Growth hormone fuels childhood growth and helps maintain tissues and organs throughout life. It’s produced by the pea-sized pituitary gland — located at the base of the brain. Beginning in middle age, however, the pituitary gland slowly reduces the amount of growth hormone it produces.
This natural slowdown has triggered an interest in using synthetic human growth hormone (HGH) as a way to stave off some of the changes linked to aging, such as decreased muscle and bone mass.
If you’re skeptical, good. There’s little evidence to suggest HGH can help otherwise healthy adults regain youth and vitality. Alternatively, HGH treatments may increase the risk of other medical conditions. Experts recommend against using HGH to treat aging or age-related conditions.
Do some adults need HGH treatment?
Adults who have a growth hormone deficiency — not the expected decline in growth hormone due to aging — might be prescribed synthetic HGH by their health care provider.
Growth hormone deficiency is usually caused by a benign tumor on the pituitary gland (pituitary adenoma) or by treatment of an adenoma with surgery or radiotherapy.
For adults who have a growth hormone deficiency, injections of HGH can:
- increase exercise capacity;
- increase bone density;
- increase muscle mass;
- decrease body fat.
HGH treatment is also approved to treat adults with AIDS- or HIV-related growth hormone deficiency that causes the irregular distribution of body fat.
How does HGH treatment affect healthy older adults?
Studies of healthy adults taking human growth hormone are limited and contradictory. Although it appears that human growth hormone can increase muscle mass and reduce the amount of body fat in healthy older adults, the increase in muscle doesn’t translate into increased strength. It isn’t clear if human growth hormone provides other benefits to healthy adults.
What are the risks of HGH treatment?
HGH treatment might cause a number of side effects for healthy adults, including:
- Carpal tunnel syndrome;
- increased insulin resistance;
- type 2 diabetes;
- swelling in the arms and legs (edema);
- joint and muscle pain;
- for men, enlargement of breast tissue (gynecomastia);
- increased risk of certain cancers.
Clinical studies of HGH treatment in healthy older adults have been relatively small and short in duration, so there’s little to no information about the long-term effects of HGH treatment.
Does HGH come in pill form?
HGH treatment is approved in the United States only for the treatment of growth hormone deficiency — and related problems associated with HIV infection. HGH is only effective if administered as an injection.
There’s no pill form of human growth hormone available. Some dietary supplements that claim to boost levels of HGH come in pill form, but research doesn’t show a benefit. HGH is considered a controlled substance by the Food and Drug Administration.
What is Ipamorelin?
Ipamorelin is a peptide that can stimulate the pituitary gland to produce a spike in growth hormone levels. This type of peptide is called Growth Hormone Secretagogues (GHS). It was initially developed to speed up the recovery of gastrointestinal function in patients after bowel surgery. However, it was discontinued due to ineffectiveness.
Bodybuilders and athletes use GHS peptides in an attempt to improve their physique and performance despite the scarcity of scientific evidence to support such claims.
Ipamorelin acts as a GHS by triggering the receptors for the hunger hormone (ghrelin) in the brain, just like MK-677 (Ibutamoren). They are called growth hormone secretagogue receptors (GHS-R) and most of them are concentrated in the hypothalamus.
Normally, ghrelin binds to them and sends a signal from the hypothalamus to the pituitary gland that stimulates the release of human growth hormone (HGH).
Ipamorelin has a selective effect on the GHS-R and studies reveal that it can cause a spike in HGH levels in both animals and humans. These effects have led to further clinical trials as well as the popularity of this peptide as a potential performance-enhancing drug.
The original drug was developed by Novo Nordisk and Helsinn Therapeutics and then clinically tested for the treatment of postoperative ileus. There were 2 large human trials with 117 and 320 patients each, but neither showed any benefits after 7-10 days of administration. Nevertheless, the trials showed a good safety profile for short-term use.
Sermorelin Acetate
Sermorelin acetate (sermorelin) is the acetate salt of an amidated 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 or GRF) consisting of 44 amino acid residues. The structural formula for sermorelin acetate is:
The free base of sermorelin has the empirical formula C 149 H 246 N 44 O 42 S and a molecular weight of 3,358 daltons.
Sermorelin is a sterile, non-pyrogenic, lyophilized powder intended for subcutaneous injection after reconstitution with Sodium Chloride Injection, USP. The reconstituted solution has a pH of 5.0 to 5.5.
Sermorelin is available in vials. The quantitative composition per vial is:
- 0.5 mg vial: Each vial contains 0.5 mg sermorelin (as the acetate) and 5 mg mannitol. The pH is adjusted with dibasic sodium phosphate and monobasic sodium phosphate buffer.
- 3.0 mg vial: Each vial contains 3.0 mg sermorelin (as the acetate) and 5 mg mannitol. The pH is adjusted with dibasic sodium phosphate and monobasic sodium phosphate buffer.
Ipamorelin vs Sermorelin
Sermorelin is another peptide, an analog of growth hormone-releasing hormone (GHRH). It has the shortest half-life of all GHS – 10-20 minutes. In contrast to other GHS, it doesn’t bind to GHS-R but directly stimulates the pituitary gland into producing a spike of growth hormone.
Comparison of Ipamorelin and Sermorelin
When compared to Ipamorelin, Sermorelin has been extensively studied in humans because it is successfully employed in the diagnosis of growth hormone deficiency (GHD). Thus it is also FDA-approved for this purpose.
According to human trials, Sermorelin leads to an increase in HGH for 2 hours after administration. Its effects are subject to a negative feedback mechanism by somatostatin, and thus it can’t push HGH levels above physiological norms.
