Lorazepam belongs to a group of drugs called benzodiazepines. It affects chemicals in the brain that may be unbalanced in people with anxiety. Lorazepam is used to treat anxiety disorders and seizure disorders. Lorazepam is a short-acting and rapidly cleared benzodiazepine used commonly as a sedative and anxiolytic.
It was developed by DJ Richards, presented and marketed initially by Wyeth Pharmaceuticals in the USA in 1977. The first historic FDA label approval is reported in 1985 by
the company Mutual Pharm
Lorazepam is FDA-approved for the short-term relief of anxiety symptoms related to anxiety disorders and anxiety associated with depressive symptoms such as anxiety-associated insomnia.
It is as well used as an anesthesia premedication in adults to relieve anxiety or to produce sedation/amnesia and for the treatment of status epilepticus.
Some off-label indications of lorazepam include rapid tranquilization of an agitated patient, alcohol withdrawal delirium, alcohol withdrawal syndrome, muscle spasms, insomnia, panic disorder, delirium, chemotherapy-associated anticipatory nausea and vomiting, and psychogenic
The effect of lorazepam in GABA-A receptors produces an increase in the frequency of opening of the chloride ion channel. However, for its effect to generate, the neurotransmitter is
The anticonvulsant properties of lorazepam are thought to be related to the binding to voltage-dependent sodium channels in which the sustained repetitive firing gets limited by the slow recovery of sodium channels due to the benzodiazepine effect.
The effect of lorazepam seems to be very compartmental which was observed with a different generation of sleepiness and a dizziness effect.
Mechanism of action
Lorazepam allosterically binds on the benzodiazepine receptors in the post-synaptic GABA-A ligand-gated chloride channel in different sites of the central nervous system (CNS).
This binding will result in an increase on the GABA inhibitory effects which is translated as an increase in the flow of chloride ions into the cell causing hyperpolarization and stabilization of the cellular plasma membrane.
According to the binding site of lorazepam, we can observe different activities as the binding in the amygdala is known to help mainly in anxiety disorders while the binding in the cerebral cortex helps in seizure disorders
How to use Lorazepam
Read the Medication Guide provided by your pharmacist before you start taking lorazepam and each time you get a refill. If you have any questions, ask your doctor or pharmacist.
The dosage is based on your medical condition, age, and response to treatment.
If directed by your doctor, use this medication regularly in order to get the most benefit from it. To help you remember, use it at the same time(s) each day.
This medication may cause withdrawal reactions, especially if it has been used regularly for a long time or in high doses (more than 1-4 weeks) or if you have a history of alcoholism, drug abuse, or personality disorder. Withdrawal symptoms (such as seizures, trouble sleeping, mental/mood changes, nausea, vomiting, diarrhea, loss of appetite, stomach pain, hallucinations, numbness/tingling of arms and legs, muscle pain, fast heartbeat, short-term memory loss, very high fever, and increased reactions to noise/touch/light) may occur if you suddenly stop using this medication.
To prevent withdrawal reactions, your doctor may reduce your dose gradually. Report any withdrawal reactions right away.
Though it helps many people, this medication may sometimes cause addiction. This risk may be higher if you have a substance use disorder (such as overuse of or addiction to drugs/alcohol). Take this medication exactly as prescribed to lower the risk of addiction. Ask your doctor or pharmacist for more details.
Do not suddenly stop using this drug without consulting your doctor. Some conditions may become worse when this drug is abruptly stopped. Your dose may need to be gradually decreased.
When this medication is used for a long time, it may not work as well. Talk with your doctor if this medication stops working well. Tell your doctor if your condition persists or worsens.
You should not use lorazepam if you have narrow-angle glaucoma, severe respiratory insufficiency, myasthenia gravis, or if you are allergic to Valium or a similar medicine.
Do not use lorazepam if you are pregnant. This medicine can cause birth defects or life-threatening withdrawal symptoms in a newborn.
Lorazepam may be habit-forming and should be used only by the person it was prescribed for. Misuse of habit-forming medicine can cause addiction, overdose, or death.
Lorazepam should never be shared with another person, especially someone who has a history of drug abuse or addiction. Keep the medication in a secure place where others cannot get to it.
Do not drink alcohol while taking lorazepam. This medication can increase the effects of alcohol.
Drowsiness, dizziness, loss of coordination, headache, nausea, blurred vision, change in sexual
interest/ability, constipation, heartburn, or change in appetite may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.
Tell your doctor right away if you have any unlikely but serious side effects, including: mental/mood changes (such as hallucinations, depression, thoughts of suicide), slurred speech or difficulty talking, vision changes, unusual weakness, trouble walking, memory problems, signs of infection (such as fever, persistent sore throat).
Get medical help right away if you have any rare but very serious side effects, including: yellowing eyes or skin, seizures, slow/shallow breathing.
A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.
Taking this medicine with other drugs that make you sleepy or slow your breathing can cause dangerous side effects or death.
Ask your doctor before taking lorazepam with a sleeping pill, narcotic pain medicine, prescription cough medicine, a muscle relaxer, or medicine for anxiety, depression or seizures.
Tell your doctor about all your current medicines and any you start or stop using, especially:
- any other medicines to treat anxiety;
- aminophylline or theophylline;
- an antidepressant, or medicine to treat mental illness;
- a barbiturate such as phenobarbital;
- narcotic pain medicine;
- seizure medicine; or
- Medicine that contains an antihistamine (such as sleep medicine, cold or allergy medicine).