Medications
Helping stop the cravings
Anti-addiction medicines are important for the treatment of drug and alcohol addiction for your loved one for many reasons. Since drug and alcohol addiction is a chronic disease that begins in the brain, Enterhealth Ranch and Enterhealth Outpatient Center of Excellence utilize anti-addiction medicines as a critical element of a comprehensive treatment plan personalized for each patient. Due to the powerful chemical changes that occur in the brain as the result of the injury from alcohol or drugs, cravings from deep inside the center of the brain drive each person to use, often overwhelming even the strongest logic and desire to quit.
Fortunately, amazing breakthroughs in drug and alcohol addiction treatment and medical scientific research have greatly facilitated long-term, successful sobriety by utilizing specific FDA-approved medications to shut down cravings in the brain.
A critical element in supporting recovery
As part of a comprehensive and personalized treatment plan, anti-addiction medications can help with the unpleasant drug and alcohol withdrawal symptoms and stop the cravings in order to promote healing.
The FDA approved Vivitrol in June 2006 for the treatment of alcohol dependence or alcoholism (as well as for the treatment of opioid addiction, heroin addiction and pain pill addiction in 2010). Vivitrol is an injection that is received in the gluteal (buttock) muscle once a month. During that one-month period, a medication called naltrexone is slowly released into the bloodstream.
Vivitrol (long-acting naltrexone) basically helps to prevent relapse to alcohol/opioid addiction by causing three things to occur:
- It decreases cravings for alcohol by up to 90%.
- If the patient does drink alcohol (or use opioids), Vivitrol blocks the euphoria (or the “high”). Therefore, when the patient is on Vivitrol, they can’t get drunk or high. When they do drink alcohol, they still have symptoms of intoxication, like driving or walking poorly; however, they do not benefit from any of the positive (pleasant) effects of alcohol. Consequently, because it is very frustrating to continue drinking when on Vivitrol, they are more likely to stop. Of course, your loved one, along with most alcoholics, are going to “test” whether they can get high (drunk) on alcohol or not. When they find out they can’t, they will say, “OK, the doctor was right. I’ll go listen to my counselor. There’s no use testing it anymore, so now I’m just going to go learn how I can stay sober.”
- Vivitrol prevents the first drink from “priming the pump” for more alcohol. Unlike alcohol use without Vivitrol – in which someone will have one beer, which then seems to set off a “cascading compulsion” to have 5 or 10 more beers in that sitting – the Vivitrol blocks that “priming” effect and the patient may only have half of a beer in total. By only having half of a beer, which does not even cause a buzz, the patient is able to maintain appropriate judgment and stop drinking, leave the situation and call a therapist or sponsor to ask for help. This “new” healthy behavior severely limits the “severity of relapse” after the attempted sobriety and frequently allows the patient to keep the relapse to a “slip” rather than it causing a full-blown relapse.
A common analogy to this situation (described in the third bullet above) is patients on a diet for weight loss. The patients may do “really well” on the diet for two weeks, and then on a Saturday evening, go for that pint of ice cream in the freezer believing they will only have one spoonful, then end up having the entire pint. Once the diet is “broken,” they give themselves permission to binge on other high-caloric foods. Either an hour later or, for certain, the next morning, they truly regret breaking their diet and wish they would have been able to have a similar agent to Vivitrol that would curb their appetite and not let them enjoy the ice cream if they did eat it.
It is important to understand that although Vivitrol was only approved for use for alcoholism in the summer of 2006, the medication within the injection – naltrexone – has been approved for use in treating alcoholism since 1994. However, the problem with taking naltrexone orally (by mouth) is that patients with any chronic illness, who have to take medications on a daily basis, many times forget or stop taking the medication for a variety of reasons. Alcoholism is a chronic medical illness and alcoholics are not immune to the same “difficulty” issues consistently experienced by anyone with other chronic medical illnesses (i.e. diabetes) in taking these medications on a daily basis.
Ensuring that the oral naltrexone is taken on a daily basis requires high levels of clinician and family diligence to ensure doses are not skipped or the patient does not stop taking the anti-addiction medication altogether. The patient might find that taking the oral naltrexone works so well in stopping from drinking alcohol that he or she might “clandestinely” stop taking the oral medication without telling their addiction support system or physician. Consequently, the patient has a much higher chance of relapse without the oral naltrexone.
