Ativan

Ativan, pharmaceutically known for its generic name Lorazepam, is a potent anxiolytic medicine classified under the class of Benzodiazepine.

Ativan, pharmaceutically known for its generic name Lorazepam, is a potent anxiolytic medicine classified under the class of Benzodiazepine. Depending on where it is being used or on the adjunct substance mixed with it during administration, Ativan has garnered few street names. Benzo, Blue V, Candy, Downers, Sleeping Pill, Sleeper, and Trank are few of the street names given to it but are not being used in the field of medicine. Ativan, first approved by the Food and Drugs Administration (FDA) is categorized as a regulated medicine, prescribed by physicians who have obtained a special license to prescribe regulated medicine and strictly dispensed by pharmacists.

Ativan is used for a long-term regimen schedule, approximately up to four months. However, precaution and additional drug monitoring of the patient are to be practiced since the “four-month” duration has not undergone a clinical evaluation. The drug monitoring is to be done at a specific time interval, helping the health practitioners to carefully monitor the patient and his response to the drug.

Ativan’s active ingredient and generic name, Lorazepam is a fine white powder that is slightly soluble in water. It is sold in the market as a tablet for its dosage form with dosage strengths of 0.5 mg, 1 mg, and 2 mg. The different dosage strengths have distinct imprints and features. Such in the case of the 0.5 mg strength, a five-sided white tablet where an imprint “A, BPI 63” is made on its surface. The 1 mg strength, still a five-sided white table, however, has two kinds, of which imprints are different: “A, BPI 64” and “A, 64 WYETH.” While the 2 mg strength, still a five-sided white tablet has an imprint on its surface, reading, “A, BPI 66.”

Ativan, like any other medicine, has different pharmaceutical excipients (the inactive ingredients that hold the tablet to ensure the safety, quality, efficacy, and efficiency of its active ingredient). It contains Lactose monohydrate acting as a diluent, Magnesium stearate as a glidant, microcrystalline cellulose as a binder, and polacrilin potassium as a disintegrant. Knowing these components is equally important as to knowing the entirety of Ativan as this information may help your physician and pharmacist know whether you may develop an allergic reaction

Clinical Indications of Ativan

Before when Ativan has not been labeled as a regulated drug, it was both used for medical and recreational purposes. However, with the advent of Lorazepam addiction, the regulation of its availability became the reason why it is not used for recreational purposes now. A few of its indications are the short-term treatment for symptoms of anxiety disorders; acute relief from panic attacks; short-term medication for insomnia; an adjuvant drug for people experiencing nausea and vomiting due to chemotherapy; and a treatment for seizures.

How Ativan works

Given the fact that Ativan, a benzodiazepine, is potent medicine, how does this minute substance able to cast its effect to the patients?

The human brain heavily depends on brain signals which are called neurotransmitters to relay a message. Neurotransmitters vary from each other, likewise, their effects. One of the important neurotransmitters is the Gamma-Aminobutyric Acid (GABA), a chief inhibitory neurotransmitter that relaxes the neural activities. It does so by increasing the chloride ion influx inside the cell, thus, relaxing the nerve and eventually the brain.

Ativan, on the other hand, potentiates the effect of GABA in the brain. Ativan specifically binds on the beta subunit found on the receptor where GABA produces its relaxation effect. By that virtue, Ativan lengthens the duration of GABA binding to its active site eventually making the nervous system in a relaxed state.

Dosage and Dose Duration of Ativan

The dose and duration of drug regimen vary depending on the disorder or disease of the patient, and of course with the jurisdiction of the licensed physician.

However, the general dose of anxiety medication is 2-8 mg to be administered orally. For patients with insomnia, the dose of 2-4 mg is administered 20 minutes before the desired time of sleep.

Pharmacokinetics

The average half-life of this drug is 12 hours. Half-life in simple terms means the time it takes to eliminate half of the dose administered to the patient. Example, if a 2 mg Ativan was administered, it will take 12 hours to eliminate the 1 mg (half of the dose administered) out of the body. Meanwhile, Lorazepam glucuronide, its metabolite, has a half-life of 18 mg. With respect to the bioavailability and individual metabolism, the rate of elimination and half-life may still vary.

When one has to undergo drug testing, Lorazepam and its metabolite are detectable on different tissues and fluids. In the blood, its presence lasts up to three days. In the urine, its presence lasts up to six days. In the saliva, its presence lasts up until eight hours. While in the hair, the presence of Lorazepam lasts for four long, whooping weeks. 

