Lexilium 6 mg. 30 tablets
Each tablet contains 3 mg bromazepam.
3. PHARMACEUTICAL FORM
4. CLINICAL DATA
4.1 Therapeutic indications
For short-term treatment of intense anxiety.
4.2 Dosage and method of administration
Treatment should be as short as possible. The overall duration of treatment generally should not be more than 8-12 weeks, including the reduction of the dose.
The patient should be checked regularly at the start of treatment to minimize the dosage and / or frequency of administration to prevent overdose due to accumulation.
These amounts are general recommendations and the dosage should be individualized. Treatment of outpatients should begin with low doses, they gradually rise to an optimum level. The patient should be reassessed regularly, as must be assessed the need for continuation of treatment, especially when the patient has no symptoms.
In some cases it may be necessary to continue therapy beyond the maximum period of treatment. In this case it should not be done without re-evaluation of the patient's condition through a special examination.
Must be administered at the lowest dose that can control the symptoms.
The optimum dosage and frequency of administration of Lexotan must be determined individually for each patient, depending on the severity of symptoms and a history of previous psychotropic drugs.
The customary dose in the general practice is from 3 to 18 mg per day in divided doses.
In exceptional cases, in hospitalized patients, can be administered a dose of 60 rag per day in divided doses.
Treatment should always be tapered off gradually. Patients who have taken benzodiazepines for a prolonged time may require a longer period of dose reduction. It may be appropriate use of special assistance.
Elderly and / or debilitated patients Elderly patients require lower doses because of individual variations in sensitivity and pharmacokinetics. Doses should not exceed half of the recommended dose (see section 5.2. Pharmacokinetics in Special Populations).
Patients with impaired hepatic and / or renal function require lower doses because of individual variations in sensitivity and pharmacokinetics.
In elderly patients and patients with impaired renal and / or hepatic function is advisable to review treatment regularly and stop as much as possible in advance. '
Lexotan is not for use in children under 12 years of age.
Hypersensitivity to benzodiazepines
Severe respiratory insufficiency
Severe hepatic insufficiency (benzodiazepines are not indicated to treat patients with severe hepatic insufficiency as they may cause encephalopathy).
4.4 Special precautions
After repeated use over several weeks may develop some loss of effectiveness of the benzodiazepines.
Use of benzodiazepines may lead to the development of physical and psychic dependence upon these products (see section 4.8. Undesirable effects) The risk of dependence increases with dose and duration of treatment. It is greater in patients with a history of alcohol abuse and drugs.
Once physical dependence has developed, abrupt termination of treatment will be accompanied by withdrawal symptoms. They may consist of headaches, muscle pain, extreme anxiety, tension, restlessness, confusion and irritability. In severe cases, you may experience the following symptoms: derealization, depersonalization, hyperacusis, numbness and tingling of extremities, hypersensitivity "to light, noise and physical contact, hallucinations or epileptic seizures (see section 4.8. Undesirable effects).
Rebound insomnia and anxiety: Upon termination of treatment may be a transient syndrome whereby the symptoms that led to treatment with a benzodiazepine recur in an enhanced form. It may be accompanied by other reactions including mood changes, anxiety or sleep disturbances and restlessness. Since the risk of withdrawal phenomena / rebound phenomena is greater after abrupt discontinuation of treatment, it is recommended to reduce the dose gradually.
Duration of treatment
Treatment duration should be as short as possible (see section 4.2. Posology and method of administration). The overall duration of treatment generally should not be more than 8-12 weeks, including the reduction of the dose. This period should not be extended without reassess the situation.
May be useful in early treatment to inform the patient, the duration will be limited and to explain precisely how the dose will be reduced gradually. It is also important that the patient be aware of the possibility of rebound phenomena, thereby minimizing anxiety when these symptoms occur after discontinuation of the drug.
There is evidence that benzodiazepines with a short duration of action, withdrawal phenomena can become manifest within the dosage interval, especially when the dosage is high. When using long-acting benzodiazepines, it is important to warn against changing to a benzodiazepine with a short duration of action, as it can develop withdrawal symptoms.
