What are the potential side effects of Ativan IV? Discover the common, mild, and serious side effects, as well as how to manage them. Get answers to your questions about Ativan’s risks and safety.

Understanding Ativan IV: Uses and Approvals

Ativan (lorazepam) is a prescription medication approved by the Food and Drug Administration (FDA) for specific uses. The FDA has approved Ativan tablets to treat anxiety disorders and anxiety related to depression in adults and children aged 13 years and older. Ativan injection is approved to treat status epilepticus (a prolonged seizure) and to assist with anesthesia in adults.

Common Side Effects of Ativan IV

Like other drugs, Ativan can cause side effects, some of which are more common than others. These side effects may be temporary, lasting a few days to weeks. However, if the side effects persist, bother you, or become severe, it’s important to consult your doctor or pharmacist. Some of the more common side effects reported in clinical trials of Ativan tablets and injection include:

• Weakness
• Dizziness
• Sleepiness
• Unsteadiness
• Lower blood pressure

Mild Side Effects of Ativan IV

Ativan treatment can also cause mild side effects. This list is not exhaustive, and you should refer to the prescribing information for Ativan tablets and injection for a more comprehensive list. Mild side effects that have been reported with Ativan include:

• Headache
• Memory loss
• Sexual side effects, such as problems with libido (sexual desire) and achieving orgasm
• Feeling restless
• Weakness
• Dizziness
• Sleepiness
• Depression
• Confusion
• Fatigue
• Hair loss
• Injection site reactions with Ativan injection, including pain, burning, and redness or discoloration
• Digestive symptoms, such as nausea, appetite changes, and constipation
• Mild allergic reaction

Serious Side Effects of Ativan IV

Ativan may also cause serious side effects. If you develop serious side effects while taking Ativan, it’s crucial to call your doctor right away. If the side effects seem life-threatening or you think you’re having a medical emergency, immediately call 911 or your local emergency number. Serious side effects that have been reported include:

• Unsteadiness
• Double vision or blurry vision
• Slurred speech or speech that is difficult to understand
• Coma
• Low body temperature
• Changes in results of certain lab tests, such as low blood sodium (salt) level, low platelet count, low blood cell count, increased liver enzymes, and increased alkaline phosphatase levels
• Breathing problems, including breathing slower than usual and, in rare cases, respiratory failure
• Jaundice and increased bilirubin levels, which can cause yellowing of the skin or whites of the eyes and abdominal pain
• Thoughts about suicide or suicide attempts
• Paradoxical reaction to Ativan, which can include symptoms like anxiety, agitation, feelings of rage or hostility, aggression, insomnia, sexual arousal, and hallucinations
• Risk of dependence and withdrawal
• Life-threatening side effects when Ativan is taken with opioid medications
• Low blood pressure
• Seizures
• Severe allergic reaction
• Risk of misuse and addiction

Side Effect Specifics: Understand the Risks

Some of the serious side effects of Ativan require more detailed explanation. Let’s take a closer look at a few of them:

Respiratory Depression

Ativan can cause breathing problems, including breathing slower than usual and, in rare cases, respiratory failure. This is a serious side effect that requires immediate medical attention.

Paradoxical Reactions

A paradoxical reaction to Ativan is the opposite effect of what is expected with the drug. Symptoms can include anxiety, agitation, feelings of rage or hostility, aggression, insomnia, sexual arousal, and hallucinations.

Dependence and Withdrawal

Ativan carries a risk of dependence and withdrawal symptoms. It’s important to follow your doctor’s instructions carefully and not suddenly stop taking the medication, as this can lead to severe withdrawal symptoms.

Interactions with Opioids

Taking Ativan with opioid medications can result in life-threatening side effects. These two classes of drugs should not be used together without close medical supervision.

Mitigating the Risks: Managing Ativan IV Side Effects

If you experience any side effects while taking Ativan, it’s crucial to inform your doctor. They can help you manage the side effects or consider alternative treatment options if necessary. Remember, the benefits of Ativan must be carefully weighed against the potential risks, and your doctor can guide you in making the best decision for your health.

What they are and what to do about them

Ativan (lorazepam) is a brand-name prescription medication. It comes in two forms, as an oral tablet or injection. The Food and Drug Administration (FDA) has approved:

• Ativan tablets to treat anxiety disorders and anxiety that’s related to depression. For these conditions, Ativan is approved for use in adults and in children ages 13 years and older.
• Ativan injection to treat status epilepticus and to help with anesthesia in adults.

Ativan is typically prescribed as a short-term treatment.

Here are some fast facts about Ativan:

• Active ingredient: lorazepam
• Drug class: benzodiazepines
• Drug forms:
  • oral tablet
  • solution for intravenous or intramuscular injection given by your doctor or another healthcare professional

As with other drugs, Ativan can cause side effects (also known as adverse effects). Read on to learn about potential common, mild, and serious side effects. For a general overview of Ativan, including details about its uses, see this article.

Ativan can cause certain side effects, some of which are more common than others. These side effects may be temporary, lasting a few days to weeks. However, if the side effects last longer than that, bother you, or become severe, be sure to talk with your doctor or pharmacist.

