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Side effects of ativan 5 mg


Uses, Risks & Overdose for Lorazepam

What are the side effects of Ativan?

Major side effects associated with Ativan use and/or abuse include:

  • Confusion
  • Lack of muscle control
  • Blood in urine or stool
  • Stomach pain
  • Weight loss
  • Tremors
  • Overdose
  • Addiction
  • Tolerance to the impact of Ativan
  • Rebound anxiety
  • Restlessness
  • Depression
  • Memory loss
  • Learning difficulties
  • Emotional blunting

About 40 million American adults ” 18 percent of the US population ” suffer from some form of anxiety, according to the Anxiety and Depression Association of America.

Many of these individuals are treated with anti-anxiety medications like lorazepam, a short-acting tranquilizer sold under the trade name Ativan. Ativan acts quickly on the central nervous system by increasing the availability of gamma-aminobutyric acid (GABA) to the brain. GABA is a brain chemical that calms the central nervous system, exerting a tranquilizing effect on the mind and body.
When taken appropriately under a doctor’s supervision, Ativan can help reduce many of the common symptoms of anxiety, including panic attacks, unjustified fears, sleeplessness, agitation, and restlessness. In addition to treating anxiety, Ativan is prescribed for seizure, spasms, alcohol withdrawal, or insomnia. Ativan can causes side effects, especially when it is taken in excessively high doses or used for recreational reasons.

Ativan Effects on the Body

By slowing the activity of the brain and nerves, Ativan also affects physical functions and responses. As a tranquilizer, Ativan can make the user feel calm and physically relaxed. Ativan can also stop painful spasms in muscles, or prevent life-threatening seizures when taken correctly. For patients who take Ativan as directed for legitimate reasons, this medication is generally safe and effective. However, all users must watch out for potential adverse reactions to the drug, such as:

  • Daytime sleepiness
  • Low energy levels
  • Confusion
  • Poor muscle coordination
  • Blurry vision
  • Loss of balance
  • Blood in stool or urine
  • Stomach pain
  • Weight loss
  • Chills
  • Pale, cool skin
  • Involuntary movements (tremors, shaking)

Because it can cause clumsiness, drowsiness, and disorientation, Ativan poses an increased risk of accidental injuries. The National Highway Traffic and Safety Administration cautions that drugs in the benzodiazepine family, like Ativan, can cause symptoms resemble alcohol intoxication, such as loss of motor coordination, slurred speech, visual disturbances, and blurred vision. Driving under the influence of Ativan, or performing other activities that require hand-eye coordination and quick reflexes, can be extremely dangerous, especially if the user has also consumed alcohol or other sedatives.

Ativan Effects on the Mind

Ativan can have powerful effects on the brain and nerves. However, many users experience “rebound” side effects, or a worsening of the same symptoms that the drug is designed to treat. In particular, Ativan can cause rebound anxiety, sleep disturbances, abnormal body movements, and agitation.

  • Rebound anxiety
  • Restlessness
  • Loss of pleasure in day-to-day experiences
  • Depression
  • Memory problem
  • Learning difficulties

The chemical structure of lorazepam is intended to reduce the excitability of the brain and nerves, while soothing emotional responses that create anxiety and restlessness. On the negative side, Ativan can flatten users’ emotional responses and blunt their experiences of the world. Individuals who take Ativan may begin to feel a loss of interest in their everyday experiences or responsibilities. They may feel constantly sluggish and tired, and have a dazed, drowsy appearance.

Signs of an Ativan Overdose: Is It Possible?

Ativan is a safe drug when taken in the prescribed doses, at the recommended times. But taking large doses of this medication puts the user at risk of an overdose, which may end in coma or even death. The number of overdose-related deaths associated with prescription benzodiazepines like Ativan has increased fourfold since 2001, according to the National Institute on Drug Abuse. In 2013, there were nearly 7,000 fatalities attributed to benzodiazepine overdose in the US.

As a central nervous system depressant, Ativan slows down activity in the brain and nerves. When taken alone and used correctly, Ativan rarely causes unconsciousness, coma, or death. However, high doses of Ativan can have fatal consequences, especially when lorazepam is combined with other drugs that also suppress the activity of the brain and vital organs. Many overdoses, either accidental or deliberate, have been linked to the use of Ativan with alcohol, prescription pain medications, other anti-anxiety drugs, and hypnotic medications used for insomnia.