On the other hand, with Vivitrol, patients and their supporting family members only need to remember to go once a month their patients’ physician’s offices to receive the Vivitrol. After that, no one has to worry about the patient adhering to the medication compliance program component of the alcohol addiction treatment for the next 30 days.
An addiction patient’s response to Vivitrol can usually be seen within the first 2-3 days of starting the first injection. Consequently, Vivitrol works very quickly and has very few side effects. The primary side effect is nausea that occurs, if at all, in the first 2-4 days during the first injection period. After that time period any nausea is not usually an issue.
Patients on Vivitrol are overwhelmingly positive about its anti-addiction effects. In theory, those suffering from alcohol addiction should not be actively drinking when they receive the initial injection of Vivitrol. Vivitrol should be used as part of a comprehensive alcohol addiction treatment program. It is very important that the family members and physician strongly encourage the patient to participate in a comprehensive, intensive treatment program while taking Vivitrol or other appropriate medications as part of the addiction treatment.
Many patients will have thoughts such as, “Doctor, you are giving me a shot; therefore, I don’t need to go to these other alcohol addiction treatments. Going to the treatment programs and trying to change my lifestyle is too difficult, and I would rather just take the easy solution and merely have to take the Vivitrol injection once a month or the injection plus other anti-addiction medication.”
Because these types of thoughts are common for all alcoholics, it is very important that family members and the physician/therapist strongly encourage and continuously check up on the patient’s progress and attendance with the additional addiction treatment compounds. As noted above, these additional treatment compounds teach patients the appropriate coping skills to allow them to learn to live in their normal environments while dealing with the stresses using healthy coping skills rather than using alcohol or drugs as their primary coping skill.
Other Relevant Safety Information for Vivitrol/Naltrexone
Another benefit to Vivitrol is that it has very few side effects. Specifically, as previously mentioned, the primary side effects are nausea (which only occurs sometimes but, if it does occur, usually only occurs during the first 2-3 days of the first injection), occasional headache, some tenderness at the injection site for a short time afterwards, and some sedation. All of these symptoms are mild in most cases and much less toxic or evident than are the side effects of alcoholism. Consequently, Vivitrol is very safe, well tolerated (meaning it has few side effects), and is not addicting.
One of the reasons Vivitrol has few side effects is the unique way it gets into the bloodstream. By being injected into the muscle and then by being released into the bloodstream from the muscle, the naltrexone medication initially avoids going through the liver before it goes into the rest of the body. One of the liver’s main functions is to break down different substances (including medications). When any medication is able to bypass the liver initially, less of it is destroyed, thus more of it is available to be used by various parts of the body. Therefore, theoretically, a patient needs a much lower dose to be effective.
Fortunately, this is the case with Vivitrol. Remember that Vivitrol is just a time-released naltrexone. If naltrexone is taken by mouth (orally), it’s necessary to take 50 mg/day for 30 days (length that Vivitrol lasts in your body) = 1,500 mg of oral naltrexone for 1 month. At 50 mg/day oral naltrexone is safe, well tolerated, and has the same types of side effects as described above for Vivitrol. Because Vivitrol bypasses the liver, only 380 mg/month of Vivitrol is needed to treat alcoholism. Consequently, the fact that almost a 70% smaller dose of naltrexone is needed through the use of Vivitrol in the patient’s body each month may account for the minimal side effects experienced by most patients on it. Also, as an added bonus, because of the way that Vivitrol gets into the bloodstream, not only does it require less than 25% of the oral dose, but it also provides four times the brain levels of the oral dose, so more medication is available to help the brain.
