Phenazepam - all about the narcotic effect of the drug

New rules for drug circulation in Russia

Now Russia, strictly in accordance with international agreements, has introduced strict subject-quantitative accounting of this drug. It follows from this that it becomes almost impossible to buy it in a “left” way. These are tough times for those addicted to phenazepam.

If previously addicts turned to drug addiction doctors when they were motivated to voluntarily quit the drug, now they find themselves in a state of threat of severe withdrawal syndrome. What is called “withdrawal” in drug addiction. There is nowhere to get medicine - how to save yourself from suffering?

Phenazepam under the new law

Where did the drug Phenazepam go and for what reason? And most importantly, what should those who needed to purchase it do? Questions that often remain unanswered, at least because new rules for the use of this medicine in Russia also introduced new rules for its storage in medical institutions and pharmacies. And for many such costs were either unaffordable or impossible for technical reasons.

Phenazepam disappeared in 2021 in St. Petersburg from regular pharmacies, but it can be obtained using special prescriptions, which are subject to separate registration and stored in the pharmacy for 3 years, and only in specialized pharmacies, of which there are only about 3% in the country. Therefore, it has become difficult, if not almost impossible, to purchase this medicine under the new law.

The conditions for the sale of Phenazepam from pharmacies have actually been equated to narcotic drugs. To be precise in the wording, it was included in the List of Potent Substances No. 964, valid in Russia and approved by decree of the Russian government.

Why was Phenazepam banned?

They did this for the good purpose of controlling the circulation of such potent drugs and followed the goal of complying with the article of the Criminal Code on the illegal trafficking and sale of potent or toxic substances. It’s a good thing, but it turned out that this drug was used by a very large number of patients (in 2021, for example, more than 3.5 million packages of this drug were sold in the country), who were immediately left without the opportunity to buy or receive it.

And the question of when it will go on sale in 2021, as patients sometimes ask, is not entirely correct - phenazepam is available, but according to the new order it is prescribed, prescribed and sold under very strict conditions.

Please note that one of the motives for the new rules was that with long-term use of phenazepam, dependence on it develops, and if the use is interrupted, withdrawal syndrome develops, which often also requires timely and qualified treatment. In our clinic we treat such conditions as well. With phenazepam withdrawal syndrome, you can come to our psychiatrists to relieve withdrawal symptoms and treat addiction.

How to prescribe phenazepam according to the new rules

In fact, today you need to go to a specialized clinic that has such an opportunity. Or be directly treated with this drug as part of outpatient or inpatient treatment. Our Lazaret clinic has prepared all the storage conditions for phenazepam and therefore has the opportunity to prescribe it to our patients. We use it to treat conditions that require the use of anxiolytics (in other words, tranquilizers).

How to replace Phenazepam?

When treated at the Lazaret clinic, both in the outpatient department and in the hospital wards, you will not need to replace this drug with anything, since we have it in stock and we are able to prescribe it in compliance with all the requirements of the new law - as a sleeping pill or sedative, for panic attacks, etc.

If you have received phenazepam and now cannot prescribe it, come to us. Sign up for a consultation with a specialized specialist by calling the clinic. If you require this type of medication for health reasons (anticonvulsants, sedatives, muscle relaxants, tranquilizers), then we also recommend that you make an appointment with our doctors and receive the necessary treatment using a truly effective medication, and not its analogues and generics.

Phenazepam withdrawal syndrome is characterized by a number of symptoms and is in many ways similar to the phenomena during withdrawal of alcohol and sleeping pills.

Contraindications

Phenazepam should not be taken on its own without consulting a doctor.
This can cause serious consequences, worsening of the condition and severe side effects. Despite the treatment of withdrawal symptoms, Phenazepam should not be combined with alcohol intake.

It is dangerous to take simultaneously with beer - this drink also affects benzodiazepine receptors and greatly increases adverse reactions.

Direct contraindications to the use of Phenazepam are as follows:

• acute alcohol poisoning
• taking other psychoactive substances
• coma, myasthenia gravis, shock
• angle-closure glaucoma
• severe depression
• pregnancy in 1st trimester
• lactation period
• acute respiratory failure
• severe obstructive pulmonary disease

If there is a history of hypersensitivity reaction to the drug, repeated use may cause a severe allergic reaction.