Benzodiazepines may induce anterograde amnesia. Anterograde amnesia may occur using higher therapeutic dosages (documented at 6 mg), the risk increases with higher doses. Amnestic effects may be associated with inappropriate behavior. The condition occurs most often several hours after ingesting the product and therefore to reduce the risk, patients must provide 7-8 hours of uninterrupted sleep (see section 4.8. Undesirable effects).
Psychiatric and "paradoxical"
It is known that the use of benzodiazepines may occur reactions such as anxiety, agitation, irritability, delusions, anger, nightmares, hallucinations, psychoses, inappropriate behavior and other adverse behavioral effects. If this occurs, the drug should be discontinued.
More likely to occur in children and the elderly. Specific patient groups
Benzodiazepines should not be given to children without careful assessment of the need. The duration of treatment should be minimal. Of elderly patients should be given a reduced dose (see section 4.2. Posology and method of administration). A lower dose is recommended for patients with chronic respiratory insufficiency due to the risk of respiratory depression. Benzodiazepines are not indicated for treatment of patients with severe liver failure, as they may cause encephalopathy.
Benzodiazepines are not recommended for the primary treatment of psychotic illness.
Benzodiazepines should not be used alone to treat depression or anxiety associated with depression (such patients may trigger suicidal ideation). Patients with known or presumed dependence on alcohol or drugs should not take benzodiazepines, except in rare situations under medical supervision.
4.5 Interaction with other medicinal products and other forms of interaction
Not recommended: Concomitant use of alcohol,
Sedative effects may be enhanced when the product is used in combination with alcohol. This may affect the ability to drive and use machines.
Interactions which should be taken into account: Combination with CNS depressants
With concomitant use with antipsychotics (neuroleptics), hnpnotitsi, anxiolytics / sedatives, antidepressants, narcotic analgesics, antiepileptic drugs, anesthetics and sedative antihistamines may be observed strengthening of the central depressant effect.
When narcotic analgesics may occur and reinforcing euphoria, resulting in an increase in physiological dependence.
Compounds that inhibit hepatic enzymes (particularly cytochrome P450) may enhance the activity of these benzodiazepines which are metabolized by these enzymes. To a lesser extent this also refers to benzodiazepines that are metabolised only by conjugation.
Co-administration of cimetidine may prolong the half-life of bromazepam.
4.6 Pregnancy and lactation
Benzodiazepines should be used during pregnancy or lactation only if the doctor considers it important. Studies of benzodiazepines in animals have shown minor effects on the fetus and several studies reported late behavioral disorders in offspring exposed in utero.
When the drug is prescribed to a woman of childbearing potential, she should be warned to contact her physician regarding discontinuance of the product if she intends to become or suspects that she is pregnant.
If for compelling medical reasons, the drug is administered during the late phase of pregnancy or during labor, can be expected effects on the neonate, such as hypothermia, hypotonia and moderate respiratory depression, due to the pharmacological action of the compound.
Moreover, infants born to mothers who took benzodiazepines chronically during the latter stages of pregnancy may have developed physical dependence and may be at risk of developing withdrawal symptoms in the postnatal period.
Since benzodiazepines are found in breast milk, they should not be given to nursing mothers.
4.7 Effects on ability to drive and use machines
Sedation, amnesia, impaired concentration and impaired muscular function may adversely affect the ability to drive or operate machinery. If insufficient sleep duration occurs, the likelihood of impaired alertness may be increased (see section 4.5. Interactions with other drugs and other forms of interaction). In addition, patients should be aware that alcohol can increase the degree of impairment and therefore, during treatment should be avoided.
4.8 Undesirable effects
Drowsiness (when the product is used as a sedative, should clearly say daytime sleepiness), blunted emotions, reduced alertness, confusion, fatigue, headache, dizziness, muscle weakness, ataxia or double vision. These phenomena occur predominantly at the start of therapy and usually disappear with repeated administration.