In addition to the nausea issue mentioned above, there is what the FDA calls a “black box warning” on the labeling on the package insert for both Vivitrol and naltrexone. This black box warning merely suggests that one might get significant liver-related problems if Vivitrol or naltrexone is used for a long period of time without appropriate monitoring of the liver’s functions with blood tests. In fact, the black box warning for Vivitrol specifically states that there is no evidence of toxicity with Vivitrol. The reason for the black box warning has nothing to do with Vivitrol or naltrexone in alcoholics. At one point, a study was done on obese people weighing more than 300 pounds who already had a large “fat load” hitting the liver, thus the liver was already slightly damaged. The people in the study were given oral naltrexone to see if it could help them lose weight by affecting the feeding center in the brain, thereby decreasing their food intake. However, the patients in the study did not receive 50 mg per dose of naltrexone, which is the normal oral dose for alcoholics. Instead, they received six times the normal dose of naltrexone, or 300 mg per dose each day. So, with six times the normal oral naltrexone dose given to these overtly obese patients, some of them developed elevated liver tests, yet nobody died. They just had elevated liver tests.
Consequently, because of the study, it is important to check baseline liver tests for new patients prior to starting Vivitrol or oral naltrexone and then continue to monitor it by getting a simple screening liver blood test three to four times a year. It is important to remember that naltrexone is a very safe medication, and it is infinitely less toxic to the patient’s body than is continuing the alcoholism. Alcohol is severely toxic to one’s liver and the rest of the body. Consequently, the use of Vivitrol will help an alcoholic to stay healthy in the long run, as it effectively prevents him or her from using alcohol.
How Does Vivitrol Work?
Addiction researchers hypothesize that Vivitrol (naltrexone) works by blocking the interaction or the stimulation of the dopamine system (the body’s main rewarding system) by the alcohol molecule. When someone drinks alcohol, the alcohol molecules get into the bloodstream through the stomach. The molecules, which are toxic the body’s cells, travel throughout various organ systems, killing all kinds of cells as they go.
It is when these molecules reach the brain that they stimulate a variety of neuroreceptors with each different set of receptors basically causing different effects. Activation of some receptor systems cause the drinker to get sleepy (or sedated), yet others cause them to stop breathing resulting in death (alcohol overdose or poisoning). Vivitrol (naltrexone) is thought to block the link between the dopamine system (pleasure or reward system) and the internal endogenous endorphin/enkephalin (opioid) systems.
Luckily, because we all have dozens of different types of neurotransmitter systems (brain chemicals) and these have a myriad of interactions with each other, even though Vivitrol can block the high/euphoria produced from alcohol (and opiates by the way, i.e., Vicodin/OxyContin), one still can experience other good/positive feelings while taking this revolutionary anti-addiction medication. For example, when someone drinks alcohol, he can’t get a high, he can’t get drunk, but at the same time, if he gets a good grade in school, earn a bonus at work, or accomplish a full year of sobriety, he can still experience “good feelings.” Consequently, when a patient is taking Vivitrol, his or her dopamine system is still functional and continues to help him or her feel good in a “normal” fashion.
Vivitrol is made up of molecules that are called microspheres, which are dissolved in a liquid and injected directly into one cheek of the buttocks (alternating sides each month). The actual Vivitrol microspheres, when dissolved in the injection solution, fill up like balloons and get “puffy.” As an analogy, picture these hydrated Vivitrol molecules as “spherical chocolate chip cookies” with big “chocolate chips” or chunks in them. Once injected, any little “chocolate chips” that are on the outside of the “cookie” that are in the body go right into the bloodstream and the patient gets a nice healthy dose of naltrexone right away. And then over the month’s time that it is in the body, the entire spherical “chocolate chip cookie” breaks down or erodes and the “chips” on the inside come out and go into the bloodstream in a very smooth fashion, so that one receives the appropriate dose of naltrexone evenly over the next 30 days.
The major scientific breakthrough of Vivitrol delivering this very effective medication for alcoholism for 30 days without stopping is a huge advance for all of us, including family members and friends, with helping the patient battle of this devastating, life-threatening disease. The fact we now have a “shot” for alcoholism and opiate addiction will change many people’s view of alcoholism from that of merely a “sin, moral weakness or character flaw” to a major medical illness that is very treatable with a high degree of successful recovery.
