgen-responsive advanced, inoperable metastasis of breast cancer in women who are 1-5 post menopausal. Also testosterone esters may be used in combination with estrogens in the managment of moderate to severe vasomotor symptoms associated with menopause in women who do not respond well to estrogen therapy alone

87
Q

What are the active major metabolites of testosterone?

A

Estradiol and DHT

88
Q

Which two drugs increase the serum level of testosterone?

A

Acyclovir and amikacin

89
Q

Testosterone increases the metabolism of which two drugs?

A

Alprazolam and sildenafil

90
Q

When taking testosterone, maximum improvement is reached in how many weeks?

A

18-30 weeks

91
Q

What are some contraindications when it comes to administering testosterone?

A

Prostate cancer, male breast cancer, severe sleep apnea, male infertility, hematocrit above 54%, BPH, heart failure

92
Q

What does danazol do?

A

Anterior pituitary suppresant

Inhibits the pituitary output of gonadotropins

93
Q

Does danazol posses androgenic properties?

A

Yes

94
Q

Danazol is used as a prophylaxis for what?

A

Hereditary angioedema in males and females

95
Q

How does danazol facilitate regression of endometriosis?

A

By decreasing IgG, IgM, and IgA concentrations as well as phospholipid and IgG isotope autoantibodies

96
Q

Danazol directly inhibits

A

Ovarian stereogenesis

97
Q

Is danazol teratogenic?

A

Yes

98
Q

The metabolism of which drugs is decreased when combined with danazol?

A

Bezafibrate, ulipristal, tamoxifen, sibutramine

99
Q

Leuprolide is a analogue of what?

A

GnRH

100
Q

Leuprolide is used to treat what?

A

Advanced prostate cancer, treat uterine fibroids, endometriosis, premature puberty

101
Q

Leuprolide is degraded by

A

Peptidases

102
Q

The metabolism of which drug can be decreased when mixed with leuprolide?

A

Atorvastatin

103
Q

The risk or severity of what conditions can be increased when captopril is mixed with leuprolide?

A

Myopathy, rhabdomyolysis, myoglobinuria

104
Q

The risk or severity of what can be increased when timolol is mixed with leuprolide?

A

QTc prolongation

105
Q

For what conidtion is flutamide used for?

A

Managment of locally confined stage B2-C and Stage D2 metastatic carcinoma lf the prostate

106
Q

What is the MOC of flutamide?

A

Nonsteroidal antiandrogen that blocks the action of both endogenous and exogenous testosterone by binding to its receptor

107
Q

Flutamide is an agonist of what receptor?

A

Artyl hydrocarbon

108
Q

Flutamide is a antagonist of what receptor?

A

Androgen receptor

109
Q

Which drugs may increase the serum level of flutamide?

A

Carboplatin and tramadol

110
Q

Which drug decreases the metabolism of flutamide?

A

Rosuvastatin

111
Q

What is finasteride?

A

Orally active testosterone 5-alpha-reductase inhibitor

112
Q

Finasteride is used for the treatment of

A

Symptomatic BPH

113
Q

Finasteride is also used for

A

Alopecia

114
Q

Finasteride blocks the production of

A

DHT

115
Q

Finasteride may decrease the antihypertensive effects of

A

Captopril

116
Q

The metabolism of what drug can be decreased when mixed with finasteride

A

Digitoxin

117
Q

What happens when finasteride is mixed with terbutaline?

A

Risk or severity of hypertension increases

118
Q

The risk or severity of hypertension is increased when finasteride is taken with

A

Naproxen

119
Q

In monophasic contraception we have

A

Constant doses of estrogen and progesterone

120
Q

In biphasic contraceptives estrogens are

A

Constant along the cycle but progesterones are increasing at the half of the cycle

121
Q

Three phases oral contraceptive estrogens

A

Increase at the half of the cycle and progesterones have a steady increase along the cycle

Pharmacology Block 9 (7 decks)

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