Lexotan: what is it and how is it used? Warnings and Precautions

Index

  • Introduction: what is it?
  • Dosage: how is it used and how does it work?
  • Warnings and Precautions
  • Interactions and side effects
  • Pregnancy and breastfeeding
  • Notes (storage methods etc.)

Questions and answers

Introduction: what is it?

Lexotan is an anxiolytic drug indicated for the treatment of anxiety , insecurity , unmotivated fear , tension and other somatic or psychiatric manifestations associated with an anxiety syndrome. It is also used in cases of insomnia . The active ingredient of Lexotan is bromazepam , a drug from the benzodiazepine family with a duration of action of 8-12 hours. It has anxiolytic, anticonvulsant, hypnotic and muscle relaxant properties. Benzodiazepines are only indicated when the disorder is severe, disabling or subjecting the subject to severe discomfort as they can causeaddiction or addiction .

Lexotan is available in the following pharmaceutical forms and strengths :

  • 5 mg, 3 mg tablets
  • Hard capsules of 3 mg, 6 mg
  • Oral drops in solution of 2.5 mg / mL

The drug is sold exclusively under a repeatable medical prescription .

Dosage: how is it used and how does it work?

Bromazepam binds to the gamma-amino-butyric acid receptor (GABA), a neurotransmitter with an inhibitory action of local interneurons in the brain and presynapses in the spinal cord, causing an increase in the inhibitory effect of GABA itself. Its effect is selective and therefore the other neurotransmitters are not affected . Bromazepam has no antidepressant effect .

Bromazepam has the side effectstypical of benzodiazepines such as the risk of abuse, tolerance and physical or psychological dependence. In his case, unlike other drugs of the same category, the possibility of abusing this substance is high because it is characterized by a rapid onset of the effect which, however, ends quickly. Given the relatively short half-life and duration of action between 8 and 12 hours , symptoms that may occur at the end of the drug’s effective period are often much more severe and frequent than with longer-lasting benzodiazepines. Given these characteristics, Bromazepam is often prescribed as a hypnotic to induce sleep more easily .

Patients taking Lexotan can have highly variable individual responses and therefore the dosage must be adjusted on a case by case basis .

  • Typically, the average dose is 1.5 to 3 mg , 2-3 times a day (1-2 tablets of 1.5 mg 2-3 times, or 1 capsule or 1 tablet of 3 mg 2-3 times, or 15-30 drops 2-3 times a day).
  • In the case of the 6 mg hard capsules , the average dose is 6-12 mg 2-3 times a day.

Elderly patients or patients with reduced hepatic function : the dosage must be carefully established by the doctor who will have to evaluate a possible reduction of the dosages indicated above.

Anxiety . Treatment should be as short as possible. The patient should be reevaluated regularly and the need for continued treatment should be carefully considered, particularly if the patient has no symptoms. The overall duration of treatment should generally not exceed 8-12 weeks , including a gradual withdrawal period. In certain cases, extension beyond the maximum processing period may be necessary; if so, this should not happen without a careful re-evaluation of the patient’s condition.

Insomnia (indications not applicable to Lexotan 6 mg hard capsules). Treatment should be as short as possible. The duration of treatment generally ranges from a few days to two weeks , up to a maximum of four weeks, including a gradual withdrawal period. In certain cases, it may be necessary to extend beyond the maximum treatment period, always after a re-evaluation of the patient’s condition by the doctor.

Treatment should be started with the lowest recommended dose. The maximum dose should not be exceeded.

Warnings and Precautions

Bromazepam is contraindicated in patients with :

  • Hypersensitivity to the active substance or to any of the excipients
  • Known hypersensitivity to benzodiazepines.
  • Myasthenia gravis.
  • Severe respiratory insufficiency.
  • Severe hepatic insufficiency (benzodiazepines are not indicated in the treatment of patients with severe hepatic insufficiency as they can cause encephalopathy).
  • Sleep apnea syndrome.
  • Narrow angle glaucoma.
  • Acute intoxication with alcohol, hypnotic, analgesic or psychotropic drugs (neuroleptics, antidepressants, lithium).

GENERAL PRECAUTIONS
Benzodiazepines should not be used alone to treat depression or anxiety associated with depression (suicide can be precipitated in such patients). Therefore, in patients with signs and symptoms of depressive disorder or suicidal tendencies, bromazepam should be used with caution and prescribing should be limited.

Benzodiazepines should be used with extreme caution in patients with a history of drug or alcohol abuse . The concomitant use of Lexotan with alcohol and / or drugs with central nervous system depressant activity should be avoided, as it may increase the clinical effects of bromazepam, including possible deep sedation andclinically relevant respiratory and / or cardiovascular depression .