These are just a few of the more common side effects reported in clinical trials of Atvian tablets and Ativan injection:

• weakness
• dizziness
• sleepiness
• unsteadiness
• lower blood pressure*

* For more information about this side effect, see “Side effect specifics” below.

Mild side effects can occur with Ativan treatment. This list doesn’t include all possible mild side effects of the drug. For more information, you can refer to the prescribing information for Ativan tablets and injection.

Mild side effects that have been reported with Ativan include:

• headache
• memory loss
• sexual side effects, including problems with libido (sexual desire) and achieving orgasm
• feeling restless
• weakness
• dizziness
• sleepiness
• depression
• confusion
• fatigue
• hair loss
• injection site reactions with Ativan injection, including pain, burning, and redness or discoloration at the injection site
• digestive symptoms, such as nausea, appetite changes, and constipation*
• mild allergic reaction*†

These side effects may be temporary, lasting a few days to weeks. However, if the side effects last longer than that, bother you, or become severe, be sure to talk with your doctor or pharmacist.

Note: After the Food and Drug Administration (FDA) approves a drug, it tracks side effects of the medication. If you develop a side effect while taking Ativan and want to tell the FDA about it, visit MedWatch.

* For more information about this side effect, see “Side effect specifics” below.
† An allergic reaction is possible after taking Ativan. This side effect occurred in clinical trials of Ativan tablets. It’s not clear if allergic reaction occurred in clinical trials of Ativan injection.

Ativan may cause serious side effects. The list below may not include all possible serious side effects of the drug. For more information, you can refer to the prescribing information for Ativan tablets and injection.

If you develop serious side effects while taking Ativan, call your doctor right away. If the side effects seem life threatening or you think you’re having a medical emergency, immediately call 911 or your local emergency number.

Serious side effects that have been reported include:

• Unsteadiness.
• Double vision or blurry vision.
• Slurred speech or speech that is difficult to understand.
• Coma.
• Low body temperature.
• Changes in results of certain lab tests, which may not cause noticeable symptoms. These include:
  • low blood sodium (salt) level
  • low platelet count
  • low blood cell count
  • increased liver enzymes, which can be a sign of liver damage
  • increased alkaline phosphatase levels
• Breathing problems. Symptoms can include:
  • breathing slower than usual
  • respiratory failure, in rare cases
• Jaundice and increased bilirubin levels. Symptoms can include:
  • yellowing of skin or whites of eyes
  • abdominal pain
• Thoughts about suicide or suicide attempts. Warning signs can include:
  • talking about suicide
  • withdrawing from friends and family
• Paradoxical reaction to Ativan. A paradoxical reaction is the opposite effect of what is expected with a drug. Symptoms can include:
  • anxiety
  • agitation
  • feelings of rage or hostility
  • aggression
  • insomnia
  • sexual arousal
  • hallucinations*
• Risk of dependence and withdrawal. † (For more information, refer to the “Ativan withdrawal symptoms” section below.)
• Life threatening side effects when Ativan is taken with opioid medications.*†
• Low blood pressure.*
• Seizures.*
• Severe allergic reaction.*‡
• Risk of misuse and addiction.† (For more details, see the “Ativan and misuse” section below.)

* To learn more about this side effect, see the “Side effect specifics” section below.
† Ativan tablets and injection have a boxed warning for this side effect. This is a serious warning from the Food and Drug Administration (FDA).
‡ An allergic reaction is possible after taking Ativan. This side effect occurred in clinical trials of Ativan tablets. It’s not clear if allergic reaction occurred in clinical trials of Ativan injection.

Long-term effects of Ativan

Ativan is meant to be a short-term treatment. Long-term Ativan treatment (more than 4 months) was not studied in clinical trials of Ativan tablets. If Ativan is taken long-term, the risks of dependence and withdrawal increase.

If you have questions about how long you’ll take Ativan or what effects it may have, talk with your doctor.

Ativan tablets are approved by the Food and Drug Administration (FDA) to treat anxiety in children 13 years and older.

Children may be more likely than adults to experience paradoxical reactions from Ativan tablets. A paradoxical reaction is an effect that is the opposite of what is expected. (For more information about this side effect, see the “Serious side effects of Ativan” section above.)

If your child is prescribed Ativan and you’re concerned about its side effects, talk with their doctor.

Note: Ativan tablets are not approved for use in children ages 12 years and younger. And Ativan injection is not approved for use in children.

Ativan tablets and Ativan injection have a boxed warning about the risk of dependence and withdrawal. This is a serious warning from the Food and Drug Administration (FDA). Boxed warnings alert doctors and patients about drug effects that may be dangerous. However, this side effect was not common in clinical trials of Ativan tablets or injection.

With dependence, you need a drug in order to function as usual. With withdrawal, you experience certain symptoms when you suddenly stop taking a drug. Your risk of withdrawal may increase if you take Ativan long term. Also, suddenly stopping Ativan or reducing its dosage* can cause withdrawal symptoms.

These symptoms, which can be mild to severe, can include:

• unusual body movements
• muscle pain and stiffness
• anxiety or panic attacks
• blurry vision
• depression
• dizziness
• fatigue
• digestive symptoms, such as nausea, vomiting, and diarrhea
• headache
• sensitivity to light
• high blood pressure or increased heart rate
• memory problems
• insomnia

Severe withdrawal symptoms can include:

• thoughts of suicide or suicidal behaviors
• seizures or convulsions
• depression
• hallucinations
• mania
• psychosis

If they occur, withdrawal symptoms typically last a short time. Rarely, they may last for up to 12 months. If you experience severe withdrawal symptoms, seek emergency medical care.

