Phenazepam

Phenazepam is a drug from the category of anxiolytic drugs.

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Indications Phenazepam

It is used in the following cases:

• in psychopathy, psychopathic-like disorders, and other conditions in which there is a feeling of strong anxiety, fear, irritability, mood instability, and increased tension;
• for neuroses and various neurosis-like conditions;
• for sleep problems;
• in the reactive form of psychosis;
• hypochondriacal disorder, against the background of which various kinds of painful or uncomfortable sensations are observed (senestopathic syndrome; also when therapy with other tranquilizers has proven ineffective);
• SVD;
• in the prevention of phobias, as well as conditions that cause a feeling of tension;
• epileptic seizures of myoclonic or temporal form;
• panic symptoms;
• nervous tics, as well as dyskinesia;
• a sharp increase in muscle tone, as well as their stable resistance to deforming effects (muscle rigidity);
• instability of the autonomic nervous system;
• alcohol withdrawal.

Phenazepam is also allowed to be used as a preliminary drug preparation for a patient undergoing general anesthesia and subsequent surgery.

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Release form

It is produced in the form of a solution for intravenous or intramuscular injections, as well as in tablets.

The pack contains 20 tablets of the medicine.

The solution is distributed into glass ampoules, the volume of which is 1 ml. The box contains 10 such ampoules complete with a scarifier. The ampoules can also be sorted into blister packs - 5 or 10 pieces.

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Pharmacodynamics

The effect of Phenazepam is determined by the ability of diazepines to influence the functioning of different parts of the central nervous system.

The anxiolytic effect of the drug is provided by the effect of the element bromdihydrochlorophenylbenzodiazepine on the amygdala complex of the limbic system. This effect is manifested by weakening emotional tension, and in addition to this, feelings of anxiety, fear and anxiety.

The anxiolytic effect of Phenazepam is stronger than most psychotropic drugs from the diazepine category.

The sedative effect is provided by the action of the active element of the drug on the nerve structures located inside the central parts of the brainstem, as well as on the non-specific thalamic nuclei that form the diffuse system of the thalamus.

The drug has a general calming effect on the central nervous system, reducing the severity of its responses to external factors, and in addition to this, to psychomotor excitability. It also partially weakens daytime activity and attention, and at the same time reduces the speed of motor and mental responses, etc.

By regulating the activity of the central nervous system, the drug reduces the intensity of the influence of various psycho-emotional, motor, and autonomic stimuli that affect the process of falling asleep.

The hypnotic effect is manifested in the fact that during the period of using the drug, the onset of sleep in the patient is significantly facilitated, the sleep itself becomes deeper, and its duration is prolonged.

At the same time, the suppressive effect on the central nervous system allows Phenazepam to enhance the effect of anesthetics, hypnotics, and analgesic drugs (in connection with this, the drug tablets are prohibited from being taken in combination with these drugs).

The effectiveness of the drug in the form of a muscle relaxant – the relaxing effect on skeletal muscles – is determined mainly by the ability of the active component to slow down polysynaptic (as well as monosynaptic, but with lesser severity) spinal-stem impulses.

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Pharmacokinetics

After oral administration, the tablets are well absorbed from the gastrointestinal tract. The period of reaching peak plasma values of the active element of the drug varies within 1-2 hours.

Phenazepam undergoes a process of hepatic metabolism. The half-life of the active substance in different people can vary within 6-18 hours. Excretion of metabolic products occurs mainly through the kidneys.

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Dosing and administration

Using medicine in tablet form.

The tablets must be taken orally. On average, it is allowed to take 0.0015-0.005 g of the medicinal substance per day. This portion should be divided into approximately 2-3 uses.

In the morning and during the day, it is necessary to consume 0.0005 or 0.001 g of Phenazepam, and in the evening it is allowed to increase the portion size to 0.0025 g. It is allowed to take no more than 0.01 g of the drug per day.

Use of tablets for various diseases:

• conditions in which sleep problems are observed: the drug should be taken approximately 30 minutes before bedtime, in a portion of 0.00025 or 0.0005 g;
• psychopathy and psychopathic-like disorders, as well as neuroses and pseudo-neurotic conditions: start therapy with a daily dose of 0.0015-0.003 g. This dose should be divided into 2-3 doses. After several days (usually after 2-4 days - taking into account the effectiveness of the treatment and the patient's tolerance of the drug), it is allowed to increase the dosage to 0.004-0.006 g / day;
• a feeling of strong anxiety or fear, motor anxiety, as well as vegetative forms of paroxysms: therapy should be started with a daily dose of 3 mg. Then it is quickly increased to obtain the required medicinal effect;
• epileptic seizures: the daily dose ranges from 0.002-0.01 g;
• alcohol withdrawal: the daily dosage is 0.0025-0.005 g;
• diseases that increase muscle tone: you need to take 0.002-0.006 g of the drug per day.