Severe anaphylactic / anaphylactoid reactionshave been reported with the use of benzodiazepines. Cases of angioedema involving the tongue, glottis or larynx have been reported in patients after taking the first or subsequent doses of benzodiazepines. In these cases, airway obstruction may occur which could be fatal. Some patients taking benzodiazepines have experienced additional symptoms such as dyspnoea, throat closure, or nausea and vomiting. Patients who develop angioedema after treatment with benzodiazepines should not be re-treated with the drug. In the early stages of treatment, the patient should be monitored regularly to identify the minimum effective dose and frequency of administration and to prevent possible overdose during treatment.

TOLERANCE
Some loss of efficacy to the hypnotic effects of benzodiazepines may develop after repeated use for a few weeks.

DEPENDENCY
The use of benzodiazepines and benzodiazepine-like compounds can lead to the development of physical and mental dependence on these drugs. The risk of addiction increases with dose and duration of treatment; it is greater in patients with a history of drug or alcohol abuse . Therefore, benzodiazepines should be used with extreme caution in patients with a history of alcohol or drug abuse. The possibility of addiction is reduced when Lexotan is used in the appropriate dosewith short-term treatment.

WITHDRAWAL SYMPTOMS
Once physical dependence has developed, abrupt discontinuation of treatment will be accompanied by withdrawal symptoms. These can consist of headache , diarrhea , muscle aches , extreme anxiety , tension , restlessness, confusion and irritability. In severe cases the following symptoms may occur: derealization, depersonalization , hyperacusis, numbness and tingling of the extremities, hypersensitivity to light, noise and physical contact, hallucinationsor epileptic seizures. Other symptoms are: depression , insomnia, sweating , persistent tinnitus, involuntary movements, vomiting , paraesthesia, perceptual changes, abdominal and muscle cramps, tremor, myalgia, agitation, palpitations, tachycardia, panic attacks, dizziness, hyper-reflexia, loss of short-term memory, hyperthermia. INSOMNIA AND BOUNCING ANXIETY Upon discontinuation of treatment, a transient syndrome may occur in which symptoms that led to treatment with benzodiazepines recur in an aggravated form. It may be accompanied by other reactions, including mood changes, anxiety, restlessness or sleep disturbances

. Since the risk of withdrawal or rebound symptoms is greater after abrupt discontinuation of treatment, a gradual decrease in dosage is suggested .

The risk of falls and fractures is increased in patients taking concomitant sedatives (including alcoholic beverages) and in the elderly. Sedation, amnesia, impaired concentration and muscle function can adversely affect the ability to drive and use machines . The simultaneous intake of alcohol can aggravate this effect. If sleep duration has been insufficient, the likelihood of impaired alertness may be increased.DURATION

OF TREATMENT
The duration of treatment should be as short as possible depending on the indication, and should not exceed four weeks for insomnia and eight to twelve weeks for anxiety, including a gradual withdrawal period. Extension of therapy beyond these periods should not occur without careful re-evaluation of the clinical situation. At the beginning of the treatment it may be useful to inform the patient that it will be of limited duration and to explain precisely how the dosage should be progressively decreased . Furthermore, it is important that the patient is informed of the possibility of rebound phenomenathus minimizing anxiety about these symptoms should they occur when the medicine is stopped.
In the case of benzodiazepines with a short duration of action, withdrawal symptoms may occur in the dose interval between doses, particularly for high doses.
When using benzodiazepines with a long duration of action, it is important to warn the patient that abrupt change to a benzodiazepine with a short duration of action is not recommended , as withdrawal symptoms may occur.

AMNESIA
Benzodiazepines can induce antegrade amnesia . This most often happens several hours after ingesting the drugand, therefore, to reduce the risk it should be ensured that patients can have an uninterrupted sleep of several hours. Amnesic effects can be associated with behavioral changes. Anterograde amnesia can appear using the highest therapeutic doses (it has been documented with 6 mg): the risk is higher at higher doses. PSYCHIATRIC REACTIONS AND PARADOX When benzodiazepines are used it is known that reactions such as restlessness , agitation , irritability , aggression , delirium , anger , nightmares , hallucinations , psychosis can occur

, Abnormal behavior and are known other adverse effects related to the behavior. Should this occur, the use of the medicinal product should be discontinued . Such reactions are more frequent in children and the elderly as well as in patients with organic brain syndrome.

The possibility cannot be excluded that in patients with acute endogenous psychosis , especially severe depressive states, the symptoms are aggravated by the use of Lexotan. Therefore, benzodiazepines are not recommended for primary treatmentpsychotic illnesses. The presence of depression must always be excluded in particular in the initial and morning sleep disturbances, since the symptoms are also differently masked and the risks caused by the underlying disease are always present.

