OPIOID FACTS AND WITHDRAWAL MECHANISM
Endogenous opioids include Enkephalin, Beta-endorphin, Dynorphin, Endomorphin, Nociceptin, opiorphin, and morphine. Enkephalin is the ligand for delta receptors and also has a high affinity for Mu-opioid receptors. Dynorphin is the ligand for kappa receptors. Beta-endorphin has an affinity for mostly Mu, but also delta and kappa. Endomorphin is the ligand for Mu. Nociceptin for ORL receptors. Opiorphin is found in saliva and inhibits the enzyme that breaks down Enkephalin and B-Endorphin called Enkephalinase. Opiates inhibit the firing of locus ceruleus neurons which is involved with physiological responses to stress and panic. The highest concentration of opioid receptors are found in the sensory, limbic and hypothalamic regions of the brain.
When exogenous opioid consumption is stopped, the increased activity of the locus coeruleus contributes to the symptoms of opiate withdrawal. The alpha2 adrenoceptor agonist clonidine is used to counteract this withdrawal effect by decreasing adrenergic neurotransmission from the locus coeruleus. Excessive cortisol secretion is seen in 40-60% of depressed patients, associated with diminished noradrenergic inhibition of corticotropin-releasing hormone secretion in the hypothalamus. Corticotropin-releasing hormone induces anxiety in experimental animals. Cortisol stimulation of the locus coeruleus due to chronic stress exacerbates norepinephrine stimulation of the amygdala. Healthy humans fed fish oil rich in the omega-3 fatty acids EPA and DHA show reduced plasma levels of the stress-associated hormone norepinephrine
(1)Drastic reduction in dopaminergic activity during opioid withdrawal likely accounts for the intense dysphoric state of the user. Therefore increased dopamine activity attenuates withdrawal
(2)Substance P is involved with expression of some symptoms of opiate withdrawal
(3)Acetylcholine outflow is increased and GABA decreased during opioid withdrawal.
(4)Anti-opioid peptides may contribute to tolerance and possibly dependence of chronically administered opioids.
(5)Lower doses of opioids are easier to come off, tapering is effective at reducing the severity of withdrawal.
(6)Nicotine withdrawal causes desensitation of the delta opioid receptors.
GOAL—HOMEOSTATIS (BALANCE)
Gamma-aminobutyric acid (GABA) is the second most abundant neurotransmitter in the brain and the primary inhibitory neurotransmitter that acts through a negative feedback system to block the transmission of a signal from one cell to another. It is important for balancing the excitation in the brain. Benzodiazepines (anti-anxiety drugs) work on the GABA receptors of the brain, inducing a state of relaxation.
Glutamate is an excitatory neurotransmitter and is the most abundant chemical messenger in the brain. It is believed to be involved in learning and memory. Certain diseases (such as Alzheimer’s disease) or brain injury (such as stroke) can cause too much glutamate to accumulate. This can set the stage for excitotoxicity, a process that can lead to damage or death of the affected brain cells.
It is important that GABA and glutamate are carefully orchestrated to balance each other. Dysfunction of one of these amino acid neurotransmitters affects the function of the other. Some experts believe that their excitatory and inhibitory balance influences all brain cells.
[SOURCES]
(1)http://www.ncbi.nlm.nih.gov/pubmed/7853194
(2)http://www.ncbi.nlm.nih.gov/pubmed/2482512
(2)http://www.ncbi.nlm.nih.gov/pubmed/12576096
(3)http://www.ncbi.nlm.nih.gov/pubmed/3814913
(4)http://www.ncbi.nlm.nih.gov/pubmed/8545244
(5)http://www.ncbi.nlm.nih.gov/pubmed/17952010
(6)http://www.ncbi.nlm.nih.gov/pubmed/20941594
EFFECTIVE METHODS TO EASE OPIOID WITHDRAWAL
{TENS}
(a) Cerebral Electrotherapy (CES/NET)
(k) EA Acupuncture
(k)*Binaural Beat Frequencies (Utilizing headphones) @ 2hz, 100hz, 111hz
{DRUGS}
(b) Baclofen
(c) THC/Marijuana
(d) Gabapentin/ Pregabalin (Lyrica)
Phenibut
(p) Gamma-Hydroxybutyric acid (GHB)
Chlordiazepoxide
(e) Clonidine
Tricyclic Anti-Depressants
-Amitriptyline
(f) Benzodiazapines
-Alprazolam
-Diazepam
Loperamide (Immodium)
(o) Cobrotoxin (Cobroxin/Nyloxin)
*Propoxyphene
*Codeine
*Ibogaine
{HERBS}
Kratom
Passion Flower
(h) Weinicom
(i) St.John’s Wort (NOTE: Do not use while tapering)
{VITAMINS}
(j) Vitamin C
Vitamin D
Vitamin E
B-Complex
Calcium
Magnesium
(NOTE: Multivitamin Suggested)
{AMINO ACIDS & NUTRIENTS}
(m) D/DL-Phenylalanine (DPA)
(l) L-Tryptophan
L-Tyrosine
Omega-3
DHA
{DRUGS TO STAY AWAY FROM}
(g) Caffiene
(NOTE: Adenosine A2 antagonists increase dopamine release and slightly reduce withdrawal, while adenosine A1 agonists inhibit excitatory amino acid release and significantly reduce withdrawal. Caffeine has been found to antagonize both A1 and A2A receptors in the brain, therefore potentiating opioid withdrawal. It also inhibits GABA and neutralizes any benzodiazepines.)
