Sermorelin

What is Sermorelin?

Sermorelin is a synthetic drug with a structure of a 29 amino acid peptide that represents a fragment of the naturally occurring GHRH.

More specifically, this sequence is the shortest version of GHRH that still retains full functionality to stimulate growth hormone synthesis in the pituitary gland.

This is why sermorelin is also known as GRF 1-29 (Growth Hormone-Releasing Factor 1-29).

Thanks to its ability to stimulate hGH synthesis, sermorelin has been used for the diagnosis and treatment of growth hormone-deficient children. Here is what you should know about it as a medication:

• The peptide was first developed as a medication by the pharmaceutical company Merck Serono (EMD Serono in the United States and Canada).
• The medication contains an acetate salt form of sermorelin, known as sermorelin acetate, which improves its stability and absorption.
• Sermorelin acetate was first approved for human use by the U.S. Food and Drug Administration (FDA) in 1990 under the brand name Geref. It was used as an intravenous injection to diagnose patients with growth hormone deficiency (GHD).
• In 1997, Geref was approved for subcutaneous injection to normalize growth rate in children with growth delays and poor growth (growth failure) due to GHD and other conditions.
• Manufacturing of Geref by Merck Serono ceased in 2008 due to production issues, unrelated to safety concerns.
• Sermorelin acetate is now available as a generic medication in the U.S. and can be obtained from pharmacies with a medical prescription. It is available only for subcutaneous administration.

Semorelin has also shown beneficial metabolic effects for adults with and without adult-onset growth hormone insufficiency when administered as once-daily or twice-daily injections.

It is known for its excellent safety profile, primarily causing only local side effects at the injection site. The peptide is available only as an injection, due to its peptide structure which limits its absorption and viability when administered via other routes.

How Does Sermorelin Work?

Sermorelin acetate for injection increases hGH by structurally mimicking natural GHRH. GHRH is the main natural hormone responsible for stimulating hGH release from the anterior pituitary gland.

By binding to GHRH receptors on the pituitary gland, sermorelin promotes the synthesis and release of hGH. This release is rapid and significant but is limited by sermorelin’s short half-life of approximately 10 minutes, as reported in clinical trials.

Typically administered via injection, the pharmacokinetics allow for a quick onset of action, which is useful in both diagnostic settings and for therapeutic use.

Following administration, sermorelin induces a spike in hGH levels within minutes. The effect on hGH levels is transient, lasting about 2 hours post-injection, correlating with sermorelin’s short half-life.

Even a single daily dose can significantly increase mean hGH levels over 12 hours. For example, a 6-week trial reported an increase in 12-hour mean hGH levels (as measured by the area under the curve) by 82% from baseline.

Over longer periods, sermorelin administration can nearly double mean hGH levels, A 16-week trial reported that sermorelin at a standard dose of 10 mcg/kg of body weight can lead to a 107% increase in mean hGH compared to baseline.

By elevating hGH levels, sermorelin also leads to an increase in its main anabolic mediator in the human body, called insulin-like growth factor-1.

More specifically, serum hGH stimulates the production of IGF-1 in different tissues, and also in the liver which releases it within the circulation. For example, the increase in intramuscular IGF-1 levels under the effects of hGH is thought to play a potential role in muscle growth and anabolism.

For example, the aforementioned 16-week trials reported a 28% increase in mean serum insulin-like growth factor-1 levels from baseline amongst elderly men.

What are The Benefits of Sermorelin Injections?

One of the main sermorelin benefits, which are also the reasons why the peptide is approved for human use, is that it effectively increases hGH levels and height in children with poor growth.

Sermorelin therapy successfully increased growth velocity in several clinical trials with children, albeit it was a less effective drug when compared to subcutaneous growth hormone therapy.

However, studies in adults have also suggested promising sermorelin benefits. Here are some of the most notable ones:

• Improved Body Composition, Muscle Growth, and Lean Body Mass – Four months of sermorelin therapy with a prescribed dose of 10mg per kg of body weight was reported to cause a +2.78 lbs (+1.26 kg) mean increase in lean mass, coupled with increased nitrogen intake which indicates elevated anabolism. This benefit was observed only in male volunteers.

• Anti-aging effects – The four-month study revealed that the peptide significantly boosts skin thickness and enhances overall appearance in both men and women. These improvements are primarily attributed to the increased proliferation of skin cells which leads to greater collagen synthesis. This process contributes to healthier and more resilient skin.

• Hormone levels – Clinical trials indicate that the peptide may cause a modest rise in luteinizing hormone (LH) and follicle-stimulating hormone (FSH) levels in men. However, these hormonal changes did not significantly affect testosterone levels in this specific study.