Summary of Vivitrol’s Benefits
Remember the active ingredient in Vivitrol is naltrexone. The FDA approved oral naltrexone for treating alcoholism in 1994 and for treatment of opiate addiction in the 1970s. Consequently, it is already known to be safe and effective. Therefore, all of the benefits and effects of naltrexone on an alcoholic or opiate addict (decrease in craving by 90%, blocking the ability for alcohol to produce euphoria or a “high” so one cannot “get drunk”, and significant reduction in the amount of alcohol or opiates used, if drinking does start again) are seen with Vivitrol, as well.
However, when patients are taking regular oral naltrexone, they must take it every day for it to be effective. If they do take oral naltrexone every day, then they will have a very high chance of staying sober. But because oral naltrexone is so effective, patients could frequently have “weak moments” and convince themselves they really are be able to drink normally again, so they will then stop taking the oral naltrexone (in many cases, they will pretend to everyone else that they are still taking it). Oral naltrexone’s positive “anti-alcohol” effects wear off after three days, then their cravings return and they can get “high” or drunk again.
Consequently, the breakthrough at the heart of Vivitrol’s success is that, in addition to delivering all of the benefits of oral naltrexone, it also addresses the “critical” compliance issue in this disease in that you cannot stop it, even though you are having a “weak moment.” For many alcoholics and opiate addicts, these weak moments will pass. And when they do, the patients on Vivitrol in the Enterhealth program are very appreciative of the fact that they are still sober and still on a medication that will help keep them that way.
Vivitrol’s Positive Impact and the Family of an Alcoholic
Another critical success factor for the use of Vivitrol for the treatment of alcoholism and opiate addiction is that the patient’s family and overall support system can significantly influence their loved one’s usage of the drug. Because of the compliance benefit mentioned above, this ability of the family members/support system to be able to encourage their beloved patients to get to their Vivitrol injection appointment each month is critical in relapse prevention.
Once Vivitrol has been prescribed and your loved one has received the injection, your family now knows that, for the next 30 days, the patient will not be able to feel “intoxicated,” “drunk” or “high.” In other words, your loved one will not be able to experience any euphoria or positive benefit from alcohol or opiate use. Additionally, cravings will decrease by 90%, in general, and if he or she does take a drink, there will be much less compulsion to have more.
In the extensive research and clinical use of Vivitrol, in addiction treatment practices, physicians have found that once a family understands these significant benefits of Vivitrol, in addition to the enhanced compliance issue, that they begin to feel some “control” returning to their very chaotic, “out-of-control” home environments experienced in living with or interacting with an active alcoholic. Vivitrol is the first anti-addiction medication for alcoholism and opiate addiction that provides this sense of “control” for the family members, as the patient cannot change the effects of the medication once the injection is received.
As soon as the patient’s family begins to feel this reassurance (control), they begin to realize just how much fear and uncertainty their loved one/patient has been living with in the past. The family/support system likely worried if the patient was really taking the anti-addiction medication as directed or even at all, worried if and when the patient would relapse again, and worried if “the chaos” would return. Consequently, the use of Vivitrol can lift a huge burden of “worrying” and concern from the family members/support system’s shoulders. Not surprisingly, the alcoholic’s family/support system is a tremendously strong and determined ally of the addiction specialist/physician in helping to ensure the patient makes the follow-up Vivitrol injection appointments. The family members and other supporters of Enterhealth patients quickly realize that if they help the alcoholic or opiate addict to just get to treatment every 30 days, Vivitrol can make a tremendous difference in all of their lives.
Suboxone is the first opioid (narcotic) medication approved for the treatment of opioid addiction in an office-based setting. Suboxone also can be dispensed for “at-home” use, just as any other medicine for other medical conditions. The primary active ingredient in Suboxone is buprenorphine. Initially developed to treat pain, buprenorphine was adapted for use in treating opioid addiction in cooperation with the National Institute of Drug Abuse (NIDA) and was approved by the FDA in October 2002.
Overview of Suboxone and its Benefits:
Buprenorphine is a partial opioid agonist, meaning its opioid effects partially mimic those produced by full opioid agonists, such as oxycodone or heroin, and partially mimic those produced by opioid antagonists, such as naltrexone. Two formulations were initially approved: Suboxone and Subutex. Recently, two more have been added under the brands Zubsolv and Bunavail.
