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Initial development of naltrexone as a medication to be marketed for the treatment of heroin addiction was initiated by the Special Action Office for Drug Abuse Prevention (SAODAP) in the early 1980s and completed by NIDA including preclinical toxicology, pharmacokinetics and clinical studies. No organ toxicity, developmental toxicity or carcinogenicity were revealed in the preclinical studies. Naltrexone was approved by the FDA in 1984 on the basis of its pharmacological efficacy as a narcotic antagonist and its safety profile. Although clinical efficacy data in the multi-site placebo controlled clinical trial were inconclusive, naltrexone was superior to placebo in producing less heroin use and more abstinence in those who tested the naltrexone blockade by using heroin at least once. In 1995, Naltrexone was approved by the FDA for the new indication of preventing relapse to alcohol use in formerly dependent alcoholic patients (Vocci).
Naltrexone has been used together with clonidine to shorten detoxification from heroin or methadone from two weeks to only one day. Withdrawal from the opiate is precipitated by naltrexone and resulting symptoms amerolirated by clonidine. The cost saving for this approach are substantial compared to use of methadone tapering (Kosten). More recently, the use of general anesthesia or heavy sedation with medazolam along with naltrexone has further shortened the detoxification to 4-6 hours. This procedure is sought by patients for reasons such as fear of withdrawal discomfort; need to shorten the hospital stay, etc (Kleber).
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Barriers for Wider Use of Naltrexone
Naltrexone has very few and minor side effects. It is the treatment of choice in highly motivated patients, especially physicians, nurses, pharmacists and attorneys (O'Brien). However, clinical experience using naltrexone for treating opiate addiction has been replete with data on the poor medication compliance. Ling reported a 6% retention for 60 days and 2% retention for 9 months in 276 methadone maintained patients who expressed some interest in trying naltrexone treatment. Another study with 252 street heroin addicted patients treated with naltrexone had only 5% retention for 60 days and no retention for 9 months. The main reason given for this poor treatment retention and low patient compliance is that naltrexone's lack of agonist activity does not provide any drug reinforcement when taken and produces no negative consequences (withdrawal symptoms) when discontinued.
Others have suggested that patients are reluctant to take naltrexone because of fear of drug related dysphoria or depression. It has been hypothesized that naltrexone may block the effects of endogenous opiate peptides and prevent normal endogenous opioid receptor activity involved in mood modulation producing a subjective state of dysphoria. Animal laboratory data suggest opioid system up regulation associated with chronic naltrexone administration. However, a review of clinical studies using naltrexone treatment for opiate and alcohol dependence showed very limited occurance of naltrexone-related dysphoria and depression. (Miotto,1997)
Some physicians report a reluctance to prescribe naltrexone due to the "black box" warning of liver toxicity in the package insert. The warning was included based on liver enzyme elevations reported with 100-300mg/day doses of naltrexone during studies of naltrexone treatment for obesity. A review of literature and adverse effect reports from the manufacture demonstrated the safety of using 50 mg/day for alcohol or opiate dependent patients (Galloway).
The lack of wider use of naltrexone by physicians may also be partly due to the lack of market promotion by the manufacturer resulting in poor understanding of how and when to use naltrexone. Treatment providers have not been fully informed about naltrexone's unique role in facilitating relapse-prevention in opioid addicted patients. An experienced clinician who has considerable success in naltrexone treatment of heroin addicts suggested that naltrexone should be viewed as an adjunct to a wide range of individualized psychobehavioral treatments which may also include the use of other psychotropic medications for comorbid mental disorders. Patients families or friends should be encouraged to participate in treatment planning and compliance monitoring (Resinick).
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Good to hear you're doing well with the drug counselor!!!
Naltrexone produces no influence on the state of health and does not result in addiction. Naltrexone blocks the effects of all opioids (heroin, morphine, tramadol, etc.). It is recognised all over the world for the treatment of opioid addiction. Naltrexone acts on opioid receptors, i.e., spinal and brain areas sensitive to narcotic substances. It displaces narcotic substances and binding to the receptors protects from the effect of narcotic substances.
Usually, naltrexone is given orally. During intensive detoxification procedure the body is saturated with naltrexone. Later on, naltrexone should be taken daily for at least twelve months. In recent years, the efforts have been made to develop and introduce the extended-release naltrexone products. Some of them are implanted subcutaneously, some are injected with the help of a special needle. The latter techniques are not finally approved or are still under studies. In rare cases they may be applied in the individual manner, if other techniques are non-effective.
Naltrexone must be taken at the presence of a close person. Sometimes we recommend especially strict conditions, e.g., we offer to crush the drug, dissolve in water and drink with a glass of liquid. Daily use of naltrexone helps to take personal responsibility for the own life, protects from unpredictable temptations and relapses. By itself, naltrexone is not sufficient for getting cured, however its therapy is a must for maintaining sobriety.
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What happens when narcotic substances are used in the background of naltrexone therapy?
Naltrexone protects from feeling “high” under the effect of opioids. Opioids used in first postdetoxification days may cause spastic headaches, nausea, vomiting and diarrhoea. Naltrexone therapy helps to gradually regain the usual sensitivity of nervous system to all substances having effect on mental system. We urgently ask you not to test the activity of naltrexone with any of narcotic substances.
Naltrexone 50 mg daily is a sufficient dose to block the effect of opioids and prevent relapse. Any patient abstaining from opioids for a longer period of time becomes more sensitive, i.e. after relapse, the former usual dose may cause severe, even fatal poisoning.
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Is the use of naltrexone sufficient?
Successful treatment depends not only on the therapy but on the proper care as well. There are other preconditions of successful treatment.
Self-motivation – desire to get rid of the dependence.
Close person able to take care of the maintenance treatment with naltrexone all year round without any breaks.
Family or other doctor who will monitor the maintenance treatment with naltrexone. Professional consultations and their attendance during the postdetoxification period.
Opi, you are doing very well!!!! Just keep it up! You've got a good head on your shoulders-even though you're a class clown.
THe real reason i'm really interested is for my brother in law to try and help him off of methadone.....I can handle my temptations, no doctors are going to give me pills, and I'm not buying them off the streets, so I think I can make it, but if it can help him suffer less getting off the methadone, I'll try to help him. We're going to go to meetings starting Friday or SUnday-if he doesn't flake....we'll see. Thanks worried, appreciate it....I've got so many open tabs in my browser it's insane!!! G'nite.
GOOD JOB!!!