Phenazepam

Phenazepam - a remedy from the category of anxiolytic drugs.

[1], [2], [3], [4], [5], [6]

Indications of the phenazepam

Applicable in the following cases:

• at psychopathy, disturbances of psychopathic character, and also other conditions at which there is a feeling of strong anxiety, fear, irritability, mood instability and increased tension;
• with neuroses and various neurosis-like conditions;
• at problems with a dream;
• with a reactive form of psychosis;
• hypochondriacal disorder, against which there are various kinds of painful or uncomfortable sensations (senestopatic syndrome, also when therapy with other tranquilizers was ineffective);
• SVD;
• in the prevention of phobias, as well as conditions against which there is a sense of tension;
• Epileptic seizures with a myoclonic or temporal form;
• panic symptoms;
• nerve tics, as well as dyskinesia;
• a sharp increase in muscle tone, as well as their resistant resistance to deforming effects (muscle rigidity);
• instability of vegetative NS;
• alcoholic abstinence.

Phenazepam is also allowed to be used as a preliminary drug preparation of the patient for general anesthesia and subsequent surgical operation.

[7],

Release form

The release is made in the form of a solution for intravenous or intravenous injections, as well as in tablets.

The pack contains 20 tablets of medicine.

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

[8], [9], [10], [11]

Pharmacodynamics

The effect of phenazepam is determined by the ability of diazepines to influence the work of different departments of the central nervous system.

The anxiolytic effect of drugs is provided by the action of the element bromodihydrochlorophenylbenzodiazepine in relation to the amygdala complex of the limbic system. This effect manifests itself through the relaxation of emotional tension, and in addition to this feeling of anxiety, fear and anxiety.

The severity of anxiolytic effects of phenazepam exceeds in its strength the majority of psychotropic drugs from the diazepine category.

The sedative effect ensures the action of the active element of the drug on the nerve structures located inside the central parts of the cerebral spinal cord, as well as on the thalamic nuclei of the nonspecific type 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 psychomotor excitability. It also partially relaxes daily activity and mindfulness, and at the same time reduces the speed of motor and mental responses, and so on.

Regulating the activity of the central nervous system, the drug reduces the intensity of the influence on it of a variety of psychoemotional, motor, and vegetative stimuli that affect the process of falling asleep.

The soporific effect is manifested in the fact that during the period of using the medicine the sleep on the patient is greatly facilitated, the sleep itself becomes deeper, and its duration is prolonged.

Along with this, the overwhelming effect on the CNS allows Phenazepam to intensify the action of anesthetics, hypnotics, and analgesic drugs (in this connection, tablets of the drug are not allowed in combination with these drugs).

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

[12], [13], [14], [15], [16],

Pharmacokinetics

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

Phenazepam is the process of hepatic exchange. The half-life of the active substance in different people can fluctuate within 6-18 hours. Excretion of metabolic products mainly occurs with the help of kidneys.

[17], [18], [19], [20], [21]

Dosing and administration

Use of medication in tablets.

Tablets should be consumed inside. For a day, on the average, it is allowed to take in the range of 0.0015-0.005 g of drug substance. Share this portion should be approximately 2-3 uses.

In the morning and in the daytime it is required to use 0.0005 or 0.001 g of phenazepam, and in the evening it is allowed to increase the portion size to 0.0025 g. No more than 0.01 g of preparation is allowed per day.

The use of tablets in various diseases:

• conditions in which there are problems with sleep: you should use medicines about 30 minutes before bedtime, in a portion of 0.00025 or 0.0005 g;
• psychopathy and disturbances of a psychopathic nature, as well as neuroses and pseudo-neurotic states: start therapy with a daily dose of 0.0015-0.003 g. It should be divided into 2-3 uses. After a few days (usually after 2-4 days - taking into account the effectiveness of treatment and the patient's tolerance of the drug), it is possible to increase the dosage to 0.004-0.006 g / day;
• a feeling of intense anxiety or fear, motor anxiety, as well as vegetative forms of paroxysms: therapy should start with a daily dose of 3 mg. Then it is quickly started to raise, in order to obtain the required medicinal effect;
• epileptic seizures: the daily dose varies between 0.002-0.01 g;
• alcoholic withdrawal: the dosage amount per day is 0.0025-0.005 g;
• disease, against which the muscle tone increases: for a day, you need to use 0.002-0.006 g of the drug.

