Anxiolytics and sedatives: dependence, symptoms and treatment

The use of anxiolytics, sedatives and hypnotics for medical reasons is widespread. When they are used, intoxication can occur, accompanied by physical and mental disorders. Repeated use can lead to the development of abuse and dependence.

Distinct behavioral, emotional and cognitive impairments even in regular consumers do not always develop, depending on the dosage and pharmacodynamic effects of the drug. To a certain extent, there is a cross-tolerance between alcohol, barbiturates and non-barbituric anxiolytics and sedatives, including benzodiazepines. (Barbiturates and alcohol are very similar in their dependence, symptoms of withdrawal, chronic intoxication.) If the consumption of anxiolytics and sedatives decreases below the critical level, then the discontinuing withdrawal syndrome develops.

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Symptoms of dependence on sedatives

Poisoning (acute intoxication). Signs of progressive intoxication with anxiolytics and sedatives are suppression of surface reflexes, small nystagmus when looking to the side, somewhat increased excitability with coarse or rapid nystagmus, ataxia, lubricated speech, instability while maintaining the posture. Further progression is manifested by nystagmus when looking forward, a doubt expressed by ataxia with falls, confusion, deep sleep, narrowed pupils, suppression of breathing and eventually can lead to death. Patients taking large doses of sedatives often find difficulty in the process of thinking, slow speech and understanding (along with some dysarthria), memory disorders, violation of the correctness of judgments, narrowed focus of attention, emotional lability.

Chronic consumption. In susceptible patients, psychological dependence on the drug can develop rapidly, even after several weeks of admission; attempts to discontinue the drug lead to the development of insomnia, manifested by anxiety, anxious sleep, frequent awakenings, a feeling of tension in the morning. The degree of physical dependence is determined by the dose and duration of use; for example, phenobarbital at a dose of 200 mg / day, taken for many months, may not cause significant tolerance, but if taken 300 mg / day more than 3 months or 500-600 mg / day for 1 month, can lead to the withdrawal of withdrawal symptoms .

The abolition of barbiturates taken in large doses causes an acute withdrawal syndrome in the form of a severe, life-threatening disorder, similar to alcoholic delirium. Sometimes even with proper treatment of withdrawal from 1 to 2 weeks, convulsions are observed. During the first 12-20 hours after the abolition of short-acting barbiturates, in the absence of treatment, the patient becomes more restless and weakened, and tremors increase. Within 2 days tremor becomes more noticeable, deep tendon reflexes can increase, the patient weakens. On the 2nd-3rd day, 75% of patients taking> 800 mg / day of barbiturates develop seizures, which can lead to the development of epileptic status and death. In the absence of treatment between the 2nd and 5th day, withdrawal syndrome is manifested by delirium, insomnia, confusion, threatening auditory and visual hallucinations. Hyperpyrexia and dehydration are often observed.

The abolition of benzodiazepines leads to the development of a similar withdrawal syndrome, although it is rarely severe and life threatening. The onset may be slow, since benzodiazepines last for a long time in the body. The withdrawal syndrome of varying severity was noted in people taking therapeutic doses, although the prevalence of this unusual phenomenon is unknown. Cancellation can be more pronounced in those who take drugs with rapid absorption and a rapid drop in serum concentration (eg, alprazolam, lorazepam, triazolam). Many patients who abuse benzodiazepines also abuse alcohol, and when the benzodiazepine withdrawal syndrome ceases, alcohol withdrawal may develop.

Treatment of dependence on sedatives

Acute intoxication usually requires nothing but observation. In some cases, the maintenance of respiratory function is required. To treat severe sedation due to an overdose of benzodiazepines, a benzodiazepine receptor antagonist, flumazenil, can be used. Its clinical effectiveness is not clearly defined, since most patients with benzodiazepine overdose recover without treatment. Sometimes, when used to reduce sedation, flumazenil provokes convulsions.

The procedure for treatment of dependence on sedatives, especially barbiturates, consists in their abolition according to a strict scheme and monitoring of withdrawal symptoms. Often the best option is to join long-lasting components, which are easier to cancel. Before starting cancellation, sedative tolerance should be assessed by testing with a test dose of phenobarbital 200 mg orally given to the patient without an intoxication; if the patient does not have tolerance, then this dose causes a nap or shallow sleep after 1-2 hours. Patients with moderate tolerance have some sedation; in patients with tolerance> 900 mg there are no signs of intoxication. If the dose of 200 mg does not have an effect, then the level of tolerance can be refined by a repeat test 3-4 hours later in a larger dose. Expressed anxiety and agitation can increase the patient's tolerance. The daily dose set in view of tolerance is usually given in four divided doses for 2-3 days to stabilize the patient's condition, and then decreases by 10% per day. Cancellation should be in the hospital. If the withdrawal syndrome has begun, returning the condition to its previous level is difficult, but with careful monitoring the symptoms can be minimized. Recovery of the central nervous system requires about 30 days.

As an alternative, phenobarbital can be used. It does not cause narcotic intoxication, unlike faster acting substances. High-speed barbiturates, other sedatives, weak anxiolytics can be replaced by a dose of phenobarbital equivalent to 1/3 of the average daily dose of the drug on which the patient is dependent; for example, for secobarbital 1000 mg / day, the stabilizing dose of phenobarbital is 300 mg / day, usually prescribed at 75 mg after 6 hours. Phenobarbital is given orally 4 times a day, and its initial dose is reduced by 30 mg / day until complete withdrawal. Since the initial dose is established on the basis of anamnestic information, there is a potential for error, so the patient must carefully observe the first 72 hours. If agitation or anxiety persists, the dose should be increased; if the patient is drowsy, dysarthritic or nystagmus is observed, the dose should be reduced. While the patient is being detoxified, other sedatives and psychoactive drugs should be avoided. However, if the patient simultaneously takes antidepressants, especially tricyclics, then you can not suddenly stop taking antidepressants, the dose should decrease gradually over 3-4 days.