Which is better: Phenazepam or Tranquesipam

Phenazepam
(active ingredient -
bromodihydrochlorophenylbenzodiazepine
) is a drug from the benzodiazepine group with tranquilizing (anxiolytic), anticonvulsant, hypnotic, muscle relaxant and sedative effects [1]. White or white with a creamy tint crystalline powder, practically insoluble in water, slightly soluble in alcohol, ether, chloroform, soluble in toluene, benzene, dioxane, dimethylformamide [2].

Content

• 1 History of the creation of the drug
• 2 Receipt
• 3 General information
• 4 Pharmacokinetics
• 5 Indications
• 6 Mechanism of action
• 7 Contraindications
• 8 Side effects 8.1 Correction of side effects

Comparison of ease of use of Phenazepam and Seduxen

This includes dose selection taking into account various conditions and frequency of doses. At the same time, it is important not to forget about the release form of the drug; it is also important to take it into account when making an assessment.

The ease of use of Phenazepam is approximately the same as Seduxen. However, they are not convenient enough to use.

The drug ratings were compiled by experienced pharmacists who studied international research. The report is generated automatically.

Last update date: 2020-12-13 10:31:30

History of the drug's creation

Phenazepam is the first benzodiazepine tranquilizer created in the USSR.

In the early 1970s, a group of scientists led by V.V. Zakusov received a state order to create a domestic tranquilizer. The molecule was synthesized at the Odessa Physicochemical Institute of the Ukrainian SSR Academy of Sciences (S. A. Andronati and A. V. Bogatsky) [3]. The names of many other prominent scientists are associated with the development of phenazepam - S. B. Seredenin and T. A. Voronina (pharmacological screening, selection and study), G. Ya. Avrutsky and Yu. A. Aleksandrovsky (clinical efficacy and safety).

For its receipt (1974), implementation (1978) and creation of the scientific basis of a new branch of military medicine (military psychopharmacology) to a group of Soviet scientists - G. Ya. Avrutsky, Yu. A. Aleksandrovsky, S. A. Andronati, A. V. Bogatsky , Yu. I. Vikhlyaev, T. A. Voronina, V. V. Zakusov, A. L. Zyuban, B. V. Ovchinnikov, S. B. Seredenin, L. I. Spivak, G. V. Chuchkin - awarded USSR State Prize (1980).[4][5]

Development of dependence on Phenazepam

When using Phenazepam as a drug, addiction develops rapidly - in just 10-14 days of daily use.

There are three types of addiction that the drug causes:

1. Chemical addiction. The human body quickly gets used to the dose of Phenazepam, and to increase the effect it is necessary to constantly increase the dose of the drug taken.
2. Physiological dependence. When the chemical components of the drug are removed from the body, a person experiences attacks of pain and nausea. Insomnia, convulsions, and constant tremors of the limbs appear.
3. Psychological withdrawal. Drug addicts who use Phenazepam perceive the drug as the only way to improve their mood, get away from problems and unpleasant sensations that the body experiences.

Prolonged and uncontrolled use of a tranquilizer causes severe addiction, and a constant increase in pill intake can lead to coma or death.

Receipt

Synthesis scheme according to the method of S. A. Andronati, A. V. Bogatsky and Yu. I. Vikhlyaev, developed at the Physico-Chemical Institute of the Academy of Sciences of the Ukrainian SSR [3]:

First, 2-(o-chlorobenzoylamino)-5-bromo-2-chlorobenzophenone is obtained by acylation of p-bromoaniline with o-chlorobenzoic acid chloride in the presence of a catalyst - zinc chloride. 2-(o-chlorobenzoylamino)-5-bromo-2-chlorobenzophenone is hydrolyzed with aqueous sulfuric acid to give 2-amino-5-bromo-2-chlorobenzophone. 2-amino-5-bromo-2-chlorobenzophone is acylated with aminoacetic acid chloride hydrochloride in chloroform. Then 2-(aminomethylcabronylamino)-5-bromo-2-chlorobenzophenone hydrochloride is formed, which is converted into a base with aqueous ammonia and then thermally cyclized to bromodihydrochlorophenylbenzodiazepine

[2].

