Naltrexone implant treatment for opioid and alcohol addiction

"Naltrexone implant have the form of small pellets placed under the skin in a low abdomen area, implants release controlled amount of Naltrexone into patient's body during the pointed time."

Naltrexone implant treatment (Pharmacological Blockade)

The method of pharmacological blockade or, in other words, the pharmacological ban on the drug/alcohol use has long been considered as one of the most efficient in addiction medicine.  Indeed, it is very difficult for an addict  to resist the temptation to use the coveted substance on his own will. There are always the reasons, the circumstances, time, money and the drug by itself which are always surprisingly folded into a perfect combination, where the dependent is neither  longer able to control himself nor to think about possible consequences.  At this point, the need of the last line of defense against the drugs/alcohol  is vital. This line is pharmacological blockade or naltrexone implant treatment.

The idea of the blockade is that medication, which violates or neutralizes  the effects of the drugs/ alcohol, is constantly presented in the patient's body. Nowadays it is naltrexone implant treatment, which blocks the opioid receptors, and Disulfiram, which distotrs the metabolism of alcohol. The scientists predicts the emergence on the market the anti-cocain vaccine in 2015. Vaccine is supposedly  have to bind the small cocain molecules with  the  large protein molecules, making the bound molecules of cocain unable to go out of the blood and thus making them unreachable for brain receptors.

Naltrexone treatment blocks the effects of opioids

Naltrexone is a full opioid antagonist.. It means that naltrexone neutralizes (blocks) the effects of Morphine, Heroin, Methadone, Codeine, OxyContin, Fentanyl, Substitol, Tramadol, opium alkaloids and other synthetic opioids. In case if a man uses one of these substances, while the opioid receptors of his brain are blocked by naltrexone treatment, the drug intoxication does not develop. He isnt able to feel  euphoria, pleasure from the drug use. The attempts to overwhelm the blockade by competitively high doses of the drug may result in unpredictable consequences of pharmacological conflict - respiratory depression, cerebral edema, coma, shock, death from cardio-respiratory arrest. Naltrexone has been used in clinical practice since the 70s of the last century.   The quality of opioid antagonist therapy is continuously improving at  the direction of strengthening the blockade effect, increasing its duration, reducing the toxic side-effects.

NOWADAYS THE FOLLOWING FORMS OF NALTREXONE ARE AVAILABLE:

1. Tablets for oral administration (Revia, Nalorex, Antaxone, Naltrexone). Each tablet contains 50mg and works for 24 hours. Usually, it is taken once in a morning under the supervision of the relatives. There is  also a scheme, when  the patient receives 2-3 tablets of Naltrexone on Friday morning in order to prolong and strengthen the intensify of the blockade in a potentially risky period for relapse.  Opioid antagonists are  included in almost all the therapeutic protocols  aimed the complete drug rejection.
Before starting Naltrexone implant, you must be sure that your body is free of opioids.  The immunohromatic  test for detection of opioids in the urine is compulsory.  Make sure that from  the last drug use  passed no  less than 7 days  and  you arent going  to have any signs of withdrawal. Even the  remains of opioids in a body, in case of receiving  Naltrexone,  provoke very strong rmanifestation of the  withdrawal syndrome. Those, who have even once experienced it, say  that 15-20 min after receiving the antagonist you start feeling  all the withdrawal symptoms 100-fold amplified  : pain, diarrhea, vomiting, sneezing, watery eyes, rolling on the floor. Taking narcotics doesn’t alleviate or ease the abstinent crisis, which may last for up to 24 hours. Be careful and  never take the blockers without primarily making sure that your body is fairly clean.
Naltrexone has a mild hepatotoxic effect. It is not recommended for people with liver problems (transaminases above 150-200 U/l, bilirubin above 50mmol / l), with the clinical signs of cytolysis and cholestasis.
Naltrexone is a very good choice for motivated patients, which along with the regular drug tests  allows the relatives to monitor the patient's condition and keep him away the drugs.

2. Naltrexone palmitate (Vivitrol, Naltrexone Depot injection) is the next generation of opioid antagonists. It is a liquid form of Naltrexone with the prolonged effect of action of 28 days.  Intramuscular injection of  Naltrexone palmitate, which is chemically bound with fatty acid molecules, provides a stable and predictable  release of Naltrexone into the blood stream during 28 days. Naltrexone palmitate is tested and approved by FDA  (Food Drug Administration. USA) for use in the U.S. for alcoholism and drug addiction treatment. Medication is safe and causes neither local inflammatory nor allergic reactions.

3.The solid Naltrexone implant (Naltrexone pellets) with prolonged effect for 2-3-4 month duration emerged in the U.S., Australia and UK in the early 90-s. Nowadays they are officially patented in many countries including USA,  Australia.
The implant has a form of a cylinder, which contains naltrexone, magnezium stearate and  triamtsinalon. Under local anesthesia  the implant is placed subcutaneously  in a low abdominal area from 2 cm skin incision.  Implantation is a painless minor surgery which takes about 5 minutes.

For a few days after implantation the patients have to avoid mechanical injury or  thermal impact on implant  area.  Due to presence of magnezium stearate in the  implant, the  local allergic reaction is possible (approx. 5% ), with symptoms of redness, swelling, itching of local tissues. Usually the 7-day course of antibiotic, antihistamine and corticosteroid thepapy is enough  to relieve these symptoms.  More than ten thousand naltrexone implantations were performed in Australia over the past 5 years.
It  is widely  recommended for obtaining the better result from Naltrexone therapy to extend the  total length of naltrexone protection up to 12-16 months.  