If you are interested in stopping Ativan treatment, talk with your doctor. Do not stop taking it on your own.

* To learn about Ativan’s dosages, see this article.

Suicide prevention

If you know someone at immediate risk of self-harm, suicide, or hurting another person:

• Ask the tough question: “Are you considering suicide?”
• Listen to the person without judgment.
• Call 911 or the local emergency number, or text TALK to 741741 to communicate with a trained crisis counselor.
• Stay with the person until professional help arrives.
• Try to remove any weapons, medications, or other potentially harmful objects.

If you or someone you know is having thoughts of suicide, a prevention hotline can help. The 988 Suicide and Crisis Lifeline is available 24 hours a day at 988. During a crisis, people who are hard of hearing can use their preferred relay service or dial 711 then 988.

Click here for more links and local resources.

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If you’re age 65 years or older, you may have an increased risk of sleepiness and unsteadiness while taking Ativan. You may also have a higher risk of paradoxical reactions from Ativan. (For more information about this side effect, see the “Serious side effects of Ativan” section above.)

If you’re within this age group and concerned about side effects of Ativan, talk with your doctor.

Ativan may cause several side effects. Here are some frequently asked questions about the drug’s side effects and their answers.

Do 1-mg and 2-mg Ativan tablets have the same side effects as the other forms?

Generally, different strengths* of Ativan tablets can cause similar side effects. However, higher doses of Ativan tablets may cause more severe side effects. But this can vary from person to person.

It’s important to note that not everyone will experience side effects during Ativan treatment. Talk with your doctor if you have concerns about side effects after starting treatment with Ativan.

* To learn about Ativan’s strengths and dosages, see this article.

Is weight gain one of Ativan’s side effects?

No, weight gain is not typically a side effect of Ativan. It wasn’t reported in clinical trials of Ativan tablets or injection.

If you have anxiety and depression, you may experience weight changes due to these conditions.* Or you may experience weight loss if you develop certain side effects of Ativan treatment. These include nausea, loss of appetite, or withdrawal.†

If you’re concerned about weight changes during your Ativan treatment, talk with your doctor.

* Ativan is approved to treat anxiety related to depression. To learn more about this use, see this article.
† Ativan tablets and injection have a boxed warning for this side effect. This is a serious warning from the Food and Drug Administration (FDA). For more information, see the “ Ativan withdrawal symptoms” section above.

Can Ativan cause memory loss?

Yes, Ativan can cause mild memory loss as a side effect. It’s usually temporary and will go away if you stop taking Ativan with your doctor’s recommendation.

Talk with your doctor if you are experiencing memory loss while taking Ativan. They may recommend a different medication for your condition.

Learn more about some of the side effects that Ativan may cause. To find out how often side effects occurred in clinical trials, see the prescribing information for Ativan tablets and injection.

Risk of life threatening effects when taken with opioids

Ativan has a boxed warning about the risk of life threatening effects that can happen when it’s taken with opioid medications. This is a serious warning from the Food and Drug Administration (FDA). Boxed warnings alert doctors and patients about drug effects that may be dangerous. This side effect was not common in clinical trials of Ativan tablets or injection, but it’s important to be aware of it.

Taking Ativan and opioids together can cause the following life threatening effects:

• extreme sedation (drowsiness)
• respiratory depression (slow breathing)
• coma
• death, if the above effects are not immediately treated

What you can do

If you experience any of the above side effects, it’s important to seek medical treatment right away. Call 911 or your local emergency number.

Before starting Ativan treatment, tell your doctor if you take any opioid medications. They will only prescribe Ativan with opioids if there are no other treatment options for your condition.

If your doctor recommends you take Ativan and opioids together, they will likely prescribe a small dose* of Ativan for a short time. Also, they may prescribe naloxone (Narcan). Naloxone is an emergency treatment for respiratory depression due to an opioid overdose. And taking Ativan with opioids can cause side effects similar to an opioid overdose. To learn more about this medication, speak with your doctor or pharmacist.

* To learn about Ativan’s dosages, see this article.

Nausea

Some people have reported nausea as a side effect of Ativan. This side effect was not common in clinical trials of Ativan tablets or injection. And typically, nausea will improve over time during your treatment.

What you can do

To help ease nausea due to Ativan tablets, below are some tips that you can follow:

• take your dose of Ativan with some crackers or toast
• avoid lying down right after taking your dose
• try taking sips of water or small amounts of crushed ice cubes

If your nausea continues or worsens while taking Ativan, talk with your doctor. They may recommend other tips to help ease this side effect.

If you’re receiving an Ativan injection and experience nausea, tell your doctor or another healthcare professional. They can help ease this side effect.

Hallucinations

Rarely, people have experienced hallucinations in clinical trials of Ativan tablets and injection. Hallucinations refer to experiencing things that aren’t real.

What you can do

If you experience hallucinations while taking Ativan, talk with your doctor. They’ll likely recommend a different medication for your condition.

