What is CBD?

Cannabidiol (CBD) is a phytocannabinoid molecule found in hemp (Cannabis sativa), just like the well-known psychotropic substance, tetrahydrocannabinol (THC). However unlike THC, CBD has no narcotic properties.

THC was the first psychoactive ingredient to be discovered in marijuana (1-3), but it was only in the 1990s that scientists identified the endogenous signalling system now known as the endocannabinoid system. This is a collection of endogenous messengers (endocannabinoids) and specific receptors located on external cell membranes (CB1 and CB2 receptors).

It works on a simple principle: when the body deems it necessary, endocannabinoid messengers are produced which bind to their corresponding receptors, triggering various cellular responses such as stimulation of appetite, limitation of synaptic transmission, anti-nociceptive effects (pain relief), hypothermia or reduction of spontaneous locomotion (4).

We know, for example, that endocannabinoids are effective at inhibiting the transmission of small diameter nociceptive fibres (which are involved in the pain process) and at reducing the release of neurotransmitters such as substance P, which are responsible for the transmission of pain. What’s less straightforward is how this system influences several complex mechanisms such as neuroplasticity, apoptosis, neuro-inflammation and traumatic memory.

It so happens that plants produce molecules that have a strong resemblance to endocannabinoids, so much so that they are able to bind to the same receptors (with varying degrees of affinity). Some of them, including THC, produce cellular responses which are very similar to – or even greater than - those triggered by endocannabinoids.

Cannabis contains more than 200 types of molecule that mimic endocannabinoids, including cannabidiol (CBD) which may account for up to 40% of the plant’s dry extract.

How does CBD work? What are its benefits?

The CB1 and CB2 receptors to which endocannabinoids and phytocannabinoids bind are not randomly located in the body. They’re primarily found on the surface of cells of the human brain, central nervous system and immune system tissues. The hippocampus (particularly the dentate gyrus) as well as the Globus pallidus which controls movements (5) have a very high concentration of CB1 receptors, whereas immune tissue has a higher density of CB2 receptors (6). Their specific siting suggests that cannabinoids are involved in modulating memory, emotion, pain (chronic, inflammatory and neuropathic) (7-8) and movements (9-10).

CBD binds more to CB2 receptors, and THC to CB1 receptors. When CBD binds to its receptors, it triggers a chain reaction which results in a decrease in the release of neurotransmitters.

The binding of CBD to CB2 receptors appears primarily to reduce the inflammatory response. This involves multiple cellular targets and leads to a rise in BDNF (a protein that encourages the growth and differentiation of new neurons), a reduction in microglial cells and a fall in pro-inflammatory mediators (11-13). It is this anti-inflammatory effect which makes CBD so useful for pain relief.

CBD thus helps lower the production of inflammatory cytokines, maintain cerebral circulation during ischaemic events and reduce neuro-inflammation (14). It also helps increase levels of adenosine in the brain which is associated with neuroprotection and decreased inflammation (15). In addition, it helps to activate PPARs (16), proteins that act as transcription factors of certain genes involved in inflammation and pain transmission.

Several studies have shown it to have additional benefits: it promotes vasodilation (17-18) and helps reduce reactive oxygen species (ROS) as well as lipid peroxidation (19-21). CBD is also involved in modulating receptors outside of the endocannabinoid system. For example, serotonin receptors also appear to play a part in CBD’s benefits and therapeutic properties.

CBD can reduce the intensity and impact of symptoms associated with chronic anxiety and stress (22-23). Human imaging has shown that CBD affects areas of the brain involved in the neurobiology of several psychiatric disorders. According to one study, a single dose of CBD administered orally to healthy volunteers altered resting activity in limbic and paralimbic regions of the brain (24-25).

Research has also shown a potential reduction in memory associated with traumatic experience.

The use of CBD oil for pain or anxiety is currently enjoying sustained popularity. Though media attention has played a substantial part in this, it is CBD’s properties and benefits, which are now well-documented, which are largely responsible for its success. Following is a summary of the properties variously demonstrated by in vitro, animal and clinical studies (26):

• pain relief;
• an effect on receptors in the brain, particularly serotonin, a neurotransmitter that regulates mood and social behaviour;
• anti-inflammatory potential against cytokines;
• neuroprotective benefits;
• anxiolytic and stress-fighting properties;
• anti-addiction benefits;
• an effect on certain stress responses.

How is CBD Oil 6% produced?

Following extraction, CBD is diluted in hemp seed oil.

