Geref® (sermorelin acetate) synthetic growth hormone-releasing hormone profile

akn · Jun 22, 2014

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Sermorelin is a synthetic analog of endogenous growth
hormone-releasing hormone (GHRH or GRF). Sermorelin is
a portion of this polypeptide hormone, specifically consisting
of the first 29 of its 44 amino acid structure. As its name
states very clearly, the biological activity of GHRH is to
stimulate the synthesis of growth hormone, which occurs in
the pituitary gland. Studies have shown, however, that the
GHRH peptide can be partly truncated without sacrificing its
GH stimulating ability.702 29NH2) was developed based on
this research, and shares the full biological activity of GHRH
with regard to increasing the endogenous production of
growth hormone. Based on its structure and action,
sermorelin is classified as a growth hormone releasing factor
(GHRF) or GH secretagogue.
Sermorelin, as an acetate salt, is used in clinical medicine
for two primary applications. The first is to diagnose
pituitary deficiency. The procedure involves measuring the
serum growth hormone response over a 1-2 hour window
following a single IV infusion of sermorelin acetate.703 An
intact hypothalamo-pituitary-growth-hormone axis should
yield a predictable increase in the GH level. The second
common medical application is the treatment of growth
hormone deficiency in children. As with recombinant growth
hormone medications (rHGH, somatropin), sermorelin
acetate can provide the benefits of sustained elevations in
GH, including enhanced IGF-1 (Insulin-like Growth Factor)
output and increased linear height.704 Sermorelin is a very
specific acting drug, and has no effect on prolactin, LH, FSH,
insulin, cortisol, glucose, glucagon, or thyroid hormone
levels.705 This also lends to its therapeutic potential.
Athletes are interested in sermorelin acetate for the same
reasons they use recombinant human growth hormone. Among
other things, growth hormone has anabolic and anti-catabolic
properties. An elevated GH level may support new muscle
tissue growth, and also enhance strength, energy levels, and
connective tissues. GH is also a potent modulator of fat loss.
The physique- and performance-enhancing properties of
growth hormone are widely accepted by the bodybuilding
and competitive athletic communities, such that rHGH
medications are very popular. Although sermorelin acetate
has a much shorter history of use, it is slowly gaining
acceptance among the community as a viable alternative to
low dose growth hormone injections. It is also presently
popular in anti-aging medicine, where again it serves as an
alternative to growth hormone in the treatment of age-related
GH deficiency (“somatopause”).
When comparing this drug to recombinant human growth
hormone, sermorelin acetate does appear to be less effective
under normal therapeutic conditions. During clinical studies,
fewer patients on average seem to respond favorably to
therapy in contrast to somatropin, and for those that do
respond the improvements are often less pronounced.706 Still,
it would be a mistake to exclude sermorelin acetate as a
viable therapeutic option. For example, studies have found
that sermorelin acetate can result in significant increases in
height velocity in children with GH deficiency.707
Furthermore, these improvements seem to be well sustained
after one year of therapy.708 709 Antibodies to GHRH do
develop in some patients during extended therapy, and may
impair the potency of the drug.710 The full biological
relevance of this antibody reaction, however, remains
unclear.
Sermorelin is approved in the United States for the
treatment of GH deficiency in children only. Prolonged
studies treating adults with somatopause are lacking. One
investigation looked at the effects of 2 mg sermorelin acetate
per day for 6 weeks in a group of eleven healthy elderly men
(aged 64 to 76) with low circulating IGF-1 levels.711
Various measures of body composition and performance
were recorded at the beginning and end of the study. As a
result of treatment, there was a significant increase in
nocturnal GH output, area under peak GH release, and GH
peak amplitude. This was accompanied by improvements in
certain measures of strength and endurance including upright
row, shoulder press, and abdominal crunch. Many other
measures did not reach statistical significance, however,
which may reflect study limitations such as small population
sizes and a short duration of intake.
Another investigation looked at the effects of sermorelin
acetate in a group of HIV+ men with lipodystrophy.712 HIV
lipodystrophy tends to be characterized by the abnormal
distribution of fat cells and suppressed levels of growth
hormone. During this investigation, 31 men aged 18 to 60
years were given 1 mg of sermorelin acetate or placebo by
subcutaneous injection twice daily for 12 weeks. The
primary outcome of the study was a significant increase in
serum IGF-1 in the sermorelin acetate group (104 ng/mL vs 6
ng/mL). This was accompanied by a favorable increase in
lean body mass (+.9 kg vs -.3 kg) and decrease in visceral
and subcutaneous fat. Sermorelin acetate was well tolerated,
and did not result in any change in other health markers
including blood pressure, cholesterol, triglycerides, insulin,
or hemoglobin. None of the participants discontinued therapy
due to side effects.
Sermorelin acetate could be viewed as offering a therapeutic