To exclude the risk of addiction, as well as the development of drug dependence, the drug should be administered in separate courses that last for a maximum of 14 days. Sometimes it is allowed to extend the course - up to 2 months. Stop taking drugs is necessary by gradually reducing the size of the taken portion.

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

The solution is usually administered in / m, either intravenously (by drip or jet). The size of a single serving is 0.0005-0.001 g (this volume has a half or a whole ampoule of the solution). For the day on average, patients are administered in the range of 0.0015-0.005 g. It is allowed to inject no more than 0.01 g of the drug per day.

The method of administration and dosage regimen in the treatment of various diseases:

• elimination of panic attacks, a feeling of intense anxiety, fears, psychotic conditions, besides psychomotor agitation: at the initial stage of therapy, a dosage of 0.003-0.005 g is required on average in a 0.1% solution, it is 3-5 ml. In extremely severe conditions, it is allowed to increase the size of the portion to 0.007-0.009 g;
• treatment of epileptic seizures: administer the drug intravenously or in the / m way. The size of the initial portion is 0.0005 g;
• alcohol abstinence: should be injected in / in or in / m method. Portion per day is in the range of 0.0025-0.005 g;
• pathology of neurological nature, against which the hypertension of muscles develops: the drug should be administered intramuscularly, at a dosage of 0.0005 g. The procedure should be performed 1-2 times / day;
• in the process of preparing for anesthesia, as well as performing a surgical operation: the drug should be administered intravenously, at the minimum speed. The dose is 0.003-0.004 g.

Upon reaching the required drug exposure from the use of the solution, it is required to transfer the patient as soon as possible to the oral administration of Phenazepam in tablets, and continue the course of treatment in this form.

Therapeutic course with the use of drugs in pricks can last no more than 14 days. Only once and with the appointment of a doctor it is allowed to extend to 3-4 weeks. During the drug cancellation process, you need to reduce the dosage gradually.

[29], [30], [31], [32]

Use of the phenazepam during pregnancy

Nursing and pregnant women are allowed to use Phenazepam only if they have life indications.

Drug use in the 1st trimester increases the likelihood of a baby developing congenital anomalies.

Use of the drug in the 3rd trimester (especially in the last weeks of the term) causes the cumulation of the active ingredient inside the fetal tissues, as a result of which the CNS activity in the newborn is suppressed.

When taking medication shortly before childbirth, the newborn baby develops such symptoms as a sucking reflex disorder, weakness in muscles, suppression of respiratory processes and hypothermia in pronounced form.

Prolonged intake of the drug during pregnancy can cause the baby to develop physical dependence on drugs, and in addition to the development of signs of withdrawal syndrome.

It is allowed to use the medicine very carefully during labor activity. For example, if labor has begun prematurely, or the woman has had a premature detachment of the placenta.

Parenteral administration of the solution in small doses usually does not adversely affect the infant. But with the use of large doses, it may cause hypothermia or suffocation, as well as a heart rhythm disorder and a decrease in blood pressure.

It is forbidden to use Phenazepam in lactation, because the active ingredient of the drug is excreted in the mother's milk. Metabolism of this component in infants occurs much slower than in an adult, so the products of its metabolism begin to accumulate inside the body, causing the development of sedative effects. Such an effect can lead to difficulties in the process of feeding and loss of weight by the baby.

Contraindications

Due to the fact that Phenazepam is included in the group of medicines with a powerful therapeutic effect, he has several contraindications, among which:

• a state of coma or shock;
• presence of myasthenia gravis symptoms;
• glaucoma of a closed-angle character (both in acute form and in those people who are predisposed to the development of this pathology);
• when diagnosed in humans COPD (because the drug can lead to the potentiation of respiratory insufficiency);
• acute form of respiratory insufficiency;
• persons under the age of 18;
• people who have intolerance with regard to drugs from the category of benzodiazepines, and in addition hypersensitivity to any of the additional elements of the drug.

People with disorders of renal or hepatic activity are heavily allowed to use the drug solely under the supervision of an experienced doctor.

Caution is required when appointing people who have previously had a drug dependence syndrome, people who are psychologically dependent on certain types of drugs, and also elderly patients.

[22], [23], [24], [25], [26]

Side effects of the phenazepam

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

More rarely there are some manifestations from the NA: such as a feeling of euphoria, tremors, depression, memory loss, headaches, problems with coordination of movements (especially if the drug is used in large portions) and extrapyramidal disorders of a dystonic nature. There are also possible violations such as mood reduction, myasthenia gravis, signs of asthenic syndrome, and at the same time dysarthria.

