What is Ativan? What is used for Ativan?
Ativan is the brand name of the medicine that contains Lorazepam as an active ingredient. It belongs to the benzodiazepine class.
It is mainly used to treat anxiety disorders because it helps to restore the chemical equilibrium between the CNS stimulant (Eg., Glutamate) and the molecules CNS depressant (Eg., GABA) in the brain. It is also a medicine antiasimiento and sedative.
Lorazepam has the chemical formula-chloro-5 (2-chlorophenyl) -1,3-dihydro-3-hydroxy-2H-1, 4-benzodiazepine-2-one.
How does Ativan work in the body?
The active ingredient in Ativan, lorazepam is a complex γ-aminobutyric acid (GABA) receptor, agonist. The receiver has five subunits since its function is very complex.
These receptors are very widespread in the brain and play a depressing role in the CNS, that is, they inhibit the activity of our brain so that it does not enter an overdrive.
Recipients do one or more of the following three actions::
- open output flow channels K +
- Close na +flow channels
- Open flow channels Cl-
All of the above actions help to achieve a common function, that is, to reduce the resting membrane potential of neurons to a hyperpolarised state and away from the depolarisation threshold value.
Another effect of the drug on neurons is that it decreases the drive of the impulse (signal) of neurons. So the overall effect of this drug on our body is that it diminishes the excitability of neurons so now a bigger one than before will be necessary impulse to excite them.
What is FDA approved for Ativan indications?
The FDA has approved Lorazepam for anxiety disorders such as general anxiety disorder (TAG), post-traumatic stress disorder (PTSD), obsessive-compulsive disorder (OCD), social phobias, phobias associated with certain things or situations such as flight and panic disorder.
The FDA has also indicated its use for the treatment of epileptic status.
Other uses not included in the label include their use in preoperative environments to relieve anxiety. It may also be used as an antiemetic medicine or as a tranquilizer agent in psychotic patients.
Another use of lorazepam is that it can be used in patients with irritable bowel syndrome.
Dosage of Ativan
Whereas the administration of a medicinal product should take into account especially the age of the patient, the presence of any other disease in particular liver or kidney disease, whether he or she is taking any other medicine and the route of administration of the drug some factors.
The normal recommended dose of IV Lorazepam injection is 4 mg slowly administered (two mg/min) for individuals over 18 decades old. If seizures persist, an extra 4mg of this medication could be given.
Patients usually require an initial dose of 2 to 3 mg/day orally given twice a day or three times a day.
A single dose daily of 2 to 4 mg orally may be given, usually at bedtime.
Elderly or weakened patients are usually given an initial dose of 1 to 2 mg/day recommended in divided doses.
When large doses are necessary, the dose of Lorazepam must be raised gradually to help avoid negative effects. In these scenarios, the evening dose ought to be increased prior to the doses during the day.
How long does it take to work Ativan?
The start of the action depends on the route of administration. If 1 mg of the drug is administered orally, it usually takes 15-30minutes for effect at first. By giving the same amount parenterally, the start is fast, that is, within 10 minutes.
The maximum appearance is reached from 1.5 to 2 h; then the drug is taken.
How long does Ativan stay in your system – urine, blood, saliva, hair?
When a 2 mg dose of lorazepam is given, the maximum serum concentration is generally reached approximately 2 hours after taking medicine and is between 17 ng/ml to 20 ng/ml. After 2 hours, serum levels begin to decline. The drug is mainly eliminated by hepatic metabolism.
The reaction is submitted in the liver is glucuronidation, i.e. the addition of glucuronic acid to lorazepam. The compound formed is glucuronide Lorazepam and is an inactive metabolite that gets excreted in the urine. The drug has a half-life of 12 hours. 7-8% of the drug is excreted in the faeces.
steady-state Lorazepam concentration can be achieved from two to three days when the user is taking the drug regularly and on time. It is not advisable to use a drug loading dose because of its severe CNS depressant effects.
The person’s age, kidney function tests, and liver function tests do not affect the time needed to reach the maximum concentration or Half-Life.
Lorazepam has poor lipid-water and solubility and has a high protein binding, so when the drug enters any compartment (as a vascular compartment), it stays there for quite some time, as it cannot easily penetrate lipid membranes separating one compartment from the other.
How is the component in question easily cleaned?
What this Signifies is that One dose of lorazepam will Require 2-3 days to be completely removed from the blood and more if there was an overdose. Similarly, if the person has taken lorazepam for days or weeks, it will take 1-2 weeks for Serum drug concentration to drop to zero.
From the urine is done by blood filtration, the urine concentration of the inactive form of the drug (Lorazepam glucuronide) will also be detectable in the urine for the same amount of time. Other sources in which the medication can be discovered are hair and saliva.
Saliva drug testing is variable and therefore unpredictable. In some cases, it is possible to detect immediately after taking the drug, which in others may take a couple of hours. If one dose is accepted, detection in saliva will not be possible following 48 hours. No instances of discovery have reported beyond this age.
