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
2
Q
What is the major metabolic pathway for ethinyl estradiol both in rats and humans?
A
Aromatic hydroxylation
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
4
Q
Ethinyl estradiol and mestranol decrease the anti coagulant activity of which medication?
A
Warfarin
5
Q
Ethynyl estradiol and mestranol decrease the effectiveness of which medication?
A
Thiazolidinedion
6
Q
The therapeutic effect of acarbose can be decreased when used in combination with
A
Ethinylestradiol
7
Q
The metabolism of ethinylestradiol can be decreased when combined with
A
Acetazolamide
8
Q
Ethinylestradiol may decrease the excretion rate of which drug?
A
Amiodarone
9
Q
Estrogens may ocasionally cause what
A
Breast tenderness
10
Q
What are some serious adverse effects of estrogens?
A
Hypertension, thromboembolic disorders, formation of gallstones
11
Q
Estrogens should be used with caution in women with what conditions?
A
Hepatic disease, endometriosis, thromboembolic disorders or hypercalcemia
12
Q
Progesterone binds to what?
A
Progesterone and estrogen receptors
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
14
Q
Progesterone acts to maintain what?
A
Pregnancy
15
Q
Progesterone also stimulates what?
A
Growth of mammary alveolar tissue and relaxes uterine smooth muscle
16
Q
What are some examples of progestins?
A
Megestrol, hydroxyprogesterone caproate, medroxyprogesterone acetate
17
Q
The metabolism of progesterone is primarily
A
Hepatic
18
Q
What is the half life of progesterone?
A
34 hours
19
Q
What is the interaction between warfarin and megestrol?
A
Megestrol decreases the anticoagulant activities of warfarin
20
Q
The therapeutic efficiency of 2,4-thiazolidinedione can be reduced when used with
A
Megestrol acetate
21
Q
Megestrol may decrease the excretion rate of
A
Abacavir
22
Q
Megesterol may decrease the anticoagulant activities of which other medication?
A
Acetylsalycilic acid
23
Q
Which medication could cause a higher serum level of megestrol?
A
Acyclovir
24
Q
What are some adverse effects of progesterones?
A
Coronary artery disease, stroke, pulmonary embolism
25
The first generation CHC consist of?
High concentration of estradiol
| Contain 50 microgram of ethinylestradiol and progesterone as lynestrenol and norethisterone
26
The second generation CHC consist of?
Low concentration of hormones
| Contain ethinylestradiol and contains levonogestrel and norgestrel as progestogen
27
The second generation CHC were made for?
Decreasing secondary effects
28
Third generation CHC consist of?
Low concentrations of hormones
| Contains ethinylestradiol and contains desogestrel, gestodeno and norgesterone
29
Fourth generation CHC contain
Low concentration of hormones and ethinylestradiol cyproterone and drospirenone
30
Diethystilbesterol has a potential to be
Carcinogenic
31
Conjugated estrogens are a mix of?
Estrogens and soluble salts as sulfate esters
32
What happens if you forget to take your birth control pill?
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
33
What happens if you forget to take more than one pill?
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
34
What should you do if miss more than one pill of the last seven active pills?
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
35
What is the effect of progesterone?
Slows the frequency and release of GnRH and blunts the LH surge
36
progesterone stimulates the growth of?
Alveolar tissue of the breast and relaxes uterine smooth muscle
37
What does estrogen do?
Suppreses FSH secretion
38
The combination of estrogen and progesterone suppreses the
Secretion of GnRH
39
What are some side effects of estrogen contraception?
Breakthrough bleeding
Nausea
Fluid retention
Non infective vaginal discharge
40
What are some progesterone side effects?
Vaginal dryness
Depression
Acne
Loss of libido
41
What are the principal risk factors for estrogen and progesterone contraceptives?
VTE
Venous thromboembolic disease
Arterial thromboembolism
Myocardial infarction
Haemorrhagic stroke
Ischemic stroke
Stroke in pregnancy
42
What are the two most important independant risk factors for Myocardial infarction and ischaemic stroke?
Hypertension and smoking
43
What are other principal risks for estrogen and progesterone contraception?
Blood pressure and breast cancer
44
What are some benefits of using estrogen and progesterone contraception?
Reduced risk of ovarian, colon and endometrial cancer, PID as well as many period related problems
45
Progesterone only pills can be indicated in what situations?
Breast feeding and in those whose estrogens are contraindicated
46
Progesterone only pills are taken how?
Every day!
47
Progesterone only pills are effective within
24 hours
48
What is an advantage of taking progesterone only pills?
Reversible without estrogen associated risk
49
What are some side effects of progesterone only pills?
Amenorrhea, ovarian cysts, if ovulation is not inhibited ectopic pregnancy is more likely and also breakthrough bleeding
50
What is the principal risk of taking progesterone only pills?
Breast cancer
51
What are some contraindications for progesterone only pills?
Breast cancer and ovarian cancer
52
What are some pharmacological effects of POP’s?
Decrease the amount of cervical mucus
Increase viscosity
Produce a thin and atrophic endometrial tissue
53
Low doses of POP’s block what percentage of ovulations?
50%
54
Middle doses (subdermal implants) of POP’s block what percentage of ovulations?
97-99%
55
High doses of POP’s (depot injectable) block what?
Follicular development and ovulation
56
Emergency contraceptives is recommended to use when?
First 120 hours after unprotected intercourse but most effective during the first 72 hours
57
Clomiphene has both what?
Estrogenic and anti-estrogenic properties
58
Clomiphene has the ability to
Stimulate the release of gonadotropins, FSH, LH at low concentrations but can block the release of these substances at high concentrations
59
What are the indications of clomiphene?
