Lorafen (Lorafen)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceLorazepamLorazepam
Dosage form: & nbspcoated tablets
Composition:

Tablets with a dosage of 1 mg

active substance: lorazepam 1 mg;

Excipients:

core tablet: potato starch 6 mg, sodium carboxymethyl starch 0.1 mg, gelatin 1.5 mg, talc 1.8 mg, magnesium stearate 1.2 mg, lactose up to 80 mg;

tablet shell: polyvinyl alcohol 0.125 mg, talc 7 mg, maltodextrin 0.23 mg, sucrose 22.5 mg, titanium dioxide 0.18 mg.

Tablets with a dosage of 2.5 mg

active substance: lorazepam 2.5 mg;

Excipients:

core tablet: potato starch 6 mg, sodium carboxymethyl starch 0.5 mg, gelatin 1,5 mg, talc 1,8 mg, dye Crimson [ponso 4R] 0.00286 mg, magnesium stearate 1.2 mg, lactose up to 80 mg;

tablet shell: polyvinyl alcohol 0.125 mg, talc 7 mg, maltodextrin 0.23 mg, sucrose 22.5 mg, dye crimson [ponso 4R] lacquer aluminum 0.01 mg, titanium dioxide 0.17 mg.

Description:

Tablets with a dosage of 1 mg - round, biconvex tablets coated with a coat, white or almost white.

Tablets with a dosage of 2.5 mg - round, biconcave tablets covered with a coat, pink.

Pharmacotherapeutic group:Anxiolytic agent
ATX: & nbsp

N.05.B.A.06   Lorazepam

N.05.B.A   Benzodiazepine derivatives

Pharmacodynamics:

The drug belongs to the list of psychotropic substances (list III).

Lorazepam belongs to the group of 1,4-benzodiazepine derivatives. The drug acts on many structures of the central nervous system - primarily on the limbic system and hypothalamus, i.e. on the structures associated with the regulation of emotional activity. Like all benzodiazepines, it increases the inhibitory effect of GABA-ergic neurons of the cerebral cortex, hypocampus, cerebellum, thalamus and hypothalamus. The existence of specific binding sites for benzodiazepines, which are protein structures of the cell membrane, which are associated with a complex consisting of the GABA-A receptor and the chlorinated capal are established. The effect of lorazepam is to modulate the "sensitivity" of the GABA-ergic receptor, which leads to an increase in the affinity of this receptor for gamma-aminobutyric acid (GABA), which is an endogenous inhibitory neurotransmitter. The consequence of activation of the benzodiazepine receptor or GABA-A is an increase in the intake of chloride ions into the neuron through the chlorine canal.This leads to hyperpolarization of the cell membrane, as a result of which the activity of the neuron is suppressed. Clinically lorazepam has an anxiolytic and hypnotic effect. It also has an anticonvulsant and central muscle relaxant effect.

Pharmacokinetics:

Suction

Lorazepam is well absorbed from the digestive tract. The maximum concentration in the blood reaches about 2 hours. After taking 2 mg of lorazepam, the maximum concentration in the blood is 20 ng / ml.

Distribution

Lorazepam is 85% bound to blood proteins. Passes through blood-brain and placental barriers. Penetrates into breast milk.

Metabolism

The process of biotransformation of lorazepam takes place in the liver. As a result of conjugation with glucuronic acid, an inactive metabolite, lorazepam glucuronate, is formed. The biological half-life of lorazepam is about 12 hours.

Excretion

Lorazepam is excreted in the urine in the form of lorazepam glucuronate.

Indications:

- Neurotic and neurosis-like conditions that occur with anxiety, irritability, increased fatigue, sleep disturbance, vegetative disorders.

- Alcohol abstinence syndrome (as part of complex therapy).

- Hypertonus of skeletal muscles of different genesis.

- Premedication (preparation for long-term diagnostic procedures and operations).

The drug should be used strictly according to the doctor's prescription in order to avoid complications.

Attention! The states of mental stress and anxiety associated with everyday problems are not an indication for the use of the drug.

Contraindications:

- Hypersensitivity to derivatives of 1,4-benzodiazepine or to any substance included in the preparation.

- Severe respiratory failure, regardless of the cause.

- Severe hepatic and renal insufficiency.

