Hexarelin — examorelin

Hexarelin is a Growth Hormone Releasing Peptide (GHRP). These are a group of synthetic compounds that mimic the effects of ghrelin, a gastrointestinal hormone involved in the regulation of food intake, body composition, and glucose metabolism. Like other GHRPs, hexarelin is an agonist of the growth hormone secretagogue receptor la (GHSRIa). It acts on hypothalamic and pituitary sites to stimulate the release of growth hormone. Hexarelin is a particularly potent member of the GHRP family, capable of substantial increases in serum GH and IGF-1. Compared to its predecessor GHRP-6, hexarelin is significantly more effective at elevating growth hormone, and displays a lower propensity for side effects. This drug is often used in the fitness community for fat loss and muscle gain, or as part of an anti-aging program.

Hexarelin is primarily a growth hormone stimulating drug. However, like many GHRPs, its effect is not entirely selective. It does have some spillover effect onto other pituitary hormones. Most notably, hexarelin has been shown to also slightly increase ACTH (adrenocorticotropic hormone), cortisol, and prolactin levels. In each case, the intensity appears to be dose dependent. During studies with hexarelin, the drug did not cause a significant issue with regard to side effects, however. While these hormones were elevated during administration, they remained within the normal range in most cases. Hexarelin is also noted for increasing appetite. Anecdotally, however, this effect is less pronounced than it is with many of the other GHRPs.

Hexarelin has been studied for its potential cardioprotective effects. This may be in part mediated by its binding to both GHSRIa and CD36 receptors in tissues of the cardiovascular system. The latter affinity is not noted in ghrelin, and thus is unique to certain synthetic growth hormone releasing peptides. Hexarelin has been studied in several human clinical trials for this. These investigations found the drug to be well tolerated, and among other things, to increase cardiac output and left ventricular ejection fraction. Research suggests it may hold therapeutic potential with cardiovascular diseases such as cardiac fibrosis, ischemic heart disease, cardiac dysfunction, and atherosclerosis. More research will be needed before hexarelin can be widely adopted for such application.

Brand name Hexarelin, Examorelin

Hexarelin Kev Points

  • Mild Increase in Appetite
  • Strong Effect on GH
  • Slight Elevations in Cortisol/Prolactin
  • Rapid Desensitization

Hexarelin History

Hexarelin was first described in 1992 by R. Deghenghi et al. Between 1999 and 2002, this drug was the subject of several investigations on human subjects. Much of the research was focused on its potential to treat GH deficiency and its possible cardioprotective effects. Though these early results appeared to be favorable, this drug has not been pushed through for approval as a medicine. Further research appears to have been halted in the mid 2000s, so the commercial future of this GHRP is unclear. Hexarelin is on the World Anti-Doping Agency's (WADA) list of prohibited substances. Screening for this drug began on a large scale during the 2014 Winter Olympics in Sochi. It is now detectable, at least for a short window after use, during routine urine analysis. A blood sample is not required.

Structural Characteristics of Hexarelin

Hexarelin is a synthetic hexapeptide with the chemical name His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2.This is a short peptide chain of 6 amino acids, which is relatively stable. Hexarelin has a half-life in serum of 50-58 minutes. It displays a poor level of bioavailability via oral (.2%) and intranasal (4-6%) administration. Injection is preferred.

Hexarelin Warnings

Hexarelin is an unapproved new drug. A thorough understanding of its safety and propensity for side effects in humans is lacking at this time.

This drug should be used with care in epileptic patients. Obesity, uncontrolled hypothyroidism, hyperglycemia, or elevated plasma fatty acids may impair the effectiveness of hexarelin. This drug should never be used during pregnancy, with cancer, a history of cancer, diabetic retinopathy, sclerosing diseases of the liver or lungs, intracranial hypertension, or uncontrolled diabetes.

Hexarelin How Supplied

Hexarelin is widely available on the underground or gray market. It is typically prepared in multi-dose vials containing 2 mg or 5 mg of dry lyophilized powder. This is reconstituted with a diluent (sterile water or bacteriostatic water) before use.