Having higher serum growth hormone levels may also have benefits for energy levels, cell regeneration, and bone density. However, long-term trials are lacking and there is no data to suggest these sermorelin benefits yet.

Risks and Common Side Effects of Sermorelin Therapy

Sermorelin is generally safe for use in humans, based on clinical data and FDA authorization for treating growth failure in children. However, it does have some potential sermorelin side effects, based on the available clinical data:

• Injection reactions: These include injection site pain, swelling, discomfort, bleeding, induration, and redness. They are usually minor and resolve on their own.
• Facial flushing
• Allergic reactions: Symptoms of allergic reactions can include rash, hives, itching, difficulty breathing, chest tightness, and swelling of the mouth, face, lips, or tongue. Severe reactions require immediate medical attention.
• Lipohypertrophy: Local side effect if injections are repeatedly administered at the same injection spot.
• Temporary rise in serum lipid levels: Reported in the 16-week study in adults.

There is also concern about sermorelin’s potential to elevate hGH and IGF-1 levels, which might increase the risk of cancer by promoting the growth of malignant cells. Despite these theoretical risks, extensive research in children has not shown sermorelin side effects that involve promoting cancerous growth.

The peptide is contraindicated for use in people with a history of malignant cancers as well as breast-feeding or pregnant women.

Overall, sermorelin is well tolerated in adults and children when used as recommended. Mild side effects are expected to resolve within a few days. Long-term risks are not well documented but could emerge with future research.

How to use Sermorelin Acetate

What Is the Proper Dosage for Sermorelin?

Sermorelin dosage typically falls into the range of 10-25 mcg per kilogram of body weight, administered daily. This can be divided into one or two injections based on the patient’s medical advice. For the management of adult-onset growth hormone insufficiency, the sermorelin dosage may vary between 1 to 2 mg of the peptide daily, tailored to individual health requirements.

When is Sermorelin Used?

Due to its short half-life, the timing of sermorelin injections is crucial for maximizing effectiveness. Evidence from studies indicates that evening injections are more effective compared to morning ones. For those on a once-daily regimen, injections should ideally be administered in the evening. If prescribed twice daily, the injections should occur before bedtime and early in the morning, several hours before breakfast.

How to Store Sermorelin Peptide?

Sermorelin injections come as a medication vial containing lyophilized powder. In its lyophilized form, the peptide should be stored in a dark, cool, dry place until it is mixed.

The lyophilized powder requires reconstitution before use. For reconstitution, a bacteriostatic water vial—containing 0.9% benzyl alcohol as a preservative—is recommended to enhance shelf life. When the solvent is injected into the peptide vial for reconstitution, it is also important that the needle is directed toward the glass vial wall rather than directly toward the powder.

Once mixed within the medication vial, the solution can be refrigerated at 36 to 46 degrees Fahrenheit (2 to 8 degrees Celsius) and will remain effective for up to 28 days.

How is Sermorelin Peptide Administered?

Sermorelin is suitable for subcutaneous administration rather than as an intramuscular injection or intravenous administration. The subcutaneous method is the most effective administration technique due to the more favorable half-life related to it. It involves administering medications into the fatty layer right under the skin.

Preferred subcutaneous injection sites include:

• The abdominal area, approximately 2 inches away from the navel
• The outer upper arms
• The front outer thighs It’s important to rotate the injection sites regularly to prevent lipodystrophy, a medical condition involving changes in body fat.

Administering sermorelin peptide correctly involves adhering to the following step-by-step instructions:

1. Wash hands thoroughly and use hand sanitizer.
2. Don sterile gloves.
3. Clean the rubber vial stopper with an alcohol swab.
4. Use a sterile syringe to draw the required amount of solution, being careful not to shake or tap the syringe. You may use a bigger needle to penetrate the rubber stopper and withdraw the peptide, before switching to a smaller one for the injection.
5. Cleanse the injection site with an alcohol swab and let it dry.
6. Pinch the skin to create a fold and insert the needle at a 45-degree angle, or at a 90-degree angle if using insulin needles.
7. Inject the solution slowly and wait a few seconds before removing the needle.
8. Safely dispose of the needle and syringe in a sharps container.
9. Apply an alcohol swab to the injection site to manage any bleeding.

These steps help ensure the injection is administered safely and effectively.

For those considering sermorelin therapy, it is crucial to follow proper injection techniques under the guidance of experienced medical professionals. Consequently, trained patients can self-administer injections on a daily basis.

Our clinic specializes in sermorelin treatment, offering customized dosage plans and thorough oversight to address any side effects and maximize treatment benefits. Contact us today to schedule a consultation and learn how sermorelin can benefit you.