Symptoms of phenazepam withdrawal syndrome:

• Sleep is disturbed.
• Anxiety arises.
• Anxiety.
• Irritability
• Discomfort in the heart area, headache, loss of appetite, and nausea are noted.

In severe cases, psychosis may develop with impaired consciousness and vivid, often frightening, hallucinations. Urinary incontinence occurs not only during sleep, but also during the daytime.

What to do?

Even if Phenazepam has disappeared from regular sales, this is not a reason to change it or suffer from withdrawal symptoms. Call or come to our clinic - we have the ability to prescribe this drug and it is in stock.

Effect on the body

The action of Phenazepam, like other benzodiazepines, is based on enhancing the action of GABA (gamma aminobutyric acid), the main inhibitory neurotransmitter of the central nervous system. The increased inhibition of neurons in subcortical formations caused by it determines the main effects of the use of Phenazepam:

• sedative;
• anxiolytic;
• muscle relaxant;
• anticonvulsant;
• hypnotic.

Phenazepam is the most popular tranquilizer in the internal medicine clinic.
Relieving anxiety, autonomic disorders, normalizing sleep, the drug helps to quickly normalize the patient’s condition in many diseases. For recreational purposes, Phenazepam is taken in increased dosages, which has a negative effect on the body.

Physiological symptoms

When using Phenazepam in large doses, the following negative symptoms are observed:

• decreased blood pressure;
• tachycardia;
• disturbance of appetite and stool;
• urinary dysfunction (urinary retention or incontinence);
• pale skin;
• chills.

From the peripheral nervous system:

• slowing of psychomotor reactions;
• slurred speech;
• unsteady gait;
• trembling of limbs;
• headache, dizziness.

Psycho-emotional manifestations

The following manifestations are observed from the psyche:

• drowsiness;
• confusion;
• general disorientation;
• restlessness;
• slurred talkativeness;
• unproductive activity.

Mental manifestations are mainly determined by individual tolerance to tranquilizers - in some patients, even therapeutic doses of the drug can cause fainting or severe headache.

It is probably difficult to imagine a more well-known anxiolytic drug, which has long been in use in psychiatric and general medical practice, than phenazepam. Such widespread use of this drug is an indirect recognition of its advantages, but also often leads to thoughtless, uncontrolled use. At the same time, among many doctors and patients there are a number of prejudices against tranquilizers in general and phenazepam in particular. However, like any other medication, it has its undoubted positive properties, as well as features that require attention and precaution. Without considering all these aspects, it is impossible to effectively use phenazepam, which, in fact, is required from a qualified doctor.

Phenazepam is an original domestic tranquilizer, synthesized and developed for use in 1970 by a group of scientists at the Institute of Pharmacology of the USSR Academy of Medical Sciences under the leadership of V.V. Zakusova. According to its chemical structure, it is a benzodiazepine derivative (7-bromo-5-(ortho-chromphenyl)-2-3-dihydro-1H-1,4-benzodiazepine-2-OH). Phenazepam, like other drugs of the same pharmacological group, has a depressant effect on the central nervous system, which is realized mainly in the thalamus, hypothalamus and limbic system, enhances the inhibitory effect of gamma-aminobutyric acid (GABA), which is one of the main mediators of pre- and postsynaptic inhibition of nerve transmission impulses in the central nervous system. The mechanism of action of phenazepam is determined by stimulation of benzodiazepine receptors of the supramolecular GABA-benzodiazepine-chlorionophore-receptor complex, leading to activation of GABA receptors, which in turn causes a decrease in the excitability of subcortical structures of the brain and inhibition of polysynaptic spinal reflexes.

Phenazepam is well absorbed from the gastrointestinal tract. The maximum concentration of the drug in the blood plasma is achieved within 1–2 hours. Phenazepam is metabolized in the liver, its half-life ranges from 6 to 18 hours. The drug is excreted mainly in the urine. Phenazepam should be taken orally. A single dose is usually 0.5–1.0 mg.