Ordinarily, hemp seed oil contains very little CBD (0.0025%). CBD is mostly found in the flowers of Cannabis sativa and, to a lesser degree, the leaves, but not in the seeds. CBD Oil 6% therefore contains hemp seed oil to which CBD extracted from hemp flowers has been added.

When cannabis grows, it produces THC-A and CBD-A, not THC or CBD. It is only when the two molecules are heated that they are decarboxylated into their active forms (27). The conversion of CBD-A into CBD can also be achieved more slowly by exposing the molecule to light, to heat (the temperature of gastric fluids is 37°C) or over time (28). CBD Oil 6% contains CBD and not CBD-A, as well as small amounts of a number of other phytocannabinoids. There is currently no product on the market offering greater CBD oil benefits.

Are there any CBD oil side-effects?

The hemp used in this product contains no THC. . It therefore has no narcotic effect and has an excellent safety profile in humans.

Once ingested, CBD is quickly distributed around the body. Its lipophilic nature means it rapidly crosses the blood-brain barrier to reach tissues in the brain. It does not alter the heart rate and affects neither blood pressure nor body temperature. The half-life of CBD is 9 hours, after which it is eliminated vie urine in a metabolised form.

Its softgel format and the fact that SuperSmart guarantees the purity of its ingredients means there are no particular contraindications associated with its use. To date, there have been no public health problems reported with the use of a THC-free hemp oil standardised in CBD.

What other steps can be combined with taking CBD Oil 6%?

CBD Oil 6% can be combined with InflaRelief Formula, an enhanced formulation for relief of inflammation problems, with Natural Pain Relief, a natural, universal painkiller, and with Posinol 50 mg, an extract of Apocynum venetum which promotes mental relaxation.

Notes

This product should not be used as a substitute for a varied, balanced diet and a healthy lifestyle. It’s important to follow the guidelines on how to take it and the recommended dose, and to use it by the ‘best before’ date. It is not recommended for women who are pregnant or breastfeeding, or for children under 15. Keep out of children’s reach. Store in a cool, dry place.