(n) Cocaine
(n) Amphetamine
{Other helpful activities to help reduce withdrawal severity and distract the mind}
Exercise
Massage
Sexual Activity
Hot Shower or Bath
Cool Mattress or Pillow
Use a Fan to Keep Cool
Watch Favorite TV series
My Personal experience: As I’ve tried nearly everything under the sun, nothing has worked as effectively for me in regards to reducing acute withdrawal as mega dose Vitamin-C supplementation (as sodium ascorbate a more bioavailable form). A daily dosage of 40-60 grams of Vitamin-C in split doses throughout the day had taken care of 80-90% of all symptoms of withdrawal. ( See cited source (j) ) This is knowledge I wish I had years ago. Another very effective method for me was listening to 2 hz binaural beat frequencies with headphones for a minimum of 20 minutes, this causes the brain to release enkephalin. Gabapentin and alprazolam were the most effective drugs and Kratom the best herb that I've used to relieve withdrawal. If you want to quit but have chronic pain in your way, Cobroxin/Nyloxin is the only over the counter pain reliever that can take the place of a high dose opiate when it comes to alleviating chronic pain. I recommend at least using the gabapentin and alprazolam along with the mega-dose sodium ascorbate if you plan to stop opioid use with as little withdrawal as possible. A good back massage, and a hot shower always takes the edge off too. I have not yet tried baclofen but I've heard and read many good things about it, I also have yet to try the Electro-Acupuncture (EA) or other TENS treatments as well but I’ve seen amazing results on video. Check them out in the links below.
http://www.netdevice.net/aboutvideojournal_2.php
http://www.netdevice.net/aboutvideojournal_1.php
http://www.netdevice.net/aboutvideojournal_3.php

[SOURCES]
(a) http://www.ncbi.nlm.nih.gov/pubmed/760910
(b) http://www.ncbi.nlm.nih.gov/pubmed/1324986
(c) http://www.ncbi.nlm.nih.gov/pubmed/11359533
(d) http://www.ncbi.nlm.nih.gov/pubmed/15093968
(e) http://www.ncbi.nlm.nih.gov/pubmed/3048954
(f) http://www.ncbi.nlm.nih.gov/pubmed/8905331
(g) http://www.ncbi.nlm.nih.gov/pubmed/12879207
(h) http://www.ncbi.nlm.nih.gov/pubmed/11061678
(i) http://www.ncbi.nlm.nih.gov/pubmed/19370548
(i) http://www.ncbi.nlm.nih.gov/pubmed/19067385
(i) http://www.ncbi.nlm.nih.gov/pubmed/12649774
(j) http://www.ncbi.nlm.nih.gov/pubmed/10836211
(j) http://www.tandfonline.com/doi/abs/10.1080/02791072.1979.10472107
(k) http://www.ncbi.nlm.nih.gov/pubmed/15135942
(l) http://www.ncbi.nlm.nih.gov/pubmed/7454382
(m) http://www.moodcure.com/restoring-natural-opioid-system.html
(n) http://www.ncbi.nlm.nih.gov/pubmed/16191669
(o) http://www.aseanbiodiversity.info/Abstract/51010802.pdf
(o) https://www.nyloxin.com/media/nyloxin_drug_insert.pdf
(p) http://www.ncbi.nlm.nih.gov/pubmed/8397726
Endogenous opioids include Enkephalin, Beta-endorphin, Dynorphin, Endomorphin, Nociceptin, opiorphin, and morphine. Enkephalin is the ligand for delta receptors and also has a high affinity for Mu-opioid receptors. Dynorphin is the ligand for kappa receptors. Beta-endorphin has an affinity for mostly Mu, but also delta and kappa. Endomorphin is the ligand for Mu. Nociceptin for ORL receptors. Opiorphin is found in saliva and inhibits the enzyme that breaks down Enkephalin and B-Endorphin called Enkephalinase. Opiates inhibit the firing of locus ceruleus neurons which is involved with physiological responses to stress and panic. The highest concentration of opioid receptors are found in the sensory, limbic and hypothalamic regions of the brain.