Anovulatory infertility and PCOS
60
The metabolism of warfarin can be decreased when interacting with?
Clomifene
61
The serum concentration of clomifene can be increased when it is combined with
Acetaminophene
62
The serum concentration of clomifene can be increased when it is combined with
Albendazole
63
The serum concentration of acetylsalycilic acid is increased when used with
Clomifene
64
Which drug causes the serum concentration of clomifene to increase?
Atorvastatin
65
What is one adverse effect of clomiphene?
Multiple births
66
which three drugs cause the serum concentration of clomifene to increase?
Acetaminophen, albendazole and atorvastatin
67
what is the MOC of tamoxifen?
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
The prolonged binding of tamoxifen to the nuclear chromatin results in
Reduced DNA polymerase activity, impaired thymidine utilization, blockage of estradiol uptake, and decreased estrogen response
69
What effect does tamoxifen have on warfarin?
Increases the anticoagulant activities
70
Which drug increase the serum level of tamoxifen?
Acetaminophen
71
The risk or severity of bleeding can be increased when tamoxifen is combined with
Acetylsalycilic acid
72
The risk or severity of liver damage can be increased when tamoxifen is used with
Verapamil
73
Which drug increases the serum level of tacrolimus?
Tamoxifen
74
What is an indication for tamoxifen?
Breast cancer
75
Tamoxifen increases the risk of which cancer?
Endometrial cancer
76
What enzyme does anastrozole and letrozole inhibit?
Aromatase
77
Anastrozole can decrease the metabolism of which drugs?
Warfarin, alprazolam, aprepitant and azithromycin
78
what are the indications for anastrazole and letrozole?
Breast cancer and metastatic breast cancer
79
Mifepristone increases the serum concentration of?
Warfarin and amiodarone
80
There is a risk of what if mifepristone and thiazolidinedione are taken together?
Hypoglycemia
81
The risk or severity of QTc prolongation can be increased when mifepristone is combined with
Amlodipine
82
Mifepristone is used to
Terminate a pregnancy
83
The adverse effects of mifepristone are
Nausea, vomiting, abdominal pain, anorexia, heavy uterine bleeding, fatigue
84
Which cells produce testosterone in males?
Leydig cells of the testes
85
What stimulates the secretion of testosterone by leydig cells?
LH
86
For what conditions is testosterone indicated in women?
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
What are the active major metabolites of testosterone?
Estradiol and DHT
88
Which two drugs increase the serum level of testosterone?
Acyclovir and amikacin
89
Testosterone increases the metabolism of which two drugs?
Alprazolam and sildenafil
90
When taking testosterone, maximum improvement is reached in how many weeks?
18-30 weeks
91
What are some contraindications when it comes to administering testosterone?
Prostate cancer, male breast cancer, severe sleep apnea, male infertility, hematocrit above 54%, BPH, heart failure
92
What does danazol do?
Anterior pituitary suppresant
| Inhibits the pituitary output of gonadotropins
93
Does danazol posses androgenic properties?
Yes
94
Danazol is used as a prophylaxis for what?
Hereditary angioedema in males and females
95
How does danazol facilitate regression of endometriosis?
By decreasing IgG, IgM, and IgA concentrations as well as phospholipid and IgG isotope autoantibodies
96
Danazol directly inhibits
Ovarian stereogenesis
97
Is danazol teratogenic?
Yes
98
The metabolism of which drugs is decreased when combined with danazol?
Bezafibrate, ulipristal, tamoxifen, sibutramine
99
Leuprolide is a analogue of what?
GnRH
100
Leuprolide is used to treat what?
Advanced prostate cancer, treat uterine fibroids, endometriosis, premature puberty
101
Leuprolide is degraded by
Peptidases
102
The metabolism of which drug can be decreased when mixed with leuprolide?
Atorvastatin
103
The risk or severity of what conditions can be increased when captopril is mixed with leuprolide?
Myopathy, rhabdomyolysis, myoglobinuria
104
The risk or severity of what can be increased when timolol is mixed with leuprolide?
QTc prolongation
105
For what conidtion is flutamide used for?
Managment of locally confined stage B2-C and Stage D2 metastatic carcinoma lf the prostate
106
What is the MOC of flutamide?
Nonsteroidal antiandrogen that blocks the action of both endogenous and exogenous testosterone by binding to its receptor
107
Flutamide is an agonist of what receptor?
Artyl hydrocarbon
108
Flutamide is a antagonist of what receptor?
Androgen receptor
109
Which drugs may increase the serum level of flutamide?
Carboplatin and tramadol
110
Which drug decreases the metabolism of flutamide?
Rosuvastatin
111
What is finasteride?
Orally active testosterone 5-alpha-reductase inhibitor
112
Finasteride is used for the treatment of
Symptomatic BPH
113
Finasteride is also used for
Alopecia
114
Finasteride blocks the production of
DHT
115
Finasteride may decrease the antihypertensive effects of
Captopril
116
The metabolism of what drug can be decreased when mixed with finasteride
Digitoxin
117
What happens when finasteride is mixed with terbutaline?
Risk or severity of hypertension increases
118
The risk or severity of hypertension is increased when finasteride is taken with
Naproxen
119
In monophasic contraception we have
Constant doses of estrogen and progesterone
120
In biphasic contraceptives estrogens are
Constant along the cycle but progesterones are increasing at the half of the cycle
121
Three phases oral contraceptive estrogens
Increase at the half of the cycle and progesterones have a steady increase along the cycle
