Fenorelaxan - instructions for use, dose, side effects, contraindications

Excipients: povidone (low molecular weight polyvinylpyrrolidone medical) - 9.0 mg; glycerol (glycerol) - 100.0 mg; sodium disulfite (sodium metabisulphite) 2.0 mg; Tween-80 (polysorbate 80) - 50.0 mg; sodium hydroxide 1 M solution - to pH 6.0-7.5; water for injection - up to 1 ml.

Description:

Transparent, colorless or slightly colored liquid.

Pharmacotherapeutic group:Anxiolytic agent (tranquilizer).

ATX: & nbsp

N.05.B.X Other anxiolytics

Pharmacodynamics:

Anxiolytic agent (tranquilizer) of benzodiazepine series. Has anxiolytic, sedative-hypnotic, anticonvulsant and central muscle relaxant effect.

Increases the inhibitory effect of gamma-aminobutyric acid (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 brainstem and intercalary neurons of the lateral horns of the spinal cord; reduces the excitability of subcortical structures of the brain (limbic system, thalamus, hypothalamus), inhibits polysynaptic spinal reflexes.

Anxiolytic action is due to the influence on the amygdala complex of the limbic system, and is manifested in a decrease in emotional tension, easing anxiety, fear, anxiety. The sedative effect is due to the influence on the reticular formation of the brainstem and the nonspecific nuclei of the thalamus and is manifested by a decrease in the symptomatology of neurotic origin (anxiety, fear). On productive symptoms of psychotic genesis (acute delusional, hallucinatory,affective disorders) is practically not affected, there is rarely a decrease in affective tension, delusional disorders.

Sleeping effect is associated with depression of the cells of the reticular formation of the brain stem. Reduces the impact of emotional, vegetative and motor stimuli, which break the mechanism of falling asleep. Anticonvulsant action is realized by strengthening presynaptic inhibition, suppressing the spread of convulsive impulse, but the excited state of the focus is not removed.

Central miorelaksiruyuschee effect due to inhibition of the polysynaptic spinal afferent inhibitory pathways (to a lesser extent, monosynaptic). Perhaps a direct inhibition of the motor nerves and muscle functions.

Pharmacokinetics:

Widely distributed in the body. Metabolised in the liver. Half-life from the body from 6 to 10-18 hours, the excretion of the drug, mainly carried out through the kidneys in the form of metabolites.

Indications:

Neurotic, neurotic, psychopathic and psychopathic and other conditions (irritability, anxiety, nervous tension, emotional lability), reactive psychoses and senesto-hypochondriacal disorders (including those resistant to the action of others.anxiolytic drugs (tranquilizers), autonomic dysfunctions and sleep disorders, prevention of states of fear and emotional stress.

As an anticonvulsant - temporal and myoclonic epilepsy.

In neurological practice - hyperkinesis, tics, rigidity of muscles, vegetative lability.

Contraindications:

Hypersensitivity (including to other benzodiazepines), coma, shock, myasthenia gravis, occlusive glaucoma (acute attack or predisposition), acute alcohol poisoning (with impaired vital functions), narcotic analgesics and hypnotic drugs, severe chronic obstructive disease lungs (possibly increased respiratory failure), acute respiratory failure, severe depression (suicidal tendencies may manifest); pregnancy (especially I trimester), lactation period, age under 18 years (safety and efficacy not determined).

Carefully:

Hepatic and / or renal failure, cerebral and spinal ataxia, drug dependence in history, propensity to abuse of psychoactive drugs,hyperkinesia, organic brain diseases, psychosis (paradoxical reactions are possible), hypoproteinemia, nocturnal apnea (established or presumed), elderly age.

Dosing and Administration:

The drug is administered intramuscularly or intravenously (either jet or drip).

For rapid relief of fear, anxiety, agitation, as well as vegetative and epileptic psychotic states, the initial dose - 0.5-1 mg (0.5-1 ml of a 0.1% solution), the average daily dose - 3.5 mg, in severe cases, - up to 7-9 mg. With epileptic status and serial epileptic seizures, the drug is administered intramuscularly or intravenously at a dose of 0.5 mg.

For the treatment of alcohol withdrawal Fenorelaxan® is prescribed, intramuscularly or intravenously at a dose of 2.5-5 mg per day.

In neurological practice for diseases with increased muscle tone, the drug is administered intramuscularly at 0.5 mg once or twice a day.

For preoperative preparation - intravenously slowly inject 3-4 ml 0.1 % solution of Phenorelaxan®.

The average daily dose of the drug is 1.5-5 mg. The maximum daily dose is 10 mg. After achieving a sustainable therapeutic effect, it is advisable to switch to oral dosage forms of the drug.

To avoid the development of drug dependence, with course treatment, the duration of Phenorelaxan®, like other benzodiazepines, is 2 weeks. But in some cases, the duration of treatment can be increased to 3-4 weeks.

With the withdrawal of the drug, the dose is reduced gradually.

