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Alchemica

Battling tianeptine (opioid) addiction?

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I'm sharing a friends battle with tianeptine which started with use as an antidepressant (at the conventional dose) and morphed into a real demon. He is in a very dark place. This post is a work in progress and will be updated as I hear of his progress. If anyone has any tips for tianeptine/opioid withdrawals, please do chime in. This is the first time I've been asked to help with them.

Aim: To cease a heavy 7 week tianeptine dependence [reaching up to 1g/day] and initiate naltrexone with as little suffering as possible.

An initial detox (using diazepam as the only aid - 1 week taper with diazepam as needed, on cessation 10mg diazepam tds for 3 days, 5mg diazepam tds for 3 days) resulted in a relapse back to dependence on day 6 and it was decided naltrexone was potentially a suitable drug to help manage his addiction(s). The initial detox was reportedly full on, resulting in typical opioid withdrawals [+more?]. This detox, I suggested the use agmatine and lavender oil as detox aids [avoiding becoming dependent on diazepam] to try and achieve the 7 days opioid free required to safely start naltrexone.

"Agmatine has several mechanisms. It can inhibit N-methyl-D-aspartate (NMDA) and nicotinic acetylcholine receptors, as well as activate imidazoline receptors. Agmatine can also inhibit nitric oxide synthase enzymes, which allows it to regulate elevated levels of nitric oxide. Agmatine can inhibit calcium channels and certain serotonin receptors as well. Further research is needed to determine the full extent of agmatine’s mechanisms.

Agmatine has high affinity for the alpha-2 adrenergic receptors, with little to no affinity for the alpha-1 subsets nor the entire class of beta-adrenergic receptors."

For several days of final decreasing tianeptine use, agmatine 5g bd was added. This is a high dose (a preliminary study to treat depression used 2-3g/day) but I assume higher doses are beneficial/neuroprotective/restorative in a withdrawal state - in retrospect, I don't suggest going to such high doses if you are to try this. At 5g agmatine administered alone, a feeling of calmness and slight dissociation was reported.

It may be best to stick with examine.com dosing protocols:

"There are no standard dosages for agmatine because of the lack of human evidence for its effects. However, a single human study used 1,300-2,670mg of agmatine, daily for the treatment of neuropathic pain. The estimated human dose for improving cognition is 1.6-6.4mg/kg of agmatine, taken orally. This is based off of the 10-40mg/kg dosage range for rats, and is equivalent to 217-435mg for a 150lb person. Supplementation should not exceed 6.4mg/kg of bodyweight."

Note: Rat doses of 20, 30 and 40 mg/kg ip and 2.5-10 mg/kg (in a dose-dependent manner) have been used in lessening naloxone-precipitated withdrawals

Agmatine lowers blood pressure: "agmatine may modulate noradrenaline release in the same way that clonidine does, i.e. via imidazoline binding sites; this involves a reduction in sympathetic tone which in turn reduces blood pressure and heart rate."

- Blood pressure raised to 150/93 [normally 120/80].

"The most fascinating aspect of agmatine, an endogenous molecule, is its ability to potentiate the analgesic effect of morphine and at the same time to reduce the morphine dependence and withdrawal. The findings from this and previous reports suggest that increasing endogenous agmatine could offer novel therapeutic advantage in morphine analgesia and dependence. For example, combining agmatine with morphine during pain management, while reducing the effective dose of morphine, will also prevent the development of dependence to morphine." [1]

Several previous studies have reported the effects of agmatine in reducing morphine withdrawal symptoms [2, 3]

Agmatine can "modulate the neuroadaptations of glutamate transmission in the nucleus accumbens in the case of morphine dependence, including modulating extracellular glutamate concentration and NMDA receptor expression" potentially restoring some deficits induced by opioid dependence. [4]

Other Withdrawal Supplements:
Multivitamin
Magnesium chelate equivalent to 1000mg elemental magnesium
Calcium citrate equivalent to 1000mg elemental calcium
Zinc (as chelate) 50mg [study]
B-complex

Vitamin B12 [study]
Vitamin D
Vitamin C 2000mg [study]
Vitamin E 1000 IU

  • On ceasing tianeptine (his self-control limits the effectiveness of tapering off), 5g agmatine will be added twice daily + prn. I'll document the withdrawal process here,
  • He's on a very high dose SNRI and antipsychotic [there may be some interactions with agmatine]

Lavender oil, containing linalool (which inhibits voltage dependent calcium channels (VDCCs) in synaptosomes and bears some similarities with the established anxiolytic pregabalin [5]), will be used to titrate symptoms [using Lavandula angustifolia]. It has potent anxiolytic effects, similarly to pregabalin which has a reputation of being a useful withdrawal aid and indeed lessens naloxone-precipitated morphine withdrawal symptoms dose dependently in mice [6].

Diazepam, metoclopramide, loperamide, quetiapine (for sleep) and pregabalin were also available if needed. Unfortunately, clonidine was unavailable

Abrupt Withdrawal Notes

- initial sweating. Resolved on dosing agmatine

- Blocked nose/'flu like' feeling still present along with minor muscle aches 15hrs in - not too distressing and not medicated. BP 140/77

(5g agmatine rapidly dropped blood pressure to 118/72)

- At doctors suggestion added 5mg diazepam

- 20hrs in: diarrhea, headache, pleasant feeling of numbness in the face/lips/feeling warm all over rest of body, mood dropping slightly

[basically, in addition to the 5g bd agmatine, what seems to be working well so far is adding smaller doses (1g-3g) to control hypertension/agitation etc as needed. Too much can push one into hypotension. The first 24hrs of this withdrawal has been much easier than his first attempt - the agitation, cravings, dysphoria aren't present. Let's see how it goes from here!]