The first, Suboxone, contains buprenorphine and naloxone, an opioid antagonist designed to discourage patients from dissolving the tablet and injecting it. Consequently, most practitioners only prescribe Suboxone to their narcotic-addicted patients, as it has even less potential for diversion (being sold on the street) or other misuse.
- Subutex is rarely prescribed in clinical practice; therefore, the discussion here will be limited to Suboxone, but most of the information prescribed here is relevant to Subutex as well.
Suboxone is used to reduce illegal opioid use and to help patients stay in treatment by blocking the effects of opioids, decreasing cravings, and suppressing any major symptoms of withdrawal. Most narcotic addicts seem to benefit from Suboxone regardless of their histories of opiate addiction.
Suboxone is safe, effective, and is a revolutionary step in the treatment of narcotic addiction. It can be easily used in both the withdrawal stabilization (detoxification) and maintenance phases of opiate addiction treatment. Also, because of its ease of use and excellent safety profile, its use by the growing number of primary care physicians who are screening for and recognizing narcotic addiction in their practice populations should make a very positive impact in the treatment success rates for narcotic addicts.
Suboxone has several advantages over other opiate addiction treatments both for withdrawal stabilization (detox) and its long-term maintenance uses. Most of the advantages to this anti-addiction medication are due to its chemical structure.
With these receptor functions (full agonist, antagonist and partial agonist) in mind, one can understand how methadone (which is a full agonist) would bind to the opiate receptors and produce the full response that would help patients reduce cravings, but it also might give them a high. When Suboxone (a partial agonist) binds to the receptor, it completely satisfies the receptor that there is an opiate there, but it doesn’t produce any high or euphoria. Consequently, its addictive potential is extremely low. Again, the receptor is activated with Suboxone, which significantly reduces the cravings for opiates that then, in turn, significantly prevents the chances of a relapse – but it also acts as a receptor antagonist, so normal agonists are not able to elicit the normal response. So, if the patient is taking Suboxone and then tries to “shoot up” heroin to get a high, Suboxone blocks the heroin from causing a high because the heroin can’t get to a receptor. Consequently, the patient doesn’t get a high, which is a very disconcerting feeling for the opiate addict who has just spent a great deal of money on an addictive drug that gave him or her no effect.
Because of the chemistry involved at its brain receptor, Suboxone has several inherent safety mechanisms:
First, it is very safe in an overdose situation because of the way it interacts with the receptor. If the patient tries to take too much of the Suboxone, it actually becomes a full antagonist and “punishes” the patient by putting him or her into withdrawal. This is quite the opposite of most agonists (such as heroin or Lortab) where the more the patient takes, the more “high” the patient gets. Yet eventually, with these full agonists, not only does the patient get a high, the patient also shuts down his or her breathing and dies inadvertently from not being able to breathe. However, because of its different chemical structure, if the patient does take an overdose of Suboxone, he or she will go into withdrawal and breathing will become extremely hyperactive rather than shut down, so the patient won’t die. The patient will be very uncomfortable – but won’t die.
Additionally, because of the way Suboxone interacts with the receptor – the medication has a very long duration of interaction – it means the patient can easily take it once a day or sometimes every other day and still achieve a certain “normal” feeling where the patient does not have cravings for opioid drugs. Also, if the patient forgets a dose on a particular day, he or she will not go into a full opiate withdrawal, so the patient can wait until the next day when he or she can get Suboxone medication.
- Because Suboxone binds so tightly to the receptor, as mentioned above, if the patient tries to “shoot up” a narcotic or take narcotics to get a “high” during a “weak” moment, the patient won’t feel any of those effects, and consequently, he or she will be less likely to have a relapse in the future when on Suboxone.
Finally, not only is buprenorphine inherently safe on its own, the medication Suboxone is actually a combination of buprenorphine and naloxone. Naloxone is an opiate antagonist like naltrexone, but it is a very short-acting one that only works if injected intravenously into the veins. Consequently, the naloxone, when taken by mouth with the buprenorphine in the Suboxone tablet, does not cause any withdrawal symptoms or even cause any uncomfortable feelings for the patient.
