"Phenazepam" is the first tranquilizer in the USSR, created by a group of scientists in the early seventies of the last century. At first, the drug was mainly used by military doctors, then its use became popular in the treatment of depression, insomnia and other neurological problems. The action of "Phenazepam" is an anticonvulsant, sedative and hypnotic effect. The drug is often highly addictive and is recognized as a drug in many countries.
General information
"Phenazepam" is a potent tranquilizer. It has a highly active effect on the nervous system. It is recommended for use as prescribed and under the supervision of a physician, as unpredictable reactions to Phenazepam may occur. What effect the drug will have in case of uncontrolled use is not known.
In the case of long-term use (more than two months), the tablets can be highly addictive, which will lead to aggravation of problems. Abuse threatens to develop severe depression and even a desire to commit suicide.
The duration of "Phenazepam" is several hours. After oral administration, the drug is easily absorbed, within 1-2 hours the maximum concentration of the active substance in the blood is observed. The half-life is six to eighteen hours, depending on the dosage.
The action of the drug
The drug is characterized by actions of a different nature. The anxiolytic effect is expressed in the form of a decrease in emotional stress, relieving feelings of fear, anxiety, anxiety and panic. It is caused by the effect of the drug on the central nervous system.
The sedative effect is manifested by a decrease in neurotic symptoms, due to the effect on the brain stem and thalamic nuclei. At the same time, patients experience gradual calming, removal of aggressiveness, irritability, nervousness.
The anticonvulsant effect is due to increased nervous inhibition. At the same time, the impulses that caused such manifestations are suppressed.
The hypnotic effect is associated with the inhibition of brain cells, which reduces the impact of stimuli that affect the mechanism of falling asleep (emotional, motor provocateurs). As a result, the duration and regularity of sleep is regulated.
Indications
The action of "Phenazepam" is depressing on the nervous system, so the need to take the drug should be determined only by a doctor. As a rule, the medicine is prescribed in the following cases:
- psychopathic and neurological conditions;
- fear;
- irritability, aggressiveness;
- panic, a state of psychosis;
- sleep disorders;
- treatment of alcoholism (acts as an aid);
- phobias, mania;
- preparation for surgery;
- epilepsy.
Contraindications
It is strictly forbidden to take the drug with alcoholic beverages. The action of "Phenazepam" with alcohol can lead to a state of shock. In addition, there are a number of other strict restrictions:
- in an acute form;
- angle-closure glaucoma (including a tendency to it);
- coma;
- shock state;
- myasthenia gravis;
- hypersensitivity to components;
- acute poisoning with drugs, sleeping pills, alcohol;
- childhood and adolescence (action and effect are unknown);
- a state of severe depression.
Pregnant and lactating women are highly discouraged from taking Phenazepam. The effect on the child's body can be overwhelming and depressing, as a result of which newborns are born lethargic (with poor breathing, appetite, sedentary), often with congenital pathologies of the nervous system. It is especially dangerous to use the drug in the first trimester of pregnancy.
Overdose
In case of abuse of the drug, the action of "Phenazepam" can be extremely unpleasant consequences, leading to disruption of the body's activity. An overdose has a negative effect on the nervous system, expressed in the following conditions:
- oppression of consciousness;
- confusion of movements;
- slurred speech;
- excessive sleepiness;
- decreased reflexes;
- coma.
An excess of a tranquilizer often leads to a violation of the cardiac and respiratory systems, provoking a decrease in pressure, shortness of breath, causing tachycardia or bradycardia. Possible digestive problems:
- constipation;
- diarrhea;
- nausea, vomiting;
- heartburn;
- dry mouth.
The action of "Phenazepam" is characterized by a negative effect on the functionality of the kidneys and the genitourinary system, therefore, in case of an overdose, violations such as:
- incontinence or urinary retention;
- acute kidney failure;
- decreased libido.
Among other things, the abuse of the drug threatens to cause fever, jaundice, breathing difficulties, or even death.
Peculiarities
The effect of tablets ("Phenazepam") is especially noticeable in cases where the patient has not previously used psychoactive drugs. In such cases, the dose of the drug should be minimal, since "beginners" are especially susceptible to pills.
With prolonged use of the drug in large doses, a strong dependence may develop, therefore it is not recommended to prescribe a course of more than 2 weeks (in rare cases, a month). Abrupt cessation of the use of tablets sometimes provokes a withdrawal reaction, which manifests itself in insomnia, aggressiveness or excessive sweating.
It is forbidden to drink any alcohol-containing drinks while using Phenazepam. The effect on the body when interacting with sleeping pills or narcotic drugs is enhanced in the manifestation of depression of the central nervous system. Such a combination guarantees a state of extreme inadequacy and can last several days.
"Phenazepam" affects, therefore, during treatment it is not recommended to drive vehicles, operate machinery and engage in any other activity that requires increased concentration.
In this medical article, you can get acquainted with the drug Phenazepam. The instructions for use will explain in which cases you can take pills, what the medicine helps with, what are the indications for use, contraindications and side effects. The annotation presents the form of release of the drug and its composition.
In the article, doctors and consumers can only leave real reviews about Phenazepam, from which you can find out if the drug helped in the treatment of neurosis, psychosis, epilepsy and other mental and psychosomatic disorders and diseases in adults and children, for which it is also prescribed. The instructions list the analogues of Phenazepam, the prices of the drug in pharmacies, as well as its use during pregnancy.