When exogenous opioid consumption is stopped, the increased activity of the locus coeruleus contributes to the symptoms of opiate withdrawal. The alpha2 adrenoceptor agonist clonidine is used to counteract this withdrawal effect by decreasing adrenergic neurotransmission from the locus coeruleus. Excessive cortisol secretion is seen in 40-60% of depressed patients, associated with diminished noradrenergic inhibition of corticotropin-releasing hormone secretion in the hypothalamus. Corticotropin-releasing hormone induces anxiety in experimental animals. Cortisol stimulation of the locus coeruleus due to chronic stress exacerbates norepinephrine stimulation of the amygdala. Healthy humans fed fish oil rich in the omega-3 fatty acids EPA and DHA show reduced plasma levels of the stress-associated hormone norepinephrine
(1)Drastic reduction in dopaminergic activity during opioid withdrawal likely accounts for the intense dysphoric state of the user. Therefore increased dopamine activity attenuates withdrawal
(2)Substance P is involved with expression of some symptoms of opiate withdrawal
(3)Acetylcholine outflow is increased and GABA decreased during opioid withdrawal.
(4)Anti-opioid peptides may contribute to tolerance and possibly dependence of chronically administered opioids.
(5)Lower doses of opioids are easier to come off, tapering is effective at reducing the severity of withdrawal.
(6)Nicotine withdrawal causes desensitation of the delta opioid receptors.
GOAL—HOMEOSTATIS (BALANCE)
Gamma-aminobutyric acid (GABA) is the second most abundant neurotransmitter in the brain and the primary inhibitory neurotransmitter that acts through a negative feedback system to block the transmission of a signal from one cell to another. It is important for balancing the excitation in the brain. Benzodiazepines (anti-anxiety drugs) work on the GABA receptors of the brain, inducing a state of relaxation.
Glutamate is an excitatory neurotransmitter and is the most abundant chemical messenger in the brain. It is believed to be involved in learning and memory. Certain diseases (such as Alzheimer’s disease) or brain injury (such as stroke) can cause too much glutamate to accumulate. This can set the stage for excitotoxicity, a process that can lead to damage or death of the affected brain cells.
It is important that GABA and glutamate are carefully orchestrated to balance each other. Dysfunction of one of these amino acid neurotransmitters affects the function of the other. Some experts believe that their excitatory and inhibitory balance influences all brain cells.
[SOURCES]
(1)http://www.ncbi.nlm.nih.gov/pubmed/7853194
(2)http://www.ncbi.nlm.nih.gov/pubmed/2482512
(2)http://www.ncbi.nlm.nih.gov/pubmed/12576096
(3)http://www.ncbi.nlm.nih.gov/pubmed/3814913
(4)http://www.ncbi.nlm.nih.gov/pubmed/8545244
(5)http://www.ncbi.nlm.nih.gov/pubmed/17952010
(6)http://www.ncbi.nlm.nih.gov/pubmed/20941594
EFFECTIVE METHODS TO EASE OPIOID WITHDRAWAL
{TENS}
(a) Cerebral Electrotherapy (CES/NET)
(k) EA Acupuncture
(k)*Binaural Beat Frequencies (Utilizing headphones) @ 2hz, 100hz, 111hz
{DRUGS}
(b) Baclofen
(c) THC/Marijuana
(d) Gabapentin/ Pregabalin (Lyrica)
Phenibut
(p) Gamma-Hydroxybutyric acid (GHB)
Chlordiazepoxide
(e) Clonidine
Tricyclic Anti-Depressants
-Amitriptyline
(f) Benzodiazapines
-Alprazolam
-Diazepam
Loperamide (Immodium)
(o) Cobrotoxin (Cobroxin/Nyloxin)
*Propoxyphene
*Codeine
*Ibogaine
{HERBS}
Kratom
Passion Flower
(h) Weinicom
(i) St.John’s Wort (NOTE: Do not use while tapering)
{VITAMINS}
(j) Vitamin C
Vitamin D
Vitamin E
B-Complex
Calcium
Magnesium
(NOTE: Multivitamin Suggested)
{AMINO ACIDS & NUTRIENTS}
(m) D/DL-Phenylalanine (DPA)
(l) L-Tryptophan
L-Tyrosine
Omega-3
DHA
{DRUGS TO STAY AWAY FROM}
(g) Caffiene
(NOTE: Adenosine A2 antagonists increase dopamine release and slightly reduce withdrawal, while adenosine A1 agonists inhibit excitatory amino acid release and significantly reduce withdrawal. Caffeine has been found to antagonize both A1 and A2A receptors in the brain, therefore potentiating opioid withdrawal. It also inhibits GABA and neutralizes any benzodiazepines.)