So not only is this combination medication a deterrent for patients on the anti-addiction medication, it is also a deterrent for patients trying to steal the medication and use it on the street. Because the naloxone is part of the Suboxone tablet, the street value of Suboxone is very low; consequently, it is much less likely to be stolen. This is not the case with methadone or other standard agonist narcotics, such as Lortab or OxyContin.
The combination of these four main attributes of Suboxone, plus many others, makes it an ideal and even a revolutionary anti-addiction medication for treating patients with opiate addiction.
Guidelines for the Use of Suboxone in Opiate Addiction
In regards to Suboxone dosing, it is very important that Suboxone is started for the first time when the opiate addict patient is in withdrawal or is in detoxification. If one were to try to start an opiate addict on Suboxone while he or she is still comfortable, when the opiate is still in patient’s system and thus not in withdrawal, the Suboxone will act like an antagonist and put the patient into chemical withdrawal immediately. However, asking the opiate addict to wait for several hours or for the appropriate time period until withdrawal begins, once the patient is in mild to moderate withdrawal and begins Suboxone, it acts as an agonist at the receptors and the patient calms down and feels much more comfortable.
Usually the first 2-3 days of being on Suboxone and adjusting it to the proper dose for the individual patient is the “rockiest time.” Once the patient is on a stable dose of Suboxone, he or she is very comfortable and has no cravings, no desire to use, and actually feels quite “normal.” It is a very positive feeling for the patient to feel “normal” and not feel desire for narcotics. These feelings allow the addicted patient to participate positively in a residential or an outpatient rehab program where he or she can finally learn the coping skills needed to maintain a sober lifestyle going forward.
Once the patient stabilizes on Suboxone (usually within 5-7 days of starting it), it is up to the patient and the physician as to how long the patient needs to be on the Suboxone. It is generally accepted that most patients will need to be on it for approximately 9 months to 1 year, as a starting point, in order to allow their systems to get stabilized, and then taper off slowly while they continue other aspects of their addiction treatment programs.
Vivitrol
Once the patient is off Suboxone, being on Vivitrol for at least another year to 2 years is a further deterrent to relapse. Consequently, once the recovering addict has tapered off of Suboxone under the direction of a physician for approximately 2 weeks, all patients should then get on Vivitrol (time-released naltrexone). Prior to the advent of Vivitrol, oral naltrexone was frequently prescribed for patients when they stopped methadone or other narcotics, because once they are taking naltrexone, if they try to use an opiate, they won’t feel any high or euphoria. With Vivitrol, there is a much less likely chance they will try an opiate during a “weak” moment in their addiction recovery process, say during a time of high stress, because they know that the opiate will not help them deal with the particular stress if it does not provide any high/euphoria or relaxation response.
However, in addition to Vivitrol, oral naltrexone has also been successfully used to treat narcotic addiction. Once-daily ingestion of a 50 mg tablet will almost completely block any narcotic that a narcotic addict may attempt to use at the receptor site. Consequently, naltrexone prevents any euphoria or other benefit that an addict may hope to achieve through a relapse. Because daily administration is required, it is best to have the patient take naltrexone under direct observation to enhance compliance. There is strong data proving that Vivitrol significantly enhances a sobriety program when used with impaired professionals who are motivated to stay sober (physicians).
Whether oral naltrexone or Vivitrol is used with a patient, he or she needs to continue to stay engaged with the rest of their comprehensive addiction treatment programs. Remember, anti-addiction medications are only one component of Enterhealth’s comprehensive plan.
Campral (generic name: Acamprosate), a medication widely used in Europe since the late 1980s to reduce alcohol cravings in alcoholics who have quit, was approved by the U.S. Food and Drug Administration in 2004 to treat alcohol dependence in the United States.
Although the precise mechanism of action or “cellular target” of Campral is unknown, it appears to decrease cravings primarily by restoring the balance in certain neurotransmitter pathways (most likely GABA + Glutamate) that have become altered by chronic alcohol abuse.
The GABA neurotransmitter system in the brain is a very important control system that is responsible for “calming you down” and helping you to relax. Because it calms you down, it is referred to as an “inhibitory” system. The Glutamate neurotransmitter system in the brain is just as important as the GABA system, but it has the opposite effect on the body: it causes you to get energized (referred to as your “excitatory” system).