Hair detection is only possible for users who have used the medication for at least 2-3 consecutive days. In such cases, the period for detection lasts up to 90 days.
This fact is used in both therapeutic and Forensic Medicine. The therapeutic part is discussed here; the forensic part is analyzed in the next subtitle.
Diazepam has been regarded as the drug of choice in the epileptic state. But, diazepam includes a higher lipid solubility so that if given IV, it leaves the vascular compartment in place quickly and the serum concentration drops below the threshold needed to produce a result called the minimum effective concentration.
To overcome this issue, there is no other alternative than to administer another dose of diazepam. However, since Lorazepam has poor lipid solubility, which has a small volume of distribution, i.e. they do not leave the vascular compartment quite quickly.
Therefore the lorazepam concentration remains above the effective minimum concentration for a longer period of time. So now is replacing Lorazepam diazepam as drug of choice in status epilepticus.
Ativan doesn’t show up on a drug test?
Tests of traditional drugs such as SAMHSA-5 are intended to detect only drugs such as cocaine, marijuana, amphetamines, opiates, and PCP. As a result, lorazepam (or other benzodiazepines) may not be tested.
However, an extensive drug test may certainly detect the presence of benzodiazepines (including lorazepam).
One of the tests that have been successfully used to detect the presence of specific drugs is liquid mass chromatography spectrometry (LC-MS).
It is an analytical chemistry technique that has been used to detect drug levels in blood, saliva, and hair for quite some time. This technique is particularly useful in the field of Forensic Science as benzodiazepines are used by sex offenders who use this drug to adulterate drinks.
The period during which the test is performed is of vital importance. Given that the concentrations of Lorazepam are rapidly running out of liquids by mouth within 48 hours, the urine samples are said to be more reliable because the concentration of lorazepam in the urine even after a single dose remains above the value detectable.
Precautions during use of Ativan
Pre-existing depression may arise or worsen during the use of lorazepam.
Lorazepam recommended for use in patients with major depressive disorder or psychosis.
There is a risk of fatal respiratory depression if lorazepam is used with other CNS depressors.
The use of lorazepam can lead to physical and psychological dependence afterward.
All patients receiving lorazepam should be advised not to drive motor vehicles or dangerous machinery.
All patients should be advised that their tolerance to alcohol and other CNS depressants will be reduced.
Withdrawal symptoms may occur after abrupt termination even at recommended doses after only one week of therapy. Therefore, it should be avoided and a gradual dosing schedule followed by prolonged therapy should be avoided.
The drug should be avoided during pregnancy as it is classified as a Class D drug by the FDA.
The use of lorazepam by nursing mothers is not advisable. Any breastfeeding or Drug Administration should be stopped.
In cases in which the medication should be administered to mothers who insist on breastfeeding, the newborns should be examined periodically to detect the side effects of the drug such as sedation, inability to suck, since the drug is excreted in the breast milk also.
Contraindications for the use of Ativan
Lorazepam should not be administered to patients with the following conditions
Known hypersensitivity to benzodiazepines
A patient experiencing narrow-angle acute glaucoma.
Pharmacological interactions Ativan
Lorazepam produces exaggerated CNS depressant effects when administered with other depressors such as alcohol, antipsychotics, anxiolytics, antidepressants, antihistamines, anticonvulsants, anesthetics, barbiturates, sedatives / hypnotics, narcotic CNS analgesics.
Simultaneous use of clozapine and lorazepam may lead to severe sedation, excessive salivation, hypotension, ataxia, delirium, and respiratory arrest.
Simultaneous administration of lorazepam with increased valproate plasma concentrations and decreased Lorazepam clearance results
Simultaneous administration of lorazepam with probenecid may result in a faster start or prolonged effect of lorazepam due to an increase in Half-Life and a decrease in total clearance. In such cases, the dose of the drug is reduced to almost 50%.
Administration of the methylxanthines, e.g., theophylline or aminophylline may antagonize the sedative effects of lorazepam.
Side effects of Ativan
In addition to its great uses and advantages all drugs come along with some side effects. The side effects of lorazepam are the following:
Most common include:
- Loss of coordination
- Blurred vision
- Inability to perform sexual procedures
- Changes in appetite
Call your health care provider as soon as you begin to experience any of these. The doctor may have recommended you because your advantages would be more than your disadvantages, but tell the doctor if you begin to experience the following important and serious side effects such as:
- Difficulty in speech as speech disorders
- Changes in vision
- Mood swings or behavior change
- Neurological effects such as suicidal thoughts, hallucinations, depression, etc.
- Weakness and fatigue
- Abnormal gait and posture
- Difficulty breathing, especially during sleep or other breathing problems such as coughing or difficulty breathing
- Signs of infection such as a sore throat, fever, etc
These are even less harmful side effects. You should consult your doctor and be treated right away if you experience seizures or yellowing of the eyes or skin.
In addition to these allergic reactions to Lorazepam are also common. However, a very serious one is rare. But if the following symptoms occur, you should get medical help as soon as possible:
- Severe dizziness
- Respiratory distress