Clinically, all benzodiazepines have anti-anxiety effects, as well as sedative, hypnotic, muscle relaxant and anticonvulsant effects. These 5 properties are expressed in drugs of this group to varying degrees. For example, clonazepam has a more pronounced muscle relaxant effect, therefore it is often used as a corrector of diencephalic disorders, incl. associated with the use of antipsychotics in psychiatric and neurological clinics. Mazepam, on the contrary, has much less pronounced muscle relaxant and sedative effects and can be used as a so-called. daytime tranquilizer, providing the ability to work and drive a car, while its anxiolytic activity is also less pronounced.

Relanium is characterized by powerful sedative and hypnotic effects and is used mainly in inpatient settings, in particular in the complex treatment of psychoses, as well as in anesthesiology. Phenazepam has all these pharmacological effects to the same extent. It is this versatility that explains its widespread use to this day, despite the availability of new generations of anti-anxiety drugs [2, 7, 26–28].

Another important advantage of phenazepam is its wide dosage range [1, 10, 22, 25, 26], when, depending on the dose used, various properties of the drug are realized:

• psychotropic (anxiolytic, sedative, hypnotic effects);
• somatotropic (muscle relaxant, anticonvulsant, vegetotropic, hypotensive effects).

The clinical use of phenazepam is possible both in monotherapy and in combination with other psychotropic drugs, which can lead to both an increase in the desired effects (synergy phenomena) and a weakening of the negative properties of the drug [4, 5, 11, 13, 14, 17– 19].

In accordance with all of the above, it becomes clear that the pharmacological activity of phenazepam allows it to be effectively used in various areas of clinical medicine. This drug is actively used in the treatment of a wide range of mental disorders (neurotic level disorders, personality disorders, diseases of the affective circle, schizophrenia, organic brain diseases, alcoholism, drug addiction) [3, 6, 8, 10, 11, 13, 15, 17 , 20, 25, 29] and for somatic pathology in neurology, cardiology, pulmonology, gynecology, oncology, resuscitation, anesthesiology [9, 12, 14, 16, 21, 22, 31].

Psychoneurological disorders

When considering painful conditions for which phenazepam is successfully used, mental disorders deserve attention first of all.

Anxiety-phobic disorders

The clinical and pharmacological effects of the drug are realized to the fullest extent in patients with anxiety-asthenic, anxiety and anxiety-phobic disorders (ATD; ICD-10 categories F40, F41, F42, F43) that are simple in structure [3, 10, 17, 19, 28] in cases where phobias show a close comorbid relationship with anxiety and are characterized by imagery and emotional intensity. However, when manifestations of exhaustion of mental activity predominate in the structure of the anxiety-asthenic syndrome, the drug does not affect the main clinical manifestations of the hypoergic component (fatigue, apathy, psychomotor retardation, daytime drowsiness) or even enhances them [30]. With optional manifestations of asthenia in the structure of anxiety-asthenic disorders, its positive changes are closely related to the anxiolytic effect and reduction of anxiety.

The results of a number of studies by A.B. Smulevich et al. (1998, 1999, 2005), Yu.A. Aleksandrovsky (2003) [3, 28] indicate that the effectiveness of benzodiazepine drugs varies depending on the structural composition of TGF. They turn out to be most effective in treating patients with affectively charged anxiety paroxysms, accompanied by isolated phobias without signs of persistent avoidance of situations in which panic attacks develop. As the clinical picture of TFD becomes more complex due to persistent agoraphobia with avoidant behavior, hypochondriacal phobias that arise out of connection with a specific situation, which indicates a high probability of chronicity of the condition, resistance to monotherapy with benzodiazepine derivatives increases.

Schizophrenia and schizotypal disorder

Phenazepam is widely used in the clinic for the correction of anxiety states within the framework of delusional and affective-delusional states, TDF in low-progressive schizophrenia (ICD-10 categories F20.0, F21, F22, F45) [1, 6, 19, 20, 25, 29 ], as well as for the treatment of diencephalic disorders that occur with long-term use of traditional and some atypical antipsychotics [31].

