he drug represents the category of tranquilizers, it’s parent component is benzodiazepine. Ativan (Lorazepam) is based on lorazepam active substance, added to the list of FDA-approved components in 1980. The drug provides anxiolytic, sedative and hypnotic actions. Ativan’s anticonvulsant, muscle relaxation and antiemetic properties have also been confirmed in clinical practice. The mechanisms of the medication’s functioning lie in an increase of GABA inhibition in the CNS. The anticonvulsant capabilities are explained by an increase in presynaptic inhibition. The preparation suppresses the spreading of epileptogenic activity occurring in the cortex of epileptogenic foci. The muscle relaxing action is provided by spinal polysynaptic afferent pathways suppression, apparently, through inhibiting monosynaptic afferent pathways; plus it is suggested that there could be a direct inhibitory effect on motor nerves and muscles function.
Indications for use
As for the mode of action, Ativan represents a tranquilizer from the group of benzodiazepines. It has a pronounced anxiolytic activity, coupled with a mild antidepressant effect; it has a proven efficiency as for eliminating the fear and anxiety, plus it provides an anti-spasmodic and mild sedative action. The medication has a clinically insignificant effect on the cardiovascular and respiratory systems. The drug is well absorbed from the gastrointestinal tract into the bloodstream, reaching a maximum concentration in plasma within up to 2.5 hours.
The medication is prescribed to treat anxiety (including the types where it is associated with depression), sleep disorders caused by short-term anxiety attacks or stressful events. Ativan is appointed to deal with prolonged panic disorders and excitement in such complicated conditions as schizophrenia and epilepsy. Ativan may be included as premedication to accelerate anesthesia; it is also used in psychosomatic disorders therapy.
Dosage and administration
You should consult your treating doctor to have a proper dose carefully selected. However, on average adults are prescribed 0.5 – 4mg of Ativan divided into up to 3 intakes. In the event of significant conditions, the drug may be administered intravenously or intramuscularly at a dose of 50 mcg per kilo of weight; injection rate is selected taking into account the clinical picture and individual characteristics of the patient. The maximum daily dose must not exceed 10mg in case of oral administration; in intramuscular/intravenous administration – 4mg.
Dosage and administration
The therapy in the elderly typically implies the following doses: the initial one doesn’t exceed 0.25 up to 3 times daily; in the event of good tolerability and clinical necessity, it can be gradually increased up to 0.75mg daily. The cessation of the therapy or reduction in the dosage should also be gradual, by 0.5mg within the minimum of 3 days; in significant conditions you may need to cancel the treatment at even more slower pace. The duration of continuous application should not exceed three months, to exclude the risks associated with dependence.
The medication must not be taken in case of myasthenia gravis, angle-closure glaucoma and serious intoxications caused by psychotropic drugs; the treatment in case of hypersensitivity to the active ingredient should be abandoned. Lorazepam and metabolites are found in milk during the therapy, and it should be taken into account that in infants the substance is metabolized slower, so accumulation of the substance in the child’s body can take place; according to FDA, there’s positive evidence of risk in lactating and pregnant women, so the preparation should be taken with extreme caution, especially during the first semester.
The drug may produce effects influencing an ability to drive vehicles and management mechanisms. The patients on lorazepam therapy should minimize or exclude activities requiring an increased attention and/or psychomotor speed reactions. Lorazepam in the form of tablets is included in the list of vital medications.
Ativan enhances the action of agents that have a depressing effect on the central nervous system. Cimetidine, estrogen oral contraceptives, disulfiram and erythromycin which inhibit oxidative conversion of benzodiazepines affect biotransformation of lorazepam glucuronide binding to a lesser extent. Probenecid was confirmed to interfere with the binding of lorazepam glucuronide, which leads to an increase in its concentration in the plasma; therefore, an increasing therapeutic action may result into an excessive sedation.