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Medical Pharmacology of Reproduction
A medical student approach to the pharmacology surrounding the reproductive system.
53
Medical
Undergraduate 3
09/09/2013

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Cards

Term
Estradio, Estrone and Estriol are the three endogenous oestrogen's. Which is secreted principally by the ovary and is most potent?
Definition
Estradiol
Term
What is the role of estrogen in regards to receptor expression?
Definition
Estrogen induces the synthesis of progesterone receptors in the uterus, hypothalamus, pituitary and vagina.
Term
Does progesterone increase or decrease estrogen receptors?
Definition
Decreases
Term
WHat is the action of Finasteride?
Definition
Finasteride is a 5a reductase inhibitor. This is the enzyme responsible for converting testosterone to the active dihydrotestosterone. Indicated in treatment of BPH.
Term
How does Anastrazole work?
Definition
Anastrazole is an Aromatase enzyme inhibitor. Aromatase is the enzyme responsible for converting testosterone to estradiol.
Term
What are three metabolic effects of oestrogen?
Definition
Increase salt and water retention
Increase plasma concentration of HDL
Increase coagulability
Term
3 general functions of oestrogen
Definition
Replacement therapy in ovarian failure
Contraception
Prostate and breast cancer
Term
2 general uses of antioestrogens
Definition
Oestrogen sensitive breast cancer
To induce ovulation
Term
Difference between natural and synthetic estrogen metabolism?
Definition
Both are well absorbed but natural estrogens are more rapidly metabolised by the liver.
Term
Group AEs of estrogen therapy?
Definition
Breast tenderness, vomiting, odema, VTE
Term
Raloxifene
Definition
Class SERM. Has an antiestrogenic effect on breasts and uterus, proestrogenic effects on bones, lipid and coagulation. Indicated in the prevention of postmenopausal osteoporosis.
Term
Tamoxifen
Definition
Is a agonist/antagonist. Proestrogenic in lipid profile, endometrium and bones and antiestrogenic effects on the mammary glands. Used in oestrogen-dependent breast cancer.
Term
Clomiphene
Definition
Is an antiestrogenic. It inhibits estrogen binding in the anterior pituitary, deregulating GnRH production resulting in ovarian enlargement and increasing fertility. It is used in infertility due to lack of ovulation.
Term
There are two types of progestogens?
Definition
Progesterone (hydroxyprgesterone) and Testosterone (norethiserone)
Term
Advantages and disadvantages of the newer progestogens (desogestrel)?
Definition
Indicated in patients who experience acne, depression or breakthrough bleeding). Increased risk of VTE.
Term
Group AEs of progesterones?
Definition
Weak androgenic effects, acne, fluid retention, weight gain, depression, menstrual changes.
Term
Main therapeutic indication of progesterone?
Definition
Contraception
Estrogen replacement (to prevent endometrial hyperplasia, because progesterone inhibits estrogen receptor synthesis)
Endometriosis
Term
Mifepristone
Definition
is an antiprogestogen. It is a partial agonist that increases the sensitivity of the uterus to proastaglandins. Given with gemeprost (a pgl) to induce termination.
Term
Pros and cons of HRT?
Definition
Short term use of HRT treats the symptoms of oestrogen reduction including hot flushes, vaginal atrophy and bone loss.