Aminoacetic acid chloride hydrochloride is prepared by treating aminoacetic acid with phosphorus(V) chloride in chloroform.

Experimental research at the Moscow Research Institute

With the advent of Phenozepam, the treatment of mental illness has become more effective. Research from the Moscow Research Institute has shown that taking the drug for three or five days can relieve symptoms of anxiety, autonomic disorders and sleep disorders.

The problems associated with relieving the symptoms of neurological abnormalities seemed to have been resolved. However, after ten years, cases of abuse and addiction were identified due to exceeding the dose of the drug and taking it for a long time.

Therefore, since the 90s of the last century, a decision was made at the international and domestic level to limit the use of this medicine. However, in the field of minor psychotherapy, Phenazepam remains indispensable. To control the dosage taken, they began to use the form of injections.

The effect of the drug is aimed at the brain, including its cortex and cerebellum. The drug is well absorbed into the blood, and the maximum concentration in the body is reached after 1-2 hours. Discharged after 10 hours.

Studies have shown that anxiety is eliminated already in the first days of use and is fixed for about a month. In affective disorders, the effect of the drug was most significant, and in cases of vital depression it was less effective.

The product also remains indispensable and superior to analogues for sleep disorders, including sudden awakenings and insomnia.

A benzodiazepine tranquilizer is prescribed for epilepsy in combination with other drugs. The practice of doctors and patient reviews have proven that the number of seizures when taking Phenozepam is reduced by half or they disappear completely.

In the treatment of cardiovascular, pulmonary and digestive organs, the drug in small doses has a muscle relaxant, anxiolytic and anticonvulsant effect.

Phenozepam is widely used in cardiological practice for the treatment of tachycardia, cardialgia associated with panic and fear of death. With the help of the drug in the complex, the condition is maintained in case of ischemia, headache, arrhythmia. It is used in gynecology to eliminate postmenstrual tension.

All studies and experiments conducted prove that the use of the product is widespread in somatic practice. Before prescribing, it is important to study interactions with other medications. Improper use of other medications after stopping Phenazepam leads to unpleasant consequences, including depression, feelings of fear, dizziness, tremors, muscle twitching and others.

general information

Phenazepam is a highly active tranquilizer. The strength of the tranquilizing and anxiolytic (anti-anxiety) action is superior to other benzodiazepine and abenzodiazepine tranquilizers[6]; It also has a pronounced anticonvulsant, muscle relaxant (muscle relaxant) and hypnotic effect. It is superior to diazepam in its anti-anxiety and hypnotic effects [7]. The strength of the hypnotic effect is close to nitrazepam[1]. When used together with hypnotic and opioid drugs, there is a mutual enhancement of the inhibitory effect on the central nervous system.

Phenazepam

Active substance:

Bromdihydrochlorphenylbenzodiazepine

Pharmgroup:

Anxiolytics

Average price in pharmacies

Indications

Phenazepam is prescribed:

• for various neurotic, neurosis-like, psychopathic and psychopath-like conditions, accompanied by anxiety, fear, increased irritability, emotional lability [1].
• for obsession, phobia, hypochondriacal syndromes, including hypochondriacal-senestopathic (including those resistant to the action of other tranquilizers); for phobias and obsessions, they are especially effective in combination with perphenazine (etaperazine) and trifluoperazine (triftazine) [8],
• for psychogenic psychoses, panic reactions, etc., as it relieves anxiety and fear[1],
• for the relief (relief) of alcohol withdrawal[1] and alcoholic delirium (a condition resulting from a sudden cessation of alcohol intake that occurs at stages II-III of alcoholism)[9],
• as an anticonvulsant (mainly for local, small, abortive seizures)[8], also for the treatment of patients with temporal lobe epilepsy and myoclonic epilepsy[10],
• as a sleeping pill,
• for premedication in preparation for surgical operations[11],
• for the prevention of emotional stress and states of fear[10],
• for the treatment of hyperkinesis and nervous tics[10],
• with muscle stiffness[10],
• for autonomic dysfunctions and autonomic lability [10].
• reduces affective tension in delusional disorders.

