Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Antiepileptic remedy from the group of benzodiazepine derivatives. Has pronounced anticonvulsant, as well as central miorelaksiruyuschee, anxiolytic, sedative and hypnotic action.
Increases the inhibitory effect of 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 postsynaptic spinal reflexes.
Anxiolytic effect 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 neurotic symptoms (anxiety, fear).
Anticonvulsant action is realized due to increased presynaptic inhibition. This suppresses the spread of epileptogenic activity that occurs in epileptogenic foci in the cortex, thalamus, and limbic structures, but the excited state of the focus is not removed.
It is shown that in a human clonazepam rapidly suppresses paroxysmal activity of various types, incl. complexes "spike-wave" with absences (petit mal), slow and generalized complexes "spike-wave", "soldering" of temporal and other localization, as well as irregular "spikes" and waves.
Changes in the generalized EEG are suppressed more than focal. In accordance with these data, clonazepam has a beneficial effect in the generalized and focal forms of epilepsy.
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
When administered, bioavailability is more than 90%. Binding to plasma proteins - more than 80%. V d - 3.2 l / kg. T 1/2 - 23 hours. It is excreted mainly in the form of metabolites.
INDICATIONS
The first-line agent is epilepsy (adults, infants and young children): typical absences (petit mal), atypical absences (Lennox-Gastaut syndrome), cramping seizures, atonic seizures (fall syndrome or drop-attacks).
The second-line agent is infantile spasms (West syndrome).
The agent of the third series is tonic-clonic convulsions (grand mal), simple and complex partial seizures and secondary generalized tonic-clonic convulsions.
Epileptic status (iv introduction).
Somnambulism, muscle hypertonicity, insomnia (especially in patients with organic brain lesions), psychomotor agitation, alcohol withdrawal syndrome (acute agitation, tremor, threatening or acute alcohol delirium and hallucinations), panic disorders.
DOSING MODE
Individual. For oral administration, an initial dose of no more than 1 mg / day is recommended. The maintenance dose is 4-8 mg / day.
For infants and children aged 1-5 years, the initial dose should not be more than 250 mcg / day, for children aged 5-12 years - 500 mcg / day. Supporting daily doses for children under 1 year of age - 0.5-1 mg, 1-5 years - 1-3 mg, 5-12 years - 3-6 mg.
For elderly patients, an initial dose of not more than 500 Ојg is recommended.
The daily dose should be divided into 3-4 equal doses. Supportive doses are prescribed after 2-3 weeks of treatment.
In / in (slowly) adults - 1 mg, children under 12 years - 500 mcg.
SIDE EFFECT
From the side of the central nervous system: at the beginning of treatment - severe inhibition, fatigue, drowsiness, lethargy, dizziness, numbness, headaches; rarely - confusion, ataxia. When used in high doses, especially with prolonged treatment - violations of articulation, diplopia, nystagmus; paradoxical reactions (including acute excitation conditions); anterograde amnesia. Rarely - hyperergic reactions, muscle weakness - depression. With prolonged treatment of some forms of epilepsy, an increase in the frequency of seizures is possible.
On the part of the digestive system: rarely - dry mouth, nausea, diarrhea, heartburn, nausea, vomiting, decreased appetite, constipation or diarrhea, impaired liver function, increased activity of hepatic transaminases and alkaline phosphatase, jaundice. Infants and young children may have increased salivation.
From the cardiovascular system: a decrease in blood pressure, tachycardia.
On the part of the endocrine system: a change in libido, dysmenorrhea, reversible premature sexual development in children (incomplete premature puberty).
On the part of the respiratory system: with intravenous administration, respiratory depression is possible, especially against the background of treatment with other drugs that cause respiratory depression; in infants and young children, bronchial hypersecretion is possible.
On the part of the hematopoiesis system: leukopenia, neutropenia, agranulocytosis, anemia, thrombocytopenia.