References

1. Gaoni Y, Mechoulam R. Isolation structure and partial synthesis of an active constituent of hashish. J Am Chem Soc. 1964;86:1646–7.
2. Mechoulam R, Braun P, Gaoni YA. Stereospecific synthesis of (-)-delta 1- and (-)-delta 1(6)-tetrahydrocannabinols. J Am Chem Soc. 1967;89:4552–4.
3. Mechoulam R, Shvo Y, Hashish I. The structure of cannabidiol. Tetrahedron. 1963;19:2073–8.
4. Venance L, Maldonado R, Manzoni O. Le système endocannabinoïde central. Med Sci (Paris) 2004 ; 20 : 45-53.
5. Pertwee RG. The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids: Δ9-tetrahydrocannabinol, cannabidiol and Δ9-tetrahydrocannabivarin. Br J Pharmacol. 2008;153:199–215.
6. Pettit DAD, Harrison MP, Olson JM, Spencer RF, Cabral GA. Immunohistochemical localization of the neural cannabinoid receptor in rat brain. J. Neurosci Res. 1998;51:391–402
7. Hill KP. Medical marijuana for treatment of chronic pain and other medical and psychiatric problems: A clinical review. JAMA. 2015;313:2474–83
8. Rog DJ, Nurmikko TJ, Friede T, Young CA. Randomized, controlled trial of cannabis-based medicine in central pain in multiple sclerosis. Neurology. 2005;65:812–9
9. Portella G, Laezza C, Laccetti P, De Petrocellis L, Di Marzo V, Bifulco M. Inhibitory effects of cannabinoid CB1 receptor stimulation on tumor growth and metastatic spreading: Actions on signals involved in angiogenesis and metastasis. FASEB J. 2003;17:1771–3
10. Freund TF, Katona I, Piomelli D. Role of endogenous cannabinoids in synaptic signaling. Physiol Rev. 2003;83:1017–66.
11. Nestler EJ, Barrot M, DiLeone RJ, Eisch AJ, Gold SJ, Monteggia LM. Neurobiology of depression. Neuron. 2002;34:13–25
12. Wang Q, Shao F, Wang W. Maternal separation produces alterations of forebrain brain-derived neurotrophic factor expression in differently aged rats. Front Mol Neurosci. 2015;8:49
13. Wee N, Kandiah N, Acharyya S, Chander RJ, Ng A, Au WL, et al. Depression and anxiety are co-morbid but dissociable in mild Parkinson's disease: A prospective longitudinal study of patterns and predictors. Parkinsonism Relat Disord. 2016;23:50–6
14. Camposa AC, Fogac MV, Sonegoa AB, Guimarãesa FS. Cannabidiol, neuroprotection and neuropsychiatric disorders. Pharmacol Res. 2016;112:119–27
15. Castillo A, Tolóna MR, Fernández-Ruizb, J, Romeroa J, Martinez-Orgadoa J. The neuroprotective effect of cannabidiol in an in vitro model of newborn hypoxic–ischemic brain damage in mice is mediated by CB2 and adenosine receptors. Neurobiol Dis. 2010;37:434–40.
16. Esposito G, Scuderi C, Valenza M, Togna GI, Latina V, et al. Cannabidiol reduces ab-induced neuroinflammation and promotes hippocampal neurogenesis through PPARc involvement. PLoS One. 2011;6:e28668.
17. Hillard CJ. Endocannabinoids and vascular function. J Pharmacol Exp Ther. 2000;294:27–32.
18. Schultes RE. Hallucinogens of Plant Origin.Science. 1969;163:245–54.
19. Esposito G, Scuderi C, Savani C, Steardo L, Jr, De Filippis D, Cottone P, et al. Cannabidiol in vivoblunts beta-amyloid induced neuroinflammation by suppressing IL-1ß and iNOS expression. Br J Pharmacol. 2007;151:1272–9.
20. Hampson AJ, Grimaldi M, Axelrod J, Wink D. Cannabidiol and (-)Δ9-tetrahydrocannabinol are neuroprotective antioxidants. Proc Natl Acad Sci USA. 1998;95:8268–73.
21. Iuvone T, Esposito G, Esposito R, Santamaria R, Di Rosa M, Izzo AA. Neuroprotective effect of cannabidiol, a non-psychoactive componentpCannabis sativa, on ß-amyloid-induced toxicity in PC12 cells. J Neurochem. 2004;89:134–41.
22. Campos AC, Moreira FA, Gomes FV, Del Bel EA, Guimarães FS. Multiple mechanisms involved in the large-spectrum therapeutic potential of cannabidiol in psychiatric disorders. Philos Trans R Soc Lond B Biol Sci. 2012;367:3364–78.
23. Bergamaschi MM, Queiroz RHC, Chagas MHN, de Oliveira DCG, De Martinis BS, Kapczinski F, et al. Cannabidiol reduces the anxiety induced by simulated public speaking in treatment-naive social phobia patients. Neuropsychopharmacology. 2011;36:1219–26.
24. Crippa JA, Zuardi AW, Garrido GE, Wichert-Ana L, Guarnieri R, Ferrari L, et al. Effects of cannabidiol (CBD) on regional cerebral blood flow. Neuropsychopharmacology. 2004;29:417–26
25. Fusar-Poli P, Crippa JA, Bhattacharyya S, Borgwardt SJ, Allen P, Martin-Santos R, et al. Distinct effects of Δ9-tetrahydrocannabinol and cannabidiol on neural activation during emotional processing. Arch Gen Psychiatry. 2009;66:95–105.
26. Pisanti, S., et al., Cannabidiol: State of the art and new challenges for therapeutic applications. Pharmacol Ther, 2017. 175: p. 133-150
27. Gowran A, Noonan J, Campbell VA. The multiplicity of action of cannabinoids: Implications for treating neurodegeneration. CNS Neurosci Ther. 2011;17:637–44.
28. Russo, E.B., Cannabidiol Claims and Misconceptions.Trends in pharmacological sciences, 2017. 38(3): p. 198-201.

Muscle Relaxing Formula is a combination of plant extracts and micronutrients designed to provide immediate and long-lasting relief from muscle pain and discomfort. It’s a 100% natural formulation containing organically-grown plant extracts recognised for their efficacy against pain.

Who is Muscle Relaxing Formula aimed at?

This innovative formulation is for anyone affected by any of the following:

• frequent muscle pain;
• muscle pain that comes on after intensive exercise;
• involuntary muscle contractions of varying pain intensity; ;
• cramps;
• age-related night-time muscle stiffness ;
• muscle pain linked to nutrient deficiency (vitamin D, essential amino acids, testosterone);
• fibromyalgia pain ;
• muscle spasms ;
• pain from trauma;
• neuropathic pain of unknown origin ;
• other related problems: varicose veins, venous insufficiency, aches, elongation, tears, sprains…

What is in Muscle Relaxing Formula?

What is in Muscle Relaxing Formula?

Muscle Relaxing Formula combines the four plant extracts most widely-studied in relation to muscle pain – and in their best form.

Lemon balm leaf.

