Sermorelin Acetate Injection

Sermorelin should not be used in patients with certain conditions where the risks outweigh potential benefits. Key contraindications and precautions include:

Hypersensitivity: Any history of allergy to sermorelin or to any of the formulation’s excipients is a contraindication to therapy.^[7] Signs of an allergic reaction (such as rash, hives, or anaphylaxis) preclude further use.

Active Malignancy: Because growth hormone can promote cell proliferation, sermorelin is contraindicated in patients with active cancers or tumors. GH stimulation may theoretically encourage tumor growth, so this therapy is avoided in anyone with an active malignancy or a history of cancer that is not in complete remission.^[8] (Patients in long-term remission should only be considered for therapy on a case-by-case basis in consultation with an oncologist.)

Intracranial Lesions: Sermorelin is not recommended for patients whose GH deficiency is caused by an intracranial tumor or lesion. Clinical trials of sermorelin did not include patients with pituitary tumors or other brain lesions causing hormone deficiencies, so safety and efficacy in this group are not established.^[9] Alternative treatments should be considered in such cases.

Uncontrolled Hypothyroidism: An underactive thyroid must be managed before starting sermorelin. Untreated hypothyroidism blunts the physiological response to sermorelin, as normal thyroid hormone levels are needed for optimal GH production.^[10] Patients should have thyroid function assessed and corrected prior to and during sermorelin therapy to ensure effectiveness.

Pregnancy: Use of sermorelin in pregnancy is not advised (see Pregnancy section below). Women who are pregnant or planning to become pregnant should avoid this medication unless clearly needed, due to unknown fetal risks.^[11]

Lactation: Caution is urged in breastfeeding mothers (see Pregnancy section). It is not known if sermorelin is excreted in human milk.^[12]

All patients should be evaluated by a healthcare professional to ensure none of the above contraindications or precautions apply. Sermorelin therapy is indicated only for individuals with demonstrated need (such as GH deficiency) – it is not intended for use in patients with normal GH levels, and it is legally prohibited to distribute GH or its secretagogues for anti-aging or athletic enhancement purposes. Providers will weigh the potential risks (e.g. tumor growth, metabolic effects) against benefits before initiating therapy in each patient.

Before starting sermorelin, patients should inform their healthcare provider of all medications and supplements they are taking, as some can interfere with sermorelin’s efficacy or safety. Notable drug interactions and related considerations include:

Glucocorticoids: Concurrent high-dose glucocorticoid (corticosteroid) therapy may inhibit the GH response to sermorelin^[6] Steroids such as prednisone can suppress pituitary growth hormone release, potentially reducing sermorelin’s effectiveness. Patients on chronic corticosteroids may require dose adjustments or careful monitoring of IGF-1 levels to ensure sermorelin is having the desired effect.

Somatostatin Analogs: Medications that mimic somatostatin (the hormone that opposes GH release) can counteract sermorelin. For example, octreotide (used in acromegaly or certain tumors) or other drugs that increase somatostatin activity may blunt the GH rise from sermorelin. These combinations should generally be avoided or approached with caution, as sermorelin may be ineffective if somatostatin analogs are on board.

Thyroid Medications: The thyroid status of the patient significantly influences sermorelin’s activity. As noted, untreated hypothyroidism will interfere with sermorelin’s effects.^[10] Conversely, starting or stopping thyroid hormone replacement could alter the growth hormone response. While levothyroxine itself is not a direct antagonist to sermorelin, thyroid levels need to be stable. In addition, anti-thyroid drugs (e.g. propylthiouracil) that induce a hypothyroid state may diminish sermorelin’s efficacy.^[13] Close coordination of thyroid treatment with sermorelin therapy is recommended.

Insulin and Blood Sugar: GH can antagonize insulin’s actions, so diabetics on insulin or oral hypoglycemics should be closely monitored when initiating sermorelin. Although not a direct “drug-drug interaction,” increased GH/IGF-1 levels may raise blood glucose. Adjustments to diabetes medications might be needed to maintain glycemic control. Patients should report significant changes in blood sugar to their provider.

Other Medications: Certain central nervous system medications used in GH stimulation tests – for example, dopamine agonists (like L-Dopa) or arginine – can affect GH release. While these are typically only relevant in diagnostic settings, any drug affecting pituitary function or hormone levels could theoretically impact sermorelin therapy. Nonsteroidal anti-inflammatory drugs (NSAIDs) such as high-dose aspirin or indomethacin have been reported to alter GH release in some contexts^[13], though this is more pertinent to GH stimulation testing than chronic therapy.