Another way to look at these two important systems is to take an analogy of a car. The GABA system is like your brakes, allowing you to slow down, while the Glutamate system acts like the accelerator. If you have a car with only one system or the other, it is not a very functional car – you need both systems to balance each other out in order to be able to use the car effectively.
So, when anyone drinks alcohol (not just an alcoholic, but anyone), Campral stimulates the GABA system in the brain and the person becomes sedated and relaxed (the brakes slow you down). At the same time, the Glutamate system is suppressed (so the accelerator is not being pressed). When the alcohol wears off, your excitatory system “rebounds” and you feel more irritable, agitated, and may find it difficult to sleep (remember: the brakes are now off and the accelerator is being pushed).
Now, if you are an alcoholic, you have been drinking regularly in most cases and you develop tolerance – meaning you require more alcohol to achieve the same effect. What tolerance basically does to the GABA/Glutamate systems is that it modifies both in some respect. But, at the end of the day, an alcoholic must consume more alcohol to “put on the brakes” (slow down and relax). Then when the alcohol wears off, the Glutamate system has become somewhat “turbocharged” and the result is that the accelerator seems to be “pressed to the floor” resulting in quite severe withdrawal symptoms in many cases.
Alcohol Withdrawal Symptoms
If you think about it, alcohol withdrawal symptoms are the result of many body systems being stimulated – blood pressure and heart rate are increased, and the drinker is irritable and has difficulty calming down or going to sleep. Even after the first 5-6 days of alcohol withdrawal have passed and the more severe withdrawal symptoms have gone away, the Glutamate system still seems to be “overly active” and the GABA system still seems to underperform. The result is the “post-acute” alcohol withdrawal phase, when the alcoholic remains irritable at times, has persistent insomnia, and has difficulty concentrating, which are all symptoms of a hyperactive accelerator and somewhat “weak brakes.”
Thankfully, in the “post-acute” alcohol withdrawal phase, these symptoms are only intermittent. Recovering alcoholics feel fine at times, but during periods of stress, they seem to get “extra hyper.” It is during these “extra hyper” times that they experience some combination of these symptoms, which then can produce alcohol cravings, which then can increase the chance of a slip or even a full relapse.
What Campral appears to do (after a 4-6 week period of taking it on a daily basis) is restore the normal balance of the GABA/Glutamate interaction. In other words, it seems to begin to restore the brake system and accelerator back to their normal functioning levels. Consequently, alcohol addiction patients on Campral report (after the first 4-6 weeks of being on it) they begin to feel calmer, can handle stress more effectively, are able to concentrate and focus better, as well as have decreased cravings or desire for alcohol.
Unfortunately, these significant improvements for the alcoholic patient take at least a month to begin to appear. Sometimes it is very hard for alcoholic patients to wait that long because they are so accustomed to “instant gratification” that they get impatient and stop the anti-addiction medication prematurely. Also, when the positive effects appear, they usually develop slowly over 2-4 weeks and so there is no overt, pronounced effect. But one day, 6-10 weeks after starting the Campral, alcoholic patients report they notice they are just “a lot better,” are more relaxed, sleeping better, and have significantly reduced alcoholic cravings.
Once the alcoholic patient is convinced to take Campral with the above facts and reasoning, in combination with a medical evaluation by an addiction specialist, the next challenge with Campral is actually taking the medication. Unfortunately, Campral is not well absorbed by the body’s gastro-intestinal tract. In fact, only 10% of each pill is absorbed. So, in order to get the 200mg/day of Campral into the patient’s bloodstream that is needed to begin healing the GABA/Glutamate systems, the patient needs to take six tablets per day (1998 mg) for the medication to work. Addiction patients usually take 2 tablets 3 times a day, but it is difficult for anyone to take any medication 3 times a day without forgetting that middle-of-the-day dose. Therefore, Enterhealth usually prescribes 2 tablets 3 times a day for the first 2 weeks and then changes to taking 3 tablets twice a day thereafter, not requiring patients to take the lunchtime or mid-day doses.