(n) Cocaine
(n) Amphetamine
{Other helpful activities to help reduce withdrawal severity and distract the mind}
Exercise
Massage
Sexual Activity
Hot Shower or Bath
Cool Mattress or Pillow
Use a Fan to Keep Cool
Watch Favorite TV series
My Personal experience: As I’ve tried nearly everything under the sun, nothing has worked as effectively for me in regards to reducing acute withdrawal as mega dose Vitamin-C supplementation (as sodium ascorbate a more bioavailable form). A daily dosage of 40-60 grams of Vitamin-C in split doses throughout the day had taken care of 80-90% of all symptoms of withdrawal. ( See cited source (j) ) This is knowledge I wish I had years ago. Another very effective method for me was listening to 2 hz binaural beat frequencies with headphones for a minimum of 20 minutes, this causes the brain to release enkephalin. Gabapentin and alprazolam were the most effective drugs and Kratom the best herb that I've used to relieve withdrawal. If you want to quit but have chronic pain in your way, Cobroxin/Nyloxin is the only over the counter pain reliever that can take the place of a high dose opiate when it comes to alleviating chronic pain. I recommend at least using the gabapentin and alprazolam along with the mega-dose sodium ascorbate if you plan to stop opioid use with as little withdrawal as possible. A good back massage, and a hot shower always takes the edge off too. I have not yet tried baclofen but I've heard and read many good things about it, I also have yet to try the Electro-Acupuncture (EA) or other TENS treatments as well but I’ve seen amazing results on video. Check them out in the links below.
http://www.netdevice.net/aboutvideojournal_2.php
http://www.netdevice.net/aboutvideojournal_1.php
http://www.netdevice.net/aboutvideojournal_3.php

[SOURCES]
(a) http://www.ncbi.nlm.nih.gov/pubmed/760910
(b) http://www.ncbi.nlm.nih.gov/pubmed/1324986
(c) http://www.ncbi.nlm.nih.gov/pubmed/11359533
(d) http://www.ncbi.nlm.nih.gov/pubmed/15093968
(e) http://www.ncbi.nlm.nih.gov/pubmed/3048954
(f) http://www.ncbi.nlm.nih.gov/pubmed/8905331
(g) http://www.ncbi.nlm.nih.gov/pubmed/12879207
(h) http://www.ncbi.nlm.nih.gov/pubmed/11061678
(i) http://www.ncbi.nlm.nih.gov/pubmed/19370548
(i) http://www.ncbi.nlm.nih.gov/pubmed/19067385
(i) http://www.ncbi.nlm.nih.gov/pubmed/12649774
(j) http://www.ncbi.nlm.nih.gov/pubmed/10836211
(j) http://www.tandfonline.com/doi/abs/10.1080/02791072.1979.10472107
(k) http://www.ncbi.nlm.nih.gov/pubmed/15135942
(l) http://www.ncbi.nlm.nih.gov/pubmed/7454382
(m) http://www.moodcure.com/restoring-natural-opioid-system.html
(n) http://www.ncbi.nlm.nih.gov/pubmed/16191669
(o) http://www.aseanbiodiversity.info/Abstract/51010802.pdf
(o) https://www.nyloxin.com/media/nyloxin_drug_insert.pdf
(p) http://www.ncbi.nlm.nih.gov/pubmed/8397726
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