Phenazepam is a highly active tranquilizer that has a pronounced anxiolytic, anticonvulsant, hypnotic and central muscle relaxant effect on the body. Instructions for use prescribes taking pills for the treatment of psychosis, sleep disorders, neurotic and psychopathic conditions.
Release form and composition
The drug Phenazepam is available in the form of tablets for oral administration with a dosage of 500 mcg, 1 mg and 2.5 mg.
Tablets are white, flat-cylindrical, scored on one side. The medicine is packed in blister packs of 10 pieces and 25 pieces in a cardboard box, an annotation with a detailed description of the characteristics is attached to the tablets.
Each tablet contains the active ingredient Phenazepam at a dosage of 500 mcg, 1 mg, 2.5 mg, respectively.
pharmachologic effect
Phenazepam instruction refers to tranquilizers that have anxiolytic, anticonvulsant, central muscle relaxant and sedative effects. The tranquilizing and anti-anxiety effect is superior in strength to Phenazepam's analogues.
Also, the drug has an anticonvulsant and hypnotic effect. The anxiolytic effect of the drug is expressed in a decrease in emotional stress, weakening fear, anxiety and anxiety. According to the reviews received, the medication has practically no effect on affective, hallucinatory and acute delusional disorders.
What helps Phenazepam?
Indications for the use of the drug include:
- neurosis, pseudo-neurotic (neurosis-like) states, psychopathy, psychopathic disorders and other conditions that are characterized by the appearance of a feeling of fear, increased anxiety, irritability, mood variability (its lability), increased tension;
- alcohol withdrawal syndrome;
- a sharp increase in tone and stable resistance of the muscles to the effects of deforming forces (muscle rigidity);
- instability (lability) of the autonomic nervous system;
- dyskinesia, tics;
- autonomic dysfunction syndrome;
- hypochondriacal syndrome, accompanied by various kinds of unpleasant or painful sensations (hypochondriac-senestopathic syndrome, including in cases where treatment with other tranquilizers did not give the expected result);
- temporal and myoclonic epilepsy;
- reactive psychosis;
- prevention of phobic conditions and conditions accompanied by a feeling of tension;
- sleep disorders;
- panic reactions.
The annotation to the drug also indicates that Phenazepam can be used for preliminary drug preparation of patients for general anesthesia and surgery.
Instructions for use
Phenazepam is prescribed orally. A single dose is usually 0.5-1 mg, and for sleep disorders - 0.25-0.5 mg 20-30 minutes before bedtime.
- For the treatment of neurotic, psychopathic, neurosis-like and psychopathic conditions, the initial dose is 0.5-1 mg 2-3 times a day. After 2-4 days, taking into account the effectiveness and tolerability of the drug, the dose can be increased to 4-6 mg per day, the morning and afternoon dose is 0.5-1 mg, at night - 2.5 mg.
- With severe agitation, fear, anxiety, treatment begins with a dose of 3 mg per day, rapidly increasing the dose until a therapeutic effect is obtained.
- In the treatment of epilepsy, the dose is 2-10 mg per day.
- For the treatment of alcohol withdrawal prescribed at a dose of 2.5-5 mg per day.
In neurological practice, in diseases with increased muscle tone, the drug is prescribed 2-3 mg 1 or 2 times a day. The average daily dose of Phenazepam is 1.5-5 mg, it is divided into 3 or 2 doses, usually 0.5-1 mg in the morning and afternoon and up to 2.5 mg at night. The maximum daily dose is 10 mg.
In order to avoid the development of drug dependence, during the course of treatment, the duration of the use of phenazepam, like other benzodiazepines, is 2 weeks. But in some cases, the duration of treatment can be increased up to 2 months. When the drug is discontinued, the dose is reduced gradually.
Contraindications
Before you start taking Phenazepam tablets, you must definitely consult a neurologist or psychiatrist. Be sure to carefully read the instructions before you start taking the drug, the tablets should not be taken orally if the patient has one or more conditions:
- shock conditions;
- coma;
- pregnancy and breastfeeding period;
- age up to 18 years;
- individual hypersensitivity or intolerance to the drug;
- myasthenia gravis;
- acute respiratory failure;
- severe chronic obstructive pulmonary disease;
- closed-angle glaucoma.
Relative contraindications for use are:
- age of patients over 65 years;
- liver failure;
- depression;
- organic brain diseases;
- taking other psychotropic drugs;
- kidney failure.
Side effects
- dizziness, headache;
- nausea;
- impaired memory, concentration, coordination of movements (especially at high doses);
- dry mouth;
- ataxia;
- possibly paradoxical arousal;
- skin rash, itching;
- diarrhea;
- decreased libido;
- violation of the menstrual cycle;
- dysuria;
- muscle weakness;
- drowsiness.
With prolonged use, especially at high doses - addiction, drug dependence.
Children, during pregnancy and lactation
Phenazepam should not be used in the 1st trimester of pregnancy and lactation period. Pregnant women can take the medicine in case of emergency: the drug has a toxic effect on the fetus. The drug is contraindicated in children under 18 years of age.
special instructions
Caution is required when using Phenazepam in patients with hepatic or renal insufficiency, persons prone to substance abuse, with organic brain damage, and elderly patients.
Like analogues, Phenazepam can cause drug dependence during long-term therapy with high doses. During treatment, the use of ethanol is strictly prohibited.
It affects the concentration of attention, therefore, special care is required when driving vehicles for persons.
drug interaction
The drug Phenazepam is not recommended to be administered simultaneously with anticonvulsants, hypnotics, sedatives, tranquilizers. This is due to the fact that under the influence of these drugs, the therapeutic effect of the drug is enhanced, which increases the risk of side effects and overdose.