- Myasthenia gravis.

- Glaucoma.

- Acute porphyria.

- Alcohol poisoning.

- The syndrome of nocturnal apnea.

- Children under 12 years.

It is not recommended to use the drug Laurafen in patients with psychoses.

In connection with the content of lactose, the drug Laurafen should not be used in patients with hereditary lactose intolerance, Lappease lactase deficiency or glucose-galactose malabsorption.

In connection with the content of sucrose, the drug Laurafen should not be used in patients with hereditary disorders associated with intolerance to fructose, a syndrome of poor absorption of glucose-galactose, or a shortage of isomaltase sugarase.

Carefully:

Hepatic and / or renal failure of mild and moderate severity, chronic respiratory failure, porphyria, depression, suicidal ideation and attempts in history, drug, narcotic or alcoholic dependence in history, cerebral and spinal ataxia, hyperkinesia, organic brain diseases, hypoproteinemia , elderly age.

It is not recommended to use the drug Laurafen in patients with psychoses.

During treatment with Laurafen and within 3 days after its completion, you should not drink any alcoholic beverages.

Pregnancy and lactation:

Before using each drug, the patient should consult a doctor.

The use of lorazepam in pregnant women is allowed only if its use in the mother has absolute indications, and the use of a safer, alternative means is impossible.

Lorazepam penetrates into the mother's milk. Therefore, if the use of the drug in a nursing mother is indicated, it is necessary to stop breastfeeding.

Dosing and Administration:

The drug should be taken orally, with a small amount of water.Dosage and duration of treatment should be strictly according to the doctor's instructions.

Adults and children over 12 years of age

With neurotic and neurosis-like states usually first prescribe from 2 mg to 3 mg of lorazepam per day, divided into 1-3 doses, and then, if necessary, increase the daily dose of the drug to the maintenance dose, which is usually from 2 mg to 6 mg per day, divided by 1 - 3 reception.

For relief of symptoms of anxiety it is recommended that the lowest possible effective dose be used.

The dose of lorazepam should be increased gradually, starting with an increase in the dose taken in the evening. Maximum can be prescribed up to 10 mg per day.

In cases of sleep disorders caused by anxiety usually prescribed once a day at bedtime from 2 mg to 5 mg of lorazepam.

For premedication prescribe from 2 mg to 5 mg at night before the planned procedure or surgery, and on the day from 2 mg to 5 mg 1-2 hours before the procedure or surgery.

Children under 12 years old

It is not recommended to apply lorazepam in children because of the lack of data on the safety and efficacy of lorazepam in children under 12 years of age.

Patients with hepatic and (or) renal failure of mild to moderate severity

Care should be taken when administering lorazepam to patients with impaired liver function and / or kidneys of mild and moderate severity. The dose is selected individually for each patient, depending on the degree of insufficiency of the diseased organ.

Elderly patients

Patients of advanced age are more sensitive to drugs acting on the central nervous system. When using lorazepam in these patients it is recommended to prescribe the lowest possible effective dose. It is usually enough to apply half the dose given to an adult.

With symptomatic treatment of anxiety disorders duration of treatment should be limited to a minimum - it usually ranges from a few days to 2 weeks. In individual cases, treatment can be prolonged. The maximum duration of treatment, including a period of gradual cancellation, should not exceed 4 weeks. Gradual withdrawal of the drug should be set individually for each patient. In individual cases, after assessing the patient's condition, the doctor may decide to extend the maximum treatment time.

In case of missed dose of Laurafen: The drug should be taken as soon as possible or continue to be taken regularly.

Do not take a double dose in order to replenish the missed dose!

Side effects:

From the nervous system (especially in elderly patients): drowsiness, fatigue, dizziness, decreased ability to concentrate, ataxia (instability of gait and poor coordination of movements, leading to loss of balance), disorientation, lethargy, muscle atony, dulling of emotions, slowing of mental and motor reactions; less often - headache, euphoria, depression, tremor, mood depression, catalepsy, amnesia, confusion, dystonic extrapyramidal reactions (uncontrolled body movements, including the eyes), myasthenia gravis during the day, dysarthria; extremely rarely - paradoxical reactions (aggressive outbursts, fear, suicidal tendencies, muscle spasm, confusion, hallucinations, acute arousal, irritability, anxiety, insomnia).

