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Author Topic: Alternative treatment modalities for opiate and opioid withdrawal  (Read 1618 times)


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During my time as a practicing herbalist, especially that when which I was involved with those addicted to opiates, I spent a lot of time trying to figure out ways to help people quit these addictive drugs.  Kratom is a god send for many who are opiate addicted, however it also has its own addictive tendencies and for most, serves as a replacement, and only some does it serve as a temporary tool.

I do not blame kratom, or the users, and instead commend them on their strength and commitment.  It is obvious that for an herb to be able to stop heroin withdrawal single-handedly, that it also may come with some of its own issues as well.  Such is the fate for all potent herbs, which can be medicinal in one regard, but poison in another.  Only tonics and certain foods are immune from this poison <-> medicine relationship.

Anyways, during my studies, I had encountered both in the literature, and from users too, that certain dopaminergics can be used to alleviate the symptoms of opioid withdrawal.  One such case is that of William S. Burroughs, a famous drug user and heroin addict, who claims he was able to quit his addiction, cold turkey, with the help of apomorphine, a dull dopamine agonist.  The herbs that immediately come to mind here with similar pharmacology are Catuaba, Fo-ti Root, Schizandra berry, Blue lotus, Sacred lotus, and to an extent, Mucuna pruriens. 

This potential treatment makes sense when one understands the basics, dopamine enhancement to cover dopamine receptor downregulation, but becomes a little more complex when one learns more about pharmacology, and the relationship between dopamine and adrenaline, and the inverse relationship between opioids and adrenaline.  So what is true here exactly?

A successful treatment of buprenorphine withdrawal with the dopamine receptor agonist pramipexole

ABSTRACT Background
Buprenorphine, used for treating opioid dependence, may have a withdrawal syndrome requiring treatment. Modulation of the dopamine system, which has been implicated in opioid withdrawal, may be a target for withdrawal for opioids such as buprenorphine.Case ReportA case is reported of a buprenorphine withdrawal syndrome with predominant symptoms of restlessness that were resistant to clonidine and benzodiazepines. It was successfully treated with the dopamine agonist pramipexole. Scientific Significance Dopamine receptor agonists may have a place in the treatment of restlessness associated with opioid withdrawal and may have value for the broader spectrum of opioid withdrawal symptoms. (Am J Addict 2014;XX:13)

The relationship is actually quite complex, but yes, dopamine itself can cover for part of the opioid withdrawal syndrome, and may be able to cover the specific part that brings people back, that state of feeling good, positive, and focused.  While heavy doses of opiates are quite sedating, any experienced addict will be happy to share how opiates help them focus.  It is this paradoxical sedative and stimulating effect that makes opiates so addictive, so unique, and so difficult to quell with other herbs and medicine.

Opioids have far reaching actions throughout the body however, and dopamine, while a very special neurotransmitter and hormone, does not cover the full extent of the withdrawal.  In addition to dopamine stimulation, one should also avoid anything that increases norepinephrine levels, and anything that exchanges ATP for cAMP (caffeine and related xanthines).  This means herbs that increase adrenaline/norepinephrine levels, such as any caffeine containing herb (white/green/black tea, guayusa, yerba mate, kola nut, guarana, coffee), and adrenal stimulants should be avoided.  Rhodiola rosea is ok as long as it is not mixed with any stimulants.

Sedatives can also come in handy, particularly those of the alpha agonist, beta blocker, cannabinoid, NMDA antagonist, benzodiazepine, and serotonergic classes.  These all help due to different reasons, but essentially they work by slowing down the functions of the body without causing the same type of tolerance and addiction that opioids can cause.  Some herbs that fall into these categories are the berberine containing plants which have alpha agonist activity (goldenseal, coptis, corydalis, phellodendron, and berberry), cannabinoid active plants such as hops, cannabis sativa, and lemongrass, NMDA antagonistic herbs (which also reduce tolerance) such as Bacopa monneiri, Calamus, Chinese Cat's claw, and Chinese Senega root, the benzodiazepine and gabanergic herbs such as Kava, Chamomile, Gotu kola, Happiness Tree bark and flower, Lavender, Lemon Balm, Magnolia bark, Skullcap, L-Theanine, and Valerian, and finally, the Serotonergic class of herbs that consists mostly of St. John's wort, Kanna, and 5-HTP.