The drug enhances the antihypertensive effect of drugs for the treatment of arterial hypertension, which should be taken into account and doses of drugs should be adjusted to avoid a rapid drop in blood pressure.
Phenazepam's analogs
According to the structure, analogues are determined:
- Fezipam.
- Phenorelaxan.
- Elzepam.
- Thezaneph.
- Tranquezipam.
Analogues of Phenazepam have a similar effect:
- Lorazepam.
- Medazepam.
- Relium.
- diazepam.
- Alprazolam.
- Valium.
- Sidenar.
- Lorenin.
- Relanium.
- Apaurin.
- Lorafen.
- Tofisopam.
- Sibazon.
- Nozepam.
- Tavor.
- Ativan.
- Seduxen.
Holiday conditions and price
The average price of Phenazepam (tablets) in Moscow is 100 rubles. It is released from pharmacies only by prescription.
Keep the tablets out of the reach of children, at room temperature. The shelf life of the drug is indicated on the package and is 4 years from the date of production.
Phenazepam - instruction .... The drug phenazepam belongs to the group of tranquilizers or anxiolytic drugs ...
Prolonged use of the drug causes addiction syndrome. The patient's blood pressure may drop, the functioning of the organs of vision may deteriorate, the heart rhythm may be disturbed, and body weight may decrease.
Phenazepam has a very bad effect on the central nervous system of the fetus if a pregnant woman takes it.
If treatment with phenazepam causes many undesirable effects, then this may be due to the individual characteristics of the patient's body. Also, with a decrease in the amount of the drug, relief of the condition is possible. Sometimes it is enough to temporarily reduce the amount or completely stop taking the medicine temporarily.
If treated with phenazepam for a long time, then it provokes addiction, akin to a drug addiction. If, on the background of long-term treatment, you abruptly stop taking the drug, then it will cause a withdrawal syndrome or "withdrawal", as well as increased intraocular pressure. Even the suspicion of angle-closure glaucoma is a contraindication.
You can not use the drug if the patient is in a state of intoxication after drinking alcohol, narcotic substances, as well as drugs to normalize sleep, especially if his main life support systems are suppressed. It is forbidden to use phenazepam in patients who are in a state of depression (treatment with this drug may cause suicide attempts).
It is strictly forbidden to use the drug during childbearing, especially the first three months, as well as during breastfeeding. In addition, many doctors consider the drug dangerous for children and adolescents. Therefore, it is not advisable to use it in the treatment of persons under the age of eighteen.
Only under the guidance and prescription of a doctor can the drug be used for people with severe disorders of the liver and kidneys. With great care, the drug should be taken by those who have previously had a drug addiction syndrome, as well as those who are psychologically dependent on taking certain types of drugs, patients with psychoses, and also patients in old age.
The drug phenazepam belongs to the group of tranquilizers or anxiolytic drugs.
Phenazepam is prescribed for neurotic conditions, for neuroses and similar disorders, for psychopathic conditions. The drug is also effective for emotional and mental instability, anxiety, irritability, as well as strong emotional stress. The drug is used to treat psychoses of a different nature, as well as hypochondria. Phenazepam is used in cases where other drugs do not help, including for the treatment of sleep disorders, with obsessive-compulsive disorders. The drug is used to normalize the patient's condition with alcohol and drug withdrawal syndrome, as well as to alleviate the condition of patients with epilepsy, including myoclonic and temporal forms.
You can use phenazepam in case of emergency for people who have suffered severe moral trauma, to relieve fear and relax.
A drug is prescribed for the treatment of schizophrenia, especially for the treatment of those patients who give a negative reaction to the use of other drugs. The drug is prescribed for muscle stiffness, hyperkinesis, athetosis and tics of various origins.
In addition, there is another use of this medicine. It is known that when giving a patient general anesthesia before surgery, several drugs are used. So one of them is sometimes phenazepam.
The drug is very serious and for some time now it has been forbidden to sell it in pharmacies without a special prescription from a doctor.
Phenazepam is available as tablets and as a liquid for injection. There are three versions of tablets with an active ingredient content of 0.5 milligrams, one milligram and two and a half milligrams. In addition to it, each tablet contains neutral components: milk sugar, potato starch, polyvidone, calcium stearate, talc. Tablets are sold in blisters of ten pieces, one or two blisters are packaged in a cardboard box. And also in plastic bottles of twenty and fifty tablets. There is a special packaging for use in hospitals, it contains one thousand tablets.
Tablets of white color, round, on the one hand divided in half by risk.
One ampoule of phenazepam contains one milliliter of liquid, including one milligram of the active ingredient. In addition to it, the liquid contains special medical glycerin, tween-80, sodium pyrosulfate, caustic soda, specially prepared water. Ampoules are packaged in blisters of five pieces. There are two blisters in one package. A special device for opening ampoules is attached to the package. The ampoule contains a completely transparent and colorless liquid.
When taken orally, phenazepam enters the bloodstream in a short time. After one hour, the maximum amount of the drug is observed in the blood. It is metabolized in the liver and has a half-life of six to eighteen hours in the solid form and six to ten hours in the liquid form. It is excreted from the body with urine.
Store drugs should be in a dark place at room temperature.
Phenazepam is a psychotropic drug under special state control. This is not harmless activated charcoal and not cough lozenges, but the most tranquilizer that has a pronounced anxiolytic (“anti-anxiety”), hypnotic, sedative (sedative), anticonvulsant and central muscle relaxant (reducing the tone of skeletal muscles) action. The international non-proprietary name of this drug - bromd- is difficult to remember even after repeated reading, but this, in fact, is not required: the main thing is to know that phenazepam belongs to the psychotropic drugs of the benzodiazepine series and has all the features inherent in benzodiazepines, while having several exclusive pharmacological "trump cards".
