Ativan the drug benzodiazepine; used to reduce moderate to severe anxiety and tension, as well as to treat insomnia.
Other names: Lorazepam
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One 1.0 mg/2.5 mg film-coated tablet contains:
Active ingredient: lorazepam - 1,000/2,500 mg.
Excipients: lactose monohydrate - 55.800 / 54.300 mg, microcrystalline cellulose - 20.000 / 20.000 mg, potassium polacrilin - 2.400 / 2.400 mg, magnesium stearate - 0.800 / 0.800 mg.
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 the hypothalamus, i.e. on the structures associated with the regulation of emotional activity. Like all benzodiazepines, it enhances the inhibitory effect of GABAergic neurons in the cerebral cortex, hypocampus, cerebellum, thalamus, and hypothalamus. The existence of benzodiazepine-specific binding sites has been established, which are protein structures of the cell membrane that are associated with a complex consisting of a GABA-A receptor and a chloride channel. The action of lorazepam is to modulate the "sensitivity" of the GABAergic 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 flow of chloride ions into the neuron through the chloride channel. This leads to hyperpolarization of the cell membrane, resulting in inhibition of neuron activity. Clinically, lorazepam has an anxiolytic and hypnotic effect. It also has an anticonvulsant and central muscle relaxant effect.
Suction: Lorazepam is well absorbed from the digestive tract, bioavailability is about 90%. The maximum concentration in the blood (TCmax) reaches approximately 2 hours later. After oral administration of 2 mg of lorazepam, the maximum concentration in the blood (Cmax) is 20 ng / ml (therapeutic concentration range - 15-25 ng / ml).
Distribution: Lorazepam is 85% bound to blood proteins. Passes through the blood-brain and placental barriers. Penetrates into mother's milk.
Metabolism: The process of biotransformation of lorazepam takes place in the liver. Lorazepam forms five metabolites, of which only the main binds to glucuronic acid. As a result of conjugation, an inactive metabolite, lorazepam glucuronate, is formed. The biological half-life of lorazepam is about 12 hours. breeding
Lorazepam is excreted in the urine as lorazepam glucuronate. T1 / 2 lorazepam - 10-20 hours, its conjugate with glucuronic acid - 18 hours. Accumulation upon re-appointment is minimal (applies to benzodiazepines with a short T1 / 2), excretion after discontinuation of treatment is rapid. In elderly patients, the pharmacokinetics of lorazepam does not change.
Read carefully about contraindications before you decice to buy ativan online! Consult your doctor before!
Liver and / or renal failure of mild and moderate severity, chronic respiratory failure, porphyria, depression, history of suicidal thoughts and attempts, history of drug, drug or alcohol addiction, cerebral and spinal ataxias, hyperkinesis, organic brain diseases, hypoproteinemia, elderly age.
If you have one of the listed diseases, be sure to consult your doctor before taking the drug.
The drug must 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 old
In case of neurotic and neurosis-like conditions, it is usually first prescribed 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 a maintenance dose, which most often ranges from 2 mg to 6 mg per day, divided into 1-3 doses.
For the relief of anxiety symptoms, it is recommended to use the smallest possible effective doses.
The dose of lorazepam should be increased gradually, starting with an increase in the dose taken in the evening. A maximum of 10 mg per day can be prescribed.
For sleep disorders caused by anxiety, 2 to 5 mg of lorazepam is usually prescribed once a day before bedtime.
For premedication, 2 to 5 mg is prescribed the night before the planned procedure or surgical intervention, and on the day of the procedure, from 2 to 5 mg 1-2 hours before the procedure or surgical intervention.
Children under 12
The use of lorazepam in children is not recommended due to the lack of data on the safety and efficacy of lorazepam in children under 12 years of age.
Patients with mild to moderate hepatic and/or renal insufficiency.
Care must be taken when prescribing lorazepam to patients with mild to moderate hepatic and/or renal impairment. The dose is selected individually, depending on the degree of hepatic and / or renal insufficiency.