In combinations:

• for severe psychomotor agitation in manic or psychotic patients (in combination with antipsychotics and lithium salts) [12]: 724.

Comparison of addiction between Phenazepam and Tazepam

Like safety, addiction also involves many factors that must be considered when evaluating a drug.

So, the totality of the values ​​of such parameters as “o syndrome” for Phenazepam is quite similar to the similar values ​​for Tazepam. Withdrawal syndrome is a pathological condition that occurs after the cessation of intake of addictive or dependent substances into the body. And resistance is understood as initial immunity to a drug; in this it differs from addiction, when immunity to a drug develops over a certain period of time. The presence of resistance can only be stated if an attempt has been made to increase the dose of the drug to the maximum possible. At the same time, Phenazepam has a fairly low syndrome value, just like Tazepam.

Mechanism of action

Increases the inhibitory effect of gamma-aminobutyric acid (GABA) on the transmission of nerve impulses[13]. Stimulates BD receptors (in the allosteric center, etc.)[13].

Inhibits polysynaptic spinal reflexes, reduces the excitability of subcortical structures of the brain (thalamus, hypothalamus and limbic system)[13].

The anti-anxiety effect is due to the influence on the amygdala complex of the limbic system [13]. This effect reduces anxiety, fear, restlessness and emotional stress.

The sedative effect is associated with the influence on the nonspecific nuclei of the thalamus and the reticular formation of the brain stem [13]. In particular, this effect also reduces symptoms of neurotic origin, fear and anxiety [13].

The hypnotic effect is associated with inhibition of the cells of the reticular formation of the brain stem. Phenazepam reduces the impact of vegetative, emotional, motor (motor) stimuli that can disrupt the sleep mechanism, and helps to fall asleep faster.

The anticonvulsant effect occurs due to increased presynaptic inhibition. The excited state of the focus (excited nervous structure or group of neurons) does not eliminate, but the spread of the convulsive impulse is suppressed.

The central muscle relaxant effect occurs due to inhibition of both monosynaptic (to a small extent) and polysynaptic spinal afferent inhibitory pathways. Direct inhibition of muscle and motor nerve function is also likely to occur.

Reviews of people who took Phenazepam

It is clear that I was interested in the opinion of non-professionals about the effectiveness of the drug. I was afraid of side effects, so I very carefully “digested” the reviews from the network. I even registered on a specialized forum. Here's what people wrote.

“With the help of Phenazepam I struggled with obsessive thoughts. The crisis destroyed my business, and I could not get back to normal again. When anxieties and fears began to arise, I decided that it was time to do something. The doctor prescribed the drug and now I feel improvements. I hope I can enjoy life again..."

There were a lot of reviews on the Internet from people struggling with various addictions. Tablets are often prescribed to suppress withdrawal symptoms after quitting alcohol and drugs. It turned out that Phenazepam acts on certain receptors, relieving pain.

“I quit drinking and almost killed my family. Irritability and aggression simply went off scale. The narcologist prescribed Phenazepam and simply saved my family. I haven’t drunk for a year now..."

There were also negative reviews. Some people noted that the drug was weak and they had to select analogues. The price of the tablets allows you to safely experiment. It's never too late to change your appointment.

Contraindications

Hypersensitivity (including to other benzodiazepines), coma, shock, myasthenia gravis, angle-closure glaucoma (acute attack or predisposition), acute alcohol poisoning (with weakening of vital functions), narcotic analgesics and hypnotics, severe chronic obstructive pulmonary disease (possibly increased respiratory failure), acute respiratory failure, severe depression (suicidal tendencies may occur) [ source not specified 331 days

]; pregnancy (especially the first trimester), lactation period, age under 18 years (safety and effectiveness have not been determined).

With caution. Hepatic and/or renal failure, cerebral and spinal ataxia, history of drug dependence, tendency to substance abuse, hyperkinesis, organic brain diseases, psychosis (paradoxical reactions are possible), hypoproteinemia, sleep apnea (established or suspected), old age.