Phenazepam inhibits the activity of the central nervous system, pointwise affecting such brain structures as the thalamus and hypothalamus, as well as the limbic system. In close cooperation with gamma-aminobutyric acid (GABA), phenazepam, which has the ability to potentiate the action of the latter, enhances pre- and postsynaptic inhibition of the transmission of nerve impulses. Activation of GABA receptors consists in the stimulation of the GABA-benzodiazepine-chlorionophore prescription complex of benzodiazepine receptors by phenazepam. As a result, the sensitivity of GABA receptors to this mediator increases, thereby enhancing the inhibitory effect of GABA on the central nervous system. At the psychological level, the patient has a decrease in emotional stress, anxiety, anxiety, glimpses of a positive attitude, depression and obsessive fears go away.
Phenazepam is available in two dosage forms: tablets and solution for intravenous and intramuscular administration, and the solution is used mainly for the relief of withdrawal symptoms and, if necessary, the rapid removal of anxiety and psychomotor agitation. The drug is taken under the strict supervision of a doctor in the dosages prescribed by him. In severe (clinical) depression, the drug is even dangerous, because. may induce the patient to commit suicide. Elderly patients or persons with a weakened body as a result of any chronic disease should take phenazepam with extreme caution. The risk of developing certain side effects is determined by the individual response to the drug of each individual patient, the dose and duration of the therapeutic course. After discontinuation of the drug, unwanted side effects disappear. Long-term use of phenazepam in significant doses, the actual abuse of it, is fraught with the development of drug dependence, which is true for any benzodiazepine. Abrupt withdrawal of the drug is also undesirable, because. can provoke the so-called rebound syndrome: in relation to phenazepam, its sign will be increased depression, irritability, hyperhidrosis - i.e. all those symptoms that were successfully defeated during the medication course.
Pharmacology
Anxiolytic agent (tranquilizer) of the benzodiazepine series. It has an anxiolytic, sedative-hypnotic, anticonvulsant and central muscle relaxant effect.
Enhances the inhibitory effect of GABA on the transmission of nerve impulses. Stimulates benzodiazepine receptors located in the allosteric center of postsynaptic GABA receptors of the ascending activating reticular formation of the brain stem and intercalary neurons of the lateral horns of the spinal cord; reduces the excitability of the subcortical structures of the brain (limbic system, thalamus, hypothalamus), inhibits polysynaptic spinal reflexes.
The anxiolytic effect is due to the effect on the amygdala complex of the limbic system and manifests itself in a decrease in emotional stress, weakening anxiety, fear, anxiety.
The sedative effect is due to the effect on the reticular formation of the brain stem and nonspecific nuclei of the thalamus and is manifested by a decrease in the symptoms of neurotic origin (anxiety, fear).
It practically does not affect the productive symptoms of psychotic genesis (acute delusional, hallucinatory, affective disorders), rarely there is a decrease in affective tension, delusional disorders.
The hypnotic effect is associated with inhibition of the cells of the reticular formation of the brain stem. Reduces the impact of emotional, vegetative and motor stimuli that disrupt the mechanism of falling asleep.
The anticonvulsant effect is realized by enhancing presynaptic inhibition, suppresses the spread of the convulsive impulse, but the excited state of the focus is not removed. The central muscle relaxant effect is due to the inhibition of polysynaptic spinal afferent inhibitory pathways (to a lesser extent, monosynaptic ones). Direct inhibition of motor nerves and muscle function is also possible.
Pharmacokinetics
After oral administration, it is well absorbed from the gastrointestinal tract, T max - 1-2 hours. It is metabolized in the liver. T 1/2 - 6-10-18 hours. Excreted mainly by the kidneys in the form of metabolites.Release form
Tablets are white, ploskotsilindrichesky, with a facet.
Excipients: lactose, potato starch, gelatin, calcium stearate, stearic acid.
10 pieces. - cellular contour packings (5) - packs of cardboard.
Dosage
In / m or / in (jet or drip): for the rapid relief of fear, anxiety, psychomotor agitation, as well as autonomic paroxysms and psychotic conditions, the initial dose is 0.5-1 mg, the average daily dose is 3-5 mg, in severe cases - up to 7-9 mg.
Inside: for sleep disorders - 250-500 mcg 20-30 minutes before bedtime. For the treatment of neurotic, psychopathic, neurosis-like and psychopathic conditions, the initial dose is 0.5-1 mg 2-3 times a day. After 2-4 days, taking into account the effectiveness and tolerability, the dose can be increased to 4-6 mg / day. With severe agitation, fear, anxiety, treatment begins with a dose of 3 mg / day, quickly increasing the dose until a therapeutic effect is obtained. In the treatment of epilepsy - 2-10 mg / day.
For the treatment of alcohol withdrawal - inside, 2-5 mg / day or / m, 500 mcg 1-2 times / day, with vegetative paroxysms - / m, 0.5-1 mg. The average daily dose is 1.5-5 mg, it is divided into 2-3 doses, usually 0.5-1 mg in the morning and afternoon and up to 2.5 mg at night. In neurological practice, in diseases with muscle hypertonicity, 2-3 mg are prescribed 1-2 times / day. The maximum daily dose is 10 mg.
