What is ATIVAN/LORAZEPAM?

• Ativan is in a class of drugs called benzodiazepines. Ativan affects chemicals in the brain that may become unbalanced and cause anxiety, insomnia, and seizures.
• Ativan is used to relieve anxiety, nervousness, and tension associated with anxiety disorders. It is also used to treat certain types of seizure disorders and to relieve insomnia (induce sleep)
• Ativan may also be used for purposes other than those listed in this medication guide.

LORAZEPAM (Ativan®) is a benzodiazepine. Benzodiazepines belong to a group of medicines that slow down the central nervous system. Lorazepam relieves anxiety and nervousness. Federal law prohibits the transfer of lorazepam to any person other than the patient for whom it was prescribed. Do not share this medicine with anyone else. Generic lorazepam tablets are available.

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DRUG CLASS AND MECHANISM

Lorazepam is an antianxiety medication in the benzodiazepine family, the same family that includes diazepam (Valium), alprazolam (Xanax), clonazepam (Klonopin), flurazepam (Dalmane), and others.

Lorazepam and other benzodiazepines act by enhancing the effects of gamma-aminobutyric acid (GABA) in the brain. GABA is a neurotransmitter, a chemical that nerves in the brain use to send messages to one another. GABA inhibits activity in many of the nerves of the brain, and it is thought that this excessive activity is what causes anxiety or other psychological disorders.

Because lorazepam is removed from the blood more rapidly than many other benzodiazepines, there is less chance that lorazepam concentrations in blood will reach high levels and become toxic. Lorazepam has fewer interactions with other medications than most of the other benzodiazepines.

PRESCRIBED FOR

Lorazepam is used for the management of anxiety disorders, the short-term relief of the symptoms of anxiety or anxiety associated with depression. The effectiveness of lorazepam, or other benzodiazepines , have not been adequately studied for treatment beyond 4 months.

Lorazepam also has been shown to be effective for improving sleep in people with insomnia, for panic attacks, and as an adjunct (i.e., when added to other medications) to prevent nausea and vomiting in patients receiving cancer chemotherapy.

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Pharmacology

Studies in healthy volunteers wshow that in single high doses lorazepam has a tranquilizing action on the central nervous system with no appreciable effect on the respiratory or cardiovascular systems.

Lorazepam is readily absorbed with an absolute bioavailability of 90 percent. Peak concentrations in plasma occur approximately 2 hours following administration. The peak plasma level of lorazepam from a 2 mg dose is approximately 20 ng/ml.

The mean half-life of unconjugated lorazepam in human plasma is about 12 hours and for its major metabolite, lorazepam glucuronide, about 18 hours. At clinically relevant concentrations, lorazepam is approximately 85% bound to plasma proteins.

Lorazepam is rapidly conjugated at its 3-hydroxy group into lorazepam glucuronide which is then excreted in the urine. Lorazepam glucuronide has no demonstrable CNS activity in animals.

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Contraindications

Unfortunately, with long-term daily use, tolerance to Lorazepam may develop, and larger doses may be needed to achieve the same beneficial effects.

This appears to be common with all benzodiazepines, and is due to the fact that compensatory changes occur in the brain’s GABA and benzodiazepine receptors, so that the inhibitory actions of GABA and benzodiazepines are decreased. As a result, GABA receptors in the brain may reduce in numbers and GABA function may decrease.

Because of this action, suddenly discontinuing the use of a medication like Lorazepam may leave the brain in a state of GABA-underactivity, resulting in hyperexcitability of the nervous system.

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