Additionally, opioid withdrawal also causes unpleasant physical sensations in most people, nerve pain, inflammation, and internal stress are all symptoms.  Having a steady supply of anti-inflammatories is very helpful here, extracts such as salicin from Willow and quinine from Cinchona can reduce inflammation and even put a damper on the dreaded RLS (Restless Legs Syndrome) that many experience while "kicking".  Herbs like Corydalis, California poppy, and Wild lettuce are also optimal pain relievers to help manage these uncomfortable symptoms.  St. John' wort, turmeric/curcumin, and Cannabis sativa are also all excellent anti-inflammatories.  Additionally, Holy basil can be used to significantly reduce cortisol and the stress response, which are definitely increased during withdrawal.  Holy basil makes a great tea with turmeric and St. John's wort to reduce stress and anxiety.

To sum everything up, here are the aforementioned herbs, and their appropriate categories for use to assist when tapering and quitting use of opioids, including kratom:

  • Dopaminergics (Mood improving, Motivation):Catuaba, Fo-ti Root, Schizandra berry, Blue lotus, Sacred lotus, and to an extent, Mucuna pruriens.
  • Alpha agonists (Adrenaline reducing): Goldenseal, Coptis, Corydalis, Phellodendron, and Berberry)
  • Cannabinoid agonists (Pain relieving, Adrenaline reducing, Muscle relaxing): Hops, Cannabis sativa, and Lemongrass
  • NMDA antagonists (Sedative, Tolerance reducing, Pain relieving): Bacopa monneiri, Calamus, Chinese Cat's claw, and Chinese Senega root
  • Benzodiazepine and GABAnergics (Calming, Muscle relaxing, Adrenaline reducing: Kava, Chamomile, Gotu kola, Happiness Tree bark and flower, Lavender, Lemon Balm, Magnolia bark, Skullcap, L-Theanine, and Valerian
  • Serotonergics (Calming, Adrenaline reducing, Mood improving): St. John's wort, Kanna, and 5-HTP
  • Anti-inflammatories (Pain relieving): Cinchona, White willow, Quinine, Salicin, Corydalis, California poppy, and Wild lettuce
  • Stress reducers (Cortisol reducing): Holy basil

To avoid:
  • Stimulants: any caffeine containing herb (white/green/black tea, guayusa, yerba mate, kola nut, guarana, coffee), and adrenal stimulants should be avoided.

I trust this information will be of value to those who seek it out.  The tools are all at our disposal, we merely need pluck them out of the earth and reclaim our health, and our lives.  Thank you for reading.


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Re: Alternative treatment modalities for opiate and opioid withdrawal
« Reply #1 on: April 19, 2016, 02:20:31 pm »

Some more info on the long term effects of opioid therapy and the cocurrent metabolic and enzymatic changes that occur:

Chronic Opioid Treatment Induces Adenylyl Cyclase V Superactivation

It has been known for some time that chronic treatment of neuronal cells and tissues with opioids, contrary to their acute effect, leads to an increase in cAMP accumulation. This phenomenon, defined as adenylyl cyclase superactivation, has been implicated in opiate addiction, yet the mechanism by which it is induced remains unclear. Here, we show that this phenomenon can be reproduced and studied in COS-7 cells cotransfected with adenylyl cyclase type V and μ-opioid receptor cDNAs. These cells display acute opioid inhibition of adenylyl cyclase activity, whereas prolonged exposure to the μ-agonist morphine or [-Ala2, N-methyl-Phe4, Gly-ol5]enkephalin leads to a time-dependent superactivation of adenylyl cyclase. This superactivated state is reversible, because it is gradually lost following agonist withdrawal. Adenylyl cyclase superactivation can be prevented by pertussis toxin pretreatment, indicating the involvement of Gi/o proteins, or by cotransfection with the carboxyl terminus of β-adrenergic receptor kinase or with α-transducin (scavengers of Gβγ dimers), indicating a role for the G protein βγ dimers in adenylyl cyclase superactivation. However, contrary to several other Gβγ-dependent signal transduction mechanisms (e.g. the extracellular signal-regulated kinase 2/MAP kinase pathway), adenylyl cyclase superactivation is not affected by the Ras dominant negative mutant N17-Ras.

Seeing how ATP is a precursor for cAMP, and cAMP levels accumulate during opioid addiction, it is believed that ATP levels must suffer accordingly.  If this hypothesis is true, increasing ATP will reduce some of the symptoms of opiate withdrawal, while explaining why substances such as caffeine can make withdrawal symptom worse.  Some herbs that increase ATP levels without converting ATP to cAMP are Rehmannia glutinosa, Cordyceps, and Ginseng.  All three are adaptogenic herbs, and increase energy levels in ways atypical of caffeine.  In essence, these herbs provide the required energy that both caffeine and opioids deplete.

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