Fenorelaxane

Phenorelaxan is an anticonvulsant, tranquilizing, and hypnotic drug from the benzodiazepine group.

Indications Fenorelaxane

Phenorelaxan is excellent for dealing with pathological processes such as:

• Withdrawal syndrome (due to abuse of alcoholic beverages and drugs);
• Status epilepticus;
• Epileptic seizures (regardless of the cause);
• Epilepsy (temporal and myoclonic);
• A sleep disorder that manifests itself as insomnia;
• Obsession;
• Reactive psychoses;
• Neurotic and neurosis-like conditions;
• Psychopathic and psycho-like conditions;
• Conditions that are accompanied by increased anxiety, irascibility, nervous tension, emotional instability;
• Seneto - hypochondriacal pathologies (including those that are resistant to other anxiolytics);
• Hyperkinesis and twitching, muscle rigidity, autonomic instability (in neurology);
• Schizophrenia (including febrile form) with increased susceptibility to antipsychotic drugs;
• For premedication (in anesthesiology, as a component of induction anesthesia);
• To reduce the feeling of fear and emotional tension (in emergency situations).

Release form

On the pharmaceutical market, the drug is presented in the form of a solution for different types of administration (intravenous and intramuscular), as well as tablets.

Pharmacodynamics

Phenorelaxan is an anxiolytic. It is a derivative of benzodiazepam. Therefore, it has such effects on the body as: calming, stopping cramps and relieving muscle tension.

The suppressive effect that Phenorelaxan has on the central nervous system is realized primarily in the thalamus and hypothalamus, and in the limbic system.

When using this medication, there is an increase in the inhibitory effect on gamma-aminobutyric acid (GABA), which is one of the main mediators of synaptic slowing (post- and pre-) transmission of nerve impulses in the central nervous system.

The main mechanism of its action is the activation of benzodiazepine nerve endings of the supramolecular GABA-benzodiazepine-chloroionophore-receptor association, due to which GABA receptors are activated and a decrease in the tension of the subcortical structures of the brain and a slowdown in polysynaptic spinal reactions occurs.

Pharmacokinetics

When taken orally, Phenorelaxan is well absorbed from the gastrointestinal tract. Its maximum density is reached within one to two hours. Metabolism occurs in the liver.

The half-life of the drug lasts from six to eighteen hours. The excretion occurs mainly with urine.

Dosing and administration

If Phenorelaxan is prescribed in the form of a solution (for intravenous (jet or drip) or intramuscular administration):

• Reduction of fear, anxiety, tension, vegetative seizures and psychotic states
• The first dose is from 0.5 to 1 ml of solution, on average reaching three to five milliliters per day. In some cases, up to seven to ten milliliters.

Epileptic seizures:

• Treatment begins with 0.5 ml of 0.1% solution, reaching an average of one to three milliliters per day.
• Withdrawal syndrome;

The recommended dose is 0.5 – 1 ml of 0.1% solution.

• Increased muscle tone (in neurology)

It is recommended to administer intramuscularly one or two times a day, half a milliliter of the solution.
Premedication:

• 0.1% solution of Phenorelaxan is administered in an amount of three to four milliliters.

The maximum amount of the drug that can be administered per day is ten milliliters. If the treatment is carried out using intravenous or intramuscular administration, the optimal course will be from three to four weeks. The treatment cannot be stopped at once (due to the possible development of withdrawal syndrome) - only by gradually reducing the dosage.

When a stable result is achieved, you can switch to using Phenorelaxan in the form of pills.

The pills should be taken orally, with a single dose usually being 0.5-1 mg.

If you take the medicine about three times a day, the average dosage will be 1.5 - 5 mg. In the morning and afternoon, 0.5 - 1 mg, and in the evening, a maximum of 2.5 mg. The maximum daily dose is no more than ten milligrams.

Recommended intake for various pathologies:

• Sleep disorders:

You should take 0.25 – 0.5 mg twenty to thirty minutes before bed.

• Pathological conditions (for example, neurotic, psychopathic, neurosis-like and psychopathic-like):

At the beginning of treatment, 0.5 - 1 mg should be taken two or three times a day. Then, after two or four days (if the patient tolerates the medication well and taking into account the effectiveness of the treatment), the dosage can be increased to four to six milligrams per day.

• If the patient has a strong feeling of fear and anxiety

Therapy should begin with three milligrams per day, quickly increasing the dose until the desired effect is achieved.

• Epilepsy

The recommended dose is two to ten milligrams per day.

• Alcohol withdrawal

The recommended intake is two and a half to five milligrams per day.

• Pathologies characterized by increased muscle tone

It is worth consuming two to three milligrams per day, dividing the daily intake into two doses.

Phenorelaxan in tablet form should not be used for more than two weeks to reduce the risk of drug dependence. Under certain circumstances, the duration of drug use can be increased to sixty days.

If the drug needs to be discontinued, the dose should be reduced gradually to minimize the risk of withdrawal syndrome.

