JohnC
02-27-2015, 07:26 PM
A Brief Summary of Dosing and Administration
Dosing GHRPs
The saturation dose in most studies on the GHRPs (GHRP-6, GHRP-2, Ipamorelin & Hexarelin) is defined as either 100mcg or 1mcg/kg.
What that means is that 100mcg will saturate the receptors fully, but if you add another 100mcg to that dose only 50% of that portion will be effective. If you add an additional 100mcg to that dose only about 25% will be effective. Perhaps a final 100mcg might add a little something to GH release but that is it.
So 100mcg is the saturation dose and you could add more up to 300 to 400mcg and get a little more effect.
A 500mcg dose will not be more effective then a 400mcg, perhaps not even more effective then 300mcg.
The additional problems are desensitization & cortisol/prolactin side-effects.
Ipamorelin is about as efficacious as GHRP-6 in causing GH release but even at higher dose (above 100mcg) it does not create prolactin or cortisol.
GHRP-6 at the saturation dose 100mcg does not really increase prolactin & cortisol but may do so slightly at higher doses. This rise is still within the normal range.
GHRP-2 is more efficacious then GHRP-6 at causing GH release but at the saturation dose or higher may produce a slight to moderate increase in prolactin & cortisol. This rise is still within the normal range although doses of 200 - 400mcg might make it the high end of the normal range.
Hexarelin in some is the most efficacious otherwise it is equipotent or a little less so then GHRP-2 at causing an increase in GH release. However it has the highest potential to also increase cortisol & prolactin. This rise will occur even at the 100mcg saturation dose. This rise will reach the higher levels of what is defined as normal.
Desensitization
GHRP-6 can be used at saturation dose (100mcg) three or four times a day without risk of desensitization.
GHRP-2 at saturation dose several times a day will not result in desensitization.
Hexarelin has been shown to bring about desensitization but in a long-term study the pituitary recovered its sensitivity so that there was not long-term loss of sensitivity at saturation dose. However dosing Hexarelin even at 100mcg three times a day will likely lead to some down regulation within 14 days.
If desensitization were to ever occur for any of these GHRPs simply stopping use for several days will remedy this effect.
Chronic use of GHRP-2 at 100mcg dosed several times a day every day will not cause pituitary problems, nor significant prolactin or cortisol problems, nor desensitize.
GHRH
Now Sermorelin, GHRH (1-44) and GRF(1-29) all are basically GHRH and have a short half-life in plasma because of quick cleavage between the 2nd & 3rd amino acid. This is no worry naturally because this hormone is secreted from the hypothalamus and travels a short distance to the underlying anterior pituitary and is not really subject to enzymatic cleavage. The release from the hypothalamus and binding to somatotrophs (pituitary cells) happens quickly.
However when injected into the body it must circulate before finding its way to the pituitary and so within 3 minutes it is already being degraded.
That is why GHRH in the above forms must be dosed high to get an effect.
GHRH analogs
All GHRH analogs swap Alanine at the 2nd position for D-Alanine which makes the peptide resistant to quick cleavage at that position. This means analogs will be more effective when injected at smaller dosing.
The analog tetra or 4 substituted GRF(1-29) sometimes called CJC w/o the DAC or referred to by me as modified GRF(1-29) has other amino acid modifications. They are a glutamine (Gln or Q) at the 8-position, alanine (Ala or A) at the 15-position, and a leucine (Leu or L) at the 27-position.
The alanine at the 8th position enhances bioavailability but the other two amino substitutions are made to enhance the manufacturing process (i.e. create manufacturing stability).
For use in vivo, in humans, the GHRH analog known as CJC w/o the DAC or tetra (4) substituted GRF(1-29) or modified GRF(1-29) is a very effective peptide with a half-life probably 30+ minutes.
That is long enough to be completely effective.
The saturation dose is also defined as 100mcg.
Problem w/ Using any GHRH alone
The problem with using a GHRH even the stronger analogs is that they are only highly effective when somatostatin is low (the GH inhibiting hormone). So if you unluckily administer in a trough (or when a GH pulse is not naturally occurring) you will add very little GH release. If however you luckily administer during a rising wave or GH pulse (somatostatin will not be active at this point) you will add to GH release.