Case study and instructions

From a clinical medical point of view, Phenazepam is a safe, fast-acting and sedative.
With its help, many tasks are solved, for example, liquefaction of painful sensations in the postoperative period. But it is not recommended to use the medicine for long-term treatment; the maximum duration of therapy should be no more than one month.

Phenazepam is a development of Soviet scientists; the first practical experience of its use was in the seventies of the last century in military medicine.

At that time, this drug was a powerful tranquilizer, sleeping pill, and anticonvulsant. Prescribed to patients with epilepsy, anxiety and rehabilitation after prolonged alcohol consumption.

If the medicine enters the body in its pure form, then the mood can change dramatically in both positive and negative directions. In other words, a surge of strength may be caused or anger may arise.

An overdose affects the normal functioning of internal organs - causing tachycardia, low blood pressure, constipation, diarrhea, vomiting, dry mouth, heartburn.

The hematopoietic system can also malfunction: blood clots form, leukopenia, anemia and other diseases occur. The function of the genitourinary tract is impaired: acute renal failure, urinary incontinence or retention, decreased libido.

Abuse is a deliberate excess of the dosage in order to change the mental state, which can lead to the development of hepatitis, seizures, fever, shortness of breath and result in death.

Duration and continuity of use leads to addiction, and in cases of abrupt withdrawal from Phenazepam, nervous system disorders, sleep disturbances, hallucinations appear, and sometimes thoughts of suicide occur.

In the UK and EU countries, this drug is used quite rarely for the purpose of treating drug addicts, so that withdrawal symptoms stop for a while or simply to normalize sleep.

This drug has a greater effect on a drug addict than on a person who is simply being treated with this medication. When interacting with alcohol, incredible energy and a desire to communicate with people for a long time appear, then this turns into aggression.

To stop taking the drug, it is best to consult a doctor, take the necessary tests and possibly spend some time in the clinic.

Side effects

From 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, unsteady gait, slowed mental and motor reactions, confusion; rarely - headache, euphoria, depression, tremor, memory loss, impaired coordination of movements (especially at high doses), depressed mood, dystonic extrapyramidal reactions (uncontrolled movements, including the eyes), asthenia, myasthenia, dysarthria, epileptic seizures (in patients with epilepsy); extremely rarely - paradoxical reactions (aggressive outbursts, psychomotor agitation, fear, suicidal tendencies, muscle spasms, hallucinations, agitation, irritability, anxiety, insomnia).

From the hematopoietic organs: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, excessive fatigue or weakness), anemia, thrombocytopenia.

From the digestive system: dry mouth or drooling, heartburn, nausea, vomiting, loss of appetite, constipation or diarrhea; liver dysfunction, increased activity of “liver” transaminases and jaundice. From the genitourinary system: urinary incontinence, urinary retention, renal dysfunction, decreased or increased libido, dysmenorrhea.

Allergic reactions: skin rash, itching.

Effect on the fetus: teratogenicity (especially the first trimester), central nervous system depression, respiratory impairment and suppression of the sucking reflex in newborns whose mothers used the drug. Local reactions: phlebitis or venous thrombosis (redness, swelling or pain at the injection site).

Other: addiction, drug dependence; decrease in blood pressure; rarely - visual impairment (diplopia), weight loss, tachycardia.

With a sharp reduction in dose or cessation of use - withdrawal syndrome (irritability, nervousness, sleep disturbances, dysphoria, spasm of smooth muscles of internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremor, perception disorders, including hyperacusis, paresthesia, photophobia; tachycardia, convulsions, rarely - acute psychosis).

Correction of side effects

Mesocarb (Sidnocarb), as well as the specific benzodiazepine receptor antagonist flumazenil, are effective as a corrector that reduces or removes the side effects of phenazepam [1].

About Sibazon

The drug is a benzodiazepine drug, which, due to its sedative effect, is used to treat neuroses. The active substance of the drug is Diazepam, which is an analogue of Phenazepam .