- Day 2: symptoms are generally mild except notable restlessness, return of tics, extreme mydriasis BP 130/77

- Even with 5mg diazepam, 25mg quetiapine and 6 gelatine caps of lavender oil [this is a very high dose for him, normally 2 is sufficient], sleep was impossible due to restlessness

- Decided 5mg diazepam tds was needed to ease agitation from now on

- Day 3: Feeling OK - mood is reasonable, still agitated, hopefully get some sleep tonight. Cravings are fairly intense. BP 118/79

- Return of restless legs - sleep was difficult

- Day 4: Extreme need to move around, diazepam at 5mg tds is helping slightly. Mood is good enough to wildly flail limbs/attempt to dance to a bit of music. I think agmatine has good potential as an antidepressant but it's probably worth dropping it at risk of flipping to hypomania - ceased agmatine and other withdrawal supplements. BP 136/87

- Diazepam 10mg and 25mg quetiapine was sufficient for some sleep.

- Day 5: Feeling quite sore all over, still agitated, restless legs. Mood getting low. Limited diazepam left for symptoms. Will initiate naltrexone tomorrow - not looking forward to the μ opioid antagonism, the kappa opioid antagonism better counter dysphoria.

Other ideas once considered:

Getting some PDE5 inhibitors

Baclofen, a selective GABAB receptor agonist, prevents the somatic expression and reestablishes the dopamine and mu-opioid receptors levels, modified during naloxone-precipitated morphine withdrawal syndrome

The Therapeutic Effect of Adding Dextromethorphan to Clonidine for Reducing Symptoms of Opioid Withdrawal: A Randomized Clinical Trial

Obviation of Opioid Withdrawal Syndrome by Concomitant Administrationof Naltrexone in Microgram Doses: Two Psychonautic Bioassays

Medication of l-tetrahydropalmatine Significantly Ameliorates Opiate Craving and Increases the Abstinence Rate in Heroin Users: A Pilot Study

More on tianeptine:

Tianeptine

Tianeptine has been further and further demonstrating what appears to be relatively high tendencies toward tolerance, withdrawals upon cessation, and potential abuse/addiction dynamics. This is even being seem within usage that adheres to therapeutic dosages, as to withdrawals upon cessation and escalation of dosages within some with a tendency toward tolerance or misuse/abuse.

Tianeptine has been demonstrated in the literature to bear mu-opioid agonist activity and indeed may bear closer resemblance to classical opiates in the respect of adverse effects of the aforementioned nature than prior thought.

Addictive potential of Tianeptine - the threatening reality.

"A total of 24 patients (male volunteers), consumers of opiates in the past and suffering from Tianeptine abuse, were under clinical observation. The age range of patients was from 21 to 33 years. Tianeptine consumption history was 5 months duration on the average. The daily dose of preparation was 40 tablets (500 mg intravenous injections on the average). Patients used Tianeptine in combination with antihistamines (Promethazine, Suprastin). Research was carried out with the use of clinical, psychological and laboratory methods. Has been used Ch. Spilberger's scale of anxiety and T. Balashov's scale of depression. Comparison of withdrawal syndrome developed after cessation of Tianeptine and opiates consumption has shown that in case of Tianeptine, in the dynamic of withdrawal syndrome predominates well expressed high-level of anxiety and depression, while at opiates consumption - withdrawal syndrome is characterized by algesic events and vegetodysfunctions. Supposedly, Tianeptine, in contrast to other anti-depressants, stimulates release of neurotransmitter dopamine in nucleus Accumbens, that probably determine addictive potential of this drug. High level of anxiety, excitability and vegetodysfunctions, presumably could be explained by activation of the NMDA (glutamate receptors) receptor system in Locus coeruleus, and in vegetative ganglion. In the present article potential threat that may develop at Tianeptine consumption, especially in former opiate consumers, without medical purposes has been emphasized."

Tianeptine abuse: a case report

"A 28-year old male patient admitted to our clinic with complaints of high-dosage tianeptine usage and difficulty in quitting the drug usage. The patient had complaints of social withdrawal, disturbances of sleep and appetite and crying 10 years ago, following his parents’ divorce. Patient was then referred to psychiatry unit and diagnosed with depression and treated with venlafaxine 75 mg/day. However, patient did not comply with the treatment because of nausea and dizziness complaints. Then the patient was switched to escitalopram 10 mg/day and benefited from this therapy, but ended the treatment because of side effects. In the next 3 years, patient had no psychiatric complaints but after the 3 years, patient had complaints of social anxiety, social withdrawal and avoidance, thoughts of self-worthlessness and social function loss and he seeked for treatment. In that term, patient was prescribed tianeptine 12.5 mg 3 times a day. He reported that he really benefited from the treatment, saying he became much more optimistic and happy, and experienced very few side effects compared with his previous antidepressant experiences, and there was a big difference in his mood when he took the drugs and when he did not. He also reported that he felt worthless and weak-willed when he did not take the medication and confident and comfortable when he did. On the other hand, the patient started to lose these effects on the 4th month of treatment. When he wanted to give up the medication, he had complaints of sweating, hot flashes on hands and feet, extreme weakness, dryness in mouth, anxiety and fear. He then took another tablet and like this, he increased the dosage up to 750 mg/day. Patient said that even though he took very high doses for the desired effect, this high dosage caused a loss of appetite, intestinal gas and a frequency in urination. The patient started to spend all his money on the medication and takes 10-15 pills before going to a social event or a job interview. He had thoughts of not getting the job or friends abandoning him if he did not take the medication. His drug cessation attempts did not last more than 3 days. When he had withdrawal symptoms, he started using tianeptine again. Patient wanted to give up this drugabuse with his own will and admitted to our clinic.

