Last reviewed by Miljan Krcobic on August 28th, 2018.
What is Ativan? What is Ativan used for?
Ativan is a Brand name for a medicine that contains short-acting benzodiazepine drug named lorazepam as an active ingredient. Lorazepam works by affecting chemicals in the CNS that are known as neurotransmitters which may be unbalanced in patients who suffer from different types of anxiety disorders. Ativan’s main indications are: anxiety disorders, insomnia caused by stress or anxiety, epilepsy and status epilepticus.
Ativan is also use in surgery to cause pre surgery sedation or to sedate patients who are on mechanic ventilation, for the therapy of alcohol withdrawal, and chemotherapy that causes anticipatory nausea and vomiting. In some cases Ativan may be used for the treatment of cocaine caused acute coronary syndrome.
Ativan is available in the form of immediate-release and sublingual tablets in doses of: 0.5 mg, 1 mg and 2 mg and in the form of solution for intramuscular or intravenous injection in concentrations of 2 mg/ml and 4 mg/ml. FDA approved lorazepam in 1977. Ativan is originally manufactured by Valeant Pharmaceuticals. It is also available in Generic form.
What is Valium? What is Valium used for?
Valium is a Brand name for a medicine that contains long-acting benzodiazepine drug named diazepam as an active ingredient. Diazepam works by affecting chemicals in the brain known as neurotransmitters that are unbalanced in patients who suffer from different types of anxiety disorder.
Valium indications are: treatment of severe anxiety disorders, short-term therapy of insomnia, premedication sedative, refractory Epilepsy, status epilepticus, anticonvulsant for muscle spasms and alcohol withdrawal.
Valium is available in the form of tablet in doses of: 2, 5 and 10 mg and also as a liquid for intramuscular or intravenous injection in dose of 10 mg. FDA approved diazepam for use in 1963 under the brand name Valium of Roche drug company.
How Ativan and Valium work in the body?
Lorazepam which is the active substance of Ativan works by binding to an allosteric site on GABA-A receptors of benzodiazepine receptor in the central nervous system. By binding to this receptor sites it potentiates the inhibitory effects of GABA neurotransmitter, which then opens the chloride channel in the receptor, allowing chloride influx and causing hyperpolerization of the neuron cell.
Diazepam binds nonspecifically to benzodiazepine receptors which are responsible for sleep induction, muscle relaxation, motor coordination and memory.
As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. After binding of GABA to its binding sites, chloride channels areopened, resulting in a hyperpolarized cell membrane thus preventing further excitation of the cell.
Differences and similarities between Ativan and Valium
Ativan and Valium are central nervous system depressants classified into the class benzodiazepines drugs. Ativan’s active ingredient is lorazepam while diazepam is active ingredient of Valium. Chemically they are similar, as they both contain benzodiazepine structure. Lorazepam’s molecular formula is C15H10Cl2N2O2 while diazepam’s is C16H13ClN2O.
So, lorazepam contains 1 chloride and 1 oxygen atom more than diazepam, which theoretically means that lorazepam should be more reactive and potent drug than diazepam. 1mg dose of Lorazepam is comparable to the effect of 10mg of Diazepam. That is why lorazepam has a higher addictive potential, compared to other benzodiazepines, including diazepam.
Both drugs works by affecting GABA neurotransmitter actions, which is a major inhibitory neurotransmitter in the brain. This causes nerve impulses to slow down, resulting in a sedating and calming effect.
Main difference between these two drugs is certainly their duration of action. Valium is known as long-acting benzodiazepine drug with half-life elimination time in the body of about 20-50 hours for diazepam and 3-100 hours for its metabolites, compared to Ativan’s half-life of 10-20 hours.
However, their onset of actions is almost the same of approximately 1-2 hours after oral administration. Maximum levels in blood are reached after the intravenuous injection within 15 minutes for Valium and within 10 minutes for Ativan.
Both drugs are efficiently used to relieve symptoms of different anxiety disorders. They are also often used to treat certain types of seizure disorders and to as a sleep inducers. Both medicines can be used as a premedication for inducing anxiolysis, sedation or amnesia before certain medical procedures such as dentistry or endoscopy to reduce anxiety.
In addition, Ativan is also used as an adjunct antiemetic in chemotherapy. Because of their anticonvulsant and anxiolytic activities, these medicines are useful for the prevention and treatment of alcohol or opiate withdrawal symptoms. Valium works especially well in such cases.
Both drugs are almost insoluble in water, but diazepam has a better lipid solubility compared to lorazepam. Lorazepam has slow absorption after oral administration and is unsuitable for rectal administration. It is mainly distributed in blood.
On the other hand, diazepam, which is well absorbed orally and rectally, because of its high lipid solubility, does not remain too long in the vascular space and quickly redistributes all over the body, particularly to body fat. Diazepam should be better for convulsions treatment as it has much longer elimination half-life time compared to lorazepam.
But, lorazepam stays in the vascular space for a longer period of time, making the anticonvulsant effects more durable thus reducing the need for repeated doses. Diazepam anticonvulsant effects last for only 15-30 minutes, but Lorazepam effects last 12-24 hours. So, in the treatment of seizures in epileptic patients, when used intravenuously, Lorazepam is usually considered to be more preferable than Diazepam.
Diazepam effects develop after 6-10 months of therapy, making it a good option for long term maintenance therapy. Diazepam use in emergency cases due to eclampsia is very effective especially when the blood pressure failed to be controlled along with other measures.