In summary, any medication that significantly alters pituitary-hypothalamic function or hormonal balance should be brought to the attention of the prescribing practitioner. Lab test interactions: Note that sermorelin can cause transient changes in certain lab values – for instance, it may increase serum levels of markers like inorganic phosphorus or alkaline phosphatase.^[9] Healthcare providers and laboratory personnel should be aware the patient is on sermorelin, so that lab results are interpreted appropriately. As always, patients are advised not to start or stop any other prescription drug, over-the-counter product, or supplement without consulting their healthcare provider during sermorelin therapy.

Common Side Effects: The most frequent adverse effects of sermorelin are related to its injection route. Approximately one in six patients (up to ~16%) experience localized reactions at the injection site.^[4] These reactions may include pain, swelling, redness, or mild bruising at the site of the subcutaneous injection. Such local side effects are usually transient and self-limited. Rotating injection sites with each dose can help minimize irritation. Patients should be taught proper injection technique to reduce the risk of injection-site injury or infection.

Systemic Side Effects: Sermorelin is generally well tolerated, and because it triggers endogenous hormone release, systemic side effects tend to be mild for most patients. Possible side effects include: headache, flushing (warmth or redness of the face), dizziness or light-headedness, nausea, or transient fatigue/somnolence.^[4] Some individuals report a temporary feeling of restlessness or hyperactivity, while others may feel sleepy after the injection – these responses vary. A temporary “strange” or metallic taste in the mouth has also been noted in some cases immediately after injection, but this is not harmful.^[13] Most of these reactions, if they occur, subside as the body adjusts to therapy.

Rare or Serious Adverse Reactions: Serious reactions to sermorelin are uncommon. Unlike recombinant GH therapy, sermorelin has not been strongly associated with severe fluid retention, insulin resistance, or joint pain in the short term, though long-term data are limited. Rarely, some patients may experience difficulty swallowing or the sensation of a lump in the throat (dysphagia) after injections^[4] – if this occurs, medical advice should be sought, as it could signify an allergic or unusual response. Allergic reactions to sermorelin are possible (as with any peptide). While no widespread anaphylactic reactions were reported in clinical trials,^[4] there has been an isolated case of a severe local hypersensitivity reaction characterized by intense redness, swelling, and urticaria (hives) at injection sites in a patient who developed anti-sermorelin antibodies. Patients should stop the medication and seek prompt medical care if they experience generalized rash, hives, chest tightness, or difficulty breathing.

Immunogenicity: A notable proportion of patients (approximately 70% or more) may develop low-titer antibodies to sermorelin with chronic use.^[4] These are antibodies directed against the GHRH analog. However, current evidence suggests that the development of such antibodies does not significantly reduce the drug’s effectiveness or cause any distinct adverse reaction profile.^[4] In other words, most patients with detectable anti-sermorelin antibodies continue to respond to therapy, and the antibodies may disappear over time even if treatment continues. Nonetheless, healthcare providers may monitor for any signs of reduced efficacy over the long term.

Metabolic Considerations: Because sermorelin increases GH and IGF-1 levels, it may have subtle effects on metabolism that warrant attention. In some patients, insulin sensitivity may be reduced, as GH tends to raise blood glucose by antagonizing insulin. While frank hyperglycemia is uncommon, those with underlying insulin resistance or diabetes should be monitored for any change in glucose control. Likewise, sermorelin therapy can unmask hypothyroidism in susceptible individuals – clinical studies in children noted a small percentage of patients developed hypothyroidism during GH/GHRH therapy and required thyroid hormone replacement.^[10] For this reason, periodic thyroid function tests are recommended, and any emerging thyroid deficiency should be treated. Unlike high-dose GH administration, sermorelin is not known to cause significant fluid retention, carpal tunnel syndrome, or organomegaly in the doses used for deficiency treatment; it aims to restore normal physiologic levels rather than create supraphysiologic levels.