advantage over recombinant growth hormone in some cases,
in that it is less likely to result in GH excess.This is due to
the fact that it relies on the body’s own hormone synthesis
instead of exogenous supplementation. Thus, normal IGF-1
feedback inhibition is likely to help set a natural limit to the
growth hormone stimulating effect.713 As such, hormone
levels are more easily controlled with sermorelin acetate.
Under normal conditions, while sermorelin will produce
significant elevations in GH and IGF-1, these levels should
not exceed the high end of the normal range.714 Given this
feature, sermorelin acetate may be a more comfortable option
for some patients. Studies seem to support this notion, finding
many of the same physical and metabolic benefits of GH
injections, without reporting the same issues with insulin
resistance, fluid retention, or muscle pain.
History:
Sermorelin acetate was developed during the early 1980s,
and approved for prescription sale by the U.S. Food and
Drug Administration in 1997. It was introduced to market
under the brand name Geref Diagnostic by the international
biotechnologies firm Serono. As the name implies, it was
primarily developed as a diagnostic tool. It was specifically
used for evaluating potential pituitary deficiency in GH
production. Given its effect on growth hormone levels,
however, the drug was also approved by the FDA for the
treatment of GH deficiency in children. Geref was never
widely prescribed, however, especially for uses relating to
childhood GH deficiency, where it was never able to
compete with somatropin. Serono ultimately discontinued the
product in October 2008, citing supply issues with the active
pharmaceutical ingredient.715 This was the only company
manufacturing sermorelin as a commercial product in the
United States, thus it is no longer available as a stock
pharmacy item.The active material sermorelin acetate is still
made by at least one licensed supplier, however, so the drug
remains available here as a compounded medicine.
How Supplied:
Geref Diagnostic was supplied in ampules containing dry
lyophilized sermorelin acetate, equivalent to 50 mcg of
sermorelin. This was reconstituted with a sterile diluent
(also supplied) before use. Generic compounded versions of
this medication typically contain between 3.0 and 7.5 mg of
dry lyophilized sermorelin acetate in a multi-dose vial.
Reconstitution before use is also required.
Structural Characteristics:
Sermorelin acetate is the acetate salt of a synthetic 29–amino
acid peptide (GRF 1-29 NH 2) that corresponds to the
amino-terminal segment of the naturally occurring human
growth hormone-releasing hormone (GHRH) with 44 amino
acid residues.
Warnings:
Sermorelin acetate should be used with care in epileptic
patients. Obesity, uncontrolled hypothyroidism,
hyperglycemia, or elevated plasma fatty acids may impair the
effectiveness of sermorelin. Therapy should be discontinued
in patients treated for childhood GH deficiency once the
epiphyses have closed.
Side Effects:
The most common side effects to sermorelin acetate therapy
are injection site reactions such as pain, redness, and
swelling. During clinical trials, this occurred in
approximately 17% of patients. Less common side effects
include difficulty swallowing, itching, dizziness, flushing,
headache, nausea, vomiting, altered sense of taste,
restlessness, and sleepiness.
Administration:
When used medically for the treatment of idiopathic growth
hormone deficiency in prepubertal children with growth
failure, sermorelin acetate is administered by subcutaneous
injection at a dosage of 0.03 mg per kg of body weight once a
day at bedtime. Injection sites should be rotated to avoid
irritation or the buildup of scar tissue. When used to evaluate
pituitary capacity in adults, a single intravenous infusion of
1.0 mcg/kg body weight is administered in the morning after
an overnight fast.This is followed by 60-120 minutes of
periodic blood sampling to measure pituitary hormone
output.
When used for physique- or performance-enhancing
purposes, sermorelin acetate is given by subcutaneous
injection. It is typically administered at a dosage of 0.2 to 0.5
mg per day (200-500 mcg), which is given before sleep.
Studies, however, do suggest that this drug is more effective
when given twice daily.716 Therefore, it is often preferred to
divide the total daily dosage into two applications,one in the
morning and one in the evening. Cycles of sermorelin acetate
usually last between 8 and 12 weeks. Some anti-aging
practitioners will prescribe the medication for much longer
periods of time, however, and cycles lasting 24-48 weeks
are not uncommon.The hope is that the extended maintenance
of youthful growth hormone levels will yield more
significant physiological changes.
Availability Trends:
Given its low financial value on global pharmaceutical
markets, sermorelin acetate is subject to limited availability
worldwide. The preparations most commonly found diverted
for bodybuilding use include those made by private
compounding pharmacies in the United States, and those sold
by gray market research chemical supply companies.

By WL

Presser · Mar 27, 2016

great read, i am not familiar with this peptide ghrh or grf. solid information on its profile and usage

Geref® (sermorelin acetate) synthetic growth hormone-releasing hormone profile

akn

Musclechemistry Member

Presser

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