There was no history of previous substance addiction or abuse. The patient’s main complaint was that he could not give up “tianeptine” and he was hospitalized for “tianeptine addiction”. First, tianeptine was stopped and diazepam 20 mg/day was started in order to control anxiety and withdrawal symptoms. Patient’s lab results (Complete blood count, routine biochemical markers, and liver, kidney and thyroid function tests) were within the normal range. On the second day of patient’s hospitalization, patient showed symptoms of excessive hunger, xerostomia, nausea and hot flashes. In a week, those complaints subsided. Diazepam dosage was lowered and finally stopped. Patient was discharged and paroxetine 20 mg/day was started for “tianeptine addiction” and “social phobia”. In the follow-up interviews, he had no complaints regarding tianeptine and he did not use tianeptine anymore. But his social phobia continued, so paroxetine dose was increased to 30 mg/day.

Various internet stories

"I fall into the category of people who start small and end up on megadoses relatively quickly. 50mg every few hours worked great for a few days. Within three weeks I was at 250mg 4 or 5 times a day. Then, upon abrupt cessation, experienced opioid-like WD symptoms. Tapering helped, along with 8-10mg of loperamide. The particular symptoms were definitely opioid -- hot flashes like a burning all over the body, allergy symptoms with an ugly cough and watery eyes/nose, and profuse night sweats. A previous tianeptine run had the same symptoms, but with diarrhea. Symptoms from other opioid WDs that were missing included restless legs, day sweats, cold flashes, and alternating hot/cold flashes. To some extent there was the inability to get comfortable, but not to the same extent as other true opioids."

" the tianeptine withdrawl is intense. moreso than traditional opiods imo. the restless leg, anxiety, dysphoria and depression is rough. i quit 100mg of methadone a day cold turkey and imo, tianeptine withdrawls are about as bad. seems to affect more than just opiate receptors. it is short lived though, and u should be OK anyday now. buprenorphine, will pretty much stop them if u dont get better quickly. benzos will help too. loperamide should help, not hurt. it will only stop the runs though and u need a high dose. these people that say u cant get high from tianeptine, dont have a clue. 350mg at once feels about like 20-30mg of oxycodone. it will put u into "full nod". really reminds me alot of oxy."

"I have just (thankfully) gotten out of a 3-4 week long dependency, that was growing in dosage by the week. Fortunately upon reading about its opioid mechanisms and how it relates to my prior opiate addiction issues, I was able to cessate entirely on the Friday, suffer some pretty terrible withdrawal symptoms over Saturday and Sunday, and be well enough to function at work beginning on Monday. Needless to say, there is a definite risk for abuse with this drug, and although I do not discount my prior addiction issues, I highly recommend caution when considering trying this drug. On the plus side, I do believe that after the withdrawal symptoms subsided completely, that I felt surprisingly better overall than I had before taking it. Make of all of this what you will. "

"I have used Tianeptine quite heavy in the past. First of all, I never felt its effects by taking 1 tablet.. or 2 or 3.. I needed like 8-10 to feel good for a few hours. This was getting too expensive, so I ordered bulk powder... my dosages and tolerance kept increasing and the last 30 days of my Tianeptine addiction I have been using about 1.2-1.5 gram a day.

I had to quit cold turkey, because my new shipment of Tianeptine accidentally got stuck at customs and that was some really hellish time... No sleep at all for 72 hours, deep depression, aching body, diarrhea, anxiety, etc etc.. needed like 2 weeks to recover from that shit."

"I came across tianeptine on a forum I found out it is marketed in other countries as antidepressant but also found out is a full agonist at the μ and δ opioid receptors. So running low on funds decided to give it a try.and bought 100 grams from a trusted nurotropic site. Wow at first I couldn't believe it almost no transition withdrawal from heroin, and also it felt like a more functional opioid than heroin with almost a light amphetamine quality. Well been doing tianeptine for about 3 months, and as of lately ran out. And let me just say the withdrawal from this drug is just as bad as heroin and I'm on day 5 and still am sore sweaty cold and with out etizolam don't think I could have made it this far... "

"But then of course curiosity got the best of me and I took a big dose. Boom, full opiate high. There seemed to be no ceiling to it either. I quickly over a few weeks got up to over 2 grams a day (!!). I was high the whole time and happy and loving it. But supplies are sketchy right now, and God caused a delivery to be lost in the mail because he obviously knows there is no limit to how high you can go with this stuff. It seems to have a ceiling effect with respiratory depression, and is generally less sedating. But the half life is a pain as towards the end you will be waking up in the middle of the night to dose.