The Diazepam advantage is less severe withdrawal symptoms when the medication is abruptly discontinued. Both drugs should be stopped by gradually decreasing the dose. In diazepam case, dose reductions have less response, because of the longer half-lives of Diazepam and its active metabolites.
Diazepam has better bioavailability after oral use than lorazepam with approximately 93-100 % compared to lorazepam’s 85%. Diazepam is metabolized in the liver by CYP2C19 and CYP3A4 enzymes, while lorazepam is metabolized via hepatic glucuronidation. Both drugs have renal excretion.
Which drug stay longer in the body, Ativan or Valium?
According some data the average half-life for Ativan is an approximate 12 hours. So, the most patients will eliminate 50% of the drug from their body after 12 hours of ingestion. According to this, it could take up to 2.75 days for the drug to have been fully eliminated from the body. Other data suggest that half-life for the drug may be slightly longer at 15.7 hours.
According to this it would take nearly 3.59 days to fully eliminate the drug from the system. But, it is important to know that lorazepam’s metabolite called lorazepam glucuronide has a longer half-life time of approximately 18 hours. To fully eliminate lorazepam glucuronide from the body it may take longer than the lorazepam itself.
Lorazepam glucuronide will remain in your system and can be detected in your urine for more than 4 days of post-ingestion. Factors that may have an influence on lorazepam elimination include: age, body weight, liver and kidney function, genetics, metabolic rate, urinary pH, dosage and frequency of use and other drugs used at the same time.
Valium elimination half-life is estimated within the range of 30 and 56 hours, for an average of 43 hours. This means that on average around 43 hours is needed to clear just 50% of the final dose after Valium oral administration. So, estimated time for fully clearance of diazepam is about 9.85 days. But, this is only the case for molecule of unmetabolized diazepam and its clearance from systemic circulation.
Diazepam’s metabolites may stay much longer in the body. The most prominent metabolite of diazepam is pharmacologically active nordiazepam or desmethyldiazepam which has a half-life within the range of 40 to 100 hours. Considering nordiazepam’s elimination half-life time on average of 70 hours it will likely take around 70 hours to eliminate %50 of the nordiazepam metabolite from your plasma.
According to these results, it can be estimated that full elimination of diazepam and nordiazepam may take up to 23 days. Many different factors may have an influence on diazepam elimination from the body such as: liver function, age, body fats, genetics, metabolic rate, formulation, dosage and frequency of use, co-administration of other drugs.
Ativan and Valium side effects
|Ativan possible side effects||Valium possible side effects|
|Suicidal ideation/attempt||Skin rash|
|Vertigo||Changes in salivation|
|Ataxia||Neutropenia (serious but rare)|
|Sleep apnea||Jaundice (serious but rare)|
|Asthenia||Local effects: Pain, swelling, thrombophlebitis, carpal tunnel syndrome, tissue necrosis|
|Extrapyramidal symptoms||Phlebitis (if too rapid injection push)|
|Change in libido|
|Increased liver transaminases|
|Increase in ALP|
|Change in appetite|
|Paradoxical reactions (anxiety, excitation, agitation, hostility, aggression, rage)|
What are withdrawal effects of Ativan and Valium?
Because Valium and Ativan have a high potential for dependence and addiction, they are not often prescribed for long-term treatments. Duration of treatment is most usually limited to 12 weeks and they are used only for the treatment of severe psychological symptoms. Patients who are on long-term treatment are at increased risk of experiencing withdrawal symptoms if one of these drugs is abruptly discontinued.
Reported side effects caused by Ativan and Valium withdrawal are:
- Increased sensitivity to stimulus (light or sound)
- Personality changes
- Numbness or tingling sensation
- Nausea and vomiting
- Irregular heartbeat and palpitations
- Memory loss
- Panic attacks
- Trouble sleeping
- Restlessness or irritability
The Valium advantage is however less severe withdrawal symptoms compared to Ativan, because of the longer elimination half-lives of diazepam and its active metabolites.
To avoid Valium or Ativan withdrawal effects, it is important for the patients to consult their healthcare provider before discontinuing this medication on their own.
For safe discontinuation, your healthcare provider will gradually reduce and taper your dose of Ativan or Valium by slowly reducing your dose. How long will taper last depends on the duration of time and doses that the patient has been taking. In most cases, the longer the duration of treatment is, the longer the taper is.
If withdrawal symptoms develop, the dosage of these drugs may have to be adjusted to its previous dose. Some doctors will prescribe medications to manage withdrawal symptoms, especially if they are severe enough. Long-acting antianxiety drugs may also be given to relieve symptoms.
If you notice unpleasant symptom while discontinuing Ativan or Valium, you should discuss it with your healthcare provider. It is important to know that Ativan and Valium may cause withdrawal symptoms even if you think you are taking them on the right way or as recommended by the doctor. If they are not properly treated withdrawal symptoms may lead to life-threatening complications.
Which one is expensive, Ativan or Valium?
According to drugs.com:
- The cost for Valium tablet 2 mg is around $350 for a supply of 100 tablets
- The cost for Valium tablet 5 mg is around $541 for a supply of 100 tablets
- The cost for Valium tablet 10 mg is around $907 for a supply of 100 tablets
- The cost for Xanax tablet 0.25 mg is around $323 for a supply of 100 tablets
- The cost for Xanax tablet 0. 5 mg is around $400 for a supply of 100 tablets
- The cost for Xanax tablet 1 mg is around $533 for a supply of 100 tablets
- The cost for Xanax tablet 2 mg is around $902 for a supply of 100 tablets
Prices depend on the pharmacy you visit. Prices are for cash paying customers only and are not valid with insurance plans.
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