Patients are encouraged to report any persistent or concerning symptoms to their healthcare provider, even if not listed here. Most side effects of sermorelin are mild, but ongoing monitoring (including periodic blood tests for IGF-1 and other parameters) is part of therapy to ensure safety. If side effects are troublesome, dose adjustments or discontinuation may be considered. Overall, when used in appropriate patients under medical supervision, sermorelin is typically well tolerated, and serious adverse effects are rare.^[5]

Pregnancy: Sermorelin is categorized as Pregnancy Category C (under the older FDA classification system).^[11] This indicates that animal reproduction studies have shown an adverse effect on the fetus, and there are no adequate, well-controlled studies in pregnant women. In animal studies, very high doses of sermorelin (several times the human dose) produced minor variations in fetal development in rats and rabbits.^[11] It is not known whether sermorelin can cause fetal harm when administered to a pregnant woman or if it can affect reproductive capacity. Use in pregnancy is not recommended unless the potential benefit justifies the potential risk to the fetus.^[11] In practice, sermorelin is almost never used during pregnancy, since treating chronic growth hormone deficiency can typically be deferred and other therapies (if needed) would be chosen if GH support was truly required. Women of childbearing potential should inform their physician if they become pregnant or intend to become pregnant while on sermorelin. If pregnancy occurs, the healthcare provider will likely discontinue sermorelin due to the lack of safety data.

Breastfeeding: It is not known whether sermorelin acetate is excreted in human breast milk.^[12] Because many drugs and small peptides can be present in breast milk, caution is advised. There is also insufficient information on the effects of sermorelin on a nursing infant. Given the essential role of GH/IGF-1 in growth and metabolism, any exposure of a newborn to sermorelin via milk is of uncertain significance. Therefore, breastfeeding is generally not advised while receiving sermorelin, or the drug should be used only if clearly needed and if the mother’s healthcare provider determines that the benefits outweigh the potential risks to the infant.^[12] Nursing mothers on sermorelin should closely collaborate with their healthcare providers; an alternative feeding plan for the infant (or alternative therapy for the mother) may be recommended to ensure safety.

In summary, women who are pregnant, breastfeeding, or planning to become pregnant should discuss thoroughly with their doctors before considering sermorelin. In almost all cases, sermorelin therapy will be avoided during pregnancy and lactation to err on the side of caution, unless there are special circumstances and a consensus that treatment is necessary. All decisions should be individualized and made in conjunction with an obstetrician or maternal-fetal medicine specialist as appropriate.

Proper storage of sermorelin is vital to maintain its stability and potency. This compounded peptide must be handled and stored according to pharmacy instructions and general guidelines for biopharmaceuticals:

Refrigeration: Store unmixed (dry) sermorelin vials in a refrigerator at 36–46°F (2–8°C) when possible.^[14] Refrigeration is recommended for long-term stability of peptide medications. Do not freeze the vials, as freezing can damage the peptide structure. Keep the medication in its original vial and box until use, to protect it from light. If refrigeration is temporarily unavailable (e.g. during shipping or travel), the lyophilized powder can remain at room temperature for short periods (generally up to 72 hours) without significant loss of potency, but it should be chilled again as soon as feasible. Do not expose sermorelin to high heat or direct sunlight.

After Reconstitution: Once you have mixed (reconstituted) sermorelin with diluent, it must be kept refrigerated at 2–8°C and should be used within the time frame specified by the pharmacy. Under refrigerated conditions, the reconstituted solution is typically stable for a limited period (often 1–2 weeks for many compounded peptides, though some preparations may remain stable up to 30 days or longer – follow your compounding pharmacy’s beyond-use date). Because no preservatives other than bacteriostatic water are present, sterility and potency beyond the recommended usage period cannot be guaranteed. It is usually advised to mark the date of mixing on the vial and discard any unused portion after the indicated expiration or beyond-use date.

Handling Precautions: Before mixing and drawing up doses, wash hands and swab the vial stopper with alcohol to maintain sterility. Use only the diluent provided (or recommended) for reconstitution. Do not shake the vial vigorously – gentle swirling is sufficient to dissolve the powder. Inspect the solution: if it is discolored or contains particulate matter that does not dissolve, do not use it. Prepare injections on a clean flat surface.

Disposal: Keep all medication and supplies out of reach of children and pets. Dispose of used needles and syringes in a FDA-cleared sharps disposal container – never in the regular trash. For any unused or expired sermorelin vials, follow pharmacy instructions for disposal. Do not flush medications down the toilet or pour them into drains. If you need to dispose of medication and do not have a take-back program or instructions, mix the residual drug with an unpalatable substance (like coffee grounds or cat litter), seal it in a bag, and discard in the trash, per FDA guidelines, to prevent accidental exposure.

Always refer to the specific storage guidelines provided with your compounded prescription, as formulation variations can exist. Some compounded sermorelin products may specify storage at room temperature prior to mixing – but in general, keeping the product refrigerated is safest to ensure maximum shelf life and efficacy.^[14] If you have any doubts about whether the medication has been stored properly or if it was left unrefrigerated for an extended time, contact the pharmacy or your healthcare provider for advice. Proper storage and handling will help maintain sermorelin’s effectiveness throughout your treatment course.