Increases risk of breast and uterine cancer, increase VTE.
Term
Tibolone
Definition
used for the short term treatment of oestrogen deficiency. Has estrogenic, progesterogenic and weak androgenic effects.
Term
FSH in males induces?
Definition
Gametogenesis, as regulated by the sertoli cells.
Term
LH in males is responsible for?
Definition
Stimulating testosterone production by the Leydig (or interstitial cells)
Term
Role of testosterone?
Definition
Development of secondary sexual characteristics
Increase in muscular strength
Development of the reproductive organs
Term
AEs of testosterone?
Definition
Down regulation of GnRH production, infertility, oedema, acne, growth impairment in children.
Term
Indications for androgens?
Definition
Hypogonadism
Hyposexuality following ovariectomy
Term
Cyproterone
Definition
is a partial agonist of androgen receptors. It depresses GnRH and therefore gonadotrophin concentration indicated in precocious puberty, masculinity in women and sex offenders, as well as an adjunct in prostate cancer.
Term
Tamsulosin
Definition
is a a1 adrenoreceptor anatagonist, which relaxes the smooth muscle in the prostate capsule to treat BPH.
Term
Goserelin
Definition
is a potent synthetic GnRH. With continuous use initially they increase the concentration of sex hormones, but quickly desensitisation occurs. Indicated for treatment of hormone sensitive cancers of the prostate, breast and endometriosis.
Term
Danazol
Definition
is a GnRH inhibitor used in sex hormone dependent conditions like gynecomastia. Adverse effects include fluid retention, GI disturbances and headache. Used as a virilising agent.
Term
The two main types of contraception pills
Definition
Combined
Progestogen only
Term
Which estrogen and progestogen are used in the COCP?
Definition
Ethinylestradiol
Levenorgesterel, Norethiserone
(Third gen --> desogestrel)
We choose the lowest dose that gives good cyclical control and is well tolerated.
Term
Third gen vs Second gen
Definition
Third have less androgenergic effect but have increased risk of VTE
Term
MoA of COCP
Definition
Estrogen inhibits FSH production
Progestogen inhibits LH production + cervical thickening
Combine to alter endometrium
21 of 28 days
Term
Side effects of the COCP
Definition
Weight gain, nausea, depression, dizziness, skin changes, amenorrhea.
Term
MoA of progestogen only, advantages disadvantages?
Definition
Cervical mucus thickening and some effects of implantation. No estrogenic effects, more sensitive to mistake in missing pill.
28 of 28 days
Term
Interactions to consider with contraceptive pills?
Definition
Affected by enzyme inducers (phenytoin, carbemazepine), action can be inhibited by antibiotics.
Term
High dose oral levonorgestrel
Definition
Emergency contraception up to 72 hours. Needs to be taken with an antiemetic.
Term
Medroxyprogesterone
Definition
IM contraception, effective and safe but increase chance of menstrual irregularities and long time return to fertility.
Term
Implanon (levonorgestrel)
Definition
Slow release sub cut capsule, 3 years of contraception. Unpredicatable menstruation + headaches.
Term
Mirena (levonorgestrel)
Definition
IUD 3-5 years contraception.
Term
Uterine myometrial pacemakers are controlled by...
Definition
sex hormones, hence the activity during menstruation.
Term
In the uterus there are B2 and alpha adrenoreceptors, which inhibits and which induces contraction.
Definition
B2 inhibits
Alpha induces.
Term
Oxytocin
Definition
Release is stimulated by cervical dilation and suckling.
Ostrogen induces oxytocin receptors
Oxytocin induces contraction
Indicated in the induction of labour and let down.
Term
Ergometrine
Definition
indicated in post partum hemorrhage (after oxytocin) Given incombination before third stage of labour. Induces strong contraction in a lax uterus. Rapid onset last 3-6 hours. Causes vasoconstriction.
Term
Dinoprostone
Definition
indicated in late therapeutic abortion
Term
Gemeprost
Definition
Given in combination with Mifepristone to medically induce abortion.
Term
Ritodrine
Definition
Is a B2 agonist in the uterus and inhibits preterm labour
Term
AEs of Oxytocin
Definition
Water retention and rebound tachycardia
Term
Atosiban
Definition
is an oxytocin antagonist, to delay preterm labour, can cause vomiting, vasodilation and hyperglycemia.
Term
Sildenafil
Definition
increase cGMP resulting in a vasodilatory effect and filling of the penile vascular bed. 30 minute onset. COntraindicatng with nicorandil. AEs include hypotension, flushing, headache.
Term
Tadalafil
Definition
has a longer half life the Sildenafil so can be taken longer before the required time.
Term
Fulvestrant
Definition
Estrogen receptor antagonist indicated in treatment of estrogen receptor positive breast cancer.
Term
Trastuzumab
Definition
is a MAb use to treat HER2 positive breast cancer
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