Right now I've taken over 200mg of loperamide in the past 12 hours just to mask the tianeptine withdrawal from 2 grams. The loperamide covers it better than it covers H withdrawals- I feel 95% normal instead of the maybe 70% normal you usually feel substituting loperamide for other opiates- but this is still a really dangerous game- not to mention I'm taking a huge dose of loperamide. Tianeptine is insanely "moreish."

"I'm 4 days into cold turkey withdrawal from this terrible drug. I only used it for about 2 months, but daily totals reached 1-2g a day of using both the sodium (short) form and sulfate (long acting) form. Tuesday was my last very small dose of 50mg sodium and 50mg sulfate which put me into withdrawals quick. I'm really not doing that bad today other than occasional emotional torment, mild lack of motivation, and mild fatigue. In the beginning i did experience mild physical withdrawals such as the sweats and chills, crawly skin, restless legs, insomnia, etc. "

"...haven't been able to titrate down and am pretty scared of stopping. I've come close and at about the 12-24 hour mark the WD's were so intense that my head felt like it was being crushed, I felt very drunk and my arms and legs were incredibly sore. "

Edited by Alchemica
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I don't know how you could mange to fulfill these requirements and I don't even know if it will work but..

Stop taking the opioid. .. start having 20 mg waffle olanzapine... should knock you out for a good period of time. In events of waking eat food drink water obtain oxycodone and have 20-40 mgs to start with and drink the highest concentrate alcohol found, like 3 or 4 shots simultaneously then have another olanzapine wafer. Should get more sleep. Repeat process but slowly reduce the oxycodone and up the dose of olanzapine wafers to remain sedated. Continue to eat food and consume heavy alcohol in short bursts to fall back asleep. Make sure you are getting enough b1 in and more importantly b6!

Hopefully after a week or two your mate is off the oxycodone completely and just consuming high voltage alcohol and olanapine to continue... then you will have potentially replaced the one habit with alcohol witch will be easier to overcome on a short course of benzos.

B1 thiamin can be iv'd to replace the physical activity of boosting also witch is a bonus but it burns like all fuck and is very unpleasant to inject.

My 2 cents.

Sorry if its just retarded bullshit alchemica because I know you know what your on about.

I'm just thinking replacing a hard habit to get over with a habit slightly less harder to get over. Plus cushy olanzapine witch really knocks you around short term so you can make big changes in little tine.

Wish you and your mate all the best.

Wert

Edited by wert
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Loperamide (immodium) is allegedly useful for reducing the severity of opiate withdrawal. Sounds like crap, very well might be, but there you are.

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When I decided it was time to quit my opiate meds I went and got some california poppy and wild lettuce. Added a bit to my mix and made myself tea with an opiate tincture made from pretty much the same stuff. Went from 2 20mg oxys and 8 fortes a day to just tea as often as I was getting shaky and slowly drank leas tea over the ensuing weeks.

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Thanks for the replies :)

When I decided it was time to quit my opiate meds...

That's probably a big part of his problem. He is trying to quit because he doesn't want to be dependent on the opioid, due to tolerance issues, the crazy dose and declining effectiveness but still wants there to be a place for the initial functionality (ability to leave the house feeling confident, no anxiety or depression) and feeling (not euphoria but it was a step up from anhedonia) it gave him to be in his life.

Anyway, he's committed to round two of withdrawals.

Edited by Alchemica

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Naltrexone is going to make the WD severe! I would never consider that for somebody unless they have time free from work, childcare, etc... I can't see them being able, or willing to function hardly at all going from a large tianeptine habit and almost immediately to precipitated withdrawals.

In the case of opiates, I am a firm believer that suffering/unpleasantness directly correlates with healing. Just as you will feel euphoria, relaxation, etc as neurotransmission in whatever parts of the brain adapting (downregulating in this case), you will feel dysphoria, unpleasantness, and anxiety as that system is working to recallibrate (upregulate). But, you still must consider the likelihood for relapse... although in theory cold-turkey is the fastest road to recovery, many (most?) people become more likely to relapse than with tapering. I have also heard tapering to be ineffective for some though, as addicts tend to rationalize using more, and make very slow or no progress.

I would recommend tapering with just the tianeptine- recognize the withdrawal symptoms, and appreciate them as a measure of healing, and keep the end goal in mind.

They will likely not find something that will substantially help them in the withdrawal. It will be unpleasant- as I just mentioned, to heal they must feel the withdrawal. Any drugs that substantially improve symptoms will likely be drugs with similar mechanisms of action. For example, kratom will ease withdrawal symptoms, but only because it stimulates the same types of neurotransmission that needs to recalibrate. With that in mind, such a drug will slow this recallibration (healing). This is why I suggest tianeptine simply being tapered down, rather than worrying about other supplements/drugs to help. Sure, drink your tea, take mellatonin, smoke some herb (if he's into that), and Valium for the worst of nights... this will probably increase his odds of making it through the acute WD. But I must emphasize that unfortunately nothing will do away with the suffering that one has to endure in order to heal.