To eliminate the risk of addiction and the development of drug dependence, the drug should be prescribed in separate courses that last a maximum of 14 days. Sometimes it is allowed to extend the course - up to 2 months. It is necessary to stop taking the drug by gradually reducing the size of the portion taken.

Use of the drug in the form of a medicinal solution.

The solution is usually administered intramuscularly or intravenously (drip or jet). The size of a single dose is 0.0005-0.001 g (this is the volume of half or a whole ampoule of the solution). On average, patients are administered 0.0015-0.005 g per day. It is permissible to administer no more than 0.01 g of the drug per day.

Method of administration and dosage regimen for the treatment of various diseases:

• elimination of panic attacks, feelings of severe anxiety, fears, psychotic states, in addition to psychomotor agitation: at the initial stage of therapy, the average daily dosage required is 0.003-0.005 g - in the form of a 0.1% solution it is equal to 3-5 ml. In extremely severe conditions, it is allowed to increase the portion size to 0.007-0.009 g;
• treatment of epileptic seizures: administer the drug intravenously or intramuscularly. The initial dose is 0.0005 g;
• alcohol withdrawal: the drug should be administered intravenously or intramuscularly. The daily dose is within 0.0025-0.005 g;
• pathologies of a neurological nature, against the background of which muscle hypertonicity develops: the drug should be administered intramuscularly, at a dosage of 0.0005 g. The procedure must be carried out 1-2 times a day;
• in preparation for anesthesia, as well as during surgery: the drug should be administered intravenously, at a minimum rate. The dose is 0.003-0.004 g.

Once the desired medicinal effect from the solution is achieved, it is necessary to transfer the patient to oral administration of Phenazepam in tablets as soon as possible and continue the course of treatment in this form.

The therapeutic course using injections of drugs can last no more than 14 days. Only occasionally and with the doctor's prescription can it be extended to 3-4 weeks. During the process of drug withdrawal, it is necessary to reduce the dosage gradually.

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Use Phenazepam during pregnancy

Nursing and pregnant women are allowed to use Phenazepam only if there are vital indications.

Taking medications in the first trimester increases the likelihood of the baby developing congenital anomalies.

Use of the drug in the 3rd trimester (especially in the last weeks of pregnancy) causes accumulation of the active component inside the tissues of the fetus, as a result of which the activity of the central nervous system in the newborn is suppressed.

When the drug is taken shortly before birth, the newborn baby develops symptoms such as a disorder of the sucking reflex, muscle weakness, respiratory depression and severe hypothermia.

Long-term use of the drug during pregnancy can cause the baby to develop physical dependence on the drug, as well as the development of signs of withdrawal syndrome.

It is permissible to use the medicine with extreme caution directly during labor. For example, if labor began prematurely or the woman had premature placental abruption.

Parenteral administration of the solution in small doses usually does not have a negative effect on the infant. However, when using large doses, hypothermia or suffocation may occur, as well as heart rhythm disturbances and a decrease in blood pressure.

It is forbidden to use Phenazepam during lactation, because the active element of the drug is excreted with mother's milk. The metabolism of this component in infants occurs much more slowly than in adults, so the products of its metabolism begin to accumulate inside the body, causing the development of a sedative effect. Such an effect can lead to difficulties with the feeding process and weight loss in the baby.

Contraindications

Due to the fact that Phenazepam is included in a group of drugs with a powerful therapeutic effect, it has several contraindications, including:

• state of coma or shock;
• presence of myasthenia symptoms;
• closed-angle glaucoma (both in acute form and in those people who are predisposed to developing this pathology);
• when a person is diagnosed with COPD (because the drug may lead to potentiation of respiratory failure);
• acute respiratory failure;
• persons under 18 years of age;
• people who have an intolerance to drugs from the benzodiazepine category, and in addition, hypersensitivity to any of the additional components of the drug.

People with severe renal or hepatic dysfunction are allowed to use the drug only under the supervision of an experienced physician.

Caution is required when prescribing to individuals who have previously experienced drug dependence syndrome, people suffering from psychological dependence on certain types of drugs, and also to elderly patients.

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Side effects Phenazepam

Many patients, especially at the initial stage of therapy, experience an increase in drowsiness, a feeling of lethargy and fatigue in a chronic form, dizziness, as well as problems with orientation in space and concentration. In addition, signs of ataxia and confusion develop, and in addition, there is a slowdown in the speed of motor and mental impulses.

Less frequently, some manifestations from the nervous system occur: such as a feeling of euphoria, tremor, depression, memory loss, headaches, problems with coordination of movements (especially if the drug is used in large doses) and extrapyramidal disorders of a dystonic nature. Such disorders as decreased mood, myasthenia, signs of asthenic syndrome, and dysarthria are also possible.