Low blood pressure

Ativan can cause low blood pressure as a serious side effect. However, this side effect was not common in clinical trials of Ativan tablets and injection.

Symptoms of low blood pressure may include:

• dizziness
• unsteadiness
• lightheadedness
• falling down more easily
• fainting

What you can do

If you experience any of the above symptoms during Ativan treatment, let your doctor know. Also, tell your doctor if you take any medications to manage your blood pressure. They may monitor your blood pressure more closely while you are taking Ativan.

Seizures

Ativan can make it more likely for those with seizure disorders to experience a seizure. (With seizures, there’s changes in the electrical activity of your brain). This side effect was rare in clinical trials of Ativan tablets and injection.

Symptoms can include:

• uncontrollable, jerky movements in your arms or legs
• stiff muscles
• loss of consciousness
• staring spells, which may be a sign of an absence seizure (short periods of unconsciousness without movement)

What you can do

If you think you’ve had a seizure, call 911 or your local emergency number. Also, tell your doctor right away if you’ve had a seizure while taking Ativan. They’ll likely recommend a different treatment for your condition.

Allergic reaction

An allergic reaction is possible after taking Ativan. This side effect occurred in clinical trials of Ativan tablets. It’s not clear if an allergic reaction occurred in clinical trials of Ativan injection.

Symptoms can be mild or serious and can include:

• skin rash
• itching
• flushing
• racing heartbeat
• swelling under your skin, typically in your eyelids, lips, hands, or feet
• swelling of your mouth, tongue, or throat, which can make it hard to breathe

What you can do

For mild symptoms of an allergic reaction, call your doctor right away. They may recommend ways to ease your symptoms and determine whether you should keep taking Ativan. However, if your symptoms are serious and you think you’re having a medical emergency, immediately call 911 or your local emergency number.

Ativan carries several boxed warnings, which are the most serious warnings from the Food and Drug Administration (FDA). They alert patients and doctors about drug effects that may be dangerous.

Boxed warnings

This drug has boxed warnings, which are serious warnings from the FDA. Ativan’s boxed warnings are about the following:

• Risk of misuse and addiction. For more information, see the “Ativan and misuse” section below.
• Risk of dependence and withdrawal. To learn more, refer to the “Ativan withdrawal symptoms” section above.
• Risk of life threatening side effects when taken with opioid drugs. For details, see the “Side effect specifics” section above.

Other precautions

Be sure to talk with your doctor about your health history before you take Ativan. This drug may not be the right treatment for you if you have certain medical conditions or other factors that affect your health. These are considered drug-condition or drug-factor interactions. The conditions and factors to consider include:

Breathing problems. Ativan can slow down your breathing. If you have certain conditions such as sleep apnea, chronic obstructive pulmonary disease, or other breathing problems, tell your doctor. They’ll advise if it’s safe for you to take Ativan.

Depression. Ativan is prescribed to treat anxiety related to depression.* However, it can also make depression symptoms worse. If you have depression, let your doctor know. They may recommend treatment for your depression before prescribing Ativan.

Kidney or liver problems. Your kidneys and liver help break down medications in your body. If you have kidney or liver problems, let your doctor know. They may prescribe a lower dosage of Ativan. †

Acute narrow-angle glaucoma. Ativan can make glaucoma worse by increasing the pressure inside the eye. So doctors typically won’t prescribe Ativan if you have acute narrow-angle glaucoma. Be sure to tell your doctor if you have this condition.

Allergic reaction. If you’ve had an allergic reaction‡ to Ativan or any of its ingredients, your doctor will likely not prescribe the drug. Ask your doctor what other medications may be better options for you.

Current treatment with opioid medication. If you currently take opioids, be sure to tell your doctor. Taking opioid drugs with Ativan can cause life threatening side effects

* To learn more about the approved uses of Ativan, see this article.
† For details about Ativan’s dosages, see this article.
‡ Ativan tablets and injection have a boxed warning for this side effect. This is a serious warning from the FDA. For more information about this side effect, see the “ Side effect specifics” section above.

Alcohol with Ativan

You should not drink alcohol with Ativan treatment. Drinking alcohol may increase the risk of serious side effects of the drug, such as:*

• breathing problems, including respiratory depression (slow breathing)
• memory problems
• extreme sleepiness
• coma

Ativan can also lower your tolerance to alcohol. This means you may feel the effects of alcohol more than you usually would after a drink.

If you have questions about drinking alcohol with Ativan, talk with your doctor.

* To learn more about the serious side effects of Ativan, see the “Serious side effects of Ativan” section above.

Pregnancy and breastfeeding while taking Ativan

It’s not safe to take Ativan during pregnancy. Doing so may harm a fetus. Newborns who were exposed to Ativan during the third trimester of pregnancy may experience withdrawal symptoms after birth. (For details about, see the “Ativan withdrawal symptoms” section above. )

Before starting treatment with Ativan, be sure to tell your doctor if you are pregnant or plan to become pregnant. They’ll recommend the best treatment option for you.

If you’re breastfeeding, you should not take Ativan. Doing so may cause side effects in your child. This is because the drug is known to pass into breast milk. Talk with your doctor about ways to safely feed your child while taking Ativan.

