Ipamorelin is a growth hormone secretagogue from the GHRP class (Growth Hormone Releasing Peptides). This is a third generation GHRP. It was developed alongside a series of other modified derivatives of a first generation GHRP. Like other GHRPs, ipamorelin binds and activates growth hormone secretagogue receptor 1a (GHSRIa). This supports the pulsatile release of growth hormone, and in turn potentially IGF-1. As a stimulator of GH release, ipamorelin appears to be moderately potent. It is stronger than GHRP-6, but less effective than GHRP-2. However, it does have unique properties regarding selectivity that make this drug of interest, discussed below. In the fitness community, ipamorelin is most often used for the support of muscle growth and fat loss. Ipamorelin is highly selective for the stimulation of growth hormone release. This means minimal spillover effects on other systems. For starters, ipamorelin has been shown to only slightly increase ACTH (adrenocorticotropic hormone) and cortisol levels. These increases are far less notable than with the non-selective GHRPs to come before it, and no more in intensity than the natural hormone GHRH. Further, this effect does not appear to be dose dependent. Related side effects are unlikely. Further, ipamorelin appears to have negligible effect on appetite. Drugs of the GHRP class often mimic ghrelin's tendency to strongly stimulate hunger, which can be problematic while dieting. This makes ipamorelin more practical for this purpose.
Ipamorelin Key Points
- Negligible effect on Appetite
- Moderate Effect on GH
- Negligible effect on Cortisol
- Negligible effect on Prolactin
Ipamorelin was first described in 1998 by Raun et al. It was developed during a series of experiments modifying a preceding hormone called GHRP-l. The researchers were looking for other small molecule GHRPs that could display acceptable potency and higher selectivity for GH release. Ipamorelin was identified as a prime candidate. It was subsequently subject to a series of animal and finally human experiments. So far, the drug has demonstrated a high level of safety and efficacy. However, we have not yet seen full clinical trials. Ipamorelin is not an approved drug at this time, and remains the subject of research and experimentation only.
Ipamorelin 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 Ipamorelin
Ipamorelin is a synthetic pentapeptide with the chemical name Aib-His-D-2-Nal-D-Phe-Lys-NH2. It has a terminal half-life of about 120 minutes, and displays an acceptable level of bioavailability (21%) via intranasal administration, though IM and SC injection routes are generally preferred.
Ipamorelin 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 ipamorelin. 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.
How is Ipamorelin Supplied
Ipamorelin 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.
Ipamorelin Side Effects (General)
Common side effects to ipamorelin include flushing, sweating, headache, increased Gl motility, and sleepiness. 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.
Ipamorelin 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.
Ipamorelin Side Effects (Impaired glucose tolerance)
Ipamorelin may reduce insulin sensitivity and raise blood sugar levels. This may occur in individuals without preexisting diabetes or impaired glucose tolerance.
This drug is not available as a pharmaceutical product. Prescribing guidelines are unavailable.
Ipamorelin 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.
When used for physique- or performance-enhancing purposes, ipamorelin is usually administered at a dosage of 0.2 to 0.3 mg (200-300 meg) per injection.This may be given 1 -3 times daily. If single episode dosing is preferred, this is taken before sleep, sometimes at a higher dose (up to 500 mcg). Day dose(s) are 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 900 mcg.
It is common to taper up the dosage, beginning with only 200 meg per injection. This may be increased by 50 mcg every few days, until a stable peak dosage is reached. Cycles of ipamorelin usually last 3-4 months in length, though programs of 6 months or longer are not uncommon.
Ipamorelin Combination Therapy
Ipamorelin (a GHRP) is often combined with a drug from the GHRH (Growth Hormone Releasing Hormone) class, 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.
Ipamorelin 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.
Wlliam Llewellyn (2017) - Anabolics