You may have heard that 'addiction' is permanent. After your brain has primed itself for addiction (tolerance), that person will tend to rapidly regain this tolerance when re-continuing use of that substance, at a rate much, much faster than when before they had first developed tolerance. This is more relevant to opiates than any other addictive drug in my experience. For example, in the case for somebody who developed a tolerance for an opiate, who quits the habit entirely for upwards to a year, and subsequently gets past all the withdrawal symptom and tolerance goes back down... if they use opiates over just one weekend, come Monday they will be back in withdrawal with most of their tolerance returned. I mention this in response to that person's motive to eventually use the medication again, effectively, at more reasonable dosages. It may not be realistic.

Lastly, he shouldn't ever give up. The acute withdrawal is only about a week long. After that it's just a matter of staying determined, and finding other, healthier vices in life. And even if he fails once, or a hundred times, there is still opportunity to change that and get clean. I've seen this first hand.

EDIT:

Might throw this in here too. Everybody will appreciate something that's easy to control, like taking another supplement, to ease and improve the situation, and I understand that completely.

There is an herb called Ashwaghanda, an adaptogen, that I use myself. In the US, encapsulated extracts are very cheap and available. It has a broad range of benefits that have been measured in studies- not only has it been shown to (greatly) improve sleep, reduce anxiety, reduce scores of depression, and etc- it also has been shown not only in vitro, but in vivo on human patients, to induce neurosurgeons- repair damaged synapses and increase dendritic branching- it basically appears to make the brain more plastic. In addition to this, it has odd effects with opiates... studies have shown it to prevent morphine tolerance from developing with co-administered; it also seems to block general effects, and increase rate of tolerance reduction when discontinuing opaites. It would appear to be greatly beneficial when recovering from an addiction to opiates.

Edited by Derkshaman
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Thanks Derkshaman.

With regard to:

Naltrexone is going to make the WD severe! I would never consider that for somebody unless they have time free from work, childcare, etc... I can't see them being able, or willing to function hardly at all going from a large tianeptine habit and almost immediately to precipitated withdrawals.

Is this even with 7 days clean from tianeptine (which has a short half-life anyway) before starting naltrexone? I'm new to the opioid field so I have lots to learn and have only heard of precipitated withdrawals occurring if a full agonist is still in one's system and displaced with an antagonist/partial agonist. Are you suggesting it will make the post-acute withdrawal syndrome severe, or something else? The idea of initiating naltrexone so quickly was talked about in consultation with a doctor. They have plenty of free time so that's not such a big issue but their mental health is poor - daily suicidal ideation and the likes so anything to minimise exacerbation of mental health issues is important.

The reason getting onto naltrexone so quickly is seemingly desirable is his impulse control is poor due to mental health issues and years of treating his brain unlovingly... relapse is imminent soon after detox and we want to make sure cravings from this legal substance don't eventually lead to cravings for harder illicit street drugs, too. His cravings were extreme during the last lot of withdrawals and it was only 6 days until he caved in. If he had some relief for the restlessness and other symptoms like the severe depression I think he could have lasted longer. Diazepam (5mg tds) was doing bugger all. I hear clonidine is excellent for some symptoms but his doctor won't prescribe it at present...

Edited by Alchemica

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My apologies; I didn't completely weigh your statements.

In that case, using naltrexone would probably be manageable, but it will do little as far as reducing cravings, perhaps even making the symptoms worse. I would predict that it will also make post-acute withdrawals more severe, yes. Although it should, as you know, prevent impulsive relapse due to its blocking/dampening effect on the opiate response. It would speed the recovery as well. So considering this, I don't have strong opinion on whether or not it should be used.

Everyone is different.

I am one to advocate tapering, depending on the person. Like a tapering period as long as a month until complete abstinence. The suffering is at least not as intense, and is more manageable... although it's more enduring. For most people they have no choice but to continue working, balancing family, school, or etc... and you have to be realistic in how you will be able to function and manage these things; life cannot always stop and wait for someone to recover.

But for many others, tapering is hardly effective, and cold-turkey w/ naltrexone will be the way to go. I can't dismiss either routes efficiency.

Edited by Derkshaman
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This might not be a nice or comfortable question to ponder but it might possibly be helpful.

*Why* is your friend quitting?

If it is for any reason other than a heartfelt burning desire to get free from that relationship, it will be a long and hard road that is more likely to fail than to succeed. Many people addicted to drugs of one sort or another (including alcohol) want to quit because they think they should or think that they have to or or they need to or they decide it is necessary because they are in some sort of trouble with the law, work, relationships or family. The majority of those people will experience a miserable path of repeated failures alternating with sober living while keenly aware of an gaping, empty hole existing in their being. Anything less than seriously wanting to be free is more likely to fail than not. The more a person actually WANTS to get free, the greater the chance of success.

The present disempowering model views addiction as a disease which is not actually correct and does not help "cure" people.

If the addication can instead be regarded as a symtom of a behavioral problem that involved developing a dysfunctional relationship with a molecule, the user has a chance of getting a handle on it and some personal empowerment capable of enabling success.

I'd suggest the best path for most people is to drop all adjunct drugs being enlisted to help stop another drug. Withdrawals suck but frankly a bad case of the flu is a far worse experience than opiate withdrawals. By the time opiates are cleared enough for adding naloxone they are also cleared enough for a drug free recovery. If someone really NEEDS naloxone or antibuse, that is fine. More power to them. But I'd say also that if those sorts of approaches are necessary that person does not really WANT to quit, instead they are quitting because they decided that they NEED to quit or are being forced to quit by someone or something else.