Ativan has a boxed warning about the risk of misuse. This is a serious warning from the Food and Drug Administration (FDA). Boxed warnings alert doctors and patients about drug effects that may be dangerous.

Drug misuse is taking a drug in a way or for a use your doctor hasn’t prescribed it for. Misuse of Ativan can lead to addiction or overdose. It can even be life threatening in rare cases.

Signs of misuse can include:

• nausea and vomiting
• sweating
• muscle weakness
• body aches
• nightmares
• depression
• anxiety

The risk of misuse is higher for people who’ve had alcohol or drug use disorder. It’s also higher for people who take high doses of Ativan or take Ativan long-term.

Due to the above risks, it’s important to take Ativan exactly as your doctor prescribes. Taking Ativan with other medications, alcohol, or illegal drugs may increase the risk of harmful outcomes. Tell your doctor about all the medications you take and if you’ve ever had problems with alcohol or drug misuse.

Treatment with Ativan can cause mild and serious side effects. Most side effects aren’t common, but if they do happen, they tend to be mild.

However, Ativan can cause serious side effects in rare cases. Talk with your doctor if you develop side effects that are serious or bothersome. For more information, see “Side effect specifics” above.

If you’d like to learn more about Ativan, talk with your doctor or pharmacist. They can help answer any questions you have about side effects from taking the drug.

Besides talking with your doctor, you can do some research on your own. These articles might help:

• More information about Ativan. For details about other aspects of Ativan, refer to this article.
• Drug comparison. Learn how Ativan compares with Xanax and other drugs, such as Klonopin, Valium, and Ambien.
• Dosage. For information about Ativan’s dosages, view this article.
• Interactions. To learn more about Ativan’s interactions, see this article.
• A look at your condition. Here are some resources to learn more about your condition:
  • For details about anxiety, see our anxiety hub.
  • For information about seizures, check out our epilepsy and seizure hub.

Disclaimer: Medical News Today has made every effort to make certain that all information is factually correct, comprehensive, and up to date. However, this article should not be used as a substitute for the knowledge and expertise of a licensed healthcare professional. You should always consult your doctor or another healthcare professional before taking any medication. The drug information contained herein is subject to change and is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. The absence of warnings or other information for a given drug does not indicate that the drug or drug combination is safe, effective, or appropriate for all patients or all specific uses.

Ativan, Loreev XR (lorazepam) dosing, indications, interactions, adverse effects, and more

Lorazepam – description of the substance, pharmacology, use, contraindications, formula

Contents

• Structural formula

• Russian name

• English name

• Latin name

• chemical name

• Gross formula

• Pharmacological group of the substance Lorazepam

• Nosological classification

• CAS code

• pharmachologic effect

• Characteristic

• Pharmacology

• The use of the substance Lorazepam

• Contraindications

• Application restrictions

• Use during pregnancy and lactation

• Side effects of Lorazepam

• Interaction

• Overdose

• Dosage and administration

• Precautionary measures

• special instructions

• Trade names with the active ingredient Lorazepam

Structural formula

Russian name

Lorazepam

English name

Lorazepam

Latin name

Lorazepamum (born 90 066 Lorazepami)

Chemical name

7-Chloro-5-(2-chlorophenyl)- 1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one

Gross formula

C ₁₅ H ₁₀ Cl ₂ N ₂ O 9 0075 2

Pharmacological substance group Lorazepam

Anxiolytics

Nosological classification

ICD-10 code list

• F10. 3 Withdrawal state

• F10.5 Alcoholic psychosis

• F25 Schizoaffective disorders

• F30 Manic Episode

• F32 Depressive episode

• F34. 1 Dysthymia

• F40.0 Agoraphobia

• F41.0 Panic disorder [episodic paroxysmal anxiety]

• F41.1 Generalized anxiety disorder

• F42 Obsessive-compulsive disorder

• F43. 0 Acute stress reaction

• F43.1 Post-traumatic stress disorder

• F43.2 Adjustment disorder

• F51.0 Insomnia of non-organic etiology

• F60 Specific personality disorders

• F91 Conduct disorders

• G40 Epilepsy

• G44. 2 Tension headache

• G47.0 Disorders of initiation and maintenance of sleep [insomnia]

• R45.0 Nervousness

• R45.1 Restlessness and agitation

• R45. 7 State of emotional shock and stress, unspecified

• Z100* CLASS XXII Surgical practice

CAS code

846-49-1

Pharmacological action

Pharmacological action –

anxiolytic , muscle relaxant , anticonvulsant , sedative , hypnotic , central .

Characteristics

Anxiolytic, benzodiazepine derivative.

Almost white powder, very slightly soluble in water.

Pharmacology

Interacts with specific benzodiazepine receptors of the GABA-benzodiazepine receptor complex, increases the sensitivity of GABA receptors to GABA. As a result, the frequency of opening of transmembrane channels for chloride ions increases, the postsynaptic membrane of the neuron is hyperpolarized, neuronal activity is inhibited, and interneuronal transmission to the CNS is inhibited. The effects are due to the influence on various parts of the central nervous system: the amygdala complex of the limbic system (anxiolytic), the reticular formation of the brain stem and nonspecific nuclei of the thalamus, hypothalamus (sedative and hypnotic), spinal cord (muscle relaxant), hippocampus (anticonvulsant). It reduces the excitability of subcortical formations (limbic system, thalamus, hypothalamus) responsible for the implementation of emotional reactions, and inhibits the interaction of these structures with the cerebral cortex. Stabilizes vegetative functions.

