Jasen Bruce
Member
Here is some basic information regarding the different GH secretagogues
Hormones involved and related analog drugs
•Growth Hormone Releasing Hormone:
1. Sermorelin
2. Tesamorelin
•Ghrelin:
1. GHRP
2. Ipamorelin
3. Ibutamoren
•Somatostatin
•Growth Hormone
1. Recumbent human growth hormone (rHGH)
•Insulin-Like Growth Factor-1
1. recumbent IGF-1
Growth Hormone Releasing Hormone (GHRH)
•Produced by hypothalamus
•Stimulates GH synthesis and RELEASE
•Binds to the GHRH-R in pituitary
•Short half-life ~12 min
•Increases # of somatotropes AND amount of GH secreted from each
•No down regulation of GH
Ghrelin
•Bind to GHRP-R (“Ghrelin receptor”) in pituitary to release GH
•Reduce inhibition by Somatostatin at pituitary
•Distinct and separate path than GHRH
•Stimulate GHRH production from hypothalamus
•Inhibit Somatostatin production from hypothalamus
Somatostatin (SS)
•“SS” aka Growth Hormone Inhibiting Hormone (GHIH) or Somatotropin Release-Inhibiting Factor (SRIF)
•Produced primarily by hypothalamus
•Inhibits GH synthesis and release
•Makes hypothalamus resistant to stimulation by GHRH and hypoglycemia
•Responsible for pulsatile GH inhibition
•Decreases number of somatotropes, not amount of GH production by each
•Increases with age
Sermorelin
•Geref—Sermorelin Acetate for Injection
•Analog of GHRH - First 29 amino acids
•Used for traditional GH stimulation testing
•T ½ 12 mins. IV or SC
•Up regulates own receptor
•Promotes non-REM slow wave sleep
•Dose: 1,000-2,000mcg SQ qhs
Growth Hormone Releasing Peptides (GHRP)
•Synthetic forms of Ghrelin
•GHRP-1, GHRP-2, GHRP-6, MK-0677,
Hexarelin, Ipamorelin, Ghrelin
•Simple, short-chained amino acid complexes
•Bind to GHRP-R GH
•“Artificial amplification” b/c works with endogenous GHRH
Sermorelin / GHRP-2 / GHRP-6
•Increases prolactin and cortisol
•Significantly increases hunger and gastric emptying
•Cost effective
•GHRPs will start a pulse, and acts synergistically with GHRPs, so there is no need to be concerned about administration timing if you co-administer GHRPs with Sermorelin.
•GHRPs Requires Endogenous Hypothalamic GHRH for Maximal GH Stimulation
–NAUSHIRA PANDYA, ROBERTA DEMOTT-FRIBERG, CYRIL Y. BOWERS, ARIEL L. BARKAN, AND CRAIG A. JAFFE, Journal of Clinical Endocrinology and Metabolism 1998 Vol. 83, No
•Dose: Recon with 7.5mL Bac Water, Inject 0.25mL SQ bid/tid
Sermorelin / Ipamorelin
•For higher GH release than Sermorelin alone
•Ipamorelin like GHRP-2 and GHRP-6, but does not induce hunger, prolactin or cortisol release
•Dose: 500/500mcg SQ qhs. Increase to 1,000/1,000mcg depending on IGF-1 lab results.
Ibutamoren
•Selective agonist of the ghrelin receptor
•Long acting (T ½ 24h)
•Orally active
•Studied in treatment of obesity, bone density and muscle mass
•Dose: 25mg po qd
rHGH vs GHRH / GHRP
•GHRH / GHRP significantly less expensive than rHGH
•HGH overdosing is minimized or completely avoided with GHRH / GHRP
•Tissue exposure to HGH released by the pituitary under the influence of GHRH / GHRP is episodic not “square wave”, preventing tachphylaxis by mimicking normal physiology
•By stimulating the pituitary, GHRH / GHRP preserves more of the growth hormone neuroendocrine axis which fails first during aging
•GHRH / GHRP blocks the cascade of hypophyseal hormone failure that occurs during aging, thereby preserving youthful anatomy and physiology
•GHRH / GHRP provides all the benefits of HGH replacement therapy and more, YET IT’S OFF LABEL USE IS NOT PROHIBITED BY FEDERAL LAW
Commonly Prescribed Protocols I have observed
•Sermorelin
–Weight Loss / Age Management (Inject 1,000 mcg SQ qhs)
–Increase up to 2,000 mcg total daily
–IGF-1 Maintenance protocol 1,000mcg tiw
•GHRP-2/GHRP-6/Sermorelin
–Weight gain and high GH Response (Inject 667/200/500mcg SQ before meals or bid/tid)
–Most significant hunger increase
•Sermorelin/Ipamorelin
–Weight Loss / Age Management / Lean Mass (Inject 500/500 mcg SQ qhs)
–Increase up to 2,000 mcg total daily
–IGF-1 Maintenance protocol 1,000mcg tiw
•Ibutamoren
–Age Management / Fat Loss / Lean Mass Increase (25mg po qd)
–No need for injections
–Long T ½
–Some patients will exhibit hunger
•Patients will not start exhibiting the benefits of GHRT until at least 3 months of being on their program and it usually takes about 6 months to see the full benefits of the therapy.
