Preparations blocking opioid receptors using alcoholism. Drug obesity correction. The mechanism of action of opioid receptor blockers
An increase in the amount of drug addicts increases the demand for narcotic blockers. This is one of the preventive options, as well as the method of combating drug use.
The use of blockers
NC "Mosnarkology" is the embodiment of the newest methods for treating dependence in drug addicts. Our team of professionals doctors will help to cope with your disease, will give advice and hold a full course of treatment over dependency to the victorious end.
Specialists of the Mosnarkology Center, if the patient is desired and the presence of testimony will be blocked by drugs. The appointment of the blocker, his choice and the introduction of a drug-dependent patient doctors are engaged.
The essence of the blocking technique is simple and consists in the introduction of a drug into the patient's body. The action of the blocker can be different, more or less long and depends on the type of blocking preparation.
More efficiently, the use of blockers together with rehabilitation courses for drug addicts, which are regularly carried out in the Mosnarkology Narcological Center. For complete cure, restoration is required not only physical, but also mental dependence.
The mechanism of action of opioid receptor blockers
Thrust for drugs is so great that returns dependent on the vicious circle again and again. To somehow solve this problem, medication blockers were found.
I had to deceive the body of the drug addict. It is injected into its body, which blocks brain receptors. After the adoption of a narcotic dose, the patient now does not feel the hadive pleasure. The pathological effect of the drug is blocked. As a result, interest in drug treatment disappears.
In this case, the blockers perform the role of an anticorcidative drug. At the heart of treatment - artificial creation of such a situation when the reception of large doses of drugs becomes impossible due to a serious deterioration of well-being.
Codings and blockers from drugs or "prohibitive techniques"
Do you need help? We not only know how you can help, but do it! The narcological clinic "Mosnarkology" will provide you with a fairly effective comprehensive treatment from dependencies in the comfortable chambers of our clinic.
54. Compare Naloxone and Naltrexone effects.
Both of these substances are competitive antagonists of opioid receptors. Naloxone has a very short period of half-life, while natrel * sleep is valid for several days
Which of the opioid receptor antagonists is more active than other ## shoots symptoms of overdose opioid analgesics in patients without medicinal dependence?
Nalmefen is a pure opioid antagonist for parenteral administration.
56. Name an easy way to diagnose opioid overdose.
Introduction Naloxone. It acts briefly and must quickly liquidir0 "present myios caused by opioids, but not by other substances.
57. Why to facilitate the discharge syndrome of opioids apply. "Amiakeson?
Naltrekson is particularly shown for the outpatient cancellation of opioids, as it has a long period of "half-life" (T / \u003d 10 hours) and its already-time administration can block the euphorizing effect of opioids within 48 hours. This prevents attempts to illegal acquisition of opioids and use them to achieve Euphoria.
58. Do Naloxone introduce inside?
Not. The maximum action is manifested in parenteral administration, as Naloxone is destroyed at the first passage through the liver.
59. Describe Naloxone's metabolism.
Naloxon is metabolized mainly by cytochrome P4 ^ on the liver. Next, the metabolites are connected to glucuronic acid.
69. How are Naltrekson introduce?
Naltrekson can be administered both inside and parenterally.
61. Tell us about the possible use of Naltrexone with alcohol abstinence.
Recently it was shown that Naltrekson reduces attraction to alcohol and can be used to treat chronic alcoholism. The effect of the drug is probably partly associated with a change in the activity of the sympathetic nervous system.
62. Describe Naloxone effects with severe intoxication opio-idi.
Naloxone quickly returns consciousness, but due to the short period of its "half-life" in patients with severe intoxication opioids in 60-90 minutes, a comatose state can again develop. In this case, the use of a longer existing means is shown.
63. Name the testimony to apply Nalmefen.
Naltexone derivative, derived, is used in overdose opi
What is the duration of Nalmefen's action?
tFTO The substance has a long period of "half-life" (8-10 hours) and is valid long enough.
65- Are the effects of antagonists of opioid recipers of streets that do not receive opioids?
NOY: These substances are practically inert, which allows them to apply them to diagnose opioid overdose, without fear of the appearance of system effects.