I got strung out when I was a teenager. I got off dope by WANTING sincerely to be free from being used by my beloved molecule (much like realizing you are in a toxic relationship with a loved one who will bring you nothing but harm). I've never looked back and have since discovered that I have no problem with being attracted to narcotics now even if I am prescribed opiates for pain.

Naloxone, methadone and 12-step models do actually work for some people but they are only a few percentage of the people using narcotics.
"WHATEVER WORKS" is a good mantra but recognizing what is not working on an individual basis is a key part of learning what does work.

One other side of this worth pondering is that some people actually need opiates due to their body making inadequate endorphins and such. Those people are literally self-medicating to address a biochemical deficiency. For that subset of narcotic users, learning how to either better regulate their use responsibly or learn to gain better control over their biochemistry through tools such as biofeedback is a far more achievable option than just getting off the drugs. Modern drug education in the USA rejects responsible use as even being possible yet in Europe this has been proven to be more effective at giving some people their lives back than AA/12-steps.

Finding the right path for the individual rather than a one size fits all solution is a valuable approach to finding success. All of those models, including AA/12-steps, can work for some individuals and will not work for others.

Thomas Szasz pointed out the single most valuable question for actually finding solutions to people's drug problems needs to be "Why is THIS particular individual self medicating with THAT particular drug and what of value is being given to them in this relationship." If that question is not honestly asked and answered the 'solution' will be focused on the drug and not actually touch the underlying causes for the use developing into a problem. The answers for resolving drug abuse lie in knowing much more about the individual and why they chose that drug than they are about the actual drug itself.

Best of successes to your friend finding internal peace.

Just my two cents' worth.

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Thanks trucha!

Why does he want to quit?

He was no longer in control of his intake and was a slave to the molecule. If he could be in control of his use and manage tolerance, he'd be content continuing. Family members and friends are pressuring him to give up all legal medications/supplements even though he feels such are a fundamental part of who he is.

Why doesn't he want to?

"On the tianeptine, I never felt euphoric or high, just 'normal'. Daily suicidal ideation became new options, cognition improved, depression and anxiety resolved, I didn't feel profoundly alone, I could catch a bus and train to visit friends etc which was previously not possible. I felt alive. I accumulated a lot of vicarious trauma and extreme social pain - I can't talk about it but it's enough to want to die. On the tianeptine, I actually wanted to be alive for once. I've been depressed for so long and none of the conventional antidepressants have done much. ECT either... I was desperate... I was at the point of kill myself or dose up - I hated myself and couldn't muster self-love"

He also has schizophrenia and has started to develop tics where he says things like "f* off" or "go away". Tianeptine seems to essentially stop them, Then there's the anhedonia which no antipsychotic medication treats...

He was initially inspired by these which really capture the psychache leading him to use:

Social Pain Revisited: Opioids for Severe Suicidal Ideation

Opioid Drugs for Mental Anguish: Basic Research and Clinical Trials

He decided he NEEDED to quit.

Edited by Alchemica

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In response to Trucha...

Yes I think that the reason that a person uses the drug is often dismissed, and that here in the US we tend to see drug use as nothing but a bad habit, that when given up or fixed, yields nothing but positives.

There is a reason for this though: there are obvious negative impacts for using drugs that would make even an open minded person feel urgency to get clean.

I don't think it's always a matter of society telling you something is definitely bad, and subsequently causing guilt...

A person who is addicted to drugs will often (usually, with some habits) notice horrible, detrimental impacts whether or not society defines this. Many people could care less about what society thinks about drug use... I mean, that's part of the reason why a person decides to self-medicate in the first place (they decide on this themselves, despite conflict from society). These same people end up feeling urgency to quit, and it is because the negative impacts they notice, rather than just beginning to feel guilty from society's judgement.

For example, the most obvious in this situation...

1g tianeptine a day would be very expensive... that's money that the person could be using to improve their life, perhaps even enough to be the matter of progress vs stagnancy. They could be failing to invest this money in more long-term happiness.

Next, they are less consistent... being on a mental teeter-totter, as mind altering drugs enter then leave their system... it's very hard to be consistent, and the person has a harder time understanding who they really are or what they want in life with all of this going on.

Anyways, I don't think this is to debate whether or not drug addiction is wrong. Yes, there is obviously physical, structural tendencies for drug use that society seems to often fail to address.

This is just helpful advice for somebody who has already decided on what they want- to get clean and become freed from their dependency.

ADDED:

The short-term goal is to become free from this addiction.

Then it is to find a better and more lasting set of solutions to address the problems that originally led to this addiction.

The second part is more complicated, indeed. It may involve lifestyle changes, but depending on your standpoint, it likely will involve other medications, drugs, or herbs. I am not capable of giving much advice more specific than this.

But when somebody opens up another world of troubles through addictions, that person often just wants to get back to where they were, even if suffering to begin with, before trying another route.

Edited by Derkshaman
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In addition, he's interested in naltrexone for its kappa opioid antagonism.