Elderly patients. Elderly patients are more sensitive to drugs that act on the central nervous system. When using lorazepam in these patients, it is recommended to prescribe the lowest possible effective dose. It is usually sufficient to use half the dose prescribed for adults. In the symptomatic treatment of anxiety disorders, the duration of treatment should be limited to a minimum - usually from a few days to a few weeks. In individual cases, treatment can be extended. The maximum duration of treatment, including the period of gradual withdrawal, should not exceed 4 weeks. The gradual withdrawal of the drug must be set individually for each patient. In individual cases, after assessing the patient's condition, the doctor may decide to extend the maximum duration of drug therapy.
Read carefully about all side effects before you order ativan online! Consult your doctor before!
From the nervous system (especially in elderly patients): often: drowsiness, fatigue, dizziness, decreased ability to concentrate, ataxia (unstability of gait and poor coordination of movements leading to loss of balance), disorientation, lethargy, muscle atony, dulling of emotions, slowing down of mental and motor reactions; infrequently - headache, euphoria, depression, tremor, depressed mood, catalepsy, amnesia, confusion, dystonic extrapyramidal reactions (uncontrolled body movements, including the eyes), myasthenia gravis during the day, dysarthria; very rarely - paradoxical reactions (aggressive outbursts, fear, suicidal tendencies, muscle spasm, confusion, hallucinations, acute agitation, irritability, anxiety, insomnia).
From the senses: infrequently - visual impairment (diplopia).
On the part of the hematopoietic organs: infrequently - leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, excessive fatigue, or weakness), anemia, thrombocytopenia.
From the digestive system: often: dryness of the oral mucosa or salivation; infrequently - heartburn, nausea and / or vomiting, loss of appetite, constipation or diarrhea; abnormal liver function, increased activity of "liver" transaminases, lactate dehydrogenase and alkaline phosphatase, jaundice.
From the genitourinary system: rarely - urinary incontinence, urinary retention, impaired renal function, impaired or decreased libido, dysmenorrhea.
Allergic reactions: skin rash (including erythematosis, urticaria), skin itching; very rarely - anaphylactic reactions.
Effect on the fetus: teratogenicity, respiratory failure and suppression of the 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; very rarely - angioedema, inadequate secretion of antidiuretic hormone.
Overdose symptoms: Drowsiness, a state of disorientation, slurred speech, and in severe cases, loss of consciousness, coma. Life-threatening poisoning can be caused by the simultaneous use of lorazepam and alcohol or lorazepam and other drugs that have a depressant effect on the central nervous system.
Treatment: In case of an overdose of lorazepam, it is necessary to take measures aimed at the speedy elimination of the drug that has not yet been absorbed from the body or a decrease in its absorption from the digestive tract (provoking vomiting, taking activated charcoal, gastric lavage - subject to preserved consciousness), monitoring basic vital functions ( respiration, pulse, blood pressure) and, if necessary, apply appropriate symptomatic treatment. The specific antidote is flumazenil.
The inhibitory effect of lorazepam on the central nervous system is enhanced by opioid analgesics, drugs for general anesthesia (anesthetics), psychotropic drugs, antidepressants, antihistamines, antihypertensive drugs of central action.
The use of alcohol during treatment with lorazepam enhances 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 increase the sedative effect of lorazepam, up to coma.
Lorazepam, taken together with other drugs that have a muscle relaxant effect, prolongs and enhances the effect of the latter.
Theophylline and caffeine can weaken the hypnotic effect of benzodiazepines, incl. lorazepam, because have a stimulating effect on the central nervous system and are able to induce hepatic enzymes responsible for the metabolism of drugs. This effect, caused by theophylline and caffeine, may not be present in smokers.
Lorazepam 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, then the patient should consult a doctor.
Regular use of benzodiazepines or drugs of similar action, incl. lorazepam, within a few weeks can lead to a decrease in the effectiveness of their action as a result of the development of tolerance.
The use of lorazepam can lead to the development of mental and physical drug dependence. The risk of developing drug dependence increases with the dose and duration of treatment and increases in patients with alcohol dependence, with drug dependence, as well as in patients with dependence on other drugs.
In the event of the development of drug dependence, abrupt cessation of the use of lorazepam can lead to the appearance of an abstinence syndrome.
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