Learning to recognize the signs of a lorazepam overdose could literally save a life:

  • Pale, cool, bluish skin or lips
  • Shallow, slow breathing
  • Over-sedation or drowsiness
  • Stumbling and loss of coordination
  • Slurred speech
  • Memory loss
  • Confusion
  • Weakness
  • Loss of consciousness

An Ativan overdose is an emergency that may end in death if the individual doesn’t receive immediate medical attention.

People who have overdosed on Ativan should never be left alone to recover from the effects of the drugs, especially if there are other drugs involved.

Ativan Addiction and Withdrawal

One of the most serious side effects of Ativan use is the possibility of developing an addiction to this medication. Ativan addiction is most common in users who take too much of the drug, who use it for nonmedical reasons, or who take Ativan with other tranquilizing drugs, like alcohol, prescription pain relievers, and sleep aids.

After taking Ativan for more than 2-3 weeks, the nervous system becomes accustomed to the effects of the drug.

Many patients require higher doses of the drug to relieve their symptoms, a phenomenon called tolerance. Tolerance may lead to dependence ” a physical or psychological reliance on the drug in order to feel normal. If the user continues to misuse Ativan, or the dose is not reduced, tolerance can lead to addiction. Addiction is a progressive disease that causes a compulsive need to seek and use a drug. The red flags of an Ativan addiction include:

  • Restlessness, irritability, or depression when the user can’t get the drug
  • An obsessive interest in getting and using more of the drug, in spite of the harmful effects on personal health or relationships
  • A loss of control over how much Ativan the user takes at any given time
  • Isolation from friends, family, or social events as a result of drug use
  • A deterioration in the quality of one’s work on the job or at school
  • A decline in physical appearance and grooming
  • Physical and psychological withdrawal symptoms when the drug is discontinued or the dose is lowered

Benzodiazepine withdrawal can have dangerous side effects, including seizures, severe agitation, and hallucinations. When individuals are suddenly deprived of the drug, they may also have headaches, nausea and vomiting, sleeping problems, sweating, and episodes of restlessness. In order to minimize withdrawal symptoms, a drug taper is advised for most Ativan users. In a drug taper, a doctor gradually lowers the dose of Ativan over a certain period of time, until the drug can be safely stopped without compromising the patient’s health or wellbeing.

Along with a physician-supervised drug taper, individuals who are addicted to Ativan need therapeutic treatment for addiction, as well as psychosocial resources to rebuild their lives. In a randomized, controlled trial of benzodiazepine users published in the Canadian Journal of Psychiatry, 180 patients were followed after completing a benzodiazepine discontinuation program. Patients who went through a drug taper were able to stop using the medication for longer periods of time. Heavier benzodiazepine users and those who were also addicted to alcohol or other drugs had more difficulty staying sober. Comprehensive recovery services include individual therapy, access to support groups, behavioral modification therapies, case management, and other research-based interventions.

Seeking Help for Ativan Abuse

Many people mistakenly believe that prescription medications like Ativan are less harmful or habit-forming than illegal drugs like meth, cocaine, or marijuana. But prescription drug addiction “including the addiction to tranquilizers like Ativan” has become a major threat to public health in the US. If individuals continue to abuse Ativan in spite of harmful side effects and negative health consequences, they may be addicted to this medication. While talking to loved ones about Ativan abuse may feel awkward or uncomfortable, this expression of concern could be the first step in helping them recover physical and psychological health. If you or a loved one is concerned about their Ativan use, rehab may be an option. See if your insurance provider may be able to cover all or part of the cost of rehab.

Ativan side effects and interactions, and how to avoid them

If you have anxiety, you’ve probably heard of Ativan. Still, you might not know that Ativan also helps with insomnia, it can prevent nausea during chemotherapy treatments, and it’s used to treat status epilepticus seizures. Ativan, a brand name of the medication lorazepam, is a quick-acting medication, with most people starting to feel its calming effects between 20 and 30 minutes after taking it. As with most medications, Ativan has side effects and it can interact with other drugs. In this article, we discuss the possible Ativan side effects, drug interactions, and warnings to safely use it. 