Lemon balm is a medicinal herb traditionally used for over 2000 years to calm the nerves and ease pain. Recent clinical trials have confirmed the anxiolytic effects of lemon balm extract (1-3) as well as its ability to reduce sensitivity to pain via modulation of certain receptors in the central nervous system (4-6). Studies have demonstrated its analgesic properties (7-8) and associated decrease in sensitivity to external stimuli (nociception).

These properties are linked to the presence of terpenes in its essential oil as well as to its high content of phenolic compounds (rosmarinic acid, caffeic acid), citral, flavonoids (luteolin) and tannins (9).

Attention: many unscrupulous manufacturers replace the costly lemon balm extract with related species that smell strongly of lemon such as citronella or lemongrass.

The aerial parts of passion flower.

Passion flower contains several substances that act as pain-relievers: indole alkaloids, flavonoids, terpenes and glucosides (10), although more than 294 volatile compounds have been identified.

The majority of pharmacological studies conducted on passion flower have demonstrated its effects on the central nervous system, particularly anxiolytic and sedative properties (11). Commission E (a European scientific advisory board) and ESCOP (the European Scientific Cooperative on Phytotherapy) also officially recognise the use of passion flower to reduce nervousness, and relieve muscle spasms and nerve pain.

The flowers of German camomile

Known for its relaxing properties, camomile has a number of anti-inflammatory and analgesic ingredients such as chamazulene, apigenin, flavonoids and alpha bisabolol. It has produced good results when administered to people suffering from various types of pain (12).

Attention: German camomile (Matricaria recutita), the flowers of which are the most beneficial parts, should not be confused with feverfew (Tanacetum parthenium), the leaves of which are used to reduce the intensity of headaches and migraines.

Valerian root.

Traditionally used by Native Americans for treating muscle injuries, valerian root is still in demand today. It contains more than 150 chemical compounds, including valerenic acid and valtrates which explain its effect on certain chemical messengers in the brain and its relaxing benefits (13).

The formulation also contains two micronutrients recognised for their physiological benefits for human health:

Vitamin E (natural form).

Well-known for its exceptional antioxidant benefits, vitamin E also has anti-inflammatory and vasodilatory properties

Attention: the most abundant form in the body is alpha-tocopherol. As the synthetic form of this molecule is much less well-absorbed, it’s important to choose supplements such as Muscle Relaxing Formula which contain the natural form (14).

Magnesium (in its most soluble and absorbable form).

Magnesium plays a role in nerve transmission and helps muscles relax after contracting. As well as this muscle-relaxant effect, it also participates in pain relief: by disrupting NMDA receptors, it impedes the entry of calcium ions into cells, producing an anti-nociceptive effect.

This effect is associated with decreased sensitivity to pain stimuli triggered by injuries or insult to tissues. Magnesium thus offers significant potential for reducing hypersensitivity to actual and phantom pain. (15-16).

Attention:The less absorbable a magnesium salt is, the less beneficial it will be for the body and the greater its laxative effect. It’s therefore essential to choose the best forms: magnesium citrate and magnesium chloride. It’s also important to control your magnesium intake from food if you are taking it in dietary supplement form.

Five good reasons to choose Muscle Relaxing Formula for fighting muscle pain:

1. The six natural ingredients in Muscle Relaxing Formula have all been scientifically studied for their anti-inflammatory, analgesic or anti-nociceptive effects.
2. Its plant extracts are all organically-produced. This is important as pesticides can be neurotoxic, potentially causing neurological dysfunction, exacerbating pain and promoting inflammation.
3. Pain-killing drugs are currently claiming record numbers of victims: in 2017, more than 50,000 people died in the United States following side-effects from pain-killing drugs prescribed by their doctors. Thus an urgent return tonatural methods is called for.
4. In Europe and the US, more than one in two people currently suffer from joint or muscle pain . Such pain has a significant impact on sleep, level of physical activity and mood.
5. Muscle Relaxing Formula contains no chemical excipients.

Additional measures to make Muscle Relaxing Formula even more effective

To maximise this formulation’s efficacy, you can also follow these steps throughout the supplementation period:

1) Make sure you stay well-hydrated by drinking at least two litres of water a day, a little at a time. Good hydration promotes healthy circulation in muscle fibres.

2) Set aside time every day to relax (meditation, visualisation, listening to relaxing music, contemplation without stimuli, etc.) and ensure you get a good night’s sleep

3) Avoid eating foods that promote systemic inflammation such as red meat, dairy products, cooked meats, processed foods and refined cereals.