Autonomic disorders

A study of the vegetotropic effect of phenazepam on neurotic patients at a daily dose of 3 mg compared with diazepam at a dose of 40 mg/day showed that it appeared on days 4–5, coinciding with the anxiolytic effect. A pronounced vegetotropic effect occurred on the 10–12th day. The use of phenazepam turned out to be more effective in the sympathoadrenal than in the vagoinsular structure of the autonomic crisis. In terms of its therapeutic effect on autonomic symptoms, phenazepam was more effective than diazepam [7, 21, 23, 26].

Sleep disorders

A study of the effect of phenazepam in sleep disorders showed its clear positive effect on all types of this pathology (disturbances in falling asleep, night awakenings, early insomnia), superior in severity and speed of onset to all other tranquilizers, including diazepam. The effect of the drug, as a rule, was not accompanied by morning drowsiness and lethargy [2, 7]. Phenazepam is also effective for sleep disorders of alcohol origin [8]. It must be emphasized that when prescribing phenazepam as a hypnotic drug, it is necessary to take into account the periods of use currently recommended by WHO and domestic guidelines, i.e. the duration of use of the drug should not exceed 1 month [7].

Epilepsy

A review summarizing the use of benzodiazepine tranquilizers in epilepsy noted that phenazepam can be successfully used in combination with anticonvulsants to treat various types of seizures [14, 21]. The inclusion of phenazepam in the treatment regimen for resistant polymorphic seizures led to a complete cessation or halving of their frequency in 60% of patients [15, 22, 23].

Neurological disorders

The presence of muscle relaxant action of phenazepam allows its use in neurological disorders, such as extrapyramidal disorders, increased muscle tone (tardive dyskinesia, essential tremor, restless legs syndrome) [23]. There is successful experience in using the drug for headaches (tension headache, migraine, post-traumatic encephalopathy) [23].

Somatic and psychosomatic diseases

As noted above, in addition to their widespread use in the treatment of mental disorders and psychoneurological disorders, benzodiazepine tranquilizers, in particular phenazepam, can be successfully used in the treatment of somatic and psychosomatic diseases. Thus, in the monographic work of V.A. Raisky [22] noted the high effectiveness of benzodiazepines in anxiety, anxiety-phobic and accompanying vegetative disorders in cardiovascular, gastrointestinal, pulmonary and other diseases. Moreover, depending on the task, the drug had both a main anxiolytic effect and hypnosedative, anticonvulsant and muscle relaxant effects. It was noted that phenazepam in doses of 1.5–2.0 mg/day was superior to diazepam and nitrazepam in all types of action, demonstrating equal results with lorazepam. A moderate analgesic effect of the drug was also noted [23].

Phenazepam is widely used in cardiology. The main indications for its use are neurohumoral disorders of the cardiovascular system in the form of vegetative paroxysms of the sympathetic-adrenal type with cardialgia, hyperhidrosis, tachycardia, accompanied by fear of death and psychomotor agitation. The use of phenazepam at a dose of 1–3 mg/day relieves vegetative paroxysms, sleep disorders and cardialgia [21]. There is evidence that phenazepam at a dose of 1.5 mg/day has an antiarrhythmic effect in various heart rhythm disorders - atrial, ventricular, supraventricular extrasystole, paroxysms of atrial fibrillation. Phenazepam is most effective (69%) for patients with an association of heart rhythm disturbances and neurotic disorders [26].

Phenazepam is successfully used in the complex therapy of coronary heart disease. Already in the first days of taking the drug, patients’ sleep at night is normalized, anxiety and fear for their life and health, irritability, and fixation on various manifestations of the disease are reduced. Phenazepam has a pronounced positive effect on autonomic-vascular dysfunctions - headache, sweating, respiratory arrhythmia. It was found that for neurosis-like disorders in patients with coronary artery disease, phenazepam is more effective (70%) than diazepam (62%) and chlordiazepoxide (49%) [27].

Benzodiazepines are widely used in anesthesiology and resuscitation. They are used for pre-operative sedation as an introductory drug for general anesthesia and potentiation of its effect.

Phenazepam is used for sedation of severely ill patients on mechanical ventilation. The drug is able to block the mechanisms of psychogenic provocation of bronchial asthma attacks, which occurs in 19–51% of patients [28].