Downside is naltrexone decreases feelings of social connection which could be really detrimental "naltrexone (vs. placebo) reduced feelings of connection both in the laboratory and in daily reports. These results highlight the importance of opioids for social bonding with close others, lending support to the brain opioid theory of social attachment" [1] but has some other interesting properties "Naltrexone (NTX) increased attention to emotional expressions, slowed identification of sadness and fear, and decreased ratings of arousal for social and non-social emotional scenes. These findings are more consistent with anxiolytic kappa-antagonist than mu-blocking effects, suggesting effects on kappa receptors may contribute to the clinical effects of NTX" [2]

Toll like receptor 4 antagonism is another interesting feature [3]

It may help his depression:

"there was a trend for those receiving naltrexone to exhibit an improvement in depression over time compared with the control group. Participants who were adherent to naltrexone treatment exhibited fewer depressive symptoms than those who were nonadherent".

There's the thing that being in the grips of addiction/withdrawal cycles is about as depressing as it gets, anything is a step up.

Might even tackle his internet addiction, too!
Edited by Alchemica

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Let it be known I have no experience or knowledge of tianeptine...

He was initially inspired by these which really capture the psychache leading him to use:

Social Pain Revisited: Opioids for Severe Suicidal Ideation

Opioid Drugs for Mental Anguish: Basic Research and Clinical Trials

These were interesting. I'm going to massively oversimplify but I hope there may be something of worth to wonder about... But if I'm understanding this right, when there is "mental pain", the dorsal anterior cingulate cortex is activated. That jogged my memory about the recent psilocybin studies which (again if reading correctly) showed decreased activation in the DACC. Ergo, perhaps the feeling of Unity and "peace" which comes about from psilocybin may potentially correct some depressive symptoms ("feeling profoundly alone")? Am I correct in thinking psilocybin also acts on DAT which may help the neurological craving aspect of the loss of tianeptine?

I've heard of low dose buprenorphine being used for depression at .2mg which is very low, if math serves correctly, a buprenorphine patch at 240micrograms/day would be around a 10mcg/hour patch which lasts for a week. Perhaps a gentler alternative? If the tianeptine has a short half life then it shouldn't be too long before buprenorphine could be introduced (opiates in system must be out before bupe, otherwise precipitated withdrawals would occur).

Someone mentioned a brain previously in a state of dependence becoming recognisant of the dependant state, and ergo making it more likely to become re-addicted. I'd agree with this, although I don't think it would always apply; and the danger of that I think would be more a case of where the person is at mentally/emotionally as to whether or not they're susceptible to becoming addicted again: this has been my experience.

Weaning/Tapering. I've done cold turkey, tapered, replaced... All three have worked for me at different times so it's hard to say what's going to work for your friend THIS time around. When I tapered, a method I liked to use is: Taper very quickly drop as much as possible in a short period of time; then when the uncomfortable feeling becomes too unbearable (particularly being careful if this point is suicidal for your friend so avoid getting that close), then have as small a dose as possible to get you through the intensity, then put up with withdrawals for as long as possible again, then when it becomes unbearable again, another small dose. Repeat up to roughly 2-3 (maybe even longer) weeks until eventually the withdrawal times become longer and more bearable until eventually you don' t feel you need the small dose (which has become less and less anyway). During the withdrawal phases it's good to keep pushing yourself to just hold out one more day... A few more hours... A few more minutes... There comes to be a sort of pride in making yourself hold out, a nice challenge and also making it a game. The nice thing is that because you do end up having a small dose (and you know you probably will have it), there's no big feeling of failure. Basically it exacerbates your pride in holding on and gaining confidence, while minimising negative feedback. Personally if your friend is in no great risk of benzo abuse (as I"m not), then I can't see how having some help in the tapering phase. Doesn't have to be benzos though, as has been mentioned lavender, chamomile, ashwaghanda (sounds interesting!), or whatever else is going to help.

Also, reading about this agmatine sounds fascinating! And I'll be reading up on ashwaghanda, as I'm currently on an opioid pain relief patch and I want to limit dosage increases as much as possible.

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Am I correct in thinking psilocybin also acts on DAT which may help the neurological craving aspect of the loss of tianeptine?

I'm not aware of psilocybin acting on the dopamine transporter. 5-HT modulation of dopamine release (an increase in endogenous dopamine) in psilocybin-induced "psychosis" in man has been reported though [1]

Dopamine reuptake inhibitors were good antidepressants initially for him, they could help with the cravings. They didn't exactly address his main problem - the social pain - but made life as it was interesting and left him feeling content even though he was still stuck in a rut. Fixed his attention problems, too. Problem is his poor self-control. He'd escalate doses to the point of exacerbating psychosis. That said, the combination of a stimulant and antipsychotic (which he's on) is an interesting approach to managing negative symptoms and cognitive deficits in schizophrenia.

The loss of tianeptine will be hard but if the naltrexone doesn't block feelings of social connection too much, he might find some humans who will counter that, and deepen his current friendships :)

Not sure psilocybin is a good tool for him at this stage. He's previously had some not so great psychedelic experiences (NOT resulting in "unity" and "peace" but more psychotic lessons that were too much for him to assimilate at that stage)

He asked his GP about buprenorphine. Apparently "it wasn't an option". Trying to get him to see an addiction medicine doctor again.

He's almost tempted to try the following over naltrexone:

Medication of l-tetrahydropalmatine Significantly Ameliorates Opiate Craving and Increases the Abstinence Rate in Heroin Users: A Pilot Study

as it seems it could best address post-acute withdrawals/cravings/dopaminergic aspects and the likes but I don't know how well it will work with his current medications.

