Opioid Replacement Therapy

In a modern world there is no country that wouldn’t have a problem with drug addiction. In China, Arab world and some other countries use and distribution of drugs is punishable by death.  However, the problem of drug abuse is still there. In some European countries (for example, Switzerland, Netherlands) where the government is very concerned about the problems of human rights violation, especially regarding people’s right to control their own lives, people addicted to drugs are given an opportunity to be treated from drug addiction free. But if a person decides to continue to be on drugs, the government provides him an opportunity to use drugs not in the street, but in specially organized places, where not only the sterile syringes but even the qualitative drugs are assured.  Indeed, for some degree these measures of drug addiction control help to reduce the risks of possible life threatening complications, but from the other hand they are neither able to decrease the number of drug users nor to improve quality of their lives. Nowadays there are few ways to manage the problem of drug addiction.

methadone opioid replacement therapyOne of them is a substitution therapy. Its aims are:  take the drug addicts out of the streets, keep them out of painful withdrawal syndrome, help them to retrieve an ability to control their behavior, and make them able to work again. To achieve these goals the patient should continue taking prescribed opioids under strict medical observation for extended period of time.  That therapy helps to "calm down" the brain. The difference between the state of “high" when the level of opioids in addict’s brain is many times higher than normal ​​ and the state of withdrawal, when the brain is starving for previously spent opioids gradually disappear . Theoretically the idea of substitution therapy makes sense and can be considered as a phase of transition from uncontrolled use of opioids to regulated one with gradual dose reduction down to zero. But unfortunately the method of substitution therapy has several drawbacks which make its practical use rather dubious.

The drawbacks are:

1. The risk of abuse of substituent.

2. The risk of using the illegal opioids in combination with opioid substituents.

3. During the course of treatment the dose of substituent may be increased instead of being supposedly reduced.

4. Uncertainty of treatment period.

5. Creation of a hard core physical dependence on opioid substituent in case of extended use with the development of expressed and prolonged withdrawal syndrome.

Methadone

In order to solve these problems many scientists, research institutions, pharmaceutical companies have been working hard for the last 30 years.  The first drug for substitution therapy was Methadone. It was synthesized during the WW 2 in Germany. Since the sixties of the last century Methadone is used in substitution therapy. It’s a long-acting opioid, which administered orally doesn’t cause expressed opioid intoxication, but is strong enough to block the withdrawal syndrome. Nowadays methadone programs are widely used around the world. However, Methadone has serious side-effects: drowsiness, lethargy, impact on appetite, negative effects on the liver, the risk of overdose, the possibility of intravenous injections, the possibility of concurrent use of heroin and methadone.  And what is most important is that after 1-2 years of use of Methadone the patient loses the ability to leave the drug by tapering the dose off to zero without special medical help. The withdrawal symptoms from Methadone are much more severe and prolonged than that of from heroin. The classical scheme of drug detoxification which includes hypnotics, analgesics, and sedatives can’t protect the patient from severity of methadone withdrawal. The problem can be solved either through the rapid detoxification under total anesthesia or a through the long lasting and pretty racking process of gradual dose reduction. It is easy to start with Methadone. But it is very hard to leave it. The necessity to solve the problem has led to the emergence of a new substitution drug - Buprenorphine.


Buprenorphine

Buprenorphine is a partial agonist - antagonist to opioid receptors. This means that it may produce effects characteristic to typical opioids:  euphoria, analgesia, pupillary constriction, respiratory depression, obstipation or it may cause anti-opioid reaction similar to abstinent syndrome: muscular pain, diarrhea, nausea, vomiting, goose bumps, watery eyes, yawning, sneezing. What effects prevail depends on the moment Subutex (Buprenorphine) is taken. If it is taken in a state when opioid receptors are not occupied by heroin or Methadone, Subutex (Buprenorphine) affects them as an opiate and its opiate effects  emerge. But if the opioid receptors have been previously occupied by highly potential opiates like Heroin or Methadone, the opioid antagonist properties of Subutex precipitate the withdrawal syndrome.