In gynecological practice, phenazepam is used in the treatment of premenstrual tension syndrome. It has been shown to be more effective than traditionally used hormonal therapy for this pathology [16].

The presence of sedative and vegetostabilizing effects in benzodiazepines, the ability to reduce spastic phenomena, reduce the content of pepsin and hydrochloric acid in gastric juice justifies their use in the treatment of gastric ulcers, dyskinesias of the gastrointestinal tract, nonspecific ulcerative colitis, etc. In a daily dose of 2–3 mg phenazepam turned out to be effective for cardio- and angioneurosis, hyperventilation syndromes, irritable stomach, irritable colon, and irritable bladder [21].

Thus, the wide range of clinical effects of phenazepam makes it possible to use it in many areas of medicine.

Phenazepam safety problem

Issues related to tolerability, adverse effects, and dosage regimen and duration of use of benzodiazepines deserve special discussion. 1,4-benzodiazepine derivatives are one of the safest groups of drugs in medicine, due to the “wide corridor” between therapeutic and toxic doses. There are no data on deaths as a consequence of treatment with phenazepam and other tranquilizers in therapeutic doses; deaths from overdose of benzodiazepines are extremely rare [31, 32]. Drugs in this group do not have a significant effect on the cardiovascular, endocrine and urinary systems, or liver [32]. However, when prescribing phenazepam, one should take into account the possibility of its interaction with certain drugs used in both psychiatric and somatic practice. It is necessary to mention the ability of benzodiazepine tranquilizers in combination with barbiturates and opiates to depress the respiratory center. It is especially important to consider the risk of this complication when prescribing phenazepam to patients with chronic obstructive pulmonary diseases [18, 22].

Withdrawal syndrome is a much more serious aspect of inappropriate use of benzodiazepine anxiolytics. Most often, this phenomenon occurs when the drug is abruptly discontinued or after an unreasonably long (more than a month) course of therapy. The most typical withdrawal symptoms include anxiety, irritability, sleep disturbances, headaches, muscle twitching, tremors, increased sweating, and dizziness. In the vast majority of cases, to relieve withdrawal symptoms, it is enough to use the discontinued drug. According to a survey of general practitioners and psychiatrists in Moscow, of the cases assessed as withdrawal syndrome, 83% of patients had a mild form of the disorder that did not require drug treatment [24, 27]. There are polar opinions on this issue in the literature. The number of patients with withdrawal syndrome when using benzodiazepine anxiolytics ranges from 0.1 to 100%. It is often extremely difficult to distinguish the manifestations of this phenomenon from the signs of the underlying disease, which occurs predominantly with alarming symptoms [34].

In conclusion, considering the features of the clinical use of phenazepam, I would like to emphasize another undeniable advantage of this drug. Phenazepam is not a drug included in the list of potent drugs and can be sold in pharmacies using prescription form 107/u, which ensures its availability and ease of use.

Addiction treatment

Treatment of addiction to Phenazepam is a complex and lengthy process, which must be started in an inpatient setting under the supervision of doctors.

How addiction is formed

There are three stages in the development of dependence on Phenazepam:

• Stage of mental dependence. Usually they start taking Phenazepam in order to get rid of insomnia, constant fears, and feelings of anxiety. After taking the first doses, a person feels inner peace, his health improves, fears disappear, a good mood and a feeling of joy appear. However, tolerance develops very quickly; previous doses of the drug do not give the desired result. In order to again receive a charge of positive emotions, the person begins to increase the dose of the tranquilizer.
• Stage of physical dependence. Taking large doses of a tranquilizer does not go away without leaving a trace. Physical and mental dysfunctions appear and begin to rapidly increase. Taking the drug no longer brings the desired result, and an attempt to cancel the tranquilizer, or reduce the dose taken, leads to the development of withdrawal syndrome.
• Stage of decompensation. Physical and mental disorders in the body become irreversible. Lost interest in life. There is degradation and then disintegration of personality.

How long do drug addicts live?