66. Describe the dynamics of the disappearance of opioid effects with the vigorous administration of the opioid antagonist.
The disappearance of opioid effects is observed after 1-3 minutes. The sizes of pupils, breathing and consciousness are restored very quickly.
67. Is addictive to antagonists of opioid receptors developing?
Not. With prolonged use of them, addictive does not develop, and the abolition of these substances of the streets without dependence to opioids is not accompanied by any negative symptoms.
68. Do antagonists have equal activity with respect to all opioid receptors?
Not. These substances tend to actively interact with MJ receptors and in varying degrees affect the receptors of other types
Cardiovascular Pharmacology
Patricia system to Anthony, Judit Cautz,
Andrew Powers and Rebeca Tome
International name: Naloxone (Naloxone)
Dosage form: injection
Pharmachologic effect:
Indications:
Naltrekson FV
International name: Naltrexone (Naltrexone)
Dosage form: Capsules
Pharmachologic effect:
Indications:
Nican
International name: Naloxone (Naloxone)
Dosage form: injection
Pharmachologic effect: Antagonist of narcotic analgesics. Blocks opiate receptors, eliminates the central (incl. Depressive influence on breathing) and peripheral ...
Indications: Overdose of narcotic analgesics, benzodiazepines, barbiturates. Coma with acute poisoning with ethanol. Postoperative application: Acceleration ...
Danish
International name: Naloxone (Naloxone)
Dosage form: injection
Pharmachologic effect: Antagonist of narcotic analgesics. Blocks opiate receptors, eliminates the central (incl. Depressive influence on breathing) and peripheral ...
Indications: Overdose of narcotic analgesics, benzodiazepines, barbiturates. Coma with acute poisoning with ethanol. Postoperative application: Acceleration ...
Revia
International name: Naltrexone (Naltrexone)
Dosage form: Capsules
Pharmachologic effect: Antagonist of narcotic analgesics. The greatest affinity has to MJ and Cappa receptors. Eliminates the effects of opioids (including endogenous). IN...
Indications: Opiate addicts (as an auxiliary drug after the abolition of opioid analgesics), alcoholism.
Antaxon
International name: Naltrexone (Naltrexone)
Dosage form: Capsules
Pharmachologic effect: Antagonist of narcotic analgesics. The greatest affinity has to MJ and Cappa receptors. Eliminates the effects of opioids (including endogenous). IN...
Indications: Opiate addicts (as an auxiliary drug after the abolition of opioid analgesics), alcoholism.
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The successes achieved in the study of the neurochemical mechanisms of alcohol addiction made it possible to offer a number of new medicines for its treatment. Thus, it was found that in the brain there is an endogenous opioid system in which morphine-like compounds (enkephalins and endorphins) caused by euphoria and painkillery effects are produced. Preparations that are opioid antagonists block opioid receptors and thus prevent pleasant effects caused by drug intake. Despite the fact that alcohol is not an agonist of olive receptors, many of its effects are implemented through an endogenous opioid system. Experiments have shown that opioid receptor antagonists block reinforcing alcohol effects. So, Naltrekson prevented an increase in the level of dopamine caused by the introduction of alcohol, and this effect was dose-dependent. As is known, Dopamine is involved in the reinforcing effects of alcohol. Double blind placebo-controlled studies have demonstrated that Naltrekson reduces the pleasant sensations related to the admission of alcohol, in individuals dependent on alcohol. In another study, it is shown to reduce stimulating and strengthening the sedative effects of alcohol in persons abusing alcohol. A decrease in pleasant, reinforcing alcohol effects and enhanced unpleasant can help maintain remission, which has been demonstrated in clinical studies. The duration of remission in patients who took Naltrekson as a supportive treatment was greater than patients who took placebo. By the end of the 12-week course of treatment, 54% of patients who received Naltrekson (against 31% receiving placebo) stopped using alcohol. It should be borne in mind that Naltrekson is effective as an anticorcidive drug under the condition of regular reception for a 12-week course. Naltrekson is prescribed after 5-7 days of abstinence from alcohol consumption. The usual dose of the drug is 50 mg per day or every other day. Naltrexon is metabolized in the liver to 6-natexol, which is a weaker opioid receptor antagonist, but has a longer half-life. The half-life of Naltrexone