A related issue that comes up for some addiction patients is they say, “Doctor, I don’t want to take 6 tablets each day. That is too much medication. I don’t want to put anything in my body that will hurt me or, I don’t want to get addicted to Campral.” Obviously, these arguments are ludicrous as this anti-addiction medication will give them a great chance to stop using alcohol – a very toxic substance that is already killing them. Also, Campral is not toxic at all to the body and, like Vivitrol or naltrexone, it is not addicting nor can it be abused. Also, once most patients understand the poor absorption of Campral is the reason that they have to take 6 pills a day, they usually do not mind taking that many pills a day.
Finally, some alcoholics are resistant to taking medication to help them because they are not truly committed to stopping alcohol. Regardless, they can be strongly encouraged (and required, if possible) to take the medications and then encouraged to work through their ambivalent feelings about starting in a treatment program and/or attending AA meetings while the medication is starting to help them feel better. Remember, Campral, just like any other addiction medications, needs to be taken as one part of a comprehensive addiction treatment plan.
Fortunately, the side effects of Campral, like Vivitrol, are minimal. The main one is diarrhea, and this is quite infrequent, especially after the first 1-3 days of taking it. If diarrhea does occur, over-the-counter medications, such as Imodium, are very effective. Other even less common side effects are nausea, itching and intestinal gas. Also, Campral, like Vivitrol, does not interact with other medications, so it can be added to just about any current medication regimen without concern, as long as the patient’s doctor is aware of all medical conditions and other medications the patient is taking.
Most patients stay on Campral for at least a year and a half and then, depending on how they are doing in their recovery program, they and their physician can consider and discuss discontinuing it.
From a scientific standpoint, 14 out of 16 controlled clinical trials in European countries have demonstrated evidence for its effectiveness, showing that acamprosate-treated patients have a significantly greater rate of treatment completion, time to first drink, and abstinence rates than patients treated with a placebo.
Disulfiram (Antabuse®), a sensitizing or deterrent agent, was approved by the FDA for the treatment of alcoholism in 1951. It has been used as an aid in managing chronic alcoholic patients who want to remain in a state of enforced sobriety so that they can participate in residential, outpatient treatment and 12-step programs effectively.
Disulfiram produces sensitivity to alcohol that results in a highly unpleasant reaction when the patient taking it drinks even small amounts. It does this by interfering in the alcohol enzymatic metabolism (breakdown) pathway resulting in an accumulation of a chemical (acetaldehyde) in the blood. This toxic by-product of normal alcohol metabolism produces a complex of highly unpleasant symptoms, including intense nausea and vomiting, sweating, flushed skin, throbbing headache, respiratory difficulties, blurred vision and confusion.
Antabuse has a valid place as an integral part of certain recovery programs. However, because of its toxic reactions, it does have some safety issues – although they are much less concerning than the safety issues related to continued alcohol use. Because of these safety issues, it is not typically used as a first-line treatment for alcoholism anymore. Rather, it is a medication to be used only if all other standard treatments fail, or it can be added to other pharmacological strategies, such as adding it to Vivitrol/Campral or Campral by itself.
When Antabuse is used, it is very important that it is given to the patient under a monitoring situation. The patient needs to be watched while taking it each morning, and the patient’s mouth should be orally inspected after swallowing each tablet to ensure compliance. If the compliance is ensured via a visual monitoring (observation) program, Antabuse can be very effective when used as a component of a comprehensive addiction treatment program.
Unlike Campral, however, Antabuse acts only as a deterrent; it does not heal any of the damage caused by the alcoholism. The usual dose of Antabuse is 250 mg/day, and liver function blood tests should be obtained by the patient’s primary care physician on a quarterly basis (4 times/year).
One of the complications of taking Antabuse is that it can cause the typical toxic reaction even with very small amounts of alcohol, even if they are taken accidentally. Consequently, a patient on Antabuse has to be very careful to not use certain alcohol-containing products (such as perfume, mouthwash) or to use them very carefully. Also, certain sauces for food can contain small amounts of alcohol and cause a reaction. However, if the patient is carefully observant of their environment, these hazards can be easily avoided.