In order to avoid the development of drug dependence during course treatment, the duration of phenazepam use is 2 weeks (in some cases, the duration of treatment can be increased to 2 months). With the abolition of phenazepam, the dose is reduced gradually.
Interaction
With the simultaneous use of phenazepam reduces the effectiveness of levodopa in patients with parkinsonism.
Phenazepam may increase the toxicity of zidovudine.
There is a mutual enhancement of the effect with the simultaneous use of antipsychotic, antiepileptic or hypnotic drugs, as well as central muscle relaxants, narcotic analgesics, ethanol.
Inhibitors of microsomal oxidation increase the risk of developing toxic effects. Inducers of microsomal liver enzymes reduce the effectiveness.
Increases the concentration of imipramine in the blood serum.
With simultaneous use with antihypertensive agents, it is possible to increase the antihypertensive effect. Against the background of the simultaneous appointment of clozapine, it is possible to increase respiratory depression.
Side effects
From the side of the central nervous system and peripheral nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, fatigue, dizziness, decreased ability to concentrate, ataxia, disorientation, gait instability, mental and motor reactions slowdown, confusion; rarely - headache, euphoria, depression, tremor, memory loss, impaired coordination of movements (especially at high doses), mood depression, dystonic extrapyramidal reactions (uncontrolled movements, including the eyes), asthenia, myasthenia gravis, dysarthria, epileptic seizures (in patients with epilepsy); extremely rarely - paradoxical reactions (aggressive outbursts, psychomotor agitation, fear, suicidal tendencies, muscle spasm, hallucinations, agitation, irritability, anxiety, insomnia).
On the part of the hematopoietic organs: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, excessive fatigue or weakness), anemia, thrombocytopenia.
From the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, loss of appetite, constipation or diarrhea; abnormal liver function, increased activity of hepatic transaminases and alkaline phosphatase, jaundice.
From the genitourinary system: urinary incontinence, urinary retention, impaired renal function, decreased or increased libido, dysmenorrhea.
Allergic reactions: skin rash, itching.
Local reactions: phlebitis or venous thrombosis (redness, swelling or pain at the injection site).
Others: addiction, drug dependence; decrease in blood pressure; rarely - visual impairment (diplopia), weight loss, tachycardia.
With a sharp decrease in the dose or discontinuation of the intake, a withdrawal syndrome (irritability, nervousness, sleep disturbances, dysphoria, spasm of the smooth muscles of the internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremor, perception disorders, incl. hyperacusis, paresthesia, photophobia; tachycardia, convulsions, rarely - acute psychosis).
Indications
Neurotic, neurosis-like, psychopathic and psychopathic and other conditions (irritability, anxiety, nervous tension, emotional lability), reactive psychoses and senesto-hypochondriac disorders (including those resistant to the action of other anxiolytic drugs (tranquilizers), obsession, insomnia, withdrawal syndrome (alcoholism, substance abuse), status epilepticus, epileptic seizures (of various etiologies), temporal and myoclonic epilepsy.
In extreme conditions - as a means of facilitating overcoming feelings of fear and emotional stress.
As an antipsychotic agent - schizophrenia with hypersensitivity to antipsychotic drugs (including febrile form).
In neurological practice - muscle rigidity, athetosis, hyperkinesis, tic, autonomic lability (sympathoadrenal and mixed paroxysms).
In anesthesiology - premedication (as a component of introductory anesthesia).
Contraindications
Coma, shock, myasthenia gravis, angle-closure glaucoma (acute attack or predisposition), acute alcohol poisoning (with weakening of vital functions), narcotic analgesics and sleeping pills, severe COPD (respiratory failure may worsen), acute respiratory failure, severe depression (may manifest suicidal tendencies) I trimester of pregnancy, lactation period, children and adolescents under 18 years of age (safety and efficacy have not been determined), hypersensitivity (including to other benzodiazepines).
Application features
Use during pregnancy and lactation
During pregnancy, the use is possible only for health reasons. It has a toxic effect on the fetus and increases the development of congenital malformations when used in the first trimester of pregnancy. Admission at therapeutic doses in later pregnancy may cause CNS depression in the newborn. Chronic use during pregnancy can lead to physical dependence with the development of withdrawal syndrome in the newborn. Children, especially at a younger age, are very sensitive to the CNS depressant effects of benzodiazepines.
Use immediately before or during labor may cause respiratory depression, decreased muscle tone, hypotension, hypothermia, and poor suckling (sluggish baby syndrome) in the newborn.
Application for violations of liver function
Use with caution in liver failure.Application for violations of kidney function
Use with caution in renal failure.
Use in children
Contraindicated in children and adolescents under 18 years of age (safety and efficacy not determined).special instructions
Use with caution in hepatic and / or renal failure, cerebral and spinal ataxia, a history of drug dependence, a tendency to abuse psychoactive drugs, hyperkinesis, organic brain diseases, psychosis (paradoxical reactions are possible), hypoproteinemia, sleep apnea (established or suspected ) in elderly patients.
With renal and / or liver failure and long-term treatment, it is necessary to monitor the picture of peripheral blood and the activity of liver enzymes.
In patients who have not previously taken psychoactive drugs, there is a therapeutic response to the use of phenazepam at lower doses, compared with patients taking antidepressants, anxiolytics or suffering from alcoholism.
Like other benzodiazepines, it has the ability to cause drug dependence with long-term use in high doses (more than 4 mg / day). With a sudden cessation of administration, a withdrawal syndrome may occur (including depression, irritability, insomnia, increased sweating), especially with prolonged use (more than 8-12 weeks). If patients experience such unusual reactions as increased aggressiveness, acute states of arousal, fear, suicidal thoughts, hallucinations, increased muscle cramps, difficulty falling asleep, superficial sleep, treatment should be discontinued.