Side effects:

From the nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, fatigue, dizziness, impaired concentration, ataxia, disorientation, slowing of mental and motor reactions, confusion; rarely - headache, euphoria, depression, tremor, memory loss, movement coordination disorders (especially at high doses), mood reduction, dystonic extrapyramidal reactions (uncontrolled movements, including the eye), asthenia, myasthenia gravis, dysarthria; extremely rarely - paradoxical reactions (aggressive outbreaks, psychomotor agitation, fear, suicidal tendencies, muscle spasm, hallucinations, anxiety, sleep disturbance).

From the hematopoiesis: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, pain in.throat, unusual fatigue or weakness), anemia, thrombocytopenia.

On the part of the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, decreased appetite, constipation or diarrhea; violations of liver function, increased activity of "liver" transaminases and alkaline phosphatase, jaundice.

On the part of the genitourinary system: urinary incontinence, urinary retention, impaired renal function, decreased or increased libido, dysmenorrhea.

Allergic reactions: skin rash, itching.

Influence on the fetus: teratogenicity (especially I trimester), central nervous system (CNS) depression, respiratory failure and suppression of sucking reflex in newborns whose mothers used the drug.

Other: addiction, drug dependence; lowering of blood pressure (BP); rarely - visual impairment (diplopia), weight loss, tachycardia. With a sharp decrease in dose or discontinuation of reception - the syndrome of "withdrawal" (sleep disturbance, dysphoric reactions, spasm of smooth muscles of the internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremor, perception disorders, incl.hyperaemia, paresthesia, photophobia; tachycardia, convulsions, rarely-psychotic reactions).

Local reactions: phlebitis or venous thrombosis (redness, swelling or pain at the injection site).

Overdose:

With a moderate overdose - increased therapeutic effect and side effects; with a significant overdose - marked depression of consciousness, cardiac and respiratory activity.

Treatment: monitoring of vital functions of the body, maintaining respiratory and cardiovascular activity, symptomatic therapy. As antagonists of the muscle relaxant action of Phenorelaxan®, strychnine nitrate is recommended (injections of 1 ml of 0.1% solution 2-3 times a day). As a specific antagonist, flumazenil (anexat) - intravenously (on a 5% solution of glucose (dextrose) or 0.9% sodium chloride solution) at an initial dose of 0.2 mg (if necessary, up to a dose of 1 mg).

Interaction:

Phenorelaxan® is compatible with other drugs that cause depression of the CNS function (hypnotics, anticonvulsants, neuroleptics, etc.), however, in case of complex application it is necessary to take into account the mutual enhancement of their function.

Reduces the effectiveness of levodopa in patients with Parkinsonism.

May increase the toxicity of zidovudine.

Inhibitors of microsomal oxidation increase the risk of toxic effects. Inducers of microsomal liver enzymes reduce efficacy. Increases the concentration of imipramine in the serum.

Hypotensive drugs can increase the severity of blood pressure lowering.

Against the background of simultaneous administration of clozapine, an increase in respiratory depression is possible.

Special instructions:

Special care must be taken when administering Fenorelaxan® in severe depression. the drug can be used to implement suicidal intentions. It is necessary to use the drug with caution in elderly and weakened patients.

With renal / hepatic insufficiency and long-term treatment, control over the picture of peripheral blood and "hepatic" enzymes is necessary.

The frequency and nature of side effects depend on the individual sensitivity, dose and duration of treatment. With reduced doses or discontinuation of Phenorelaxan, side effects disappear.

Like other benzodiazepines, it has the ability to induce drug dependence in long-term admission in large doses (more than 4 mg / day).

With a sudden discontinuation of the reception can be noted the syndrome of "withdrawal" (depression, irritability, insomnia, increased sweating, etc.), especially with prolonged admission (more than 8-12 weeks).

During pregnancy apply only for "vital" indications. Has a toxic effect on the fetus and increases the risk of congenital malformations when used in the trimester of pregnancy. Taking therapeutic doses at a later time of pregnancy can cause depression of the newborn's central nervous system. Continuous use during pregnancy can lead to physical dependence with the development of the "cancellation" syndrome in a newborn.

Children, especially at a young age, are very sensitive to the CNS depressing action of benzodiazepines.

The use directly before childbirth or during labor can cause a respiratory depression in the newborn, a reduction in muscle tone, hypotension, hypothermia, and a weak act of sucking ("sluggish child" syndrome).

The drug enhances the effect of alcohol, so the use of alcoholic beverages during the treatment with Phenorelaxan® is not recommended.

Effect on the ability to drive transp. cf. and fur:Phenorelaxan® is contraindicated during work by drivers of transport and other persons performing work requiring quick reactions and precise movements.

Form release / dosage:Solution for intravenous and intramuscular injection 1 mg / ml.

Packaging:

1 ml per ampoule of neutral glass.

5 ampoules per contour cell packaging made of polyvinyl chloride film. Two contour mesh packs together with instruction for use and scapegrator ampullum in a pack of cardboard. 10 ampoules are placed in a box of cardboard. In each box, the instructions for use and the ampoule scaler are put. When using ampoules with a dot or a ring of fracture, the scarifier is not inserted.

Storage conditions:In a dark place at a temperature of 15 to 25 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N003863 / 01

Date of registration:25.11.2009

The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia

Manufacturer: & nbsp

MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia

Information update date: & nbsp09.12.2015

Illustrated instructions

Instructions

Phenorelaxan® (Phenorelaxan)