Solution is GHRP + GHRH analog
The solution is simple and highly effective. You administer a GHRH analog with a GHRP. The GHRP creates a pulse of GH. It does this through several mechanisms. One mechanism is the reduction of somatostatin release from the hypothalamus, another is a reduction of somatostatin influence at the pituitary, still another is increased release of GHRH from the brain and finally GHRPs act on the same pituitary cells (somatotrophs) as do GHRHs but use a different mechanism to increase cAMP formation which will further cause GH release from somatotroph stores.
GHRH also has a way of reciprocally reinforcing GHRPs action.
The result is a synergistic GH release.
The GH is not additive it is synergistic. By that I mean:
If GHRH by itself will cause a GH release valued at 2
and GHRP itself will cause a GH release valued at 5
Together the GH is not 7 (5+2) it turns out to say 16!
A solid protocol
A solid protocol would be to use a GHRP + a GHRH analog pre-bed (to support the nightime pulse) and once or twice throughout the day.
For anti-aging, deep restful restorative sleep, the once at night dosing is all you need. For an adult aged 40+ it is enough to restore GH to youthful levels.
However for bodybuilding or fatloss or injury repair multiple dosings can be effective.
The GHRH analog can be used at 100mcg and as high as you want without problems.
The GHRP-2 can always be used at 100mcg w/o problems but a dose of 200mcg will probably be fine as well.
Again desensitization is something to keep an eye on particularly with the highest doses of GHRP-2 and all doses of Hexarelin.
So 100 - 200mcg of GHRP-2 + 100 - 500mcg+ of a GHRH analog taken together will be effective.
This may be dosed several times a day to be highly effective.
A solid approach is a bit more conservative at 100mcg of GHRP-2 + 100mcg of a GHRH analog dosed either once, twice, three or four times a day.
When dosing multiple times a day at least 3 hours should separate the administrations.
The difference is once a day dosing pre-bed will give a youthful restorative amount of GH while multiple dosing and or higher levels will give higher GH & IGF-1 levels when coupled with diet & exercise will lead to muscle gain & fatloss.
Dose w/o food
Administration should ideally be done on either an empty stomach or with only protein in the stomach. Fats & carbs blunt GH release. So administer the peptides and wait about 20 minutes (no more then 30 but no less then 15 minutes) to eat. AT that point the GH pulse has about hit the peak and you can eat what you want.
Dosing GHRPs
The saturation dose in most studies on the GHRPs (GHRP-6, GHRP-2, Ipamorelin & Hexarelin) is defined as either 100mcg or 1mcg/kg.
What that means is that 100mcg will saturate the receptors fully, but if you add another 100mcg to that dose only 50% of that portion will be effective. If you add an additional 100mcg to that dose only about 25% will be effective. Perhaps a final 100mcg might add a little something to GH release but that is it.
So 100mcg is the saturation dose and you could add more up to 300 to 400mcg and get a little more effect.
A 500mcg dose will not be more effective then a 400mcg, perhaps not even more effective then 300mcg.
The additional problems are desensitization & cortisol/prolactin side-effects.
Ipamorelin is about as efficacious as GHRP-6 in causing GH release but even at higher dose (above 100mcg) it does not create prolactin or cortisol.
GHRP-6 at the saturation dose 100mcg does not really increase prolactin & cortisol but may do so slightly at higher doses. This rise is still within the normal range.
GHRP-2 is more efficacious then GHRP-6 at causing GH release but at the saturation dose or higher may produce a slight to moderate increase in prolactin & cortisol. This rise is still within the normal range although doses of 200 - 400mcg might make it the high end of the normal range.
Hexarelin in some is the most efficacious otherwise it is equipotent or a little less so then GHRP-2 at causing an increase in GH release. However it has the highest potential to also increase cortisol & prolactin. This rise will occur even at the 100mcg saturation dose. This rise will reach the higher levels of what is defined as normal.
Desensitization
GHRP-6 can be used at saturation dose (100mcg) three or four times a day without risk of desensitization.
GHRP-2 at saturation dose several times a day will not result in desensitization.
Hexarelin has been shown to bring about desensitization but in a long-term study the pituitary recovered its sensitivity so that there was not long-term loss of sensitivity at saturation dose. However dosing Hexarelin even at 100mcg three times a day will likely lead to some down regulation within 14 days.
If desensitization were to ever occur for any of these GHRPs simply stopping use for several days will remedy this effect.