Hexarelin Side Effects (General)

Common side effects to hexarelin therapy include flushing, sweating, sleepiness, reduced REM sleep, increased Gl motility, and increased appetite. Also frequently reported are adverse effects typically associated with other types of growth hormone therapy, such as water retention (edema), joint pain (arthralgias), carpal tunnel syndrome, and numbness or tingling in the extremities. Note that the incidence of side effects tends to be lower with GHRP therapy as compared to traditional hGH. This is because GH/IGF-1 release is subject to endogenous synthesis, and as such the drug is less amenable to overdosing.

Hexarelin Side Effects (Injection site)

The subcutaneous administration of this drug may cause redness, itching, pain, or lumps at the site of injection. Injection site redness and discomfort is sometimes reported with intramuscular injection as well.

Hexarelin Side Effects (Impaired glucose tolerance)

Hexarelin may reduce insulin sensitivity and raise blood sugar levels. This may occur in individuals without preexisting diabetes or impaired glucose tolerance.

Hexarelin Administration

Hexarelin may be given orally, via intranasal administration, subcutaneous (SC) injection, intramuscular (IM) injection, or IV infusion. However, given its high cost and lower bioavailability via other routes, injection is used almost exclusively.

This drug has not been approved for use in humans. Prescribing guidelines are unavailable.

When used for physique- or performance-enhancing purposes, hexarelin is usually administered at a dosage of 0.05 to 0.2 mg (50-200 meg) per injection. This may be given 1 -2 times daily. If single episode dosing is preferred, this is taken before sleep. Day dose (if used) is taken on an empty stomach, 30-60 minutes before a meal. This is to preserve optimal GH release, as elevated plasma fatty acids and/or glucose may blunt the GH elevating effects of GHRPs. Total daily dosage generally does not exceed 400 meg.

It is common to taper up the dosage, beginning with only 50 meg per injection. This may be increased by 50 meg every several days, until a stable peak dosage is reached.

The efficacy of doses above 200 meg remains unclear. In studies giving hexarelin via IV infusion, the drug seemed to approach its maximum effect at about 2 meg/kg of bodyweight. This dose was also only incrementally better than 1 meg/kg, suggesting the point of maximum cost effectiveness is somewhere between 1-2 meg/kg. This would equate to an individual dosage of 100-200 meg for a person of 220 lbs. So no more than 400 meg per day seems reasonable if giving the drug on two instances, and no more than 200 meg with single episode dosing. Significantly more than this might be wasteful, and possibly increase the incidence of side effects.

The body becomes desensitized to the GH-elevating effects of Hexarelin overtime. For this reason, cycles are usually limited to 4 weeks in length. This time frame was chosen out of an abundance of caution. One study that examined desensitization found it does occur sometime after 4 weeks of use, and before 16 weeks (other time points were not examined). It is quite possible that longer cycles can be used without noticing significant downregulation.

Some people alternately opt to use hexarelin in long cycles, but do so on an intermittent schedule. This may be once every 2nd or 3rd day instead of daily. Hexarelin has not been subject to extensive study in humans. As such, a full understanding of the phenomenon of desensitization, and an optimal intake schedule, are lacking.

After each cycle, a minimum of 4 weeks is taken off of the drug. This period of time has been shown to reverse desensitization to hexarelin's GH-elevating effects.

Hexarelin Combination Therapy

Hexarelin is often combined with a drug from the GHRH (Growth Hormone Releasing Hormone) category, such as sermorelin or CJC-1295. These two drug types alter GH release through two distinct and complimentary mechanisms. Such combination therapy produces substantial synergy with regard to GH release, producing maximum GH elevations that are unobtainable with either drug alone.

Hexarelin Availability

Hexarelin is not available as a prescription drug product. It is sold exclusively as a "research compound" or gray market supplement. Note that the quality of gray market products can be difficult to assure.

References

Wlliam Llewellyn (2017) - Anabolics

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