What is Ativan?

Ativan (lorazepam) is in a class of medication called benzodiazepines. It is available as a prescription drug. It’s approved in the U.S. for the following treatments: 

  • Short-term relief of symptoms from anxiety disorders and anxiety-associated depression
  • Management of anxiety disorders

Doctors sometimes prescribe it off-label, meaning that although it isn’t approved to treat a specific medical condition, anecdotal evidence has found it helpful. According to the National Center for Biotechnology Information, these conditions include:

  • Alcohol withdrawal syndrome and delirium
  • Panic disorders
  • Preventing nausea during cancer treatment
  • Muscle spasms
  • Relaxation and sedation before anesthesia
  • Psychogenic catatonia
  • Short-term use for insomnia
  • Status epilepticus seizures

Ativan is quick-acting. When taking orally, most people start to feel the effects in 20 to 30 minutes. Ativan is effective within one to three minutes when given intravenously. 

RELATED: Anxiety treatments and medications

Why is lorazepam a controlled substance?

There is a risk of Ativan abuse and dependence. The United States Food and Drug Administration (FDA) has labeled Ativan a Schedule IV controlled substance. There are five levels of controlled substances based on the drug’s risk of abuse or harm, such as if the drug has the potential to lead to psychological or physical dependence. Schedule I has the highest potential for drug abuse, such as heroin. These drugs have no accepted medical use and are not legal in the United States. Schedule V drugs have the lowest potential for abuse, such as certain cough syrups that contain codeine. Benzodiazepines such as Ativan are in Schedule IV, meaning they have a moderate potential for substance abuse, as well as having legitimate medical use. Other medications in this category include Xanax (alprazolam), Klonopin (clonazepam), and Valium (diazepam). 

Is Ativan a narcotic?

Although it is a controlled substance, Ativan is not a narcotic. Narcotics reduce a person’s perception of pain, while benzodiazepines have calming effects. Both narcotics and benzodiazepines have the potential to be habit-forming. Although medical practitioners consider Ativan safe and effective when used as directed, physical dependence can develop as quickly as two weeks, according to the National Alliance on Mental Illness (NAMI).

Common side effects of Ativan

Ativan’s side effects tend to be more severe with higher doses. Some of the most common side effects include:

  • Dizziness
  • Drowsiness or sleepiness
  • Sedation
  • Lightheadedness
  • Unsteadiness
  • Decreased ability to concentrate
  • Muscle weakness
  • Dry mouth

“Decreased blood pressure is a side effect of Ativan, but it is not prescribed for lowering blood pressure,” explains Amanda Brown, NP, a psychiatric mental health nurse practitioner at New York-Presbyterian Hospital and associate at Columbia University Irving Medical Center. 

Ativan can also cause sleep disturbances, erectile dysfunction, and changes in appetite. 

Ativan works by calming the nervous system to balance activity in the brain, promoting a relaxing, calming effect. It also raises dopamine, and when taken in high doses, feel-good neurotransmitters in the brain increase, causing a euphoric feeling, which is one of the reasons it is addictive. 

Serious side effects of Ativan

Some people could experience more severe side effects from Ativan use. These include:

  • Shuffling walk
  • Tremors or inability to sit still
  • Fever
  • Breathing problems
  • Difficulty swallowing
  • Skin rash or hives
  • Yellowing of skin or eyes
  • Irregular heartbeat 
  • Memory loss or memory problems
  • Disorientation
  • Sleep apnea or worsening of sleep apnea

Most of the time, side effects lessen as the medication’s effect decreases, usually in six to eight hours. However, if you are experiencing severe side effects or effects do not go away within a few hours, you should seek medical attention. 

“Side effects that warrant stopping the medication include extreme sleepiness, memory loss, irritability, markedly impaired coordination, and dizziness,” Brown says. Because suddenly stopping Ativan can cause withdrawal symptoms, you should talk to your doctor before discontinuing it. 

Ativan warnings

Ativan is a short-term medication. When prescribed for daily use, the recommended course of treatment is four weeks or less.  