Suppresses anxiety, fear, reduces psychomotor agitation, emotional stress. It has anti-panic and amnestic (mainly for parenteral use) action. It is effective for insomnia caused by anxiety or a short-term stressful situation: it facilitates the onset of sleep (shortens the period of falling asleep), reduces the number of night awakenings, and increases the duration of sleep. It inhibits polysynaptic spinal reflexes and lowers the tone of skeletal muscles.

Lorazepam has low toxicity and a wide range of therapeutic effects.

An animal reproduction study showed that administration of lorazepam at doses of 40 mg/kg orally and 4 mg/kg or more IV to rabbits resulted in fetal resorption and an increased incidence of fetal death. Causes developmental anomalies in rabbits, regardless of dose. In an 18-month study in rats, no carcinogenic activity was found.

Good but slowly absorbed from the gastrointestinal tract when taken orally, bioavailability is 90%. max “> C _max is achieved within 2 hours and is dose dependent: at a dose of 2 mg max”> C _max is 20 ng / ml. About 85% binds to plasma proteins. The equilibrium concentration in the blood is usually reached after 2-3 days. Passes through the BBB and the placental barrier. It is rapidly metabolized in the liver by conjugation to form the main inactive metabolite, lorazepam glucuronide. 1/2 “> T _1/2 unconjugated lorazepam – about 12 hours, the main metabolite – 18 hours. Excreted mainly by the kidneys mainly in the form of glucuronide.

When administered intramuscularly, max “> C _max is achieved in 60-90 minutes. 1/2″> T _1/2 when administered parenterally is 16 hours. When used for 6 months, no cumulation phenomena are observed. The pharmacokinetic parameters of lorazepam do not change in the elderly.

Application of the substance Lorazepam

Neurosis accompanied by anxiety, agitation, incl. generalized anxiety disorder, post-traumatic stress disorder, phobias, obsessive-compulsive disorder, psychoreactive states, emotional reactive disorders, anxiety in depressive states of various origins (usually in combination with antidepressants), insomnia, psychosomatic disorders (including heart – vascular, gastrointestinal and other diseases), premedication before surgical and diagnostic manipulations (in combination with analgesics), tension headache; nausea and vomiting caused by chemotherapy, epilepsy (as part of combination therapy), alcoholic delirium and withdrawal syndrome in chronic alcoholism (as part of combination therapy).

Contraindications

Hypersensitivity, incl. to other benzodiazepines, myasthenia gravis, angle-closure glaucoma, acute intoxication with CNS depressants, respiratory depression, liver failure, pregnancy (especially the first trimester), breast-feeding, age up to 18 years.

Restrictions for use

Chronic respiratory failure, sleep apnea syndrome, open-angle glaucoma, drug and alcohol dependence, depression (see Precautions), psychosis, severe renal dysfunction.

Use during pregnancy and lactation

Contraindicated during pregnancy (especially in the first trimester). At the time of treatment should stop breastfeeding.

Side effects of the substance Lorazepam

From the nervous system and sensory organs: lethargy, fatigue, drowsiness, disorientation, headache, dizziness, depression, ataxia, sleep disturbance, agitation, visual impairment, amnesia episodes.

From the digestive tract: dry mouth, nausea, vomiting, diarrhea, change in appetite.

On the part of the skin: erythema, urticaria.

Others: changes in blood composition (leukopenia), increased LDH activity.

May develop addiction, drug dependence, withdrawal syndrome, rebound syndrome (see “Precautions”).

Interaction

Lorazepam enhances the effect of CNS depressants, incl. phenothiazines, narcotic analgesics, barbiturates, antidepressants, hypnotics, anticonvulsants, antihistamines with a sedative effect. Potentiates the action of general and local anesthetics, enhances the action of curare-like drugs. With simultaneous use with alcohol, in addition to increasing the inhibitory effect on the central nervous system, paradoxical reactions are possible (psychomotor agitation, aggressive behavior, a state of pathological intoxication). Nicotine inhibits the activity of lorazepam (accelerates its metabolism).

Overdose

Symptoms: drowsiness, arterial hypotension, confusion, depression of reflexes, coma.

Treatment: induction of vomiting, gastric lavage, intravenous administration of norepinephrine to increase blood pressure, symptomatic therapy, monitoring of vital functions. The introduction of a specific antidote – an antagonist of benzodiazepine receptors flumazenil (in a hospital setting).

Dosage and administration

Inside. The dosage regimen and the duration of the course of treatment are set strictly individually.

In neurological practice – 1 mg 2-3 times a day; in psychiatric practice – 4-6 mg / day; with insomnia – 1-2 mg 30 minutes before bedtime. In elderly and debilitated patients, the dose should not exceed 2 mg / day (in divided doses). In patients with liver and / or kidney disease, as well as in patients with cerebral sclerosis, hypotension, heart failure, underweight, dose adjustment is recommended.