Chronic use of GHRP-2 at 100mcg dosed several times a day every day will not cause pituitary problems, nor significant prolactin or cortisol problems, nor desensitize.
GHRH
Now Sermorelin, GHRH (1-44) and GRF(1-29) all are basically GHRH and have a short half-life in plasma because of quick cleavage between the 2nd & 3rd amino acid. This is no worry naturally because this hormone is secreted from the hypothalamus and travels a short distance to the underlying anterior pituitary and is not really subject to enzymatic cleavage. The release from the hypothalamus and binding to somatotrophs (pituitary cells) happens quickly.
However when injected into the body it must circulate before finding its way to the pituitary and so within 3 minutes it is already being degraded.
That is why GHRH in the above forms must be dosed high to get an effect.
GHRH analogs
All GHRH analogs swap Alanine at the 2nd position for D-Alanine which makes the peptide resistant to quick cleavage at that position. This means analogs will be more effective when injected at smaller dosing.
The analog tetra or 4 substituted GRF(1-29) sometimes called CJC w/o the DAC or referred to by me as modified GRF(1-29) has other amino acid modifications. They are a glutamine (Gln or Q) at the 8-position, alanine (Ala or A) at the 15-position, and a leucine (Leu or L) at the 27-position.
The alanine at the 8th position enhances bioavailability but the other two amino substitutions are made to enhance the manufacturing process (i.e. create manufacturing stability).
For use in vivo, in humans, the GHRH analog known as CJC w/o the DAC or tetra (4) substituted GRF(1-29) or modified GRF(1-29) is a very effective peptide with a half-life probably 30+ minutes.
That is long enough to be completely effective.
The saturation dose is also defined as 100mcg.
Problem w/ Using any GHRH alone
The problem with using a GHRH even the stronger analogs is that they are only highly effective when somatostatin is low (the GH inhibiting hormone). So if you unluckily administer in a trough (or when a GH pulse is not naturally occurring) you will add very little GH release. If however you luckily administer during a rising wave or GH pulse (somatostatin will not be active at this point) you will add to GH release.
Solution is GHRP + GHRH analog
The solution is simple and highly effective. You administer a GHRH analog with a GHRP. The GHRP creates a pulse of GH. It does this through several mechanisms. One mechanism is the reduction of somatostatin release from the hypothalamus, another is a reduction of somatostatin influence at the pituitary, still another is increased release of GHRH from the brain and finally GHRPs act on the same pituitary cells (somatotrophs) as do GHRHs but use a different mechanism to increase cAMP formation which will further cause GH release from somatotroph stores.
GHRH also has a way of reciprocally reinforcing GHRPs action.
The result is a synergistic GH release.
The GH is not additive it is synergistic. By that I mean:
If GHRH by itself will cause a GH release valued at 2
and GHRP itself will cause a GH release valued at 5
Together the GH is not 7 (5+2) it turns out to say 16!
A solid protocol
A solid protocol would be to use a GHRP + a GHRH analog pre-bed (to support the nightime pulse) and once or twice throughout the day.
For anti-aging, deep restful restorative sleep, the once at night dosing is all you need. For an adult aged 40+ it is enough to restore GH to youthful levels.
However for bodybuilding or fatloss or injury repair multiple dosings can be effective.
The GHRH analog can be used at 100mcg and as high as you want without problems.
The GHRP-2 can always be used at 100mcg w/o problems but a dose of 200mcg will probably be fine as well.
Again desensitization is something to keep an eye on particularly with the highest doses of GHRP-2 and all doses of Hexarelin.
So 100 - 200mcg of GHRP-2 + 100 - 500mcg+ of a GHRH analog taken together will be effective.
This may be dosed several times a day to be highly effective.
A solid approach is a bit more conservative at 100mcg of GHRP-2 + 100mcg of a GHRH analog dosed either once, twice, three or four times a day.
When dosing multiple times a day at least 3 hours should separate the administrations.
The difference is once a day dosing pre-bed will give a youthful restorative amount of GH while multiple dosing and or higher levels will give higher GH & IGF-1 levels when coupled with diet & exercise will lead to muscle gain & fatloss.
Dose w/o food
Administration should ideally be done on either an empty stomach or with only protein in the stomach. Fats & carbs blunt GH release. So administer the peptides and wait about 20 minutes (no more then 30 but no less then 15 minutes) to eat. AT that point the GH pulse has about hit the peak and you can eat what you want.