Epithalon (also known as Epitalon or Epithalone) is the synthetic version of the polypeptide Epithalamin which is naturally produced in humans. This pineal peptide preparation is secreted in the epithlamium-epiphyseal region of the brain. Its more prominent tasks are: to regulate metabolism in the epiphysis, increase the sensitivity of hypothalamus to its natural hormonal influences, normalize the function of the anterior pituitary, regulate the levels of gonadotropins and melatonin in the body. Epithalamin increases a person's resistance to emotional stress and also acts as an antioxidant.
Epithalamin was first discovered in the late 1980's by Prof. Vladimir Khavinson from St. Petersburg, Russia. It has been studied extensively ever since. It is known by several names, including Epitalon, Epithalon, Epithalone, Epithalamin and Epithalamine. Since all the patents are held by the Russian inventor there is not much interest for this tetra-peptide from the western big pharma industry. This makes the substance fairly unknown in the west due to the absence of marketing usually seen with big pharma products. In Russia it is currently in clinical studies and shows prospective results as treatment for liver disorders, neuropathology, psychiatry and geriatrics.
Human life extension via Telomerase activation and elongation of Telomeres
Epitalon is one of the very few substances which are able to activate Telomerase (telomere terminal transferase) enzyme in humans. Telomerase renews (elongates) the telomeres, which are responsible for protection of the human DNA from damage and cancer causing errors.
Treatment of aging cells in culture with Epithalon induced elongation of telomeres to the size comparable to their length during the early cell divisions. Epitalon treated cells with elongated telomeres made 10 extra divisions (44 passages) in comparison with the control and continued dividing. Thus, Epithalon prolonged the vital cycle of normal human cells due to overcoming the Heyflick cell division limit. (reference: V. Khavinson et all. in Bulletin of Experimental Biology and Medicine. June 2003.
Epitalon used for Anti Aging
Epitalon decreases the age-related changes in immune and neuroendocrine systems, reduces the incidence of recurrent infections and chronic diseases. Long term clinical trials have shown that in patients with age-related pathology Epithalamin eliminates imbalance in prooxidation and antioxidation systems. (reference: N. Anisimov et all. Neuroendocrinology Letters, 2011.
Results of 12-months treatment with Epithalon in patients with signs of accelerated aging showed normalizing effect on metabolism and condition of various functional systems. Elevated uric acid, alkaline phosphate and cholesterol in elder patients returned to normal after 10 days of treatment, and remained stable in a several months peroid afterwards.
Epitalon effects
Experimental and clinical studies of Epitalon showed the following pharmacologist properties of Epithalamin (Epitalon):
- Telomerase activation (consequently, elongation of Telomeres)
- regulates neuroendocrinous system
- increases the hypothalamic sensitivity to the endogenous hormonal effects
- decrease or suppression of proliferative changes in vaginal epithelium and endometrium in anovulatory phase
- normalization of gonadotropic hormones levels (FSG, LG, prolactin)
- positive influence on peripheral haemodynamics: improvement of blood rheology, decrease of intravessel thrombogenesis
- regulation of the levels of reactants in the acute inflammation phase (c3-component of the complement, pre-albumin, C-reactive protein, alpha-orosomucoids
- normalization of T-cell immunity
- normalization of aqua-electrolyte balance indices
- normalization of uric acid levels
- normalization of Cholesterol
- rejuvenation / strengthening of the immune system
- inhibition of spontaneous and induced carcinogenics (tumor prevention)
Epitalon side effects
There have been no reported side effects of Epithalon in any of the clinical and experimental trials. Likewise there are no reports of any Epithalamin adverse reactions on various internet forums, where people have been documenting repeated courses every 10-15 days for several years.
Epithalon dosage and course (cycle) duration
Dosage depends on the purpose and severity of the damage which is treated. Epitalon can be used orally (less effective and large dose) or injected intramuscular or under the skin (more effective at much smaller dose).
1. Oral Epithalon use (least effective):
- duration: between 10 - 20 days
- dosage: between 400 - 600 mg of Epithalon per day
- daily frequency:200 mg per serving, between 2 - 3 servings per day (depending on the dosage)
2. Epithalon as nasal spray or drops (medium effectiveness):
- duration: between 10 - 20 days
- dosage: between 15 - 30 mg of Epithalon per day
- daily frequency:total daily dosage split into 3 servings throughout the day
3. Injectable Epithalon use (most effective):
- duration: 10 - 20 days
- dosage: between 5 - 10 mg per day (20 mg intravenous for terminal patients)
- frequency of injection:1 injection per day for low dose, 2 injections for higher dose (divided between morning and late afternoon injection)
Each 10 - 20 days course of Epithalamin is followed by 4-6 months pause before repeating the course again. Epitalon treatment can be repeated indefintely.
Reconstituting (dissolving, mixing) the freeze dried Epitalon:
Plain sterile water for injection is the most suitable diluent for freeze dried Epithalamin (Epitalon). Alternatively it can also be reconstituted with bacteriostatic water (0.9% sodium chloride), normal saline (0.9% NaCl) or water containing 0.9% (9 mg/mL) of benzyl alcohol. It all works the same, but you probably want to use the least amount of additives in the water - therefore plain sterile water.
Lyophilized (freeze dried) Epitalon usually comes in 10 mg vials. Gently inject 1 to 2 ml of water into the vial. Let it sit in refrigerator for 10 - 15 minutes. If there are any undissolved particles left after 15 minutes, gently rotate the vial between your fingers until all of the powder has dissolved and you are left with clear liquid.
Injecting Epitalon
Epithalon has a systemic effect regardless of the injection spot. It can be injected subcutaneously (under the skin) or intramuscular (into the muscle). People usually inject it into the shoulder, tigh, buttocks or under the skin in the stomach fat area.
Proper storage of Epitalon:
If possible, always store both the freeze dried powder and the mixed solution in refrigerator (do not freeze).
Before mixing (lyophilized / freeze dried Epitalon powder):
- refrigerated between 2 - 8 degrees Celsius (36 - 46 Fahrenheit) it can be used for 24 months
- at room temperature (up to 37 degrees Celsius or 98.6 Fahrenheit) it can be used for over 90 days
After reconstitution (liquid Epithalon):
- liquid Epithalamin should be refrigerated between 2 - 8 degrees Celsius (36 - 46 Fahrenheit) at all times. It should not be frozen.
- once reconstituted, the Epitalon should be used within 20 days
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