Precautions

Use with caution in patients with depression, given the tendency to suicide. In patients with drug and alcohol dependence, use under close medical supervision.

Side effects are usually observed at the beginning of therapy. The possibility of a more frequent occurrence of side effects in elderly and debilitated patients should be taken into account.

During treatment and for 2 days after its completion, it is necessary to exclude the intake of alcoholic beverages; drivers of vehicles and people whose work requires a quick mental and physical reaction, and is also associated with increased concentration of attention, should not engage in professional activities during this period.

Long-term use may cause addiction and drug dependence (especially when taking high doses). In this regard, lorazepam should not be used for longer than 4-6 weeks. If long-term treatment is necessary, weekly breaks in taking the drug should be periodically taken. With a sharp cessation of treatment, a withdrawal syndrome may occur (tremor, convulsions, abdominal or muscle cramps, vomiting, perspiration), and symptoms similar to those of the disease (anxiety, agitation, irritability, emotional stress, insomnia, convulsions) may also occur.

With prolonged use, it is necessary to periodically monitor the picture of peripheral blood, liver and kidney function.

Special instructions

Note that anxiety or tension associated with everyday stress does not usually require treatment with anxiolytics.

Trade names with active substance Lorazepam

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All dosages 1 mg 2.5 mg No dosage

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All manufacturers of Cambrex Propharmaco Milan S.r.L. Moscow Endocrine Plant Federal State Unitary Enterprise Tarkhominsk Pharmaceutical Plant Polfa, JSC

Lorazepam – description of the substance, pharmacology, use, contraindications, formula

Contents

• Structural formula

• Russian name

• English name

• Latin name

• chemical name

• Gross formula

• Pharmacological group of the substance Lorazepam

• Nosological classification

• CAS code

• pharmachologic effect

• Characteristic

• Pharmacology

• The use of the substance Lorazepam

• Contraindications

• Application restrictions

• Use during pregnancy and lactation

• Side effects of Lorazepam

• Interaction

• Overdose

• Dosage and administration

• Precautionary measures

• special instructions

• Trade names with the active ingredient Lorazepam

Structural formula

Russian name

Lorazepam

English name

Lorazepam

Latin name

Lorazepamum (born 90 066 Lorazepami)

Chemical name

7-Chloro-5-(2-chlorophenyl)- 1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one

Gross formula

C ₁₅ H ₁₀ Cl ₂ N ₂ O 9 0075 2

Pharmacological substance group Lorazepam

Anxiolytics

Nosological classification

ICD-10 code list

• F10. 3 Withdrawal state

• F10.5 Alcoholic psychosis

• F25 Schizoaffective disorders

• F30 Manic Episode

• F32 Depressive episode

• F34. 1 Dysthymia

• F40.0 Agoraphobia

• F41.0 Panic disorder [episodic paroxysmal anxiety]

• F41.1 Generalized anxiety disorder

• F42 Obsessive-compulsive disorder

• F43. 0 Acute stress reaction

• F43.1 Post-traumatic stress disorder

• F43.2 Adjustment disorder

• F51.0 Insomnia of non-organic etiology

• F60 Specific personality disorders

• F91 Conduct disorders

• G40 Epilepsy

• G44. 2 Tension headache

• G47.0 Disorders of initiation and maintenance of sleep [insomnia]

• R45.0 Nervousness

• R45.1 Restlessness and agitation

• R45. 7 State of emotional shock and stress, unspecified

• Z100* CLASS XXII Surgical practice

CAS code

846-49-1

Pharmacological action

Pharmacological action –

anxiolytic , muscle relaxant , anticonvulsant , sedative , hypnotic , central .

Characteristics

Anxiolytic, benzodiazepine derivative.

Almost white powder, very slightly soluble in water.

Pharmacology

Interacts with specific benzodiazepine receptors of the GABA-benzodiazepine receptor complex, increases the sensitivity of GABA receptors to GABA. As a result, the frequency of opening of transmembrane channels for chloride ions increases, the postsynaptic membrane of the neuron is hyperpolarized, neuronal activity is inhibited, and interneuronal transmission to the CNS is inhibited. The effects are due to the influence on various parts of the central nervous system: the amygdala complex of the limbic system (anxiolytic), the reticular formation of the brain stem and nonspecific nuclei of the thalamus, hypothalamus (sedative and hypnotic), spinal cord (muscle relaxant), hippocampus (anticonvulsant). It reduces the excitability of subcortical formations (limbic system, thalamus, hypothalamus) responsible for the implementation of emotional reactions, and inhibits the interaction of these structures with the cerebral cortex. Stabilizes vegetative functions.

Suppresses anxiety, fear, reduces psychomotor agitation, emotional stress. It has anti-panic and amnestic (mainly for parenteral use) action. It is effective for insomnia caused by anxiety or a short-term stressful situation: it facilitates the onset of sleep (shortens the period of falling asleep), reduces the number of night awakenings, and increases the duration of sleep. It inhibits polysynaptic spinal reflexes and lowers the tone of skeletal muscles.

Lorazepam has low toxicity and a wide range of therapeutic effects.

An animal reproduction study showed that administration of lorazepam at doses of 40 mg/kg orally and 4 mg/kg or more IV to rabbits resulted in fetal resorption and an increased incidence of fetal death. Causes developmental anomalies in rabbits, regardless of dose. In an 18-month study in rats, no carcinogenic activity was found.