and 6-Naltrexol - respectively 4 and 13 hours. Clinical studies in which 570 patients participated, did not find serious side effects of the drug. However, in doses of 300 mg and above, the hepatotoxic effects of the drug may appear, therefore Naltrekson is contraindicated to persons with hepatitis and hepatic insufficiency. As a rule, the drug is well tolerated, but side effects in the form of headaches, flu-like state, nausea, anorexia are possible. Naltrekson can be applied by short courses after the completion of the main course of treatment against the background of psychosocial stress in order to prevent recurrence. Naltrexone is especially recommended for patients with a strong, uncontrolled alcohol (compulsive attraction). At the same time, treatment presupposes a high motivation. The effectiveness of treatment is significantly increased in combination with supportive psychotherapy. The drug is Nalmefen structurally similar to Naltrexon. Unlike Naltrexone, it does not have hepatotoxicity. In addition, Nalmifen is a universal opioid receptor antagonist, which blocks three types of them. Studies have shown that in the group of patients with alcohol dependence on the background of taking namphene in a daily dose of 40 mg, there were significantly fewer recurrences compared to the placebo group. In later studies, it was shown that patients receiving landfied at a dose of 20 and 80 mg for 12 weeks, the "disorder" was observed 2.4 times less frequently compared to patients receiving placebo. Nevertheless, a third of the patients against the background of taking Nalmefen were recurrent. During the study, there were no differences in the effectiveness of different doses of the drug. Side events were also not.
AKAMPROSAT (acetylgomotaurine). To date, the exact mechanism of the drug is not set. It is known that it modulates the activity of glutamate and gamke receptors. Chronic alcohol intoxication leads to a decrease in the activity of the brake gamke-eergic system and increase the activity of the exciting glutamate system in the brain. These violations remain for a long time after refusing to use alcohol. AkamProst is structurally similar to the GABC and increases the activity of the GAB-Ergic system, increasing the number of places of binding to the GABA on the synoptic membrane. AkamProst reduces the activity of the glutamate system, affecting the N-methyl-D-aspartate (NMDA) -receptors and calcium channels. For the first time in clinical practice, AKOSPROSAT began to apply in France in 1989. Currently, the drug is allowed in more than 30 countries of the world; The total number of patients under the course of treatment exceeds 1 million. Experiments have shown that AKOSProst reduces alcohol consumption in free access conditions, without affecting food behavior, does not have narcural potential and other pharmacological effects except those that contribute to the reduction of alcohol consumption. In 11 clinical studies in which 3338 patients participated, it was shown that against the background of the admission of akamosphat, patients refrain from alcohol for a longer time than amid placebo. A particularly distinct effect of the akkospar was in the first 30-90 days. After 6 and 12 months after the completion of the course of supporting therapy, the akamospar in the state of remission was a larger number of patients compared to the placebo group. AKAMPROZAT increased by 30- 50% the number of days in which patients did not use alcohol. By the end of the 12-week course of treatment, 51% of patients who received AKAMPROSAT (against 26% receiving placebo), stopped using alcohol. According to other studies, AKAMPROZAT does not reduce pathological attraction to alcohol. The drug is prescribed after relieving the phenomena of the abstinence syndrome.
Akamprospa is produced in the form of tablets of 333 mg. The recommended daily dose is about 2 R / day when weighing more than 60 kg and about 1.3 g / day with weight less than 60 kg. The drug is accepted three times a day with food. Typically, the treatment is beginning with half the therapeutic dose and each daily add one tablet. The duration of the course of treatment is 3-12 months. AKAMPROSAT Pharmacologically does not interact with other drugs used to treat alcoholism, such as disulfiram, antidepressants. Only 10% of the drug is metabolized, and 90% is released with urine unchanged, therefore, unlike Naltrexone, it does not have hepatotoxicity. Akamproshat is well tolerated. Possible side effects, such as diarrhea, abdominal pain, paresthesia, the decrease in the libido, as a rule, quickly pass. Avoiding them helps the gradual increase in the dose.
