Growth hormone, reproductive hormone Flashcards
GHRH analogues
- Sermorelin
- Macimorelin
- Tesamorelin
Used: - Diagnosis of cause of dwarfism:
After sermorelin administration, if GH 🔼 ➡️ hypothalamic dwarfism otherwise pituitary dwarfism - In patients of AIDS associated lipodystrophy
GH analogues
Examples and mnemonic
Somatrem and Somatropin Small Children: Small uses Child S/E ren CI
GH analogue uses
S. Small for gestation baby M. Malabsorption in short bowel syndrome A. AIDS related wasting LL. 🔽 length, dwarfism Eg., Turner syndrome, Prader Willi syndrome, Noonan syndrome
GH analogues
side effects and contraindications
S/E: C. Carpel tunnel syndrome H. Hyperglycemia I. 🔼 Intracranial pressure L. Leukemia D. DM CI: RE. Retinopathy (🔼 vascularity) N. Neoplasia
IGF-1 analogues
Mecasermin & Mecasermin rinfabate (bound to IGF BP-3) Rx of dwarfisms due to: 1. 🔽 IGF-1 2. GH-R mutation 3. Anti GH antibodies S/E: 1. Hypoglycemia (unlike others) 2. Lipohypertrophy
Somatostatin analogues
examples and effects
- Octreotide: most useful
- Lanreotide
- Paseriotide
Effects: 🔽 TSH & GH
Somatostatin analogues
Uses
1. Octreotide is DoC for: • Secretory diarrhea • Glucagonoma, VIPoma, somatostatinoma, GRFoma • Acute variceal bleeding 2. Radio-labeled octreotide: diagnosis of pituitary adenoma, carcinoid tumour 3. Vasoconstrictor to 🔽 bleeding. Eg., pancreatic surgery 4. Acromegaly (DoC is cabergoline) 5. Thyrotroph adenoma
Somatostatin analogues
side effects
- Hypothyroidism
- 🔽 gall bladder contraction ➡️ cholelithiasis (like estrogen)
- M/C: 🤢, 🤮
GH receptor antagonist
Pegvisomant
Use: resistant hypertrophy
S/E:
Pituitary adenoma ➡️ regular visual field examinations to be done
Gonadorelin
GnRH analogue
🔼 LH / FSH
Uses:
1. Anovulation
2. Diagnosis of hypogonadotropic hypogonadism:
After giving gonadorelin, if LH/FSH 🔼, defect in hypothalamus
S/E: multiple gestation (🔽 risk than GnRH agonists)
Examples of GnRH agonists
- Goserelin
- Buserelin
- Nafarelin
- Histrelin
- Triptorelin
- Leuprolide
GnRH agonists with intermittent dosing
effects, uses
Pulsatile release & 🔼 LH/FSH Uses: 1. Anovulation or Oligospermia 2. Delayed puberty 3. Sexual infantilism
GnRH agonists with continuous dosing
effects
In the beginning: 🔼 LH/FSH (initial worsening of symptoms) ➡️
Continuous stimulation downregulates receptor ➡️
🔽 LH/ FSH
GnRH agonists with continuous dosing
uses
In 👱🏽♀️: 1. Estrogen receptor +ve breast cancer 2. Fibroids 3. Endometriosis In👨🦰: 1. Prostate cancer DoC: goserelin
GnRH agonists with intermittent dosing
Side effects
S/E: 1. Multiple gestation 2. Ovarian cyst 3. Ovarian cancer CI: 🤰
GnRH antagonists &
GnRH agonists with continuous dosing
side effects
In 👨🦰: 1. Impotence 2. Gynecomastia 3. Osteoporosis In 👱🏽♀️: due to 🔽 estrogen 1. Hot flashes 2. Vaginal atrophy 3. Osteoporosis CI: 🤰
GnRH antagonists
effects and examples
🔽 LH/FSH 1. Granirelix 👵🏽 2. Abarelix 3. Cetrorelix: fibroids 4. Dagarelix: prostate cancer 5. Elagolix (recent and different): endometriosis CI: 🤰
GnRH antagonists
uses
- To prevent premature ovulation with ovarian stimulation protocol
- Cetrorelix: endometriosis, fibroids
- Dagarelix: prostate cancer
- Elagolix: endometriosis
Estradiol
• Metabolised in liver to estrone & estriol (can be synthesized by peripheral tissues)
• Cannot be used for therapeutic purpose due to high 1st pass metabolism and poor oral absorption
📝: estrogen 🔽LDL/🔼HDL but does not 🔽 cardiovascular related ☠️
Synthetic estrogen
1. Ethinyl estradiol: M/C 🔼 oral bioavailability 2. Mestronol: Activated in liver to ethyl estradiol 3. Stilbesterol: S/E: 🔼 risk of vaginal cancer in offspring ➡️ not used
Estrogen uses
- Combined OCP
- Hormone Replacement Therapy GRT:
• 1° ovary failure. Eg., Turner’s syndrome
• post menopausal symptoms:
a) 🔽 vasomotor symptoms:
Main aim of HRT (hot flushes)
b) Vaginal dryness - Post menopausal osteoporosis:
prophylaxis and Rx
Estrogen
side effects
- Uterine bleeding
- Gall stones (like somatostatin analogues)
- 🤢, 🤮
- 🔼 coagulation factors ➡️ thrombosis and DVT
- Na+/H2O retention ➡️ edema
- Worsens bp and migraine
- 🔼 risk of uterine cancer but 🔽 risk of colon cancer, ovarian cancer
Progesterone types
1. Progesterone derivatives: Poor inhibitors of ovulation 2. Testosterone derivatives 3. Spironolactone derivatives Both are potent inhibitors of ovulation
Progesterone derivatives
uses
- HRT
- Premenstrual syndrome
- Threatened abortion
- Diagnosis of estrogen secretion:
Progesterone given for 5-7 days, then stopped: if bleeding +ve then estrogen +ve - Good effect on uterus:
Endometriosis, DUB, endometrial cancer