Good but slowly absorbed from the gastrointestinal tract when taken orally, bioavailability is 90%. max “> C _max is achieved within 2 hours and is dose dependent: at a dose of 2 mg max”> C _max is 20 ng / ml. About 85% binds to plasma proteins. The equilibrium concentration in the blood is usually reached after 2-3 days. Passes through the BBB and the placental barrier. It is rapidly metabolized in the liver by conjugation to form the main inactive metabolite, lorazepam glucuronide. 1/2 “> T _1/2 unconjugated lorazepam – about 12 hours, the main metabolite – 18 hours. Excreted mainly by the kidneys mainly in the form of glucuronide.

When administered intramuscularly, max “> C _max is achieved in 60-90 minutes. 1/2″> T _1/2 when administered parenterally is 16 hours. When used for 6 months, no cumulation phenomena are observed. The pharmacokinetic parameters of lorazepam do not change in the elderly.

Application of the substance Lorazepam

Neurosis accompanied by anxiety, agitation, incl. generalized anxiety disorder, post-traumatic stress disorder, phobias, obsessive-compulsive disorder, psychoreactive states, emotional reactive disorders, anxiety in depressive states of various origins (usually in combination with antidepressants), insomnia, psychosomatic disorders (including heart – vascular, gastrointestinal and other diseases), premedication before surgical and diagnostic manipulations (in combination with analgesics), tension headache; nausea and vomiting caused by chemotherapy, epilepsy (as part of combination therapy), alcoholic delirium and withdrawal syndrome in chronic alcoholism (as part of combination therapy).

Contraindications

Hypersensitivity, incl. to other benzodiazepines, myasthenia gravis, angle-closure glaucoma, acute intoxication with CNS depressants, respiratory depression, liver failure, pregnancy (especially the first trimester), breast-feeding, age up to 18 years.

Restrictions for use

Chronic respiratory failure, sleep apnea syndrome, open-angle glaucoma, drug and alcohol dependence, depression (see Precautions), psychosis, severe renal dysfunction.

Use during pregnancy and lactation

Contraindicated during pregnancy (especially in the first trimester). At the time of treatment should stop breastfeeding.

Side effects of the substance Lorazepam

From the nervous system and sensory organs: lethargy, fatigue, drowsiness, disorientation, headache, dizziness, depression, ataxia, sleep disturbance, agitation, visual impairment, amnesia episodes.

From the digestive tract: dry mouth, nausea, vomiting, diarrhea, change in appetite.

On the part of the skin: erythema, urticaria.

Others: changes in blood composition (leukopenia), increased LDH activity.

May develop addiction, drug dependence, withdrawal syndrome, rebound syndrome (see “Precautions”).

Interaction

Lorazepam enhances the effect of CNS depressants, incl. phenothiazines, narcotic analgesics, barbiturates, antidepressants, hypnotics, anticonvulsants, antihistamines with a sedative effect. Potentiates the action of general and local anesthetics, enhances the action of curare-like drugs. With simultaneous use with alcohol, in addition to increasing the inhibitory effect on the central nervous system, paradoxical reactions are possible (psychomotor agitation, aggressive behavior, a state of pathological intoxication). Nicotine inhibits the activity of lorazepam (accelerates its metabolism).

Overdose

Symptoms: drowsiness, arterial hypotension, confusion, depression of reflexes, coma.

Treatment: induction of vomiting, gastric lavage, intravenous administration of norepinephrine to increase blood pressure, symptomatic therapy, monitoring of vital functions. The introduction of a specific antidote – an antagonist of benzodiazepine receptors flumazenil (in a hospital setting).

Dosage and administration

Inside. The dosage regimen and the duration of the course of treatment are set strictly individually.

In neurological practice – 1 mg 2-3 times a day; in psychiatric practice – 4-6 mg / day; with insomnia – 1-2 mg 30 minutes before bedtime. In elderly and debilitated patients, the dose should not exceed 2 mg / day (in divided doses). In patients with liver and / or kidney disease, as well as in patients with cerebral sclerosis, hypotension, heart failure, underweight, dose adjustment is recommended.

Precautions

Use with caution in patients with depression, given the tendency to suicide. In patients with drug and alcohol dependence, use under close medical supervision.

Side effects are usually observed at the beginning of therapy. The possibility of a more frequent occurrence of side effects in elderly and debilitated patients should be taken into account.

During treatment and for 2 days after its completion, it is necessary to exclude the intake of alcoholic beverages; drivers of vehicles and people whose work requires a quick mental and physical reaction, and is also associated with increased concentration of attention, should not engage in professional activities during this period.

Long-term use may cause addiction and drug dependence (especially when taking high doses). In this regard, lorazepam should not be used for longer than 4-6 weeks. If long-term treatment is necessary, weekly breaks in taking the drug should be periodically taken. With a sharp cessation of treatment, a withdrawal syndrome may occur (tremor, convulsions, abdominal or muscle cramps, vomiting, perspiration), and symptoms similar to those of the disease (anxiety, agitation, irritability, emotional stress, insomnia, convulsions) may also occur.