Ativan withdrawal symptoms

“Long-term use can lead to dependency and tolerance, meaning a person may need a higher dose to have the same effect or may experience withdrawal from not taking the medication,” says Wendi D. Jones, Pharm.D., a pharmacist in North Carolina. “Psychologically, it may be more difficult to go without the drug, leading to increased anxiety. Stopping the medication after a few weeks of use shouldn’t cause significant problems. However, if you have been using the medication for longer than two to four weeks, dependence can occur, and tapering off it could be required.” 

Depression

For some people, Ativan could exacerbate depression symptoms. Ativan is a central nervous system depressant. When it builds up in your system or if you take it at high doses, it’s possible for depression to worsen and even result in suicidal thoughts or feelings. The drug information outlined in the package insert indicates Ativan should only be used in patients with depression when the patient is also on antidepressant treatment.  

Age restrictions

Ativan is on the Beers Criteria Medication List of drugs that are potentially inappropriate for older adults. Older adults have increased sensitivity to benzodiazepines. In these patients, there is an increased risk of cognitive impairment, delirium, falls, fractures, and motor vehicle crashes when Ativan is used. Despite being on the Beers List, Ativan is frequently prescribed to older adults. In these patients, the lowest possible dose should be used and the patient should be closely monitored. 

Because lorazepam is a sedative, you should not drive a car or operate machinery until you know how this medication affects you. 

Memory impairment

There is also conflicting information as to whether Ativan causes or is a risk factor for memory impairment or Alzheimer’s disease. One study found the benzodiazepines could be a risk factor for dementia. And another study, published in 2014, found an association between taking lorazepam and the risk of Alzheimer’s disease. However, more recent research, published in 2016, showed that the risk of dementia was only slightly higher in people taking low doses of benzodiazepines, and it was not present in those taking it at higher doses.

Respiratory depression

Benzodiazepines can cause respiratory depression, or hypoventilation, when used on their own, and even more when combined with another central nervous system (CNS) depressant. This breathing disorder causes slow, ineffective breathing, creating a higher level of carbon dioxide and a lower level of oxygen in your body.

Benzodiazepines such as Ativan can also cause respiratory depression when combined with other sedating medications or substances such as alcohol, muscle relaxants, sedating antihistamines, antipsychotics, anticonvulsants, and antidepressants. Always consult your healthcare provider to make sure that Ativan is safe in combination with other medications you take.

Pregnancy and breastfeeding

If you are pregnant or planning to become pregnant, seek medical advice before taking this medication. Animal studies have shown occasional abnormalities in the fetus. There is an increased risk of malformations from tranquilizers during the first trimester. The use of Ativan during the third trimester is also associated with an increased risk of neonatal withdrawal. Lorazepam may pass to babies in breast milk and may cause sedation and irritability in the baby. If you are breastfeeding, consult your healthcare provider.

Ativan interactions

“Alcohol and opioids should be avoided when taking Ativan,” says Dr. Jones, “In general, anything that makes you feel tired, including CBD oil and melatonin, need to be taken carefully until you know how your body reacts. There are several medications that can increase the adverse or toxic effects of lorazepam. It is always good to ask your pharmacist if something is safe for you to take, including prescription, over-the-counter, and herbal medicines.” 

Drug-drug interactions

Before taking Ativan, or any medication, you should tell your doctor about all medications—prescription or over-the-counter, supplements, and vitamins—you are taking especially:

  • Anticonvulsants
  • Antidepressants
  • Asthma medications: theophylline
  • Cold medicine
  • Gout medication: probenecid
  • Medications for Parkinson’s disease: Rytary, Sinemet, and Stalevo (levodopa)
  • Muscle relaxants
  • Opioid pain medications
  • Oral antifungals
  • Oral contraceptives (birth control pills)
  • Sedatives, tranquilizers, or sleeping pills
  • Sedating allergy medicine/antihistamines
  • Pain medications or cough medications that contain codeine

If you are taking any of these medications, your doctor might want to adjust your dosage, switch to a different medicine, or closely monitor you for side effects and adverse reactions.  

Food-drug interactions

You should not consume grapefruit or grapefruit products while taking this medication as this can increase the effects and lead to toxicity or adverse reactions. 

You should not drink alcohol while taking it as you can experience life-threatening side effects.