Currently it is difficult to compare the effectiveness of the akamprosite and nitrexone in the treatment of alcohol addiction. In one of the studies, it was shown that 47% of patients who received Naltrekson in the form of supporting therapy, and 17% of patients who received AKOSProsat abstained from alcohol use throughout the year. However, later studies have established approximately the same efficacy of both drugs. According to some reports, AKAMPROZAT has a prolonged effect, and patients refrain from taking alcohol a year after discontinuation of drug treatment, while the effectiveness of Naltrexone is maximum in the first three months.
The relationship between serotonin and alcohol is complex. It is assumed that alcoholics are trying to normalize the low basal level of serotonin in the brain with alcohol. It was found that serotonin is involved in the reinforcing effects of alcohol. In addition, the low level of serotonin contributes to impulsive behavior, which leads to alcohol consumption. The abnormality of serotonin metabolism may be accompanied by anxiety and depression, and in this case alcohol can be used as a means of self-treatment. Serotoniner inhibitors are inhibitors of serotonin (SSRS) inhibitors (SOROP), fluoofsetin (prozac), fluouxamine (feven), cytalopram. This class of drugs was developed in the 80s of the last century for the treatment of depressive disorders. The mechanism of action of the SIRES is to block the reverse seizure of serotonin with the presynaptic endings, as a result of which the level of serotonin in the synoptic slot rises.
The results of the study of the effectiveness of SSRS in the treatment of alcohol dependence of contradictory. Clinical trials have shown that SSRs causes a moderate effect at domestic drunks and is practically not effective in patients dependent on alcohol. The preparation of ritanserin, blocking serotonin receptors 5-NT2, was no more effective than placebo, in reducing alcohol consumption and reduce thrust to it. Moreover, high doses of alcohol caused cardiotoxic effects that were registered on the ECG. Antidepressants cytalopram and buxpurone were also ineffective in the treatment of the main symptoms of alcohol dependence. In another study, fluoofsetin did not have the benefits of placebo in the prevention of relapses.
Studies Effectiveness SSIRS continue. The experiment showed that a combination of fluoofsetine with WAY 100635 serotonin receptor antagonist significantly reduces alcohol consumption. Selective antagonist 5-NTZ ondansetron receptors turned out to be effective in the early stages of alcohol dependence. Clinical studies show that SFORS is effective in treating not so much alcohol dependence, how many comorbide pathology, in particular depression.
Patients with alcohol addiction often suffer from depression. Most of these, the symptoms of depression are reduced two weeks after stopping alcohol. About a third of patients continue to complain about the poor mood during the remission. In such cases, we are talking about comorbide depression or a double diagnosis. Since depression often becomes a reason for recurrence, its timely diagnosis and adequate treatment are an extremely important task. The use of SIRES allows adequate therapy of comorbide depression. Compared with tricyclic antidepressants, SSRs have advantages in the treatment of comorbide depression, since they have minimal side effects and do not interact with alcohol. In general, regardless of the drug, the use of antidepressants is more efficient compared to placebo in the treatment of comorbide depression during alcohol addiction.
When choosing therapeutic tactics, it is necessary to distinguish the type of depression. Primary depression is a background and, possibly, the etiological factor in the development of alcoholism, while the secondary depression is a consequence of neurochemical disorders caused by chronic alcohol intoxication. It should be noted that antidepressants are effective in both cases. Many patients with alcohol addiction suffer impaired liver function of varying severity, which can affect the metabolism of antidepressants and requires correction of dosages towards a decrease in or increasing. Studies show that patients with liver cirrhosis should be prescribed less doses of drugs, while patients without signs of cirrhosis dosage should be higher due to the acceleration of their metabolism in the liver.
Combined use of drugs. Due to the fact that during alcohol addiction, the functioning of many neurotransmitter systems is disturbed, the effect of drugs affecting any single system may be insufficient. Combined therapy allows you to affect several neurotransmitter systems, while the dose of drugs decreases and the risk of side effects decreases accordingly. A double-blind placebo-controlled study showed that in patients who received combined treatment with AKOSPROSATOM and disulfiram, the duration of remission was more compared to patients who took only Akakospros. Promising is the joint use of nitrexone and akamospress, as well as naltrexone and fluoroxamine in the treatment of patients with alcohol addiction .