Sometimes reported other side effects such as gastrointestinal disturbances, changes in libido or skin reactions.
Anterograde amnesia may occur at therapeutic doses, the risk increasing at higher doses. Amnestic effects may be associated with inappropriate behavior (see section 4.4. Special warnings and precautions for use)
Existing depression may be unmasked during benzodiazepine use.
Psychiatric and "paradoxical"
It is known that the use of benzodiazepines and benzodiazepine-like drugs, can occur reactions such as anxiety, agitation, irritability, aggression, delusions, anger, nightmares, hallucinations, psychoses, inappropriate behavior and other adverse behavioral effects (see section 4.4. special warnings and precautions for use). If this occurs, the drug should be discontinued. More likely to occur in children and elderly patients than in other patients.
Use (even at therapeutic doses) can result in the development of physical dependence. Discontinuation of treatment may cause withdrawal phenomena or rebound phenomena (see section 4.4. Special warnings and precautions for use). May occur psychological dependence. There are reports of abuse of benzodiazepines.
As with other benzodiazepines, overdose should not present a hazard to life unless the drug is not combined with other CNS depressants (including alcohol).
In the treatment of overdose with any medicinal product, it should be borne in mind that you may have used multiple medications.
Following overdose with any medicinal product should be induced vomiting (within one hour) if the patient is conscious or gastric lavage with respiratory protection if the patient is unconscious. If there is no advantage in emptying the stomach, should be given activated charcoal to reduce absorption. Special attention should be paid to intensive care of respiratory and cardiovascular function.
Overdose of benzodiazepines is usually manifested by the suppression of the central nervous system, ranging from somnolence to coma. In mild cases, symptoms include drowsiness, mental confusion and lethargy. In most cases it is sufficient to monitor vital functions and await recovery. Higher doses, especially in combination with other centrally acting drugs may cause ataxia, hypotonia, hypotension, respiratory depression, rarely coma and very rarely - death.
Flumazenil may be useful as an antidote. Patients who need such intervention must be carefully monitored in the hospital (see separate prescribing information). The administration of flumazenil is not recommended in patients with epilepsy who have been treated with
recommended in patients with epilepsy who were treated with benzodiazepines. Antagonism in these patients can cause
5. PHARMACOLOGICAL PROPERTIES
5.1 Pharmacodynamic properties
Bromazepam is piridilbenzodiazepinovo compound with anxiolytic properties.
5.2 Pharmacokinetic properties
Lexotanil is rapidly absorbed from the gastrointestinal tract. Maximum plasma concentrations typically occur within 2 hours after oral administration of bromazepam. Absolute (as opposed to intravenous solution) and relative (versus oral solution) bioavailability of the tablet is 60% and 100% respectively.
An average of 70% of bromazepam is bound to plasma proteins. The volume of distribution is 50 liters. Steady-state plasma concentrations are reached after about 5-9 days.
Bromazepam is metabolized in the liver. Quantitatively predominant two metabolites: W-hydroxy-bromazepam and 2- (2-amino-5-bromo-3-hydroxybenzoyl) pyridine. Lexotanil metabolites do not contribute significantly to the effects of the drug.
Urinary excretion of intact bromazepam and glucuronide conjugates of 3-hydroxy-bromazepam and 2- (2-amino-5-bromo-3-hydroxybenzoyI) pyridine is 2%, 27% and 40% of the administered dose. Bromazepam has a half-life of about 20 hours (between about 16 and 30 hours). Clearance is 40 ml / min.
Pharmacokinetics in Special Populations
The half-life may be prolonged in elderly patients (see section 4.2. Posology and method of administration).
5.3 Preclinical safety data
No additional information from preclinical studies that might be relevant to the administration of the drug and which were not included in other sections of the SPC.
6.1 List of excipients
Microcrystalline cellulose, lactose, magnesium stearate, Erythrosine aluminium lake (E127)
Are not known.
6.3. Expiration date
PVC blister packs: 5 years
6.4 Special precautions for storage
Do not store above 25 ° C. Store in tightly closed container in a dry place, protected from light.