While there are no specific warnings against drinking coffee or other foods and beverages containing caffeine, it is essential to remember that caffeine is a stimulant and could potentially counteract the effects of lorazepam. 

How to avoid Ativan side effects

Side effects, such as tiredness, usually start shortly after taking the medication, often within 30 minutes of taking the medication. They generally lessen as the effects of the drug decrease, typically between six and eight hours after taking it. Some people also notice that side effects decrease as they continue taking the medication, and their body adjusts to it, for example, they might not feel as tired after taking it regularly for several days or weeks.  

1. Take Ativan according to your doctor’s instructions.

Taking the correct Ativan dosage helps reduce the side effects you might experience. Some people take them “as needed,” which means only at times you feel anxious, and others take them at regular intervals throughout the day to keep anxiety symptoms at bay. If you are experiencing side effects, talk to your doctor about whether changing the time you take the medication could reduce your discomfort. 

Ativan is available in different forms and doses:

  • Intramuscular injection: 2 mg/ml, 4 mg/ml
  • Intravenously: 2 mg/ml, 4 mg/ml 
  • Oral tablet: 0.5 mg, 1 mg, 2 mg

You should start at a low dose and slowly work your way up, assuring you are taking the lowest dose that provides a benefit to you. The Prescriber’s Digital Reference (PDR) suggests the following doses for anxiety:

For insomnia, the recommended adult dosage starts at 2 mg at bedtime, to be increased to 4 mg, if needed, with the course of treatment four months or less.  

2. Take Ativan with food.

Most people do not experience stomach pain or upset when taking Ativan; however, if you do, it might help to take it with food. 

3. Do not suddenly stop taking Ativan.

Symptoms from withdrawal from Ativan can be more uncomfortable than the side effects. You should not stop taking the medication suddenly, especially if you are taking it regularly. Withdrawal symptoms include rebound anxiety, restlessness, tremor, sweating, agitation, insomnia, and possibly seizures. These symptoms begin within one to two days after your last dose and can last for seven days or more, depending on how long you have been taking it. It is best to taper how much and how often you take it slowly. 

Your doctor will work with you to set up a safe tapering schedule. The San Mateo County Health Department suggests two methods of tapering:

  • A reduction of 25% of the initial dose every two weeks, or 
  • Decreasing the dose by 25% the first week, 25% the second week, and then by 10% each week until you have discontinued the medication 

The tapering process can take several weeks to a few months to completely stop the medication. Doing it this way eliminates or dramatically reduces any withdrawal symptoms you experience. 

4. Ask your doctor about switching to a different medication.

Your healthcare provider might suggest trying other anxiety medications in place of Ativan. Some antidepressants can reduce symptoms of anxiety. These include:

  • Cymbalta (duloxetine) 
  • Silenor (doxepin) 
  • Lexapro (escitalopram) 
  • Paxil, Paxil CR, Pexeva, Brisdelle (paroxetine) 
  • Effexor XR (venlafaxine) 

There are also other benzodiazepines, which include:

  • Xanax (alprazolam) 
  • Valium (diazepam) 
  • Klonopin (clonazepam)

Everyone reacts to medication differently. What works best for one person may not work for another. It is best to work closely with your doctor and learn about all of your treatment options so you can find the drug that works best for you. 

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

Contents

  • Structural formula
  • Russian name
  • English name
  • Latin name of the substance Lorazepam
  • Chemical name
    • nine0007 Gross formula
  • Pharmacological group of the substance Lorazepam
  • Nosological classification
  • CAS code
  • Pharmacological action
  • Characteristic
  • Pharmacology
    • nine0007 Use of the substance Lorazepam
  • Contraindications
  • Restrictions for use
  • Use in pregnancy and lactation
  • Side effects of the substance Lorazepam
  • Interaction
  • Overdose
    • nine0007 Route of administration and doses
  • Precautions
  • Special instructions
  • Trade names with the active substance Lorazepam