Indications for use

• neuroses, neurotic disorders
• psychoses
• hypertension
• insomnia, sleep disorder
• myositis
• schizophrenia
• PMS, menopause
• myocardial infarction
• premedication
• alcohol withdrawal

In fact, the medicine is used to treat many diseases, but the complete list is so long that only basic information about the indications for the drug is provided here.

If we compare Phenazepam and Sibazon, then the second drug can be taken by children, unlike the first.

Application, dosage

Phenazepam is prescribed orally in tablet form. On an outpatient basis, adults are prescribed 0.00025-0.0005 g (0.25-0.5 mg) 2-3 times a day[1]. In a hospital setting, the daily dose can be increased to 0.003-0.005 g (3-5 mg) [1]; in the treatment of epilepsy, the daily dose ranges from 0.002 to 0.01 g (2-10 mg)[1].

To relieve alcohol withdrawal, 0.0025-0.005 g (2.5-5 mg) per day is prescribed[1]. For sleep disorders, take 0.00025-0.001 g (0.25-1 mg) 20-30 minutes before bedtime[1]. Sometimes the dose is increased to 0.0025 g (2.5 mg)[1]. The maximum daily dose should not exceed 0.01 g[1].

In the treatment of depersonalization, phenazepam is prescribed in large (4-8 mg) and very large (up to 20 mg) daily doses, which is explained by the fact that patients with depersonalization are resistant not only to the therapeutic effect of benzodiazepines, but also to their side effects [14]

For the treatment of mild anxiety during long-term therapy - 0.5-3 mg per day, for severe anxiety (maximum doses) - 3-10 mg[12]:726.

Phenazepam substitutes by composition

Combining a tranquilizer and alcohol is strictly unacceptable! Consequences:

1. Multiple increases in the effect of the drug, which can lead to an overdose
2. Powerful intoxication of the body
3. Multiple increase in adverse reactions
4. Coma
5. Death

Any medications should not be combined with alcohol. The most dangerous duo is alcohol and tranquilizers. There are many known cases of death.

Phenazepam is a time-tested drug. It has practically no analogues in terms of its effect on the human nervous system, therefore it effectively fights psycho-emotional disorders.

It is dangerous due to the development of addiction; with prolonged use and a spontaneous increase in the dose, it begins to act like a narcotic drug, causing powerful dependence.

Structural analogues of Phenazepam are medications with one main component, but may have different dosages of this component. Structural substitutes for Phenazepam have identical indications to the original, negative reactions of the body to taking the medication, and contraindications.

Tranquesipam

The active ingredient in Tranquesipam is bromodihydrochlorophenylbenzodiazepine. Tranquesipam belongs to the pharmacological group of anxiolytics. The drug is produced in tablets and is prescribed for:

• neuroses and neurosis-like pathologies;
• psycho-like states and psychoses, which are accompanied by anxiety, panic and fears;
• emotional stress and phobias;
• vegetative lability;
• convulsive attacks;
• epilepsy of various etiologies;
• muscle fiber rigidity;
• hyperkinesis and athetosis.

Also used as part of combination therapy for withdrawal symptoms and schizophrenia.

The medication is not prescribed for:

• allergies to medicinal composition;
• intoxication with alcohol, drugs and medications;
• myasthenia gravis;
• liver cirrhosis and hepatitis;
• kidney failure;
• lactation and pregnancy.

The initial dosage for the treatment of psychoneurotic conditions is 0.5-1 mg 2-3 times a day, followed by increasing the dosage to 4-6 mg.

Side effects:

• dizziness, drowsiness;
• headache and muscle pain;
• decreased memory, attention and concentration;
• ataxia;
• dyspepsia;
• bronchospasms and skin allergies;
• decreased libido and impotence.

Elzepam

Elzepam is a tranquilizing drug of the benzodiazepine group with the active ingredient bromodihydrochlorophenylbenzodiazepine.

The drug has a sedative and hypnotic effect and an anxiolytic effect on the body. Elzepam also has anticonvulsant and muscle relaxant properties. Elzepam is produced in tablets and also in parenteral solution.