Contraindications
•Pregnancy
•Malignancy
•History of Malignancy
•Diabetic proliferative retinopathy
•Sclerosing diseases of the liver and lungs
•Benign intracranial hypertension
•Uncontrolled diabetes
Hormones involved and related analog drugs
•Growth Hormone Releasing Hormone:
1. Sermorelin
2. Tesamorelin
•Ghrelin:
1. GHRP
2. Ipamorelin
3. Ibutamoren
•Somatostatin
•Growth Hormone
1. Recumbent human growth hormone (rHGH)
•Insulin-Like Growth Factor-1
1. recumbent IGF-1
Growth Hormone Releasing Hormone (GHRH)
•Produced by hypothalamus
•Stimulates GH synthesis and RELEASE
•Binds to the GHRH-R in pituitary
•Short half-life ~12 min
•Increases # of somatotropes AND amount of GH secreted from each
•No down regulation of GH
Ghrelin
•Bind to GHRP-R (“Ghrelin receptor”) in pituitary to release GH
•Reduce inhibition by Somatostatin at pituitary
•Distinct and separate path than GHRH
•Stimulate GHRH production from hypothalamus
•Inhibit Somatostatin production from hypothalamus
Somatostatin (SS)
•“SS” aka Growth Hormone Inhibiting Hormone (GHIH) or Somatotropin Release-Inhibiting Factor (SRIF)
•Produced primarily by hypothalamus
•Inhibits GH synthesis and release
•Makes hypothalamus resistant to stimulation by GHRH and hypoglycemia
•Responsible for pulsatile GH inhibition
•Decreases number of somatotropes, not amount of GH production by each
•Increases with age
Sermorelin
•Geref—Sermorelin Acetate for Injection
•Analog of GHRH - First 29 amino acids
•Used for traditional GH stimulation testing
•T ½ 12 mins. IV or SC
•Up regulates own receptor
•Promotes non-REM slow wave sleep
•Dose: 1,000-2,000mcg SQ qhs
Growth Hormone Releasing Peptides (GHRP)
•Synthetic forms of Ghrelin
•GHRP-1, GHRP-2, GHRP-6, MK-0677,
Hexarelin, Ipamorelin, Ghrelin
•Simple, short-chained amino acid complexes
•Bind to GHRP-R GH
•“Artificial amplification” b/c works with endogenous GHRH
Sermorelin / GHRP-2 / GHRP-6
•Increases prolactin and cortisol
•Significantly increases hunger and gastric emptying
•Cost effective
•GHRPs will start a pulse, and acts synergistically with GHRPs, so there is no need to be concerned about administration timing if you co-administer GHRPs with Sermorelin.
•GHRPs Requires Endogenous Hypothalamic GHRH for Maximal GH Stimulation
–NAUSHIRA PANDYA, ROBERTA DEMOTT-FRIBERG, CYRIL Y. BOWERS, ARIEL L. BARKAN, AND CRAIG A. JAFFE, Journal of Clinical Endocrinology and Metabolism 1998 Vol. 83, No
•Dose: Recon with 7.5mL Bac Water, Inject 0.25mL SQ bid/tid
Sermorelin / Ipamorelin
•For higher GH release than Sermorelin alone
•Ipamorelin like GHRP-2 and GHRP-6, but does not induce hunger, prolactin or cortisol release
•Dose: 500/500mcg SQ qhs. Increase to 1,000/1,000mcg depending on IGF-1 lab results.
Ibutamoren
•Selective agonist of the ghrelin receptor
•Long acting (T ½ 24h)
•Orally active
•Studied in treatment of obesity, bone density and muscle mass
•Dose: 25mg po qd
rHGH vs GHRH / GHRP
•GHRH / GHRP significantly less expensive than rHGH
•HGH overdosing is minimized or completely avoided with GHRH / GHRP
•Tissue exposure to HGH released by the pituitary under the influence of GHRH / GHRP is episodic not “square wave”, preventing tachphylaxis by mimicking normal physiology
•By stimulating the pituitary, GHRH / GHRP preserves more of the growth hormone neuroendocrine axis which fails first during aging
•GHRH / GHRP blocks the cascade of hypophyseal hormone failure that occurs during aging, thereby preserving youthful anatomy and physiology
•GHRH / GHRP provides all the benefits of HGH replacement therapy and more, YET IT’S OFF LABEL USE IS NOT PROHIBITED BY FEDERAL LAW
Commonly Prescribed Protocols I have observed
•Sermorelin
–Weight Loss / Age Management (Inject 1,000 mcg SQ qhs)
–Increase up to 2,000 mcg total daily
–IGF-1 Maintenance protocol 1,000mcg tiw
•GHRP-2/GHRP-6/Sermorelin
–Weight gain and high GH Response (Inject 667/200/500mcg SQ before meals or bid/tid)
–Most significant hunger increase
•Sermorelin/Ipamorelin
–Weight Loss / Age Management / Lean Mass (Inject 500/500 mcg SQ qhs)
–Increase up to 2,000 mcg total daily
–IGF-1 Maintenance protocol 1,000mcg tiw
•Ibutamoren
–Age Management / Fat Loss / Lean Mass Increase (25mg po qd)
–No need for injections
–Long T ½
–Some patients will exhibit hunger
•Patients will not start exhibiting the benefits of GHRT until at least 3 months of being on their program and it usually takes about 6 months to see the full benefits of the therapy.
Contraindications
•Pregnancy
•Malignancy
•History of Malignancy
•Diabetic proliferative retinopathy
•Sclerosing diseases of the liver and lungs
•Benign intracranial hypertension
•Uncontrolled diabetes
