GHRP-2 Key Points
- Mild/Moderate Increase in Appetite
- Strong Effect on GH
- Moderate Elevations in Cortisol
- Moderate Elevations in Prolactin
This agent has a fairly long history for a class of agents that is regarded as relatively new from an approval and sales perspective. GHRP-2 was discovered by Dr. C. Y. Bowers at Tulane University, and first disclosed back in 1993. Dr. Bowers is a prominent figure in the field of GH secretagogues, and is credited with discovering or providing key research on many of these compounds. Dr. Bowers partnered with Keken Pharmaceuticals to develop GHRP-2 as a drug product. After a series of clinical trials, the drug (as pralmorelin) gained approval in Japan for the diagnosis of growth hormone deficiency. It was launched in 2005 under the brand name GHRP Kaken 100 Injection.
In 2012, this agent was also granted orphan drug status in the United States for the same application, where it is marketed by Sella Pharmaceuticals. GHRP-2 has also been investigated in several clinical trials for the treatment of short stature in children. However, though early results seemed promising, no such product has yet been approved for this application.
GHRP-2 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. This drug is now specifically detectable, at least for a short window after use, during routine urine analysis. A blood sample is not required.
How is GHRP-2 Supplied
GHRP Kaken 100 Injection is supplied in a multi-dose vial containing a single 100 meg dose.Compounded medicine and gray market versions typically contain 5 mg or 10 mg of dry lyophilized powder in a multi-dose vial. This is reconstituted with a diluent (sterile water or bacteriostatic water) before use.
Structural Characteristics of GHRP-2
GHRP-2 is a synthetic hexapeptide with the chemical name D-alanyl-3-(2-naphthyl)-D-alanyl-L-alanyl-L-tryptophyl-D-phenylalanyl-L-lysinamide hydrochloride, dihydrochloride. This is a short peptide chain, which is relatively stable. GHRP-2 has a half-life in serum of approximately 30 minutes. It displays a poor but viable level of bioavailability via oral administration (.3-1%). Intranasal bioavailability is high at 53%, though injection is the preferred route of administration.
GHRP-2 should be used with care in epileptic patients. Obesity, uncontrolled hypothyroidism, hyperglycemia, or elevated plasma fatty acids may impair the effectiveness of GHRP-2. 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.
GHRP-2 Side Effects (General)
Common side effects to GHRP-2 therapy include flushing, sweating, sleepiness, 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.
GHRP-2 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.
GHRP-2 Side Effects (Impaired glucose tolerance)
GHRP-2 may reduce insulin sensitivity and raise blood sugar levels. This may occur in individuals without preexisting diabetes or impaired glucose tolerance.
GHRP-2 may be given orally, via intranasal administration, subcutaneous (SC) injection, or intramuscular (IM) injection. However, given its high cost and lower bioavailability via other routes, injection is used almost exclusively.
When used for physique- or performance-enhancing purposes, GHRP-2 is usually administered at a dosage of 0.1 to 0.3 mg (100-300 meg) per injection. This may be given 1 -3 times daily. If single episode dosing is preferred, this is taken before sleep. Day dose(s) are taken on an empty stomach, 30-60 minutes before feeding. This is to preserve optimal GH release, as elevated plasma fatty acids and/or glucose may blunt the GH elevating effects of GHRP-2. Total daily dosage generally does not exceed 900 meg.
It is common to taper up the dosage, beginning with 100 meg per injection. The dosage may then be increased in increments of 50 meg every 3-7 days, until a stable dosage is reached.
Cycles of GHRP-2 usually last 3-4 months in length, though programs of 6 months or longer are not uncommon. Although desensitization to GHRPs may occur over time, this drug appears to maintain an acceptable level of effectiveness during longer cycles.
GHRP-2 Combination Therapy
Drugs of the GHRP class are often combined with those of 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. Note that injections of GHRP-2 are typically reduced to no more than 200 meg each during combination therapy, and 600 meg total per day.
Below is an example of combination therapy with GHRP-2
GHRP-2: 100-200mcg 1-3x daily
Sermorelin: 100-200mcg 1-3x daily
GHRP-2 is available as a prescription drug product under the brand name GHRP Kaken 100 Injection. It is also widely available in the United States as a compounded medicine, and is often offered at anti-aging and hormone replacement clinics. Lastly, the drug is widely sold as a gray market "research compound" as well, though the quality of gray market GHRP-2 products can be difficult to assure.
Wlliam Llewellyn (2017) - Anabolics