Orthoplex Inkephalin
Excipients
Calcium hydrogen phosphate, ethylcellulose, crospovidone, microcrystalline
cellulose, magnesium stearate, povidone, silicon dioxide, carnauba wax, opadry
clear coating.
Pack size
60 tablets.
Dosage
1-3 tablets daily one hour before meals,or as prescribed.
Indications
May be beneficial for:
* Supporting healthy mood
* Inhibiting enkephalinase pathways
Orthoplex Inkephalin Interactions
Use with caution in patients taking antidepressant medications.
Contraindications
Patients with phenylketonuria need to be cautious of supplements containing
phenylalanine.
Each tablet of Orthoplex Inkephalin contains:
|
dl-Phenylalanine |
400 mg |
|
Glutamine |
25 mg |
|
Magnesium oxide |
100 mg |
|
(equiv. magnesium 60 mg) |
|
|
Pyridoxine hydrochloride (vitamin B6) |
5 mg |
|
Thiamine hydrochloride (vitamin B1) |
50 mg |
|
Tryptophan |
25 mg |
|
Zinc gluconate |
25 mg |
|
(equiv. zinc 3.6 mg) |
|
TECHNICAL INFORMATION
d-Phenylalanine inhibits enkephalinase, an enzyme involved
in the breakdown of enkephalin and endorphin. Inhibition of this enzyme
therefore increases brain levels of enkephalin and endorphin.[3] The
enkephalinergic system is an important inhibitory neurotransmitter system which
has been termed the body's endogenous opioid system.
Decreased enkephalin levels have been associated with
chronic alcoholism, stress and chronic pain. Supplementation with
d-Phenylalanine may improve these conditions.[4, 5]
Pain
Many studies have described the analgesic effect as well as degree of
efficacy of d-Phenylalanine. d-Phenylalanine potentiates the effect of other
analgesic agents such as acupuncture and anti-inflammatory agents such as
flavonoids and aspirin. A study has investigated the analgesic effect of
acupuncture in combination with d-Phenylalanine. Pain tolerance raised after
acupuncture was significantly prolonged by the administration of
d-Phenylalanine. The rise in pain tolerance was most prominent when
d-Phenylalanine was administered 30 minutes before the start of acupuncture
anaesthesia.
Addictive Behaviour
Enkephalin and endorphin are endogenous peptide and polypeptide opioid-like
substances found in the brain. The endogenous opioids appear to be modulators of
neural reward centres. Ethanol-like opioids alter the brain concentrations of
beta-endorphin, enkephalin and other opioid peptides. Ethanol and its metabolic
by-products acetaldehyde and tetrahydroisoquinolines (TIQs) bind to one or more
multiple opioid receptors. It has been demonstrated that isoquinolines can be
formed in mammalian tissue from the ingestion of ethanol and the isoquinoline
precursors are converted to morphine in mammals. Morphine has been identified in
the CSF of non addicted individuals. Therefore, it is possible that part of the
ethanol's effect is due to the production of TIQs or morphine, or both.
Chronic use of alcohol or opioids such as morphine and
heroin results in a significant reduction of the endogenous opioids. Stressful
situations also alter endorphin levels and animal studies have shown reduction
of brain enkephalin and stimulation of alcohol consumption following stressful
situations. In chronic alcoholics beta-endorphin levels in CSF are threefold
lower than those of controls, and significant increases in adrenocorticotropic
hormone levels have been demonstrated.
L-phenylalanine can also convert to tyrosine in the body,
which in turn can be converted to dopamine. Dopamine release is also
specifically involved in the reward pathways of the brain and therefore
addictive behaviour.
Depression
l-Phenylalanine is a precursor of the neurotransmitters dopamine and
noradrenaline. Decreased levels of brain noradrenaline have been found in
depressive states associated with fatigue[10] and an increase in noradrenaline
levels results in a sense of reward and wellbeing.
Pyridoxal 5-phosphate, zinc and magnesium are cofactors in
neurotransmitter synthesis and their inclusion in the formula enhances the
action of the amino acids. Zinc is the major cofactor for the enzyme alcohol
dehydrogenase which is responsible for the degradation of alcohol in the liver.
