GHRH

GHRH (GH – releasing hormone)

Growth hormone releasing hormone (GHRH) is a naturally occurring peptide released by nerves, called arcuate neurons, in the hypothalamus. The peptide travels from the hypothalamus to the pituitary gland where it binds to the growth hormone releasing hormone receptor and causes the release of growth hormone (GH). GHRH is critical for proper growth and development, increasing lean body mass and reducing adiposity (fat tissue). GHRH is indirectly responsible for muscle growth and long bone growth, but has also been found to regulate inflammation, mitigate pain, and play an important role in the sleep-wake (diurnal cycle). It is released in a pulsatile manner from the hypothalamus and thus causes the pulsatile release of GH as well. This pattern of release is important to the function of growth hormone and thus to physiology in general.

Sequence: DL-Tyr-DL-Ala-DL-Asp-DL-Ala-DL-xille-DL-Phe-DL.xiThr-DL-Asn-DL-Ser-DL-Tyr-DL- Arg-DL-LYS-DL-Val-DL-Leu-Gly-DL-Gln-DL-Leu-DL-Ser-DL-Ala-DL-Arg-DL-Lys-DL-Leu-DL-Leu- DL-Gln-DL-Asp-DL-xille-DL-Met-DL-Ser-DL-Arg-DL-Gln-DL-Gin-Gly-DL-Glu-DL-Ser-DL-Asn-DL- Gin-DL-Glu-DL-Arg- Gly-DL-Ala-DL-Arg-DL-Ala-DL-Arg-OL-Leu

Molecular Formula: C215H358N72066S

CAS Number: 9064-39-3

Appearance      White powder

Purity (HPLC)     >95%

Store at Coo dry place (-20°C. away From the light)

Administration:

A dosage of 0.2 – 0.3 mcg once daily at bedtime by subcutaneous injection is recommended. It is also recommended that subcutaneous injection sites be periodically rotated.

To prevent possible contamination, wipe the rubber vial stopper with an antiseptic solution before puncturing it with the needle. It is recommended that GHRH be administered using sterile, disposable syringes and needles. The syringes should be of small enough volume that the prescribed dose can be drawn from the vial with reasonable accuracy.

To reconstitute GHRH, inject the diluent into the vial of GHRH aiming the liquid against the glass vial wall. Swirl the vial with a GENTLE rotary motion until contents are dissolved completely. Do not administer GHRH if particles are visible in the reconstituted solution or if the reconstituted solution is cloudy.

Precautions:

GHRH therapy should be carried out under the regular guidance of a physician who is experienced in the diagnosis and management of growth hormone deficiencies.

In clinical studies, the incidence of hypothyroidism during GHRH therapy was 6.5%. In the largest clinical study, 8 of 110 enrolled patients were on thyroid replacement therapy prior to GHRH therapy and an additional 5 after initiating therapy. Untreated hypothyroidism can jeopardize the response to GHRH. Therefore, thyroid hormone determinations should be performed before the initiation and throughout the duration of GHRH therapy. Thyroid hormone replacement therapy should be initiated when indicated.

Patients with growth hormone deficiency secondary to an intracranial lesion were not studied in clinical trials. It is not recommended that such patients be treated with GHRH .

As with the administration of any peptide, local or systemic allergic reactions may occur. P atients should be informed that such reactions are possible and that prompt medical attention should be sought if allergic reactions occur.

Side Effects:

A large proportion of patients develop anti- GRF antibodies at least once during treatment with GHRH. The significance of these antibodies is not clear and often a positive test at one growth assessment will become negative by the next assessment. The presence of antibodies does not appear to affect growth or appear to be related to a specific adverse reaction profile. No generalized allergic reactions to GHRH have been reported.

The most common treatment-related adverse event (occurring in about 1 patient in 6) is local injection reaction characterized by pain, swelling or redness. Of 350 patients exposed to GHRH in clinical trials, three discontinued therapy due to injection reactions. Other treatment-related adverse events had individual occurrence rates of less than 1% and include: headache, flushing, dysphagia, dizziness, hyperactivity, somnolence and urticaria.

When administered intravenously for diagnostic use, the following adverse reactions have been noted: flushing of the face, injection site pain, redness and/or swelling, nausea, headache, vomiting, dysgeusia, pallor and tightness in the chest.