In the process of treatment, patients are strictly prohibited from using ethanol.
The efficacy and safety of the drug in patients under 18 years of age has not been established.
In case of an overdose, severe drowsiness, prolonged confusion, decreased reflexes, prolonged dysarthria, nystagmus, tremor, bradycardia, shortness of breath or shortness of breath, decreased blood pressure, coma are possible. Gastric lavage, activated charcoal are recommended; symptomatic therapy (maintenance of breathing and blood pressure), the introduction of flumazenil (in a hospital setting); hemodialysis is ineffective.
Influence on the ability to drive vehicles and control mechanisms
During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.
Catad_tema Psychiatry - articles
Phenazepam: a modern view on efficacy and safety
Phenazepam is effective in various conditions and is used in almost any field of medicine, being a highly effective, fast-acting and safe agent for solving a huge number of tactical problems that clinicians face in their practice. At the same time, the appointment of phenazepam (as well as all benzodiazepine derivatives) is not recommended as a long-term therapy. The course of treatment with the drug should not exceed 1 month. Obviously, the combination of a wide therapeutic profile of the drug, the power and safety of its action still determines the high demand for phenazepam in the treatment of mental disorders with anxiety manifestations, psychosomatic disorders and, in some cases, somatic diseases as an adjuvant therapy.
Keywords: phenazepam, benzodiazepines, anxiety, insomnia, vegetosis, psychosomatic disorders
It is probably difficult to imagine a better known anxiolytic drug, which has long come into use in psychiatric and general medical practice, than phenazepam. Such a wide distribution of this drug is an indirect recognition of its merits, but also often leads to thoughtless, uncontrolled intake. At the same time, among many doctors and patients there are a number of prejudices against tranquilizers in general and phenazepam in particular. Nevertheless, like any other drug, it has its undoubted positive properties, as well as features that require attention and precautions. Without consideration of all these aspects, the effective use of phenazepam is impossible, 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 from the Institute of Pharmacology of the USSR Academy of Medical Sciences under the direction of V.V. Zakusova. According to its chemical structure, it is a benzodiazepine derivative (7-bromo-5-(orthochromphenyl)-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 transmission of nerve impulses to the CNS. The mechanism of action of phenazepam is determined by stimulation of the benzodiazepine receptors of the supramolecular GABA-benzodiazepine-chlorionophore-receptor complex, leading to the activation of GABA receptors, which in turn causes a decrease in the excitability of the 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 blood plasma is reached within 1-2 hours. Phenazepam is metabolized in the liver, its half-life is 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, sedative, hypnotic, muscle relaxant, and anticonvulsant effects. These 5 properties are expressed in drugs of this group to varying degrees. So, 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 neuroleptics, in a psychiatric and neurological clinic.
Mazepam, on the contrary, has a much less pronounced muscle relaxant and sedative effect 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 stationary conditions, in particular in the complex treatment of psychoses, as well as in anesthesiology. Phenazepam has all the named pharmacological effects equally. It is this versatility that explains its widespread use to this day, despite the availability of new generations of anti-anxiety drugs.
Another important advantage of phenazepam is a wide dosing rangewhen, depending on the dose used, various properties of the drug are realized:
- psychotropic (anxiolytic, sedative, hypnotic effects);
- somatotropic (muscle relaxant, anticonvulsant, vegetotropic, hypotensive effects).
In accordance with all of the above, it becomes clear that the pharmacological activity of phenazepam allows it to be effectively used in various fields of clinical medicine. This drug is actively used in the treatment of a wide range of mental disorders (neurotic disorders, personality disorders, affective disorders, schizophrenia, organic brain diseases, alcoholism, drug addiction) and somatic pathology in neurology, cardiology, pulmonology, gynecology, oncology, resuscitation , anesthesiology .
Psychoneurological disorders
When considering the disease states in which phenazepam is successfully used, mental disorders deserve attention first of all.
Anxiety-phobic disorders
To the fullest extent, the clinical and pharmacological effects of the drug are realized in patients with anxiety-asthenic, anxious and anxiety-phobic disorders that are simple in structure (TFR; ICD-10 headings F40, F41, F42, F43) in cases where phobias show a close comorbidity. connection with anxiety and are characterized by figurativeness, emotional richness. However, with the predominance of manifestations of mental exhaustion 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 sleepiness) or even enhances them. With facultative 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) indicate that the effectiveness of benzodiazepine drugs differs depending on the structural composition of TGF. They are most effective in the treatment of 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 TFR becomes more complicated due to persistent agoraphobia with avoidant behavior, hypochondriacal phobias arising 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 in the framework of delusional and affective-delusional states, TFR in low-progressive schizophrenia (sections according to ICD-10 F20.0, F21, F22, F45), as well as for the treatment of diencephalic disorders that occur with long-term use of traditional and some atypical antipsychotics.
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 manifested itself on the 4–5th day, coinciding with the anxiolytic effect. A pronounced vegtotropic effect occurred on the 10–12th day. The use of phenazepam turned out to be more effective in symptomatic-adrenal than in vagoinsular structure of the vegetative crisis. According to the therapeutic effect on autonomic symptoms, phenazepam was more effective than diazepam.