The use of the drug alone causes paradoxical symptoms - the development of phobias, uncontrolled outbreaks of aggression, the emergence of a feeling of intense anxiety, hallucinations, muscle spasticity, and besides suicidal tendencies and sleep disorders.

Hemopoietic organs: a decrease in the level of the main components of this system (leukocytes, as well as postcellular structures, including platelets with erythrocytes), and in addition granulocytes of neutrophilic haarction and hemoglobin.

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

Defeat of reproductive organs: increase or vice versa decrease in libido. In addition, women may have signs of dysmenorrhea. Individuals have allergy symptoms, including the occurrence of itching and rash on the skin surface.

Among other side effects, which sometimes arise due to the use of medication:

• development of addiction to the drug;
• the appearance of drug dependence;
• decrease in blood pressure;
• visual disorders (among them double vision);
• weight reduction;
• problems with the rhythm of the heartbeat.

With a sharp abolition of the use of the drug or a reduction in its dosage in patients, development of withdrawal syndrome is noted. It usually manifests itself in the form of the same signs that caused the patient to start using drugs.

[27], [28]

Overdose

With intoxication with phenazepam may develop violations that pose a serious danger to the health and life of the patient. Because of this, it is extremely important to keep track of the dosage used.

With a slight excess of dosage, the patient has side effects, mainly affecting the function of the central nervous system. Together with this, potentiation of the therapeutic effect of drugs is possible.

If the dosage is significantly exceeded, there is a danger not only for HC, but also for the heart with a respiratory system. It is caused by the fact that the medicine has the ability to suppress cardiac function and the activity of the respiratory center.

Overdose can cause a fatal outcome, which usually comes as a result of stopping breathing or the heart. In this regard, after the appearance of the first signs of a violation, you should immediately turn to medical specialists. Trying to eliminate the violation on its own is strictly prohibited - this can only aggravate the problem.

To reduce the severity of the toxic effect of the drug, drugs that can block the conductors of benzodiazepine (among them Anexat, which is a special antidote for the drug Phenazepam) are usually prescribed.

Enter such a blocker should be intravenously, previously diluted in a solution of sodium chloride or glucose, at a dosage of 0.2 mg. It is extremely rare to allow an increase in the size of a portion up to 1 mg.

In addition, in case of poisoning with the drug, it is necessary to perform symptomatic treatment procedures to support the lungs and the heart. If you abandon these procedures, the patient can develop a coma.

If you have negative symptoms from other systems and organs, you should use medications that reduce the severity of these disorders.

The fatal outcome as a result of intoxication with phenazepam is quite frequent in people with alcoholism who take the medicine along with alcohol. This is due to the fact that the drug potentiates the likelihood of side effects when used together with alcohol.

[33], [34], [35],

Interactions with other drugs

Combined use of the drug with funds that suppress the activity of the central nervous system (in this list anticonvulsants, hypnotic drugs, and antipsychotics), causes mutual potentiation of their medicinal properties.

A combination with levodopa (used in Parkinson's disease) weakens its therapeutic effect.

Combination with zidovudine (antiviral drug) increases the toxic properties of the latter.

When combined with medications that inhibit the oxidation of microsomes, the likelihood of toxic manifestations of phenazepam increases.

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

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

Admission in combination with antihypertensive drugs leads to a potentiation of the hypotensive properties of these drugs.

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

[36], [37], [38], [39]

Storage conditions

Phenazepam should be kept in a dark and dry place, closed from the access of young children. Temperatures are not higher than 25 ° C.

[40], [41], [42], [43]

Shelf life

Phenazepam is allowed to be used for 3 years from the date of manufacture of the drug.

[44], [45], [46]

Reviews

Phenazepam, according to doctors, is a very effective drug that works great for the elimination of sleep disorders and alcohol withdrawal, as well as for the treatment of tics and psychotic conditions.

But it must be taken into account that the medicine has a rather powerful therapeutic effect, because of which it can not be taken for a long time - courses should have a minimum duration - no more than for 14 days.

The responses left by the patients using the medication are quite different: some of them speak of high drug efficacy, but there are also those who complain of its side effects.

In addition, judging by the comments in the medical forums, the drug quickly becomes addictive. And so, although it allows you to achieve the desired result (for example, by eliminating the feeling of anxiety and speeding up the process of diving into sleep), it becomes increasingly difficult to do without using it in the course of time.

Also, many patients noted that in the intervals between the use of tablets there is an aggravation of negative manifestations and emotions, and this problem can be removed only by taking a new tablet of the drug.