From the sense organs: impaired vision (diplopia).

On the part of the organs of 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; impaired liver function, increased activity of "liver" transaminases, lactate dehydrogenase and alkaline phosphatase, jaundice.

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

Allergic reactions: skin rash (including erythematosus, urticaria), itching of the skin; extremely rare - anaphylactic reactions.

Influence on the fetus: teratogenicity, respiratory failure and suppression of sucking reflex in newborns whose mothers used the drug.

Other: addiction, drug dependence, lowering blood pressure; rarely - depression of the respiratory center, bulimia, weight loss, tachycardia.

With a sharp decrease in dose or discontinuation of reception - withdrawal syndrome (irritability, headache, anxiety, excitement, arousal, a sense of fear, nervousness,sleep disorders, a spasm of smooth muscles of internal organs and skeletal muscles, myalgia, depersonalization, sweating, sweating, depression, nausea, vomiting, tremor, disorders of perception, including hyperacusis, paresthesia, photophobia, tachycardia, convulsions, hallucinations, rare - acute psychosis).

Overdose:

The following symptoms may occur as a result lorazepam overdose: drowsiness, disorientation, slurred speech, and in severe cases, loss of consciousness, coma. Life-threatening poisoning may be caused by the simultaneous intake of alcohol or lorazepam and lorazepam and other drugs have a depressing effect on the central nervous system.

In the case of poisoning lorazepam must take measures aimed at how to fast elimination from the body more nevsosavsheysya medicament or decrease its absorption from the digestive tract (induced vomiting, reception of activated charcoal, gastric lavage - subject to a saved consciousness), to monitor the vital functions (breathing , pulse, blood pressure) and, if necessary,apply appropriate symptomatic treatment.

A specific antidote is flumazenil.

Interaction:

Pharmaceutical

Pharmaceutical types of incompatibility are not defined.

Pharmacodynamic

- The oppressive effect of lorazepam on the central nervous system is enhanced by opioid analgesics, preparations for general anesthesia (anesthetics), psychotropic drugs, antidepressants, antihistamines, antihypertensive drugs of central action.

- The use of alcohol during treatment with lorazepam increases the inhibitory effect on the central nervous system and can lead to the development of paradoxical reactions such as: psychomotor agitation, aggressive behavior. In addition, alcohol can enhance the sedative effect of lorazepam, up to coma.

- Lorazepam taken together with other drugs that have a muscle relaxant effect, prolongs and intensifies the effect of the latter.

Pharmacokinetic

- Disulfiram, cimetidine, erythromycin, ketoconazole being inhibitors of cytochrome P450 isoenzymes inhibit the biotransformation of derivatives 1,4-benzodiazepine and enhance their inhibitory effect on the central nervous system.

- Drugs that induce cytochrome P450 activity (for example, rifampicin, phenobarbital, phenytoin. carbamazepine) affect the biotransformation of 1,4-benzodiazepine derivatives and lead to a weakening of their pharmacological action.

- Theophylline and caffeine can alleviate the hypnotic effect of benzodiazepines (including lorazepam), t. have a stimulating effect on the central nervous system and are capable of inducing hepatic enzymes responsible for the metabolism of drugs. This effect caused by theophylline and caffeine may be absent in smokers.

- Oral contraceptives used together with lorazepam may enhance its metabolism, the half-life of lorazepam may decrease.

Special instructions:

- The drug Laurafen should be used under strict medical supervision.

- If after 7-14 days of use of the drug there is no relief of the symptoms of the disease or a relapse occurs, the patient should consult a doctor.

- Regular use of benzodiazepines or preparations of similar action,including lorazepam for several weeks, may lead to a decrease in their effectiveness as a result of the development of tolerance.

- The use of benzodiazepines or drugs of this type may lead to the development of mental and physical drug dependence. The risk of developing drug dependence increases along with the dose and duration of treatment and increases in patients with alcohol dependence, drug dependence, and also in patients with addiction to other medicines.