Sleep disorders
The study of the action of phenazepam in sleep disorders showed its clear positive effect on all types of this pathology (sleep disturbances, nocturnal awakenings, early insomnia), surpassing all other tranquilizers, including diazepam, in severity and speed of onset. The action of the drug, as a rule, was not accompanied by morning drowsiness and lethargy. Effective phenazepam and sleep disorders of alcoholic origin. It should be emphasized that when prescribing phenazepam as a hypnotic drug, it is necessary to take into account the currently recommended by the WHO and domestic guidelines for the timing of use, i.e. the duration of use of the drug should not exceed 1 month.
Epilepsy
A review summarizing the use of benzodiazepine tranquilizers in epilepsy notes that phenazepam can be successfully used in combination with anticonvulsants to treat various types of seizures. The inclusion of phenazepam in the treatment regimen for resistant polymorphic seizures led to a complete cessation or a halving of their frequency in 60% of patients.
Neurological disorders
The presence of a muscle relaxant effect in phenazepam allows its use in neurological disorders, such as extrapyramidal disorders, increased muscle tone (tardive dyskinesia, essential tremor, restless leg syndrome). There is a successful experience of using the drug for headaches (tension headache, migraine, post-traumatic encephalopathy).
Somatic and psychosomatic diseases
As noted above, in addition to being widely used in the treatment of mental disorders and neuropsychiatric disorders, benzodiazepine tranquilizers, in particular phenazepam, can be successfully used in the treatment of somatic and psychosomatic diseases. So, in the monographic work of V.A. Raisky noted the high effectiveness of benzodiazepines in anxiety, anxiety-phobic and accompanying autonomic disorders in cardiovascular, gastrointestinal, pulmonary and other diseases. At the same time, depending on the task, the drug had both the 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 in all types of action to diazepam and nitrazepam, demonstrating equal results with lorazepam. A moderate analgesic effect of the drug was also noted.
Phenazepam has been 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 stops autonomic paroxysms, sleep disorders and cardialgia. There is evidence that phenazepam at a dose of 1.5 mg / day has an antiarrhythmic effect in various cardiac arrhythmias - atrial, ventricular, supraventricular extrasystoles, paroxysms of atrial fibrillation. The most effective is phenazepam (69%) for patients with an association of cardiac arrhythmias and neurotic disorders.
Phenazepam is successfully used in the complex therapy of coronary heart disease. Already in the first days of taking the drug in patients, night sleep normalizes, anxiety and fear for one's life and health, irritability, and fixation on various manifestations of the disease decrease. Phenazepam has a pronounced positive effect on vegetative-vascular dysfunctions such as headache, sweating, and respiratory arrhythmia. It was found that in neurosis-like disorders in patients with IHD, phenazepam is more effective (70%) than diazepam (62%) and chlordiazepoxide (49%).
Benzodiazepines are widely used in anesthesiology and resuscitation. They are used for preoperative 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 asthma attacks, which occurs in 19-51% of patients.
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 in this pathology.
The presence of sedative and vegetative-stabilizing 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 ulcer, dyskinesia of the gastrointestinal tract, nonspecific ulcerative colitis, etc. In a daily dose of 2–3 mg phenazepam proved to be effective in cardio- and angioneurosis, hyperventilation syndromes, irritable stomach, irritated colon, irritated bladder.
Thus, a wide range of clinical effects of phenazepam makes it possible to use it in many fields of medicine.
Phenazepam safety issue
Issues relating to tolerability, adverse effects, as well as dosing regimen and duration of use of benzodiazepines deserve special discussion. Derivatives of 1,4-benzodiazepine 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 are extremely rare with an overdose of benzodiazepines.
Drugs in this group do not have a significant effect on the cardiovascular, endocrine and urinary systems, liver. However, when prescribing phenazepam, one should take into account the possibility of its interaction with some drugs used both in 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 disease.
Withdrawal 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 twitches, tremors, increased sweating, and dizziness. In the vast majority of cases, it is enough to use the canceled drug to stop the phenomena of the withdrawal syndrome. According to a survey of general practitioners and psychiatrists in Moscow, of the cases assessed as a withdrawal syndrome, 83% of patients had a mild form of the disorder that did not require medical treatment. There are conflicting opinions in the literature on this issue. 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 mainly with alarming symptoms.
In conclusion, considering the features of the clinical use of phenazepam, I would like to emphasize one more indisputable advantage of this drug. Phenazepam does not belong to the list of strong drugs and can be sold in pharmacies with prescriptions form 107 / y, which ensures its availability and ease of use. Literature 1. Avrutsky G.Ya., Aleksandrovsky Yu.A., Berezova N.Yu. Application of the new tranquilizer phenazepam in psychiatric practice. Journal. neuropatol. and a psychiatrist. them. S.S. Korsakov. 1979;3:344–50.
2. Aleksandrovsky Yu.A. Clinical pharmacology of tranquilizers. M., 1973.
3. Alexandrovsky Yu.A. The role of tranquilizers in the treatment of borderline mental disorders. Psychiatrist. and a psychopharmacologist. 2003;3:94-6.
4. Belousova S.G., Sigunova E.A. Clinical and experimental study of the effect of neuroleptics on the tranquilizing effect of phenazepam. In: New in therapy and organization of care for patients with borderline neuropsychiatric disorders. M., 1986. S. 88-94.
5. Valueva L.N. The dependence of the effectiveness of combination therapy with phenazepam and psychoanaleptics on the sequence
6. Vasiliev A.A., Nuller Yu.L. Study of the structure of anxiety-delusional syndrome in patients with schizophrenia during anxiolytic therapy. Journal. neuropatol. and a psychiatrist. them. S.S. Korsakov. 1986; 8:1217-22.
