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

auxiliary substances: lactose monohydrate - 81.5 mg or 122.0 mg or 161.5 mg, potato starch - 15.0 mg or 22.5 mg or 30.0 mg, croscarmellose sodium (impellose) 2.0 mg or 3.0 mg or 4.0 mg, calcium stearate 1.0 mg or 1.5 mg or 2.0 mg.

Description:Tablets are white, flat-cylindrical with a bevel (for dosages of 0.5 mg and 2.5 mg), with a facet and a risk (for a dosage of 1 mg).

ATX: & nbsp

N.05.B.X Other anxiolytics

Pharmacodynamics:

Strengthens the inhibitory effect of gamma-aminomalic acid (GABA) on the transmission of nerve impulses.Stimulates benzodiazepine receptors located in the allosteric center of postsynaptic GABA receptors. ascending activating reticular formation of the brain stem and intercalary neurons of the lateral troughs 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, alleviation of anxiety, fear, anxiety.

The sedative effect is due to the effect on the reticular formation of the brainstem and the nonspecific nuclei of the thalamus and is manifested by a decrease in symptoms. neurotic origin (anxiety, fear).

The productive symptomatology of psychotic genesis (acute delusional, hallucinatory, affective disorders) practically does not affect, 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:

After oral intake is well absorbed from the gastrointestinal tract (GIT), the time to reach the maximum concentration (TCmax) in blood plasma - 1-2 hours.

Metabolised in the liver. The half-life (T1 / 2) is 6-10-18 hours. It is excreted mainly by kidneys in the form of metabolites.

Indications:

The drug is used for various neurotic, neurotic-like psychopathic, psychopathic and other conditions, accompanied by anxiety, fear, increased irritability, tension, emotional lability. With reactive psychoses, hypochondriacelo-sensopathic syndrome (including those resistant to the action of other tranquilizers), autonomic dysfunction and sleep disorders,for the prevention of states of fear and emotional stress.

As an anticonvulsant - temporal and myoclonic epilepsy.

In neurological practice, phenazepam® is used to treat hyperkinesis and tics, muscle stiffness, and vegetative lability.

Contraindications:

Coma, shock, myasthenia gravis, zakratougolnaya glaucoma (acute attack or predisposition), acute alcohol poisoning (with weakening vital functions), narcotic analgesics and hypnotics, severe chronic obstructive pulmonary disease (possibly increased respiratory failure), acute respiratory failure, severe Depression (suicidal tendencies may manifest); pregnancy (especially I trimester), lactation period, children and adolescence under 18 years (safety and efficacy not determined), hypersensitivity (including other benzodiazepines).

Carefully:

Use with caution in hepatic and / or renal failure, cerebral and spinal ataxia, drug dependence in history, propensity to abuse psychoactive drugs, hyperkinesia,organic brain diseases, psychosis (paradoxical reactions are possible), hypoproteinemia, nocturnal apnea (established or suspected), elderly patients.

Pregnancy and lactation:

In pregnancy, use is only possible for life indications. Has a toxic effect on the fetus and increases the development of congenital malformations when applied in the first trimester of pregnancy. Admission to therapeutic doses in later periods of pregnancy can cause central nervous system (CNS) depression in a newborn. Continuous use during pregnancy can lead to physical dependence with the development of withdrawal syndrome in a newborn. Children, especially at a young age, are very sensitive to the CNS depressing action of benzodiazepines.

The use immediately 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).

Dosing and Administration:

Inside: for sleep disorders - 0.5 mg for 20-30 minutes before sleep.

For treatment of neurotic, psychopathic, neurosis-like and psychopathic-like conditions, the initial dose is 0.5-1 mg 2-3 times a day.After 2-4 days, taking into account the effectiveness and tolerability, the dose can be increased to 4-6 mg / day.

With severe agitation, fear, anxiety, treatment starts with a dose of 3 mg / day, rapidly increasing the dose to obtain a therapeutic effect.

In the treatment of epilepsy - 2-10 mg / day.

For treatment of alcohol withdrawal - inside, 2-5 mg / day.