From the urinary system: urinary incontinence, urinary retention, impaired renal function.
Allergic reactions: urticaria, skin rash, itching, extremely rarely - anaphylactic shock.
Dermatological reactions: transient alopecia, change in pigmentation.
Other: addiction, drug dependence; with a sharp decrease in dose or discontinuation of reception - withdrawal syndrome.
CONTRAINDICATIONS
Inhibition of the respiratory center, severe COPD (progression of the degree of respiratory failure), acute respiratory failure, myasthenia gravis, coma, shock, occlusive glaucoma (acute attack or predisposition), acute alcohol intoxication with impaired vital functions, acute poisoning with narcotic analgesics and hypnotics, severe depression (there may be suicidal tendencies), pregnancy, lactation, increased sensitivity to clonazepam.
PREGNANCY AND LACTATION
Contraindicated in pregnancy and lactation. Clonazepam penetrates the placental barrier. Clonazepam may be excreted in breast milk.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With extreme caution apply in patients with severe liver disease.
APPLICATION FOR CHILDREN
With prolonged use of clonazepam in children, one should keep in mind the possibility of side effects on physical and mental development, which may not manifest itself for many years.
APPLICATION IN ELDERLY PATIENTS
With caution apply in elderly patients, tk. they can be slowed withdrawal of clonazepam and reduced tolerance, especially in the presence of cardiopulmonary insufficiency.
SPECIAL INSTRUCTIONS
With extreme caution apply in patients with ataxia, severe liver disease, severe chronic respiratory failure, especially in the acute deterioration phase, with episodes of nocturnal apnea.
With caution apply in elderly patients, tk. they can be slowed withdrawal of clonazepam and reduced tolerance, especially in the presence of cardiopulmonary insufficiency.
With prolonged use, it is possible to develop drug dependence. With the abrupt withdrawal of clonazepam after prolonged treatment, the development of the withdrawal syndrome is possible.
With prolonged use of clonazepam in children, one should keep in mind the possibility of side effects on physical and mental development, which may not manifest itself for many years.
During the treatment period, do not drink alcohol.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, the speed of psychomotor reactions slows down. This should be taken into account by persons engaged in potentially hazardous activities requiring increased attention and speed of psychomotor reactions.
DRUG INTERACTION
When used simultaneously with drugs that exert a depressing effect on the central nervous system, ethanol, ethanol-containing drugs, it is possible to intensify the inhibitory effect on the central nervous system.
With the simultaneous use of clonazepam enhances the effect of muscle relaxants; with valproate sodium - the weakening of sodium valproate and the provocation of convulsive seizures.
With simultaneous application, the case of decreasing the concentration of desipramine in the blood plasma was 2 times and its increase after the withdrawal of clonazepam.
When used simultaneously with carbamazepine, which induces the induction of microsomal liver enzymes, it is possible to increase metabolism and, as a result, reduce the concentration of clonazepam in the blood plasma, reducing it T 1/2 .
With simultaneous application with caffeine, a decrease in the sedative and anxiolytic effect of clonazepam is possible; with lamotrigine - a decrease in the concentration of clonazepam in the blood plasma; with lithium carbonate - the development of neurotoxicity.
With simultaneous application with the primidon, the concentration of primidone in the blood plasma increases; with tiapridom - the development of the NSA is possible.
When used simultaneously with toremifene, a significant decrease in AUC and T 1/2 of toremifene is possible due to induction of microsomal liver enzymes under the influence of clonazepam, which leads to an acceleration of the metabolism of toremifene.
A case of development of a headache with localization in the occipital region is described with simultaneous application with phenelzine.
With simultaneous use, an increase in the concentration of phenytoin in the blood plasma and the development of toxic reactions, a decrease in its concentration or the absence of these changes is possible.
With simultaneous use with cimetidine, side effects from the CNS are increased, however, the frequency of convulsive seizures in some patients decreased.