Structural formula

Russian name

Lorazepam

English name

Lorazepam

Latin name of the substance Lorazepam

Lorazepamum ( genus 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 2

Pharmacological group of the substance Lorazepam 9004 9002 Anxiolytics

Nosological classification

ICD-10 code list

  • R45. 1 Restlessness and agitation
  • F51.0 Insomnia of non-organic etiology
  • G47.0 Disorders of falling asleep and maintaining sleep [insomnia]
  • F10.5 Alcoholic psychosis
  • F91 Conduct disorders
  • F30 Manic episode
  • F42 Obsessive-compulsive disorder
  • F25 Schizoaffective disorders
  • F41.0 Panic disorder [episodic paroxysmal anxiety]
  • Z100* CLASS XXII Surgical practice
  • F60 Specific personality disorders
  • G44. 2 Tension headache type
  • R45.0 Nervousness
  • R45.7 State of emotional shock and stress, unspecified
  • F32 Depressive episode
  • F43.1 Post-traumatic stress disorder
  • F40.0 Agoraphobia
  • F43.2 Adjustment disorder
  • F34.1 Dysthymia
  • F41.1 Generalized anxiety disorder
  • F43.0 Acute stress reaction
  • G40 Epilepsy
  • F10.3 Withdrawal state

CAS code

846-49-1

Pharmacological action

Pharmacological action - nine0067 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. nine0005

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. nine0005

Lorazepam has low toxicity and wide therapeutic range.

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.

Use of the substance Lorazepam

Neuroses 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). nine0005

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 on use

Chronic respiratory failure, sleep apnea syndrome, open-angle glaucoma, drug and alcohol dependence, depression (see "Precautions"), psychosis, severe renal dysfunction. nine0005

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). nine0005

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. nine0068 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. nine0005

Precautions

Use with caution in depressed patients due to suicidal tendencies. 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. nine0005

With prolonged use, addiction and drug dependence may occur (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. nine0005

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

Reset filters

Lek. form All lek. dragee forms substance-powder tablets, coated tablets, film-coated

Dosage All dosages 1 mg 2.5 mg No dosage

Manufacturer 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
    • nine0007 Russian name
  • English name
  • Latin name of the substance Lorazepam
  • Chemical name
  • Gross formula
  • Pharmacological group of the substance Lorazepam
  • Nosological classification
    • nine0007 CAS code
  • Pharmacological action
  • Characteristic
  • Pharmacology
  • Use of the substance Lorazepam
  • Contraindications
  • Restrictions for use
  • Use in pregnancy and lactation
  • Side effects of the substance Lorazepam
  • Interaction
  • Overdose
  • Dosage and Administration
  • Precautions
  • Special instructions
  • Trade names with the active substance Lorazepam

Structural Formula

Name

Lorazes

9000 )-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one

Gross formula

C 15 H 10 Cl 2 N 2 O 2

Pharmacological group of the substance Lorazepam

Anxiolytics

Nosological classification

ICD-10 code list

  • R45. 1 Restlessness and agitation
  • F51.0 Insomnia of non-organic etiology
  • G47.0 Disorders of falling asleep and maintaining sleep [insomnia]
  • F10.5 Alcoholic psychosis
  • F91 Conduct disorders
  • F30 Manic Episode
  • F42 Obsessive-compulsive disorder
  • F25 Schizoaffective disorders
  • F41.0 Panic disorder [episodic paroxysmal anxiety]
  • Z100* CLASS XXII Surgical practice
  • F60 Specific personality disorders
  • G44. 2 Tension headache
  • R45.0 Nervousness
  • R45.7 State of emotional shock and stress, unspecified
  • F32 Depressive episode
  • F43.1 Post-traumatic stress disorder
  • F40.0 Agoraphobia
  • F43.2 Adjustment disorder
  • F34.1 Dysthymia
  • F41.1 Generalized anxiety disorder
  • F43.0 Acute stress reaction
  • G40 Epilepsy
  • F10.3 Withdrawal state

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. nine0005

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. nine0005

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. nine0005

Lorazepam has low toxicity and wide therapeutic range.

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.

Use of the substance Lorazepam

Neuroses 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). nine0005

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 on use

Chronic respiratory failure, sleep apnea syndrome, open-angle glaucoma, drug and alcohol dependence, depression (see "Precautions"), psychosis, severe renal dysfunction. nine0005

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). nine0005

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. nine0068 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. nine0005

Precautions

Use with caution in depressed patients due to suicidal tendencies. 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. nine0005

With prolonged use, addiction and drug dependence may occur (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.

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