The average daily dose is 1.5-5 mg, it is divided into 2-3 doses, usually 0.5-1 mg in the morning and in the afternoon and up to 2.5 mg at night. In neurological practice, for diseases with muscular hypertension, 2-3 mg 1-2 times / day are prescribed.

The maximum daily dose is 10 mg.

To avoid the development of drug dependence in course treatment, the duration of the use of phenazepam is 2 weeks (in some cases, the duration of treatment can be increased to 2 months). With the abolition of phenazepam, the dose is reduced gradually.

Side effects:

From the side of the central nervous system and the peripheral nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, fatigue, dizziness, decreased ability to concentrate, ataxia, disorientation, unsteadiness of gait, slowing of mental and motor reactions,confusion of consciousness; rarely - headache, euphoria, depression, tremor, memory loss, movement coordination disorders (especially at high doses), mood depression, dystonic extrapyramidal reactions (uncontrolled movements, including the eye), asthenia, muscle weakness, dysarthria, epileptic seizures (in patients with epilepsy); extremely rarely - paradoxical reactions (aggressive outbreaks, psychomotor agitation, fear, suicidal tendencies, muscle spasm, hallucinations, agitation, irritability, anxiety, insomnia).

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

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

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

Allergic reactions: skin rash, itching.

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 - withdrawal syndrome (irritability, nervousness, sleep disturbances, dysphoria, spasm of smooth muscles of internal organs and skeletal muscles, depersonalization, enhancement sweating, depression, nausea, vomiting, tremor, perception disorders, incl. hyperaemia, paresthesia, photophobia; tachycardia, convulsions, rarely - acute psychosis).

Overdose:

Symptoms: severe depression of consciousness, cardiac and respiratory activity, pronounced drowsiness, prolonged confusion, decreased reflexes, prolonged dysarthria, nystagmus, tremor, bradycardia, shortness of breath or shortness of breath, lowering of blood pressure, coma.

Treatment: gastric lavage, reception of activated charcoal, hemodialysis ineffective, control of vital body functions, maintenance of respiratory and cardiovascular activity, symptomatic therapy. Specific antagonist flumazenil (in hospital conditions) (iv 0.2 mg, if necessary up to 1 mg in a 5% solution of glucose or 0.9% solution of sodium chloride).

Interaction:

With simultaneous use of phenazepam reduces the effectiveness of levodopa in patients with Parkinsonism.

Phenazepam may increase the toxicity of zidovudine.

There is a mutual enhancement of the effect with simultaneous application antipsychotic, antiepileptic or hypnotics, as well as central muscle relaxants, narcotic analgesics, ethanol.

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

With simultaneous use with antihypertensive agents, it is possible to increase antihypertensive action. Against the background of simultaneous administration of clozapine, an increase in respiratory depression is possible.

Special instructions:

With renal and / or hepatic insufficiency and long-term treatment, it is necessary to control the picture of peripheral blood and the activity of hepatic enzymes.

Patients who had not previously taken psychoactive drugs had a therapeutic response to the use of phenazepam in lower doses, compared with patients taking antidepressants, anxiolytics or alcoholism.

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 reception may be a withdrawal syndrome (including depression, irritability, insomnia, increased sweating), especially with prolonged admission (more than 8-12 weeks). When patients develop such unusual reactions as increased aggressiveness, acute excitations, feelings of fear, thoughts of suicide, hallucinations, increased muscle cramps, difficulty falling asleep, superficial sleep, treatment should be discontinued.

In the course of treatment, patients are strictly prohibited from drinking ethanol. The efficacy and safety of the drug in patients under the age of 18 years is not established.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets 0.5 mg, 1 mg and 2.5 mg.

Packaging:

For 10 or 25 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 50 tablets in cans of polymeric with a cover of the control of the first opening.

Each jar, 5 contiguous cell packs of 10 tablets or 2 contourcell packs of 25 tablets together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperaturenot more than 25 ° C.

Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N003672 / 01

Date of registration:16.06.2009

The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Manufacturer: & nbsp

VALENTA PHARMACEUTICS, JSC Russia

Representation: & nbspVALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Information update date: & nbsp09.12.2015

Illustrated instructions

Instructions

Phenazepam® (Phenazepamum)