7. Voronina T.A. The position of Phenazepam among the drugs of the benzodiazepine series. New psychotropic drugs. Symposium materials. Lvov, 1978, p. 100.
8. Danilin V.P., Krylov E.N., Magalif A.Yu., Wright M.L. Influence of phenazepam on nocturnal sleep in patients with alcohol withdrawal syndrome. Journal. neuropatol. and a psychiatrist. them. S.S. Korsakov. 1985;2:263-66.
9. Drobizhev M.Yu. Psychopharmacotherapy in the general somatic network (somatotropic effects, compatibility with somatotropic drugs). Psychiatrist. and a psychopharmacologist. 2000;2:2.
10. Dubnitskaya E.B., Basov A.M. The use of phenazepam in the treatment of neurotic conditions. Journal. neuropatol. and a psychiatrist. them. S.S. Korsakov. 1978;9:1382-88.
11. Ivanets N.N., Igonin A.L. Clinical experience of the combined use of grandaxin, phenazepam and tranxen in chronic alcoholism. In the book: Small tranquilizers. L., 1979. S. 134-39.
12. P. A. Kanitsev and I. N. Kononov, 1982. Quoted from: Raisky V.A. Psychotropic drugs in the clinic of internal diseases. M., 1988.
13. Knyazeva N.A. The effect of tranquilizers and nootropics in asthenic disorders in patients with traumatic brain injury. In: New in therapy and organization of care for patients with borderline neuropsychiatric disorders. M., 1986. S. 95-9.
14. Kosoy M.Yu. Combined action of phenazepam with anticonvulsants. Diss. cand. honey. Sciences. M., 1982.
15. Levinsky M.V. The use of benzodiazepine drugs in the treatment of epilepsy (review). Journal. neuropatol. and a psychiatrist. them. S.S. Korsakov. 1989; 6:118-26.
16. Mezhevitinova A.E. Premenstrual syndrome (to help the practitioner). Gynecology. 2002;4:23.
17. Neznamov G.G. Clinical and pharmacological analysis of the action of combinations of psychotropic drugs in patients with borderline conditions. In: New in therapy and organization of care for patients with borderline neuropsychiatric disorders. M., 1986. S. 46-50.
18. Neznamov G.G. Interaction of tranquilizers and other psychopharmacological drugs. Psychopharmacotherapy of neurotic disorders. M., 1987. S. 252-68.
19. Neznamov GG, Molodavkin G.N., Zherdev V.P. Clinical and pharmacological patterns of the interaction of tranquilizers and neuroleptics in the treatment of anxiety and obsessive-phobic disorders. In book. Anxiety and obsessions / Ed. A.B. Smulevich. M., 1998. S. 191-204.
20. Nuller Yu.L., Tochilov V.A. Experience in the use of phenazepam for the treatment of patients with psychosis. Journal. neuropatol. and a psychiatrist. them. S.S. Korsakov. 1980;6:914-20.
21. Patsernyak S.A. Stress. Vegetoses. Psychosomatics. SPb., 2002. 384 p.
22. Raisky V.A. Psychotropic drugs in the clinic of internal diseases. M., 1988.
23. Rudenko G.M., Shatrova N.G., Lepakhin V.K. Psychotropic activity and effectiveness of phenazepam in the treatment of various conditions. In: Phenazepam. K, 1982.
24. Seredenin S.B., Voronina T.A., Neznamov GG., Zherdev V.P. Phenazepam. 25 years in medical practice. M., 2007.
25. Smulevich A.B., Vorobyov V.Yu., Dubnitskaya E.B. Some aspects of tranquilizer therapy for low-progressive schizophrenia. Sat: Topical issues of prevention and treatment of major mental illnesses. M., 1986. S. 116-21.
26. Smulevich A.B., Drobizhev M.Yu., Ivanov SV. Clinical effects of benzodiazepine tranquilizers in psychiatry and general medicine. M., 2005. S. 68.
27. Smulevich A.B., Ivanov SV., Drobizhev M.Yu. Benzodiazepines: history and current state of the problem. Journal. neuropatol. and a psychiatrist. them. S.S. Korsakov. 1998; 98(8):4-13.
28. Smulevich A.B., Mazaeva N.A., Golovanova L.A. and others. Differentiated pharmacotherapy of neurotic conditions (comparative efficacy of benzodiazepine derivatives). Journal. neuropatol. and a psychiatrist. them. S.S. Korsakov. 1976; 2:255-62.
29. Smulevich A.B., Tkhostov A.Sh., Ivanov SV., Andreev A.M. Treatment of anxiety-phobic disorders: immediate and long-term results, prognosis of effectiveness (clinical follow-up study. In the book. Anxiety and obsessions / Edited by A.B. Smulevich. M., 1998. S. 158-90.
30. Syunyakov S.A., Teleshova E.S. Phenazepam is an effective benzodiazepine anxiolytic in the treatment of borderline mental disorders. Journal. psychiatrist. and a psychopharmacologist. them. P.B. Gannushkin. 2013;6.
31. Schmauss C., Krieg J.C. Enlargement of cerebrospinal fluid spaces in long-term benzodiazepine users. Psychol. Med. 1987;17:869-73.
32. Laughren T.P., Baltey Y., Greenblat D.J. Chronic diazepam treatment in psychiatric outpatients. Asta Psychiatr. Scand. 1982; 65:171-79.
33. Wapler F. Cardiac and thoracic vascular surgery. Clin. Anaesthiol. 2003;17(2):219-33.
34. WHO. Program on substance abuse. Rational use of benzodiazepines. 1996.
