How to inject Sermorelin

Corpas E, Harman SM, Pineyro MA, Roberson R, Blackman MR · 1992

This landmark study showed that twice-daily GHRH (sermorelin) injections in older men completely restored their GH and IGF-1 levels to match those of young men. After just 14 days, the age-related hormone decline was reversed, suggesting that the pituitary gland can still respond—it just needs the right signal.

Khorram O, Laughlin GA, Yen SS · 1997

Four months of nightly sermorelin in older adults increased GH, IGF-1, skin thickness, and lean body mass in men. Men also experienced improved insulin sensitivity, well-being, and libido. Women showed increased skin thickness but less dramatic metabolic effects, highlighting gender differences in response.

Vittone J, Blackman MR, Busby-Whitehead J, et al. · 1997

Six weeks of nightly sermorelin increased nocturnal GH release and improved some measures of muscle strength in healthy elderly men. The study suggested that once-daily dosing helps, but twice-daily dosing may be more effective for maximizing benefits.

Russell-Aulet M, Jaffe CA, Demott-Friberg R, Barkan AL · 1999

This study proved that aging causes reduced GHRH output from the hypothalamus—not just a tired pituitary. The pituitary still responds well to GHRH stimulation in elderly people, which is why sermorelin works: it provides the signal the aging hypothalamus no longer sends strongly enough.

Sigalos JT, Pastuszak AW, Allison A, Khera M · 2017

Men taking sermorelin combined with GHRPs three times daily showed significant increases in IGF-1 levels (from 160 to 239 ng/mL on average). The study confirmed that growth hormone secretagogues are effective for raising IGF-1 in adults seeking to improve body composition.

Prakash A, Goa KL · 1999

Sermorelin is the shortest synthetic fragment of growth hormone-releasing hormone that retains full biological activity. A single intravenous 1 mcg/kg dose is a rapid, relatively specific provocative test for growth hormone deficiency, and once-daily subcutaneous 30 mcg/kg at bedtime raised height velocity over 12 months in some prepubertal children with idiopathic deficiency. Intravenous single doses and repeated once-daily subcutaneous doses were well tolerated; transient facial flushing and pain at the injection site were the most commonly reported adverse events.

US Food and Drug Administration · 2013

FDA's regulatory record for sermorelin. GEREF injection 0.5 and 1.0 mg base/vial is NDA 20-443, held by EMD Serono and initially approved on September 26, 1997, indicated for the treatment of idiopathic growth hormone deficiency in children with growth failure; GEREF injection 0.05 mg base/amp is NDA 19-863, initially approved December 28, 1990, indicated for evaluating the ability of the pituitary somatotroph to secrete growth hormone. EMD Serono notified FDA in letters dated July 11 and December 2, 2008 that the products were being discontinued and requested withdrawal of the applications; approval of both NDAs was withdrawn effective June 18, 2009. FDA determined that neither product was withdrawn from sale for reasons of safety or effectiveness.

Sigalos JT, Pastuszak AW · 2018

Review of clinical studies of growth hormone secretagogues in humans. Secretagogues promote pulsatile release of GH that remains subject to negative feedback and can prevent supra-therapeutic GH levels and their sequelae, in contrast to exogenous GH whose drawbacks are believed to be due in part to impaired regulatory feedback. Across the available studies secretagogues improved growth velocity in children, stimulated appetite, improved lean mass in wasting states and in obese individuals, increased fat-free mass and improved sleep, and were well tolerated, with some concern for increases in blood glucose from decreased insulin sensitivity. The authors note that few long-term, rigorously controlled studies exist.

Iranmanesh A, Lizarralde G, Veldhuis JD · 1991

Twenty-one healthy men aged 21-71 of near-normal body weight were sampled every 10 minutes for 24 hours and analysed by deconvolution. At a normal body mass index, each decade of increasing age attenuated the GH production rate by 14% and the GH half-life by 6%; age and body mass index together accounted for more than 60% of the variability in 24-hour GH production rates.

Van Cauter E, Plat L, Copinschi G · 1998

In normal young adults a major GH secretory episode occurs shortly after sleep onset, in temporal association with the first period of slow-wave sleep; in men approximately 70% of daily GH output occurs during early sleep. The sleep-onset GH pulse is caused by a surge of hypothalamic GHRH release coinciding with a circadian period of relative somatostatin disinhibition, and there is a linear relationship between the amount of slow-wave sleep and the amount of concomitant GH secretion. GHRH itself promotes NREM and slow-wave sleep through central mechanisms. During ageing, slow-wave sleep and GH secretion decline with the same chronology.

Bowers CY, Reynolds GA, Durham D, Barrera CM, Pezzoli SS, Thorner MO · 1990

Eighteen normal men received GH-releasing peptide (GHRP-6) alone and combined with GHRH. Submaximal GHRP doses plus 1 mcg/kg GHRH stimulated GH release synergistically, which the authors take as evidence that GHRP and GHRH act independently through separate mechanisms. Mild facial flushing lasting 1 to 3 minutes occurred in 16 of the 18 subjects who received GHRH.

Park C, Yang I, Woo J, Kim S, Kim J, Kim Y, Park S · 2003

In healthy subjects given a 100 g oral glucose load 30 minutes before an intravenous GHRH bolus, pretreatment with glucose significantly suppressed GHRH-induced GH secretion. Acute hyperglycaemia stimulates hypothalamic somatostatin release, which in turn suppresses GH secretion from the anterior pituitary; the suppression was independent of beta-adrenergic tone.

Walker RF · 2006

Editorial contrasting sermorelin with recombinant human GH in age-management practice. Because rhGH is given as a subcutaneous bolus, the amount entering the circulation is not controlled by normal feedback mechanisms, so tissue exposure to elevated concentrations is persistent and may eventually lead to tachyphylaxis and reduced efficacy. Sermorelin instead stimulates the patient's own pituitary by binding specific receptors to increase production and secretion of endogenous GH. The molecule was marketed for years for children with growth retardation but could not compete with rhGH and was withdrawn as a therapeutic entity by the manufacturer; off-label prescribing of sermorelin is not prohibited by federal law.

Cunha SR, Mayo KE · 2002

GHRH stimulates GH secretion from somatotroph cells of the anterior pituitary via a pathway in which the GHRH receptor activates adenylyl cyclase and increases cAMP production. GH secretagogues bind a distinct G protein-coupled receptor that activates phospholipase C and raises calcium and diacylglycerol rather than cAMP; co-activation of the two receptors roughly doubled the cAMP response to GHRH alone.

Alba M, Salvatori R · 2004

GHRH is necessary for the proliferation of the somatotropic cells of the anterior pituitary and for the synthesis and secretion of GH. It is released by the hypothalamus into the portal hypophysial circulation and binds a membrane surface receptor, the GHRH receptor, expressed by the somatotropic cells; inactivating mutations of that receptor are a relatively common cause of inherited isolated GH deficiency.

Serono Laboratories / RxList (WebMD) · 2001

Repeated subcutaneous treatment: the most common treatment-related adverse event, in about 1 patient in 6, is a local injection reaction of pain, swelling or redness. Other treatment-related events occurred individually at under 1% — headache, flushing, dysphagia, dizziness, hyperactivity, somnolence and urticaria. Intravenous diagnostic use: flushing of the face, injection site pain, redness and/or swelling, nausea, headache, vomiting, dysgeusia, pallor and tightness in the chest. A large proportion of patients develop anti-GRF antibodies at least once during treatment. GEREF was discontinued in the US in 2008 and FDA no longer hosts the label for either NDA 19-863 or NDA 20-443; this is a publisher's reproduction of it, not an FDA-hosted document.