4) Prioritise anti-inflammatory foods, particularly those rich in omega-3 fatty acids (fats that are able to reduce pain) as well as fresh fruits and vegetables, all rich in antioxidants. You can combine Muscle Relaxing Formula with a daily dose of Super DHA, a natural formulation rich in omega-3 which provides a much higher intake than can be obtained from everyday diets.

Note: This product should not be used as a substitute for a varied, balanced diet and a healthy lifestyle. It’s important to follow the guidelines on how to take it and the recommended dose, and to use it by the ‘best before’ date. Nie zaleca się stosowania produktu kobietom w ciąży i karmiącym piersią ani osobom cierpiącym na schorzenia wątroby. Produkt może wchodzić w reakcje ze środkami przeciwzakrzepowymi oraz lekami obniżającymi ciśnienie krwi. W razie stosowania innych leków lub występowania problemów ze zdrowiem, przed zastosowaniem produktu należy skonsultować się z lekarzem. Nie stosować produktu, jeśli w niewielkim odstępie czasu planuje się prowadzić samochód lub maszynę. Keep out of children’s reach. Store in a cool, dry place.

Written: December 2018.

References

1. Kennedy DO, Little W, Scholey AB. Attenuation of laboratory-induced stress in humans after acute administration of Melissa officinalis (Lemon Balm). Psychosom Med. 2004 Jul-Aug;66(4):607-13. Texte intégral : www.psychosomaticmedicine.org
2. Kennedy DO, Scholey AB, et al. Modulation of mood and cognitive performance following acute administration of Melissa officinalis (lemon balm). Pharmacol Biochem Behav. 2002 Jul;72(4):953-64.
3. Santos-Neto LL, Toledo MAV, Medeiros-Souza P, Souza GA. The use of Herbal medicine in Alzheimer's disease — a sistematic review. Adv Acc Public 2006;23:441–5.
4. Kennedy DO, Wake G, et al. Modulation of mood and cognitive performance following acute administration of single doses of Melissa officinalis (Lemon balm) with human CNS nicotinic and muscarinic receptor-binding properties. Neuropsychopharmacology. 2003 Oct;28(10):1871-81.
5. Neuroprotective and neurological properties of Melissa officinalis. López V, Martín S, et al. Neurochem Res. 2009 Nov;34(11):1955-61.
6. Pharmacological profile of an essential oil derived from Melissa officinalis with anti-agitation properties: focus on ligand-gated channels. Abuhamdah S, Huang L, et al. J Pharm Pharmacol. 2008 Mar;60(3):377-84.
7. Capasso R, Savino F, Capasso F. Effects of the herbal formulation ColiMil on upper gastrointestinal transit in mice in vivo. Phytother Res 2007;21:999-1101
8. Vejdani R, Shalmani HR, Mir-Fattahi M, Sajed-Nia F, Abdollahi M, Zali MR, et al. The efficacy of an herbal medicine, Carmint, on the relief of abdominal pain and bloating in patients with irritable bowel syndrome: a pilot study. Dig Dis Sci 2006;51:1501–7.
9. Guginski G, Luiz AP et al. Mechanisms involved in the antinociception caused by ethanolic extract obtained from the leaves of Melissa officinalis (lemon balm) in mice. Parmacology, Biochemistry and Behavior 93 (2009) 10-16.
10. Dhawan K, Dhawan S, Sharma A. Passiflora: a review update. J Ethnopharmacol. 2004 Sep;94(1):1-23. Review.
11. Sasikala V, Saravanan S, Parimelazhagan T. Analgesic and anti-inflammatory activities of Passiflora foetida L. Asian Pacific Journal of Tropical Medicine (2011)600-603.
12. Sharifi F, Simbar M, Mojab F, Majd HA. Comparison of the effects of Matricaria chamomila (Chamomile) extract and mefenamic acid on the intensity of premenstrual syndrome. Complement Ther Clin Pract. 2014 Feb;20(1):81-8. doi: 10.1016/j.ctcp.2013.09.002. Epub 2013 Oct 9.
13. Weeks BS. Formulations of dietary supplements and herbal extracts for relaxation and anxiolytic action: Relarian. Med Sci Monit. 2009 Nov;15(11):RA256-62.
14. Institute of Medicine (IOM). Dietary Reference Intakes for Vitamin C, Vitamin E, Selenium, and Carotenoids (2000) : Vitamin E., États-Unis, 2000.
15. Latremoliere A, Woolf CJ. Central sensitization: a generator of pain hypersensitivity by central neural plasticity. J Pain. 2009;10:895–926.
16. Woolf CJ, Salter MW. Neuronal plasticity: increasing the gain in pain. Science. 2000;288:1765–9.