SPECIFIC GROUPS OF PATIENTS

  • Pediatric Patients : Benzodiazepines should not be administered to patients under the age of 18 without careful consideration of the actual need for treatment; the duration of treatment should be as short as possible.
  • Elderly patients : The use of benzodiazepines may be associated with an increased risk of falls due to undesirable effects such as ataxia, muscle weakness, dizziness, somnolence, tiredness, fatigue and therefore it is recommended to treat elderly patients with caution. Elderly people should take a reduced dose.
  • Patients with chronic respiratory failure : use a lower dose due to the risk of respiratory depression.
  • Patients with severe hepatic insufficiency : Benzodiazepines are not indicated as they can precipitate hepatic encephalopathy.
  • Patients with renal insufficiency : Lexotan should be administered with caution.
  • The same prudential measures should be taken for patients with heart failure and low blood pressure who should be regularly monitored during Lexotan therapy (as is recommended with other benzodiazepines and other psychopharmacological agents).
  • Patients with psychosis : Benzodiazepines are not recommended for the primary treatment of psychotic illness.

OVERDOSE
Benzodiazepines commonly cause somnolence, ataxia, dysarthria and nystagmus . Bromazepam overdose rarely poses a risk to life if the drug is taken alone, but can lead to dysarthria (difficulty in articulating the syllables that make up a word), areflexia (absolute lack of reflexes), apnea , hypotension , depression cardiorespiratory and coma .

Benzodiazepine overdose usually results in varying degrees of central nervous system depressionranging from drowsiness to coma. In mild cases, symptoms include drowsiness, mental confusion, and lethargy. In severe cases, symptoms may include ataxia, hypotonia, hypotension, respiratory depression , rarely coma, and very rarely death. Coma, if it occurs, usually lasts a few hours but can last longer and be cyclical, especially in elderly patients. Respiratory depressive effects associated with benzodiazepines are more serious in patients with respiratory conditions .

In the treatment of overdose of any drug, the possibility that other substances have been taken at the same time should be considered. Benzodiazepines potentiate the effects of other CNS depressant substances including alcohol . The patient’s vital signs should be monitored and supportive measures instituted based on the patient’s clinical picture. In particular, symptomatic treatment may be required for cardiorespiratory or central nervous system effects.
Take activated charcoal within 1-2 hours to reduce absorption . In the case of unconscious patients, airway protection is essential. In case of mixed ingestion , gastric lavage should be considered , but not as a routine treatment.

In emergency therapy, special attention should be paid to respiratory cardiovascular and central nervous system functions . If CNS depression is severe, consideration should be given to the administration of flumazenil , a benzodiazepine antagonist, which may be useful as an antidote. Flumazenil should only be administered under closely monitored conditions .
The use of flumazenil is not indicated in patients with epilepsy being treated with benzodiazepines. The antagonistic effect in these patients can trigger seizures. Flumazenil has a short half-life(about an hour), then patients who have been given it should be monitored after its effects wear off. Flumazenil should be used with extreme caution in the presence of drugs that can lower the seizure threshold (e.g. tricyclic antidepressants).

IMPORTANT INFORMATION ABOUT SOME EXCIPIENTS
Both tablets and capsules contain lactose therefore patients with rare hereditary problems of galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take this medicine.

INTERACTIONS AND UNDESIRABLE EFFECTS

Taking Lexotan in combination with other drugs should be carefully considered, as bromazepam can interact with other drug classes. There may be interactions at the level of the benzodiazepine mechanism of action (pharmacodynamics) or at the level of metabolic processes (pharmacokinetics). PHARMACODYNAMIC INTERACTIONS The effects of benzodiazepines, when administered concomitantly with alcohol or other CNS depressant drugs , may be increased with a consequent enhancement of the sedative effect.

. Therefore, concomitant alcohol intake should be avoided. The association with alcohol adversely affects the ability to drive or use machines.

The central system depressant effect may increase in cases of concomitant use of antipsychotics (neuroleptics), hypnotics , anxiolytics / sedatives , some antidepressant agents , opioids , narcotic analgesics , antiepileptics , anesthetics and sedative antihistamines . Narcotic analgesics can cause an increase in euphoria leading to an increase in psychic dependence .
Care should be especially careful when bromazepam is administered with drugs that depress the respiratory functions such as opioids ( analgesics, antitussives, substitution treatment ), particularly in elderly patients.

PHARMACOKINETIC INTERACTIONS
Compounds that inhibit major oxidative liver enzymes (especially cytochrome P450) may increase the activity of benzodiazepines. Pharmacokinetic interactions can occur when bromazepam is co-administered with drugs that inhibit the hepatic enzyme CYP3A4 , resulting in increased plasma levels of bromazepam .

