Ativan (Lorazepam). Dosage, Side Effects, Interactions
Lorazepam is one of the so-called medium-acting benzodiazepines . It has a calming effect, relieves anxiety and tension and promotes sleep. It is therefore used, among other things, for symptomatic short-term treatment. Due to its long duration of action, the active ingredient is particularly suitable for sleep disorders. However, it can also be used to treat anxiety disorders, especially panic attacks. In contrast to antipsychotics and antidepressants , it is also anticonvulsant and is used in status epilepticus. Lorazepam is also used as a muscle relaxant and for nausea and vomiting.
Before and after diagnostic and surgical procedures, lorazepam can act as a tranquilizer and anxiolytic to calm or induce anesthesia.
How Ativan Lorazepam works
Lorazepam is a benzodiazepine agonist. Like most benzodiazepines, its targets are GABA (gamma-aminobutyric acid) receptors in the central nervous system. There it binds to a specific modulatory site on the receptor. As a result, the inhibitory effect of the neurotransmitter GABA is increased.
At the same time, chloride ion channels in the cell membrane open. The cell membrane hyperpolarizes, the transmission of signals in the nerves decreases and with it the excitation of the nerves. Depending on the dosage, the effect on the central nervous system changes. In low doses, lorazepam is primarily sedative and anxiolytic. Increasing the dose also creates a muscle-relaxing effect. If the dose is increased even further, lorazepam has a sleep-inducing to sleep-enforcing effect. In very high doses, lorazepam can be used intravenously to interrupt status epilepticus.
Lorazepam is well absorbed when given orally and has a high bioavailability of 90%. When administered intramuscularly, it is completely and rapidly absorbed. The maximum plasma concentration is reached after about three hours after oral or intramuscular administration. Most of the active ingredient is bound to plasma proteins. The plasma half-life is 11 to 18 hours.
In the liver, the active substance is conjugated with glucuronic acid. The resulting inactive metabolite is excreted primarily via the kidneys. A small part can also be eliminated via the chair.
Lorazepam is usually administered orally as a tablet, but can also be injected intramuscularly or intravenously. It is available in tablet form of 0.5 mg, 1 mg and 2 mg, and as a solution for injection of 2 mg or 4 mg.
The dosage depends on the reason for treatment and the severity of the disease. The dose should be as low as possible and the treatment should be as short as possible. The daily dose in tablet form is usually 0.5 mg to 2.5 mg lorazepam. It can be given as a single evening dose or divided into two to three single doses. In individual cases, the daily dose can be increased to a maximum of 7.5 mg. However, all precautions should be carefully observed. In the meantime, patients with acute psychiatric symptoms can be treated briefly in a hospital setting via intravenous or intramuscular injections of 0.05 mg per kilogram of body weight. However, the preferred dosage form should be tablets.
If sedation is required before or after diagnostic or surgical interventions with lorazepam, 1 mg to 2.5 mg of the active substance should be given on the evening before the intervention and/or, if necessary, 2 mg to 4 mg one to two hours before the intervention. If the administration is intravenous, a guide value of 0.044 mg per kilogram of body weight is set 15 to 20 minutes before the procedure. Here, too, a maximum dose of 4 mg applies. It is administered intramuscularly at least two hours before the operation and should be calculated at 0.05 mg per kilogram of body weight.
In children, the single dose is 0.5 mg to 1 mg, but should not exceed a maximum dose of 0.05 mg per kilogram of body weight, regardless of the reason for treatment.
Elderly and debilitated patients
The total daily dose must be halved in elderly or debilitated patients, and even further in patients with mild, moderate or severe hepatic or renal insufficiency. This is particularly true for intravenous administration.
Side effects of Ativan
Lorazepam side effects are listed below in order of frequency.
- Movement and gait insecurity (ataxia)
- Depression or the emergence of an existing depression
- Muscle weakness
- Changes in sex desire
- Decreased orgasm
If lorazepam is given at the same time as other medications, the effect or side effects may be increased. This is especially true for opioids . Simultaneous administration can lead to increased drowsiness, impaired breathing and coma and even death.
Benzodiazepines can also increase side effects and increase the risk of suicide.
Furthermore, interactions for the following drugs and substances are known:
- Psychotropic drugs
- Sleeping pills, sedatives and anesthetics
- Beta blockers
- Muscle relaxants
- Valproic acid => increased concentration of lorazepam in the blood; Reduction of lorazepam necessary
- Probenecid => faster onset of action and prolonged effect
- Theophylline and aminophylline => weakened effect of lorazepam
Lorazepam must not be administered in the following conditions:
- Known allergies to lorazepam or other benzodiazepines and other components of the dosage form
- existing or past addiction
- Children and young people under the age of 18 (only in urgently needed situations)
In many cases, Ativan lorazepam should only be given after consultation with the doctor treating you, after a risk-benefit assessment and caution:
- Myasthenia gravis
- spinal and cerebellar ataxias
- Acute intoxication with alcohol or central depressant drugs
- respiratory dysfunction
- sleep apnea syndrome
- chronic obstructive pulmonary disease
- Kidney or liver dysfunction
- heart failure
- Lorazepam should not be taken during pregnancy or breastfeeding.
- If lorazepam must be given during breast-feeding, medical supervision of the infant is recommended.
Because lorazepam affects the ability to react, do not drive or operate machinery during the first few days of treatment. Participation in road traffic is also not possible.
- Lorazepam therapy carries a high risk of developing addiction.
- At the beginning of the treatment, the patient should be checked regularly in order to notice as early as possible if overdoses occur.
- If lorazepam is used to promote sleep, sufficient sleep time, around seven to eight hours, should be scheduled.
- Paradoxical reactions with lorazepam occur particularly in children and the elderly.
Further information can be found in the respective technical information.
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