In the case of drug dependence, a sharp discontinuation of the drug may lead to the emergence of an abstinence syndrome.Characteristic manifestations of the withdrawal syndrome are: headache, increased irritability, muscle pain, psychomotor agitation and emotional stress, motor anxiety, confusion and disorientation, sleep disturbance. In severe cases, there may be: loss of a sense of reality surrounding (derealization), personality disorder (depersonalization), increased sensitivity to touch (tactile hyperstasy),increased sensitivity to auditory and visual stimuli (acoustic and light hypersthenia), a sense of "crawling crawling" and numbness of the limbs, hallucinations or seizures. Especially dangerous may be a sharp cessation of treatment conducted for a long time, during which lorazepam was used in doses exceeding the average. The manifestations of the withdrawal syndrome are then more pronounced.

There is evidence that in the case of short-acting benzodiazepines and benzodiazepine-like drugs, symptoms of withdrawal symptoms can be observed even in the intervals between taking single doses. especially if the drug is used in large doses.

- After the end of treatment, there may come a temporary relapse of symptoms to a more pronounced extent than those that were the cause of the initial treatment (so-called insomnia as "ricochet"). These symptoms are often accompanied by mood changes, fear, anxiety, increased motor activity. The patient should be informed of the possibility of insomnia as a "ricochet", which will reduce his anxiety if such symptoms appear after discontinuing drug treatment.

The likelihood of developing an abstinence syndrome or the appearance of insomnia such as "ricochet" increases with a sharp discontinuation of the drug. It is recommended to gradually reduce the dose of the drug in order to minimize the risk of such symptoms.

- Lorazepam, like benzodiazepines and preparations of similar action, can cause antegrade amnesia. This condition is most often observed a few hours after taking the drug, especially in a large dose. In order to minimize the risk of developing amnesia, the use of lorazepam is recommended half an hour before bedtime and providing conditions for a continuous 7-8 hour sleep.

- Lorazepam, like benzodiazepines and preparations of similar action, can cause paradoxical reactions, such as psychomotor agitation, increased irritability, aggressiveness, nightmares, hallucinations, psychoses, somnambulism, depersonalization disorders expressed by sleep disturbances and other behavioral side effects. These reactions are much more common in elderly patients.

If such symptoms appear, stop Lorafen immediately.

- The drug Laurafen should be used with great care in elderly patients (over 65 years of age), due to the growth of unwanted phenomena in this age group, mainly by disrupting the orientation and coordination of movements, which can lead to loss of balance.

- Lorazepam should be used with caution in patients with chronic respiratory failure, since it has been established that benzodiazepines exert a depressant effect on the respiratory center.

- Lorazepam should be used with great caution in patients with symptoms of depression. Suicidal thoughts may appear in these patients. In connection with the possibility of deliberate overdose, these patients should prescribe the drug Laurafen in the smallest possible doses. Also, benzodiazepines and preparations of similar action should not be used as a single drug for the treatment of depression or anxiety associated with depression. Monotherapy with these drugs can increase suicidal tendencies.

- Benzodiazepines and preparations of similar action should be used with great care in patients with alcohol, drug or drug dependence in history.These patients should be under strict medical supervision when taking lorazepam; are at risk of developing addiction, mental and physical dependence.

- The drug Laurafen should be used with caution in patients with an uncomfortable form of porphyria. The use of the drug may lead to an increase in the symptoms of this disease.

- During prolonged therapy with Laurafen, periodic blood tests (morphological analysis with smear) and urinalysis are shown.

- During treatment with Laurafen and 3 days after its completion, you should not drink any alcoholic beverages.

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

During treatment with Laurafen and within 3 days after it is completed, you can not drive vehicles and engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:Coated tablets, 1 mg; 2.5 mg.
Packaging:

For 25 tablets in a blister of aluminum foil and orange PVC film. One blister along with instruction on the use of the drug in a cardboard pack, equipped with stickers of control of the first autopsy.

Storage conditions:

The drug belongs to the list of psychotropic substances (list III).

Keep in dry the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription
Registration number:П N016057 / 01
Date of registration:16.10.2009 / 12.08.2010
Expiration Date:Unlimited
The owner of the registration certificate:Tarkhominsky pharmaceutical factory "Polfa", A.O.Tarkhominsky pharmaceutical factory "Polfa", A.O. Poland
Manufacturer: & nbsp
Representation: & nbspFARMEXPERT LLCFARMEXPERT LLCRussia
Information update date: & nbsp19.03.2018
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