The drug is prescribed for:

• neurotic and psychopathic disorders;
• emotional overstrain;
• senesto-hypochondriasis syndrome;
• insomnia;
• suicidal thoughts;
• alcohol syndrome;
• epileptic seizures;
• hyperkinesis and athetosis;
• muscle rigidity.

Elzepam is not prescribed for:

• sensitivity to the drug composition;
• cardiogenic shock and coma;
• myasthenia gravis;
• angle-closure glaucoma;
• intoxication of the body with drugs and alcohol;
• depression.

It is also prohibited to use Elzepam in pediatrics, women in the 1st trimester of pregnancy and during lactation.

Prescribe with extreme caution when:

• severe pathologies of the liver and kidneys;
• cerebral pathologies of the brain;
• hyperkinesis;
• apnea.

The solution is administered intramuscularly or intravenously. The average dosage per day of the drug is 3-5 mg, for severe pathologies - 7-9 mg.

Treatment of epileptic seizures - taking tablets 2-3 times a day. The average daily dose is 2-10 mg. Relief of alcohol syndrome is carried out with a parenteral solution with a dose of 2.5 mg per day.

Side symptoms:

• blurred vision and dizziness;
• lethargy and decreased concentration;
• sexual dysfunction;
• dyspepsia and jaundice;
• skin itching, rash and redness of the epidermis.

Legal status

By country

In Russia, phenazepam is permitted and is not included in the list of restricted psychotropic substances (unlike some other benzodiazepines that are in List III: diazepam, clonazepam, lorazepam, etc.).

In Ukraine, in accordance with Resolution of the Cabinet of Ministers of Ukraine dated May 6, 2000 No. 770, phenazepam belongs to List II of the list of narcotic drugs, psychotropic substances and precursors, the circulation of which is limited on the territory of Ukraine and in respect of which exceptions to certain control measures are allowed[16].

In the United States, phenazepam is not approved by the Food and Drug Administration, so it is prohibited from sale as a drug, but it is also not included in the list of controlled substances[17].

In Germany, phenazepam is in Schedule III (German: Anlage III), and the sale and possession of this drug without a prescription is considered illegal[18]. The drug can be prescribed by doctors, but a special prescription form is required.

UN and WHO decisions

On March 18, 2021, it was included in the list of substances subject to special control by the UN Commission on Narcotic Drugs[19]. The WHO Committee recommended the addition of phenazepam to Schedule IV of the 1971 Convention on Psychotropic Substances[20].

Import into customs territory

Phenazepam is listed in the annex to the Decision of the Board of the Eurasian Economic Commission “On non-tariff regulation measures” in the list of the section “Narcotic drugs, psychotropic substances and their precursors” in the list of goods for which a permitting procedure has been established for import into the customs territory of the Eurasian Economic Union and/or export from the customs territory of the Eurasian Economic Union[21]. This means that the drug is necessarily subject to customs declaration; failure to declare phenazepam at customs is an administrative offense under Article 16.2 Part 1 of the Code of Administrative Offenses of the Russian Federation.

Expert opinion on the effectiveness of Phenazepam

I went to the clinic because problems with the nervous system began to “rotten” my life. I quarreled with friends, for no apparent reason, and ruined family relationships. In general, my irritability overflowed. I decided that it was time to rebuild my life and made an appointment with a psychotherapist. The doctor listened to my complaints and prescribed Phenazepam.

“We should have come earlier, without prolonging the problem so much.
Most likely, the cause of your insomnia was some kind of nervous breakdown. Everything can be improved by teaching the body to relax. I'll prescribe you a tranquilizer. My patients leave a lot of positive feedback on it. Take the course, and then we’ll see what to do next...” Nikolai Antonovich, psychotherapist, Moscow

In a further conversation, the doctor talked about the dangers of taking such a drug, but clarified that provided that the recommendations specified in the instructions are followed, the risk of side effects and severe addiction is minimal. But the effect of Phenazepam should be quite strong.