Endocrine 5 (Disorders) Flashcards
Somatropin
Recombinant Growth Hormone
- Stimulates Hepatic Production of IGF
- Stimulates Growth
Mecasermin
Recombinant IGF
- Promotes uptake of amino acids
- Promotes protein synthesis
Affecting Skeletal Muscle and Cartilage of Long Bone
IGF-1
Insulin-Like Growth Factor
- Bind to IGF-1 Receptors to stimulate Cell Growth
Two Pathways
- Activation of Ras –> Activation of MEK –> Self-Proliferation
- Activation of Akt –> Activation of mTOR –> Stimulates Protein synthesis
Pegvisomant
Growth Hormone Receptor Antagonist
- Competitive Antagonist of GH
- Prevents GH from acting on liver receptors, preventing IGF secretion
Octreotide
Somatostatin Analogues
- Mimics action of somatostatin and inhibits Pituitary Gland
- Inhibits GH secretion
Octreotide inhibits Somatostatin Receptors 2 and 5
Lanreotide
Somatostatin Analogues
- Mimics action of somatostatin and inhibits Pituitary Gland
- Inhibits GH secretion
Pasireotide
Somatostatin Analogues
- Mimics action of somatostatin and inhibits Pituitary Gland
- Inhibits GH secretion
Testosterone
Acts on Androgen Receptors (Nuclear Receptor Signalling)
- Maturation of reproductive organs
- Development of secondary sexual characteristics
- Maintenance of spermatogenesis and maturation of spermatozoa
FSH
Follicle Stimulating Hormone
- Stimulates spermatogenesis and maturation of spermatozoa
ICSH
Interstitial Cell Stimulating Hormone
- Maturation of reproductive organs
- Development of secondary sexual characteristics
- Testes secrete testosterone
Gonadorelin
Pulse Administration:
- Secretion of LH and FSH
Chronic Administration
1. Down regulation of receptors in anterior pituitary
2. Inhibition of LH and FSH
3. Suppression of testicular steroidogenesis due to decreased LH and FSH
Result: Decrease in Testosterone
Buserelin
Pulse Administration:
- Secretion of LH and FSH
Chronic Administration
1. Down regulation of receptors in anterior pituitary
2. Inhibition of LH and FSH
3. Suppression of testicular steroidogenesis due to decreased LH and FSH
Result: Decrease in Testosterone
Leuprorelin
Pulse Administration:
- Secretion of LH and FSH
Chronic Administration
1. Down regulation of receptors in anterior pituitary
2. Inhibition of LH and FSH
3. Suppression of testicular steroidogenesis due to decreased LH and FSH
Result: Decrease in Testosterone
Goserelin
Pulse Administration:
- Secretion of LH and FSH
Chronic Administration
1. Down regulation of receptors in anterior pituitary
2. Inhibition of LH and FSH
3. Suppression of testicular steroidogenesis due to decreased LH and FSH
Result: Decrease in Testosterone
Nafarelin
Pulse Administration:
- Secretion of LH and FSH
Chronic Administration
1. Down regulation of receptors in anterior pituitary
2. Inhibition of LH and FSH
3. Suppression of testicular steroidogenesis due to decreased LH and FSH
Result: Decrease in Testosterone
Degarelix
Reversibly binds GnRH receptor in anterior pituitary and blocks it
- Decrease LH and FSH resulting in decreased testosterone
More rapid acting
Does not cause transient testosterone surge
Bicalutamide
Competitive Antagonist of Androgens
- Binds to androgen receptors on target tissue and inhibits androgen action
- Controls testosterone surges caused by GnRH analogues
–> Combine with GnRH analogues
Result: Inhibits Androgen Action to control testosterone flares
Enzalutamide
Competitive Antagonist of Androgens
- Binds to androgen receptors on target tissue and inhibits androgen action
- Controls testosterone surges caused by GnRH analogues
–> Combine with GnRH analogues
Result: Inhibits Androgen Action to control testosterone flares
Flutamide
Competitive Antagonist of Androgens
- Binds to androgen receptors on target tissue and inhibits androgen action
- Controls testosterone surges caused by GnRH analogues
–> Combine with GnRH analogues
Result: Inhibits Androgen Action to control testosterone flares
Nilutamide
Competitive Antagonist of Androgens
- Binds to androgen receptors on target tissue and inhibits androgen action
- Controls testosterone surges caused by GnRH analogues
–> Combine with GnRH analogues
Result: Inhibits Androgen Action to control testosterone flares
Cyproterone
Competitive Antagonist of Androgens
- Binds to androgen receptors on target tissue and inhibits androgen action
- Controls testosterone surges caused by GnRH analogues
–> Combine with GnRH analogues
Result: Inhibits Androgen Action to control testosterone flares
Abiraterone
Selectivity inhibits CYP17
- Enzyme needed for androgen biosynthesis in testicular, adrenal, and prostatic tumour tissues
Result: Decreases androgen in prostate tissue
Finasteride
Inhibits 5alpha-Reductase
- Prevents conversion of testosterone into the more potent dihydrotestosteron
- Treats benign prostatic hyperplasia
Result: Prevent formation of powerful testosterone, preventing inhibition of hair growth
Minoxidil
Hair follicles convert it into Minoxidil Sulfate
- Potent vasodilator that increases blood supply to hair follicles
Result: Stimulates growth of new hair follicles