Concomitant administration of bromazepam with potent cytochrome P3A4 inhibitors (e.g. azole antifungals, protease inhibitors or some macrolides) should be done with caution considering a potential dose reduction. In the case of narcotic analgesics , an increase in euphoria may also occur , related to an increase in psychic dependence .
Concomitant administration of cimetidine (an inhibitor of several cytochromes) and possibly propranolol may prolong the elimination half-life of bromazepam through a substantial reduction in clearance (with cimetidine: 50% reduction).
Concomitant administration of fluvoxamine, an inhibitor of CYP1A2, leads to a significant increase in exposure to bromazepam (2.4-fold increase in AUC, i.e. the amount of unchanged drug reaching the systemic circulation after administration of a given dose ), and the elimination half-life (1.9-fold increase).
Administration of theophylline or aminophylline may reduce the effects of benzodiazepines.

Like all medicines, Lexotan can cause side effects, although not everybody gets them. Contact your doctor immediatelyif during treatment with Lexotan you experience any of the following serious side effects depression, restlessness, agitation, irritability, aggression, distorted perception of reality (delirium), anger, nightmares, perception of things that do not exist in reality (hallucinations), behavioral changes, psychosis (mental disorder that causes an altered perception of reality, thought disturbances, mental confusion). These reactions may be more frequent if the patient is elderly .

Pregnancy and breastfeeding

PREGNANCY
The safe use of bromazepam in pregnancy has not yet been established . A review of spontaneous reports of adverse drug events showed an incidence comparable to what might be expected in a similar untreated population. Benzodiazepine exposure in the first trimester of pregnancy does not appear to be associated with an increased risk of major malformations. However, some preliminary epidemiological studies have shown an increased incidence of oral cleft risk in neonates.

Treatment with benzodiazepines at high doses, during the second and / or third trimester of pregnancy, revealed adecreased active fetal movements and a variability of the fetal heart rhythm .

If the product is prescribed to a woman of childbearing age , the patient must tell her doctor whether she intends to become pregnant or suspects she is pregnant .

If, for serious medical reasons, the product is administered during the last period of pregnancy , or during labor even at low doses, the ” flaccid baby ” syndrome characterized by axial hypotonia and problems in sucking may occur in the newborn.resulting in poor weight gain. These signs are reversible but can last from 1 to 3 weeks, depending on the half-life of the product. Respiratory depression or apnea and hypothermia may occur in newborns at high doses . Furthermore, infants born to mothers who have chronically taken benzodiazepines during late pregnancy may develop physical dependence and may be at some risk of developing postnatal withdrawal symptoms such as hyperexcitability, agitation and tremor even after a few days after birth and in the absence of “flaccid baby” syndrome.

Taking into account these data, the use of bromazepam during pregnancy could only be considered if thetherapeutic indications and dosage are strictly respected . If treatment with bromazepam is necessary during the last trimester of pregnancy, avoid high doses and neonates should be monitored to avoid withdrawal symptoms and / or “flaccid baby” syndrome.

BREASTFEEDING
Since bromazepam is excreted in breast milk, it is not recommended for use in breastfeeding mothers.

Notes (storage methods etc.)

Expiry of the unopened package correctly stored:

  • capsules and tablets : 5 years
  • oral drops solution : 3 years, validity after the first opening of the oral drops solution 16 days

The drug should not be used after the expiry date stated on the package.
The hard capsules should not be stored above 30 ° C.

Unused medicine and wastes derived from this medicine must be disposed of in accordance with local regulations .

Questions and answers

HOW LONG DOES THE EFFECT OF LEXOTAN LAST?

The duration of action of Lexotan does not exceed 24 hours.

IS LEXOTAN A SEDATIVE?

Lexotan has an inhibitory action on the nervous system and the consequent sedation and alteration of muscle concentration and function can negatively affect the ability to drive and use machines. The simultaneous intake of alcohol can aggravate this effect.

DOES LEXOTAN LOWER BLOOD PRESSURE?

The use of Lexotan can cause a moderate reduction in blood pressure , but this is not the main effect of this drug.

SIDE EFFECTS OF LEXOTAN?

Like all medicines, Lexotan can cause side effects, although not everybody gets them. The most common side effects are depression, restlessness, agitation, irritability, aggression , distorted perception of reality (delirium), anger, nightmares, perception of things that do not exist in reality ( hallucinations ), behavioral changes , psychosis (mental disorder that causes a altered perception of reality, thought disturbances, mental confusion).

DOES LEXOTAN RELAX THE MUSCLES?

The inhibiting action of the nervous system by Lexotan can also cause muscle relaxation

 

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