4.The third generation of naltrexone-implants with 6 and 12 month blockade duration have recently emerged on the pharmaceutical market. The long-term implants are manufactured in Hong Kong and Japan. The controlled release of Naltrexone is provided by polymer matrices.  The long-term implants  have the same side-effects as the  “regular” Naltrexone implants: the mild liver toxic effect and possible local allergic reaction in 5% of cases.

It is also a proven fact about the effectiveness of naltrexone treatment in alcohol dependence. There is a positive experience with simultaneous implantation of both naltrexone and disulfiram implants for the  patients with multiaddiction problems and severe forms of alcoholism.

NALTREXONE THERAPY

Naltrexone therapy in treatment of all kind of addiction  (especially in case of alcoholism and opioid dependence) is getting more and more popular nowadays.

Naltrexone is a pure opioid antagonist which has better binding affinity to the opiate receptors than opiates. Due to that unique property  Naltrexone reliably blocks the effects of opioids.  Besides  Naltrexone  is neither addictive nor pleasurable substance. It effectively bans the physical dependence on Morphine, Heroin, Methadone and other opiates. Clinical research indicates that 50 mg of Naltrexone effectively neutralizes  the pharmacological effects of 500 mg of intravenously administered Heroin for 24 hours.

Because naltrexone does not cause physical dependence, there is no withdrawal syndrome in  the case of abrupt discontinuation. Naltrexone doesn't have sedative effect. So it hasn't  restrictions in driving and  other activities requiring concentration.

It is important to understand that Naltrexone therapy doesn't erase the craving for drugs. 

Sustainable lack of willingness to take narcotics, perceived  rejection of them can be achieved only by complex and prolonged  treatment.  Treatment of psychological dependence, coupled with the reliable pharmacological blockade and  rehabilitation programs provides the most  positive and stable prognosis.

THE ANTI-ALCOHOL BLOCKADE

Disulfiram (Antabus, Esperal, Tetidis) is a medication that affects the function of the liver enzymes. Disrupted by Disulfiram  the metabolism of ethanol results in rapidly growing concentration of acetaldehyde in a patient”s body.  Acetaldehyde is a highly toxic metabolite. As soon as it appears in a blood,  the person starts feeling hot, his face is getting red and swollen. A man feels heaviness in the chest and short of breath.  His  cardiovascular system  initially responds by the increased blood pressure and rapid heartbeat, which in 10-15minutes after are replaced by blood hypotension and inner organ hypoperfusion which in its turn may lead to a heart and/or brain infarction. The consequences of such condition might be very serious. Even the taste of alcohol can trigger nausea, vomiting, and sometimes fainting.
In Russia, where the problem of  alcoholism is traditionally serious, the so-called, sensibilizing therapy has been successfully used for a long time. In hospital conditions the patients receive disulfiram. For the creation of the negative reflex on alcohol and, thus, reducing craving for it, the patients undergo through, so called, “alcohol-disulfiram” tests which cause very unpleasant, aversive reaction to alcohol.  After 3-4 such tests, which result in violent vomiting, dizziness, weakness, fatigue, the patients usually dont feel even the slightest desire to use alcohol for a long time ater. Even the sight of a bottle of beer is getting repulsive. "Take this stuff away from me" -this is what the patients usually say at the end of the treatment, responding to offer  have a bit alcohol. After being discharged from the hospital the patients take disulfiram from 250mg  to 750mg  per day.  On average, it is usually one  pill in the morning. The most frequent side effects of the naltrexone implant treatment are the slightly increased transaminases, possible symptoms of polyneuropathy, a metallic taste in the mouth. In case of a long-term disulfiram  therapy, use of multivitamins is recommended.
Colme (cyanamide) is produced by Laboratories Victoria (Spain). The therapeutic effect of that medicine is also based on the blockade of the enzyme called alcohol dehydrogenase. Colme in comparison  to Disulfiram  has less negative side-effects on internal organs and more pronounced aversive reaction to alcohol. Reliable anti-alcohol protection develops  as early as 1 hour after receiving the medicine. In some situations  Colme is a  drug of choice. Because it is odorless, tasteless, colorless, ready for use liquid, it can be added to  drink or food without the knowledge of the patient. Even if the person refuses to take anti-alcohol tablets, with the help of Colme  the alcohol blockade may be continued,  making use of alcohol  impossible.
Tetlong is an oil solution of disulfiram (a similar technology is used in manufacturing of Vivitrol). This is a 3.0ml  intramuscular injection. It works for about 1 month, causing a strong reaction even to a small amount of alcohol. Two or three sips of beer may cause severe shock  and result in hospitalization to emergency center.
Disulfiram Implant is a single cylinder, or 12 -24 pellets for implantation (for 2-6-12 month dutation).  In some countries  this medicine is  called  a “silver bullet” against alcoholism. It is implanted under skin in a low abdominal area. Contact with alcohol in this case leads to a rapidly developing  strong negative reaction, which can be very dangerous especially in older people with concomitant cardiovascular problems. . In case of receiving long-term Naltrexone implant, it is  necessary to monitor the level of transaminases 2 times a year. Rejection of the implant  occurs in 5 percents of cases.

The advantages of using the block-implants

 1. Use of the drug/alcohol  becomes impossible /or very dangerous.
2. The method of choice for the patients with  inconsistent motivation and compliance for treatment.
3. Blockade is prolonged and effective method of treatment for drug/ alcohol addiction.
4. Pharmacological isolation allows the patients to remain socially active, to work, to travel, to have normal relationship with relatives, without being locked in rehab for months.
5. The patient is medically forced to come to terms with the fact that drug or alcohol use is impossible. Many patients  only then begin to consider  sober life as the only possible long-term condition.
6. Blockade  reinforces the  remission. It  allows  the patients to be protected from possible relapse in the most difficult initial period of staying away from the drugs/alcohol. It creates  the experience of sobriety.