Nowadays Buprenorphine is the best drug for substitution therapy.  It's not as heavy as Methadone. It doesn’t cause overdose. It doesn’t accumulate. It is not hepatotoxic. But if it is taken intravenously it may produce expressed euphoric effect. That is why Buprenorphine is potential for abuse. To exclude that possibility the 2mg of Naloxone were introduced into a tablet of Subutex (Buprenorphine). Naloxone is a pure opioid antagonist and being taken intravenously causes immediate unpleasant reaction similar to withdrawal. The modified Buprenorphine mixed with Naloxone is called Suboxone

 

Substitol

substitol i.v.Substitol – is one of the major disappointments in attempts to find the best drug to replace heroin. The chemical basis of Substitol is Morphine sulfate, a strong opioid, which is put in microbeads for controlled release into blood stream during 24 hours. Morphine itself is very close to natural neurotransmitters. That is why it is usually very well perceived by the patients. The problem is that you always want it a bit more than you need it. In that connection, the desire to take the higher dose or use the substituent intravenously for a stronger euphoric effect is a major issue of control of Substitol use. It isn’t a secret that many patients consider Substitol as a drug, not as a medicine. Having tried Substitol intravenously even once any heroin addict would say that it is much better, cleaner, stronger than heroin, which, as a rule, is numerously diluted by paracetamol, glucose, or something else. Due to the fact that Substitol from the drug clinics is handed out to the patients for several days ahead, and it is on their liability to take it as prescribed, the new epidemic of Substitol abuse has emerged. In Austria the green capsules of Substitol of 120 mg can be bought for 20 euros, the red ones of 200mg for 25 euros.  And you can easily buy Substitol in the street. Many addicts enter the Substitol treatment programs not because they honestly want to leave heroin, but simply because they don’t want to spend money on buying heroin in the street and continue to use high quality opioid which they can get from the doctor free. Within short period of time the tolerance to Substitol increases, the previous effects even after receiving Substitol intravenously weaken, the increased dose is required. The patient begins to beg the doctor for the higher doses, blackmails him that in case of being denied he will return to heroin. The doctor is forced to give him the maximum dose. But soon after even that dose is not enough, and the person starts buying Substitol in the street. We had the patients who were on 1600-1800mg of Substitol intravenously daily.  substitol abuse i.v.At such high doses a person is completely out of control, he is terrified by the idea to be left without next dose of Substitol . Everyone knows how torturous the withdrawal from heroin is, but the withdrawal from Substitol is many times harder. Excruciating pain, sneezing, vomiting, diarrhea become unbearable just few hours after the last short. The symptoms usually last for about 3-4 weeks.  Naturally, no one is able to sustain that condition.  And again there are two options: the Rapid Detoxification under total anesthesia or gradual dose reduction for 3-4 months.  The second option is always rather dubious. Usually it works like that: one step forward (for example:  minus 200mg) in one week and then two steps backwards (plus 400mg) in the following week. On contrary, the Ultra Rapid Opioid Detoxification procedure protects the patient from withdrawal symptoms for 100 percents. To complete the whole process of detoxification from Substitol 2-3 detox procedures are needed. The best result in terms of a long time recovery brings the combination of rapid detoxification + Ibogaine therapy (Ibogaine is an effective means to eliminate craving for the drug) + Naltrexone blockade (Naltrexone is a reliable opioid receptors blocker in means of prophylactic of relapse). Substitol is a trap in which many smart people found themselves thinking they had found the way to get rid of heroin addiction easily. Free cheese is only in a mousetrap. Nowadays the problem of Substitol and Somnubene abuse in Austria is worse than that of heroin, cocaine, marijuana or AIDS. Substitol ousted the other illegal substances from the drug trafficking. The level of crime associated with the use and sale of Substitol is incredibly high.

substitolsubstitol on the street