Overload
Alcoholism treatments
Category: Medicines
Type
Involuntary
Introduction and description
Alcohol acts on the GABAA receptor as an allosteric modulator. It sedates, it reduces anxiety, it has a slightly hypnotic effect, and it can be calming. But it is also addictive.
Tolerance to alcohol is developed as the GABAA receptor adapts to the drug by increasing the number of receptors so more of the drug is needed to have the effect. This is a most unusual way for any drug to work. Most drugs tend to kill off cells when taken in high amounts, but all the GABAA agonists and allosteric modulators, when taken in very high quantities on a regular basis, cause the system to adapt by increasing the receptors and thus toning down the effect of continual intake.
But, if the alcohol is withdrawn, the receptors become hyperactive – stimulated – because there is not enough calming agent – GABA or alcohol or similar to tone down the excitability induced by the glutamate in the body.
The results are highly dangerous and can cause seizures, hallucinations, anxiety, depression, irritability, hypertension, tachcardia, muscle tension, insomnia and many other symptoms associated with tolerance and withdrawal. Additionally, the upregulated Calcium Channels are linked to an increase in neuropathy pain. Headaches, migraines and other sorts of sensitivity to pain.
The Drugs
In order to help alcoholics, a class of drug was developed that aims to replace the alcohol - the alcohol treatment drugs.
There are two types of drug that have been developed in this respect:
- GABAA drugs - This replacement is, interestingly enough a GABAA allosteric modulator, which means you are replacing one allosteric modulator with another. So not treatment really – just replacement.
- Opioids - Another solution that scientists appear to have come up with is to provide people with opioids. This is indeed novel, the opioids relieves the pain and suffering of the withdrawal, sedate the person and ensure that the person is dependent on two types of substances – opioids and GABA related alcohol.[sorry for the slight cynical slant here]. ………….
And these have produced hallucinations, although it is often difficult to tell whether the hallucinations are caused by the drug or the alcohol withdrawal or withdrawal from the drug - it is, in the long term, often the latter.
Background
The fact that some of these drugs are simply a replacement of one GABAA allosteric modulator with another has not gone unnoticed in the research community …………
Substitution therapy for alcoholism: time for a reappraisal? Chick J, Nutt DJ.; Health Sciences, Queen Margaret University, Edinburgh, UK.
A number of compounds already in use as medications for various indications substitute for ethanol at clinically relevant brain pathways, in particular, at gamma-aminobutyric acid (GABA) receptors. Nevertheless, although substitute medications have been recognized for heroin and tobacco dependence, patients with alcohol dependence are rarely offered an analogous approach. Benzodiazepines may have paradoxical effects, and abuse and dependence are known.
GABA-ergic anticonvulsants, helpful in treating withdrawal, have yet to emerge as effective in relapse prevention. Clomethiazole and sodium oxybate, the latter having been shown to be effective in relapse prevention, have incurred a reputation for dependence and abuse. However, data have emerged showing that the risk of abuse of sodium oxybate is lower than many clinicians had foreseen. For a condition where existing therapies are only effective in a proportion of patients, and which has high morbidity and mortality, the time now seems right for reappraising the use of substitute prescribing for alcohol dependence
As you can see, it has also not gone unnoticed that drugs like clomethiazole are abused and also bring with them problems of dependence. On the other hand, the message has not entirely got through to all researchers that drugs are drugs are drugs…………
Medications acting on the GABA system in the treatment of alcoholic patients. Caputo F, Bernardi M - Department of Internal Medicine, SS Annunziata Hospital, Cento (Ferrara), Italy.
Gamma aminobutyric acid (GABA) represents the major inhibitory neurotransmitter of the central nervous system. Ethanol as well as benzodiazepines (BDZs) and some anticonvulsant drugs directly affect GABAA receptors inducing similar anxiolytic, sedative hypnotic, and anticonvulsant effects.
Since BDZs have proven their efficacy in ameliorating symptoms and in decreasing the risk of seizures and delirium tremens, they are the drugs of choice for the treatment of alcohol withdrawal syndrome (AWS). However, due to their addictive potential and lack of safety when combined with alcohol, BDZs are usually not recommended for the maintenance of alcohol abstinence.
Other GABA-ergic medications represent potentially promising drugs useful in the treatment of AWS and in maintaining alcohol abstinence. Indeed, available studies have demonstrated that clomethiazole, gabapentin and gamma hydroxybutyrate (GHB) present a similar efficacy to BDZs in suppressing AWS.
In addition, current evidence also indicates that gabapentin and GHB do not have significant interactions with ethanol that render them safe to use in maintaining alcohol abstinence. Moreover, gabapentin and valproic acid may be beneficial in maintaining alcohol abstinence in alcoholics with psychiatric co-morbidity.
Pregabalin, neurosteroids, tiagabine, and vigabatrin need further clinical evidence of efficacy, safety and tolerability. Thus, given the importance of GABA-ergic mechanisms in the development and maintenance of alcohol dependence, and the very interesting results currently achieved, more research on GABAergic agents is warranted.
As a small aside, (GHB), also known as 4-hydroxybutanoic acid and sodium oxybate is categorized as an illegal drug in many countries. It is currently regulated in Australia and New Zealand, Canada, most of Europe and in the US. GHB has been used in a medical setting as a general anaesthetic, but has also been used as an intoxicant (illegally in many jurisdictions) or as a date rape drug.
If you were an alcoholic trying to get off the alcohol, which would you prefer – a gradually reducing supply of 1989 Beaujolais or a date rape drug?