Thanks for your interesting post FancyPants

Edited by Alchemica

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Immodium in large doses accompanied with an antacid proton pump inhibitor and a litre of grapefruit juice generally allows the loperamide to cross the bbb in small amounts. It's structurally quite similar to methadone and should have someone with a tianeptine habit up on their feet and feeling fine without cravings in 2 hours.

Should last 3 days. 40mg plus of immodium ( loperamide) though.

I've read of it working for heroin withdrawal and Ive known someone who used it for morphine wd successfully.

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Does anyone have any idea about the safety of introducing a small dose of naltrexone and get this process started ASAP? His cravings are intense and he wants something to block a return to use. He's in day 3 of withdrawals - most of the troubling physical WDs have passed - and the drug has a half-life of ~3hrs. I don't think he can last 7days. We can use a bit of diazepam.

Thanks in advance for any advice

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I suggest going the diazepam route till day 5. You do not want to take it early.

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We finally got there and initiated the naltrexone without too much suffering :) Lots of agitation, tics and psychological torment for all involved though. Thanks for the support.

As you can tell, adding surplus supplements is another of his addictions :wink:

Hopefully this is the start of a less self-destructive life path!

Now just to deal with the PAWS

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Has your mate been through paws before?

I know I've mentioned memantine more than once on this forum but the stuff is a godsend for managing addiction and depression over an extended period.

Ceretropic.com

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He's probably had plenty of PAWS that he's always been in denial about and instead let masquerade as mental illness.

Thanks for the memantine tip. I'll get him to ask his doctor about it.

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Not sure why it hasnt been brought up but kratom is an amazing medicine for greatly reducing withdrawal. I've seen quite a few people use it to quit an opiate habit with little to no withdrawal. You dont have to suffer whilst quitting, in fact it makes it easier to quit because you know its not going to be that bad. It makes it easier to slip back into a habit but the slips are less long in duration because you know you can stop at any time with the kratom.

Kratom is also great as a maintenance tool.

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Just a quick update for anyone else who's interested:

In the case of opiates, I am a firm believer that suffering/unpleasantness directly correlates with healing.

Think I've started to discover that. Trying to attenuate the withdrawals my way didn't help him out.

"It's been pretty full on but an interesting experience... Stopped trying to medicate all the pain away/distract myself with supplements and just 'feel' it but it's seriously intense having all the pain I'd been running from for so long back in my head/heart. Trying to stay positive and give the suicidal thoughts some distance but they're pretty persistent. It's been enough that my auditory hallucinations have picked up and I'm getting slight visual hallucinations which I hope aren't going to progress into psychosis.

Anyway, it's been good to have a proper detox and get back to feeling things deeply even if that includes the current dysphoria... haven't relapsed or had intense cravings for opioids which is nice. Letting myself adjust to the naltrexone and hoping for some improvement mood wise."


Seems his tics, which really spiked in frequency have mostly passed and were an outlet for lots of internalised negative energy.

Thanks again for all your support.



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Re:

It may be possible to get the best of both worlds for addictions... interesting recent research:

Combination of levo-tetrahydropalmatine and low dose naltrexone: a promising treatment for the prevention of cocaine relapse.

Relapse to drug use is often cited as the major obstacle in overcoming a drug addiction. While relapse can occurs for a myriad of reasons it is well established the complex neuroadaptations, which occur over the course of addiction, are major factors. Cocaine, as a potent dopamine transporter blocker, specifically induces alterations in the dopaminergic as well as other monoaminergic neurotransmissions, which lead to cocaine abuse and dependence. Evidence also suggests that adaptations in the endogenous opioids play important roles in pathophysiology of cocaine addiction. Following this evidence, we investigated a combination medication, levo-tetrahydropalmatine (l-THP) and low dose naltrexone (LDN), targeting primarily dopaminergic and endogenous opioid systems as a cocaine relapse prevention treatment. In the present study Wistar rats were used to assess the effects of l-THP and LDN on cocaine self-administration, drug-seeking behavior during cocaine reinstatement, spontaneous locomotion, and effects on the endogenous opioid system. We determine the combination of l-THP and LDN reduces drug-seeking behavior during reinstatement potently than l-THP alone. Additionally, the combination of l-THP and LDN attenuates the sedative locomotor effect induced by l-THP. Furthermore, we revealed that treatment with the combination of l-THP and LDN has an upregulatory effect on both plasma β-endorphin and hypothalamic POMC that was not observed in l-THP-treated groups. These results suggest that the combination of l-THP and LDN has great potential as an effective and well-tolerated medication for cocaine relapse prevention.

For the moment, the naltrexone is doing its job though :)

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High dose vitamin c may be worth considering. I believe it is a mammalian response to dealing with fight or flight responses that we are deficient in as humans, so it can be a worthwhile compliment when recovering from trauma. It will also aid in repairing the immune system which has its own cascade affects on the body such as the nervous system, cells, bowels etc. all of which become suppressed with opiod addictions. Treating the body like this frees up energy to allow or emotions to start moving again which is normally very important in recovering from addiction. As always true healing requires a combination of approaches but perhaps this may provide an avenue to help with that. Best wishes.

P.S. Something like Lypricel might be suitable as digestion can also be impaired.

Edited by courage
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