Single use of the drug causes the appearance of paradoxical symptoms - the development of phobias, uncontrollable outbursts of aggression, the emergence of a feeling of severe anxiety, hallucinations, muscle spasticity, as well as a tendency to suicide and sleep disorders.

Hematopoietic organs: a decrease in the level of the main components of this system (leukocytes, as well as post-cellular structures, including platelets with erythrocytes), and in addition to this, neutrophilic granulocytes and hemoglobin is observed.

Among the negative effects affecting the digestive function: severe dryness of the oral mucosa, loss of appetite, diarrhea or constipation, increased salivation, nausea and heartburn. In addition, the development of jaundice and an increase in the activity of liver transaminases, as well as alkaline phosphatase levels in the blood.

Damage to the reproductive organs: increased or, on the contrary, decreased libido. In addition, women may experience signs of dysmenorrhea. Some people experience allergy symptoms, including itching and rashes on the skin surface.

Other side effects that sometimes occur due to the use of the drug include:

• development of addiction to the drug;
• the emergence of drug dependence;
• decrease in blood pressure values;
• visual disturbances (including double vision);
• weight loss;
• problems with heart rhythm.

When the drug is abruptly discontinued or its dosage is reduced, patients develop withdrawal syndrome. It usually manifests itself in the form of the same symptoms that caused the patient to start using the drug.

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Overdose

In case of intoxication with Phenazepam, disorders may develop that pose a serious danger to the health and life of the patient. Because of this, it is extremely important to monitor the sizes of the dosages used.

With a slight excess of dosage, the victim develops side effects, mainly affecting the function of the central nervous system. At the same time, potentiation of the therapeutic effect of the drug is possible.

If the dosage is significantly exceeded, there is a danger not only for the nervous system, but also for the heart and respiratory system. This is due to the fact that the drug has the ability to suppress cardiac function and the activity of the respiratory center.

An overdose can also cause death, which usually occurs due to respiratory or cardiac arrest. In this regard, it is necessary to immediately contact medical specialists after the first signs of a disorder appear. Trying to eliminate the disorder on your own is strictly prohibited - this can only aggravate the problem.

To reduce the severity of the toxic effects of the drug, drugs that can block benzodiazepine conductors are usually prescribed (including Anexat, which is a special antidote to the drug Phenazepam).

This blocker should be administered intravenously, after diluting it in a solution of sodium chloride or glucose, in a dosage of 0.2 mg. In extremely rare cases, an increase in the portion size to 1 mg may be allowed.

In addition, in case of poisoning with the drug, symptomatic treatment procedures must be carried out to support the functioning of the lungs and heart. If these procedures are refused, the patient may develop a comatose state.

If negative symptoms appear on the part of other systems and organs, medications should be used that reduce the severity of these disorders.

Fatalities due to Phenazepam intoxication are quite common in alcoholics who take the drug with alcohol. This is because the drug potentiates the likelihood of side effects when used with alcohol.

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Interactions with other drugs

The combined use of the drug with agents that suppress the activity of the central nervous system (this list includes anticonvulsants, sleeping pills, and neuroleptics) causes a mutual potentiation of their medicinal properties.

Combined use with levodopa (used for Parkinson's disease) weakens its therapeutic effect.

The combination with zidovudine (an antiviral drug) enhances the toxic properties of the latter.

When taken together with drugs that inhibit the oxidation processes of microsomes, the likelihood of toxic manifestations of Phenazepam increases.

Combined use with drugs that induce microsomal oxidation processes leads to a decrease in the medicinal effect of the drug.

When combined with the tricyclic imipramine, an increase in its serum values is observed.

Taking it in combination with antihypertensive drugs leads to potentiation of the hypotensive properties of these drugs.

When combined with the neuroleptic clozapine, the effect of respiratory depression may be enhanced.

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Storage conditions

Phenazepam should be kept in a dark and dry place, out of the reach of small children. Temperature indicators - no higher than 25°C.

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Shelf life

Phenazepam can be used for 3 years from the date of manufacture of the drug.

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Reviews

Phenazepam, according to doctors, is a very effective drug that works well in eliminating sleep-related disorders and alcohol withdrawal, as well as in the treatment of tics and psychotic conditions.

But it should be taken into account that the drug has a rather powerful therapeutic effect, which is why it cannot be taken for a long time - courses should have a minimum duration - no more than 14 days.

Reviews left by patients who have used the drug are quite different: some of them talk about the high effectiveness of the drug, but there are also those who complain about its side effects.

In addition, judging by the comments on medical forums, the drug quickly causes addiction. And therefore, although it allows you to achieve the desired result (for example, eliminating anxiety and speeding up the process of falling asleep), over time it becomes increasingly difficult to do without it.

Also, many patients noted that in the intervals between taking the pills, negative manifestations and emotions worsen, and this problem can only be eliminated by taking a new pill of the medicine.