Precautions and Adverse Drug Reactions

Ativan, albeit shows lesser adverse drug reactions compared to other benzodiazepines, is dangerous for two primary reasons. First, it has a higher detrimental effect along with high doses. And second, it has fatal drug-drug interactions.

When taken with Loxapine, another depressant drug, the depressant effect of Ativan is magnified. Other substances that may magnify the effect of Ativan are neural depressants like alcohol, antipsychotics, barbiturates, sedatives, narcotics, anticonvulsant and anesthetics, and even the simple over-the-counter analgesics and antihistamines. Magnified effects of Ativan may lead to respiratory depression.

Suicidal behavior, coma, lowering of platelet count, and decrease of granulocyte white blood cells are the common adverse drug reactions of Ativan. Short term effects of Ativan are feeling of light-headedness; muscle weakness; disorientation; and loss of appetite. While the long-term effects are: poor body coordination; poor body strength; vertigo; nausea; vomiting; jaundice; difficulty in speaking; photosensitivity.

Ativan has also shown potential fetal damages and is not suited for nursing mothers. It is to be noted that it should only be prescribed for 2-4 weeks so to prevent dependence and withdrawal symptoms. Close monitoring of drug intake must also be done as the administration of drug more than the dose of what is just required may cause addiction. People with a history of alcoholism are noted for their high chance of developing an addiction to this regulated drug.

Overdose and Treatment

OVERDOSE. Lorazepam overdose usually occurs when one intakes more than what is prescribed or above the general dose of 2-8 mg. Excessive intake due to recreational purposes causes overdose as well.

One has to be well oriented and keen on spotting the signs of Lorazepam overdose. Some of the signs are as follows; confusion; slow reflexes; disorientation; deep sleep; sudden unconsciousness; uncontrolled muscle contractions; involuntary eye movement; and bleary eyesight.

TREATMENT. There are many approaches and factors to consider in addressing Lorazepam overdose. These factors are important since they will be the deciding agents to which intervention shall be made during an emergency case such as this.

  1. PRIMARY ANTIDOTE. Flumazenil is the primary antidote as it will antagonize the effects of Lorazepam.
  2. WHEN DRUG HAS NOT BEEN ABSORBED YET IN THE INTESTINE. Administration of activated charcoal is useful. The activated charcoal will act as an organic magnet so that the Lorazepam moiety will no longer be absorbed in the small intestine. Next, performing stomach lavage will be helpful in taking away the Lorazepam moiety out from the stomach, thus, no further absorption to the circulatory system may occur.
  3. WHEN DRUG HAS REACHED THE SYSTEMIC CIRCULATION. Performing dialysis will be helpful in separating the toxic dose out from the blood. Administration of intravenous fluids and monitoring vital signs are to be performed as well. 

Withdrawal and Addiction Treatment

A person who abuses the said medicine for more than four weeks may become dependent on the substance. Thus, sudden cessation of the drug may lead the person to experience withdrawal symptoms.

Several withdrawal symptoms are as follows: irregular sleep pattern; irritability; increased anxiety level; panic attacks; uncontrolled sweating; poor focus; frequent headaches; muscle spasm; insomnia; and unstable mood swings.

TREATMENT. The first thing to be done when addiction is detected from the person taking the said medicine is to consult the clinician or physician. However, usually, there are different methods used to address the addiction of the patient.

  1. Medicine. Clonazepam, a benzodiazepine will cure seizure, panic attacks, and anxiety. Phenobarbital, a barbiturate, will minimize seizures and anxiety. Buspirone, a serotonin receptor agonist, elevates the mood. Carbamazepine relaxes the brain and reduces anxiety. And Imipramine, a tricyclic antidepressant, cures depression by inhibiting the reuptake of the neurotransmitters responsible for good mood.
  2. Reward System. A contingency management plan where sets of rewards will be given to the patient who will avoid the substance. This is a positive reinforcement to address addiction.
  3. Cognitive Behavioral Therapy. A treatment process seeking to determine the variables causing drug abuse, risk reduction methods and enhancing coping mechanism.
  4. Recovery Group. A community-based plan which allows the patient to meet other victims and have a sharing about their experiences and success in gradually overcoming their addiction.

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