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Use Fenorelaxane during pregnancy

Due to the fact that the drug has a teratogenic effect, which contributes to damage to the fetus and can cause mutation (congenital) at the DNA level, it is strictly forbidden to use it during the gestation period. This is especially true for women in the first trimester, due to the most active cell division during the entire pregnancy. After all, the child is very likely to develop severe congenital malformations if his mother takes Phenorelaxan during this period of time.

Later (in the second and third trimesters) the teratogenic effect decreases, but the threat to the child's health remains the same. Therefore, in this period of gestation, this drug can be used, but is not advisable.

If a woman takes Phenorelaxan before giving birth, it can cause breathing problems in the newborn.

If the attending physician cannot prescribe another, safer medication, and the patient has vital indications for taking Phenorelaxan, the use of the medication is possible.

Since there is evidence that Phenorelaxan in small quantities will enter the mother's milk and, accordingly, affect the health of the child (and thereby cause harm), its use during lactation is also prohibited.

Contraindications

The medication should not be used in the following cases:

• Increased individual sensitivity to the active substance Phenorelaxan;
• Coma;
• State of shock;
• Myasthenia;
• Closed-type glaucoma (in the acute period or in the presence of a predisposition);
• Acute poisoning with alcoholic beverages, narcotic drugs or sleeping pills;
• Chronic obstructive pulmonary disease;
• Acute respiratory failure;
• Gestation period;
• Severe depression;
• Breastfeeding period;

Taking into account all the risks, the medication can be used in the following cases:

• Insufficiency of liver or kidney function;
• Ataxia (cerebral or spinal);
• The presence of drug dependence in the patient's medical history;
• Predisposition to abuse of psychoactive drugs;
• Hyperkinesis;
• Basic type of brain pathology;
• If the patient belongs to the elderly population.

Side effects Fenorelaxane

When using Phenorelaxan, there is a possibility of the following side effects:

• Nervous system: fatigue, decreased concentration, disorientation, confusion, impaired memory function, unsteady gait.
• Hematopoietic system: decreased levels of leukocytes, neutrophils, platelets, agranulocytosis, anemia.
• Digestive system: liver dysfunction, jaundice, bowel movement disorder, loss of appetite.
• Urogenital system: anuria, renal dysfunction, libido disorder, dysmenorrhea.
• Allergy: rashes on the skin surface, itching;
• Effects on the fetus during gestation: teratogenicity, depression of the central nervous system and respiratory function.
• Locally: inflammation of the veins or venous blockage of the lumen by a thrombus;
• General: addiction, drug dependence; decreased blood pressure, visual impairment, decreased body weight, increased heart rate.

It is also worth keeping in mind that a rapid reduction in dosage or complete cessation of the use of Phenorelaxan can contribute to the development of withdrawal syndrome.

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Overdose

If the recommended dose of Phenorelaxan is exceeded slightly, there is a possibility of an increase in the therapeutic effect and an undesirable effect.

If the recommended dose is exceeded very much, severe depression of consciousness, heart and lung function occurs.

The therapy requires:

• Monitoring vital signs of the body;
• Supports heart and lung function;
• Symptomatic therapy;
• Introduction of Strychnine Nitrate (1 ml of 0.1% solution 2-3) – in the role of an antagonist of the muscle relaxant Phenorelaxan;
• Introduction of a special antagonist – Flumazenil (Anexate): intravenously 0.2 mg (if necessary, the dosage can be increased to 1 mg) in 5% glucose solution or 0.9% NaCl solution.

Interactions with other drugs

In patients with Parkinson's disease, who simultaneously take Levodopa and Phenorelaxan, the effectiveness of the former is reduced.

With Zidovudine – combined administration with Phenorelaxan leads to increased toxicity of Zidovudine.

If Phenorelaxan is used together with drugs of the following groups: antipsychotics (neuroleptics), antiepileptics, muscle relaxants, narcotic analgesics or with a hypnotic effect, a mutual increase in effects will occur.

Microsomal oxidation inhibitors – increase the likelihood of adverse effects.

Liver catalyst inducers (microsomal) – reduce the effectiveness of Phenorelaxan.

Phenorelaxan, when used simultaneously with Imipramine, increases the density of the latter in the blood plasma.

When used with drugs that lower blood pressure, a more pronounced hypotensive effect occurs.

Respiratory depression may occur when Clozapine is used with Phenorelaxanthin.

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Storage conditions

Phenorelaxan belongs to list B (potent drugs).

It should be stored in a dry place, away from direct sunlight, and out of the reach of children. The temperature should be around 25°C.

Shelf life

If all storage conditions are met, the medicine can be stored for three years.

Reviews

Phenorelaxan is not a new product on the pharmaceutical market. During its existence, it has proven itself as an excellent, effective remedy. The area for its use is very large, from withdrawal syndrome to schizophrenia. But at the same time, both doctors and patients note the occurrence of many undesirable effects, and most importantly, the development of addiction, which makes its long-term use problematic.