Regular use of large doses of Phenazepam, especially in combination with alcohol and other psychotropics, sharply shortens life. Barbituromaniacs rarely live more than 15 years from the start of regular abuse. The most common causes of death are:

• severe overdose of a tranquilizer (death occurs as a result of stopping the respiratory and vasomotor centers);
• severe conditions developing against the background of withdrawal syndrome (sharp drop in blood pressure, severe forms of arrhythmias, status epilepticus);
• chronic intoxication with the development of internal organ failure (acute renal, liver failure);
• suicide.

Rehabilitation

Rehabilitation is the longest and most difficult stage of addiction treatment. Psychological work is one of the most difficult in medicine, requiring a lot of patience and perseverance. First of all, it is necessary to identify the reason why the patient decided to stop taking the tranquilizer, and then unobtrusively and constantly strive to strengthen this motivation.

The drug on which a person depends, and everything connected with it, occupy a very large place in the addict’s value system. It is important not only to remove the tranquilizer from the patient’s life, but also to fill the void left by this. Form a new view on the system of life values. This is facilitated by individual conversations, group classes, and various psychological techniques.

The program is considered completed if the addict sincerely, without coercion, completely voluntarily decides to stop taking the tranquilizer.

Why you can’t treat yourself at home

One of the main symptoms of drug addiction is anosognosia. A person does not realize that he is sick until it is too late. The appearance of withdrawal syndrome indicates an advanced disease. It is impossible to cope with the disease at home:

• the process of gradual withdrawal of the drug should be carried out under the supervision of a doctor and adjusted in time;
• it is impossible to complete a rehabilitation course without constant monitoring of the patient’s condition by a psychotherapist;
• at home, a tranquilizer is constantly available;
• misunderstanding by relatives of the condition in which the addict is.

Working with codependents

Often the patient’s relatives also need psychological help.

When working with codependents, a psychologist strives to:

• relieve relatives from feelings of guilt and inferiority;
• bring codependents out of a state of chronic depression;
• explain the essence of their loved one’s illness, teach them how to properly communicate with them, so as not to provoke a breakdown.

Resocialization

Resocialization is the last stage of inpatient treatment. At this stage, the convalescent is prepared for the most painless return to social life. It is important that the person recovering is not an outside observer of the efforts of social workers and psychotherapists, but that he himself directly participates in this process.

Convalescent is helped by:

• find a new job and, if necessary, undergo retraining;
• strengthen weakened relationships with family;
• solve the problem of free time and changing social circles.

Ambulatory treatment

Upon discharge from hospital, the risk of relapse of the disease is highest, so it is necessary to register with an outpatient psychotherapist as quickly as possible.

The doctor will help the convalescent to cope with the difficulties that he will encounter, especially in the first days outside the hospital, without resorting to a tranquilizer. Participating in various programs and communicating with other recovering people will help solve the problem of free time and change the circle of friends.

Consequences of long-term use

In the clinic, Phenazepam is prescribed in minimal dosages for a period of no more than a week. Long-term use of large doses of the drug leads to dysfunction of internal organs, peripheral and central nervous systems:

• myocardial dystrophy;
• renal failure;
• toxic hepatitis;
• severe sleep disturbances;
• rapid development of mental and physical dependence;
• convulsive readiness, muscle twitching,
• emotional lability, anxiety, aggressiveness;
• instability of attention, inability to assimilate any information;
• depression;
• polydrug addiction,
• suicide.

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Phenazepam analogs

Phenazepam is part of a large group of medications - benzodiazepines. They all have a similar mechanism of action and effect on the human body. Among the representatives of this class are:

• Diazepam is one of the oldest drugs, has a powerful anticonvulsant, hypnotic and sedative effect;
• Clonazepam – has a good hypnotic effect, reduces the tone of striated muscles;
• Bromazepam – in small doses causes an anxiolytic effect;
• Flunitrazepam – has a hypnotic, sedative, anticonvulsant effect.

All benzodiazepines suppress the activity of the central nervous system, which causes changes on both the physical and mental levels. Abuse of benzodiazepines leads to impairment of memory and intelligence, speech is impaired, lethargy appears, and moral and ethical standards of behavior are violated.

Long-term use of drugs disrupts the function of all somatic organs, as well as brain structures. The group of benzodiazepines, and therefore Phenazepam, is similar in mechanism of action to the action of barbiturates and ethanol.