Nevertheless, daily injections can lead to a notable increase in mean GH levels, IGF-1 levels, and a minor increase in lean body mass after long-term use. However, unlike Ipamorelin, Sermorelin doesn’t lead to any changes in fat mass and body composition.
Sermorelin acetate benefits are also slightly less selective towards HGH stimulation and might lead to minor increases in luteinizing (LH) and follicle-stimulating hormones (FSH).
Adverse effects after Sermorelin administration may include local injection reaction, nausea, and facial flushing.
What for and how Ipamorelin is used?
Ipamorelin is a white powder that must be reconstituted with bacteriostatic water before use. Similar to other peptides, it has to be injected subcutaneously and injection sites must be rotated to prevent lipodystrophy.
The dosage used in medical settings and clinical trials is 0.03 mg per kg of body weight administered intravenously twice daily.
In its off-label use for anti-aging or bodybuilding, it is used in doses of 200 to 300 µg taken subcutaneously 2-3 times per day due to the short half-life.
Currently, Ipamorelin is not manufactured by any worldwide pharmaceutical company. It can be purchased from websites that do not require a prescription and the average cost for a 15mg vial is over $200. Doing so carries risk since it is impossible to guarantee the quality of the purchased product.
The internet is full of reviews that attribute different effects such as:
- muscle and strength gains;
- fat loss;
- higher energy levels;
- improved skin;
- increased bone mineral density;
- repaired joints and ligaments;
- Better sleep;
- Improved sex drive;
- Slowed aging.
However, there is nothing but modest evidence from animal studies that may suggest only a few of the claims above.
In fact, Ipamorelin is more likely to cause fat gain rather than fat loss according to studies
Benefits and Side Effects of Ipamorelin Injections
The main effect of Ipamorelin is a spike in GH levels which occurs about 40 minutes after injection, according to clinical studies.
However, the spike is followed by a rapid decline and HGH levels return back to baseline after 3 hours. That’s because the half-life of Ipamorelin is less than 2 hours when injected subcutaneously and even shorter when taken intravenously.
The main side effects of ipamorelin are increased appetite and fat gain.
Evidence from experiments with rats has found that 4x daily administration of ipamorelin leads to an increase in mean HGH levels, IGF-1 levels, and weight gain. Rat studies have also suggested that it may increase nitrogen balance and reduce muscle wasting, similarly to HGH.
Apart from the outcome of ipamorelin treatment on postoperative ileus, other effects haven’t been studied in humans. Human trials haven’t shown any side effects in the short term, except nausea and gastrointestinal problems.
The main side effect observed in animal trials is increased appetite and weight gain, including fat gain. Whether Ipamorelin might increase the risk of obesity in humans is unknown.
The increase in appetite might be related to the agonistic effect of Ipamorelin on ghrelin receptors which may stimulate hunger, as well as the increase in insulin production observed in animal experiments.
Sermorelin Therapy Benefits
- The goal of sermorelin therapy is to get your pituitary gland to produce more HGH naturally. This can reverse or stop many issues that develop due to HGH deficiency. Sermorelin therapy benefits include:
- Increase in muscle mass development after exercise, faster recovery from strenuous exercise, increased energy and endurance, better strength, and joint and muscle pain relief for patients with arthritis and chronic pain.
- Improved cognitive function (better mental clarity), better vision, better bone health, enhanced immune system, stronger heart, and improved cardiovascular function.
- Fat reduction (especially abdominal fat), restored vitality, youthful and glowing skin, thicker hair and nails, and an improved sense of well-being.
- Accelerated healing from wounds or surgery, increase in libido and better sexual performance, improved sleep quality, and better mood.
HGH vs Ipamorelin
In comparison to HGH therapy, Ipamorelin has a significantly shorter half-life and leads to a short-lived spike in GH levels. According to trials, subcutaneous injection of HGH leads to a peak after 4 hours and an increase in HGH levels which lasts up to 15-20 hours.
Comparison of Ipamorelin and HGH
HGH therapy increases lean body weight but decreases abdominal and visceral fat. In comparison, Ipamorelin increases body fat, especially at the start of the therapy.
Unlike growth hormone therapy, Ipamorelin and other GHS might fail to induce similar increases in HGH and IGF-1 in chronically ill patients when compared to healthy individuals. Studies in animal models of diabetes and obesity have shown that Ipamorelin is not as effective in increasing IGF-1 as in healthy rats.
Ipamorelin and other GHS are also less convenient than HGH therapy. They require 2-3 daily injections to stimulate a sufficient increase in growth hormone levels in healthy individuals. In comparison, HGH can be taken once daily.
Furthermore, there is no evidence to confirm that Ipamorelin might provide benefits for bone density in humans, similar to the effects seen after the growth hormone replacement therapy.
GHRP-2 (pralmorelin) and GHRP-6 vs Ipamorelin
GHRP-2 and GHRP-6 are also peptides that trigger the ghrelin receptor (GHS-R) and lead to a spike in growth hormone levels. They notably increase mean GH levels and IGF-1 levels after prolonged use. The half-life of GHRP-2 is about 30 minutes and about 2-3 hours for GHRP-6.
All 3 peptides can increase bone mineral content in rats. However, the increase in mineral content is mainly due to growth stimulation and an increase in total body weight. The experiments reported that bone mineral density remained the same.
Similar to Ipamorelin, GHRP-2 and GHRP-6 lead to an increase in appetite and weight gain.
Furthermore, GHRP-2 and GHRP-6 are not as selective as Ipamorelin. They stimulate GH as well as other hormones such as ACTH and cortisol.
In comparison, studies have shown that Ipamorelin is highly selective and the only hormone it increases is HGH.
Please get in touch with our team of experts to learn more about the therapy.