Reproductive Pharmacology

Question 1

Oestrogen: Acts on, Uses, ADE (e.g. ethinylestradiol)

Answer 1

Acts on oestrogen receptors. Promotes breast growth, bone mass, endometrial thickening.
Used in HRT, COC
ADE: increased breast, endometrial and ovarian cancer risk. Migraines. Increased clotting, vasodilation. Hyperpigmentation. Uterine bleeding. Oedema (sodium/water retention). Breast Tenderness. Migraines

Question 2

Raloxifene

Answer 2

SERM. Reduces oestrogen driven breast cancer growth, partial agonist for bone growth. Ednometrial antagonist. Used in breast cancer/oesteoporosis.
ADEL clotting, VTE risk. Increased TG/HDL

Question 3

Tamoxifen

Answer 3

SERM. Reduced oestrogen driven breast cancer growth. Partial agonist for bone growth. Agonist for endometrium.
ADEs:VTE risk, clotting, increased TG/HDL

Question 4

Clomiphene

Answer 4

Oestrogen antagonist. Induces ovulation. Acts at hypothalamus/puitary, but agonist at ovary and reduces negative feedback (FSH/GnRH increase gives LHsurge/ovulation).
Used for PCOS
ADE: GI discomfort, bleeding. can cause ovarian overstimulation syndrome

Question 5

Norethisterone

Answer 5

Progesterone agonist.
Suppresses GnRH, decreases endometrial proliferation, increases cervical mucus viscosity, decreased sodium reabsoption, decreased breast development.
Used as contraception (POP, COCP, implant), HRT with oestrogen. Endometriosis treatment. Endometrial carcinoma treatment
ADEs: acne, fluid retention, wt change, depression, libido effects, breast discomfort, menstrual irregularities, increased VTE risk

Question 6

Mifepristone

Answer 6

Progestoerone antagonist (competitive with partial agonist activity). Used for medical aborption with prostaglanding (gemeprost)
Has anti glucocorticoid activity, so CI in women taking glucocorticoids

Question 7

Testosterone /analogues

Answer 7

AR agonist. Promotes spermatogenesis, gives feedback to ant pit (LH secretion feedback). Anabolic on muscle/bone/sebum. Increased EPO.
Used in bodybuilding, pit/testicular hypogonadism, female hyposexuality
ADEs: limited at endogenous. Increase prostate cancer risk, sodium retention (oedema/HT), infertility, erthryocytosis, gynaecomastia, liver damage

Question 8

Flutamide

Answer 8

Androgen antagonist. Used in prostate cancer, and to counter spironolactone induced hisutism.

Question 9

Cyproterone

Answer 9

Androgen antagonist - chemical castration

Question 10

Finasteride

Answer 10

5-alpha reductase inhibitor. Prevents testerone to DHT conversion - used in BHP, androgenic alopoecia.

Question 11

Anastrazole

Answer 11

Aromatase inhibitor. Prevents conversion of testosterond to oestradiole, and androstenedione to oestrone. Used in breast cancer treatment (causes menopausal ADEs)

Question 12

Synthetic GnRH (gonadorelin)

Answer 12

GnRH agonist/antagonist. If pulse the agonist, continous is antagonist. Causes gonadal suppresion.
Used in breast cancer, prostate cancer, endometriosis, large uterine fibroids.
ADEs: menopausal symptoms, osteoporosis, androgen deprivation symtpoms

Question 13

Doxazosin

Answer 13

alpha blocker. Antiadrenergic drug with vasodilating actions. Used in BPH, Raynaulds and HT.
ADEs: postural hypotension, dizziness, priapism,fatigue, SOB>

Question 14

Levornogestrel

Answer 14

Used for emergency contraception

Question 15

Tamsulosin

Answer 15

Alpha adrenergic blocker. Used in BPH. Can cause SOB, priapism, postural hypotension, dizziness.

Question 16

Medroxyprogesterone acetate

Answer 16

Prosterone receptor agonist (thickens cervical mucus). Used for dysfunctional uterine bleeding, endometriosis, endometrial, renal, breast cancer. Contraception. HRT
ADEs: depression, fluid retention