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Block 8 Pharmacology (Wk1+2) (Androgen Nuclear Hormone Receptor Agonist…
Block 8 Pharmacology (Wk1+2)
Oestragen Nuclear Hormone Receptor Agonist
High E2: acne, constipation, libido loss
Low E2: Slows bone growth and development
Oestradiol (E2) (Ethinylestradiol synthetic)
Increases SHBG and TBg, suppresses FSH
Menstruation: Maturation and release of egg. Endometrium thickening
Interacts wit Erα or Erβ present on organs, breasts, hypothal and pit. gland
Made in ovaries by oocytes: Their depletion main cause of menopause.
GnRH Receptor Agonist
Goserelin
Increase in LH: ^E2 female, ^Androgen male
However: chronic administration downregulates GnRH receptors: Lowers LH secretion
GnRH analogue (super agonist)
Inhibits growth of prostate cancer
Prostaglandin Receptor Agonist
Alprostadil (PGE-1 synth)
Binds EP1/2 receptors: ^cAMP and PKA
Intracavernosal/intraurethral suppository
Acts to relax smooth muscle of corpora cavernosa and arteries
Swelling, elongation. Venous outflow reduced to maintain
Androgen Nuclear Hormone Receptor Agonist
Nandrolone
Increases production and excretion of EPO
Naturally occuring anabolic steroid
Testosterone
Allows movement into cell nucleus and binds to Hormone Response Elements (HREs) influencing transcription activity.
Binds androgen receptor (AR) or reduced to DHT.
Antagonist: Bicalutamide
Binds AR blocking androgen action
Stops testosterone reaching cancer cells (prostate) to aid shrinkage/slowing of growth
Finasteride 5-α-R inhibitor
DHT associated with prostatic growth
Finasteride lowers [DHT]
5-α-reductase converts testosterone to DHT.
PDE5 Inhibitor
Sildafinil (viagra)
PDE5 breaks down cGMP which reduces cell response to NO
Therefore inhibition of PDE5 protects NO
NO causes vasodilation via ^cGMP
Mefenamic Acid
NSAID for menstrual pain
Tranexamic Acid (TXA)
Antifibrinolytic
Inhibits plasmin so degradation of fibrin clot cannot occur during heavy mestruation