There is one advantage of some of these drugs – some not all - over alcohol as the means of withdrawal and that is that they give the liver a chance to recover.
Side-effects
A glance at the eHealthme site which reports on the actual side effects reported by doctors as experienced by their patients describes common side effects as follows:
Female | Male |
Nausea | Death |
Fall | Fall |
Dizziness | Insomnia |
Insomnia | Condition Aggravated |
Headache | Convulsion |
Somnolence | Somnolence |
Vomiting | Headache |
Condition Aggravated | Weight Decreased |
Fatigue | Fatigue |
Weight Decreased | Nausea |
As of mid 2014 in the USA, Xyrem had caused 314 deaths; Oxazepam had caused 160 deaths; Vivitrol had caused 43 deaths; Revex had caused 1 death.
How it works
Why do these drugs produce hallucinations, visions, near death experiences etc?
All the drugs in this class are potentially addictive.
All of them produce sedative effects just like alcohol which they mimic. So ultimately the hallucinations being experienced in theory from these drugs is actually not caused by the drugs but by withdrawal from the drugs.
And here the experiences mimic those of alcohol withdrawal with delirium tremens, wild hallucinations and so on.
But Xyrem may produce hallucinations for a different reason. Xyrem is the sodium salt of γ-hydroxybutyric acid (GHB). The section on this drug should help in explaining why hallucinations occur with Xyrem
Ann Emerg Med. 1998 Jun;31(6):723-8. A tale of novel intoxication: seven cases of gamma-hydroxybutyric acid overdose. Li J1, Stokes SA, Woeckener A.
We describe seven patients presenting with combination substance abuse involving gamma-hydroxybutyric acid (GHB)……………. All patients presented with acute delirium and transient but severe respiratory depression. …….. Two findings are remarkable …... The first is the observation of a peculiar state of violent aggression present on stimulation of the GHB-intoxicated patient despite near or total apnea. .....The second is the observation of ECG abnormalities in several cases, including U waves in five patients. PMID: 9624312
References and further reading
[Driving under the influence (DUI)]
Observations
The table below shows the summary of the number of hallucinations according to eHealthme. The link provided with each drug takes you to the eHealthme site and shows the side-effects of each drug, as compiled from actual patient reports and experiences
Medicine |
Total number of hallucinations |
1 |
|
34 |
|
20 |
|
2 |
|
|
57 |
Related observations
Healing observations
- A Psycho-Spiritual Experience Ibogaine by KBF 017434
- Assessment of addiction severity among ritual users of ayahuasca 017555
- Ayahuasca-assisted therapy for addiction: results from a preliminary observational study in Canada 017553
- Coffee Consumption Decreases Risks for Hepatic Fibrosis and Cirrhosis: A Meta-Analysis. 027131
- Dr Duke's list of activity for the chemical Daidzein 017895
- Dr Duke's list of chemicals and activity for the Shallot 017969
- Dr Duke's list of Plants with Antialcoholic Activity 018406
- Dr William Sargant – The Initiation ceremony of the Macumba of Brazil and Orisha cult, from Nigeria and Dahomey 024397
- Hallucinogens and redemption 017557
- Involvement of the GABAA Receptor in Age-Dependent Differences in Binge-Like Ethanol Intake 020135
- Khristophorous Gallowglaich - Rebirth 016769
- Lindsay Lohan talks about how Ayahuasca has changed her life 017560
- No Boundaries Ibogaine by TPTB 017442
- Report on psychoactive drug use among adolescents using ayahuasca within a religious context 017556
- The efficacy of Liv-52 on liver cirrhotic patients: a randomized, double-blind, placebo-controlled first approach 022060
- The Emerging Role of Mindfulness Meditation as Effective Self-Management Strategy, Part 2: Clinical Implications for Chronic Pain, Substance Misuse, and Insomnia 023459
- Treating drug dependence with the aid of Ibogaine: A retrospective study in Brazil 017450
Hallucination
- A Psycho-Spiritual Experience Ibogaine by KBF 017434
- Acute psychotic symptoms induced by topiramate 029489
- Campral 018162
- Chlormethiazole withdrawal and hallucinations 005126
- Clomethiazole 005584
- Clonidine 005096
- Clonidine and alcohol withdrawal 005099
- Disulfiram and Antabuse 005697
- Dr Penny Sartori - Hallucinations are usually caused by pharmaceuticals in hospitals 014533
- From frying pans to fires 005136
- GHB withdrawal 005134
- Hallucinations from alcohol withdrawal 005124
- Hallucinations from withdrawal 005135
- Khristophorous Gallowglaich - Time stood still 016770
- Ondansetron 005699
- Oxazepam and Serax 002207
- Prazosin and Minipress 017867
- Revex Nalmefene 005125
- Vivitrol, Naltrexone and Revia 005127
- Xyrem 005430
Out of time
- A Psycho-Spiritual Experience Ibogaine by KBF 017434
- Khristophorous Gallowglaich - Overloaded into hell 016768
- Khristophorous Gallowglaich - Rebirth 016769
- Khristophorous Gallowglaich - Time stood still 016770
- Lindsay Lohan talks about how Ayahuasca has changed her life 017560
- No Boundaries Ibogaine by TPTB 017442
Enlightenment
In time
- A Psycho-Spiritual Experience Ibogaine by KBF 017434
- Danielou, Alain – On drugs you are possessed by the spirit being of the drug 022582
- GHB withdrawal 005134
- No Boundaries Ibogaine by TPTB 017442